Assay Detail
Binding
CHEMBL679286
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Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A7R5 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 5.59 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55909 | — | — | 1 | 6.50 |
| CHEMBL54773 | — | — | 1 | 6.42 |
| CHEMBL298340 | — | — | 1 | 6.40 |
| CHEMBL59425 | — | — | 1 | 6.28 |
| CHEMBL54770 | — | — | 1 | 6.20 |
| CHEMBL53168 | — | — | 1 | 6.11 |
| CHEMBL55664 | — | — | 1 | 6.10 |
| CHEMBL54274 | — | — | 1 | 5.89 |
| CHEMBL300066 | — | — | 1 | 5.89 |
| CHEMBL54998 | — | — | 1 | 5.85 |
| CHEMBL54703 | — | — | 1 | 5.82 |
| CHEMBL54057 | — | — | 1 | 5.77 |
| CHEMBL55405 | — | — | 1 | 5.47 |
| CHEMBL55406 | — | — | 1 | 5.46 |
| CHEMBL53097 | — | — | 1 | 5.37 |
| CHEMBL26630 | SULFATROXAZOLE | 2.0 | 1 | 5.30 |
| CHEMBL55876 | — | — | 1 | 5.21 |
| CHEMBL298395 | — | — | 1 | 5.20 |
| CHEMBL453 | SULFISOXAZOLE | 4.0 | 1 | 5.05 |
| CHEMBL298976 | — | — | 1 | 4.96 |
| CHEMBL299831 | — | — | 1 | 4.55 |
| CHEMBL292355 | — | — | 1 | 4.55 |
| CHEMBL293376 | — | — | 1 | 4.15 |
| CHEMBL53114 | — | — | 1 | - |
| CHEMBL443 | SULFAMETHOXAZOLE | 4.0 | 1 | - |
| CHEMBL415942 | — | — | 1 | - |
| CHEMBL417595 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55909 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL54773 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL298340 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL59425 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL54770 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL53168 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL55664 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL54274 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL300066 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL54998 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL54703 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL54057 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL55405 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL55406 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL53097 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL26630 | SULFATROXAZOLE | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL55876 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL298395 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL453 | SULFISOXAZOLE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL298976 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL299831 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL292355 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL293376 | — | IC50 | = | 71000.0 | nM | 4.15 |
| CHEMBL53114 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL443 | SULFAMETHOXAZOLE | IC50 | = | 333000.0 | nM | - |
| CHEMBL415942 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL417595 | — | IC50 | > | 100000.0 | nM | - |