ChEMBL ligand: CHEMBL344159 (Jinarc, Jynarque, OPC-41061, OPC-41061(TOLVAPTAN), Samsca, Tolvaptan)
V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] V1A receptor in Rat [GtoPdb: 366] [UniProtKB: P30560] There should be some charts here, you may need to enable JavaScript!
V2 receptor/Vasopressin V2 receptor in Human [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] V2 receptor in Rat [GtoPdb: 368] [UniProtKB: Q00788] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL	Displacement of [3H]-vasopressin from human V1A receptor expressed in CHO cells membrane by microbeta scintillation counter analysis	B	6.53	pKi	296	nM	Ki	J Med Chem (2022) 65: 9295-9311 [PMID:35579344]
ChEMBL	Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay	B	7.49	pKi	32	nM	Ki	J Med Chem (2021) 64: 10445-10468 [PMID:34255509]
GtoPdb	-	-	7.9	pKi	-	-	-	J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL	Inhibition of human V1A receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescent plate reader	F	6.33	pIC50	470	nM	IC50	J Med Chem (2021) 64: 10445-10468 [PMID:34255509]
V1A receptor in Rat [GtoPdb: 366] [UniProtKB: P30560]
GtoPdb	-	-	6.5	pKi	-	-	-	J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL	Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay	B	8.62	pKi	2.4	nM	Ki	J Med Chem (2022) 65: 9295-9311 [PMID:35579344]
ChEMBL	Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay	B	8.77	pKi	1.7	nM	Ki	J Med Chem (2022) 65: 7717-7728 [PMID:35363466]
ChEMBL	Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay	B	9	pKi	1	nM	Ki	J Med Chem (2021) 64: 10445-10468 [PMID:34255509]
ChEMBL	Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%	B	9.37	pKi	0.43	nM	Ki	J Med Chem (2000) 43: 4388-4397 [PMID:11087564]
GtoPdb	-	-	9.37	pKi	0.43	nM	Ki	J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]
ChEMBL	Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins	F	7.95	pIC50	11.22	nM	IC50	J Med Chem (2022) 65: 7717-7728 [PMID:35363466]
V2 receptor in Rat [GtoPdb: 368] [UniProtKB: Q00788]
GtoPdb	-	-	8.9	pKi	-	-	-	J Pharmacol Exp Ther (1998) 287: 860-7 [PMID:9864265]

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]