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Assay Detail

CHEMBL4136966

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at 6xHis tagged human RORgammat LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) assessed as biotinylated SRC1-2 peptide coactivator recruitment by AlphaScreen assay
4
Total Activities
4
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

Target

Nuclear receptor ROR-gamma (CHEMBL1741186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Agonists as Potential Small Molecule Therapeutics for Cancer Immunotherapy.
Qiu R, Wang Y.
J Med Chem (2018) 61 : 5794 -5804
PubMed 29412659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169046 1 7.70
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL 1 7.70
CHEMBL1233249 1 7.70
CHEMBL112570 CHOLESTEROL 2.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169046 EC50 = 20.0 nM 7.70
CHEMBL422904 22(R)-HYDROXYCHOLESTEROL EC50 = 20.0 nM 7.70
CHEMBL1233249 EC50 = 20.0 nM 7.70
CHEMBL112570 CHOLESTEROL EC50 = 20.0 nM 7.70