lixivaptan [Ligand Id: 2238] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL49429 (CRTX 080, CRTX-080, Lixar, Lixivaptan, Vpa-985, VPA 985, VPA-985, WAY-VPA-985)
  • OT receptor/Oxytocin receptor in Human [ChEMBL: CHEMBL2049] [GtoPdb: 369] [UniProtKB: P30559]
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  • 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]
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  • 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]
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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 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 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]