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Assay Detail

CHEMBL3291827

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

Binding
Displacement of [125I]AZ11931285 from human P2Y12 receptor expressed in CHOK1 cell membrane after 10 seconds
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimization of ketone-based P2Y(12) receptor antagonists as antithrombotic agents: pharmacodynamics and receptor kinetics considerations.
Giordanetto F, Bach P, Zetterberg F, Antonsson T, Bylund R, Johansson J, Sellén M, Brown D, Hideståhl L, Berntsson P, Hovdal D, Zachrisson H, Björkman JA, van Giezen JJ.
Bioorg Med Chem Lett (2014) 24 : 2963 -2968
PubMed 24835983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.13 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419490 1 7.36
CHEMBL3288123 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419490 IC50 = 44.0 nM 7.36
CHEMBL3288123 IC50 = 126.0 nM 6.90