Assay Detail
Binding
CHEMBL681513
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Binding affinity for human Endothelin A receptor expressed in LtK- cells
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.70 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319452 | — | — | 1 | 9.46 |
| CHEMBL8981 | PD-156707 | — | 1 | 9.43 |
| CHEMBL450337 | — | — | 1 | 9.40 |
| CHEMBL316523 | — | — | 1 | 9.30 |
| CHEMBL103846 | — | — | 1 | 9.22 |
| CHEMBL320839 | — | — | 1 | 9.10 |
| CHEMBL322920 | — | — | 3 | 9.00 |
| CHEMBL51530 | — | — | 1 | 8.13 |
| CHEMBL320183 | — | — | 1 | 8.05 |
| CHEMBL103501 | — | — | 1 | 7.75 |
| CHEMBL276173 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319452 | — | IC50 | = | 0.35 | nM | 9.46 |
| CHEMBL8981 | PD-156707 | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL450337 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL316523 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL103846 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL320839 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL322920 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL322920 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL322920 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL51530 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL320183 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL103501 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL276173 | — | IC50 | = | 300.0 | nM | 6.52 |