Assay Detail
Functional
CHEMBL876876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity against human Endothelin A receptor expressed in LtK
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.21 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8981 | PD-156707 | — | 1 | 9.52 |
| CHEMBL25438 | PD-156707 SODIUM | — | 1 | 9.51 |
| CHEMBL11115 | — | — | 1 | 8.74 |
| CHEMBL10924 | — | — | 1 | 8.62 |
| CHEMBL274383 | PD-155080 | — | 1 | 8.13 |
| CHEMBL10588 | — | — | 1 | 7.92 |
| CHEMBL10374 | — | — | 1 | 7.29 |
| CHEMBL10733 | — | — | 1 | 6.96 |
| CHEMBL10996 | — | — | 1 | 6.77 |
| CHEMBL11162 | — | — | 1 | 6.72 |
| CHEMBL275991 | — | — | 1 | 6.40 |
| CHEMBL267094 | — | — | 1 | 6.37 |
| CHEMBL10951 | — | — | 1 | 6.24 |
| CHEMBL11131 | — | — | 1 | 6.22 |
| CHEMBL10648 | — | — | 1 | 6.16 |
| CHEMBL10897 | — | — | 1 | 5.66 |
| CHEMBL273613 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8981 | PD-156707 | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL25438 | PD-156707 SODIUM | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL11115 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL10924 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL274383 | PD-155080 | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL10588 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL10374 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL10733 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL10996 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL11162 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL275991 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL267094 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL10951 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL11131 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL10648 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL10897 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL273613 | — | IC50 | = | 4900.0 | nM | 5.31 |