Assay Detail
Binding
CHEMBL682356
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In vitro binding affinity in a radioligand binding experiment by competition with [125I]-labeled endothelin-1 for ETA receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.17 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL302872 | — | — | 1 | 8.08 |
| CHEMBL292802 | — | — | 1 | 8.05 |
| CHEMBL293877 | — | — | 1 | 8.03 |
| CHEMBL65407 | — | — | 1 | 6.83 |
| CHEMBL45269 | — | — | 1 | 6.78 |
| CHEMBL65488 | — | — | 1 | 6.57 |
| CHEMBL63937 | — | — | 1 | 6.54 |
| CHEMBL304481 | — | — | 1 | 6.26 |
| CHEMBL293232 | — | — | 1 | 6.22 |
| CHEMBL303203 | — | — | 1 | 6.19 |
| CHEMBL63805 | — | — | 1 | 6.17 |
| CHEMBL65531 | — | — | 1 | 6.13 |
| CHEMBL67664 | — | — | 1 | 5.97 |
| CHEMBL63169 | — | — | 1 | 5.96 |
| CHEMBL291404 | — | — | 1 | 5.92 |
| CHEMBL63938 | — | — | 1 | 5.60 |
| CHEMBL304406 | — | — | 1 | 5.57 |
| CHEMBL66641 | — | — | 1 | 5.49 |
| CHEMBL65639 | — | — | 1 | 5.46 |
| CHEMBL63611 | — | — | 1 | 5.38 |
| CHEMBL291891 | — | — | 1 | 5.36 |
| CHEMBL64006 | — | — | 1 | 5.22 |
| CHEMBL63290 | — | — | 1 | 5.21 |
| CHEMBL434983 | — | — | 1 | 4.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL302872 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL292802 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL293877 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL65407 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL45269 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL65488 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL63937 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL304481 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL293232 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL303203 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL63805 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL65531 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL67664 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL63169 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL291404 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL63938 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL304406 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL66641 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL65639 | — | IC50 | = | 3470.0 | nM | 5.46 |
| CHEMBL63611 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL291891 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL64006 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL63290 | — | IC50 | = | 6140.0 | nM | 5.21 |
| CHEMBL434983 | — | IC50 | = | 10210.0 | nM | 4.99 |