Assay Detail
Binding
CHEMBL2406174
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Antagonist activity at human Gal4-ERalpha assessed as inhibition of 17beta-estradiol-induced effect by reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationships of bisphenol A analogs at estrogen receptors (ERs): discovery of an ERα-selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.91 | 8.31 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403356 | — | — | 1 | 8.31 |
| CHEMBL2403357 | — | — | 1 | 7.85 |
| CHEMBL2403355 | — | — | 1 | 7.60 |
| CHEMBL2403349 | — | — | 1 | 7.14 |
| CHEMBL2403347 | — | — | 1 | 7.13 |
| CHEMBL2403362 | — | — | 1 | 7.10 |
| CHEMBL2403358 | — | — | 1 | 7.08 |
| CHEMBL1782331 | — | — | 1 | 7.07 |
| CHEMBL2403348 | — | — | 1 | 7.01 |
| CHEMBL2403361 | — | — | 1 | 7.00 |
| CHEMBL2403346 | — | — | 1 | 6.96 |
| CHEMBL1208076 | — | — | 1 | 6.77 |
| CHEMBL2403359 | — | — | 1 | 6.64 |
| CHEMBL2403360 | — | — | 1 | 6.64 |
| CHEMBL2403363 | — | — | 1 | 6.31 |
| CHEMBL1231453 | — | — | 1 | 6.28 |
| CHEMBL2392777 | — | — | 1 | 5.92 |
| CHEMBL2403351 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403356 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2403357 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2403355 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2403349 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2403347 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2403362 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2403358 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1782331 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2403348 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL2403361 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2403346 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1208076 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2403359 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2403360 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL2403363 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL1231453 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL2392777 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2403351 | — | IC50 | = | 2900.0 | nM | 5.54 |