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Assay Detail

CHEMBL4133156

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 ATP-induced IL-1beta release preincubated for 30 mins followed by ATP addition measured after 30 mins by ELISA
2
Total Activities
2
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

1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
Gonzaga DTG, Ferreira LBG, Moreira Maramaldo Costa TE, von Ranke NL, Anastácio Furtado Pacheco P, Sposito Simões AP, Arruda JC, Dantas LP, de Freitas HR, de Melo Reis RA, Penido C, Bello ML, Castro HC, Rodrigues CR, Ferreira VF, Faria RX, da Silva FC.
Eur J Med Chem (2017) 139 : 698 -717
PubMed 28858765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.13 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4162056 1 7.17
CHEMBL255787 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4162056 IC50 = 67.0 nM 7.17
CHEMBL255787 IC50 = 82.0 nM 7.09