sitaxsentan [Ligand Id: 3950] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL282724 (IPI-1040, Sitaxentan, Sitaxsentan, TBC-11251) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Binding affinity against human Endothelin A receptor | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (1997) 40: 1690-1697 [PMID:9171878] |
| ChEMBL | Inhibitory concentration towards Endothelin A receptor in human | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
| ChEMBL | Displacement of [125I]ET-1 from Endothelin A receptor | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
| ChEMBL | Inhibitory concentration was determined against selective Endothelin A receptor | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (2001) 44: 1211-1216 [PMID:11312921] |
| ChEMBL | In vitro inhibition of endothelin binding to human Endothelin A receptor using [125I]-labeled ET-1 competition assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | J Med Chem (1997) 40: 1690-1697 [PMID:9171878] |
| GtoPdb | - | - | 8 | pA2 | - | - | - | J Med Chem (1997) 40: 1690-7 [PMID:9171878] |
| ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | Binding affinity towards Endothelin A receptor | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | In vitro inhibition of endothelin binding to human Endothelin B receptor using [125I]-labeled ET-1 competition assay | B | 5.01 | pIC50 | 9800 | nM | IC50 | J Med Chem (1997) 40: 1690-1697 [PMID:9171878] |
| ChEMBL | Inhibitory concentration towards endothelin B receptor in human | F | 8.01 | pIC50 | 9.8 | nM | IC50 | J Med Chem (2004) 47: 1969-1986 [PMID:15055997] |
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]
