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-1 receptor 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 | Displacement of [125I]ET-1 from ETA receptor in human TE-671 cells Membrane assessed as inhibition constant incubated for 16 to 18 hrs by gamma counter analysis | B | 9.37 | pKi | 0.43 | nM | Ki | Eur J Pharmacol (1999) 366: 189-201 [PMID:10082200] |
| 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-1 receptor 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 type 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 36:
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]
