Assay Detail
Binding
CHEMBL4393302
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcriptional activity by luciferase reporter gene assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 7.33 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 9.74 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 9.11 |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | 9.10 |
| CHEMBL149791 | — | — | 1 | 8.48 |
| CHEMBL2403356 | — | — | 1 | 8.31 |
| CHEMBL4473971 | — | — | 1 | 8.09 |
| CHEMBL2403357 | — | — | 1 | 7.85 |
| CHEMBL2403355 | — | — | 1 | 7.60 |
| CHEMBL141305 | CYCLOFENIL | 4.0 | 1 | 7.57 |
| CHEMBL4531047 | — | — | 1 | 7.51 |
| CHEMBL4103516 | — | — | 1 | 7.44 |
| CHEMBL4538877 | — | — | 1 | 7.36 |
| CHEMBL2403362 | — | — | 1 | 7.10 |
| CHEMBL1782331 | — | — | 1 | 7.07 |
| CHEMBL4469862 | — | — | 1 | 7.03 |
| CHEMBL2403361 | — | — | 1 | 7.00 |
| CHEMBL4449028 | — | — | 1 | 7.00 |
| CHEMBL4459248 | — | — | 1 | 6.68 |
| CHEMBL4449497 | — | — | 1 | 6.67 |
| CHEMBL4571357 | — | — | 1 | 6.67 |
| CHEMBL2403360 | — | — | 1 | 6.63 |
| CHEMBL2403363 | — | — | 1 | 6.31 |
| CHEMBL4585080 | — | — | 1 | 6.28 |
| CHEMBL4585892 | — | — | 1 | 6.25 |
| CHEMBL2392777 | — | — | 1 | 5.92 |
| CHEMBL4524860 | — | — | 1 | 5.92 |
| CHEMBL2403354 | — | — | 1 | - |
| CHEMBL418971 | BISPHENOL A | — | 1 | - |
| CHEMBL138061 | — | — | 1 | - |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL81 | RALOXIFENE | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL1358 | FULVESTRANT | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL489 | AFIMOXIFENE | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL149791 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2403356 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL4473971 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL2403357 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2403355 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL141305 | CYCLOFENIL | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4531047 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4103516 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4538877 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL2403362 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1782331 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4469862 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2403361 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4449028 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4459248 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4449497 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4571357 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL2403360 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL2403363 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL4585080 | — | IC50 | = | 522.0 | nM | 6.28 |
| CHEMBL4585892 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL2392777 | — | IC50 | = | 1198.0 | nM | 5.92 |
| CHEMBL4524860 | — | IC50 | = | 1198.0 | nM | 5.92 |
| CHEMBL2403354 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL418971 | BISPHENOL A | IC50 | > | 10000.0 | nM | - |
| CHEMBL138061 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL411 | DIETHYLSTILBESTROL | IC50 | - | — | - | |
| CHEMBL135 | ESTRADIOL | IC50 | - | — | - |