Assay Detail

CHEMBL2444554

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Binding

Antagonist activity at CRTh2 receptor in human isolated eosinophil assessed as inhibition of delta12-PGD2-induced shape change after 5 mins by flow cytometry

ChEMBL ↗

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Target

Prostaglandin D2 receptor 2 (CHEMBL5071) ↗

Open DB target context

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Prostaglandin D2 receptor 2 (CHEMBL5071) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Prostaglandin D2 receptor 2

CHEMBL5071

Anchored from Assay target.

Protein identity Prostaglandin D2 receptor 2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
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

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.

Sandham DA, Arnold N, Aschauer H, Bala K, Barker L, Brown L, Brown Z, Budd D, Cox B, Docx C, Dubois G, Duggan N, England K, Everatt B, Furegati M, Hall E, Kalthoff F, King A, Leblanc CJ, Manini J, Meingassner J, Profit R, Schmidt A, Simmons J, Sohal B, Stringer R, Thomas M, Turner KL, Walker C, Watson SJ, Westwick J, Willis J, Williams G, Wilson C.
Bioorg Med Chem (2013) 21 : 6582 -6591
PubMed 24021582 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.40	8.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2442750	QAV680	2.0	1	8.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2442750	QAV680	IC50	=	4.0	nM	8.40