Assay Detail
Binding
CHEMBL675748
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In vitro ability to inhibit specific [125I]ET1 binding to porcine kidney (inner medulla) membranes Endothelin B receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.16 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 6.96 |
| CHEMBL298725 | — | — | 1 | 6.80 |
| CHEMBL51234 | — | — | 1 | 6.75 |
| CHEMBL276362 | — | — | 1 | 6.66 |
| CHEMBL295483 | — | — | 1 | 6.58 |
| CHEMBL300201 | — | — | 1 | 6.54 |
| CHEMBL25438 | PD-156707 SODIUM | — | 1 | 6.47 |
| CHEMBL48907 | — | — | 1 | 6.47 |
| CHEMBL301577 | — | — | 1 | 6.47 |
| CHEMBL299328 | — | — | 1 | 6.40 |
| CHEMBL49675 | — | — | 1 | 6.34 |
| CHEMBL48411 | — | — | 1 | 6.32 |
| CHEMBL48315 | — | — | 1 | 6.26 |
| CHEMBL431160 | — | — | 1 | 6.09 |
| CHEMBL51890 | — | — | 1 | 6.00 |
| CHEMBL48881 | — | — | 1 | 5.92 |
| CHEMBL262000 | — | — | 1 | 5.85 |
| CHEMBL52535 | — | — | 1 | 5.82 |
| CHEMBL52338 | — | — | 1 | 5.80 |
| CHEMBL301971 | — | — | 1 | 5.75 |
| CHEMBL299572 | — | — | 1 | 5.75 |
| CHEMBL433090 | — | — | 1 | 5.72 |
| CHEMBL299521 | — | — | 1 | 5.54 |
| CHEMBL51030 | — | — | 1 | 5.50 |
| CHEMBL51530 | — | — | 1 | 5.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL298725 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL51234 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL276362 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL295483 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL300201 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL25438 | PD-156707 SODIUM | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL48907 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL301577 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL299328 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL49675 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL48411 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL48315 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL431160 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL51890 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL48881 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL262000 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL52535 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL52338 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL301971 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL299572 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL433090 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL299521 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL51030 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL51530 | — | IC50 | = | 4550.0 | nM | 5.34 |