GLP1R
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Also known as GLP-1R
Summary
GLP1R (glucagon like peptide 1 receptor, HGNC:4324) is a protein-coding gene on chromosome 6p21.2, encoding Glucagon-like peptide 1 receptor (P43220). G-protein coupled receptor for glucagon-like peptide 1 (GLP-1).
This gene encodes a 7-transmembrane receptor for glucagon-like peptide 1 (GLP-1), which stimulates glucose-dependent insulin secretion. The receptor, located on the cell surface, is internalized upon ligand binding and triggers signaling pathways that regulate insulin release, appetite, gastric emptying, and energy balance. It also has neuroprotective and cardiovascular effects. Polymorphisms in this gene are linked to type 2 diabetes risk, and the receptor is a key drug target for diabetes, obesity, and stroke therapies.
Source: NCBI Gene 2740 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 53 total
- Druggable target: yes — 18 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_002062
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:4324 |
| Approved symbol | GLP1R |
| Name | glucagon like peptide 1 receptor |
| Location | 6p21.2 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | GLP-1R |
| Ensembl gene | ENSG00000112164 |
| Ensembl biotype | protein_coding |
| OMIM | 138032 |
| Entrez | 2740 |
Gene structure
Transcript identifiers
Ensembl transcripts: 1 — 1 protein_coding
ENST00000373256
RefSeq mRNA: 1 — MANE Select: NM_002062
NM_002062
CCDS: CCDS4839
Canonical transcript exons
ENST00000373256 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000750428 | 39056397 | 39056493 |
| ENSE00000750429 | 39057472 | 39057579 |
| ENSE00000750430 | 39065711 | 39065829 |
| ENSE00000750431 | 39066197 | 39066303 |
| ENSE00000750432 | 39072862 | 39073015 |
| ENSE00000750433 | 39073610 | 39073769 |
| ENSE00000750434 | 39078322 | 39078382 |
| ENSE00000750435 | 39078957 | 39079026 |
| ENSE00000750436 | 39079112 | 39079200 |
| ENSE00000750438 | 39079564 | 39079702 |
| ENSE00000750439 | 39080698 | 39080739 |
| ENSE00001027349 | 39085906 | 39091303 |
| ENSE00001459910 | 39048781 | 39048918 |
Expression profiles
Bgee: expression breadth ubiquitous, 117 present calls, max score 87.55.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1315 / max 16.2234, expressed in 59 samples.
FANTOM5 promoters (1 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 67686 | 0.1315 | 59 |
Top tissues by expression
216 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| islet of Langerhans | UBERON:0000006 | 87.55 | gold quality |
| type B pancreatic cell | CL:0000169 | 85.96 | silver quality |
| pancreatic ductal cell | CL:0002079 | 85.36 | silver quality |
| sperm | CL:0000019 | 85.12 | silver quality |
| gluteal muscle | UBERON:0002000 | 85.06 | gold quality |
| male germ cell | CL:0000015 | 84.94 | silver quality |
| olfactory bulb | UBERON:0002264 | 84.84 | gold quality |
| triceps brachii | UBERON:0001509 | 84.51 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 83.26 | gold quality |
| buccal mucosa cell | CL:0002336 | 81.87 | gold quality |
| pancreas | UBERON:0001264 | 80.49 | gold quality |
| vena cava | UBERON:0004087 | 79.75 | silver quality |
| left ventricle myocardium | UBERON:0006566 | 78.78 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 78.24 | gold quality |
| body of pancreas | UBERON:0001150 | 78.13 | gold quality |
| oocyte | CL:0000023 | 77.77 | silver quality |
| inferior olivary complex | UBERON:0002127 | 77.30 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 76.74 | gold quality |
| diaphragm | UBERON:0001103 | 76.57 | gold quality |
| deltoid | UBERON:0001476 | 76.28 | gold quality |
| CA1 field of hippocampus | UBERON:0003881 | 76.06 | gold quality |
| periodontal ligament | UBERON:0008266 | 75.63 | silver quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 75.14 | gold quality |
| tibialis anterior | UBERON:0001385 | 75.05 | silver quality |
| cartilage tissue | UBERON:0002418 | 74.50 | silver quality |
| secondary oocyte | CL:0000655 | 74.19 | gold quality |
| superficial temporal artery | UBERON:0001614 | 73.84 | silver quality |
| epithelial cell of pancreas | CL:0000083 | 73.54 | gold quality |
| cardia of stomach | UBERON:0001162 | 73.40 | silver quality |
| medulla oblongata | UBERON:0001896 | 73.19 | silver quality |
Single-cell (SCXA)
Detected in 5 experiment(s), a significant marker in 5.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-5061 | yes | 18.96 |
| E-GEOD-81608 | yes | 18.11 |
| E-ENAD-27 | yes | 11.21 |
| E-GEOD-83139 | yes | 8.99 |
| E-ANND-3 | yes | 4.06 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): MAFA, NKX6-1, PDX1, SP1, SP3, ZGLP1
miRNA regulators (miRDB)
182 targeting GLP1R, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-5193 | 100.00 | 67.26 | 1744 |
| HSA-MIR-8485 | 100.00 | 77.57 | 4731 |
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-3120-5P | 100.00 | 65.56 | 965 |
| HSA-MIR-6740-5P | 100.00 | 65.64 | 932 |
| HSA-MIR-150-5P | 99.99 | 66.69 | 1976 |
| HSA-MIR-6870-5P | 99.99 | 68.55 | 2115 |
| HSA-MIR-513B-5P | 99.99 | 69.96 | 2150 |
| HSA-MIR-34A-5P | 99.99 | 71.21 | 1784 |
| HSA-MIR-449A | 99.99 | 71.05 | 1776 |
| HSA-MIR-27A-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-27B-3P | 99.98 | 72.13 | 2955 |
| HSA-MIR-9985 | 99.98 | 72.11 | 2939 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-512-3P | 99.97 | 67.35 | 1049 |
| HSA-MIR-4723-5P | 99.97 | 68.70 | 2034 |
| HSA-MIR-5698 | 99.97 | 68.49 | 2029 |
| HSA-MIR-7111-5P | 99.97 | 68.48 | 2062 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-1229-3P | 99.97 | 66.49 | 906 |
| HSA-MIR-34C-5P | 99.97 | 70.45 | 1577 |
| HSA-MIR-449B-5P | 99.97 | 70.26 | 1580 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-2110 | 99.96 | 66.68 | 1930 |
| HSA-MIR-6845-3P | 99.94 | 66.88 | 1439 |
Literature-anchored findings (GeneRIF, showing 40)
- In vitro folding, functional characterization, and disulfide pattern of the extracellular domain (PMID:12034449)
- Missenses mutations in Japaneses type 2 diabetes patients. (PMID:15364163)
- analysis of the glucagon-like peptide-1 receptor beta-arrestin 2 interaction (PMID:15528268)
- Experimental evidence indicates that the GLP-1 receptor gene is expressed in human brain as a protein, with binding properties similar to those of the GLP-1R located in peripheral tissues. (PMID:15686481)
- glucagon-like peptide-1 receptor polymorphism results in reduced agonist responsiveness (PMID:15975668)
- GLP-1R stimulation does not modify the growth or survival of human pancreatic cancer cells. (PMID:16644694)
- The interaction of the GLP-1R with caveolin-1 regulates subcellular localization, trafficking, and signaling activity. (PMID:16931572)
- results suggest that the differential affinity of nGLP-1R is explained almost entirely by divergent residues in the central part of the ligands: Leu10-Gly30 of Exendin-4 and Val16-Arg36 of GLP-1. (PMID:17444618)
- For GLP-1 receptor scintigraphy, a low-background signal can be expected, on the basis of the low receptor expression in the normal tissues surrounding tumors. (PMID:17475961)
- analysis of the crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain (PMID:18287102)
- Structural basis of endogenous agonist activation of family B G protein-coupled receptors. (PMID:18372345)
- Our data suggest that the GLP-1 receptor is restricted to the pancreatic beta cells. (PMID:18541709)
- Decreased TCF7L2 protein levels in type 2 diabetes mellitus correlate with downregulation of GLP-1R and GIP-R. (PMID:19386626)
- Data demonstrate that the GLP-1R agonist, exendin-4, significantly improves the efficiency of PDX-1-mediated transdifferentiation. (PMID:19755420)
- analysis of the molecular basis of natural agonist ligand binding to the GLP1 receptor (PMID:19815559)
- In vivo GLP-1R imaging is an innovative, noninvasive diagnostic approach that successfully localizes small insulinomas. (PMID:19820010)
- GFP-GLP-1 receptor is weakly expressed in the plasma membranes and is functionally coupled to adenylyl cyclase via heterotrimeric G-proteins, similarly as its wild type. (PMID:19859570)
- The crystal structure of the extracellular domain of GLP-1 receptor in complex with GLP-1 was solved to 2.1 A resolution. (PMID:19861722)
- GLP-1 receptor scintigraphy is a novel tool to facilitate the detection of insulinomas. (PMID:19890029)
- the putative signal peptide of GLP-1R was cleaved during synthesis and processing of the receptor; while cleavage was not essential for receptor synthesis, it was obligatory for effective processing and trafficking to the plasma membrane (PMID:20002095)
- GLP-1R is present on human hepatocytes. (PMID:20225248)
- In prolonged ventricular fibrillation followed by resuscitation, myocardial microcirculatory function was enhanced with administration of GLP-1. Treatment was not associated with significant improvement in post-resuscitation myocardial function. (PMID:20347207)
- The data of this study confirmed that GLP-1R agonists have clinical potential in treating neuronal stresses relevant to neurodegenerative conditions. (PMID:20374430)
- Exendin-4 stimulates proliferation of coronary artery endothelial cells via a GLP-1R dependent mechanism. (PMID:20452396)
- Our results identify associations between a novel genetic variant of GLP-1R and hypothalamus-pituitary-adrenal (HPA) axis regulation. (PMID:20483198)
- analysis of the amino-terminal region of glucagon-like peptide 1 and its receptor, a region critical for biological activity (PMID:20529866)
- The major determinant of exendin-4/glucagon-like peptide 1 differential affinity at the rat glucagon-like peptide 1 receptor N-terminal domain is a hydrogen bond from SER-32 of exendin-4. (PMID:20649595)
- Recombinant expression, in vitro refolding, and biophysical characterization of the human glucagon-like peptide-1 receptor (PMID:20690636)
- Variation in GLP1R may alter insulin secretion in response to exogenous GLP-1. (PMID:20805279)
- Low molecular weight pyrimidine-based compounds can activate the GLP-1 receptor and stimulate glucose-dependent insulin secretion. (PMID:20823098)
- In contrast to insulinoma, hyperinsulinaemic hypoglycaemia after gastric bypass surgery is not accompanied by overexpression of GLP-1 receptor in individual islets. (PMID:20835917)
- cAMP-mediated pathways are modelled by glucose, and downregulation of the calcium-sensitive ADCY8 plays a central role herein, including signalling via the GLP1R. (PMID:21046358)
- Targeting GLP-1R by (111)In-DOTA-exendin-4 or (111)In-DPTA-exendin-4 offers a new approach that permits the successful localization of small benign insulinomas. (PMID:21095545)
- A GLP-1 receptor agonist liraglutide inhibits endothelial cell dysfunction and vascular adhesion molecule expression in an ApoE-/- mouse model. (PMID:21562063)
- regulation of GLP-1R function is complex with endogenous peptides that interact with the receptor, including full-length and truncated forms of GLP-1 that can exist in an amidated form (GLP-1(1-36)NH and GLP-1(7-36)NH) and related peptide oxyntomodulin (PMID:21616920)
- greater proportion of patients with type 2 diabetes can achieve the HbA(1c) goal <7% with GLP-1 agonists compared to placebo or other antidiabetic drugs; in absolute terms, exenatide LAR was best for the attainment of the HbA(1c) goal. (PMID:21663496)
- GLP-1 signaling through GLP-1 receptor modulates cytokine production in natural killer T-cells; GLP-1 signaling appears to be important in psoriasis patients with type 2 diabetes mellitus (e.g., GLP-1 mimetic analogs may be used therapeutically). (PMID:21744074)
- Glucagon-like peptide-1 receptor activation stimulates hepatic lipid oxidation and restores hepatic signalling alteration induced by a high-fat diet in nonalcoholic steatohepatitis. (PMID:21745271)
- evidence for the presence of GLP-1R in adipose tissue and show that its mRNA and protein expressions are increased in visceral adipose depots from morbidly obese patients with a high degree of insulin resistance (PMID:21862620)
- Data show important roles in ligand binding and receptor activation of conserved residues within the transmembrane domain of the GLP-1R. (PMID:21868452)
Cross-species orthologs
2 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Glp1r | ENSMUSG00000024027 |
| rattus_norvegicus | Glp1r | ENSRNOG00000001152 |
Paralogs (42): CALCR (ENSG00000004948), GIPR (ENSG00000010310), ADGRA2 (ENSG00000020181), CALCRL (ENSG00000064989), GLP2R (ENSG00000065325), ADGRF5 (ENSG00000069122), ADGRL1 (ENSG00000072071), ADCYAP1R1 (ENSG00000078549), SCTR (ENSG00000080293), VIPR2 (ENSG00000106018), CRHR2 (ENSG00000106113), GHRHR (ENSG00000106128), ADGRD1 (ENSG00000111452), ADGRG6 (ENSG00000112414), VIPR1 (ENSG00000114812), ADGRL2 (ENSG00000117114), CRHR1 (ENSG00000120088), ADGRB2 (ENSG00000121753), ADGRE5 (ENSG00000123146), ADGRE2 (ENSG00000127507), ADGRE3 (ENSG00000131355), ADGRB3 (ENSG00000135298), PTH2R (ENSG00000144407), ADGRG7 (ENSG00000144820), ADGRL3 (ENSG00000150471), ADGRA3 (ENSG00000152990), ADGRF1 (ENSG00000153292), ADGRF4 (ENSG00000153294), ADGRG4 (ENSG00000156920), ADGRG5 (ENSG00000159618), PTH1R (ENSG00000160801), ADGRL4 (ENSG00000162618), EVA1C (ENSG00000166979), ADGRF3 (ENSG00000173567), ADGRG2 (ENSG00000173698), ADGRE1 (ENSG00000174837), ADGRD2 (ENSG00000180264), ADGRB1 (ENSG00000181790), ADGRG3 (ENSG00000182885), ADGRA1 (ENSG00000197177)
Protein
Protein identifiers
Glucagon-like peptide 1 receptor — P43220 (reviewed: P43220)
All UniProt accessions (1): P43220
UniProt curated annotations — full annotation on UniProt →
Function. G-protein coupled receptor for glucagon-like peptide 1 (GLP-1). Ligand binding triggers activation of a signaling cascade that leads to the activation of adenylyl cyclase and increased intracellular cAMP levels. Plays a role in regulating insulin secretion in response to GLP-1.
Subunit / interactions. May form homodimers and heterodimers with GIPR.
Subcellular location. Cell membrane.
Post-translational modifications. N-glycosylation enhances cell surface expression and lengthens receptor half-life by preventing degradation in the ER.
Activity regulation. The allosteric modulators NNC0640, PF-06372222 and MK-0893 inhibit the increase of intracellular cAMP levels in response to GLP-1.
Miscellaneous. Selective recognition of glucagon-like peptide over glucagon is determined by residues located at the C-terminal end of the glucagon-like peptide.
Similarity. Belongs to the G-protein coupled receptor 2 family.
RefSeq proteins (1): NP_002053* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000832 | GPCR_2_secretin-like | Family |
| IPR001879 | GPCR_2_extracellular_dom | Domain |
| IPR003290 | GPCR_2_GLP1/glucagon_rcpt | Family |
| IPR003292 | GPCR_2_GLP1_rcpt | Family |
| IPR017981 | GPCR_2-like_7TM | Domain |
| IPR017983 | GPCR_2_secretin-like_CS | Conserved_site |
| IPR036445 | GPCR_2_extracell_dom_sf | Homologous_superfamily |
| IPR047033 | GLP1R_7TM | Domain |
| IPR050332 | GPCR_2 | Family |
Pfam: PF00002, PF02793
UniProt features (94 total): helix 17, mutagenesis site 14, strand 11, sequence variant 9, topological domain 8, transmembrane region 7, sequence conflict 7, turn 7, disulfide bond 4, glycosylation site 3, site 2, modified residue 2, signal peptide 1, chain 1, region of interest 1
Structure
Experimental structures (PDB)
70 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 4ZGM | X-RAY DIFFRACTION | 1.8 |
| 5OTU | X-RAY DIFFRACTION | 1.8 |
| 5OTT | X-RAY DIFFRACTION | 1.92 |
| 5E94 | X-RAY DIFFRACTION | 2 |
| 5OTV | X-RAY DIFFRACTION | 2 |
| 5OTX | X-RAY DIFFRACTION | 2 |
| 3C5T | X-RAY DIFFRACTION | 2.1 |
| 3IOL | X-RAY DIFFRACTION | 2.1 |
| 5OTW | X-RAY DIFFRACTION | 2.1 |
| 6X18 | ELECTRON MICROSCOPY | 2.1 |
| 6X19 | ELECTRON MICROSCOPY | 2.1 |
| 7RTB | ELECTRON MICROSCOPY | 2.14 |
| 9MZE | ELECTRON MICROSCOPY | 2.2 |
| 9N05 | ELECTRON MICROSCOPY | 2.2 |
| 3C59 | X-RAY DIFFRACTION | 2.3 |
| 9BYO | ELECTRON MICROSCOPY | 2.31 |
| 7S1M | ELECTRON MICROSCOPY | 2.41 |
| 8JIS | ELECTRON MICROSCOPY | 2.46 |
| 6X1A | ELECTRON MICROSCOPY | 2.5 |
| 7DUQ | ELECTRON MICROSCOPY | 2.5 |
| 7EVM | ELECTRON MICROSCOPY | 2.5 |
| 7KI0 | ELECTRON MICROSCOPY | 2.5 |
| 7KI1 | ELECTRON MICROSCOPY | 2.5 |
| 9MXU | ELECTRON MICROSCOPY | 2.5 |
| 9MZF | ELECTRON MICROSCOPY | 2.5 |
| 7S3I | ELECTRON MICROSCOPY | 2.51 |
| 8WG7 | ELECTRON MICROSCOPY | 2.54 |
| 8JIR | ELECTRON MICROSCOPY | 2.57 |
| 7X8R | ELECTRON MICROSCOPY | 2.61 |
| 8YW3 | ELECTRON MICROSCOPY | 2.68 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P43220-F1 | 82.63 | 0.48 |
Antibody-complex structures (SAbDab): 40 — 5E94, 6B3J, 6LN2, 6VCB, 6X18, 6X19, 6X1A, 6XOX, 7C2E, 7DUQ, 7DUR, 7E14, 7EVM, 7FIM, 7KI0, 7KI1, 7LLL, 7LLY, 7RG9, 7RGP, 7RTB, 7S1M, 7S3I, 7VBH, 7VBI (+15 more)
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (2): 121 (interaction with the endogenous ligand glp-1); 128 (interaction with the endogenous ligand glp-1)
Post-translational modifications (2): 341, 348
Disulfide bonds (4): 46–71, 62–104, 85–126, 226–296
Glycosylation sites (3): 63, 82, 115
Mutagenesis-validated functional residues (14):
| Position | Phenotype |
|---|---|
| 32 | no effect on stimulation of camp accumulation and on glp-1 binding. |
| 69 | abolishes stimulation of camp accumulation in response to glp-1. |
| 88 | abolishes stimulation of camp accumulation in response to glp-1. |
| 89 | abolishes stimulation of camp accumulation in response to glp-1. |
| 90 | strongly decreased stimulation of camp accumulation in response to glp-1. |
| 121 | strongly decreased stimulation of camp accumulation in response to glp-1. |
| 127 | no effect on stimulation of camp accumulation in response to glp-1. |
| 128 | slightly decreases stimulation of camp accumulation in response to glp-1. |
| 128 | no effect on stimulation of camp accumulation in response to glp-1. |
| 176 | decreases sensitivity to glp-1. |
| 317 | causes the formation of an artifactual disulfide bond that abolishes signaling in response to glp-1 binding; when associ |
| 352 | abolishes inhibition by negative allosteric modulators. |
| 355 | abolishes inhibition by the negative allosteric modulators nnc0640 and pf-06372222, but does not abolish inhibition by m |
| 361 | causes the formation of an artifactual disulfide bond that abolishes signaling in response to glp-1 binding; when associ |
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-381676 | Glucagon-like Peptide-1 (GLP1) regulates insulin secretion |
| R-HSA-418555 | G alpha (s) signalling events |
| R-HSA-420092 | Glucagon-type ligand receptors |
MSigDB gene sets: 131 (showing top):
GOBP_RESPONSE_TO_NITROGEN_COMPOUND, REACTOME_GLUCAGON_TYPE_LIGAND_RECEPTORS, GOBP_COGNITION, GOBP_BEHAVIOR, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOBP_PROTEIN_TARGETING, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_ESTABLISHMENT_OF_PROTEIN_LOCALIZATION_TO_ENDOPLASMIC_RETICULUM, GOBP_POSITIVE_REGULATION_OF_LYASE_ACTIVITY, GOBP_HORMONE_TRANSPORT, GOBP_ESTABLISHMENT_OF_PROTEIN_LOCALIZATION_TO_ORGANELLE, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELL_CELL_SIGNALING
GO Biological Process (15): cell surface receptor signaling pathway (GO:0007166), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), activation of adenylate cyclase activity (GO:0007190), positive regulation of cytosolic calcium ion concentration (GO:0007204), learning or memory (GO:0007611), regulation of heart contraction (GO:0008016), post-translational protein targeting to membrane, translocation (GO:0031204), negative regulation of blood pressure (GO:0045776), positive regulation of blood pressure (GO:0045777), hormone secretion (GO:0046879), response to psychosocial stress (GO:1990911), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), regulation of biological quality (GO:0065008), cellular response to glucagon stimulus (GO:0071377)
GO Molecular Function (8): transmembrane signaling receptor activity (GO:0004888), glucagon receptor activity (GO:0004967), peptide hormone binding (GO:0017046), glucagon-like peptide 1 receptor activity (GO:0044508), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515), G protein-coupled peptide receptor activity (GO:0008528), signaling receptor activity (GO:0038023)
GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| Regulation of insulin secretion | 1 |
| GPCR downstream signalling | 1 |
| Class B/2 (Secretin family receptors) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| signal transduction | 2 |
| regulation of blood pressure | 2 |
| G protein-coupled receptor activity | 2 |
| G protein-coupled peptide receptor activity | 2 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase activator activity | 1 |
| positive regulation of adenylate cyclase activity | 1 |
| regulation of biological quality | 1 |
| behavior | 1 |
| cognition | 1 |
| heart contraction | 1 |
| regulation of blood circulation | 1 |
| post-translational protein targeting to endoplasmic reticulum membrane | 1 |
| intracellular protein transmembrane transport | 1 |
| hormone transport | 1 |
| signal release | 1 |
| multicellular organismal response to stress | 1 |
| cell communication | 1 |
| cellular process | 1 |
| signaling | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| biological regulation | 1 |
| response to glucagon | 1 |
| cellular response to peptide hormone stimulus | 1 |
| signaling receptor activity | 1 |
| cellular response to glucagon stimulus | 1 |
| hormone binding | 1 |
| transmembrane signaling receptor activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| binding | 1 |
| peptide receptor activity | 1 |
| molecular transducer activity | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1862 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| GLP1R | GCG | P01275 | 999 |
| GLP1R | GIP | P09681 | 996 |
| GLP1R | DPP4 | P27487 | 965 |
| GLP1R | SLC5A2 | P31639 | 908 |
| GLP1R | INS | P01308 | 897 |
| GLP1R | VIP | P01282 | 882 |
| GLP1R | GNAQ | P50148 | 878 |
| GLP1R | SCT | P09683 | 861 |
| GLP1R | PYY | P10082 | 828 |
| GLP1R | GHRL | Q9UBU3 | 826 |
| GLP1R | IAPP | P10997 | 796 |
| GLP1R | SI | P14410 | 790 |
| GLP1R | MGAM | O43451 | 785 |
| GLP1R | ALB | P02768 | 754 |
| GLP1R | TCF7L2 | Q9NQB0 | 752 |
IntAct
141 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 | |
| KRTAP10-7 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | KRTAP10-8 | psi-mi:“MI:0915”(physical association) | 0.560 |
| KRTAP10-9 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | NOTCH2NLA | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | KRTAP10-9 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 | |
| KRTAP1-3 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| NOTCH2NLC | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| KRTAP5-9 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| CYSRT1 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | KRTAP1-1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | KRTAP17-1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| GLP1R | ACSF3 | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | AP2M1 | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | APLP1 | psi-mi:“MI:0915”(physical association) | 0.540 |
| ELOVL1 | GLP1R | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | GPR37 | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | HPN | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | MRPL22 | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | PAQR6 | psi-mi:“MI:0915”(physical association) | 0.540 |
| GLP1R | SLC15A4 | psi-mi:“MI:0915”(physical association) | 0.540 |
BioGRID (311): KRTAP10-7 (Two-hybrid), KRTAP10-9 (Two-hybrid), KRTAP10-8 (Two-hybrid), KRTAP10-3 (Two-hybrid), NOTCH2NL (Two-hybrid), TMBIM6 (PCA), CLIP4 (PCA), CELA3B (PCA), CLDN7 (PCA), CCDC167 (PCA), CLPS (PCA), DAD1 (PCA), GNAS (PCA), IFITM3 (PCA), SCGB2A1 (PCA)
ESM2 similar proteins: A0A2Z2U4G9, O35659, O46502, O95838, P23811, P25107, P25117, P25961, P30082, P30083, P30988, P32082, P32214, P32215, P32241, P32301, P34999, P35000, P41587, P41588, P41593, P43218, P43219, P43220, P47871, P47872, P48546, P49190, P50133, P51839, P70555, P79222, P97751, Q02643, Q02644, Q03431, Q0P543, Q1LZF7, Q28992, Q29627
Diamond homologs: A0A2Z2U4G9, A6QP74, O35659, O42602, O42603, O46502, O62772, O95838, P23811, P25107, P25117, P25961, P30082, P30083, P32082, P32215, P32241, P32301, P34998, P34999, P35000, P35347, P35353, P41586, P41587, P41588, P41593, P43218, P43219, P43220, P47866, P47871, P47872, P48546, P48960, P49190, P50133, P70205, P70555, P97751
SIGNOR signaling
4 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| MAFA | “up-regulates quantity by expression” | GLP1R | “transcriptional regulation” |
| GCG | “up-regulates activity” | GLP1R | binding |
| GLP1R | “up-regulates activity” | GNAS | binding |
| GCG | up-regulates | GLP1R | binding |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 56 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Keratinization | 7 | 10.0× | 9e-04 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| receptor internalization | 5 | 34.5× | 1e-04 |
| intracellular protein transport | 6 | 8.3× | 6e-03 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
53 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 35 |
| Likely benign | 4 |
| Benign | 8 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2108 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 6:39056395:AG:A | acceptor_gain | 1.0000 |
| 6:39056396:GG:G | acceptor_gain | 1.0000 |
| 6:39057471:GACTT:G | acceptor_gain | 1.0000 |
| 6:39066299:TTCAG:T | donor_loss | 1.0000 |
| 6:39066300:TCAG:T | donor_loss | 1.0000 |
| 6:39066301:CAGG:C | donor_loss | 1.0000 |
| 6:39066302:AGGT:A | donor_loss | 1.0000 |
| 6:39066303:GG:G | donor_loss | 1.0000 |
| 6:39066304:G:GA | donor_loss | 1.0000 |
| 6:39066305:T:A | donor_loss | 1.0000 |
| 6:39073747:GCTC:G | donor_gain | 1.0000 |
| 6:39078380:GGG:G | donor_gain | 1.0000 |
| 6:39078381:GGG:G | donor_gain | 1.0000 |
| 6:39079024:GGG:G | donor_gain | 1.0000 |
| 6:39079024:GGGGT:G | donor_loss | 1.0000 |
| 6:39079025:GG:G | donor_gain | 1.0000 |
| 6:39079025:GGG:G | donor_gain | 1.0000 |
| 6:39079025:GGGTG:G | donor_loss | 1.0000 |
| 6:39079026:GG:G | donor_gain | 1.0000 |
| 6:39079026:GGTG:G | donor_loss | 1.0000 |
| 6:39079027:G:GG | donor_gain | 1.0000 |
| 6:39079027:GT:G | donor_loss | 1.0000 |
| 6:39079028:T:A | donor_loss | 1.0000 |
| 6:39079559:CTCA:C | acceptor_loss | 1.0000 |
| 6:39079560:TCA:T | acceptor_loss | 1.0000 |
| 6:39079561:CA:C | acceptor_loss | 1.0000 |
| 6:39079562:A:AG | acceptor_gain | 1.0000 |
| 6:39079563:G:GG | acceptor_gain | 1.0000 |
| 6:39079563:G:GT | acceptor_loss | 1.0000 |
| 6:39079563:GA:G | acceptor_gain | 1.0000 |
AlphaMissense
3019 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 6:39057512:G:C | W72C | 1.000 |
| 6:39057512:G:T | W72C | 1.000 |
| 6:39057480:T:A | C62S | 0.999 |
| 6:39057481:G:C | C62S | 0.999 |
| 6:39065737:T:A | C104S | 0.999 |
| 6:39065738:G:C | C104S | 0.999 |
| 6:39065757:G:C | W110C | 0.999 |
| 6:39065757:G:T | W110C | 0.999 |
| 6:39078963:G:C | W297C | 0.999 |
| 6:39078963:G:T | W297C | 0.999 |
| 6:39057481:G:A | C62Y | 0.998 |
| 6:39065738:G:A | C104Y | 0.998 |
| 6:39065739:C:G | C104W | 0.998 |
| 6:39072900:T:C | L183P | 0.998 |
| 6:39057482:C:G | C62W | 0.997 |
| 6:39057510:T:A | W72R | 0.997 |
| 6:39057510:T:C | W72R | 0.997 |
| 6:39057549:T:A | C85S | 0.997 |
| 6:39057550:G:C | C85S | 0.997 |
| 6:39066246:G:A | G151D | 0.997 |
| 6:39073766:T:A | W274R | 0.997 |
| 6:39073766:T:C | W274R | 0.997 |
| 6:39078958:T:A | C296S | 0.997 |
| 6:39078959:G:C | C296S | 0.997 |
| 6:39080698:G:A | G395R | 0.997 |
| 6:39080698:G:C | G395R | 0.997 |
| 6:39056443:A:G | Y42C | 0.996 |
| 6:39057481:G:T | C62F | 0.996 |
| 6:39057492:T:C | F66L | 0.996 |
| 6:39057494:C:A | F66L | 0.996 |
dbSNP variants (sampled 300 via entrez): RS1000144199 (6:39088253 C>A,T), RS1000181238 (6:39072557 C>T), RS1000184256 (6:39049340 C>G,T), RS1000260493 (6:39087506 G>A), RS1000262617 (6:39050521 G>C), RS1000269784 (6:39061347 G>A), RS1000352728 (6:39082773 G>A), RS1000398216 (6:39075863 G>A), RS1000411593 (6:39081899 G>A), RS1000616004 (6:39065343 A>C), RS1000617370 (6:39076075 C>A,T), RS1000657531 (6:39049601 C>T), RS1000670119 (6:39065565 G>C,T), RS1000698124 (6:39050770 A>C,G), RS1000821140 (6:39081846 T>C)
Disease associations
OMIM: gene MIM:138032 | disease phenotypes: MIM:125853
GenCC curated gene-disease
Mondo (1): type 2 diabetes mellitus (MONDO:0005148)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST006002_20 | Blood sugar levels | 7.000000e-10 |
| GCST007858_10 | Fasting blood glucose adjusted for BMI | 5.000000e-07 |
| GCST007899_21 | Fasting blood glucose | 3.000000e-12 |
| GCST010118_136 | Type 2 diabetes | 2.000000e-22 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004468 | glucose measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D003924 | Diabetes Mellitus, Type 2 | C18.452.394.750.149; C19.246.300 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL1784 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
18 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 117,986 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).
| Molecule | Name | Phase | Patents |
|---|---|---|---|
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4 | 2,704 |
| CHEMBL1707 | LOPERAMIDE HYDROCHLORIDE | 4 | 59,532 |
| CHEMBL2108724 | SEMAGLUTIDE | 4 | |
| CHEMBL344159 | TOLVAPTAN | 4 | 3,645 |
| CHEMBL4084119 | LIRAGLUTIDE | 4 | 10,473 |
| CHEMBL414357 | EXENATIDE | 4 | 17,302 |
| CHEMBL4297839 | TIRZEPATIDE | 4 | |
| CHEMBL502182 | ELAGOLIX SODIUM | 4 | 214 |
| CHEMBL5314341 | GLUCAGON | 4 | |
| CHEMBL567 | PERPHENAZINE | 4 | 21,883 |
| CHEMBL6067494 | SECRETIN | 4 | |
| CHEMBL4446782 | ORFORGLIPRON | 3 | 59 |
| CHEMBL1240772 | GLP-1 | 2 | 308 |
| CHEMBL2381848 | PF-06291874 | 2 | 26 |
| CHEMBL4297630 | COTADUTIDE | 2 | 587 |
| CHEMBL4518483 | DANUGLIPRON | 2 | 512 |
| CHEMBL5314631 | LOTIGLIPRON | 2 | 133 |
| CHEMBL9506 | DEVAZEPIDE | 2 | 608 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
7 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs10305420 | Efficacy | 4 | liraglutide | |
| rs2268639 | Toxicity | 3 | clozapine | Schizophrenia;Weight gain |
| rs2268639 | Toxicity | 3 | olanzapine | Schizophrenia;Weight gain |
| rs3765467 | Efficacy | 3 | exenatide | Diabetes Mellitus;Type 2 |
| rs3765467 | Efficacy | 3 | sitagliptin | Diabetes Mellitus;Type 2 |
| rs6923761 | Efficacy | 3 | sitagliptin;vildagliptin | Diabetes Mellitus;Type 2 |
| rs6923761 | Efficacy | 3 | liraglutide |
PharmGKB variants
6 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs2268639 | GLP1R | 3 | 0.00 | 2 | olanzapine;clozapine |
| rs6923761 | GLP1R | 3 | 4.00 | 2 | sitagliptin;vildagliptin;liraglutide |
| rs10305420 | GLP1R | 4 | -1.00 | 1 | liraglutide |
| rs3765467 | GLP1R | 3 | 2.62 | 2 | exenatide;sitagliptin |
| rs761386 | GLP1R | 0.00 | 0 | ||
| rs2254336 | GLP1R | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — Glucagon receptor family
Most potent curated ligand interactions (33 total), top 25:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| semaglutide | Agonist | 11.21 | pEC50 |
| Peptide 5 [PMID: 28562585] | Agonist | 10.8 | pEC50 |
| ecnoglutide | Agonist | 10.74 | pEC50 |
| liraglutide | Full agonist | 10.52 | pEC50 |
| conveglipron | Full agonist | 10.52 | pEC50 |
| taspoglutide | Agonist | 10.22 | pEC50 |
| BETP | Positive | 9.9 | pEC50 |
| dapiglutide | Agonist | 9.72 | pEC50 |
| survodutide | Agonist | 9.48 | pEC50 |
| [125I]GLP-1-(7-36)-amide | Full agonist | 9.3 | pKd |
| glucagon-like peptide 1-(7-36) amide | Full agonist | 9.2 | pKi |
| exendin-4 | Agonist | 9.18 | pIC50 |
| lotiglipron | Agonist | 9.02 | pEC50 |
| naperiglipron | Agonist | 8.94 | pEC50 |
| DA-302168S | Full agonist | 8.88 | pEC50 |
| lixisenatide | Agonist | 8.88 | pKi |
| elecoglipron | Agonist | 8.62 | pIC50 |
| orforglipron | Partial agonist | 8.49 | pKi |
| tirzepatide | Agonist | 8.37 | pKi |
| [125I]exendin-(9-39) | Antagonist | 8.3 | pKd |
| glutazumab | Binding | 8.29 | pKd |
| retatrutide | Full agonist | 8.14 | pKi |
| exendin-(9-39) | Antagonist | 8.1 | pKi |
| LSN3318839 | Positive | 7.85 | pEC50 |
| albiglutide | Agonist | 7.7 | pEC50 |
Binding affinities (BindingDB)
744 measured of 773 human assays (773 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 3-[(1S,2S)-1-[2-[(4S)-3-[3-(1-cyclopropyl-4-fluoroindazol-5-yl)-2-oxoimidazol-1-yl]-2-(7-fluoro-2,3-dihydro-1H-inden-4-yl)-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]-5-(oxan-4-yl)indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one | EC50 | 0.015 nM | US-20250257062: GLP-1R Agonist and Therapeutic Method Thereof |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-3- fluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.015 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 3-[(1S,2S)-1-[2-[(4S)-3-[3-(1-cyclopropyl-4-fluoroindazol-5-yl)-2-oxoimidazol-1-yl]-2-(3-cyclopropyl-4-fluorophenyl)-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]-5-(oxan-4-yl)indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one | EC50 | 0.02 nM | US-20250257062: GLP-1R Agonist and Therapeutic Method Thereof |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,6- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.024 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | EC50 | 0.028 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 3-[(1S,2S)-1-[2-[(4S)-2-(3-cyclopropyl-4-fluorophenyl)-3-[3-[4-(dimethylphosphorylmethyl)phenyl]-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]-5-(oxan-4-yl)indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one | EC50 | 0.028 nM | US-20250257062: GLP-1R Agonist and Therapeutic Method Thereof |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,5- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.033 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,5- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.034 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[2-[3-(1H-imidazol-4-yl)propanoylamino]acetyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.039 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| BCN-PEG4- carbamate-P9 | EC50 | 0.044 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.047 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.05 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,6- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.07 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-(4-(2-(5- chloropyridin-2- yl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,5- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.076 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| BCN-PEG4- triazole-P8 | EC50 | 0.078 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)- 2,3,6- trifluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.089 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-(hydroxyamino)-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.115 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-1-[[(2S)-1-anilino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-3-[4-[4-[4-[[(2R)-2-[[2-[[2-[[2-[[2-[[4-(2-azatricyclo[10.4.0.04,9]hexadeca-1(16),4,6,8,12,14-hexaen-10-yn-2-yl)-4-oxobutanoyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]butoxy]-2-ethylphenyl]phenyl]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.117 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-1-[[(2S)-1-amino-5-[4-(4-aminobutoxy)phenyl]-1-oxopentan-2-yl]amino]-3-[4-(2-ethyl-4-methoxyphenyl)phenyl]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.136 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2- cyano-6- fluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.14 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[(3-amino-2,2-dimethyl-3-oxopropanoyl)amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.156 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-2-methylpropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.156 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)-2,6-difluorobenzyl)-7-fluoro-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid (Example 2) | EC50 | 0.17 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-(4-(2-(5- chloropyridin-2- yl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,5- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.19 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-anilino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.198 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2-(4-cyano- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)- 2,3,6- trifluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.23 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-yl}-2-methylpiperazin-1-yl]methyl}-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.28 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-yl}-2-methylpiperazin-1-yl]methyl}-3-[(2S)-oxetan-2-ylmethyl]-3H-imidazo[4,5-b]pyridine-5-carboxylic acid | EC50 | 0.3 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperazin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.3 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-{[(2S)-4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}-2-methylpiperazin-1-yl]methyl}-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.3 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-(4-(2-(4-cyano- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,5- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.3 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-(4-(2-(5- chloropyridin-2- yl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,6- difluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.31 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| DIBAC-suc- (glucose) SG4-P9 | EC50 | 0.314 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| NH2-PEG8- triazole-P8 | EC50 | 0.318 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-(4-(2-(4-cyano- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)- 2,3,6- trifluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.32 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| 2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-yl}piperazin-1-yl)methyl]-1-[(1-methyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.33 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperazin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.34 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.34 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.37 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.37 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| DIBAC-suc- SG4-P9 | EC50 | 0.378 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.39 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2,6- difluorobenzyl)-1- ((1- (cyanomethyl)cyclo- propyl)methyl)- 4-fluoro-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.41 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| DIBAC-suc- PEG4-triazole-P8 | EC50 | 0.412 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| (3S)-4-[[(2S)-3-[4-[4-(4-aminobutoxy)-2-ethylphenyl]phenyl]-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-(2-fluorophenyl)-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.427 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| DIBAC-suc- G4S-P9 | EC50 | 0.436 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| BCN-NHC2H4CO- (glucose) SG4-P9 | EC50 | 0.458 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
| 2-[(4-{6-[(2,4-difluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(1-ethyl-1H-imidazol-5-yl)methyl]-1H-benzimidazole-6-carboxylic acid | EC50 | 0.47 nM | US-10208019: GLP-1 receptor agonists and uses thereof |
| 2-(4-(2-(4-chloro- 2-fluorophenyl)-2- methylbenzo[d][1, 3]dioxol-4-yl)-2- fluorobenzyl)-1- (((S)-oxetan-2- yl)methyl)-1H- benzo[d]imidazole- 6-carboxylic acid | EC50 | 0.49 nM | US-20250099431: GLP-1R MODULATING COMPOUNDS |
| (3S)-4-[[(2S)-1-[[(2S)-1-amino-5-(3,5-dimethylphenyl)-1-oxopentan-2-yl]amino]-3-[4-[4-(4-azidobutoxy)-2-ethylphenyl]phenyl]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-(2-fluorophenyl)-2-[[(2S,3R)-3-hydroxy-2-[[2-[[(2S)-2-[[3-[2-(1H-imidazol-5-yl)ethylamino]-2,2-dimethyl-3-oxopropanoyl]amino]-3-(2H-tetrazol-5-yl)propanoyl]amino]acetyl]amino]butanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | EC50 | 0.497 nM | US-20250161476: ANTIBODY-DRUG CONJUGATES COMPRISING GLP1 PEPTIDOMIMETICS AND USES THEREOF |
ChEMBL bioactivities
2288 potent at pChembl≥5 of 2312 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 11.00 | EC50 | 0.01 | nM | CHEMBL4070096 |
| 11.00 | EC50 | 0.0101 | nM | CHEMBL4867885 |
| 11.00 | EC50 | 0.01 | nM | CHEMBL524907 |
| 10.97 | EC50 | 0.0107 | nM | CHEMBL3616760 |
| 10.96 | EC50 | 0.011 | nM | CHEMBL4065403 |
| 10.96 | EC50 | 0.011 | nM | CHEMBL5573719 |
| 10.96 | EC50 | 0.011 | nM | CHEMBL1222096 |
| 10.95 | EC50 | 0.0111 | nM | CHEMBL3616740 |
| 10.94 | EC50 | 0.0115 | nM | CHEMBL3616762 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL526516 |
| 10.92 | EC50 | 0.01202 | nM | CHEMBL526516 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL5416222 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL5575146 |
| 10.92 | EC50 | 0.01201 | nM | CHEMBL6171144 |
| 10.92 | EC50 | 0.012 | nM | CHEMBL6162106 |
| 10.89 | EC50 | 0.013 | nM | CHEMBL4084829 |
| 10.89 | EC50 | 0.013 | nM | CHEMBL5203806 |
| 10.89 | EC50 | 0.013 | nM | CHEMBL1222174 |
| 10.88 | EC50 | 0.0132 | nM | CHEMBL3616771 |
| 10.85 | EC50 | 0.0142 | nM | CHEMBL4875374 |
| 10.85 | EC50 | 0.014 | nM | CHEMBL526685 |
| 10.85 | EC50 | 0.014 | nM | CHEMBL1222102 |
| 10.84 | EC50 | 0.0143 | nM | CHEMBL4228978 |
| 10.84 | EC50 | 0.0145 | nM | CHEMBL6152883 |
| 10.83 | EC50 | 0.0147 | nM | CHEMBL3616741 |
| 10.83 | EC50 | 0.0147 | nM | CHEMBL4755815 |
| 10.82 | EC50 | 0.0153 | nM | CHEMBL4090347 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL4226514 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL5399932 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL6168874 |
| 10.82 | EC50 | 0.015 | nM | CHEMBL1222086 |
| 10.80 | EC50 | 0.0157 | nM | CHEMBL3616746 |
| 10.80 | EC50 | 0.016 | nM | EXENATIDE |
| 10.80 | EC50 | 0.016 | nM | CHEMBL5573706 |
| 10.80 | EC50 | 0.016 | nM | CHEMBL6167455 |
| 10.80 | EC50 | 0.016 | nM | CHEMBL6142223 |
| 10.79 | EC50 | 0.0162 | nM | CHEMBL428139 |
| 10.79 | EC50 | 0.01608 | nM | CHEMBL6143044 |
| 10.77 | EC50 | 0.0171 | nM | CHEMBL3616712 |
| 10.77 | EC50 | 0.0169 | nM | CHEMBL4549928 |
| 10.77 | EC50 | 0.017 | nM | CHEMBL5415681 |
| 10.76 | EC50 | 0.0174 | nM | CHEMBL4065846 |
| 10.76 | EC50 | 0.0172 | nM | CHEMBL4069307 |
| 10.74 | EC50 | 0.0181 | nM | CHEMBL3110317 |
| 10.74 | EC50 | 0.0182 | nM | CHEMBL4466667 |
| 10.74 | EC50 | 0.0183 | nM | CHEMBL4098061 |
| 10.74 | EC50 | 0.018 | nM | CHEMBL5567643 |
| 10.74 | EC50 | 0.018 | nM | CHEMBL5574936 |
| 10.74 | EC50 | 0.018 | nM | CHEMBL5579680 |
| 10.73 | EC50 | 0.0187 | nM | SEMAGLUTIDE |
PubChem BioAssay actives
1408 with measured affinity, of 2334 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxy-3-iodophenyl)-1-oxopropan-2-yl]amino]-3-[4-(2-ethyl-4-methoxyphenyl)phenyl]-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(2-fluorophenyl)-2-methyl-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid | 1206322: Agonist activity at human GLP-1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2R)-5-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-(octadecanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2S)-5-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-(icosanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2S)-5-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-(hexadecanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]hexanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2R)-5-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-(hexadecanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[2-[2-[2-[[2-[2-[2-(hexadecanoylamino)ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl]amino]hexanoyl]amino]-5-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2S)-5-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-(hexadecanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2R)-5-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-(hexadecanoylamino)-5-oxopentanoic acid | 1247343: Displacement of [125I]-GLP1 from human GLP1 receptor expressed in BHK cells after 2 hrs in absence of human serum albumin | ic50 | <0.0001 | uM |
| (2S)-5-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-(octadecanoylamino)-5-oxopentanoic acid | 1247343: Displacement of [125I]-GLP1 from human GLP1 receptor expressed in BHK cells after 2 hrs in absence of human serum albumin | ic50 | <0.0001 | uM |
| (2S)-5-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-(icosanoylamino)-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 12-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-12-oxododecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 14-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-14-oxotetradecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 16-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-16-oxohexadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (2R)-5-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-[(18-amino-18-oxooctadecanoyl)amino]-5-oxopentanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1R)-4-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1R)-4-[2-[2-[2-[2-[2-[2-[2-[2-[3-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-3-oxopropoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[4-[[(1S)-4-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 20-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-20-oxoicosanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 22-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-22-oxodocosanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-6-(carboxymethylamino)-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-2-methylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carboxypentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-6-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-6-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carboxypentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[[(1S)-4-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carboxypentyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-1-carboxy-4-oxobutyl]amino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| 18-[2-[2-[2-[2-[2-[2-[[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]acetyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[2-[[(2S)-5-carbamimidamido-1-(carboxymethylamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-oxohexyl]amino]-2-oxoethoxy]ethoxy]ethylamino]-2-oxoethoxy]ethoxy]ethylamino]-18-oxooctadecanoic acid | 1247346: Agonist activity at human GLP1 receptor expressed in BHK cells after 3 hrs by CRE firefly luciferase reporter gene assay in absence of human serum albumin | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[3-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoylamino]-5-oxopentanoic acid | 1281870: Activation of human GLP1R expressed in HEK293 cells preincubated for 30 mins followed by addition of cAMP-d2 conjugate/cryptate conjugate incubated for 60 mins by fluorescence analysis | ec50 | <0.0001 | uM |
| 2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]-2-pyridinyl]piperidin-1-yl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid | 1991163: Agonist activity at N-terminal HA-tagged human GLP-1R expressed in HEK293 cells assessed as effect on intracellular cAMP accumulation incubated for 30 mins by LANCA ultra cAMP assay | ec50 | <0.0001 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,5S,8S,11S,19S)-11-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamoyl]-2-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-3,6,9,13,20-pentaoxo-8-propan-2-yl-1,4,7,10,14-pentazacycloicos-19-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S,5S,8S,11S,19S)-19-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-2,5-bis(hydroxymethyl)-8-[(4-hydroxyphenyl)methyl]-3,6,9,13,20-pentaoxo-1,4,7,10,14-pentazacycloicosane-11-carbonyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-6-[[(4S)-5-amino-4-(hexadecanoylamino)-5-oxopentanoyl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,5S,8S,11S,19S)-11-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamoyl]-2-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-3,6,9,13,20-pentaoxo-8-propan-2-yl-1,4,7,10,14-pentazacycloicos-19-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,5S,8S,11S,19S)-11-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamoyl]-2-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-3,6,9,13,20-pentaoxo-8-propan-2-yl-1,4,7,10,14-pentazacycloicos-19-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,5S,8S,11S,19S)-11-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamoyl]-2-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-3,6,9,13,20-pentaoxo-8-propan-2-yl-1,4,7,10,14-pentazacycloicos-19-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S,5S,8S,11S,19S)-19-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-2,5-bis(hydroxymethyl)-8-[(4-hydroxyphenyl)methyl]-3,6,9,13,20-pentaoxo-1,4,7,10,14-pentazacycloicosane-11-carbonyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (2S)-5-[[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-6-oxohexyl]amino]-2-(hexadecanoylamino)-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-4-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 1483054: Agonist activity at human GLP-1 receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay | ec50 | <0.0001 | uM |
| (4S)-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,5S,8S,11S,19S)-11-[[2-[[(2S)-1-[(2-amino-2-oxoethyl)amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-2-oxoethyl]carbamoyl]-2-(1H-indol-3-ylmethyl)-5-(2-methylpropyl)-3,6,9,13,20-pentaoxo-8-propan-2-yl-1,4,7,10,14-pentazacycloicos-19-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 1427872: Agonist activity at human GLP1R expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE assay | ec50 | <0.0001 | uM |
CTD chemical–gene interactions
15 total (human), top 15 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Liraglutide | affects binding, increases activity | 2 |
| Benzo(a)pyrene | decreases expression, increases methylation | 2 |
| bisphenol A | decreases methylation | 1 |
| ethyl-p-hydroxybenzoate | decreases expression | 1 |
| morroniside | affects response to substance | 1 |
| Exenatide | affects binding, increases activity | 1 |
| Cyclic AMP | increases chemical synthesis, increases reaction, affects localization, affects binding, increases activity | 1 |
| Amino Acids, Peptides, and Proteins | decreases expression | 1 |
| Atrazine | increases expression | 1 |
| Cadmium | decreases expression, increases abundance | 1 |
| Methotrexate | decreases expression | 1 |
| Phthalic Acids | decreases expression | 1 |
| Tretinoin | decreases expression | 1 |
| Triclosan | decreases expression | 1 |
| Cadmium Chloride | decreases expression, increases abundance | 1 |
ChEMBL screening assays
314 unique, capped per target: 230 functional, 84 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1048996 | Functional | Agonist activity at human GLP1R expressed in CHO cells assessed as stimulation of intracellular [3H]cAMP accumulation after 30 mins by scintillation proximity assay | Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity. — J Med Chem |
| CHEMBL1048998 | Binding | Displacement of [125I]GLP1 from human GLP1R expressed in CHO cells | Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity. — J Med Chem |
Cellosaurus cell lines
17 cell lines: 6 spontaneously immortalized cell line, 4 transformed cell line, 4 cancer cell line, 2 induced pluripotent stem cell, 1 undefined cell line type
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_A1WG | KAUSTi011-A | Induced pluripotent stem cell | Male |
| CVCL_A1WH | KAUSTi011-B | Induced pluripotent stem cell | Male |
| CVCL_C0SQ | ACTOne GLP1R | Transformed cell line | Female |
| CVCL_E1CW | Ubigene THP-1 GLP1R KO | Cancer cell line | Male |
| CVCL_E4IV | Genomeditech HEK-293 H_GLP1R Reporter subclone DDX35 | Transformed cell line | Female |
| CVCL_E4IY | Genomeditech HEK-293 H_GLP1R Reporter | Transformed cell line | Female |
| CVCL_E6QK | Genomeditech CHO-K1 H_GLP1R Reporter | Spontaneously immortalized cell line | Female |
| CVCL_H438 | CHO-K1/GLP1/Galpha15 | Spontaneously immortalized cell line | Female |
| CVCL_KA20 | HEK293/CRE-Luc/GLP1R | Transformed cell line | Female |
| CVCL_KR98 | GeneBLAzer GLP1R-CRE-bla CHO-K1 | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
300 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT00006163 | PHASE4 | COMPLETED | Computer-assisted Diabetes Self-management Interventions |
| NCT00036504 | PHASE4 | COMPLETED | Efficacy and Safety of Twice-Daily Insulin Lispro Low Mixture Compared to a Once-Daily Long Acting Insulin Comparator in Patients Who Have Been Using One or More Oral Antihyperglycemic Agents Without Insulin |
| NCT00044460 | PHASE4 | COMPLETED | Efficacy and Safety In Poorly Controlled Type 2 Diabetics |
| NCT00095446 | PHASE4 | COMPLETED | NovoLog Observation Trial in Subjects With Type 1 and Type 2 Diabetes |
| NCT00101751 | PHASE4 | COMPLETED | INITIATE Plus (INITiation of Insulin to Reach A1c TargEt) Study |
| NCT00110370 | PHASE4 | COMPLETED | Comparing Pre-Mixed Insulin With Insulin Glargine Combined With Rapid-Acting Insulin in Patients With Type 2 Diabetes |
| NCT00110448 | PHASE4 | COMPLETED | Japanese Primary Prevention of Atherosclerosis With Aspirin for Diabetes (JPAD) Trial |
| NCT00118950 | PHASE4 | COMPLETED | Effect of Metformin Versus Repaglinide Treatment in Non-Obese Type 2 Diabetic Patients Uncontrolled by Diet |
| NCT00118963 | PHASE4 | COMPLETED | Effect of Repaglinide Versus Metformin Treatment in Non-Obese Patients With Type-2-Diabetes |
| NCT00121966 | PHASE4 | COMPLETED | South Danish Diabetes Study: Evaluation of the Antidiabetic Treatment of Type 2 Diabetes Mellitus |
| NCT00123604 | PHASE4 | COMPLETED | Vascular Effects of Carvedilol Versus Metoprolol in Hypertensive Patients With Type 2 Diabetes |
| NCT00123643 | PHASE4 | COMPLETED | Vascular Effects of Rosiglitazone Versus Glyburide in Type 2 Diabetic Patients |
| NCT00124397 | PHASE4 | COMPLETED | Atorvastatin and Endothelial Function in Type 2 Diabetes Mellitus (ATTEND-Study) |
| NCT00129233 | PHASE4 | COMPLETED | Comparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance |
| NCT00133718 | PHASE4 | COMPLETED | A 2 Year Trial of Patients With Type 2 Diabetes Focusing on Cardiovascular Diagnostics and Metabolic Control |
| NCT00135070 | PHASE4 | TERMINATED | Hospital In-Patient Insulin Study |
| NCT00141232 | PHASE4 | COMPLETED | Evaluating Atorvastatin With Omega-3 Fatty Acids in Cardiovascular Risk Reduction in Patients With Type 2 Diabetes |
| NCT00144144 | PHASE4 | UNKNOWN | A Study on Ca Blocker Versus AII Antagonists in Hypertension With Type 2 Diabetes |
| NCT00149331 | PHASE4 | COMPLETED | The Effects of Two Education Strategies About Insulin on Patient Preferences and Perceptions About Insulin Therapy |
| NCT00162357 | PHASE4 | COMPLETED | Post-PCI:Cardiac Imaging in Patients With Diabetes to Detect Coronary Artery Blockages Previously Opened by Angioplasty |
| NCT00174681 | PHASE4 | COMPLETED | Tulip Study: Testing the Usefulness of Lantus When Initiated Prematurely In Patients With Type 2 Diabetes |
| NCT00174824 | PHASE4 | COMPLETED | Comparison of Insulin Glargine and NPH Human Insulin in Progression of Diabetic Retinopathy in Type 2 Diabetic Patients |
| NCT00177398 | PHASE4 | COMPLETED | Effect of Glargine Insulin on Glucose Control in Hospitalized Patients Who Receive Tube Feedings |
| NCT00179400 | PHASE4 | COMPLETED | The Role of Acute Combined PPAR Alpha and Gamma Stimulation on Insulin Action in Humans |
| NCT00184561 | PHASE4 | COMPLETED | Effectiveness and Safety of Biphasic Insulin Aspart 70/30 in Subjects With Type 2 Diabetes |
| NCT00184626 | PHASE4 | COMPLETED | Comparison of Insulin Glargine Versus Biphasic Insulin Aspart 30/70 or Biphasic Insulin Aspart 30/70 in Combination With Metformin in Subjects With Type 2 Diabetes. |
| NCT00191178 | PHASE4 | COMPLETED | Effects of Insulin in Perceived Mood Symptoms in Patients With Type 2 Diabetes |
| NCT00191282 | PHASE4 | COMPLETED | Hyperglycemia and Cardiovascular Outcomes With Type 2 Diabetes |
| NCT00191464 | PHASE4 | COMPLETED | Long-Term Effects of Insulin Plus Metformin Regimens on the Overall and Postprandial Glycemic Control of Patients With Type 2 Diabetes |
| NCT00192803 | PHASE4 | UNKNOWN | Non-Insulin Dependent Diabetes Mellitus (NIDDM) and Angiotensin Converting Enzyme 2 (ACE2): Diabetic Patients Treated With Antihypertensive Drugs |
| NCT00202033 | PHASE4 | COMPLETED | Impact of Self-Monitoring Blood Glucose Frequency on Glycemic Control in Patients With Type 2 Diabetes |
| NCT00205660 | PHASE4 | COMPLETED | Changes in Adiposity, Metabolic Measures From Atypicals to Aripiprazole |
| NCT00212290 | PHASE4 | COMPLETED | Insulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes |
| NCT00212303 | PHASE4 | COMPLETED | Exercise Training in Type 2 Diabetes and Hypertension |
| NCT00225342 | PHASE4 | WITHDRAWN | Study Protocol for Rosiglitazone Versus Gliclazide in Diabetics With Angina |
| NCT00238472 | PHASE4 | COMPLETED | A Pilot Study to Evaluate the Effects of Nateglinide vs. Glibenclamide on Renal Hemodynamics and Albumin Excretion |
| NCT00239538 | PHASE4 | COMPLETED | SMOOTH - Blood Pressure Control in Diabetic/Obese Patients |
| NCT00240253 | PHASE4 | COMPLETED | A Study Evaluating the Efficacy and Safety of Adding Symlin® to Lantus® (Insulin Glargine) in Subjects With Type 2 Diabetes |
| NCT00240422 | PHASE4 | COMPLETED | Trial to Compare the Effects of Either Telmisartan (40-80 mg PO Once Daily) or Ramipril (5-10 mg PO Once Daily) on Renal Endothelial Dysfunction in Hypertensive Patients With Type 2 Diabetes |
| NCT00241085 | PHASE4 | COMPLETED | Effect of Valsartan on Proteinuria in Patients With Hypertension and Diabetes Mellitus |
Related Atlas pages
- Targeted by drugs: Albiglutide, Ecnoglutide, Exenatide, Glucagon, Liraglutide, Lixisenatide, Mazdutide, Orforglipron, Retatrutide, Semaglutide, Survodutide, Taspoglutide, Tirzepatide
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): type 2 diabetes mellitus