Assay Detail
Binding
CHEMBL3857086
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of fluorescien-conjugated coactivator PGC1a binding to GST-tagged human ERRgamma LBD after 1 hr by TR-FRET assay
28
Total Activities
28
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
Synthesis and biological evaluation of novel 4-hydroxytamoxifen analogs as estrogen-related receptor gamma inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.24 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3961676 | — | — | 1 | 7.70 |
| CHEMBL3897416 | — | — | 1 | 7.05 |
| CHEMBL3932162 | — | — | 1 | 6.96 |
| CHEMBL3978054 | — | — | 1 | 6.93 |
| CHEMBL3957546 | — | — | 1 | 6.75 |
| CHEMBL3968559 | — | — | 1 | 6.72 |
| CHEMBL3973526 | — | — | 1 | 6.57 |
| CHEMBL3891326 | — | — | 1 | 6.32 |
| CHEMBL3956562 | — | — | 1 | 6.32 |
| CHEMBL3982516 | — | — | 1 | 6.30 |
| CHEMBL3940124 | — | — | 1 | 6.28 |
| CHEMBL3965511 | — | — | 1 | 6.05 |
| CHEMBL3893563 | — | — | 1 | 6.00 |
| CHEMBL3953814 | — | — | 1 | 5.96 |
| CHEMBL3904163 | — | — | 1 | 5.89 |
| CHEMBL3986248 | — | — | 1 | 5.82 |
| CHEMBL3969681 | — | — | 1 | 5.41 |
| CHEMBL3952876 | — | — | 1 | 5.28 |
| CHEMBL3908431 | — | — | 1 | 5.25 |
| CHEMBL3916962 | — | — | 1 | 5.17 |
| CHEMBL3919418 | — | — | 1 | - |
| CHEMBL3944120 | — | — | 1 | - |
| CHEMBL3916169 | — | — | 1 | - |
| CHEMBL3981543 | — | — | 1 | - |
| CHEMBL3944236 | — | — | 1 | - |
| CHEMBL3962561 | — | — | 1 | - |
| CHEMBL3911541 | — | — | 1 | - |
| CHEMBL3902534 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3961676 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3897416 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3932162 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3978054 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL3957546 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3968559 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3973526 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3891326 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3956562 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3982516 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3940124 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3965511 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL3893563 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3953814 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3904163 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3986248 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3969681 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3952876 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3908431 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3916962 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL3919418 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3944120 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3916169 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3981543 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3944236 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3962561 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3911541 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3902534 | — | IC50 | > | 10000.0 | nM | - |