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Assay Detail

CHEMBL4818412

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

Binding
Inhibition of NLRP3 inflammasome activation in LPS/nigericin-treated mouse BMDM cells assessed as inhibition of LPS and nigericin-induced IL-1beta production pre-treated for 1 hr measured after 1 hr of stimulation by ELISA
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BMDM
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NACHT, LRR and PYD domains-containing protein 3 (CHEMBL3779755)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.
Zhang C, Yue H, Sun P, Hua L, Liang S, Ou Y, Wu D, Wu X, Chen H, Hao Y, Hu W, Yang Z.
Eur J Med Chem (2021) 219 : 113417 -113417
PubMed 33845232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.06 8.12
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3183703 1 8.12
CHEMBL488823 1 6.00
CHEMBL4862238 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3183703 IC50 = 7.5 nM 8.12
CHEMBL488823 IC50 = 1000.0 nM 6.00
CHEMBL4862238 Inhibition - % -