Assay Detail
Binding
CHEMBL670477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding ability determined by the displacement of [125 I]ET-3 from the human Endothelin B 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 | 8.15 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332289 | — | — | 1 | 9.15 |
| CHEMBL123316 | — | — | 1 | 9.03 |
| CHEMBL330895 | — | — | 1 | 8.96 |
| CHEMBL332109 | — | — | 1 | 8.96 |
| CHEMBL123654 | — | — | 2 | 8.77 |
| CHEMBL273642 | — | — | 2 | 8.72 |
| CHEMBL121647 | — | — | 1 | 8.68 |
| CHEMBL123408 | — | — | 1 | 8.66 |
| CHEMBL123107 | — | — | 1 | 8.59 |
| CHEMBL123206 | — | — | 1 | 8.48 |
| CHEMBL333034 | — | — | 1 | 8.47 |
| CHEMBL432227 | — | — | 1 | 8.47 |
| CHEMBL122933 | — | — | 1 | 8.30 |
| CHEMBL334076 | — | — | 1 | 8.30 |
| CHEMBL332424 | — | — | 1 | 8.21 |
| CHEMBL122673 | — | — | 1 | 8.18 |
| CHEMBL331936 | — | — | 1 | 8.14 |
| CHEMBL123994 | — | — | 1 | 8.09 |
| CHEMBL123146 | — | — | 1 | 7.75 |
| CHEMBL121761 | — | — | 1 | 7.70 |
| CHEMBL331548 | — | — | 1 | 7.51 |
| CHEMBL122614 | — | — | 1 | 7.33 |
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 7.20 |
| CHEMBL332808 | — | — | 1 | 6.97 |
| CHEMBL332144 | — | — | 1 | 6.22 |
| CHEMBL434986 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332289 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL123316 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL330895 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL332109 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL123654 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL123654 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL273642 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL121647 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL123408 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL123107 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL123206 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL273642 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL333034 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL432227 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL334076 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL122933 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL332424 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL122673 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL331936 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL123994 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL123146 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL121761 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL331548 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL122614 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL9194 | ATRASENTAN | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL332808 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL332144 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL434986 | — | IC50 | = | 744.0 | nM | 6.13 |