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 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]
