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Assay Detail

CHEMBL4136967

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

Binding
Agonist activity at Gal4-fused RORgammat DNA binding domain (unknown origin) expressed in 293T cells assessed as SRC1 coactivator recruitment in presence of ursolic acid by TR-FRET assay
2
Total Activities
2
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 2 7.03 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL455876 DESMOSTEROL 1 7.10
CHEMBL4171014 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL455876 DESMOSTEROL EC50 = 80.0 nM 7.10
CHEMBL4171014 EC50 = 110.0 nM 6.96