Assay Detail
Binding
CHEMBL676583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace [125I]ET1 from the rat endothelin A receptor expressed in rat aorta smooth muscle cells.
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Chemical function based pharmacophore generation of endothelin-A selective receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.82 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL323464 | — | — | 1 | 10.40 |
| CHEMBL177973 | — | — | 1 | 10.30 |
| CHEMBL177378 | — | — | 1 | 9.92 |
| CHEMBL61211 | — | — | 1 | 9.72 |
| CHEMBL353560 | — | — | 1 | 9.54 |
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 9.51 |
| CHEMBL62264 | — | — | 1 | 9.38 |
| CHEMBL368558 | — | — | 1 | 9.30 |
| CHEMBL174573 | — | — | 1 | 9.30 |
| CHEMBL112832 | — | — | 1 | 9.30 |
| CHEMBL366441 | — | — | 1 | 9.15 |
| CHEMBL111218 | — | — | 1 | 9.11 |
| CHEMBL435773 | — | — | 1 | 8.89 |
| CHEMBL175129 | — | — | 1 | 8.74 |
| CHEMBL177221 | — | — | 1 | 8.52 |
| CHEMBL177886 | — | — | 1 | 8.46 |
| CHEMBL66264 | — | — | 1 | 8.42 |
| CHEMBL427303 | — | — | 1 | 8.41 |
| CHEMBL9162 | — | — | 1 | 8.34 |
| CHEMBL176661 | — | — | 1 | 8.28 |
| CHEMBL295440 | — | — | 1 | 8.27 |
| CHEMBL369085 | — | — | 1 | 8.17 |
| CHEMBL176696 | — | — | 1 | 7.96 |
| CHEMBL321852 | — | — | 1 | 7.85 |
| CHEMBL368270 | — | — | 1 | 7.85 |
| CHEMBL264543 | — | — | 1 | 7.82 |
| CHEMBL332231 | — | — | 1 | 7.80 |
| CHEMBL348407 | — | — | 1 | 7.68 |
| CHEMBL293702 | — | — | 1 | 7.54 |
| CHEMBL64851 | — | — | 1 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL323464 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL177973 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL177378 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL61211 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL353560 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL9194 | ATRASENTAN | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL62264 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL368558 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL174573 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL112832 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL366441 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL111218 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL435773 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL175129 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL177221 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL177886 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL66264 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL427303 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL9162 | — | IC50 | = | 4.62 | nM | 8.34 |
| CHEMBL176661 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL295440 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL369085 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL176696 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL321852 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL368270 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL264543 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL332231 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL348407 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL293702 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL64851 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL175545 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL9141 | — | IC50 | = | 45.3 | nM | 7.34 |
| CHEMBL62363 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL431372 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL417050 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL49040 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL64244 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL366442 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL368668 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL293161 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL177287 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL64832 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL360066 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL177123 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL367032 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL62659 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL62425 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL305117 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL177999 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL305149 | — | IC50 | = | 67000.0 | nM | 4.17 |