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Assay Detail

CHEMBL3365973

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

Binding
Antagonist activity at P2Y1 receptor in platelet-enriched human plasma assessed as 10 uM ADP-induced platelet aggregation preincubated for 1 min followed by ADP induction measured at 5 mins by aggregometric analysis
33
Total Activities
33
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 1 (CHEMBL4315)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.
Yang W, Wang Y, Lai A, Qiao JX, Wang TC, Hua J, Price LA, Shen H, Chen XQ, Wong P, Crain E, Watson C, Huang CS, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.
J Med Chem (2014) 57 : 6150 -6164
PubMed 24931384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.60 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314307 1 7.30
CHEMBL3314296 1 7.10
CHEMBL3314308 1 7.05
CHEMBL3314305 1 7.05
CHEMBL3314314 1 6.96
CHEMBL3263056 1 6.89
CHEMBL3314313 1 6.89
CHEMBL3314320 1 6.85
CHEMBL3314315 1 6.82
CHEMBL3314316 1 6.80
CHEMBL3314298 1 6.80
CHEMBL3314301 1 6.80
CHEMBL3314303 1 6.75
CHEMBL3314295 1 6.75
CHEMBL3314321 1 6.75
CHEMBL3314309 1 6.72
CHEMBL3314319 1 6.70
CHEMBL3314299 1 6.68
CHEMBL3314304 1 6.64
CHEMBL3314300 1 6.64
CHEMBL3314311 1 6.62
CHEMBL3314297 1 6.62
CHEMBL3314318 1 6.58
CHEMBL3314312 1 6.52
CHEMBL3314310 1 6.41
CHEMBL3314302 1 6.40
CHEMBL3314306 1 6.37
CHEMBL3314291 1 6.21
CHEMBL3314288 1 6.06
CHEMBL3314317 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314307 IC50 = 50.0 nM 7.30
CHEMBL3314296 IC50 = 80.0 nM 7.10
CHEMBL3314308 IC50 = 90.0 nM 7.05
CHEMBL3314305 IC50 = 90.0 nM 7.05
CHEMBL3314314 IC50 = 110.0 nM 6.96
CHEMBL3263056 IC50 = 130.0 nM 6.89
CHEMBL3314313 IC50 = 130.0 nM 6.89
CHEMBL3314320 IC50 = 140.0 nM 6.85
CHEMBL3314315 IC50 = 150.0 nM 6.82
CHEMBL3314316 IC50 = 160.0 nM 6.80
CHEMBL3314298 IC50 = 160.0 nM 6.80
CHEMBL3314301 IC50 = 160.0 nM 6.80
CHEMBL3314303 IC50 = 180.0 nM 6.75
CHEMBL3314295 IC50 = 180.0 nM 6.75
CHEMBL3314321 IC50 = 180.0 nM 6.75
CHEMBL3314309 IC50 = 190.0 nM 6.72
CHEMBL3314319 IC50 = 200.0 nM 6.70
CHEMBL3314299 IC50 = 210.0 nM 6.68
CHEMBL3314304 IC50 = 230.0 nM 6.64
CHEMBL3314300 IC50 = 230.0 nM 6.64
CHEMBL3314311 IC50 = 240.0 nM 6.62
CHEMBL3314297 IC50 = 240.0 nM 6.62
CHEMBL3314318 IC50 = 260.0 nM 6.58
CHEMBL3314312 IC50 = 300.0 nM 6.52
CHEMBL3314310 IC50 = 390.0 nM 6.41
CHEMBL3314302 IC50 = 400.0 nM 6.40
CHEMBL3314306 IC50 = 430.0 nM 6.37
CHEMBL3314291 IC50 = 610.0 nM 6.21
CHEMBL3314288 IC50 = 870.0 nM 6.06
CHEMBL3314317 IC50 = 950.0 nM 6.02
CHEMBL3314287 IC50 = 1400.0 nM 5.85
CHEMBL3314289 IC50 = 2900.0 nM 5.54
CHEMBL3314290 IC50 = 3100.0 nM 5.51