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Assay Detail

CHEMBL5531433

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

Functional
Antagonist activity at GPR183 (unknown origin) transfected in HEK293 cells cotransfected with CRE-luciferase plasmid assessed as restoration of luciferase activity preincubated for 30 mins followed by 7alpha,25-dihydroxycholesterol induction and measured after 4 hrs by dual luciferase assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 183 (CHEMBL3259470)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Highly Potent Oxysterol Receptor GPR183 Antagonist Bearing the Benzo[<i>d</i>]thiazole Structural Motif for the Treatment of Inflammatory Bowel Disease (IBD).
Zeng R, Fang M, Shen A, Chai X, Zhao Y, Liu M, Zhu L, Rui W, Feng B, Hong L, Ding C, Song Z, Lu W, Zhang A.
J Med Chem (2024) 67 : 3520 -3541
PubMed 38417036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.74 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567610 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567610 IC50 = 1.83 nM 8.74