Assay Detail
Binding
CHEMBL3607381
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at APC-labeled RORgammat-LBD (unknown origin) assessed as inhibition of N-(2-chloro-6-fluorobenzyl)-N-((2'-methoxy-[1,1'-biphenyl]-4-yl)-methyl)benzenesulfonamide-induced europium-labeled SRC1 recruitment after 1 hr by FRET analysis
36
Total Activities
18
Compounds Tested
2
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 N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.68 | 8.00 |
| Imax | 18 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3314014 | — | — | 2 | 8.00 |
| CHEMBL3605092 | — | — | 2 | 7.50 |
| CHEMBL3605090 | — | — | 2 | 7.30 |
| CHEMBL3605089 | — | — | 2 | 7.20 |
| CHEMBL3605083 | — | — | 2 | 7.20 |
| CHEMBL3605082 | — | — | 2 | 7.10 |
| CHEMBL3605081 | — | — | 2 | 7.00 |
| CHEMBL3605085 | — | — | 2 | 6.80 |
| CHEMBL3605079 | — | — | 2 | 6.80 |
| CHEMBL3605084 | — | — | 2 | 6.80 |
| CHEMBL3605088 | — | — | 2 | 6.70 |
| CHEMBL3605087 | — | — | 2 | 6.60 |
| CHEMBL3605086 | — | — | 2 | 6.50 |
| CHEMBL3105815 | — | — | 2 | 6.00 |
| CHEMBL3605080 | — | — | 2 | 5.90 |
| CHEMBL3605091 | — | — | 2 | 5.90 |
| CHEMBL3605078 | — | — | 2 | 5.60 |
| CHEMBL3605077 | — | — | 2 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3314014 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3605092 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3605090 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3605089 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3605083 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3605082 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL3605081 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3605085 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3605084 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3605079 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3605088 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3605087 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3605086 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3105815 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3605080 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3605091 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3605078 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3605077 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3105815 | — | Imax | = | 116.0 | % | - |
| CHEMBL3605077 | — | Imax | = | 79.0 | % | - |
| CHEMBL3605078 | — | Imax | = | 115.0 | % | - |
| CHEMBL3605079 | — | Imax | = | 56.0 | % | - |
| CHEMBL3605080 | — | Imax | = | 46.0 | % | - |
| CHEMBL3605081 | — | Imax | = | 112.0 | % | - |
| CHEMBL3605082 | — | Imax | = | 101.0 | % | - |
| CHEMBL3605083 | — | Imax | = | 49.0 | % | - |
| CHEMBL3605084 | — | Imax | = | 91.0 | % | - |
| CHEMBL3605085 | — | Imax | = | 117.0 | % | - |
| CHEMBL3605086 | — | Imax | = | 97.0 | % | - |
| CHEMBL3605087 | — | Imax | = | 115.0 | % | - |
| CHEMBL3605088 | — | Imax | = | 106.0 | % | - |
| CHEMBL3605089 | — | Imax | = | 107.0 | % | - |
| CHEMBL3605090 | — | Imax | = | 98.0 | % | - |
| CHEMBL3605091 | — | Imax | = | 120.0 | % | - |
| CHEMBL3605092 | — | Imax | = | 111.0 | % | - |
| CHEMBL3314014 | — | Imax | = | 110.0 | % | - |