Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3365972

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

Functional
Antagonist activity at P2Y1 receptor in washed human platelets assessed as 1 uM 2-methylthio-ADP-induced calcium flux by FLIPR assay
ChEMBL ↗
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
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 36 9.60 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314307 — — 1 10.70
CHEMBL3314305 — — 1 10.52
CHEMBL3314308 — — 1 10.40
CHEMBL3314291 — — 1 10.30
CHEMBL3314306 — — 1 10.10
CHEMBL3314320 — — 1 10.05
CHEMBL3314290 — — 1 10.05
CHEMBL3314321 — — 1 9.92
CHEMBL3263056 — — 1 9.92
CHEMBL3314304 — — 1 9.89
CHEMBL3314299 — — 1 9.89
CHEMBL3314287 — — 1 9.85
CHEMBL3314297 — — 1 9.82
CHEMBL3314319 — — 1 9.80
CHEMBL3314309 — — 1 9.64
CHEMBL3314317 — — 1 9.52
CHEMBL3314298 — — 1 9.48
CHEMBL3314296 — — 1 9.43
CHEMBL3314295 — — 1 9.43
CHEMBL3314288 — — 1 9.41
CHEMBL3314310 — — 1 9.35
CHEMBL3314316 — — 1 9.33
CHEMBL3314315 — — 1 9.29
CHEMBL3314301 — — 1 9.28
CHEMBL3314314 — — 1 9.24
CHEMBL3314303 — — 1 9.24
CHEMBL3314311 — — 1 8.97
CHEMBL3314300 — — 1 8.82
CHEMBL3314302 — — 1 8.74
CHEMBL3314289 — — 1 8.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314307 — IC50 = 0.02 nM 10.70
CHEMBL3314305 — IC50 = 0.03 nM 10.52
CHEMBL3314308 — IC50 = 0.04 nM 10.40
CHEMBL3314291 — IC50 = 0.05 nM 10.30
CHEMBL3314306 — IC50 = 0.08 nM 10.10
CHEMBL3314320 — IC50 = 0.09 nM 10.05
CHEMBL3314290 — IC50 = 0.09 nM 10.05
CHEMBL3314321 — IC50 = 0.12 nM 9.92
CHEMBL3263056 — IC50 = 0.12 nM 9.92
CHEMBL3314304 — IC50 = 0.13 nM 9.89
CHEMBL3314299 — IC50 = 0.13 nM 9.89
CHEMBL3314287 — IC50 = 0.14 nM 9.85
CHEMBL3314297 — IC50 = 0.15 nM 9.82
CHEMBL3314319 — IC50 = 0.16 nM 9.80
CHEMBL3314309 — IC50 = 0.23 nM 9.64
CHEMBL3314317 — IC50 = 0.3 nM 9.52
CHEMBL3314298 — IC50 = 0.33 nM 9.48
CHEMBL3314295 — IC50 = 0.37 nM 9.43
CHEMBL3314296 — IC50 = 0.37 nM 9.43
CHEMBL3314288 — IC50 = 0.39 nM 9.41
CHEMBL3314310 — IC50 = 0.45 nM 9.35
CHEMBL3314316 — IC50 = 0.47 nM 9.33
CHEMBL3314315 — IC50 = 0.51 nM 9.29
CHEMBL3314301 — IC50 = 0.52 nM 9.28
CHEMBL3314314 — IC50 = 0.57 nM 9.24
CHEMBL3314303 — IC50 = 0.57 nM 9.24
CHEMBL3314311 — IC50 = 1.06 nM 8.97
CHEMBL3314300 — IC50 = 1.51 nM 8.82
CHEMBL3314302 — IC50 = 1.8 nM 8.74
CHEMBL3314289 — IC50 = 1.96 nM 8.71
CHEMBL3314313 — IC50 = 2.3 nM 8.64
CHEMBL3314312 — IC50 - — -
CHEMBL3314292 — IC50 - — -
CHEMBL3314293 — IC50 - — -
CHEMBL3314294 — IC50 - — -
CHEMBL3314318 — IC50 - — -