Assay Detail
Functional
CHEMBL796077
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Inhibitory potency at native endothelin A and B receptors by inhibiting sarafotoxin Sf6 contractions of rat tracheal rings
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Publication
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 9 | 7.02 | 7.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330135 | — | — | 1 | 7.88 |
| CHEMBL330354 | — | — | 1 | 7.72 |
| CHEMBL96303 | — | — | 1 | 7.44 |
| CHEMBL318086 | — | — | 1 | 7.37 |
| CHEMBL319754 | — | — | 1 | 7.07 |
| CHEMBL96347 | — | — | 1 | 7.02 |
| CHEMBL96704 | — | — | 1 | 6.89 |
| CHEMBL329477 | — | — | 1 | 6.18 |
| CHEMBL1111 | AMBRISENTAN | 4.0 | 1 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330135 | — | Kd | = | 13.18 | nM | 7.88 |
| CHEMBL330354 | — | Kd | = | 19.05 | nM | 7.72 |
| CHEMBL96303 | — | Kd | = | 36.31 | nM | 7.44 |
| CHEMBL318086 | — | Kd | = | 42.66 | nM | 7.37 |
| CHEMBL319754 | — | Kd | = | 85.11 | nM | 7.07 |
| CHEMBL96347 | — | Kd | = | 95.5 | nM | 7.02 |
| CHEMBL96704 | — | Kd | = | 128.82 | nM | 6.89 |
| CHEMBL329477 | — | Kd | = | 660.69 | nM | 6.18 |
| CHEMBL1111 | AMBRISENTAN | Kd | = | 2344.23 | nM | 5.63 |