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

CHEMBL4479309

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

Binding
Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake measured after 2 hrs by fluorescence analysis
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 7 (CHEMBL4805)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion.
Park JH, Williams DR, Lee JH, Lee SD, Lee JH, Ko H, Lee GE, Kim S, Lee JM, Abdelrahman A, Müller CE, Jung DW, Kim YC.
J Med Chem (2016) 59 : 7410 -7430
PubMed 27427902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 7.15 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4165149 1 9.96
CHEMBL3415305 1 9.64
CHEMBL4582650 1 9.31
CHEMBL4584526 1 8.83
CHEMBL4561852 1 8.81
CHEMBL4594110 1 8.15
CHEMBL4542014 1 7.89
CHEMBL4526937 1 7.60
CHEMBL4521847 1 7.60
CHEMBL4534068 1 7.57
CHEMBL4592534 1 7.51
CHEMBL4531777 1 7.50
CHEMBL3741159 1 7.40
CHEMBL4529842 1 7.39
CHEMBL4582804 1 7.36
CHEMBL4559257 1 7.35
CHEMBL4570660 1 7.35
CHEMBL4586600 1 7.26
CHEMBL4585050 1 7.21
CHEMBL3415342 1 7.16
CHEMBL4529050 1 7.14
CHEMBL4513283 1 7.11
CHEMBL4536033 1 7.06
CHEMBL4573595 1 6.96
CHEMBL4560935 1 6.95
CHEMBL4590758 1 6.84
CHEMBL4535840 1 6.83
CHEMBL4527934 1 6.82
CHEMBL4582217 1 6.81
CHEMBL4551449 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4165149 IC50 = 0.11 nM 9.96
CHEMBL3415305 IC50 = 0.23 nM 9.64
CHEMBL4582650 IC50 = 0.49 nM 9.31
CHEMBL4584526 IC50 = 1.49 nM 8.83
CHEMBL4561852 IC50 = 1.53 nM 8.81
CHEMBL4594110 IC50 = 7.0 nM 8.15
CHEMBL4542014 IC50 = 13.0 nM 7.89
CHEMBL4526937 IC50 = 25.0 nM 7.60
CHEMBL4521847 IC50 = 25.0 nM 7.60
CHEMBL4534068 IC50 = 27.0 nM 7.57
CHEMBL4592534 IC50 = 31.0 nM 7.51
CHEMBL4531777 IC50 = 32.0 nM 7.50
CHEMBL3741159 IC50 = 40.0 nM 7.40
CHEMBL4529842 IC50 = 41.0 nM 7.39
CHEMBL4582804 IC50 = 44.0 nM 7.36
CHEMBL4559257 IC50 = 45.0 nM 7.35
CHEMBL4570660 IC50 = 45.0 nM 7.35
CHEMBL4586600 IC50 = 55.0 nM 7.26
CHEMBL4585050 IC50 = 62.0 nM 7.21
CHEMBL3415342 IC50 = 70.0 nM 7.16
CHEMBL4529050 IC50 = 73.0 nM 7.14
CHEMBL4513283 IC50 = 77.0 nM 7.11
CHEMBL4536033 IC50 = 88.0 nM 7.06
CHEMBL4573595 IC50 = 109.0 nM 6.96
CHEMBL4560935 IC50 = 112.0 nM 6.95
CHEMBL4590758 IC50 = 143.0 nM 6.84
CHEMBL4535840 IC50 = 149.0 nM 6.83
CHEMBL4527934 IC50 = 152.0 nM 6.82
CHEMBL4582217 IC50 = 155.0 nM 6.81
CHEMBL4551449 IC50 = 159.0 nM 6.80
CHEMBL4575784 IC50 = 187.0 nM 6.73
CHEMBL4549063 IC50 = 202.0 nM 6.70
CHEMBL4571782 IC50 = 202.0 nM 6.70
CHEMBL4542468 IC50 = 238.0 nM 6.62
CHEMBL4483719 IC50 = 244.0 nM 6.61
CHEMBL4548337 IC50 = 249.0 nM 6.60
CHEMBL4519323 IC50 = 259.0 nM 6.59
CHEMBL4580923 IC50 = 269.0 nM 6.57
CHEMBL4531079 IC50 = 312.0 nM 6.51
CHEMBL4551632 IC50 = 400.0 nM 6.40
CHEMBL4537806 IC50 = 430.0 nM 6.37
CHEMBL4537272 IC50 = 565.0 nM 6.25
CHEMBL4588622 IC50 = 702.0 nM 6.15
CHEMBL4575046 IC50 = 896.0 nM 6.05
CHEMBL4544899 IC50 = 1440.0 nM 5.84
CHEMBL4527182 IC50 = 1570.0 nM 5.80
CHEMBL4533569 IC50 = 3520.0 nM 5.45
CHEMBL4538742 IC50 > 10000.0 nM -
CHEMBL4547543 IC50 > 10000.0 nM -
CHEMBL4548453 IC50 > 10000.0 nM -