Assay Detail
Binding
CHEMBL679285
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Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Pituitary gland cell |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent and selective non-benzodioxole-containing endothelin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.42 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 9.40 |
| CHEMBL112832 | — | — | 1 | 9.30 |
| CHEMBL110366 | — | — | 1 | 9.22 |
| CHEMBL112685 | — | — | 1 | 9.15 |
| CHEMBL113611 | — | — | 1 | 9.10 |
| CHEMBL326191 | — | — | 1 | 9.00 |
| CHEMBL113529 | — | — | 1 | 8.89 |
| CHEMBL419211 | — | — | 1 | 8.82 |
| CHEMBL113400 | — | — | 1 | 8.82 |
| CHEMBL558148 | — | — | 1 | 8.70 |
| CHEMBL112347 | — | — | 1 | 8.43 |
| CHEMBL326719 | — | — | 1 | 8.30 |
| CHEMBL321852 | — | — | 1 | 7.85 |
| CHEMBL114084 | — | — | 1 | 6.89 |
| CHEMBL109736 | — | — | 1 | 6.89 |
| CHEMBL113379 | — | — | 1 | 6.86 |
| CHEMBL331577 | — | — | 1 | 6.75 |
| CHEMBL326690 | — | — | 1 | 6.59 |
| CHEMBL331375 | — | — | 1 | 6.59 |
| CHEMBL113184 | — | — | 1 | 6.51 |
| CHEMBL325444 | — | — | 1 | 6.51 |
| CHEMBL112325 | — | — | 1 | 6.39 |
| CHEMBL110794 | — | — | 1 | 6.14 |
| CHEMBL113494 | — | — | 1 | 6.03 |
| CHEMBL326951 | — | — | 1 | 5.77 |
| CHEMBL324301 | — | — | 1 | 5.70 |
| CHEMBL325418 | — | — | 1 | 5.64 |
| CHEMBL444061 | — | — | 1 | 5.64 |
| CHEMBL322935 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL112832 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL110366 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL112685 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL113611 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL326191 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL113529 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL419211 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL113400 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL558148 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL112347 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL326719 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL321852 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL114084 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL109736 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL113379 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL331577 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL326690 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL331375 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL113184 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL325444 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL112325 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL110794 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL113494 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL326951 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL324301 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL325418 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL444061 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL322935 | — | IC50 | = | 5100.0 | nM | 5.29 |