Assay Detail
Binding
CHEMBL3242033
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Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.32 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3234259 | — | — | 1 | 7.70 |
| CHEMBL3234255 | — | — | 1 | 7.40 |
| CHEMBL3234251 | — | — | 1 | 7.30 |
| CHEMBL1494527 | — | — | 1 | 7.10 |
| CHEMBL3234252 | — | — | 1 | 7.05 |
| CHEMBL3234256 | — | — | 1 | 7.05 |
| CHEMBL3234030 | — | — | 1 | 6.82 |
| CHEMBL3234246 | — | — | 1 | 6.82 |
| CHEMBL3234248 | — | — | 1 | 6.75 |
| CHEMBL3234247 | — | — | 1 | 6.70 |
| CHEMBL3234241 | — | — | 1 | 6.54 |
| CHEMBL3234262 | — | — | 1 | 6.39 |
| CHEMBL3234240 | — | — | 1 | 6.39 |
| CHEMBL2137199 | — | — | 1 | 6.38 |
| CHEMBL3234034 | — | — | 1 | 6.26 |
| CHEMBL3234253 | — | — | 1 | 6.23 |
| CHEMBL169 | URSOLIC ACID | 2.0 | 1 | 5.97 |
| CHEMBL3234263 | — | — | 1 | 5.97 |
| CHEMBL3234025 | — | — | 1 | 5.87 |
| CHEMBL3234249 | — | — | 1 | 5.47 |
| CHEMBL62136 | T091317 | — | 1 | 5.46 |
| CHEMBL3234285 | — | — | 1 | 5.29 |
| CHEMBL3234024 | — | — | 1 | 5.12 |
| CHEMBL3234257 | — | — | 1 | 5.00 |
| CHEMBL3234027 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3234259 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3234255 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3234251 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1494527 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3234252 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3234256 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3234030 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3234246 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3234248 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3234247 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3234241 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3234262 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3234240 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2137199 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3234034 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3234253 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL169 | URSOLIC ACID | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL3234263 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL3234025 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL3234249 | — | IC50 | = | 3390.0 | nM | 5.47 |
| CHEMBL62136 | T091317 | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3234285 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL3234024 | — | IC50 | = | 7560.0 | nM | 5.12 |
| CHEMBL3234257 | — | IC50 | = | 9980.0 | nM | 5.00 |
| CHEMBL3234027 | — | IC50 | = | 12760.0 | nM | 4.89 |