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Assay Detail

CHEMBL4252249

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

Functional
Antiinflammatory activity in LPS/IFNgamma-differentiated human THP1 cells assessed as inhibition of ATP-induced IL-1beta release after 30 mins by ELISA
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Intermediate

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

1,4-Naphthoquinones potently inhibiting P2X7 receptor activity.
Faria RX, Oliveira FH, Salles JP, Oliveira AS, von Ranke NL, Bello ML, Rodrigues CR, Castro HC, Louvis AR, Martins DL, Ferreira VF.
Eur J Med Chem (2018) 143 : 1361 -1372
PubMed 29133043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.50 8.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4281588 1 8.01
CHEMBL4292211 1 7.40
CHEMBL4291798 1 6.20
CHEMBL255787 1 6.16
CHEMBL4173394 BRILLIANT BLUE G 4.0 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4281588 IC50 = 9.8 nM 8.01
CHEMBL4292211 IC50 = 40.2 nM 7.40
CHEMBL4291798 IC50 = 633.0 nM 6.20
CHEMBL255787 IC50 = 689.0 nM 6.16
CHEMBL4173394 BRILLIANT BLUE G IC50 = 19270.0 nM 4.71