Assay Detail
Binding
CHEMBL674069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells.
87
Total Activities
87
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | VSM-A10 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery and structure-activity relationships of sulfonamide ETA-selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 87 | 5.52 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267458 | BMS-182874 | — | 1 | 7.82 |
| CHEMBL416026 | — | — | 1 | 7.70 |
| CHEMBL30032 | — | — | 1 | 7.52 |
| CHEMBL26978 | — | — | 1 | 7.22 |
| CHEMBL25816 | — | — | 1 | 7.22 |
| CHEMBL27299 | — | — | 1 | 7.10 |
| CHEMBL283652 | — | — | 1 | 6.89 |
| CHEMBL26079 | — | — | 1 | 6.89 |
| CHEMBL27370 | — | — | 1 | 6.89 |
| CHEMBL27063 | — | — | 1 | 6.82 |
| CHEMBL26630 | SULFATROXAZOLE | 2.0 | 1 | 6.58 |
| CHEMBL284177 | — | — | 1 | 6.57 |
| CHEMBL285122 | — | — | 1 | 6.54 |
| CHEMBL29448 | — | — | 1 | 6.40 |
| CHEMBL440653 | — | — | 1 | 6.23 |
| CHEMBL30075 | — | — | 1 | 6.18 |
| CHEMBL453 | SULFISOXAZOLE | 4.0 | 1 | 6.11 |
| CHEMBL27073 | — | — | 1 | 6.08 |
| CHEMBL26252 | — | — | 1 | 6.06 |
| CHEMBL283175 | — | — | 1 | 6.06 |
| CHEMBL30199 | — | — | 1 | 6.06 |
| CHEMBL26522 | — | — | 1 | 6.00 |
| CHEMBL27344 | — | — | 1 | 5.93 |
| CHEMBL27187 | — | — | 1 | 5.89 |
| CHEMBL286521 | — | — | 1 | 5.89 |
| CHEMBL26090 | — | — | 1 | 5.85 |
| CHEMBL282401 | — | — | 1 | 5.85 |
| CHEMBL27178 | — | — | 1 | 5.75 |
| CHEMBL418202 | — | — | 1 | 5.71 |
| CHEMBL281199 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267458 | BMS-182874 | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL416026 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL30032 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL26978 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL25816 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL27299 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL283652 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL26079 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL27370 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL27063 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL26630 | SULFATROXAZOLE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL284177 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL285122 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL29448 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL440653 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL30075 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL453 | SULFISOXAZOLE | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL27073 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL26252 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL283175 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL30199 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL26522 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL27344 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL27187 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL286521 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL26090 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL282401 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL27178 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL418202 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL281199 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL281511 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL30077 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL27525 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL431300 | — | IC50 | = | 2890.0 | nM | 5.54 |
| CHEMBL26786 | — | IC50 | = | 3050.0 | nM | 5.52 |
| CHEMBL26527 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL283195 | — | IC50 | = | 3380.0 | nM | 5.47 |
| CHEMBL286406 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL433234 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL30039 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL443 | SULFAMETHOXAZOLE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL27256 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL283300 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL30078 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL417651 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL287451 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL281942 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL26470 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL28692 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL29954 | — | IC50 | = | 7800.0 | nM | 5.11 |