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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  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
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  • V1B receptor/Vasopressin V1b receptor in Human [ChEMBL: CHEMBL1921] [GtoPdb: 367] [UniProtKB: P47901]
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  • V2 receptor/Vasopressin V2 receptor in Human [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
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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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]