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Assay Detail

CHEMBL923909

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

Binding
Displacement of [125I] labeled ligand from human P2Y12 receptor in human platelets
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 14 8.45 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251041 1 9.60
CHEMBL249790 1 9.20
CHEMBL266922 1 8.80
CHEMBL398435 TICAGRELOR 4.0 1 8.70
CHEMBL398295 1 8.70
CHEMBL398434 1 8.60
CHEMBL274713 1 8.50
CHEMBL250847 1 8.30
CHEMBL250687 1 8.30
CHEMBL249789 1 8.30
CHEMBL249584 1 8.30
CHEMBL535189 1 8.20
CHEMBL250848 1 7.70
CHEMBL401158 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251041 Ki = 0.2512 nM 9.60
CHEMBL249790 Ki = 0.631 nM 9.20
CHEMBL266922 Ki = 1.585 nM 8.80
CHEMBL398435 TICAGRELOR Ki = 1.995 nM 8.70
CHEMBL398295 Ki = 1.995 nM 8.70
CHEMBL398434 Ki = 2.512 nM 8.60
CHEMBL274713 Ki = 3.162 nM 8.50
CHEMBL250847 Ki = 5.012 nM 8.30
CHEMBL250687 Ki = 5.012 nM 8.30
CHEMBL249789 Ki = 5.012 nM 8.30
CHEMBL249584 Ki = 5.012 nM 8.30
CHEMBL535189 Ki = 6.31 nM 8.20
CHEMBL250848 Ki = 19.95 nM 7.70
CHEMBL401158 Ki = 79.43 nM 7.10