Assay Detail
Binding
CHEMBL4701575
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Inverse agonist activity at Gal4-fused RORgammat (unknown origin)
6
Total Activities
6
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
Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.40 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741799 | — | — | 1 | 8.55 |
| CHEMBL4759786 | — | — | 1 | 8.49 |
| CHEMBL4776069 | — | — | 1 | 8.02 |
| CHEMBL4752644 | — | — | 1 | 7.77 |
| CHEMBL4799160 | — | — | 1 | 6.06 |
| CHEMBL4750060 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741799 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4759786 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4776069 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4752644 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4799160 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4750060 | — | EC50 | = | 3300.0 | nM | 5.48 |