ChEMBL ligand: CHEMBL49429 (CRTX 080, CRTX-080, CRTX080, Lixar, Lixivaptan, Vpa-985, VPA 985, VPA-985, VPA985, WAY-VPA-985)
OT receptor/Oxytocin receptor in Human [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559] There should be some charts here, you may need to enable JavaScript!
V1A receptor/Vasopressin V1a receptor in Human [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] V1A receptor/Vasopressin V1a receptor in Rat [ChEMBL: CHEMBL2868] [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/Vasopressin V2 receptor in Rat [ChEMBL: CHEMBL3766] [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
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	6.28	pIC50	519	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087]
V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288]
ChEMBL	Inhibition of 1 nM AVP-induced calcium mobilisation in cells expressing human vasopressin V1a receptor	B	5.22	pKi	6000	nM	Ki	Bioorg Med Chem Lett (2004) 14: 2747-2752 [PMID:15125926]
ChEMBL	Inhibition of [3H]AVP binding to recombinant human vasopressin V1a receptor	B	7.36	pKi	44	nM	Ki	Bioorg Med Chem Lett (2004) 14: 2747-2752 [PMID:15125926]
ChEMBL	Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level	F	5.3	pIC50	>5000	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6623-6628 [PMID:17942308]
ChEMBL	Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.	B	6.64	pIC50	230	nM	IC50	J Med Chem (1998) 41: 2442-2444 [PMID:9651149]
ChEMBL	In vitro inhibition of [3H]- AVP binding to V1a receptor from human platelet membrane	B	6.64	pIC50	230	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1733-1736 [PMID:10406632]
ChEMBL	In vitro binding affinity to human V1a receptor	B	6.64	pIC50	230	nM	IC50	Bioorg Med Chem Lett (2000) 10: 695-698 [PMID:10782666]
ChEMBL	Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor	B	6.74	pIC50	180	nM	IC50	Bioorg Med Chem Lett (2005) 15: 5003-5006 [PMID:16153837]
ChEMBL	Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor	B	6.82	pIC50	150	nM	IC50	Bioorg Med Chem Lett (2002) 12: 3081-3084 [PMID:12372506]
ChEMBL	Binding affinity towards human V1a receptors	B	6.82	pIC50	150	nM	IC50	Bioorg Med Chem Lett (2003) 13: 753-756 [PMID:12639574]
ChEMBL	Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells	B	6.82	pIC50	150	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6623-6628 [PMID:17942308]
ChEMBL	Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells	B	6.91	pIC50	124	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087]
V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560]
ChEMBL	Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.	B	6.39	pIC50	410	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2195-2198 [PMID:12798333]
ChEMBL	In vitro binding affinity for rat V1a receptor	B	6.47	pIC50	340	nM	IC50	Bioorg Med Chem Lett (2000) 10: 695-698 [PMID:10782666]
ChEMBL	Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.	B	6.47	pIC50	340	nM	IC50	J Med Chem (1998) 41: 2442-2444 [PMID:9651149]
ChEMBL	Displacement of (Phe-3,4,5 [3H]-) AVP from isolated rat hepatic V1a receptor	B	7.09	pIC50	82	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1737-1740 [PMID:10406633]
V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518]
ChEMBL	Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells	B	7.05	pKi	90	nM	Ki	Bioorg Med Chem Lett (2002) 12: 3081-3084 [PMID:12372506]
ChEMBL	Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor	F	7.64	pKi	23	nM	Ki	Bioorg Med Chem Lett (2004) 14: 2747-2752 [PMID:15125926]
ChEMBL	Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor	B	8.64	pKi	2.3	nM	Ki	Bioorg Med Chem Lett (2004) 14: 2747-2752 [PMID:15125926]
GtoPdb	-	-	9.2	pKi	-	-	Ki	Kidney Int (2000) 58: 1613-22 [PMID:11012895]; J Med Chem (1998) 41: 2442-4 [PMID:9651149]
ChEMBL	Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels	F	7.04	pIC50	91	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6623-6628 [PMID:17942308]
ChEMBL	Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.	F	7.04	pIC50	91	nM	IC50	Bioorg Med Chem Lett (2003) 13: 753-756 [PMID:12639574]
ChEMBL	Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2002) 12: 3081-3084 [PMID:12372506]
ChEMBL	Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.	F	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2003) 13: 753-756 [PMID:12639574]
ChEMBL	Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells	B	8.3	pIC50	5	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6623-6628 [PMID:17942308]
ChEMBL	In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1733-1736 [PMID:10406632]
ChEMBL	Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2000) 10: 783-786 [PMID:10782686]
ChEMBL	In vitro binding affinity to human V2 receptor	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2000) 10: 695-698 [PMID:10782666]
ChEMBL	Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes	B	8.92	pIC50	1.2	nM	IC50	J Med Chem (1998) 41: 2442-2444 [PMID:9651149]
ChEMBL	Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells	B	8.92	pIC50	1.2	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5796-5800 [PMID:17855087]
ChEMBL	Inhibition of [3H]-AVP binding to human V2 receptor	B	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (2005) 15: 5003-5006 [PMID:16153837]
V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788]
ChEMBL	Binding affinity to rat V2 receptor	B	8.64	pIC50	2.3	nM	IC50	Bioorg Med Chem Lett (2000) 10: 695-698 [PMID:10782666]
ChEMBL	Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.	B	8.64	pIC50	2.3	nM	IC50	Bioorg Med Chem Lett (2003) 13: 2195-2198 [PMID:12798333]
ChEMBL	Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (1998) 41: 2442-2444 [PMID:9651149]
ChEMBL	Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1737-1740 [PMID:10406633]

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]