Assay Detail
Binding
CHEMBL4426321
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Antagonist activity at ETA receptor (unknown origin)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 8 | 8.29 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2165332 | — | — | 1 | 9.15 |
| CHEMBL2163716 | — | — | 1 | 8.72 |
| CHEMBL2163702 | — | — | 1 | 8.66 |
| CHEMBL2163715 | — | — | 1 | 8.37 |
| CHEMBL2165328 | — | — | 1 | 8.16 |
| CHEMBL2163698 | — | — | 1 | 8.10 |
| CHEMBL2163695 | — | — | 1 | 7.60 |
| CHEMBL4562189 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2165332 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2163716 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2163702 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2163715 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2165328 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2163698 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2163695 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4562189 | — | IC50 | = | 26.0 | nM | 7.58 |