Assay Detail
Binding
CHEMBL3757818
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 4-[(benzimidazol-1-yl) methyl]biphenyl-2-amides as dual angiotensin II and endothelin A receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.87 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 8.08 |
| CHEMBL3753406 | — | — | 1 | 8.00 |
| CHEMBL3752680 | — | — | 1 | 6.90 |
| CHEMBL3752947 | — | — | 1 | 6.78 |
| CHEMBL3753134 | — | — | 1 | 6.20 |
| CHEMBL3751899 | — | — | 1 | 6.05 |
| CHEMBL3753458 | — | — | 1 | 5.16 |
| CHEMBL3753888 | — | — | 1 | 5.15 |
| CHEMBL3752117 | — | — | 1 | 5.14 |
| CHEMBL3751986 | — | — | 1 | 5.04 |
| CHEMBL3751994 | — | — | 1 | 5.00 |
| CHEMBL3753277 | — | — | 1 | 4.96 |
| CHEMBL3752145 | — | — | 1 | 4.89 |
| CHEMBL3752444 | — | — | 1 | 4.85 |
| CHEMBL3752198 | — | — | 1 | - |
| CHEMBL3753007 | — | — | 1 | - |
| CHEMBL3754267 | — | — | 1 | - |
| CHEMBL3754661 | — | — | 1 | - |
| CHEMBL3754198 | — | — | 1 | - |
| CHEMBL3752530 | — | — | 1 | - |
| CHEMBL3752160 | — | — | 1 | - |
| CHEMBL3754394 | — | — | 1 | - |
| CHEMBL3753047 | — | — | 1 | - |
| CHEMBL3754010 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL957 | BOSENTAN | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL3753406 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3752680 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3752947 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3753134 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL3751899 | — | IC50 | = | 886.0 | nM | 6.05 |
| CHEMBL3753458 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3753888 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3752117 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL3751986 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL3751994 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3753277 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3752145 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL3752444 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3752198 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3753007 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3754267 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3754661 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3754198 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3752530 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3752160 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3754394 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3753047 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3754010 | — | IC50 | > | 20000.0 | nM | - |