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Assay Detail

CHEMBL4153215

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

Binding
Antagonist activity at human P2X2 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced calcium flux measured for 30 secs at 0.4 secs intervals by Flou-4-AM dye based fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

P2X purinoceptor 2 (CHEMBL2531)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.
Kwak SH, Shin S, Lee JH, Shim JK, Kim M, Lee SD, Lee A, Bae J, Park JH, Abdelrahman A, Müller CE, Cho SK, Kang SG, Bae MA, Yang JY, Ko H, Goddard WA, Kim YC.
Eur J Med Chem (2018) 151 : 462 -481
PubMed 29649742 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.16 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672104 1 6.16
CHEMBL265502 SURAMIN 3.0 1 -
CHEMBL4160315 1 -
CHEMBL2180179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672104 IC50 = 690.0 nM 6.16
CHEMBL265502 SURAMIN IC50 - -
CHEMBL4160315 IC50 - -
CHEMBL2180179 IC50 - -