L-365,209 [Ligand Id: 2241] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL127686 (L-365209)
  • OT receptor in Human [GtoPdb: 369] [UniProtKB: P30559]
  • OT receptor/Oxytocin receptor in Rat [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536]
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  • V1A receptor/Vasopressin V1a receptor in Rat [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
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  • V2 receptor/Vasopressin V2 receptor in Rat [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
OT receptor in Human [GtoPdb: 369] [UniProtKB: P30559]
GtoPdb - - 8.5 pKi - - - Life Sci (1995) 57: 2253-61 [PMID:7475979]
OT receptor/Oxytocin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3996] [GtoPdb: 369] [UniProtKB: P70536]
ChEMBL Binding affinity towards rat uterine receptor was determined using [3H]oxytocin as radioligand B 8.14 pKi 7.3 nM Ki J Med Chem (1992) 35: 3905-3918 [PMID:1331448]
ChEMBL Inhibition of [3H]- oxytocin binding to rat uterine Oxytocin receptor B 8.14 pKi 7.3 nM Ki J Med Chem (1990) 33: 1843-1845 [PMID:2163451]
ChEMBL Concentration required to displace 50% of [3H]oxytocin from rat uterine receptor. B 7.74 pIC50 18 nM IC50 J Med Chem (1992) 35: 3905-3918 [PMID:1331448]
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
ChEMBL Binding affinity towards rat liver V1a receptor was determined using [3H]arginine vasopressin as radioligand B 6.43 pKi 370 nM Ki J Med Chem (1992) 35: 3905-3918 [PMID:1331448]
ChEMBL Concentration required to displace 50% of [3H]arginine vasopressin from rat liver arginine vasopressin 1A (AVP-V1a) site. B 5.89 pIC50 1300 nM IC50 J Med Chem (1992) 35: 3905-3918 [PMID:1331448]
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
ChEMBL Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand B 6.09 pKi 820 nM Ki J Med Chem (1992) 35: 3905-3918 [PMID:1331448]
ChEMBL Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor B 6.27 pKi 540 nM Ki J Med Chem (1990) 33: 1843-1845 [PMID:2163451]
ChEMBL Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla. B 5.64 pIC50 2300 nM IC50 J Med Chem (1992) 35: 3905-3918 [PMID:1331448]

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]