Assay Detail
Binding
CHEMBL831663
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Inhibition of transcriptional activation by human estrogen receptor alpha
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
QSAR of estrogen receptor modulators: exploring selectivity requirements for ER(alpha) versus ER(beta) binding of tetrahydroisoquinoline derivatives using E-state and physicochemical parameters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.44 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328388 | — | — | 1 | 9.22 |
| CHEMBL100617 | — | — | 1 | 9.15 |
| CHEMBL328810 | — | — | 1 | 8.82 |
| CHEMBL101997 | — | — | 1 | 8.80 |
| CHEMBL98558 | — | — | 1 | 8.74 |
| CHEMBL101083 | — | — | 1 | 8.72 |
| CHEMBL101807 | — | — | 1 | 8.59 |
| CHEMBL98470 | — | — | 1 | 8.59 |
| CHEMBL319678 | — | — | 1 | 8.54 |
| CHEMBL174502 | — | — | 1 | 8.54 |
| CHEMBL319211 | — | — | 1 | 8.52 |
| CHEMBL103294 | — | — | 1 | 8.51 |
| CHEMBL100763 | — | — | 1 | 8.48 |
| CHEMBL327515 | — | — | 1 | 8.46 |
| CHEMBL103305 | — | — | 1 | 8.35 |
| CHEMBL100231 | — | — | 1 | 8.28 |
| CHEMBL316080 | — | — | 1 | 7.97 |
| CHEMBL100595 | — | — | 1 | 7.79 |
| CHEMBL101382 | — | — | 1 | 7.78 |
| CHEMBL323119 | — | — | 1 | 7.72 |
| CHEMBL434346 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328388 | — | IC50 | = | 0.5998 | nM | 9.22 |
| CHEMBL100617 | — | IC50 | = | 0.6998 | nM | 9.15 |
| CHEMBL328810 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL101997 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL98558 | — | IC50 | = | 1.799 | nM | 8.74 |
| CHEMBL101083 | — | IC50 | = | 1.901 | nM | 8.72 |
| CHEMBL101807 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL98470 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL319678 | — | IC50 | = | 2.897 | nM | 8.54 |
| CHEMBL174502 | — | IC50 | = | 2.897 | nM | 8.54 |
| CHEMBL319211 | — | IC50 | = | 2.999 | nM | 8.52 |
| CHEMBL103294 | — | IC50 | = | 3.097 | nM | 8.51 |
| CHEMBL100763 | — | IC50 | = | 3.304 | nM | 8.48 |
| CHEMBL327515 | — | IC50 | = | 3.499 | nM | 8.46 |
| CHEMBL103305 | — | IC50 | = | 4.498 | nM | 8.35 |
| CHEMBL100231 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL316080 | — | IC50 | = | 10.69 | nM | 7.97 |
| CHEMBL100595 | — | IC50 | = | 16.11 | nM | 7.79 |
| CHEMBL101382 | — | IC50 | = | 16.48 | nM | 7.78 |
| CHEMBL323119 | — | IC50 | = | 19.01 | nM | 7.72 |
| CHEMBL434346 | — | IC50 | = | 19.82 | nM | 7.70 |