Assay Detail
Binding
CHEMBL884979
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Transcriptional activation of estrogen receptor alpha in U2OS cell using estrogen-regulated luciferase reporter gene plasmid upon incubation for 20-30 mins at RT
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 8.05 | 10.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | 10.72 |
| CHEMBL306878 | — | — | 1 | 10.23 |
| CHEMBL69408 | — | — | 1 | 9.51 |
| CHEMBL371236 | — | — | 1 | 8.41 |
| CHEMBL48352 | — | — | 1 | 8.37 |
| CHEMBL380565 | — | — | 1 | 8.17 |
| CHEMBL26865 | — | — | 1 | 8.15 |
| CHEMBL199140 | — | — | 1 | 7.85 |
| CHEMBL197080 | — | — | 1 | 7.82 |
| CHEMBL364442 | — | — | 1 | 7.77 |
| CHEMBL197188 | — | — | 1 | 7.77 |
| CHEMBL383372 | — | — | 1 | 7.00 |
| CHEMBL372526 | — | — | 1 | 6.96 |
| CHEMBL371192 | — | — | 1 | 6.82 |
| CHEMBL370609 | — | — | 1 | 6.80 |
| CHEMBL198042 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL135 | ESTRADIOL | EC50 | = | 0.019 | nM | 10.72 |
| CHEMBL306878 | — | EC50 | = | 0.059 | nM | 10.23 |
| CHEMBL69408 | — | EC50 | = | 0.31 | nM | 9.51 |
| CHEMBL371236 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL48352 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL380565 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL26865 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL199140 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL197080 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL364442 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL197188 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL383372 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL372526 | — | EC50 | = | 109.0 | nM | 6.96 |
| CHEMBL371192 | — | EC50 | = | 152.0 | nM | 6.82 |
| CHEMBL370609 | — | EC50 | = | 158.0 | nM | 6.80 |
| CHEMBL198042 | — | EC50 | = | 427.0 | nM | 6.37 |