Assay Detail
Binding
CHEMBL4714673
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Orthosteric agonist activity at recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as increase in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment incubated for 60 mins by TR-FRET assay
3
Total Activities
3
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
Covalent Occlusion of the RORγt Ligand Binding Pocket Allows Unambiguous Targeting of an Allosteric Site.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 3 | 7.09 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL173898 | — | — | 1 | 7.57 |
| CHEMBL455876 | DESMOSTEROL | — | 1 | 7.32 |
| CHEMBL112570 | CHOLESTEROL | 2.0 | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL173898 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL455876 | DESMOSTEROL | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL112570 | CHOLESTEROL | EC50 | = | 418.0 | nM | 6.38 |