Assay Detail
Binding
CHEMBL877809
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Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Cell Type | A10 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.23 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL267458 | BMS-182874 | — | 1 | 6.82 |
| CHEMBL453 | SULFISOXAZOLE | 4.0 | 1 | 6.11 |
| CHEMBL30199 | — | — | 1 | 6.06 |
| CHEMBL27525 | — | — | 1 | 5.55 |
| CHEMBL30039 | — | — | 1 | 5.40 |
| CHEMBL281942 | — | — | 1 | 5.24 |
| CHEMBL28692 | — | — | 1 | 5.19 |
| CHEMBL282961 | — | — | 1 | 5.04 |
| CHEMBL25730 | — | — | 1 | 5.01 |
| CHEMBL30246 | — | — | 1 | 4.89 |
| CHEMBL27065 | — | — | 1 | 4.70 |
| CHEMBL286682 | — | — | 1 | 4.57 |
| CHEMBL283941 | — | — | 1 | 4.55 |
| CHEMBL332471 | — | — | 1 | 4.08 |
| CHEMBL325690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL267458 | BMS-182874 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL453 | SULFISOXAZOLE | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL30199 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL27525 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL30039 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL281942 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL28692 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL282961 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL25730 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL30246 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL27065 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL286682 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL283941 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL332471 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL325690 | — | IC50 | > | 32000.0 | nM | - |