Assay Detail
Binding
CHEMBL3607384
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Inverse agonist activity at RORgammat in mouse Th17 cells assessed as inhibition of IL-17 production after 3 days by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | Th17 |
| 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 | 12 | 6.10 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3314014 | — | — | 1 | 6.80 |
| CHEMBL3605083 | — | — | 1 | 6.60 |
| CHEMBL3605090 | — | — | 1 | 6.60 |
| CHEMBL3605092 | — | — | 1 | 6.40 |
| CHEMBL3605085 | — | — | 1 | 6.20 |
| CHEMBL3605082 | — | — | 1 | 6.00 |
| CHEMBL3605081 | — | — | 1 | 5.80 |
| CHEMBL3605084 | — | — | 1 | 5.80 |
| CHEMBL3605088 | — | — | 1 | 5.80 |
| CHEMBL3605089 | — | — | 1 | 5.70 |
| CHEMBL3605087 | — | — | 1 | 5.40 |
| CHEMBL3605086 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3314014 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3605083 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3605090 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3605092 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3605085 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3605082 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3605081 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3605084 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3605088 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3605089 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3605087 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3605086 | — | IC50 | > | 10000.0 | nM | - |