Assay Detail
Binding
CHEMBL676097
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Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Thoracic aorta |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Three-dimensional quantitative structure-activity relationships of sulfonamide endothelin inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.90 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL283652 | — | — | 1 | 8.40 |
| CHEMBL416026 | — | — | 1 | 8.30 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.82 |
| CHEMBL25816 | — | — | 1 | 7.82 |
| CHEMBL345247 | — | — | 1 | 7.80 |
| CHEMBL30228 | — | — | 1 | 7.17 |
| CHEMBL30199 | — | — | 1 | 7.06 |
| CHEMBL30039 | — | — | 1 | 6.82 |
| CHEMBL26630 | SULFATROXAZOLE | 2.0 | 1 | 6.58 |
| CHEMBL348641 | — | — | 1 | 6.29 |
| CHEMBL30075 | — | — | 1 | 6.22 |
| CHEMBL453 | SULFISOXAZOLE | 4.0 | 1 | 6.10 |
| CHEMBL27073 | — | — | 1 | 6.08 |
| CHEMBL283175 | — | — | 1 | 6.06 |
| CHEMBL27187 | — | — | 1 | 5.89 |
| CHEMBL286521 | — | — | 1 | 5.89 |
| CHEMBL282401 | — | — | 1 | 5.85 |
| CHEMBL26090 | — | — | 1 | 5.84 |
| CHEMBL281511 | — | — | 1 | 5.62 |
| CHEMBL30077 | — | — | 1 | 5.57 |
| CHEMBL27065 | — | — | 1 | 5.51 |
| CHEMBL26527 | — | — | 1 | 5.47 |
| CHEMBL286406 | — | — | 1 | 5.46 |
| CHEMBL433234 | — | — | 1 | 5.42 |
| CHEMBL443 | SULFAMETHOXAZOLE | 4.0 | 1 | 5.40 |
| CHEMBL30078 | — | — | 1 | 5.30 |
| CHEMBL287451 | — | — | 1 | 5.25 |
| CHEMBL282961 | — | — | 1 | 5.05 |
| CHEMBL283879 | — | — | 1 | 5.01 |
| CHEMBL281427 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL283652 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL416026 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL25816 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL267458 | BMS-182874 | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL345247 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL30228 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL30199 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL30039 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL26630 | SULFATROXAZOLE | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL348641 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL30075 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL453 | SULFISOXAZOLE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL27073 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL283175 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL286521 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL27187 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL282401 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL26090 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL281511 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL30077 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL27065 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL26527 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL286406 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL433234 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL443 | SULFAMETHOXAZOLE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL30078 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL287451 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL282961 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL283879 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL281427 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL25756 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL25977 | — | IC50 | = | 27500.0 | nM | 4.56 |
| CHEMBL29705 | — | IC50 | = | 31500.0 | nM | 4.50 |
| CHEMBL28751 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL27248 | — | IC50 | = | 53000.0 | nM | 4.28 |
| CHEMBL332471 | — | IC50 | = | 84000.0 | nM | 4.08 |