macitentan [Ligand Id: 7352] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2103873 (ACT 064992, ACT-064992, Macitentan, Opsumit) |
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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 | Antagonist activity at human ETA receptor expressed in CHO cells in presence of ET1 | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| GtoPdb | - | - | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2012) 55: 7849-61 [PMID:22862294] |
| ChEMBL | Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2012) 55: 7849-7861 [PMID:22862294] |
| ChEMBL | Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| ChEMBL | Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1 | B | 6.01 | pIC50 | 987 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| ChEMBL | Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis | B | 6.41 | pIC50 | 391 | nM | IC50 | J Med Chem (2012) 55: 7849-7861 [PMID:22862294] |
| ChEMBL | Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | B | 6.41 | pIC50 | 391 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813] |
| GtoPdb | - | - | 6.41 | pIC50 | 391 | nM | IC50 | J Med Chem (2012) 55: 7849-61 [PMID:22862294] |
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]
