Assay Detail
Binding
CHEMBL4394436
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Inverse agonist activity at Gal4-fused FXR LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay
5
Total Activities
5
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
Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.90 | 5.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4465197 | — | — | 1 | 5.90 |
| CHEMBL4455520 | — | — | 1 | - |
| CHEMBL4537738 | — | — | 1 | - |
| CHEMBL4558865 | — | — | 1 | - |
| CHEMBL4439690 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4465197 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4455520 | — | IC50 | - | — | - | |
| CHEMBL4537738 | — | IC50 | - | — | - | |
| CHEMBL4558865 | — | IC50 | - | — | - | |
| CHEMBL4439690 | — | IC50 | - | — | - |