Assay Detail
Binding
CHEMBL4182853
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at Gal4-tagged human RORgammat ligand binding domain expressed in human Jurkat cells by native IL17 promoter driven luciferase reporter gene assay
38
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 38 | 6.69 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4214210 | — | — | 1 | 7.92 |
| CHEMBL4211051 | — | — | 2 | 7.82 |
| CHEMBL4215334 | — | — | 1 | 7.82 |
| CHEMBL4216643 | — | — | 1 | 7.55 |
| CHEMBL4214711 | — | — | 1 | 7.51 |
| CHEMBL4206368 | — | — | 3 | 7.50 |
| CHEMBL4212978 | — | — | 1 | 7.41 |
| CHEMBL4214055 | — | — | 1 | 7.33 |
| CHEMBL4205428 | — | — | 1 | 7.24 |
| CHEMBL4218626 | — | — | 1 | 7.10 |
| CHEMBL4209091 | — | — | 1 | 7.08 |
| CHEMBL4217890 | — | — | 1 | 7.03 |
| CHEMBL4209808 | — | — | 1 | 6.94 |
| CHEMBL4210034 | — | — | 1 | 6.78 |
| CHEMBL4210791 | — | — | 1 | 6.78 |
| CHEMBL4217418 | — | — | 1 | 6.77 |
| CHEMBL4206170 | — | — | 1 | 6.77 |
| CHEMBL4209665 | — | — | 1 | 6.71 |
| CHEMBL4212995 | — | — | 1 | 6.69 |
| CHEMBL4214020 | — | — | 1 | 6.65 |
| CHEMBL4212014 | — | — | 1 | 6.64 |
| CHEMBL4213493 | — | — | 1 | 6.62 |
| CHEMBL4212458 | — | — | 1 | 6.55 |
| CHEMBL62136 | T091317 | — | 1 | 6.48 |
| CHEMBL4210530 | — | — | 1 | 6.28 |
| CHEMBL4208087 | — | — | 1 | 6.22 |
| CHEMBL4206412 | — | — | 1 | 6.09 |
| CHEMBL4207135 | — | — | 1 | 5.90 |
| CHEMBL4213534 | — | — | 1 | 5.79 |
| CHEMBL4211266 | — | — | 1 | 5.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4214210 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4211051 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4215334 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4216643 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4214711 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4206368 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4212978 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4214055 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4205428 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4218626 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4209091 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4217890 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4206368 | — | EC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4209808 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4210034 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4210791 | — | EC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4217418 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4206170 | — | EC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4209665 | — | EC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4212995 | — | EC50 | = | 203.0 | nM | 6.69 |
| CHEMBL4214020 | — | EC50 | = | 225.0 | nM | 6.65 |
| CHEMBL4212014 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4213493 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4212458 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL62136 | T091317 | EC50 | = | 333.0 | nM | 6.48 |
| CHEMBL4210530 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4208087 | — | EC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4206412 | — | EC50 | = | 815.0 | nM | 6.09 |
| CHEMBL4207135 | — | EC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL4211051 | — | EC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL4213534 | — | EC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL4211266 | — | EC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4218423 | — | EC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4206368 | — | EC50 | = | 7380.0 | nM | 5.13 |
| CHEMBL4204747 | — | EC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4203724 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4205663 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4208603 | — | EC50 | > | 10000.0 | nM | - |