Assay Detail
Binding
CHEMBL4426307
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 125I-ET1 from human placenta cell membrane ETA receptor expressed in Baculovirus-infected insect cells
9
Total Activities
9
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 | 9 | 7.22 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70385 | — | — | 1 | 9.52 |
| CHEMBL4456288 | — | — | 1 | 8.85 |
| CHEMBL4579445 | — | — | 1 | 8.00 |
| CHEMBL4447261 | — | — | 1 | 7.46 |
| CHEMBL4562189 | — | — | 1 | 7.30 |
| CHEMBL324304 | — | — | 1 | 6.00 |
| CHEMBL4584753 | — | — | 1 | 5.70 |
| CHEMBL4447655 | — | — | 1 | 4.89 |
| CHEMBL4438411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70385 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4456288 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4579445 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4447261 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4562189 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL324304 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4584753 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4447655 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4438411 | — | IC50 | > | 100000.0 | nM | - |