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Assay Detail

CHEMBL1920643

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Functional
Antagonist activity at human CRTH2 expressed in human CHO cells by cellular dielectric spectroscopy
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of potent, selective, and orally bioavailable alkynylphenoxyacetic acid CRTH2 (DP2) receptor antagonists for the treatment of allergic inflammatory diseases.
Crosignani S, Prêtre A, Jorand-Lebrun C, Fraboulet G, Seenisamy J, Augustine JK, Missotten M, Humbert Y, Cleva C, Abla N, Daff H, Schott O, Schneider M, Burgat-Charvillon F, Rivron D, Hamernig I, Arrighi JF, Gaudet M, Zimmerli SC, Juillard P, Johnson Z.
J Med Chem (2011) 54 : 7299 -7317
PubMed 21916510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.33 7.55
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1917592 1 7.55
CHEMBL1917584 1 7.50
CHEMBL1917389 1 6.94
CHEMBL1917407 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1917592 IC50 = 28.0 nM 7.55
CHEMBL1917584 IC50 = 32.0 nM 7.50
CHEMBL1917389 IC50 = 114.0 nM 6.94
CHEMBL1917407 Inhibition = 70.0 % -