Assay Detail
Binding
CHEMBL3097489
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis
29
Total Activities
29
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
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 6.25 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3094369 | — | — | 1 | 7.72 |
| CHEMBL3094368 | — | — | 1 | 7.70 |
| CHEMBL62136 | T091317 | — | 1 | 7.27 |
| CHEMBL3094367 | — | — | 1 | 7.21 |
| CHEMBL3094366 | — | — | 1 | 7.00 |
| CHEMBL2326845 | — | — | 1 | 6.72 |
| CHEMBL3094384 | — | — | 1 | 6.05 |
| CHEMBL3094365 | — | — | 1 | 6.04 |
| CHEMBL3094388 | — | — | 1 | 6.04 |
| CHEMBL3094370 | — | — | 1 | 6.00 |
| CHEMBL3094373 | — | — | 1 | 6.00 |
| CHEMBL3094385 | — | — | 1 | 5.40 |
| CHEMBL3094378 | — | — | 1 | 5.40 |
| CHEMBL205937 | — | — | 1 | 5.30 |
| CHEMBL3094379 | — | — | 1 | 5.10 |
| CHEMBL3094380 | — | — | 1 | 5.05 |
| CHEMBL3094387 | — | — | 1 | - |
| CHEMBL3094375 | — | — | 1 | - |
| CHEMBL3094374 | — | — | 1 | - |
| CHEMBL3094383 | — | — | 1 | - |
| CHEMBL3094372 | — | — | 1 | - |
| CHEMBL3094371 | — | — | 1 | - |
| CHEMBL3094376 | — | — | 1 | - |
| CHEMBL3094377 | — | — | 1 | - |
| CHEMBL382792 | — | — | 1 | - |
| CHEMBL389979 | — | — | 1 | - |
| CHEMBL3094381 | — | — | 1 | - |
| CHEMBL3094382 | — | — | 1 | - |
| CHEMBL3094386 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3094369 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3094368 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL62136 | T091317 | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3094367 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3094366 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2326845 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3094384 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3094365 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3094388 | — | EC50 | = | 911.0 | nM | 6.04 |
| CHEMBL3094370 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3094373 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3094385 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3094378 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL205937 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3094379 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3094380 | — | EC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3094387 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094375 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094374 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094383 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094372 | — | EC50 | > | 2000.0 | nM | - |
| CHEMBL3094371 | — | EC50 | - | — | - | |
| CHEMBL3094376 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094377 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL382792 | — | EC50 | - | — | - | |
| CHEMBL389979 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094381 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094382 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL3094386 | — | EC50 | > | 10000.0 | nM | - |