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 34:
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]
