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Assay Detail

CHEMBL4833103

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

Binding
Inverse agonist activity at mouse RORC ligand binding domain incubated for 30 mins by scintillation proximity binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor ROR-gamma (CHEMBL1293231)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2.
Narjes F, Llinas A, von Berg S, Jirholt J, Lever S, Pehrson R, Collins M, Malmberg A, Svanberg P, Xue Y, Olsson RI, Malmberg J, Hughes G, Hossain N, Grindebacke H, Leffler A, Krutrök N, Bäck E, Ramnegård M, Lepistö M, Thunberg L, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG.
J Med Chem (2021) 64 : 13807 -13829
PubMed 34464130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.00 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4864604 1 7.08
CHEMBL4562895 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4864604 IC50 = 84.0 nM 7.08
CHEMBL4562895 IC50 = 120.0 nM 6.92