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 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]
