Assay Detail
Binding
CHEMBL4701576
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at RORgammat in CD3 and CD28-stimulated human whole blood assessed as reduction in IL17A production incubated for 1 hr before CD3 and CD28 stimulation for 20 hrs by AlphaLISA method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 9 | 7.56 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4752644 | — | — | 1 | 7.89 |
| CHEMBL4776069 | — | — | 1 | 7.75 |
| CHEMBL4634542 | BMS-986251 | 1.0 | 1 | 7.62 |
| CHEMBL4763134 | — | — | 1 | 7.52 |
| CHEMBL4759786 | — | — | 1 | 7.48 |
| CHEMBL4741799 | — | — | 1 | 7.40 |
| CHEMBL4750276 | — | — | 1 | 7.28 |
| CHEMBL4750060 | — | — | 1 | - |
| CHEMBL4799160 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4752644 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4776069 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4634542 | BMS-986251 | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4763134 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4759786 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4741799 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4750276 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4750060 | — | EC50 | - | — | - | |
| CHEMBL4799160 | — | EC50 | - | — | - |