Assay Detail
Binding
CHEMBL3607383
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Inverse agonist activity at APC-labeled RORgammat-LBD (unknown origin) assessed as inhibition of europium-labeled SRC1 recruitment after 1 hr by dual FRET analysis
30
Total Activities
15
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 | 15 | 7.29 | 8.10 |
| Imax | 15 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3605084 | — | — | 2 | 8.10 |
| CHEMBL3605081 | — | — | 2 | 7.90 |
| CHEMBL3605088 | — | — | 2 | 7.90 |
| CHEMBL3605090 | — | — | 2 | 7.90 |
| CHEMBL3605082 | — | — | 2 | 7.80 |
| CHEMBL3605085 | — | — | 2 | 7.70 |
| CHEMBL3605086 | — | — | 2 | 7.70 |
| CHEMBL3605092 | — | — | 2 | 7.70 |
| CHEMBL3314014 | — | — | 2 | 7.70 |
| CHEMBL3605089 | — | — | 2 | 7.50 |
| CHEMBL3605087 | — | — | 2 | 7.40 |
| CHEMBL3605091 | — | — | 2 | 6.40 |
| CHEMBL3105815 | — | — | 2 | 6.00 |
| CHEMBL3605078 | — | — | 2 | 5.90 |
| CHEMBL3605077 | — | — | 2 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3605084 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3605081 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3605088 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3605090 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3605082 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3314014 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3605092 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3605085 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3605086 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3605089 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3605087 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3605091 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3105815 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3605078 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3605077 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3105815 | — | Imax | = | 91.0 | % | - |
| CHEMBL3605077 | — | Imax | = | 58.0 | % | - |
| CHEMBL3605078 | — | Imax | = | 76.0 | % | - |
| CHEMBL3605081 | — | Imax | = | 58.0 | % | - |
| CHEMBL3605082 | — | Imax | = | 52.0 | % | - |
| CHEMBL3605084 | — | Imax | = | 31.0 | % | - |
| CHEMBL3605085 | — | Imax | = | 60.0 | % | - |
| CHEMBL3605086 | — | Imax | = | 45.0 | % | - |
| CHEMBL3605087 | — | Imax | = | 57.0 | % | - |
| CHEMBL3605088 | — | Imax | = | 52.0 | % | - |
| CHEMBL3605089 | — | Imax | = | 53.0 | % | - |
| CHEMBL3605090 | — | Imax | = | 40.0 | % | - |
| CHEMBL3605091 | — | Imax | = | 85.0 | % | - |
| CHEMBL3605092 | — | Imax | = | 79.0 | % | - |
| CHEMBL3314014 | — | Imax | = | 61.0 | % | - |