Assay Detail
Binding
CHEMBL677304
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Binding ability determined by the displacement of [125I]ET1 from the human endothelin A receptor
28
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.05 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 10.47 |
| CHEMBL121647 | — | — | 1 | 9.15 |
| CHEMBL123107 | — | — | 1 | 9.00 |
| CHEMBL334076 | — | — | 1 | 8.80 |
| CHEMBL330895 | — | — | 1 | 8.60 |
| CHEMBL331936 | — | — | 1 | 8.43 |
| CHEMBL122614 | — | — | 1 | 8.41 |
| CHEMBL121761 | — | — | 1 | 8.26 |
| CHEMBL123316 | — | — | 1 | 8.06 |
| CHEMBL333034 | — | — | 1 | 7.87 |
| CHEMBL123146 | — | — | 1 | 7.80 |
| CHEMBL123994 | — | — | 1 | 7.34 |
| CHEMBL432227 | — | — | 1 | 7.20 |
| CHEMBL122673 | — | — | 1 | 7.00 |
| CHEMBL331548 | — | — | 1 | 6.91 |
| CHEMBL122933 | — | — | 1 | 6.88 |
| CHEMBL332109 | — | — | 1 | 6.79 |
| CHEMBL332808 | — | — | 1 | 6.70 |
| CHEMBL332289 | — | — | 1 | 6.49 |
| CHEMBL434986 | — | — | 1 | 6.37 |
| CHEMBL123408 | — | — | 1 | 6.31 |
| CHEMBL332424 | — | — | 1 | 6.13 |
| CHEMBL332144 | — | — | 1 | 5.91 |
| CHEMBL123206 | — | — | 1 | 4.85 |
| CHEMBL123654 | — | — | 2 | 4.69 |
| CHEMBL273642 | — | — | 2 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | IC50 | = | 0.034 | nM | 10.47 |
| CHEMBL121647 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL123107 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL334076 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL330895 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL331936 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL122614 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL121761 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL123316 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL333034 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL123146 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL123994 | — | IC50 | = | 45.9 | nM | 7.34 |
| CHEMBL432227 | — | IC50 | = | 63.5 | nM | 7.20 |
| CHEMBL122673 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL331548 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL122933 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL332109 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL332808 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL332289 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL434986 | — | IC50 | = | 432.0 | nM | 6.37 |
| CHEMBL123408 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL332424 | — | IC50 | = | 749.0 | nM | 6.13 |
| CHEMBL332144 | — | IC50 | = | 1228.0 | nM | 5.91 |
| CHEMBL123206 | — | IC50 | = | 14270.0 | nM | 4.85 |
| CHEMBL123654 | — | IC50 | = | 20560.0 | nM | 4.69 |
| CHEMBL123654 | — | IC50 | = | 27014.0 | nM | 4.57 |
| CHEMBL273642 | — | IC50 | = | 51703.0 | nM | 4.29 |
| CHEMBL273642 | — | IC50 | = | 77360.0 | nM | 4.11 |