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Assay Detail

CHEMBL2182576

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Functional
Antagonist activity at CRTH2 expressed in Th2 cells assessed as inhibition of PGD2-induced antiapoptotic activity
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Th2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor 2 (CHEMBL5071)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Pettipher R, Whittaker M.
J Med Chem (2012) 55 : 2915 -2931
PubMed 22224640 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.46 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL560993 TIMAPIPRANT 3.0 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL560993 TIMAPIPRANT IC50 = 35.0 nM 7.46