L-371,257 [Ligand Id: 2252] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL24781 (L-371257) |
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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 | Antagonist activity at human cloned oxytocin receptor by cell based beta lactamase reporter assay | F | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4278-4281 [PMID:18639455] |
| ChEMBL | Ability to displace [3H]oxytocin from human OT receptor (hOT) | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1399-1404 [PMID:11992786] |
| ChEMBL | Binding affinity against cloned human oxytocin receptor from human embryonic kidney cells | B | 8.03 | pKi | 9.3 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3081-3086 [PMID:9873680] |
| ChEMBL | Binding affinity for human oxytocin receptor | B | 8.03 | pKi | 9.3 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1311-1316 [PMID:10340620] |
| ChEMBL | Displacement of 3[H]oxytocin from human oxytocin receptor | B | 8.2 | pKi | 6.31 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1405-1411 [PMID:11992787] |
| ChEMBL | Binding affinity for cloned human oxytocin receptor (OT-R) | B | 8.32 | pKi | 4.8 | nM | Ki | J Med Chem (1998) 41: 2146-2163 [PMID:9622556] |
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]OT (oxytocin) from specific binding sites in uterine tissue obtained from human | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| GtoPdb | - | - | 8.8 | pKi | - | - | - | Br J Pharmacol (2005) 146: 744-751 [PMID:16158071] |
| ChEMBL | Activity at human oxytocin receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 8.34 | pEC50 | 4.6 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| 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 | 7.72 | pKi | 19 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Binding affinity for rat uterine oxytocin receptor (rOTr) | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1311-1316 [PMID:10340620] |
| ChEMBL | Binding affinity against oxytocin receptor (rOTr) in DES pretreated rat uterine | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3081-3086 [PMID:9873680] |
| ChEMBL | Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Compound was tested for displacement of 3[H] oxytocin from rat OT receptor (in vitro) | F | 6.19 | pIC50 | 640 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1405-1411 [PMID:11992787] |
| 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 | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Binding affinity towards human Vasopressin V1a receptor by using functional assay | B | 5.49 | pKi | 3200 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1311-1316 [PMID:10340620] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Compound was tested for its ability to displace vasopressin from human Vasopressin V1a receptor | B | 5.7 | pKi | <1995.26 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 1405-1411 [PMID:11992787] |
| ChEMBL | Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560] | ||||||||
| ChEMBL | Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver | B | 8.43 | pKi | 3.7 | 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 | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| 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 | 4.43 | pKi | 37000 | nM | Ki | J Med Chem (1995) 38: 4634-4636 [PMID:7473590] |
| ChEMBL | Binding affinity towards human kidney Vasopressin V2 receptor by using functional assay | B | 4.43 | pKi | 37000 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 1311-1316 [PMID:10340620] |
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue | B | 4.43 | pKi | 37000 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay | B | 4.43 | pEC50 | 37000 | nM | EC50 | J Med Chem (2010) 53: 1546-1562 [PMID:20104850] |
| 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 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]
