Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL49429 (CRTX 080, CRTX-080, Lixar, Lixivaptan, Vpa-985, VPA 985, VPA-985, WAY-VPA-985) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]