VNA932 [Ligand Id: 3537] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL363910 (VNA-932, WAY-VNA-932) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| OT receptor/Oxytocin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559] | ||||||||
| ChEMBL | Displacement of [3H]AVP from human oxytocin receptor expressed in CHO cells | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| ChEMBL | Displacement of [3H]-AVP from human OXR receptor expressed in CHO cell membranes by radioligand binding assay | B | 6.7 | pKi | 199 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Binding affinity to OTR receptor (unknown origin) | B | 6.9 | pKi | 125 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Displacement of [3H]oxytocin from human oxytocin receptor expressed in CHO cells | B | 6.45 | pIC50 | 353 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
| ChEMBL | Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 6.9 | pEC50 | 125 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536] | ||||||||
| ChEMBL | Antagonist activity at OXR receptor in rat uterus | F | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Binding affinity to V1A receptor (unknown origin) | B | 6.33 | pKi | 465 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells | B | 6.46 | pKi | 344 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| ChEMBL | Displacement of [3H]-AVP from human V1A receptor expressed in CHO cell membranes by radioligand binding assay | B | 6.46 | pKi | 344 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Antagonist activity at V1A receptor (unknown origin) by cAMP accumulation assay | F | 5.78 | pIC50 | 1660 | nM | IC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Displacement of [3H]AVP from human V1a receptor expressed in CHO cells | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
| ChEMBL | Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells | B | 6.11 | pIC50 | 778 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
| ChEMBL | Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 6.33 | pEC50 | 465 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| V1B receptor/Vasopressin V1b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901] | ||||||||
| ChEMBL | Binding affinity to V1B receptor (unknown origin) | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| ChEMBL | Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Binding affinity to V2 receptor (unknown origin) | B | 7.4 | pKi | 39.9 | nM | Ki | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
| ChEMBL | Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells | B | 7.1 | pIC50 | 80.3 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087] |
| ChEMBL | Displacement of [3H]AVP from human V2 receptor transfected in LV2 cells | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
| GtoPdb | - | - | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 954-9 [PMID:16297621] |
| ChEMBL | Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 7.4 | pEC50 | 39.9 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| ChEMBL | Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay | F | 9 | pEC50 | <1 | nM | EC50 | J Med Chem (2008) 51: 8124-8134 [PMID:19053774] |
| ChEMBL | Binding to human V2 receptor expressed in LV2 cells by cAMP production | F | 9.13 | pEC50 | 0.74 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 954-959 [PMID:16297621] |
| ChEMBL | Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Med Chem (2018) 61: 8670-8692 [PMID:30199637] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
