Assay Detail
Functional
CHEMBL676489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Potency on ETA receptor assessed by inhibition of the contraction induced by ET-1 in rat aortic rings
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 7.12 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL175058 | — | — | 1 | 8.11 |
| CHEMBL94786 | — | — | 1 | 7.70 |
| CHEMBL275897 | — | — | 1 | 7.70 |
| CHEMBL368996 | — | — | 1 | 7.58 |
| CHEMBL368386 | — | — | 1 | 7.57 |
| CHEMBL367453 | — | — | 1 | 7.56 |
| CHEMBL366885 | — | — | 1 | 7.29 |
| CHEMBL174607 | — | — | 1 | 7.15 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 7.14 |
| CHEMBL175435 | — | — | 1 | 6.97 |
| CHEMBL367382 | — | — | 1 | 6.83 |
| CHEMBL264035 | — | — | 1 | 6.68 |
| CHEMBL163638 | — | — | 1 | 6.64 |
| CHEMBL368383 | — | — | 1 | 6.37 |
| CHEMBL176741 | — | — | 1 | 6.30 |
| CHEMBL367036 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL175058 | — | Kd | = | 7.762 | nM | 8.11 |
| CHEMBL94786 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL275897 | — | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL368996 | — | Kd | = | 26.3 | nM | 7.58 |
| CHEMBL368386 | — | Kd | = | 26.92 | nM | 7.57 |
| CHEMBL367453 | — | Kd | = | 27.54 | nM | 7.56 |
| CHEMBL366885 | — | Kd | = | 51.29 | nM | 7.29 |
| CHEMBL174607 | — | Kd | = | 70.79 | nM | 7.15 |
| CHEMBL957 | BOSENTAN | Kd | = | 72.44 | nM | 7.14 |
| CHEMBL175435 | — | Kd | = | 107.15 | nM | 6.97 |
| CHEMBL367382 | — | Kd | = | 147.91 | nM | 6.83 |
| CHEMBL264035 | — | Kd | = | 208.93 | nM | 6.68 |
| CHEMBL163638 | — | Kd | = | 229.09 | nM | 6.64 |
| CHEMBL368383 | — | Kd | = | 426.58 | nM | 6.37 |
| CHEMBL176741 | — | Kd | = | 501.19 | nM | 6.30 |
| CHEMBL367036 | — | Kd | = | 562.34 | nM | 6.25 |