Assay Detail
Functional
CHEMBL879064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory potency at native endothelin A and endothelin B receptors by inhibiting endothelin-1 contractions of rat aortic rings
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 27 | 7.56 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL319754 | — | — | 1 | 9.03 |
| CHEMBL318086 | — | — | 1 | 8.98 |
| CHEMBL330135 | — | — | 1 | 8.72 |
| CHEMBL94580 | — | — | 1 | 8.38 |
| CHEMBL330354 | — | — | 1 | 8.36 |
| CHEMBL96347 | — | — | 1 | 8.27 |
| CHEMBL419136 | — | — | 1 | 8.10 |
| CHEMBL93084 | — | — | 1 | 7.93 |
| CHEMBL406551 | — | — | 1 | 7.87 |
| CHEMBL415010 | — | — | 1 | 7.84 |
| CHEMBL96303 | — | — | 1 | 7.83 |
| CHEMBL422068 | — | — | 1 | 7.69 |
| CHEMBL96932 | — | — | 1 | 7.55 |
| CHEMBL314755 | — | — | 1 | 7.46 |
| CHEMBL96171 | — | — | 1 | 7.46 |
| CHEMBL95013 | — | — | 1 | 7.32 |
| CHEMBL316453 | — | — | 1 | 7.28 |
| CHEMBL96723 | — | — | 1 | 7.22 |
| CHEMBL1111 | AMBRISENTAN | 4.0 | 1 | 7.09 |
| CHEMBL94964 | — | — | 1 | 6.99 |
| CHEMBL316301 | — | — | 1 | 6.98 |
| CHEMBL330425 | — | — | 1 | 6.87 |
| CHEMBL328878 | — | — | 1 | 6.79 |
| CHEMBL94810 | — | — | 1 | 6.71 |
| CHEMBL96704 | — | — | 1 | 6.59 |
| CHEMBL94934 | — | — | 1 | 6.53 |
| CHEMBL317510 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL319754 | — | Kd | = | 0.9333 | nM | 9.03 |
| CHEMBL318086 | — | Kd | = | 1.047 | nM | 8.98 |
| CHEMBL330135 | — | Kd | = | 1.905 | nM | 8.72 |
| CHEMBL94580 | — | Kd | = | 4.169 | nM | 8.38 |
| CHEMBL330354 | — | Kd | = | 4.365 | nM | 8.36 |
| CHEMBL96347 | — | Kd | = | 5.37 | nM | 8.27 |
| CHEMBL419136 | — | Kd | = | 7.943 | nM | 8.10 |
| CHEMBL93084 | — | Kd | = | 11.75 | nM | 7.93 |
| CHEMBL406551 | — | Kd | = | 13.49 | nM | 7.87 |
| CHEMBL415010 | — | Kd | = | 14.45 | nM | 7.84 |
| CHEMBL96303 | — | Kd | = | 14.79 | nM | 7.83 |
| CHEMBL422068 | — | Kd | = | 20.42 | nM | 7.69 |
| CHEMBL96932 | — | Kd | = | 28.18 | nM | 7.55 |
| CHEMBL314755 | — | Kd | = | 34.67 | nM | 7.46 |
| CHEMBL96171 | — | Kd | = | 34.67 | nM | 7.46 |
| CHEMBL95013 | — | Kd | = | 47.86 | nM | 7.32 |
| CHEMBL316453 | — | Kd | = | 52.48 | nM | 7.28 |
| CHEMBL96723 | — | Kd | = | 60.26 | nM | 7.22 |
| CHEMBL1111 | AMBRISENTAN | Kd | = | 81.28 | nM | 7.09 |
| CHEMBL94964 | — | Kd | = | 102.33 | nM | 6.99 |
| CHEMBL316301 | — | Kd | = | 104.71 | nM | 6.98 |
| CHEMBL330425 | — | Kd | = | 134.9 | nM | 6.87 |
| CHEMBL328878 | — | Kd | = | 162.18 | nM | 6.79 |
| CHEMBL94810 | — | Kd | = | 194.98 | nM | 6.71 |
| CHEMBL96704 | — | Kd | = | 257.04 | nM | 6.59 |
| CHEMBL94934 | — | Kd | = | 295.12 | nM | 6.53 |
| CHEMBL317510 | — | Kd | = | 478.63 | nM | 6.32 |