Assay Detail
Binding
CHEMBL4393303
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Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation 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 |
|---|---|---|---|
| EC50 | 31 | 7.35 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 10.05 |
| CHEMBL411 | DIETHYLSTILBESTROL | 4.0 | 1 | 9.96 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 9.18 |
| CHEMBL149791 | — | — | 1 | 9.00 |
| CHEMBL1358 | FULVESTRANT | 4.0 | 1 | 8.85 |
| CHEMBL4473971 | — | — | 1 | 8.05 |
| CHEMBL2403356 | — | — | 1 | 8.00 |
| CHEMBL141305 | CYCLOFENIL | 4.0 | 1 | 7.58 |
| CHEMBL2403355 | — | — | 1 | 7.55 |
| CHEMBL2403361 | — | — | 1 | 7.19 |
| CHEMBL4449497 | — | — | 1 | 7.10 |
| CHEMBL2403357 | — | — | 1 | 7.06 |
| CHEMBL4538877 | — | — | 1 | 7.03 |
| CHEMBL4531047 | — | — | 1 | 6.98 |
| CHEMBL4449028 | — | — | 1 | 6.94 |
| CHEMBL1782331 | — | — | 1 | 6.74 |
| CHEMBL4585892 | — | — | 1 | 6.71 |
| CHEMBL4469862 | — | — | 1 | 6.69 |
| CHEMBL4524860 | — | — | 1 | 6.37 |
| CHEMBL4585080 | — | — | 1 | 6.36 |
| CHEMBL4459248 | — | — | 1 | 6.26 |
| CHEMBL2403362 | — | — | 1 | 6.22 |
| CHEMBL2403360 | — | — | 1 | 6.14 |
| CHEMBL2392777 | — | — | 1 | 5.86 |
| CHEMBL418971 | BISPHENOL A | — | 1 | 5.77 |
| CHEMBL4103516 | — | — | 1 | - |
| CHEMBL489 | AFIMOXIFENE | 3.0 | 1 | - |
| CHEMBL4571357 | — | — | 1 | - |
| CHEMBL138061 | — | — | 1 | - |
| CHEMBL2403363 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.09 | nM | 10.05 |
| CHEMBL411 | DIETHYLSTILBESTROL | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL81 | RALOXIFENE | EC50 | = | 0.66 | nM | 9.18 |
| CHEMBL149791 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1358 | FULVESTRANT | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4473971 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2403356 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL141305 | CYCLOFENIL | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2403355 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2403361 | — | EC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4449497 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2403357 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4538877 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4531047 | — | EC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4449028 | — | EC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1782331 | — | EC50 | = | 181.0 | nM | 6.74 |
| CHEMBL4585892 | — | EC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4469862 | — | EC50 | = | 204.0 | nM | 6.69 |
| CHEMBL4524860 | — | EC50 | = | 427.0 | nM | 6.37 |
| CHEMBL4585080 | — | EC50 | = | 437.0 | nM | 6.36 |
| CHEMBL4459248 | — | EC50 | = | 545.0 | nM | 6.26 |
| CHEMBL2403362 | — | EC50 | = | 606.0 | nM | 6.22 |
| CHEMBL2403360 | — | EC50 | = | 729.0 | nM | 6.14 |
| CHEMBL2392777 | — | EC50 | = | 1382.0 | nM | 5.86 |
| CHEMBL418971 | BISPHENOL A | EC50 | = | 1689.0 | nM | 5.77 |
| CHEMBL4103516 | — | EC50 | - | — | - | |
| CHEMBL489 | AFIMOXIFENE | EC50 | - | — | - | |
| CHEMBL4571357 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL138061 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2403363 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2403354 | — | EC50 | > | 10000.0 | nM | - |