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Assay Detail

CHEMBL4306845

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

Binding
Displacement of tritiated 2-(4-(ethylsulfonyl)phenyl)-N-(4-(2-(methoxymethyl)phenyl)thiophen-2-yl)acetamide from mouse HN-AVI-GST-TCS-RORC (256 to 516 residues) incubated for 8 to 20 hrs by scintillation proximity competition binding assay
3
Total Activities
3
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

Discovery of Potent and Orally Bioavailable Inverse Agonists of the Retinoic Acid Receptor-Related Orphan Receptor C2.
von Berg S, Xue Y, Collins M, Llinas A, Olsson RI, Halvarsson T, Lindskog M, Malmberg J, Jirholt J, Krutrök N, Ramnegård M, Brännström M, Lundqvist A, Lepistö M, Aagaard A, McPheat J, Hansson EL, Chen R, Xiong Y, Hansson TG, Narjes F.
ACS Med Chem Lett (2019) 10 : 972 -977
PubMed 31223457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.63 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4458320 1 7.60
CHEMBL4562895 1 6.90
CHEMBL4445354 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4458320 IC50 = 25.12 nM 7.60
CHEMBL4562895 IC50 = 125.89 nM 6.90
CHEMBL4445354 IC50 = 3981.07 nM 5.40