VIPR2
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Also known as VPAC2VPAC2R
Summary
VIPR2 (vasoactive intestinal peptide receptor 2, HGNC:12695) is a protein-coding gene on chromosome 7q36.3, encoding Vasoactive intestinal polypeptide receptor 2 (P41587). G protein-coupled receptor activated by the neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (ADCYAP1/PACAP).
This gene encodes a receptor for vasoactive intestinal peptide, a small neuropeptide. Vasoactive intestinal peptide is involved in smooth muscle relaxation, exocrine and endocrine secretion, and water and ion flux in lung and intestinal epithelia. Its actions are effected through integral membrane receptors associated with a guanine nucleotide binding protein which activates adenylate cyclase.
Source: NCBI Gene 7434 — RefSeq curated summary.
At a glance
- GWAS associations: 12
- Clinical variants (ClinVar): 67 total
- Druggable target: yes — 2 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_003382
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:12695 |
| Approved symbol | VIPR2 |
| Name | vasoactive intestinal peptide receptor 2 |
| Location | 7q36.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | VPAC2, VPAC2R |
| Ensembl gene | ENSG00000106018 |
| Ensembl biotype | protein_coding |
| OMIM | 601970 |
| Entrez | 7434 |
Gene structure
Transcript identifiers
Ensembl transcripts: 9 — 9 protein_coding
ENST00000262178, ENST00000377633, ENST00000402066, ENST00000421760, ENST00000865374, ENST00000865375, ENST00000865376, ENST00000958129, ENST00000958130
RefSeq mRNA: 3 — MANE Select: NM_003382
NM_001304522, NM_001308259, NM_003382
CCDS: CCDS5950, CCDS78295
Canonical transcript exons
ENST00000262178 — 13 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000731012 | 159109812 | 159109919 |
| ENSE00000731015 | 159103757 | 159103854 |
| ENSE00000731018 | 159058481 | 159058578 |
| ENSE00000731020 | 159043035 | 159043176 |
| ENSE00000868045 | 159036752 | 159036902 |
| ENSE00000868046 | 159035952 | 159036012 |
| ENSE00000868047 | 159034581 | 159034650 |
| ENSE00000868048 | 159034213 | 159034304 |
| ENSE00000868049 | 159031938 | 159032067 |
| ENSE00000868051 | 159028175 | 159030789 |
| ENSE00001309515 | 159144721 | 159144867 |
| ENSE00002510971 | 159031828 | 159031869 |
| ENSE00003363471 | 159142446 | 159142545 |
Expression profiles
Bgee: expression breadth ubiquitous, 169 present calls, max score 89.68.
FANTOM5 (CAGE): breadth broad, TPM avg 1.1431 / max 54.9618, expressed in 347 samples.
FANTOM5 promoters (5 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 87127 | 0.6082 | 229 |
| 87130 | 0.2750 | 160 |
| 87129 | 0.1390 | 78 |
| 87128 | 0.1058 | 57 |
| 87126 | 0.0152 | 11 |
Top tissues by expression
279 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| mucosa of stomach | UBERON:0001199 | 89.68 | gold quality |
| apex of heart | UBERON:0002098 | 88.39 | gold quality |
| heart left ventricle | UBERON:0002084 | 85.82 | gold quality |
| body of pancreas | UBERON:0001150 | 85.81 | gold quality |
| cardiac ventricle | UBERON:0002082 | 85.45 | gold quality |
| endocervix | UBERON:0000458 | 84.69 | gold quality |
| esophagogastric junction muscularis propria | UBERON:0035841 | 84.10 | gold quality |
| parotid gland | UBERON:0001831 | 83.59 | gold quality |
| ascending aorta | UBERON:0001496 | 83.48 | gold quality |
| thoracic aorta | UBERON:0001515 | 83.47 | gold quality |
| aorta | UBERON:0000947 | 83.04 | gold quality |
| popliteal artery | UBERON:0002250 | 82.83 | gold quality |
| tibial artery | UBERON:0007610 | 82.83 | gold quality |
| descending thoracic aorta | UBERON:0002345 | 82.62 | gold quality |
| heart | UBERON:0000948 | 82.61 | gold quality |
| left ovary | UBERON:0002119 | 82.36 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 82.20 | gold quality |
| myocardium | UBERON:0002349 | 81.75 | gold quality |
| right atrium auricular region | UBERON:0006631 | 81.65 | gold quality |
| cardiac atrium | UBERON:0002081 | 81.17 | gold quality |
| parietal pleura | UBERON:0002400 | 80.77 | gold quality |
| right ovary | UBERON:0002118 | 79.82 | gold quality |
| triceps brachii | UBERON:0001509 | 79.47 | gold quality |
| omental fat pad | UBERON:0010414 | 79.28 | gold quality |
| peritoneum | UBERON:0002358 | 79.26 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 79.25 | silver quality |
| gluteal muscle | UBERON:0002000 | 79.19 | gold quality |
| lower esophagus muscularis layer | UBERON:0035833 | 78.98 | gold quality |
| sigmoid colon | UBERON:0001159 | 78.91 | gold quality |
| lower esophagus | UBERON:0013473 | 78.83 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-8498 | yes | 144.02 |
| E-ANND-3 | yes | 3.36 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
45 targeting VIPR2, 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-3613-3P | 100.00 | 76.36 | 7965 |
| HSA-MIR-188-3P | 100.00 | 68.76 | 1240 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-3692-3P | 99.98 | 70.27 | 2139 |
| HSA-MIR-507 | 99.97 | 70.11 | 1915 |
| HSA-MIR-557 | 99.96 | 70.01 | 1640 |
| HSA-MIR-6825-5P | 99.96 | 69.81 | 3431 |
| HSA-MIR-450B-5P | 99.92 | 71.48 | 3175 |
| HSA-MIR-589-3P | 99.91 | 69.62 | 2088 |
| HSA-MIR-153-5P | 99.89 | 73.86 | 6317 |
| HSA-MIR-6780A-5P | 99.88 | 66.69 | 2776 |
| HSA-MIR-4728-5P | 99.85 | 69.39 | 4718 |
| HSA-MIR-383-3P | 99.85 | 65.84 | 1359 |
| HSA-MIR-4447 | 99.85 | 67.81 | 2900 |
| HSA-MIR-6785-5P | 99.82 | 68.68 | 4428 |
| HSA-MIR-4713-5P | 99.78 | 67.80 | 1794 |
| HSA-MIR-3680-3P | 99.75 | 72.51 | 3095 |
| HSA-MIR-12130 | 99.75 | 65.47 | 452 |
| HSA-MIR-1827 | 99.63 | 68.57 | 3265 |
| HSA-MIR-4328 | 99.57 | 71.06 | 4094 |
| HSA-MIR-7106-5P | 99.53 | 67.47 | 3574 |
| HSA-MIR-190B-3P | 99.33 | 68.29 | 1382 |
| HSA-MIR-4311 | 99.31 | 70.47 | 3041 |
| HSA-MIR-6799-5P | 99.14 | 65.72 | 2093 |
| HSA-MIR-7160-5P | 99.11 | 67.17 | 2207 |
| HSA-MIR-670-3P | 99.03 | 68.88 | 2404 |
| HSA-MIR-3135B | 98.61 | 65.33 | 1470 |
| HSA-MIR-4768-3P | 98.16 | 66.02 | 2330 |
Literature-anchored findings (GeneRIF, showing 40)
- Detection of beta-galactosidase marker for human VPAC2/VIPR2 in cells withinin the suprachiasmatic nucleus (SCN) of transgenic mice indicates that VPAC2 may contribute to autoregulation and/or coupling within the SCN core and to control of the SCN shell. (PMID:15090046)
- analysis of a mutant form of VPAC2 shows its role in signaling and ligand binding (PMID:15302876)
- a novel recombinant agonist for VPAC2 is not active against PAC1 (PMID:16500728)
- The abnormal expression of VPCAP2-R mRNA in gallbladder tissue may play a role in the formation of gallbladder stones and gallbladder polyps (PMID:16552823)
- VPAC2-R mRNA was visualized only in the cerebellum of 7-22-year-old subjects. (PMID:16572459)
- splice variants may modify the immunoregulatory contributions of the VIP-VPAC2 axis (PMID:16888203)
- identification and characterization of novel five-transmembrane(5TM) isoforms of VPAC2 (PMID:16934434)
- altered expression of VPAC2 in activated CD4+ T cells derived from multiple sclerosis (MS) patients rendered CD4+ T cells less responsive to VIP and skewed the system to a predominantly T(h)1 direction. (PMID:17077178)
- Daily stimulation of VPAC2, but not VPAC1 or PAC1, resulted in up to 90% inhibition of X4 or R5 productive infections in either cell lines or PBMCs. (PMID:17257640)
- analysis of VIP 16gamma-glutamyl diamino derivative positive charges on hVPAC1 and hVPAC2 receptor function (PMID:17883247)
- VIP(Vasoactive intestinal peptide) expression was decreased in Rhematoid Arthritis (RA) synovial fibroblasts (FLS) compared with Osteoarthritis(OA) FLS;in RA FLS, VPAC2 (VIP receptor type 2) mediates the antiinflammatory effects of VIP (PMID:18383383)
- a novel mechanism of calmodulin in regulating PACAP signaling by possible interaction with the inactive state of PAC1 and VPAC2 receptors. (PMID:19269029)
- Results indicate that VPAC1, but not VPAC2 or PAC1, up-regulation in macrophages is a common mechanism in response to acute and chronic pro-inflammatory stimuli. (PMID:20026142)
- VPAC2 and/or PAC1 receptor activation is involved in cutaneous active vasodilation in humans. (PMID:20395540)
- VPAC(2) receptor presents an extranuclear localization and its protein expression is lower than that of VPAC(1) receptor in human breast tissue samples (PMID:20691743)
- increased expression in patients with allergic rhinitis (PMID:21711977)
- gene expression level and cAMP signaling of VIPR2 were increased in patients carrying 7q36.3 microduplications, thus implicating VIPR2 in the etiology of schizophrenia.[review] (PMID:21721910)
- mRNA expression of the VPAC1 receptor was detected in 51% of the tumor specimens, while the incidence of mRNA expression for VPAC2 was 46%. (PMID:21769421)
- The overexpression of VPAC1 and VPAC2 receptors and COX-2 in cancer tissue gives them a potential role as targets for diagnosis of prostate cancer. (PMID:22763881)
- PACAP causes PAC1/VPAC2 receptor mediated hypertension and sympathoexcitation in normal and hypertensive rats. (PMID:22886412)
- Conclude that VPAC2/PAC1 receptors require NO in series to effect cutaneous active vasodilation during heat stress in humans. (PMID:22961270)
- Genetic testing for VIPR2-LCR-associated inversions should be performed on available cohorts of psychiatric patients to evaluate their potential pathogenic role (PMID:23073313)
- This is the first study to suggest a role of VIPR2 in the genetic susceptibility to high myopia. EGR1, JUN, FOS and VIP are unlikely to be important in predisposing humans to high myopia. (PMID:23637909)
- Data indicate that VIP and PACAP increased macrophage resistance to HIV-1 replication by inducing the synthesis of beta-chemokines CCL3 and CCL5 and IL-10 following preferential activation of the receptors VPAC2 and PAC1. (PMID:23818986)
- CD4+ T cells in HIV infection show increased levels of expression of VPAC2 (PMID:24469917)
- This study suggest that carriers of microduplication genotypes of VIPR2 are predisposed to SCZ in Han Chinese. (PMID:24794882)
- Monocytes from Sjogren’s syndrome patients display increased vasoactive intestinal peptide receptor 2 expression and impaired apoptotic cell phagocytosis. (PMID:24827637)
- Lower CpG methylation of VIPR2 in the saliva of children with ADHD. (PMID:26304033)
- The results reveal that more severe inflammation, based on high levels of IL-6, is associated with lower expression of VPAC1 and, conversely, with increased expression of VPAC2. (PMID:26881970)
- The ‘CC’ genotype of the VIPR2 gene was nominally associated with an increased risk of SCZ in male Han Chinese patients. (PMID:27156032)
- In vitro-polarized macrophages by GM-CSF (GM-MO), with a proinflammatory profile, expressed higher levels of VIP receptors, vasoactive intestinal polypeptide receptors 1 and 2 (VPAC1 and VPAC2, respectively), than macrophages polarized by M-CSF (M-MO) with anti-inflammatory activities. RA synovial macrophages, according to their GM-CSF-like polarization state, expressed both VPAC1 and VPAC2. (PMID:27381006)
- a novel gene duplication syndrome (10q21.2q21.3 microduplication) and new evidence for VIPR2 duplication, as a candidate gene for autism, are reported. (PMID:27796743)
- Data suggest that VIPR2, which is a negative regulator of smooth muscle cell proliferation, might be a novel tumor suppressor gene in uterine leiomyosarcomas. (PMID:29063609)
- Activation of Th lymphocytes alters pattern expression and cellular location of VIP receptors in healthy donors and early arthritis patients. (PMID:31089161)
- Predictive Genes for the Prognosis of Central Serous Chorioretinopathy. (PMID:31331787)
- Study reports for a first time an association of a (3’ UTR) variant rs885863 in VIPR2 gene and opioid addiction. This single nucleotide polymorphism is an expression quantitative trait locus for VIPR2 and a long intergenic non-coding RNA, lincRNA 689. The study provides preliminary insight into the relationship between genetic variants in circadian rhythm genes and lincRNA in their vicinity, and opioid addiction. (PMID:31689297)
- The myopia susceptibility locus vasoactive intestinal peptide receptor 2 (VIPR2) contains variants with opposite effects. (PMID:31796800)
- Association of VIPR2 and ZMAT4 with high myopia. (PMID:32166996)
- Dysfunction of VIPR2 leads to myopia in humans and mice. (PMID:33318135)
- Identification of rare mutations of the vasoactive intestinal peptide receptor 2 gene in schizophrenia. (PMID:35353798)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | vipr2 | ENSDARG00000012353 |
| mus_musculus | Vipr2 | ENSMUSG00000011171 |
| rattus_norvegicus | Vipr2 | ENSRNOG00000004317 |
Paralogs (42): CALCR (ENSG00000004948), GIPR (ENSG00000010310), ADGRA2 (ENSG00000020181), CALCRL (ENSG00000064989), GLP2R (ENSG00000065325), ADGRF5 (ENSG00000069122), ADGRL1 (ENSG00000072071), ADCYAP1R1 (ENSG00000078549), SCTR (ENSG00000080293), CRHR2 (ENSG00000106113), GHRHR (ENSG00000106128), ADGRD1 (ENSG00000111452), GLP1R (ENSG00000112164), 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
Vasoactive intestinal polypeptide receptor 2 — P41587 (reviewed: P41587)
Alternative names: Helodermin-preferring VIP receptor, Pituitary adenylate cyclase-activating polypeptide type III receptor, VPAC2 receptor
All UniProt accessions (4): C9JCP7, E9PCR5, P41587, X5D7Q6
UniProt curated annotations — full annotation on UniProt →
Function. G protein-coupled receptor activated by the neuropeptides vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating polypeptide (ADCYAP1/PACAP). Binds VIP and both PACAP27 and PACAP38 bioactive peptides with the following order of potency PACAP38 = VIP > PACAP27. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. Activates cAMP-dependent pathway. May be coupled to phospholipase C.
Subunit / interactions. Interacts with ADCYAP1/PACAP (via N-terminal extracellular domain); activated by PACAP27 and CAPAC38 neuropeptides. Interacts with VIP; the interaction results in VIPR1 activation.
Subcellular location. Cell membrane.
Tissue specificity. Expressed in CD4+ T-cells, but not in CD8+ T-cells. Expressed in the T-cell lines Jurkat, Peer, MOLT-4, HSB, YT and SUP-T1, but not in the T-cell lines HARRIS and HuT 78.
Similarity. Belongs to the G-protein coupled receptor 2 family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P41587-1 | 1 | yes |
| P41587-2 | 2 |
RefSeq proteins (3): NP_001291451, NP_001295188, NP_003373* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000832 | GPCR_2_secretin-like | Family |
| IPR001571 | GPCR_2_VIP_rcpt | Family |
| IPR001879 | GPCR_2_extracellular_dom | Domain |
| IPR002284 | GPCR_2_VIP_rcpt_2 | Family |
| IPR017981 | GPCR_2-like_7TM | Domain |
| IPR017983 | GPCR_2_secretin-like_CS | Conserved_site |
| IPR036445 | GPCR_2_extracell_dom_sf | Homologous_superfamily |
| IPR047035 | VIP-R2_7TM | Domain |
| IPR050332 | GPCR_2 | Family |
Pfam: PF00002, PF02793
UniProt features (57 total): helix 16, topological domain 8, transmembrane region 7, strand 6, mutagenesis site 5, disulfide bond 4, glycosylation site 3, splice variant 2, sequence variant 2, signal peptide 1, chain 1, sequence conflict 1, turn 1
Structure
Experimental structures (PDB)
3 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2X57 | X-RAY DIFFRACTION | 2.1 |
| 7VQX | ELECTRON MICROSCOPY | 2.74 |
| 7WBJ | ELECTRON MICROSCOPY | 3.42 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P41587-F1 | 74.63 | 0.26 |
Antibody-complex structures (SAbDab): 2 — 7VQX, 7WBJ
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 (4): 38–61, 52–93, 75–109, 202–271
Glycosylation sites (3): 58, 88, 92
Mutagenesis-validated functional residues (5):
| Position | Phenotype |
|---|---|
| 79 | decreased adcyap1/pacap27 potency for vipr2. |
| 123 | decreased adcyap1/pacap27 potency for vipr2. |
| 184 | decreased adcyap1/pacap27 potency for vipr2. |
| 209 | increased adcyap1/pacap27 potency for vipr2. |
| 357 | decreased adcyap1/pacap27 potency for vipr2. |
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-418555 | G alpha (s) signalling events |
| R-HSA-420092 | Glucagon-type ligand receptors |
MSigDB gene sets: 112 (showing top):
REACTOME_GLUCAGON_TYPE_LIGAND_RECEPTORS, ROVERSI_GLIOMA_COPY_NUMBER_UP, GOBP_CELL_CELL_SIGNALING, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, MODULE_99, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, AACTTT_UNKNOWN, MORF_WNT1, GRYDER_PAX3FOXO1_ENHANCERS_IN_TADS, ACEVEDO_METHYLATED_IN_LIVER_CANCER_DN, IVANOVA_HEMATOPOIESIS_EARLY_PROGENITOR, YAGI_AML_WITH_11Q23_REARRANGED, RAAGNYNNCTTY_UNKNOWN, GRYDER_PAX3FOXO1_TOP_ENHANCERS
GO Biological Process (6): signal transduction (GO:0007165), cell surface receptor signaling pathway (GO:0007166), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), cell-cell signaling (GO:0007267), G protein-coupled receptor signaling pathway (GO:0007186)
GO Molecular Function (6): pituitary adenylate cyclase-activating polypeptide receptor activity (GO:0001634), G protein-coupled receptor activity (GO:0004930), vasoactive intestinal polypeptide receptor activity (GO:0004999), G protein-coupled peptide receptor activity (GO:0008528), peptide hormone binding (GO:0017046), transmembrane signaling receptor activity (GO:0004888)
GO Cellular Component (2): plasma membrane (GO:0005886), 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 |
|---|---|
| G protein-coupled receptor activity | 4 |
| cell communication | 2 |
| signaling | 2 |
| signal transduction | 2 |
| G protein-coupled receptor signaling pathway | 2 |
| cellular process | 1 |
| regulation of cellular process | 1 |
| cellular response to stimulus | 1 |
| adenylate cyclase activity | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase activator activity | 1 |
| transmembrane signaling receptor activity | 1 |
| peptide receptor activity | 1 |
| hormone binding | 1 |
| signaling receptor activity | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1198 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| VIPR2 | VIP | P01282 | 999 |
| VIPR2 | ADCYAP1 | P18509 | 998 |
| VIPR2 | PPIP5K2 | O43314 | 845 |
| VIPR2 | SCT | P09683 | 788 |
| VIPR2 | PER2 | O15055 | 773 |
| VIPR2 | RAMP1 | O60894 | 748 |
| VIPR2 | CRY1 | Q16526 | 744 |
| VIPR2 | RAMP2 | O60895 | 733 |
| VIPR2 | GRP | P07491 | 711 |
| VIPR2 | VIPR1 | P32241 | 710 |
| VIPR2 | GCG | P01275 | 620 |
| VIPR2 | NMU | P48645 | 606 |
| VIPR2 | PROK2 | Q9HC23 | 595 |
| VIPR2 | GHRH | P01286 | 570 |
| VIPR2 | RAMP3 | O60896 | 562 |
IntAct
18 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| VIPR2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP2 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| VIPR2 | RAMP3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP1 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| VIPR2 | Hacd3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| URM1 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| DBNDD2 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| RGS14 | VIPR2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| VIPR2 | C15orf61 | psi-mi:“MI:0914”(association) | 0.350 |
| VIPR2 | RABGAP1L | psi-mi:“MI:0914”(association) | 0.350 |
| VIPR2 | EI24 | psi-mi:“MI:0914”(association) | 0.350 |
| GPRC5C | PLAU | psi-mi:“MI:0914”(association) | 0.350 |
| VIPR2 | SLC33A1 | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (272): SNX17 (Affinity Capture-MS), RABGAP1 (Affinity Capture-MS), VPS8 (Affinity Capture-MS), PLIN3 (Affinity Capture-MS), VEZT (Affinity Capture-MS), CERS5 (Affinity Capture-MS), RABGAP1L (Affinity Capture-MS), SLC35F1 (Affinity Capture-MS), CDS1 (Affinity Capture-MS), PDS5B (Affinity Capture-MS), PDS5A (Affinity Capture-MS), ELOVL2 (Affinity Capture-MS), ORC5 (Affinity Capture-MS), CYP2S1 (Affinity Capture-MS), KIAA1524 (Affinity Capture-MS)
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
0 interactions.
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 13 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.
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| G protein-coupled receptor signaling pathway | 5 | 16.5× | 1e-04 |
Disease & clinical
Clinical variants and AI predictions
ClinVar
67 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 53 |
| Likely benign | 5 |
| Benign | 4 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3640 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 7:159031867:GCCC:G | acceptor_loss | 1.0000 |
| 7:159031869:CCT:C | acceptor_loss | 1.0000 |
| 7:159031870:CTGCA:C | acceptor_loss | 1.0000 |
| 7:159031871:T:C | acceptor_loss | 1.0000 |
| 7:159034211:A:AC | donor_gain | 1.0000 |
| 7:159034212:C:CC | donor_gain | 1.0000 |
| 7:159034651:C:CC | acceptor_gain | 1.0000 |
| 7:159035818:T:TA | donor_gain | 1.0000 |
| 7:159036748:TTAC:T | donor_loss | 1.0000 |
| 7:159036749:TACCC:T | donor_loss | 1.0000 |
| 7:159036750:A:AC | donor_gain | 1.0000 |
| 7:159036750:A:C | donor_loss | 1.0000 |
| 7:159036750:AC:A | donor_gain | 1.0000 |
| 7:159036750:ACC:A | donor_gain | 1.0000 |
| 7:159036751:C:CC | donor_gain | 1.0000 |
| 7:159036751:CC:C | donor_gain | 1.0000 |
| 7:159036751:CCC:C | donor_gain | 1.0000 |
| 7:159036751:CCCCA:C | donor_gain | 1.0000 |
| 7:159036904:T:A | acceptor_loss | 1.0000 |
| 7:159036911:C:CT | acceptor_gain | 1.0000 |
| 7:159036911:C:T | acceptor_gain | 1.0000 |
| 7:159103752:CCTA:C | donor_loss | 1.0000 |
| 7:159103755:ACCT:A | donor_loss | 1.0000 |
| 7:159103756:C:A | donor_loss | 1.0000 |
| 7:159109920:C:CC | acceptor_gain | 1.0000 |
| 7:159142556:T:C | acceptor_gain | 1.0000 |
| 7:159031822:ACTT:A | donor_loss | 0.9900 |
| 7:159031823:CTTAC:C | donor_loss | 0.9900 |
| 7:159031825:T:TG | donor_loss | 0.9900 |
| 7:159031826:A:C | donor_loss | 0.9900 |
AlphaMissense
2849 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 7:159103820:C:A | W98C | 1.000 |
| 7:159103820:C:G | W98C | 1.000 |
| 7:159034644:C:A | W272C | 0.999 |
| 7:159034644:C:G | W272C | 0.999 |
| 7:159103822:A:G | W98R | 0.999 |
| 7:159103822:A:T | W98R | 0.999 |
| 7:159103836:C:G | C93S | 0.999 |
| 7:159103837:A:T | C93S | 0.999 |
| 7:159109885:C:A | W62C | 0.999 |
| 7:159109885:C:G | W62C | 0.999 |
| 7:159109903:C:A | W56C | 0.999 |
| 7:159109903:C:G | W56C | 0.999 |
| 7:159034646:A:G | W272R | 0.998 |
| 7:159034646:A:T | W272R | 0.998 |
| 7:159103835:A:C | C93W | 0.997 |
| 7:159109847:C:G | C75S | 0.997 |
| 7:159109848:A:T | C75S | 0.997 |
| 7:159109887:A:G | W62R | 0.997 |
| 7:159109887:A:T | W62R | 0.997 |
| 7:159109889:C:G | C61S | 0.997 |
| 7:159109890:A:T | C61S | 0.997 |
| 7:159034648:C:G | C271S | 0.996 |
| 7:159034649:A:T | C271S | 0.996 |
| 7:159035986:A:G | W259R | 0.996 |
| 7:159035986:A:T | W259R | 0.996 |
| 7:159036755:A:G | W249R | 0.996 |
| 7:159036755:A:T | W249R | 0.996 |
| 7:159058538:C:T | G133D | 0.996 |
| 7:159103836:C:T | C93Y | 0.996 |
| 7:159103837:A:G | C93R | 0.996 |
dbSNP variants (sampled 300 via entrez): RS1000030277 (7:159037319 A>G), RS1000040364 (7:159037632 A>G), RS1000056135 (7:159073754 C>T), RS1000062169 (7:159075767 C>A,T), RS1000086988 (7:159073576 C>T), RS1000105836 (7:159114323 C>T), RS1000122440 (7:159094707 G>A), RS1000174701 (7:159051662 C>G,T), RS1000181647 (7:159083673 C>T), RS1000203087 (7:159085426 G>A), RS1000243459 (7:159109783 A>C), RS1000281732 (7:159040275 C>T), RS1000286955 (7:159052715 A>G), RS1000341746 (7:159063613 C>A,T), RS1000380214 (7:159131182 G>A)
Disease associations
OMIM: gene MIM:601970 | disease phenotypes:
GenCC curated gene-disease
Mondo (1): myoepithelial tumor (MONDO:0002380)
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
12 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST001881_4 | Myopia (pathological) | 9.000000e-14 |
| GCST006068_2 | Sub-foveal choroidal thickness | 7.000000e-08 |
| GCST006291_101 | Spherical equivalent or myopia (age of diagnosis) | 5.000000e-08 |
| GCST006291_75 | Spherical equivalent or myopia (age of diagnosis) | 5.000000e-10 |
| GCST007159_26 | Corneal astigmatism | 3.000000e-06 |
| GCST010002_267 | Refractive error | 2.000000e-37 |
| GCST010256_1 | Diastolic blood pressure x quantitative lifestyle risk score interaction (2df test) | 3.000000e-07 |
| GCST010257_1 | Diastolic blood pressure x quantitative lifestyle risk score interaction (1df test) | 1.000000e-07 |
| GCST010397_49 | Gut microbiota (bacterial taxa, rank normal transformation method) | 3.000000e-06 |
| GCST011358_4 | Academic attainment (English) | 8.000000e-06 |
| GCST011920_2 | Hearing loss in noise exposure | 2.000000e-06 |
| GCST012490_559 | Femur bone mineral density x serum urate levels interaction | 9.000000e-12 |
EFO canonical traits (9, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004207 | pathological myopia |
| EFO:0009281 | choroidal thickness measurement |
| EFO:0004847 | age at onset |
| EFO:1002040 | Corneal astigmatism |
| EFO:0006336 | diastolic blood pressure |
| EFO:0010724 | lifestyle measurement |
| EFO:0007874 | gut microbiome measurement |
| EFO:0011015 | educational attainment |
| EFO:0004531 | urate measurement |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D009208 | Myoepithelioma | C04.557.435.585 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL4524128 (PROTEIN FAMILY), CHEMBL4532 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 830 (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 |
|---|---|---|---|
| CHEMBL1981592 | AVIPTADIL | 3 | 623 |
| CHEMBL1933349 | MK-0893 | 2 | 207 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: gpcr — VIP and PACAP receptors
Most potent curated ligand interactions (19 total), top 19:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| [125I]VIP (human, mouse, rat) | Agonist | 9.2 | pKd |
| [125I]BAY 55-9837 | Agonist | 9.2 | pKd |
| N-stearyl-[Nle17]VIP | Agonist | 9.0 | pIC50 |
| helodermin | Agonist | 8.5 | pIC50 |
| Ro 25-1553 | Agonist | 8.3 | pEC50 |
| PHV | Agonist | 8.0 | pIC50 |
| Ro 25-1392 | Agonist | 8.0 | pKi |
| PACAP-38 | Agonist | 7.7 | pEC50 |
| PACAP-27 | Agonist | 7.6 | pEC50 |
| PG 99-465 | Partial agonist | 7.6 | pIC50 |
| PHI | Agonist | 7.5 | pIC50 |
| VIP | Agonist | 7.3 | pEC50 |
| N-stearyl-[Nle17] neurotensin-(6-11)/VIP-(7-28) | Antagonist | 7.3 | pIC50 |
| BAY 55-9837 | Agonist | 7.2 | pIC50 |
| PG 97-269 | Antagonist | 5.5 | pIC50 |
| secretin | Agonist | 5.3 | pIC50 |
| [Arg16]chicken secretin | Agonist | 5.3 | pIC50 |
| [Ala11,22,28]VIP | Agonist | 5.0 | pEC50 |
| [Lys15,Arg16,Leu27]VIP-(1-7)/GRF-(8-27)-NH2 | Agonist | 4.5 | pIC50 |
Binding affinities (BindingDB)
6 measured of 6 human assays (28 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| VIP Ala9 | KI | 0.29 nM |
| VIP Ala19 | KI | 0.59 nM |
| NSC_0 | KI | 1.7 nM |
| VIP Ala15 | KI | 2.1 nM |
| CAS_150828-75-4 | KI | 3.4 nM |
| Ac-L-His-L-Ser-L-Asp-L-Ala-L-Val-L-Phe-L-Thr-L-Glu-L-Asn-L-Tyr-L-Thr-L-Lys-L-Leu-L-Arg-L-Lys-L-Gln-L-Nle-L-Ala-L-Ala-L-Lys-L-Lys(1)-L-Tyr-L-Leu-L-Asn-L-Asp(1)-L-Leu-L-Lys-L-Lys-Gly-Gly-L-Thr-NH2 | KI | 1020 nM |
ChEMBL bioactivities
81 potent at pChembl≥5 of 86 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.31 | EC50 | 0.049 | nM | CHEMBL3102930 |
| 10.22 | EC50 | 0.06 | nM | CHEMBL5220770 |
| 10.11 | EC50 | 0.07845 | nM | CHEMBL4294827 |
| 10.10 | EC50 | 0.08 | nM | CHEMBL1893324 |
| 10.06 | EC50 | 0.087 | nM | CHEMBL219499 |
| 10.00 | EC50 | 0.1 | nM | CHEMBL3102924 |
| 9.96 | EC50 | 0.11 | nM | CHEMBL3102925 |
| 9.85 | EC50 | 0.14 | nM | CHEMBL3102919 |
| 9.74 | EC50 | 0.1804 | nM | CHEMBL4277441 |
| 9.72 | EC50 | 0.19 | nM | AVIPTADIL |
| 9.68 | EC50 | 0.21 | nM | CHEMBL3102929 |
| 9.68 | EC50 | 0.21 | nM | CHEMBL3102922 |
| 9.48 | EC50 | 0.33 | nM | CHEMBL3102931 |
| 9.42 | EC50 | 0.38 | nM | CHEMBL3102921 |
| 9.41 | EC50 | 0.39 | nM | CHEMBL3105020 |
| 9.38 | EC50 | 0.422 | nM | CHEMBL4291119 |
| 9.28 | EC50 | 0.5286 | nM | CHEMBL4277799 |
| 9.23 | EC50 | 0.5928 | nM | CHEMBL4285873 |
| 9.22 | EC50 | 0.6 | nM | CHEMBL440082 |
| 9.19 | EC50 | 0.646 | nM | CHEMBL4282016 |
| 9.09 | EC50 | 0.8162 | nM | CHEMBL4281547 |
| 9.07 | EC50 | 0.8586 | nM | CHEMBL4277870 |
| 9.02 | EC50 | 0.9629 | nM | CHEMBL4294951 |
| 8.99 | EC50 | 1.018 | nM | CHEMBL4289726 |
| 8.94 | EC50 | 1.16 | nM | CHEMBL3102923 |
| 8.93 | EC50 | 1.166 | nM | CHEMBL4291903 |
| 8.90 | EC50 | 1.266 | nM | CHEMBL4286419 |
| 8.90 | EC50 | 1.258 | nM | CHEMBL4276843 |
| 8.88 | EC50 | 1.334 | nM | CHEMBL4282364 |
| 8.86 | EC50 | 1.37 | nM | CHEMBL3102926 |
| 8.86 | EC50 | 1.372 | nM | CHEMBL4283432 |
| 8.83 | EC50 | 1.49 | nM | CHEMBL3102927 |
| 8.82 | EC50 | 1.52 | nM | CHEMBL3105019 |
| 8.46 | EC50 | 3.472 | nM | CHEMBL4284858 |
| 8.45 | EC50 | 3.515 | nM | CHEMBL4287451 |
| 8.42 | EC50 | 3.8 | nM | CHEMBL3102928 |
| 8.35 | IC50 | 4.5 | nM | CHEMBL5219662 |
| 8.25 | EC50 | 5.579 | nM | CHEMBL4278228 |
| 8.18 | EC50 | 6.6 | nM | CHEMBL3102920 |
| 7.99 | IC50 | 10.23 | nM | CHEMBL524852 |
| 7.89 | IC50 | 13 | nM | CHEMBL219499 |
| 7.64 | IC50 | 22.91 | nM | CHEMBL507480 |
| 7.57 | IC50 | 27 | nM | CHEMBL440082 |
| 7.44 | IC50 | 36.31 | nM | CHEMBL3736134 |
| 7.44 | IC50 | 36 | nM | CHEMBL3736134 |
| 7.30 | EC50 | 50.25 | nM | CHEMBL4281905 |
| 7.28 | IC50 | 53 | nM | CHEMBL3736230 |
| 7.27 | IC50 | 53.7 | nM | CHEMBL3736230 |
| 7.10 | EC50 | 79.64 | nM | CHEMBL4280734 |
| 7.02 | EC50 | 95.59 | nM | CHEMBL4284961 |
PubChem BioAssay actives
32 with measured affinity, of 61 total; 28 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 |
|---|---|---|---|---|
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,5S,8S,11S,16Z,22S)-22-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-(4-aminobutyl)-8-(3-amino-3-oxopropyl)-2-(3-carbamimidamidopropyl)-11,22-dimethyl-3,6,9,23-tetraoxo-1,4,7,10-tetrazacyclotricos-16-ene-11-carbonyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | <0.0001 | uM |
| (3S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1,4-diamino-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1915942: Agonist activity at VPAC2 in human SH-SY5Y cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | ec50 | 0.0001 | uM |
| (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]acetyl]amino]-3-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoic acid | 274566: Activity at human VPAC2 receptor in CHO cells by measuring cAMP accumulation | ec50 | 0.0001 | uM |
| (3S)-4-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1915942: Agonist activity at VPAC2 in human SH-SY5Y cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | ec50 | 0.0001 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,5S,8S,11S,20S)-20-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-8-(4-aminobutyl)-2-methyl-3,6,9,17,21-pentaoxo-5-propan-2-yl-1,4,7,10,16-pentazacyclohenicosane-11-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0001 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S,5S,8S,11S,20S)-20-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-8-(2-amino-2-oxoethyl)-2-[(4-hydroxyphenyl)methyl]-5-(2-methylpropyl)-3,6,9,17,21-pentaoxo-1,4,7,10,16-pentazacyclohenicosane-11-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0001 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0001 | uM |
| (2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0002 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-2-methylhept-6-enoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-2-methylhept-6-enoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0002 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0002 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,5S,8S,11S,16Z,22S)-22-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-8-(4-aminobutyl)-2,11,22-trimethyl-3,6,9,23-tetraoxo-5-propan-2-yl-1,4,7,10-tetrazacyclotricos-16-ene-11-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0003 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0004 | uM |
| (2S)-6-amino-2-[[2-[[(2S,5S,8S,11S,16Z,22S)-22-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-5-[(2S)-butan-2-yl]-2-(hydroxymethyl)-11,22-dimethyl-8-(2-methylpropyl)-3,6,9,23-tetraoxo-1,4,7,10-tetrazacyclotricos-16-ene-11-carbonyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0004 | uM |
| (3S)-3-[[(2S)-2-[[(2S)-2-acetamido-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-5-carbamimidamido-1-[[(2S)-1-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoic acid | 274566: Activity at human VPAC2 receptor in CHO cells by measuring cAMP accumulation | ec50 | 0.0006 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,5S,8S,11S,20S)-20-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-(4-aminobutyl)-8-(3-amino-3-oxopropyl)-2-(3-carbamimidamidopropyl)-3,6,9,17,21-pentaoxo-1,4,7,10,16-pentazacyclohenicosane-11-carbonyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0012 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-2-methylhept-6-enoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-2-methylhept-6-enoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0014 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-2-methylhept-6-enoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-2-methylhept-6-enoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0015 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S,5S,8S,11S,16Z,22S)-22-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-8-(2-amino-2-oxoethyl)-2-[(4-hydroxyphenyl)methyl]-11,22-dimethyl-5-(2-methylpropyl)-3,6,9,23-tetraoxo-1,4,7,10-tetrazacyclotricos-16-ene-11-carbonyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0015 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-2-methylhept-6-enoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-2-methylhept-6-enoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0038 | uM |
| (2S)-6-amino-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-sulfanylbutanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]hexanoic acid | 1915945: Antagonist activity at VPAC2 in human SH-SY5Y cells assessed as inhibition of PACAP38-induced cAMP accumulation pre-incubated for 30 mins followed by agonist addition and measured after 75 mins by Eu-cAMP tracer based LANCE ultra cAMP assay | ic50 | 0.0045 | uM |
| (2S)-6-amino-2-[[2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]propanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]acetyl]amino]hexanoic acid | 1062174: Agonist activity at human VPAC2 expressed in CHO Flp-in cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay | ec50 | 0.0066 | uM |
| (3S)-4-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1261358: Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ic50 | 0.0102 | uM |
| (3S)-4-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-(4-phenylphenyl)propan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1261358: Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ic50 | 0.0229 | uM |
| (3S)-4-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-[4-[2-(4-fluorophenyl)ethynyl]phenyl]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1261358: Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ic50 | 0.0360 | uM |
| (3S)-4-[[2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-[4-(2-phenylethynyl)phenyl]propan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoic acid | 1261358: Displacement of Ac-[125I]-PACAP27 from recombinant human VPAC2 expressed in CHO cells after 90 mins by gamma counting analysis | ic50 | 0.0530 | uM |
| 3-[[4-[(1S)-1-[3-(3,4-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid | 693739: Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ic50 | 1.7000 | uM |
| 3-[[4-[(1S)-1-[3-(2,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid | 693739: Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ic50 | 2.6000 | uM |
| 3-[[4-[(1S)-1-[3-[3-chloro-5-(trifluoromethyl)phenyl]-5-(6-methoxynaphthalen-2-yl)pyrazol-1-yl]ethyl]benzoyl]amino]propanoic acid | 693739: Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter | ic50 | 2.6000 | uM |
CTD chemical–gene interactions
22 total (human), top 22 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| bisphenol A | decreases methylation, increases expression | 2 |
| Tobacco Smoke Pollution | decreases expression, increases methylation | 2 |
| Valproic Acid | affects expression, decreases methylation | 2 |
| Aflatoxin B1 | decreases methylation, increases methylation | 2 |
| sulforaphane | decreases expression | 1 |
| benzo(e)pyrene | increases methylation | 1 |
| aflatoxin B2 | increases methylation | 1 |
| Olanzapine | affects expression | 1 |
| Amisulpride | decreases expression | 1 |
| Acetaminophen | decreases expression | 1 |
| Cyclic AMP | affects binding, increases abundance | 1 |
| Ethanol | affects cotreatment, increases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Doxorubicin | affects expression | 1 |
| Estradiol | decreases expression | 1 |
| Folic Acid | affects cotreatment, increases expression | 1 |
| Haloperidol | decreases expression | 1 |
| Methapyrilene | increases methylation | 1 |
| Tetradecanoylphorbol Acetate | affects cotreatment, affects expression | 1 |
| Tunicamycin | increases expression | 1 |
| Zinc | affects cotreatment, affects expression | 1 |
| Thapsigargin | increases expression | 1 |
ChEMBL screening assays
27 unique, capped per target: 14 functional, 13 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4880302 | Binding | Vasoactive intestinal peptide receptor CEREP ligand profiling | Data for DCP probe ABT-546 |
| CHEMBL2160805 | Functional | Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillati | Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes. — J Med Chem |
Cellosaurus cell lines
11 cell lines: 6 spontaneously immortalized cell line, 3 cancer cell line, 1 transformed cell line, 1 induced pluripotent stem cell
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C0TW | ACTOne VIPR2 | Transformed cell line | Female |
| CVCL_E0SX | Ubigene HeLa VIPR2 KO | Cancer cell line | Female |
| CVCL_E4PY | KOLF2.1J VIPR2 72.1kbdel DEL/DEL | Induced pluripotent stem cell | Male |
| CVCL_H492 | CHO-K1/PAC1/Galpha15 | Spontaneously immortalized cell line | Female |
| CVCL_H511 | CHO-K1/VPAC2/Galpha15 | Spontaneously immortalized cell line | Female |
| CVCL_KA21 | CHO-K1/CRE-Luc/VPAC2 | Spontaneously immortalized cell line | Female |
| CVCL_KV89 | cAMP Hunter CHO-K1 VIPR2 Gs | Spontaneously immortalized cell line | Female |
| CVCL_KZ25 | PathHunter CHO-K1 VIPR2 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_LB48 | PathHunter U2OS VIPR2 Total GPCR Internalization | Cancer cell line | Female |
| CVCL_YK66 | U2OS VIPR2 cAMP-Nomad | Cancer cell line | Female |
Clinical trials (associated diseases)
5 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT03600649 | PHASE1 | UNKNOWN | Clinical Trial of SP-2577 (Seclidemstat) in Patients With Relapsed or Refractory Ewing or Ewing-related Sarcomas |
| NCT05266196 | PHASE1/PHASE2 | UNKNOWN | A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) |
| NCT06239272 | PHASE1/PHASE2 | RECRUITING | NRSTS2021, A Risk Adapted Study Evaluating Maintenance Pazopanib, Limited Margin, Dose-Escalated Radiation Therapy and Selinexor in Non-Rhabdomyosarcoma Soft Tissue Sarcoma (NRSTS) |
| NCT06625190 | PHASE1/PHASE2 | RECRUITING | Alpha/Beta T and B Cell Depletion With Zoledronic Acid for Solid Tumors |
| NCT06244420 | Not specified | COMPLETED | Malignant Myoepithelioma of Bone and Soft Tissues: Diagnostic Imaging and Histology in Relation to Prognosis |
Related Atlas pages
- Targeted by drugs: Secretin
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): myoepithelial tumor, noise induced hearing loss, refractive error