Assay Detail
Binding
CHEMBL682969
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Inhibitory concentration was determined against selective Endothelin A receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Acyl substitution at the ortho position of anilides enhances oral bioavailability of thiophene sulfonamides: TBC3214, an ETA selective endothelin antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.10 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19950 | — | — | 1 | 10.40 |
| CHEMBL19661 | — | — | 1 | 10.00 |
| CHEMBL277706 | — | — | 1 | 9.92 |
| CHEMBL19921 | — | — | 1 | 9.85 |
| CHEMBL18626 | — | — | 1 | 9.85 |
| CHEMBL279471 | — | — | 1 | 9.77 |
| CHEMBL277595 | — | — | 1 | 9.77 |
| CHEMBL280659 | — | — | 1 | 9.72 |
| CHEMBL283582 | — | — | 1 | 9.37 |
| CHEMBL282724 | SITAXENTAN | 4.0 | 1 | 8.85 |
| CHEMBL20168 | — | — | 1 | 8.48 |
| CHEMBL19808 | — | — | 1 | 8.47 |
| CHEMBL283535 | — | — | 1 | 8.00 |
| CHEMBL278114 | — | — | 1 | 7.82 |
| CHEMBL283136 | — | — | 1 | 7.72 |
| CHEMBL282470 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19950 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL19661 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL277706 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL19921 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL18626 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL279471 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL277595 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL280659 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL283582 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL282724 | SITAXENTAN | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL20168 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL19808 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL283535 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL278114 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL283136 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL282470 | — | IC50 | = | 21.0 | nM | 7.68 |