Assay Detail
Binding
CHEMBL4047019
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Displacement of [3H]E2 from GST-fused ERbeta-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method
10
Total Activities
10
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
Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.54 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.80 |
| CHEMBL83 | TAMOXIFEN | 4.0 | 1 | 7.10 |
| CHEMBL4087989 | — | — | 1 | 6.81 |
| CHEMBL4088694 | — | — | 1 | 6.51 |
| CHEMBL4092300 | — | — | 1 | 6.03 |
| CHEMBL4094003 | — | — | 1 | 5.77 |
| CHEMBL4105062 | — | — | 1 | 5.70 |
| CHEMBL4071813 | — | — | 1 | 5.60 |
| CHEMBL4066690 | — | — | 1 | - |
| CHEMBL4071506 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 1.59 | nM | 8.80 |
| CHEMBL83 | TAMOXIFEN | IC50 | = | 79.7 | nM | 7.10 |
| CHEMBL4087989 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4088694 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4092300 | — | IC50 | = | 939.0 | nM | 6.03 |
| CHEMBL4094003 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL4105062 | — | IC50 | = | 1977.0 | nM | 5.70 |
| CHEMBL4071813 | — | IC50 | = | 2525.0 | nM | 5.60 |
| CHEMBL4066690 | — | IC50 | - | — | - | |
| CHEMBL4071506 | — | IC50 | - | — | - |