Assay Detail
Binding
CHEMBL4681572
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Binding affinity to GST-tagged ERRgamma LBD (unknown origin) using fluorescein PGC1alpha as coactivator incubated for 1 hr by LanthaScreen TR-FRET co-regulator assay
45
Total Activities
45
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
Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 45 | 6.34 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4757503 | — | — | 1 | 7.70 |
| CHEMBL4744529 | — | — | 1 | 7.58 |
| CHEMBL4791981 | — | — | 1 | 7.52 |
| CHEMBL4792390 | — | — | 1 | 7.47 |
| CHEMBL4764979 | — | — | 1 | 7.30 |
| CHEMBL4791571 | — | — | 1 | 7.19 |
| CHEMBL4756698 | — | — | 1 | 7.17 |
| CHEMBL4747616 | — | — | 1 | 7.16 |
| CHEMBL4783287 | — | — | 1 | 7.10 |
| CHEMBL4764628 | — | — | 1 | 7.08 |
| CHEMBL4742785 | — | — | 1 | 7.04 |
| CHEMBL4760692 | — | — | 1 | 7.03 |
| CHEMBL4759824 | — | — | 1 | 6.97 |
| CHEMBL201013 | — | — | 1 | 6.96 |
| CHEMBL4751445 | — | — | 1 | 6.78 |
| CHEMBL4764022 | — | — | 1 | 6.61 |
| CHEMBL4745603 | — | — | 1 | 6.57 |
| CHEMBL4790844 | — | — | 1 | 6.53 |
| CHEMBL4785294 | — | — | 1 | 6.50 |
| CHEMBL4760430 | — | — | 1 | 6.49 |
| CHEMBL4757562 | — | — | 1 | 6.34 |
| CHEMBL4750108 | — | — | 1 | 6.11 |
| CHEMBL4747810 | — | — | 1 | 6.09 |
| CHEMBL4789507 | — | — | 1 | 6.05 |
| CHEMBL4790063 | — | — | 1 | 5.98 |
| CHEMBL4782385 | — | — | 1 | 5.96 |
| CHEMBL4742330 | — | — | 1 | 5.90 |
| CHEMBL4785673 | — | — | 1 | 5.89 |
| CHEMBL4788812 | — | — | 1 | 5.82 |
| CHEMBL4793778 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4757503 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4744529 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4791981 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4792390 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4764979 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4791571 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4756698 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4747616 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4783287 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4764628 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4742785 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4760692 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4759824 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL201013 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4751445 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4764022 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4745603 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL4790844 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL4785294 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL4760430 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4757562 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4750108 | — | IC50 | = | 784.0 | nM | 6.11 |
| CHEMBL4747810 | — | IC50 | = | 813.0 | nM | 6.09 |
| CHEMBL4789507 | — | IC50 | = | 894.0 | nM | 6.05 |
| CHEMBL4790063 | — | IC50 | = | 1044.0 | nM | 5.98 |
| CHEMBL4782385 | — | IC50 | = | 1089.0 | nM | 5.96 |
| CHEMBL4742330 | — | IC50 | = | 1256.0 | nM | 5.90 |
| CHEMBL4785673 | — | IC50 | = | 1281.0 | nM | 5.89 |
| CHEMBL4788812 | — | IC50 | = | 1522.0 | nM | 5.82 |
| CHEMBL4793778 | — | IC50 | = | 1546.0 | nM | 5.81 |
| CHEMBL4762231 | — | IC50 | = | 1657.0 | nM | 5.78 |
| CHEMBL4753234 | — | IC50 | = | 2131.0 | nM | 5.67 |
| CHEMBL4748869 | — | IC50 | = | 2205.0 | nM | 5.66 |
| CHEMBL4781743 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL4745913 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4757449 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4795473 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4793939 | — | IC50 | = | 3610.0 | nM | 5.44 |
| CHEMBL4800141 | — | IC50 | = | 6295.0 | nM | 5.20 |
| CHEMBL4747466 | — | IC50 | = | 7416.0 | nM | 5.13 |
| CHEMBL4787770 | — | IC50 | = | 8015.0 | nM | 5.10 |
| CHEMBL4794943 | — | IC50 | = | 8233.0 | nM | 5.08 |
| CHEMBL4754948 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4800204 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4789561 | — | IC50 | > | 10000.0 | nM | - |