L-368,899 [Ligand Id: 2249] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1253853 |
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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 | Displacement of [3H]-oxytocin from oxytocin receptor in human uterus tissue | B | 7.89 | pKi | 13 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Binding affinity to human OT receptor | B | 7.89 | pKi | 13 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
| GtoPdb | - | - | 8.1 | 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 | Displacement of [3H]-oxytocin from oxytocin receptor in rat uterus tissue | B | 8.44 | pKi | 3.6 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Inhibition of rat uterus OT receptor | B | 8.05 | pIC50 | 8.9 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
| V1A receptor/Vasopressin V1a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1889] [GtoPdb: 366] [UniProtKB: P37288] | ||||||||
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Binding affinity to human liver V1A receptor | B | 6.74 | pKi | 180 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
| V1A receptor/Vasopressin V1a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2868] [GtoPdb: 366] [UniProtKB: P30560] | ||||||||
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Inhibition of rat liver V1a receptor | B | 6.43 | pIC50 | 370 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
| V2 receptor/Vasopressin V2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1790] [GtoPdb: 368] [UniProtKB: P30518] | ||||||||
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue | B | 6.23 | pKi | 590 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Binding affinity to human V2 receptor | B | 6.23 | pKi | 590 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
| V2 receptor/Vasopressin V2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3766] [GtoPdb: 368] [UniProtKB: Q00788] | ||||||||
| ChEMBL | Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2010) 53: 6525-6538 [PMID:20550119] |
| ChEMBL | Inhibition of rat kidney V2 receptor | B | 6.24 | pIC50 | 570 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 902-906 [PMID:23270988] |
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]
