RAMP1
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Summary
RAMP1 (receptor activity modifying protein 1, HGNC:9843) is a protein-coding gene on chromosome 2q37.3, encoding Receptor activity-modifying protein 1 (O60894). Accessory protein that interacts with and modulates the function of G-protein coupled receptors including calcitonin gene-related peptide type 1 receptor (CALCRL) and calcitonin receptor (CALCR).
The protein encoded by this gene is a member of the RAMP family of single-transmembrane-domain proteins, called receptor (calcitonin) activity modifying proteins (RAMPs). RAMPs are type I transmembrane proteins with an extracellular N terminus and a cytoplasmic C terminus. RAMPs are required to transport calcitonin-receptor-like receptor (CRLR) to the plasma membrane. CRLR, a receptor with seven transmembrane domains, can function as either a calcitonin-gene-related peptide (CGRP) receptor or an adrenomedullin receptor, depending on which members of the RAMP family are expressed. In the presence of this (RAMP1) protein, CRLR functions as a CGRP receptor. The RAMP1 protein is involved in the terminal glycosylation, maturation, and presentation of the CGRP receptor to the cell surface. Alternative splicing results in multiple transcript variants encoding different isoforms.
Source: NCBI Gene 10267 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 40 total
- Druggable target: yes — 10 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_005855
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:9843 |
| Approved symbol | RAMP1 |
| Name | receptor activity modifying protein 1 |
| Location | 2q37.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000132329 |
| Ensembl biotype | protein_coding |
| OMIM | 605153 |
| Entrez | 10267 |
Gene structure
Transcript identifiers
Ensembl transcripts: 7 — 7 protein_coding
ENST00000254661, ENST00000403885, ENST00000404910, ENST00000409726, ENST00000884470, ENST00000884471, ENST00000951440
RefSeq mRNA: 2 — MANE Select: NM_005855
NM_001308353, NM_005855
CCDS: CCDS2522, CCDS77546
Canonical transcript exons
ENST00000254661 — 3 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001073872 | 237859623 | 237859727 |
| ENSE00001073873 | 237911528 | 237912106 |
| ENSE00003594791 | 237877224 | 237877362 |
Expression profiles
Bgee: expression breadth ubiquitous, 269 present calls, max score 99.55.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 9.6863 / max 363.6931, expressed in 929 samples.
FANTOM5 promoters (6 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 26306 | 8.5133 | 885 |
| 26303 | 0.6372 | 186 |
| 26305 | 0.3102 | 130 |
| 26304 | 0.1019 | 38 |
| 26302 | 0.0761 | 20 |
| 26301 | 0.0476 | 21 |
Top tissues by expression
290 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| body of uterus | UBERON:0009853 | 99.55 | gold quality |
| ascending aorta | UBERON:0001496 | 99.31 | gold quality |
| thoracic aorta | UBERON:0001515 | 99.30 | gold quality |
| endocervix | UBERON:0000458 | 99.18 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 99.18 | gold quality |
| right coronary artery | UBERON:0001625 | 99.12 | gold quality |
| aorta | UBERON:0000947 | 98.83 | gold quality |
| left uterine tube | UBERON:0001303 | 98.80 | gold quality |
| apex of heart | UBERON:0002098 | 98.63 | gold quality |
| popliteal artery | UBERON:0002250 | 98.55 | gold quality |
| tibial artery | UBERON:0007610 | 98.55 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 98.46 | gold quality |
| mucosa of stomach | UBERON:0001199 | 98.44 | gold quality |
| lower esophagus | UBERON:0013473 | 98.34 | gold quality |
| myometrium | UBERON:0001296 | 98.31 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 98.19 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 98.18 | gold quality |
| body of pancreas | UBERON:0001150 | 98.16 | gold quality |
| right atrium auricular region | UBERON:0006631 | 98.12 | gold quality |
| heart left ventricle | UBERON:0002084 | 97.88 | gold quality |
| cardiac ventricle | UBERON:0002082 | 97.67 | gold quality |
| nucleus accumbens | UBERON:0001882 | 97.56 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 97.49 | gold quality |
| left coronary artery | UBERON:0001626 | 97.38 | gold quality |
| cardiac atrium | UBERON:0002081 | 97.22 | gold quality |
| amygdala | UBERON:0001876 | 97.17 | gold quality |
| coronary artery | UBERON:0001621 | 97.05 | gold quality |
| gastrocnemius | UBERON:0001388 | 96.97 | gold quality |
| right frontal lobe | UBERON:0002810 | 96.92 | gold quality |
| caudate nucleus | UBERON:0001873 | 96.87 | gold quality |
Single-cell (SCXA)
Detected in 16 experiment(s), a significant marker in 16.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-10287 | yes | 2092.41 |
| E-MTAB-6701 | yes | 1335.61 |
| E-HCAD-24 | yes | 1059.36 |
| E-HCAD-36 | yes | 993.18 |
| E-MTAB-9906 | yes | 561.89 |
| E-GEOD-125970 | yes | 296.81 |
| E-CURD-84 | yes | 236.19 |
| E-HCAD-1 | yes | 31.99 |
| E-HCAD-6 | yes | 30.32 |
| E-MTAB-6678 | yes | 29.91 |
| E-MTAB-8142 | yes | 27.98 |
| E-MTAB-5061 | yes | 18.83 |
| E-HCAD-25 | yes | 17.29 |
| E-CURD-112 | yes | 5.25 |
| E-HCAD-10 | yes | 4.10 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): NKX3-1
miRNA regulators (miRDB)
15 targeting RAMP1, 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-4719 | 99.73 | 72.10 | 3329 |
| HSA-MIR-6832-3P | 99.52 | 70.44 | 1726 |
| HSA-MIR-520A-5P | 99.35 | 66.72 | 1632 |
| HSA-MIR-525-5P | 99.35 | 66.85 | 1615 |
| HSA-MIR-4505 | 99.27 | 67.81 | 2678 |
| HSA-MIR-5787 | 99.22 | 67.86 | 2628 |
| HSA-MIR-328-5P | 99.08 | 64.65 | 1000 |
| HSA-MIR-6885-5P | 98.71 | 64.33 | 902 |
| HSA-MIR-6881-5P | 98.16 | 67.38 | 665 |
| HSA-MIR-6870-3P | 98.08 | 65.10 | 692 |
| HSA-MIR-6842-3P | 98.07 | 66.33 | 1325 |
| HSA-MIR-3652 | 97.71 | 65.43 | 1890 |
| HSA-MIR-4430 | 97.47 | 65.61 | 1813 |
| HSA-MIR-4474-3P | 96.97 | 65.87 | 870 |
| HSA-MIR-6890-5P | 92.89 | 65.83 | 442 |
Literature-anchored findings (GeneRIF, showing 40)
- Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells (PMID:11693189)
- Co-expression of RAMP1 and CRLR reconstituted a CGRP receptor that was able to activate the pheromone-signaling pathway with pharmacological properties similar to those observed previously in mammalian cells. (PMID:11733510)
- Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists. (PMID:11847213)
- The CGRP receptor components, RAMP1 and CRLR, are down-regulated during myeloid differentiation of CD34+ cells, and CGRP receptor selectively promotes the development of CFU-GM. (PMID:11937264)
- results show the presence of calcitonin receptor-like receptor and receptor activity-modifying proteins in middle meningeal, middle cerebral, pial, and superficial temporal vessels (PMID:11973435)
- Co-expression of calcitonin receptors (CT) lacking a portion of domain 1 with receptor activity-modifying protein (RAMP) 1, 2, or 3 appears to produce functional CT-(8-32)-sensitive adrenomedullin receptors. (PMID:12565884)
- The extracellular domain of receptor activity-modifying protein 1 is sufficient for calcitonin receptor-like receptor function (PMID:12574158)
- identification of domains responsible for agonist binding specificity (PMID:12684503)
- TNF-alpha induced time- and dose-dependent decreases in the expression of RAMP1 mRNA in cultured human coronary artery smooth muscle cells, thereby diminishing AM-evoked cAMP production (PMID:15245870)
- Data found that expressions of RAMP1, RAMP2 and RAMP3 mRNAs increased with the worsening of heart function, but the expressions of RAMP1 and RAMP2 mRNA decreased at level IV of heart failure. (PMID:15300632)
- calcitonin receptor-like receptor heterodimer with RAMP1 yields a calcitonin gene-related peptide receptor (PMID:15613468)
- This study reveals important functionality of the RAMP C-terminal domain and identifies key differences in the role of the RAMP C terminus for calcitonin receptor versus calcitonin receptor-like receptor-based receptors. (PMID:16912219)
- CLR and RAMP1 traffic from endosomes to lysosomes by ubiquitin-independent mechanisms, where they are degraded at different rates (PMID:17310067)
- RAMP1 interacts with tubulin. (PMID:17493758)
- Functional calcitonin gene-related peptide receptors are formed by the asymmetric assembly of a calcitonin receptor-like receptor and RAMP1. (PMID:17785463)
- We did not observe any difference in mRNA for CL-R and RAMPs in arteries from patients with hemorrhagic stroke, arteriosclerosis and acute myocardial infarction when compared to patients without these diagnoses (PMID:18198792)
- RAMP1 may be strongly considered as a candidate gene for migraine. (PMID:18240900)
- Identification of RAMP1 residues important for calcitonin gene-related peptide are reported. (PMID:18593822)
- the crystal structure of the extracellular domain of human RAMP1 at 2.4 A resolution was determined. (PMID:18725456)
- The T-A-C haplotype is a genetic marker for cerebral infarction, and RAMP1 is associated with increased susceptibility to cerebral infarction. (PMID:19710695)
- RAMP1 overexpression attenuates Ang-II-induced hypertension and induces a protective change in cardiovascular autonomic regulation (PMID:20100989)
- These data for the first time pinpoint a specific RAMP1 residue important for both antagonist and agonist potency and are consistent with the N-terminal domain of RAMP1 forming the binding pocket interface with calcitonin receptor-like receptor. (PMID:20188075)
- lower expression in bronchial biopsies from subjects with asthma (PMID:20933260)
- The present finding demonstrated that RAMP1 immunoreactivity was localized in many neurons and phenopalatine ganglion. (PMID:22208649)
- CLR and RAMP1 co-localize in the enteric nervous system of human stomach, ileum, and colon, and are in close proximity to their ligands CGRP and IMD (PMID:22484227)
- RAMP1 overexpression enhances the promoting effect that exogenous CGRP has on osteogenic differentiation (PMID:22949393)
- No significant association of the tested SNPs of the RAMP1 gene were found with migraine susceptibility. (PMID:23237777)
- multiple NKX3.1 binding sites were found in the RAMP1 locus in human prostate cancer cells and in the normal mouse prostate. (PMID:23867798)
- A novel functional role for RAMP1 in regulation of CaSR signalling in addition to its known role in receptor trafficking, is reported. (PMID:24454825)
- RAMP1 rs7590387 has a role in the transformation of episodic migraine into medication overuse headache. (PMID:25881990)
- Data suggest that ligand binding of a G protein-coupled receptor (GPCR) may inform drug development targeting calcitonin receptor-like receptor (CLR):receptor activity-modifying proteins RAMP1/2 complexes. (PMID:25982113)
- Evidence that DNA methylation at RAMP1 gene promoter plays a role in migraine was described. (PMID:26501962)
- T-A-T RAMP1 gene haplotype might have utility as a genetic marker for Essential Hypertension and that the RAMP1 gene may be associated with increased susceptibility to Essential Hypertension in a Japanese population. (PMID:28181496)
- Data suggest CGRP receptor (CGRPR) ECL2 (extracellular loop 2 domain) enables interaction with N-terminal residues of CGRP; this provides evidence for dual involvement of ECL2 in two-domain binding model of CGRP/CGRPR interaction; CGRPR is obligate heterodimer of CLR/RAMP1. (CGRP = calcitonin gene-related peptide; CLR = calcitonin receptor-like receptor; RAMP1 = receptor [calcitonin] activity modifying protein 1) (PMID:28691801)
- in nestin/hRAMP1 transgenic mice, hypertension caused by Ang II or phenylephrine was greatly attenuated, and associated autonomic dysregulation and increased sympathetic vasomotor tone were diminished or abolished. (PMID:29297736)
- structure of the human CGRP receptor in complex with CGRP and the Gs-protein heterotrimer at 3.3 A global resolution, determined by Volta phase-plate cryo-electron microscopy (PMID:30209400)
- Based on the finding that an acylated chimeric ADM/ADM2 analog potently stimulates CLR/RAMP1 and 2 signaling, we hypothesized that the binding domain of this analog could have potent inhibitory activity on CLR/RAMP receptors. (PMID:31150417)
- Structure and dynamics of the CGRP receptor in apo and peptide-bound forms. (PMID:33602864)
- Peptide ligand interaction with maltose-binding protein tagged to the calcitonin gene-related peptide receptor: The inhibitory role of receptor N-glycosylation. (PMID:35007660)
- Involvement of RAMP1/p38MAPK signaling pathway in osteoblast differentiation in response to mechanical stimulation: a preliminary study. (PMID:38825686)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ramp1 | ENSDARG00000056704 |
| mus_musculus | Ramp1 | ENSMUSG00000034353 |
| rattus_norvegicus | ENSRNOG00000089232 |
Paralogs (2): RAMP3 (ENSG00000122679), RAMP2 (ENSG00000131477)
Protein
Protein identifiers
Receptor activity-modifying protein 1 — O60894 (reviewed: O60894)
Alternative names: Calcitonin-receptor-like receptor activity-modifying protein 1
All UniProt accessions (2): O60894, E9PC20
UniProt curated annotations — full annotation on UniProt →
Function. Accessory protein that interacts with and modulates the function of G-protein coupled receptors including calcitonin gene-related peptide type 1 receptor (CALCRL) and calcitonin receptor (CALCR). Required for the transport of CALCRL to the plasma membrane. Together with CALCRL, form the receptor complex for the calcitonin gene-related peptides CGRP1/CALCA and CGRP2/CALCB. Together with CALCR, form the AMYR1 receptor complex for amylin/IAPP and CGRP1/CALCA.
Subunit / interactions. Heterodimer of CALCRL and RAMP1; the interaction induces allosteric modulation of CALCRL function and CGRP1/CALCA and CGRP2/CALCB ligand specificity. Heterodimer of CALCR and RAMP1; interaction forms the AMYR1 receptor complex for amylin/IAPP and CGRP1/CALCA ligands.
Subcellular location. Cell membrane.
Tissue specificity. Expressed in many tissues including the uterus, bladder, brain, pancreas and gastro-intestinal tract.
Similarity. Belongs to the RAMP family.
RefSeq proteins (2): NP_001295282, NP_005846* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR006985 | RAMP | Family |
| IPR038126 | RAMP_sf | Homologous_superfamily |
Pfam: PF04901
UniProt features (19 total): helix 7, strand 3, disulfide bond 3, topological domain 2, signal peptide 1, chain 1, turn 1, transmembrane region 1
Structure
Experimental structures (PDB)
26 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 6ZHO | X-RAY DIFFRACTION | 1.6 |
| 8AX7 | X-RAY DIFFRACTION | 1.65 |
| 6ZIS | X-RAY DIFFRACTION | 1.73 |
| 7P0F | X-RAY DIFFRACTION | 1.85 |
| 8AX6 | X-RAY DIFFRACTION | 1.9 |
| 6D1U | X-RAY DIFFRACTION | 2.05 |
| 3N7S | X-RAY DIFFRACTION | 2.1 |
| 7TYF | ELECTRON MICROSCOPY | 2.2 |
| 9BP3 | ELECTRON MICROSCOPY | 2.2 |
| 7P0I | X-RAY DIFFRACTION | 2.3 |
| 2YX8 | X-RAY DIFFRACTION | 2.4 |
| 9AUC | ELECTRON MICROSCOPY | 2.4 |
| 4RWG | X-RAY DIFFRACTION | 2.44 |
| 6UMG | X-RAY DIFFRACTION | 2.7 |
| 8AX5 | X-RAY DIFFRACTION | 2.75 |
| 3N7P | X-RAY DIFFRACTION | 2.8 |
| 5V6Y | X-RAY DIFFRACTION | 2.8 |
| 3N7R | X-RAY DIFFRACTION | 2.9 |
| 7TYW | ELECTRON MICROSCOPY | 3 |
| 9UWQ | ELECTRON MICROSCOPY | 3.1 |
| 7KNT | ELECTRON MICROSCOPY | 3.15 |
| 9BLW | ELECTRON MICROSCOPY | 3.2 |
| 9MM5 | ELECTRON MICROSCOPY | 3.26 |
| 6E3Y | ELECTRON MICROSCOPY | 3.3 |
| 7KNU | ELECTRON MICROSCOPY | 3.49 |
| 9MNI | ELECTRON MICROSCOPY | 4.06 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O60894-F1 | 89.95 | 0.75 |
Antibody-complex structures (SAbDab): 6 — 6E3Y, 6UMG, 7TYF, 7TYW, 9AUC, 9BLW
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (3): 27–82, 40–72, 57–104
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-418555 | G alpha (s) signalling events |
| R-HSA-419812 | Calcitonin-like ligand receptors |
MSigDB gene sets: 362 (showing top):
GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_DN, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_UP, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, VERHAAK_AML_WITH_NPM1_MUTATED_DN, BENPORATH_ES_WITH_H3K27ME3, YAGI_AML_WITH_INV_16_TRANSLOCATION, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, GOCC_CELL_SURFACE, GOBP_VESICLE_MEDIATED_TRANSPORT, GOBP_PROTEIN_LOCALIZATION_TO_CELL_PERIPHERY, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, GOBP_MONOATOMIC_CATION_TRANSPORT, PATIL_LIVER_CANCER, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_REGULATION_OF_GLYCOPROTEIN_METABOLIC_PROCESS
GO Biological Process (15): angiogenesis (GO:0001525), calcium ion transport (GO:0006816), intracellular protein transport (GO:0006886), G protein-coupled receptor signaling pathway (GO:0007186), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), regulation of G protein-coupled receptor signaling pathway (GO:0008277), positive regulation of glycoprotein biosynthetic process (GO:0010560), protein transport (GO:0015031), receptor internalization (GO:0031623), cellular response to hormone stimulus (GO:0032870), protein localization to plasma membrane (GO:0072659), amylin receptor signaling pathway (GO:0097647), amylin receptor 1 signaling pathway (GO:0150059), calcitonin gene-related peptide receptor signaling pathway (GO:1990408), obsolete positive regulation of protein glycosylation (GO:0060050)
GO Molecular Function (5): calcitonin gene-related peptide receptor activity (GO:0001635), coreceptor activity (GO:0015026), amylin receptor activity (GO:0097643), calcitonin gene-related peptide binding (GO:1990407), protein binding (GO:0005515)
GO Cellular Component (5): plasma membrane (GO:0005886), cell surface (GO:0009986), signaling receptor complex (GO:0043235), CGRP receptor complex (GO:1990406), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-2 pathways:
| Category | Pathways |
|---|---|
| GPCR downstream signalling | 1 |
| Class B/2 (Secretin family receptors) | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| intracellular protein localization | 2 |
| calcitonin family receptor signaling pathway | 2 |
| calcitonin family receptor activity | 2 |
| cellular anatomical structure | 2 |
| blood vessel morphogenesis | 1 |
| anatomical structure formation involved in morphogenesis | 1 |
| metal ion transport | 1 |
| protein transport | 1 |
| intracellular transport | 1 |
| G protein-coupled receptor activity | 1 |
| signal transduction | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase activator activity | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| regulation of signal transduction | 1 |
| glycoprotein biosynthetic process | 1 |
| positive regulation of macromolecule biosynthetic process | 1 |
| regulation of glycoprotein biosynthetic process | 1 |
| positive regulation of glycoprotein metabolic process | 1 |
| transport | 1 |
| establishment of protein localization | 1 |
| receptor-mediated endocytosis | 1 |
| response to hormone | 1 |
| cellular response to chemical stimulus | 1 |
| cellular response to endogenous stimulus | 1 |
| protein localization to membrane | 1 |
| protein localization to cell periphery | 1 |
| amylin receptor signaling pathway | 1 |
| signaling receptor activity | 1 |
| calcitonin family binding | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| protein-containing complex | 1 |
| calcitonin family receptor complex | 1 |
Protein interactions and networks
STRING
622 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| RAMP1 | CALCR | P30988 | 999 |
| RAMP1 | CALCRL | Q16602 | 999 |
| RAMP1 | CRCP | O75575 | 981 |
| RAMP1 | IAPP | P10997 | 980 |
| RAMP1 | ADM | P35318 | 976 |
| RAMP1 | CALCB | P10092 | 965 |
| RAMP1 | CALCA | P01258 | 929 |
| RAMP1 | ADM2 | Q7Z4H4 | 922 |
| RAMP1 | VIPR1 | P32241 | 766 |
| RAMP1 | VIPR2 | P41587 | 748 |
| RAMP1 | TAC1 | P20366 | 700 |
| RAMP1 | CASR | P41180 | 696 |
| RAMP1 | RAMP2 | O60895 | 653 |
| RAMP1 | RAMP3 | O60896 | 651 |
| RAMP1 | TACR1 | P25103 | 618 |
IntAct
396 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CALCRL | RAMP1 | psi-mi:“MI:0407”(direct interaction) | 0.810 |
| RAMP1 | CALCRL | psi-mi:“MI:0407”(direct interaction) | 0.810 |
| RAMP1 | CALCRL | psi-mi:“MI:0915”(physical association) | 0.810 |
| CALCA | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.610 |
| NKG7 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MAL | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| MS4A13 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RAMP1 | NKG7 | psi-mi:“MI:0915”(physical association) | 0.560 |
| RAMP1 | MAL | psi-mi:“MI:0915”(physical association) | 0.560 |
| RAMP1 | MS4A13 | psi-mi:“MI:0915”(physical association) | 0.560 |
| ACKR3 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADGRE5 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADGRG3 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADGRG5 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADORA1 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP1 | ADORA2A | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADORA2B | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADRB1 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| ADRB2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| AVPR1A | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| AVPR1B | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| BDKRB1 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| BDKRB2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
BioGRID (46): RAMP1 (Synthetic Growth Defect), RAMP1 (Synthetic Growth Defect), CALCRL (Affinity Capture-Luminescence), CALCRL (Reconstituted Complex), RAMP1 (Affinity Capture-RNA), RAMP1 (Reconstituted Complex), RAMP1 (Reconstituted Complex), RAMP1 (Reconstituted Complex), RAMP1 (Reconstituted Complex), RAMP1 (Affinity Capture-Western), RAMP1 (Two-hybrid), MAL (Two-hybrid), MS4A13 (Two-hybrid), RAMP1 (Reconstituted Complex), RAMP1 (Co-localization)
ESM2 similar proteins: A7MBM2, E9PY61, O00391, O08542, O60894, O60895, O76095, O77049, O88824, P52798, Q15904, Q16586, Q5Q0T9, Q5RJL6, Q641Q3, Q6IUU3, Q6P5F7, Q6PRD1, Q6UWJ8, Q6ZVN8, Q6ZVW7, Q7TQ32, Q80YF6, Q864V4, Q867C0, Q86WC4, Q8BGT0, Q8BH06, Q8BND5, Q8C1Q4, Q8K4C2, Q8N271, Q8N7M5, Q8NAC3, Q8R4C4, Q8R4C5, Q8R4C6, Q8VE43, Q91ZV8, Q96F46
Diamond homologs: O60894, O60896, Q7YS88, Q867C0, Q8R4C4, Q8R4C6, Q9JJ73, Q9JJ74, Q9WTJ5, Q9WUP1, Q8R4C5, Q9JHJ1, Q9WUP0, O60895
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| RAMP1 | “form complex” | “Amylin receptor 1 complex” | binding |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 165 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 |
|---|---|---|---|
| Amine ligand-binding receptors | 20 | 50.1× | 1e-29 |
| Class A/1 (Rhodopsin-like receptors) | 58 | 31.2× | 6e-73 |
| GPCR ligand binding | 55 | 25.6× | 2e-63 |
| Peptide ligand-binding receptors | 44 | 23.6× | 2e-48 |
| G alpha (q) signalling events | 50 | 20.8× | 4e-52 |
| G alpha (s) signalling events | 32 | 17.0× | 1e-29 |
| GPCR downstream signalling | 53 | 16.7× | 2e-50 |
| Chemokine receptors bind chemokines | 12 | 16.3× | 1e-10 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| activation of adenylate cyclase activity | 8 | 55.1× | 3e-11 |
| complement receptor mediated signaling pathway | 7 | 48.2× | 2e-09 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 22 | 42.1× | 1e-28 |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | 30 | 40.3× | 7e-39 |
| dendritic cell chemotaxis | 6 | 36.5× | 4e-07 |
| phospholipase C-activating G protein-coupled receptor signaling pathway | 43 | 34.7× | 3e-53 |
| vasoconstriction | 6 | 32.6× | 7e-07 |
| positive regulation of cytosolic calcium ion concentration | 45 | 32.3× | 4e-54 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
40 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 27 |
| Likely benign | 6 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
898 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 2:237859725:TGGG:T | donor_loss | 1.0000 |
| 2:237859726:GG:G | donor_gain | 1.0000 |
| 2:237859726:GGGT:G | donor_loss | 1.0000 |
| 2:237859727:GG:G | donor_gain | 1.0000 |
| 2:237859728:G:GA | donor_loss | 1.0000 |
| 2:237859728:G:GG | donor_gain | 1.0000 |
| 2:237859729:T:G | donor_loss | 1.0000 |
| 2:237859732:G:GG | donor_gain | 1.0000 |
| 2:237859723:CCTGG:C | donor_gain | 0.9900 |
| 2:237859725:TGG:T | donor_gain | 0.9900 |
| 2:237859726:GGG:G | donor_gain | 0.9900 |
| 2:237877222:A:AG | acceptor_gain | 0.9900 |
| 2:237877223:G:GG | acceptor_gain | 0.9900 |
| 2:237877359:TCAGG:T | donor_loss | 0.9900 |
| 2:237877363:G:T | donor_loss | 0.9900 |
| 2:237877364:T:A | donor_loss | 0.9900 |
| 2:237911523:CGCA:C | acceptor_loss | 0.9900 |
| 2:237911524:GCA:G | acceptor_loss | 0.9900 |
| 2:237911525:CA:C | acceptor_loss | 0.9900 |
| 2:237911526:A:AG | acceptor_gain | 0.9900 |
| 2:237911526:AG:A | acceptor_gain | 0.9900 |
| 2:237911527:G:GG | acceptor_gain | 0.9900 |
| 2:237911527:G:GT | acceptor_loss | 0.9900 |
| 2:237911527:GG:G | acceptor_gain | 0.9900 |
| 2:237911527:GGA:G | acceptor_gain | 0.9900 |
| 2:237859724:CTGG:C | donor_gain | 0.9800 |
| 2:237859730:GA:G | donor_gain | 0.9800 |
| 2:237877223:GCCC:G | acceptor_gain | 0.9800 |
| 2:237911525:CAGG:C | acceptor_gain | 0.9800 |
| 2:237911526:AGGA:A | acceptor_gain | 0.9800 |
AlphaMissense
958 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 2:237877302:T:G | F44C | 0.984 |
| 2:237877301:T:C | F44L | 0.983 |
| 2:237877303:C:A | F44L | 0.983 |
| 2:237877303:C:G | F44L | 0.983 |
| 2:237877348:G:C | W59C | 0.980 |
| 2:237877348:G:T | W59C | 0.980 |
| 2:237911637:T:C | F101L | 0.980 |
| 2:237911638:T:G | F101C | 0.980 |
| 2:237911639:C:A | F101L | 0.980 |
| 2:237911639:C:G | F101L | 0.980 |
| 2:237911588:G:C | W84C | 0.970 |
| 2:237911588:G:T | W84C | 0.970 |
| 2:237911638:T:C | F101S | 0.962 |
| 2:237877302:T:C | F44S | 0.958 |
| 2:237877340:T:A | C57S | 0.957 |
| 2:237877341:G:C | C57S | 0.957 |
| 2:237911637:T:A | F101I | 0.950 |
| 2:237911647:G:A | C104Y | 0.939 |
| 2:237877339:G:C | W56C | 0.933 |
| 2:237877339:G:T | W56C | 0.933 |
| 2:237911583:T:C | F83L | 0.932 |
| 2:237911585:C:A | F83L | 0.932 |
| 2:237911585:C:G | F83L | 0.932 |
| 2:237911614:T:G | F93C | 0.930 |
| 2:237911637:T:G | F101V | 0.930 |
| 2:237911613:T:C | F93L | 0.926 |
| 2:237911615:C:A | F93L | 0.926 |
| 2:237911615:C:G | F93L | 0.926 |
| 2:237877341:G:A | C57Y | 0.925 |
| 2:237911552:C:G | C72W | 0.924 |
dbSNP variants (sampled 300 via entrez): RS1000069537 (2:237860308 A>G), RS1000092442 (2:237865938 G>A), RS1000126621 (2:237903059 A>C), RS1000155108 (2:237876597 G>A), RS1000213712 (2:237884991 C>T), RS1000270684 (2:237879250 G>A), RS1000300869 (2:237895615 G>A), RS1000321310 (2:237881750 G>A,C), RS1000322604 (2:237879455 G>T), RS1000346965 (2:237871280 G>A,T), RS1000415620 (2:237912388 C>T), RS1000471340 (2:237897732 C>G,T), RS1000488882 (2:237893478 T>C), RS1000495195 (2:237885718 C>G,T), RS1000565652 (2:237884844 G>C)
Disease associations
OMIM: gene MIM:605153 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001762_366 | Obesity-related traits | 8.000000e-06 |
| GCST004523_9 | Resting metabolic rate | 8.000000e-06 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0006336 | diastolic blood pressure |
| EFO:0008004 | resting metabolic rate measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL2107838 (PROTEIN COMPLEX), CHEMBL2111189 (PROTEIN COMPLEX)
Molecules with ChEMBL bioactivity
10 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 3,069 (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 |
|---|---|---|---|
| CHEMBL2103758 | PRAMLINTIDE | 4 | 883 |
| CHEMBL2364638 | UBROGEPANT | 4 | 428 |
| CHEMBL3989767 | CALCITONIN SALMON | 4 | 666 |
| CHEMBL3991065 | ATOGEPANT | 4 | 251 |
| CHEMBL236593 | TELCAGEPANT | 3 | 254 |
| CHEMBL4802169 | CAGRILINTIDE | 3 | |
| CHEMBL1910936 | MK3207 | 2 | 163 |
| CHEMBL207197 | OLCEGEPANT | 2 | 347 |
| CHEMBL3334624 | BI-44370 | 2 | 62 |
| CHEMBL4635331 | HTL-0022562 | 1 | 15 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
3 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs6431564 | RAMP1 | 0.00 | 0 | ||
| rs13386048 | RAMP1 | 0.00 | 0 | ||
| rs12465864 | RAMP1 | 0.00 | 0 |
Binding affinities (BindingDB)
14 measured of 14 human assays (14 total across all organisms); most potent 14 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | KI | 0.02 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-1-[[(2S)-3-[1-[2-(dimethylamino)ethyl]piperidin-4-yl]-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]-3-(7-methyl-2,3,3a,4,5,6,7,7a-octahydro-1H-indazol-5-yl)-1-oxopropan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | KI | 0.025 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(7-methyl-2,3,3a,4,5,6,7,7a-octahydro-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4’-piperidine]-1’-carboxamide | KI | 0.032 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-(1-propylpiperidin-4-yl)-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxoquinolin-3-ylidene)piperidine-1-carboxamide | KI | 0.04 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-1-[[(2S)-3-(1-ethylpiperidin-4-yl)-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl]-4-(2-oxoquinolin-3-ylidene)piperidine-1-carboxamide | KI | 0.04 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | KI | 0.04 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxoquinolin-3-ylidene)piperidine-1-carboxamide | KI | 0.063 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide | KI | 0.063 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxoquinolin-3-ylidene)piperidine-1-carboxamide | KI | 0.079 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide | KI | 0.079 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4’-piperidine]-1’-carboxamide | KI | 0.079 nM | US-10300056: CGRP receptor antagonists |
| tert-butyl 4-[(2S)-2-[[(2R)-3-(7-methyl-1H-indazol-5-yl)-2-[[4-(2-oxoquinolin-3-ylidene)piperidine-1-carbonyl]amino]propanoyl]amino]-3-oxo-3-(4-pyridin-4-ylpiperazin-1-yl)propyl]piperidine-1-carboxylate | KI | 0.1 nM | US-10300056: CGRP receptor antagonists |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-(1-pentanoylpiperidin-4-yl)-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxoquinolin-3-ylidene)piperidine-1-carboxamide | KI | 0.1 nM | US-10300056: CGRP receptor antagonists |
| 3-[4-[(2S)-2-[[(2R)-3-(7-methyl-2,3,3a,4,5,6,7,7a-octahydro-1H-indazol-5-yl)-2-[[4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carbonyl]amino]propanoyl]amino]-3-oxo-3-(4-pyridin-4-ylpiperazin-1-yl)propyl]piperidin-1-yl]-3-oxopropanoate | KI | 0.1 nM | US-10300056: CGRP receptor antagonists |
ChEMBL bioactivities
234 potent at pChembl≥5 of 237 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 11.00 | IC50 | 0.01 | nM | CHEMBL4643006 |
| 10.96 | Ki | 0.011 | nM | CHEMBL3893283 |
| 10.85 | Ki | 0.014 | nM | CHEMBL2035984 |
| 10.82 | Ki | 0.015 | nM | CHEMBL3981883 |
| 10.82 | Ki | 0.015 | nM | ATOGEPANT |
| 10.80 | Ki | 0.016 | nM | CHEMBL2035985 |
| 10.77 | Ki | 0.017 | nM | CHEMBL3914484 |
| 10.73 | EC50 | 0.01862 | nM | CAGRILINTIDE |
| 10.70 | Ki | 0.02 | nM | CHEMBL264010 |
| 10.70 | Ki | 0.02 | nM | CHEMBL2371890 |
| 10.70 | Ki | 0.01995 | nM | CHEMBL4638112 |
| 10.70 | Ki | 0.02 | nM | CHEMBL4638635 |
| 10.70 | Ki | 0.02 | nM | CHEMBL4638112 |
| 10.66 | Ki | 0.022 | nM | MK3207 |
| 10.66 | EC50 | 0.02188 | nM | PRAMLINTIDE |
| 10.60 | Ki | 0.02512 | nM | CHEMBL4638938 |
| 10.60 | Ki | 0.025 | nM | CHEMBL5813875 |
| 10.55 | Ki | 0.028 | nM | CHEMBL2035982 |
| 10.52 | IC50 | 0.03 | nM | OLCEGEPANT |
| 10.50 | Ki | 0.03162 | nM | OLCEGEPANT |
| 10.50 | Ki | 0.03162 | nM | HTL-0022562 |
| 10.49 | Ki | 0.032 | nM | HTL-0022562 |
| 10.40 | Ki | 0.04 | nM | CHEMBL2035981 |
| 10.40 | Ki | 0.04 | nM | CHEMBL3099918 |
| 10.40 | Ki | 0.03981 | nM | CHEMBL4635521 |
| 10.40 | Ki | 0.04 | nM | HTL-0022562 |
| 10.40 | Ki | 0.04 | nM | CHEMBL5997296 |
| 10.40 | Ki | 0.04 | nM | CHEMBL5747971 |
| 10.40 | Ki | 0.04 | nM | CHEMBL4635521 |
| 10.35 | IC50 | 0.045 | nM | CHEMBL4647045 |
| 10.33 | Ki | 0.047 | nM | CHEMBL2035983 |
| 10.30 | Ki | 0.05 | nM | CHEMBL3099931 |
| 10.30 | Ki | 0.05 | nM | CHEMBL3099925 |
| 10.26 | Ki | 0.055 | nM | CHEMBL3968568 |
| 10.24 | EC50 | 0.05754 | nM | CHEMBL5567377 |
| 10.20 | Ki | 0.0631 | nM | CHEMBL4640887 |
| 10.20 | Ki | 0.063 | nM | CHEMBL5907647 |
| 10.20 | Ki | 0.063 | nM | CHEMBL4640887 |
| 10.18 | Ki | 0.066 | nM | CHEMBL3890519 |
| 10.17 | Ki | 0.067 | nM | CHEMBL3944519 |
| 10.17 | Ki | 0.067 | nM | UBROGEPANT |
| 10.10 | Ki | 0.08 | nM | CHEMBL3099920 |
| 10.10 | Ki | 0.07943 | nM | CHEMBL4642755 |
| 10.10 | Ki | 0.07943 | nM | CHEMBL4649523 |
| 10.10 | Ki | 0.079 | nM | CHEMBL4642755 |
| 10.10 | Ki | 0.079 | nM | CHEMBL4649523 |
| 10.10 | Ki | 0.079 | nM | CHEMBL5916604 |
| 10.05 | Ki | 0.09 | nM | CHEMBL3099916 |
| 10.03 | Ki | 0.093 | nM | CHEMBL3971313 |
| 10.00 | IC50 | 0.1 | nM | OLCEGEPANT |
PubChem BioAssay actives
141 with measured affinity, of 168 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 |
|---|---|---|---|---|
| (3S)-3-[[(2S,3R)-2-[[(3S)-2-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]-3,4-dihydro-1H-isoquinoline-3-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 257877: Displacement of [3H-propionyl-K24] from halphaCGRP expressed in human neuroblastoma SK-N-MC cells | ki | <0.0001 | uM |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | <0.0001 | uM |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-2-oxospiro[1H-pyrido[2,3-d][1,3]oxazine-4,4’-piperidine]-1’-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | <0.0001 | uM |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | <0.0001 | uM |
| N-[(2S,5R,8R)-5-(2-cyanopropan-2-yl)-8-(4-fluoro-2-methylphenyl)-3-oxo-2,5,6,7-tetrahydro-1H-pyrrolizin-2-yl]-3-fluoro-5-methyl-4-[(3-methyl-6-oxo-1H-pyridazin-5-yl)oxy]benzamide | 1657084: Inhibition of human CLR/RAMP1 | ki | <0.0001 | uM |
| N-[2-[(2S,5R)-2-(2-cyanopropan-2-yl)-5-(3-methylphenyl)pyrrolidin-1-yl]-2-oxoethyl]-3-methyl-4-[(3-methyl-6-oxo-1H-pyridazin-5-yl)methyl]benzamide | 1657084: Inhibition of human CLR/RAMP1 | ki | <0.0001 | uM |
| N-[(2R)-1-[[(2S)-6-amino-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)hexan-2-yl]amino]-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | <0.0001 | uM |
| 4-[1-[5-[(2,6-dimethyl-4-pyridinyl)-methylamino]-4-[2-(2-methoxypropan-2-yl)-4-pyridinyl]-2-pyridinyl]piperidin-4-yl]-3,5-dihydro-1H-1,4-benzodiazepin-2-one | 1657093: Inhibition of human CLR/RAMP1 by cAMP assay | ic50 | <0.0001 | uM |
| N-[(2-cyclobutyl-6-methyl-4-pyridinyl)methyl]-5-[(1R)-1-[(3R)-3-methyl-2-oxo-1H-pyrrolo[2,3-b]pyridin-3-yl]ethyl]pyridine-2-carboxamide | 1657084: Inhibition of human CLR/RAMP1 | ki | <0.0001 | uM |
| (4S)-4-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(4R,7S,10S,13S,16S,19S,22R)-22-amino-16-(2-amino-2-oxoethyl)-7-[(1R)-1-hydroxyethyl]-10,19-bis(hydroxymethyl)-13-(2-methylpropyl)-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexazacyclotricosane-4-carbonyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S,3R)-1-[[2-[[(2S)-1-[[2-[[(2S,3R)-1-[(2S)-2-carbamoylpyrrolidin-1-yl]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid | 2085717: Agonist activity at human AMY1R complex of CTR/RAMP1 transduced in human HeLa cells by cAMP assay | ec50 | <0.0001 | uM |
| 2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| (3S)-3-[[(2S,3R)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 257877: Displacement of [3H-propionyl-K24] from halphaCGRP expressed in human neuroblastoma SK-N-MC cells | ki | <0.0001 | uM |
| (3S)-3-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-3-hydroxybutanoyl]amino]-4-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 257877: Displacement of [3H-propionyl-K24] from halphaCGRP expressed in human neuroblastoma SK-N-MC cells | ki | <0.0001 | uM |
| 2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| 2-[(8R)-8-(3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| N-[(2R)-1-[[(2S)-6-amino-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)hexan-2-yl]amino]-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxopropan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | <0.0001 | uM |
| 2-[(8R)-8-(4-chloro-3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| 2-[(8R)-8-(4-chloro-3,5-difluorophenyl)-8-methyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| Pramlintide | 2085717: Agonist activity at human AMY1R complex of CTR/RAMP1 transduced in human HeLa cells by cAMP assay | ec50 | <0.0001 | uM |
| 2-[(8R)-8-(3,5-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | <0.0001 | uM |
| Atogepant | 1657091: Antagonist activity at human CLR/RAMP1 | ki | <0.0001 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-2,2-dimethyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | <0.0001 | uM |
| (3S)-3-[[(2S,3R)-2-[[(2S,4R)-1-[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-methylbutanoyl]-4-hydroxypyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-oxobutanoic acid | 257877: Displacement of [3H-propionyl-K24] from halphaCGRP expressed in human neuroblastoma SK-N-MC cells | ki | <0.0001 | uM |
| N-[(3S,4R)-3-fluoro-1-(oxan-4-yl)piperidin-4-yl]-4-[[(4S)-4-methyl-2-oxopyrrolidin-1-yl]methyl]-3-[4-(6-propan-2-ylpyridazin-3-yl)phenoxy]benzamide | 1657093: Inhibition of human CLR/RAMP1 by cAMP assay | ic50 | <0.0001 | uM |
| (2S)-2-[[4-amino-3-chloro-5-(trifluoromethyl)phenyl]methyl]-1-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]-4-[4-(2-oxo-4,5-dihydro-1H-1,3-benzodiazepin-3-yl)piperidin-1-yl]butane-1,4-dione | 1657084: Inhibition of human CLR/RAMP1 | ic50 | 0.0001 | uM |
| N-[(2-cyclobutyl-6-methyl-4-pyridinyl)methyl]-4-[(1R)-1-[(3S)-3-methyl-2,5-dioxopyrrolidin-3-yl]ethyl]benzamide | 1657084: Inhibition of human CLR/RAMP1 | ki | 0.0001 | uM |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | 0.0001 | uM |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1H-quinolin-3-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | 0.0001 | uM |
| N-[(2R)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-[[(2S)-1-oxo-3-piperidin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-1,4-dihydroquinazolin-3-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | 0.0001 | uM |
| 2-[(2S,6R)-2-(3-chlorophenyl)-6-fluoro-4-oxo-1,8-dioxa-3-azaspiro[4.5]decan-3-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[c]pyridine]-3’-yl]acetamide | 1657084: Inhibition of human CLR/RAMP1 | ki | 0.0001 | uM |
| N-[(2R)-3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-[[(2S)-1-oxo-3-pyridin-4-yl-1-(4-pyridin-4-ylpiperazin-1-yl)propan-2-yl]amino]propan-2-yl]-4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | 1652728: Displacement of [3H]telcagepant from recombinant human CLR/RAMP1 expressed in Sf21 insect cell membranes measured after 60 mins by microbeta scintillation counting method | ki | 0.0001 | uM |
| (3S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S,3S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(4R,7S,10S,13S,16S,19R)-16-(2-amino-2-oxoethyl)-19-[[(2S)-2,6-diaminohexanoyl]amino]-7,13-bis[(1R)-1-hydroxyethyl]-10-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]propanoyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-4-oxobutanoic acid | 2085717: Agonist activity at human AMY1R complex of CTR/RAMP1 transduced in human HeLa cells by cAMP assay | ec50 | 0.0001 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]-1-(trifluoromethyl)cyclopropane-1-carboxamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| N-[(1R)-1-(3-fluoro-4-methylphenyl)ethyl]-2,2-dimethyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| Ubrogepant | 1657091: Antagonist activity at human CLR/RAMP1 | ki | 0.0001 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[(E)-3-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]prop-2-enyl]oxane-4-carboxamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| N-[(1R)-2,3-dihydro-1H-inden-1-yl]-2,2-dimethyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| N-[(1R)-2,3-dihydro-1H-inden-1-yl]-2,2-dimethyl-N-[3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-ynyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| 2,2-dimethyl-N-[3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-ynyl]-N-[(1R)-1-phenylethyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-3-methyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]thiophene-2-carboxamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0001 | uM |
| N-[(1R)-2,3-dihydro-1H-inden-1-yl]-2,2-dimethyl-N-[(E)-3-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]prop-2-enyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| 2,2-dimethyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]-N-[(1R)-1-phenylethyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| N-[(1R)-2,3-dihydro-1H-inden-1-yl]-2,2-dimethyl-N-[3-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]prop-2-ynyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-2,2-dimethyl-N-[3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]propyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-2,2-dimethyl-N-[(E)-3-[(2R)-2’-oxospiro[1,3-dihydroindene-2,3’-1H-pyrrolo[2,3-b]pyridine]-5-yl]prop-2-enyl]propanamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| N-[(1R)-1-(3,5-difluorophenyl)ethyl]-1-methyl-N-[(E)-3-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]prop-2-enyl]imidazole-2-carboxamide | 1061708: Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranes | ki | 0.0002 | uM |
| N-[(2R)-1-[[(2S)-6-amino-1-oxo-1-(4-pyridin-4-ylpiperazin-1-yl)hexan-2-yl]amino]-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxopropan-2-yl]-4-(2-oxo-3H-benzimidazol-1-yl)piperidine-1-carboxamide | 1657084: Inhibition of human CLR/RAMP1 | ic50 | 0.0002 | uM |
| (1S,10R,20E)-12-methyl-10-[(7-methyl-1H-indazol-5-yl)methyl]-15,18-dioxa-5,9,12,24,26-pentazapentacyclo[20.5.2.11,4.13,7.025,28]hentriaconta-3,5,7(30),20,22(29),23,25(28)-heptaene-8,11,27-trione | 1657084: Inhibition of human CLR/RAMP1 | ki | 0.0003 | uM |
| [(2R)-3-(4-hydroxy-3,5-dimethylphenyl)-1-(4-morpholin-4-ylpiperidin-1-yl)-1-oxopropan-2-yl] 4-(2-oxo-4,5-dihydro-1H-1,3-benzodiazepin-3-yl)piperidine-1-carboxylate | 1657084: Inhibition of human CLR/RAMP1 | ic50 | 0.0003 | uM |
| 2-[(8R)-8-(3,5-difluorophenyl)-8-ethyl-10-oxo-6,9-diazaspiro[4.5]decan-9-yl]-N-[(3S)-2-oxospiro[1H-pyrrolo[2,3-b]pyridine-3,6’-5,7-dihydrocyclopenta[b]pyridine]-3’-yl]acetamide | 665599: Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | ki | 0.0003 | uM |
CTD chemical–gene interactions
56 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | decreases expression, decreases methylation, affects cotreatment | 4 |
| Benzo(a)pyrene | decreases methylation, increases expression | 2 |
| Cyclophosphamide | increases expression, affects cotreatment, affects response to substance | 2 |
| Dexamethasone | increases expression, affects cotreatment, decreases expression | 2 |
| Doxorubicin | increases expression, affects cotreatment, affects response to substance | 2 |
| Fluorouracil | affects cotreatment, affects response to substance, decreases expression | 2 |
| Tetrachlorodibenzodioxin | increases expression | 2 |
| Valproic Acid | affects cotreatment, increases expression, decreases expression | 2 |
| pirinixic acid | affects binding, decreases expression, increases activity | 1 |
| deoxynivalenol | decreases expression | 1 |
| terbufos | increases methylation | 1 |
| trimellitic anhydride | decreases expression | 1 |
| sodium arsenite | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| nickel sulfate | increases expression | 1 |
| 1-nitropyrene | decreases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide | increases expression, affects cotreatment | 1 |
| dorsomorphin | affects cotreatment, increases expression | 1 |
| bisphenol S | affects cotreatment, decreases expression | 1 |
| NSC 689534 | affects binding, decreases expression | 1 |
| MT19c compound | decreases expression | 1 |
| Temozolomide | increases expression | 1 |
| Sunitinib | decreases expression | 1 |
| Air Pollutants | decreases expression, increases abundance | 1 |
| Arsenic | affects methylation | 1 |
| Atrazine | decreases expression | 1 |
| Cadmium | increases expression | 1 |
| Calcitriol | increases expression, affects cotreatment | 1 |
ChEMBL screening assays
43 unique, capped per target: 32 binding, 11 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2040005 | Binding | Displacement of [125I]CGRP from human recombinant CALCRL/RAMP1 receptor expressed in HEK293 cells after 3 hrs | MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. — Bioorg Med Chem Lett |
| CHEMBL4612975 | Functional | Antagonist activity at human CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-induced cAMP production preincubated for 30 mins followed by CGRP addition and measured after 30 mins by HTRF assay | Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2’-oxo-1’,2’-dihydrospiro[piperidine-4,4’-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine. — J Med Chem |
Cellosaurus cell lines
11 cell lines: 5 spontaneously immortalized cell line, 4 transformed cell line, 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_E4J2 | Genomeditech HEK-293 H_CALCRL+RAMP1 Reporter | Transformed cell line | Female |
| CVCL_H398 | CHO-K1/AMY1/CRE-Luc | Spontaneously immortalized cell line | Female |
| CVCL_H399 | CHO-K1/AMY1/Galpha15 | Spontaneously immortalized cell line | Female |
| CVCL_KA08 | CHO-K1/Galpha15/AMY1 | Spontaneously immortalized cell line | Female |
| CVCL_KU85 | cAMP Hunter CHO-K1 CALCRL-RAMP1 Gs | Spontaneously immortalized cell line | Female |
| CVCL_KW48 | PathHunter CHO-K1 CALCR-RAMP1 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_TI43 | HAP1 RAMP1 (-) 1 | Cancer cell line | Male |
| CVCL_TI44 | HAP1 RAMP1 (-) 2 | Cancer cell line | Male |
| CVCL_ZK45 | GeneBLAzer CALCRL:RAMP1-CRE-bla FreeStyle 293F | Transformed cell line | Female |
| CVCL_ZK46 | GeneBLAzer CALCRL:RAMP2-CRE-bla FreeStyle 293F | Transformed cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.