Assay Detail
Binding
CHEMBL4144984
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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 co-activator SRC1 peptide recruitment after 1 hr by FRET based LANCE assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
From RORγt Agonist to Two Types of RORγt Inverse Agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.32 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4171547 | — | — | 1 | 7.80 |
| CHEMBL3609392 | — | — | 1 | 7.80 |
| CHEMBL4172665 | — | — | 1 | 7.50 |
| CHEMBL4163226 | — | — | 1 | 7.50 |
| CHEMBL4173830 | — | — | 1 | 7.50 |
| CHEMBL3105674 | — | — | 1 | 7.40 |
| CHEMBL4166984 | — | — | 1 | 7.10 |
| CHEMBL4163533 | — | — | 1 | 7.00 |
| CHEMBL4159083 | — | — | 1 | 6.90 |
| CHEMBL4164766 | — | — | 1 | 6.70 |
| CHEMBL4160934 | — | — | 1 | - |
| CHEMBL4161349 | — | — | 1 | - |
| CHEMBL4169276 | — | — | 1 | - |
| CHEMBL4171142 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4171547 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3609392 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL4172665 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4163226 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4173830 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3105674 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4166984 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4163533 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4159083 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4164766 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4160934 | — | IC50 | > | 2511.89 | nM | - |
| CHEMBL4161349 | — | IC50 | > | 25118.86 | nM | - |
| CHEMBL4169276 | — | IC50 | > | 25118.86 | nM | - |
| CHEMBL4171142 | — | IC50 | > | 25118.86 | nM | - |