Assay Detail
Binding
CHEMBL828092
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Inhibition of [3H]17-beta-estradiol binding to rat ER alpha expressed in Escherichia coli
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design and synthesis of aryl diphenolic azoles as potent and selective estrogen receptor-beta ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.53 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 8.72 |
| CHEMBL188528 | — | — | 1 | 6.88 |
| CHEMBL187207 | — | — | 1 | 6.77 |
| CHEMBL186513 | — | — | 1 | 6.44 |
| CHEMBL450940 | PRINABEREL | 2.0 | 1 | 6.21 |
| CHEMBL188882 | — | — | 1 | 6.14 |
| CHEMBL187673 | — | — | 1 | 6.09 |
| CHEMBL187392 | — | — | 1 | 5.89 |
| CHEMBL188230 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL188528 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL187207 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL186513 | — | IC50 | = | 362.0 | nM | 6.44 |
| CHEMBL450940 | PRINABEREL | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL188882 | — | IC50 | = | 716.0 | nM | 6.14 |
| CHEMBL187673 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL187392 | — | IC50 | = | 1295.0 | nM | 5.89 |
| CHEMBL188230 | — | IC50 | = | 2252.0 | nM | 5.65 |