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Assay Detail

CHEMBL1646948

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Functional
Antagonist activity at CRTH2 in human eosinophil assessed as effect of cellular shape change by EOS assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Azaindoles as potent CRTH2 receptor antagonists.
Simard D, Leblanc Y, Berthelette C, Zaghdane MH, Molinaro C, Wang Z, Gallant M, Lau S, Thao T, Hamel M, Stocco R, Sawyer N, Sillaots S, Gervais F, Houle R, Lévesque JF.
Bioorg Med Chem Lett (2011) 21 : 841 -845
PubMed 21185722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.52 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1641811 1 8.92
CHEMBL1641816 1 8.92
CHEMBL561132 MK-7246 1.0 1 8.66
CHEMBL1641813 1 8.64
CHEMBL1641815 1 8.62
CHEMBL1641814 1 8.51
CHEMBL1641809 1 8.48
CHEMBL1641817 1 8.47
CHEMBL1641808 1 8.15
CHEMBL1641810 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1641811 IC50 = 1.2 nM 8.92
CHEMBL1641816 IC50 = 1.2 nM 8.92
CHEMBL561132 MK-7246 IC50 = 2.2 nM 8.66
CHEMBL1641813 IC50 = 2.3 nM 8.64
CHEMBL1641815 IC50 = 2.4 nM 8.62
CHEMBL1641814 IC50 = 3.1 nM 8.51
CHEMBL1641809 IC50 = 3.3 nM 8.48
CHEMBL1641817 IC50 = 3.4 nM 8.47
CHEMBL1641808 IC50 = 7.0 nM 8.15
CHEMBL1641810 IC50 = 15.8 nM 7.80