Assay Detail
Binding
CHEMBL677305
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Binding affinity towards human Endothelin A receptor (hET -A)
31
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.02 | 10.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL111277 | — | — | 1 | 10.10 |
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 10.10 |
| CHEMBL420729 | — | — | 1 | 8.00 |
| CHEMBL123305 | — | — | 1 | 7.92 |
| CHEMBL421073 | — | — | 1 | 7.82 |
| CHEMBL123997 | — | — | 1 | 7.82 |
| CHEMBL122832 | — | — | 1 | 7.80 |
| CHEMBL332231 | — | — | 1 | 7.80 |
| CHEMBL2370534 | — | — | 1 | 7.75 |
| CHEMBL333972 | — | — | 1 | 7.66 |
| CHEMBL120106 | — | — | 1 | 7.60 |
| CHEMBL122111 | — | — | 1 | 7.48 |
| CHEMBL331767 | — | — | 1 | 7.48 |
| CHEMBL339657 | — | — | 2 | 7.35 |
| CHEMBL332431 | — | — | 1 | 7.30 |
| CHEMBL123926 | — | — | 1 | 7.21 |
| CHEMBL435185 | — | — | 1 | 7.00 |
| CHEMBL123077 | — | — | 1 | 6.80 |
| CHEMBL332093 | — | — | 1 | 6.72 |
| CHEMBL332387 | — | — | 1 | 6.70 |
| CHEMBL435385 | — | — | 2 | 6.47 |
| CHEMBL331758 | — | — | 1 | 6.08 |
| CHEMBL332627 | — | — | 1 | 6.04 |
| CHEMBL333009 | — | — | 1 | 5.82 |
| CHEMBL331625 | — | — | 2 | 5.43 |
| CHEMBL332794 | A-192621 | — | 2 | 5.09 |
| CHEMBL331066 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL111277 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL9194 | ATRASENTAN | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL420729 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL123305 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL123997 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL421073 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL122832 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL332231 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2370534 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL333972 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL120106 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL331767 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL122111 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL339657 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL332431 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL123926 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL339657 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL435185 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL123077 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL332093 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL332387 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL435385 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL331758 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL332627 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL435385 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL333009 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL331625 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL331625 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL332794 | A-192621 | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL332794 | A-192621 | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL331066 | — | IC50 | = | 11000.0 | nM | 4.96 |