Assay Detail

CHEMBL907960

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Binding

Activity at CRTH2 receptor

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	Expert

Target

Prostaglandin D2 receptor 2 (CHEMBL5071) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM.
J Med Chem (2007) 50 : 794 -806
PubMed 17300164 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	6.13	6.13

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL426559	LAROPIPRANT	4.0	1	6.13

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL426559	LAROPIPRANT	Ki	=	745.0	nM	6.13