Assay Detail
Functional
CHEMBL857233
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Phosphoinositol hydrolysis in TE671 or transfected cos 7 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | cos 7 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 4 | 7.81 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297783 | — | — | 1 | 8.47 |
| CHEMBL282724 | SITAXENTAN | 4.0 | 1 | 8.00 |
| CHEMBL295557 | — | — | 1 | 8.00 |
| CHEMBL282470 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297783 | — | Kd | = | 3.388 | nM | 8.47 |
| CHEMBL282724 | SITAXENTAN | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL295557 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL282470 | — | Kd | = | 177.83 | nM | 6.75 |