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Assay Detail

CHEMBL5264104

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

Binding
Inhibition of human RORgamma by TR-FRET assay
5
Total Activities
5
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

Target

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

Publication

Combating Autoimmune Diseases With Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ or RORc) Inhibitors: Hits and Misses.
Pandya VB, Kumar S, Sachchidanand, Sharma R, Desai RC.
J Med Chem (2018) 61 : 10976 -10995
PubMed 30010338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.82 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5270756 1 8.70
CHEMBL4172726 1 7.80
CHEMBL5287608 1 7.80
CHEMBL5205826 1 7.40
CHEMBL4864604 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5270756 IC50 = 2.0 nM 8.70
CHEMBL4172726 IC50 = 16.0 nM 7.80
CHEMBL5287608 IC50 = 15.8 nM 7.80
CHEMBL5205826 IC50 = 40.0 nM 7.40
CHEMBL4864604 IC50 = 40.0 nM 7.40