Assay Detail
Binding
CHEMBL5044069
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human APC-labeled RORgammat LBD (262 to 518 residues) transfected in Escherichia coli BL21 (DE3) assessed as biotinylated SRC recruitment incubated for 1 hr by dual FRET assay
10
Total Activities
10
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 of Orally Available Retinoic Acid Receptor-Related Orphan Receptor γ-t/Dihydroorotate Dehydrogenase Dual Inhibitors for the Treatment of Refractory Inflammatory Bowel Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.92 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3609408 | — | — | 1 | 8.00 |
| CHEMBL5075214 | — | — | 1 | 6.83 |
| CHEMBL5093830 | — | — | 1 | 6.68 |
| CHEMBL62136 | T091317 | — | 1 | 6.62 |
| CHEMBL5086318 | — | — | 1 | 6.49 |
| CHEMBL5075277 | — | — | 1 | - |
| CHEMBL5082345 | — | — | 1 | - |
| CHEMBL5086624 | — | — | 1 | - |
| CHEMBL5085951 | — | — | 1 | - |
| CHEMBL5089276 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3609408 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5075214 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5093830 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL62136 | T091317 | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL5086318 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL5075277 | — | IC50 | - | — | - | |
| CHEMBL5082345 | — | IC50 | - | — | - | |
| CHEMBL5086624 | — | IC50 | - | — | - | |
| CHEMBL5085951 | — | IC50 | - | — | - | |
| CHEMBL5089276 | — | IC50 | - | — | - |