Assay Detail
Binding
CHEMBL4667416
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Inverse agonist activity at pSG5GAL4-DBD/LBD fused human RORgamma receptor expressed in COS7 cells co-expressing 5 copies of GAL4 response element after 18 hrs by luciferase reporter gene based assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 6.30 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4779716 | — | — | 1 | 7.00 |
| CHEMBL4795788 | — | — | 1 | 6.80 |
| CHEMBL4787298 | — | — | 1 | 6.77 |
| CHEMBL4752983 | — | — | 1 | 6.77 |
| CHEMBL4745208 | — | — | 1 | 6.66 |
| CHEMBL4786942 | — | — | 1 | 6.66 |
| CHEMBL4763038 | — | — | 1 | 6.66 |
| CHEMBL4779432 | — | — | 1 | 6.60 |
| CHEMBL4763421 | — | — | 1 | 6.50 |
| CHEMBL4779817 | — | — | 1 | 6.46 |
| CHEMBL4776309 | — | — | 1 | 6.41 |
| CHEMBL4740086 | — | — | 1 | 6.36 |
| CHEMBL4751554 | — | — | 1 | 6.28 |
| CHEMBL4800301 | — | — | 1 | 6.20 |
| CHEMBL4788490 | — | — | 1 | 6.12 |
| CHEMBL4749883 | — | — | 1 | 6.09 |
| CHEMBL4792595 | — | — | 1 | 6.06 |
| CHEMBL4760072 | — | — | 1 | 6.05 |
| CHEMBL4747263 | — | — | 1 | 6.04 |
| CHEMBL4763665 | — | — | 1 | 6.03 |
| CHEMBL4759286 | — | — | 1 | 6.02 |
| CHEMBL2326845 | — | — | 1 | 5.97 |
| CHEMBL4745812 | — | — | 1 | 5.87 |
| CHEMBL4752056 | — | — | 1 | 5.86 |
| CHEMBL4739928 | — | — | 1 | 5.82 |
| CHEMBL4782026 | — | — | 1 | 5.78 |
| CHEMBL4787560 | — | — | 1 | - |
| CHEMBL4786464 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4779716 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4795788 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4787298 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4752983 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4745208 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4786942 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4763038 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4779432 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4763421 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4779817 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4776309 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4740086 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4751554 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4800301 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4788490 | — | EC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4749883 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4792595 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4760072 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4747263 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4763665 | — | EC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4759286 | — | EC50 | = | 960.0 | nM | 6.02 |
| CHEMBL2326845 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4745812 | — | EC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL4752056 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL4739928 | — | EC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL4782026 | — | EC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4787560 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4786464 | — | EC50 | > | 10000.0 | nM | - |