ambrisentan [Ligand Id: 3951] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1111 (Ambrisentan, GSK-1325760, GSK1325760, GSK-1325760A, GSK1325760A, Letairis, LU-208075, Volibris) |
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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] | ||||||||
| GtoPdb | - | - | 7.66 | pIC50 | 21.7 | nM | IC50 | J Med Chem (2004) 47: 2776-95 [PMID:15139756] |
| ChEMBL | Antagonist activity towards human recombinant Endothelin A receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand | F | 7.66 | pIC50 | 21.7 | nM | IC50 | J Med Chem (2004) 47: 2776-2795 [PMID:15139756] |
| ChEMBL | Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| GtoPdb | - | - | 7.1 | pA2 | - | - | - | J Med Chem (2004) 47: 2776-95 [PMID:15139756] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| GtoPdb | - | - | 5.92 | pIC50 | 1190 | nM | IC50 | J Med Chem (2004) 47: 2776-95 [PMID:15139756] |
| ChEMBL | Antagonist activity towards human recombinant Endothelin B receptor expressed in chinese hamster ovary (CHO) cells determined using [125I]ET1 as radioligand | F | 5.92 | pIC50 | 1190 | nM | IC50 | J Med Chem (2004) 47: 2776-2795 [PMID:15139756] |
| ChEMBL | Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 6.71 | pIC50 | 195 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| Kv7.1/Voltage-gated potassium channel, IKs; KCNQ1(Kv7.1)/KCNE1(MinK) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2221347] [GtoPdb: 560] [UniProtKB: P15382, P51787] | ||||||||
| ChEMBL | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform | F | 4.2 | pIC50 | 63095.73 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
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]
