Assay Detail
Binding
CHEMBL682103
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Binding affinity against human ETA receptor in TE 671(ATCC# HTB 139) cell membrane preparation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HTB 139) |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.80 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80782 | — | — | 1 | 8.96 |
| CHEMBL267458 | BMS-182874 | — | 1 | 8.24 |
| CHEMBL310427 | — | — | 1 | 8.08 |
| CHEMBL80980 | — | — | 1 | 6.96 |
| CHEMBL76860 | — | — | 1 | 6.85 |
| CHEMBL27065 | — | — | 1 | 6.36 |
| CHEMBL76623 | — | — | 1 | 5.54 |
| CHEMBL77962 | — | — | 1 | 5.23 |
| CHEMBL311258 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80782 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL267458 | BMS-182874 | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL310427 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL80980 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL76860 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL27065 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL76623 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL77962 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL311258 | — | IC50 | = | 9900.0 | nM | 5.00 |