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Assay Detail

CHEMBL923908

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Functional
Antagonist activity at human P2Y12 receptor assessed as ADP-induced human platelet aggregation
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2Y purinoceptor 12 (CHEMBL2001)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA.
Bioorg Med Chem Lett (2007) 17 : 6013 -6018
PubMed 17827008 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.60 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251024 1 9.50
CHEMBL437204 1 9.30
CHEMBL250832 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251024 IC50 = 0.3162 nM 9.50
CHEMBL437204 IC50 = 0.5012 nM 9.30
CHEMBL250832 IC50 = 100.0 nM 7.00