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Assay Detail

CHEMBL907941

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Activity at human TP receptor in platelet rich plasma assessed as inhibition U44619-induced platelet aggregation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thromboxane A2 receptor (CHEMBL2069)
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
IC50 5 5.70 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426387 1 7.10
CHEMBL426559 LAROPIPRANT 4.0 1 6.11
CHEMBL385126 1 5.85
CHEMBL383484 1 5.08
CHEMBL207203 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426387 IC50 = 80.0 nM 7.10
CHEMBL426559 LAROPIPRANT IC50 = 770.0 nM 6.11
CHEMBL385126 IC50 = 1400.0 nM 5.85
CHEMBL383484 IC50 = 8400.0 nM 5.08
CHEMBL207203 IC50 = 43000.0 nM 4.37