Assay Detail
Binding
CHEMBL671335
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Binding affinity towards endothelin B receptor in porcine cerebellar tissue using [125I]-ET-1 as radioligand.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 4.91 | 6.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 6.28 |
| CHEMBL113611 | — | — | 1 | 6.03 |
| CHEMBL326191 | — | — | 1 | 6.02 |
| CHEMBL110366 | — | — | 1 | 5.58 |
| CHEMBL113529 | — | — | 1 | 5.39 |
| CHEMBL112685 | — | — | 1 | 5.30 |
| CHEMBL112832 | — | — | 1 | 5.29 |
| CHEMBL113379 | — | — | 1 | 5.19 |
| CHEMBL419211 | — | — | 1 | 5.10 |
| CHEMBL325444 | — | — | 1 | 4.96 |
| CHEMBL558148 | — | — | 1 | 4.96 |
| CHEMBL326690 | — | — | 1 | 4.89 |
| CHEMBL331577 | — | — | 1 | 4.80 |
| CHEMBL326719 | — | — | 1 | 4.80 |
| CHEMBL113400 | — | — | 1 | 4.77 |
| CHEMBL109736 | — | — | 1 | 4.72 |
| CHEMBL325418 | — | — | 1 | 4.60 |
| CHEMBL110794 | — | — | 1 | 4.51 |
| CHEMBL444061 | — | — | 1 | 4.50 |
| CHEMBL331375 | — | — | 1 | 4.47 |
| CHEMBL322935 | — | — | 1 | 4.46 |
| CHEMBL114084 | — | — | 1 | 4.46 |
| CHEMBL326951 | — | — | 1 | 4.46 |
| CHEMBL113184 | — | — | 1 | 4.46 |
| CHEMBL112347 | — | — | 1 | 4.32 |
| CHEMBL112325 | — | — | 1 | 4.14 |
| CHEMBL321852 | — | — | 1 | 4.11 |
| CHEMBL324301 | — | — | 1 | - |
| CHEMBL113494 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL113611 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL326191 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL110366 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL113529 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL112685 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL112832 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL113379 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL419211 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL325444 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL558148 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL326690 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL331577 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL326719 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL113400 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL109736 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL325418 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL110794 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL444061 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL331375 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL322935 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL114084 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL326951 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL113184 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL112347 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL112325 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL321852 | — | IC50 | = | 77000.0 | nM | 4.11 |
| CHEMBL324301 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL113494 | — | IC50 | > | 100000.0 | nM | - |