OPC-21268 [Ligand Id: 2196] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL296908 (OPC-1268, OPC-21268) |
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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 | Binding affinity was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from human. | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| GtoPdb | - | - | 6.8 | 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 was evaluated by measuring the displacement of [3H]-OT (oxytocin) from specific binding sites in uterine tissue obtained from rats | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in human platelets. | B | 4.28 | pKi | 52000 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue | B | 4.28 | pKi | 52000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Binding affinity towards Vasopressin V1a receptor in human liver | B | 4.85 | pKi | 14000 | nM | Ki | J Med Chem (2000) 43: 4388-4397 [PMID:11087564] |
| ChEMBL | Binding affinity at cloned human Vasopressin V1a receptor stably expressed in CHO cells, using [3H]AVP as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 2589-2598 [PMID:12036368] |
| GtoPdb | - | - | 5.1 | pKi | - | - | - | Endocrinology (1997) 138: 4109-22 [PMID:9322919] |
| ChEMBL | Binding affinity to vasopressin V1a receptor | B | 6.46 | pKi | 350 | nM | Ki | J Nat Prod (1994) 57: 1329-1335 [PMID:7807119] |
| V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560] | ||||||||
| ChEMBL | Binding affinity towards Vasopressin V1a receptor in rat liver | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2000) 43: 4388-4397 [PMID:11087564] |
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver. | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue | B | 7.49 | pKi | 32 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Evaluated for the binding affinity towards Vasopressin V1a receptor in rat liver membrane using [3H]AVP as radioligand | B | 7.63 | pKi | 23.5 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 229-232 [PMID:11755361] |
| ChEMBL | Binding affinity at Vasopressin V1a receptor, performed using [3H]AVP on rat liver | B | 7.63 | pKi | 23.5 | nM | Ki | J Med Chem (2002) 45: 2589-2598 [PMID:12036368] |
| ChEMBL | Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor) | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (1993) 36: 2011-2017 [PMID:8393113] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors. | B | 4.09 | pKi | >81000 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue | B | 4.09 | pKi | >81000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| GtoPdb | - | - | 4.5 | pKi | - | - | - | Endocrinology (1997) 138: 4109-22 [PMID:9322919] |
| ChEMBL | Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 2589-2598 [PMID:12036368] |
| V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788] | ||||||||
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats. | B | 4.52 | pKi | >30000 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue | B | 4.52 | pKi | >30000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Evaluated for the binding affinity towards Vasopressin V2 receptor in rat kidney membrane using [3H]-AVP as radioligand | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 229-232 [PMID:11755361] |
| ChEMBL | Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2002) 45: 2589-2598 [PMID:12036368] |
| ChEMBL | Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1993) 36: 2011-2017 [PMID:8393113] |
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]
