Assay Detail
Binding
CHEMBL4393300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to GST-tagged human ER alpha ligand-binding domain by TR-FRET assay
31
Total Activities
31
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 relationship study of estrogen receptor down-regulators with a diphenylmethane skeleton.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.39 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL149791 | — | — | 1 | 10.22 |
| CHEMBL2403356 | — | — | 1 | 8.89 |
| CHEMBL2403355 | — | — | 1 | 8.85 |
| CHEMBL4473971 | — | — | 1 | 8.77 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 8.68 |
| CHEMBL2403361 | — | — | 1 | 8.23 |
| CHEMBL4459248 | — | — | 1 | 8.12 |
| CHEMBL4538877 | — | — | 1 | 7.66 |
| CHEMBL1782331 | — | — | 1 | 7.62 |
| CHEMBL2403357 | — | — | 1 | 7.58 |
| CHEMBL4585080 | — | — | 1 | 7.43 |
| CHEMBL4531047 | — | — | 1 | 7.37 |
| CHEMBL4103516 | — | — | 1 | 7.28 |
| CHEMBL4449497 | — | — | 1 | 7.11 |
| CHEMBL4449028 | — | — | 1 | 7.05 |
| CHEMBL2403362 | — | — | 1 | 7.00 |
| CHEMBL4469862 | — | — | 1 | 7.00 |
| CHEMBL2392777 | — | — | 1 | 6.88 |
| CHEMBL4524860 | — | — | 1 | 6.80 |
| CHEMBL2403360 | — | — | 1 | 6.55 |
| CHEMBL4585892 | — | — | 1 | 6.52 |
| CHEMBL4571357 | — | — | 1 | 6.45 |
| CHEMBL418971 | BISPHENOL A | — | 1 | 6.30 |
| CHEMBL2403354 | — | — | 1 | 6.10 |
| CHEMBL2403363 | — | — | 1 | 5.89 |
| CHEMBL138061 | — | — | 1 | 5.85 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | - |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | - |
| CHEMBL141305 | CYCLOFENIL | 4.0 | 1 | - |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL149791 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL2403356 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2403355 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4473971 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2403361 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4459248 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4538877 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1782331 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2403357 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4585080 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4531047 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4103516 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4449497 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4449028 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2403362 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4469862 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2392777 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4524860 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2403360 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4585892 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL4571357 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL418971 | BISPHENOL A | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL2403354 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2403363 | — | IC50 | = | 1279.0 | nM | 5.89 |
| CHEMBL138061 | — | IC50 | = | 1427.0 | nM | 5.85 |
| CHEMBL81 | RALOXIFENE | IC50 | - | — | - | |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | - | — | - | |
| CHEMBL141305 | CYCLOFENIL | IC50 | - | — | - | |
| CHEMBL1358 | FULVESTRANT | IC50 | - | — | - | |
| CHEMBL135 | ESTRADIOL | IC50 | - | — | - |