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Assay Detail

CHEMBL3101028

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

Binding
Antagonist activity at P2Y12 receptor in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation incubated for 5 mins prior to ADP-challenge by light transmission-based assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of cyclopentyl-triazolol-pyrimidine (CPTP) based P2Y12 antagonists.
Tu W, Fan J, Zhang H, Xu G, Liu Z, Qu J, Yang F, Zhang L, Luan T, Yuan J, Gong A, Feng J, Sun P, Dong Q.
Bioorg Med Chem Lett (2014) 24 : 141 -146
PubMed 24332627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.83 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3098241 1 6.66
CHEMBL3098234 1 6.55
CHEMBL3098247 1 6.48
CHEMBL3098242 1 6.46
CHEMBL398435 TICAGRELOR 4.0 1 6.30
CHEMBL3098243 1 5.78
CHEMBL3098240 1 5.76
CHEMBL3098246 1 5.71
CHEMBL3098250 1 5.32
CHEMBL3098244 1 5.20
CHEMBL3098239 1 4.95
CHEMBL3098238 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3098241 IC50 = 220.0 nM 6.66
CHEMBL3098234 IC50 = 280.0 nM 6.55
CHEMBL3098247 IC50 = 330.0 nM 6.48
CHEMBL3098242 IC50 = 350.0 nM 6.46
CHEMBL398435 TICAGRELOR IC50 = 500.0 nM 6.30
CHEMBL3098243 IC50 = 1670.0 nM 5.78
CHEMBL3098240 IC50 = 1730.0 nM 5.76
CHEMBL3098246 IC50 = 1970.0 nM 5.71
CHEMBL3098250 IC50 = 4820.0 nM 5.32
CHEMBL3098244 IC50 = 6350.0 nM 5.20
CHEMBL3098239 IC50 = 11280.0 nM 4.95
CHEMBL3098238 IC50 = 16300.0 nM 4.79