Assay Detail
Binding
CHEMBL4426323
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
37
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.74 | 10.00 |
| Ki | 2 | 9.09 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4467748 | — | — | 1 | 10.00 |
| CHEMBL4559129 | — | — | 1 | 9.96 |
| CHEMBL4553625 | — | — | 1 | 9.70 |
| CHEMBL4455360 | — | — | 1 | 9.52 |
| CHEMBL4458005 | — | — | 1 | 9.52 |
| CHEMBL4521348 | — | — | 1 | 9.30 |
| CHEMBL2110610 | FANDOSENTAN | 2.0 | 1 | 9.30 |
| CHEMBL2103873 | MACITENTAN | 4.0 | 1 | 9.30 |
| CHEMBL4528516 | — | — | 1 | 9.30 |
| CHEMBL4565926 | — | — | 1 | 9.15 |
| CHEMBL4463633 | — | — | 1 | 9.15 |
| CHEMBL1111 | AMBRISENTAN | 4.0 | 1 | 9.00 |
| CHEMBL4448273 | — | — | 1 | 9.00 |
| CHEMBL293012 | — | — | 1 | 9.00 |
| CHEMBL4542394 | — | — | 1 | 9.00 |
| CHEMBL4549357 | — | — | 1 | 9.00 |
| CHEMBL4528664 | — | — | 1 | 8.96 |
| CHEMBL4573273 | — | — | 1 | 8.89 |
| CHEMBL4519822 | — | — | 1 | 8.85 |
| CHEMBL4436531 | — | — | 1 | 8.82 |
| CHEMBL4572734 | — | — | 1 | 8.70 |
| CHEMBL4540866 | — | — | 1 | 8.70 |
| CHEMBL4573806 | — | — | 1 | 8.70 |
| CHEMBL4449731 | — | — | 1 | 8.66 |
| CHEMBL4536769 | — | — | 1 | 8.62 |
| CHEMBL4574034 | — | — | 1 | 8.52 |
| CHEMBL4566095 | — | — | 1 | 8.48 |
| CHEMBL2165326 | APROCITENTAN | 4.0 | 1 | 8.47 |
| CHEMBL4568468 | — | — | 1 | 8.22 |
| CHEMBL23261 | DARUSENTAN | 3.0 | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4467748 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4559129 | — | Ki | = | 0.11 | nM | 9.96 |
| CHEMBL4553625 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4455360 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4458005 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4521348 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2110610 | FANDOSENTAN | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL2103873 | MACITENTAN | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4528516 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4463633 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4565926 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4542394 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL293012 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4549357 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4448273 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1111 | AMBRISENTAN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4528664 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4573273 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4519822 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4436531 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4573806 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4572734 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4540866 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4449731 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4536769 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4574034 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4566095 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2165326 | APROCITENTAN | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4568468 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL23261 | DARUSENTAN | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4444355 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL330425 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4570529 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL1628688 | ZIBOTENTAN | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL367444 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4435789 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4465332 | — | IC50 | = | 33.0 | nM | 7.48 |