LS-192629 [Ligand Id: 2192] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1254024
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  • V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
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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]-oxytocin from human oxytocin receptor expressed in CHO cells B 7.55 pKi 28 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue B 7.55 pKi 28 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
GtoPdb - - 7.8 pKi - - - J Pharmacol Exp Ther (2003) 306: 253-61 [PMID:12660315]
OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536]
ChEMBL Antagonist activity at oxytocin receptor in rat uterine strips assessed as inhibition of oxytocin-induced contraction F 7.8 pKd 15.85 nM Kd J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
ChEMBL Displacement of [3H]-oxytocin from rat oxytocin receptor expressed in CHO cells B 6.87 pKi 135 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
GtoPdb - - 6.9 pKi - - - J Pharmacol Exp Ther (2003) 306: 253-61 [PMID:12660315]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
GtoPdb - - 6.7 pKi - - - J Pharmacol Exp Ther (2003) 306: 253-61 [PMID:12660315]
ChEMBL Displacement of [3H]vasopressin from human vasopressin V1a receptor expressed in CHO cells B 6.77 pKi 170 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells B 5 pKi >10000 nM Ki J Med Chem (2010) 53: 6525-6538 [PMID:20550119]

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]