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Assay Detail

CHEMBL5392121

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

Binding
Inhibition of NLRP3 in human THP-1 cells assessed as reduction in IL-1beta production preincubated for 1 hrs followed by ATP addition measured after 18 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type THP-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NACHT, LRR and PYD domains-containing protein 3 (CHEMBL1741208)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Progress and Prospects of Small Molecules for NLRP3 Inflammasome Inhibition.
Li N, Zhang R, Tang M, Zhao M, Jiang X, Cai X, Ye N, Su K, Peng J, Zhang X, Wu W, Ye H.
J Med Chem (2023) 66 : 14447 -14473
PubMed 37879043 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.56 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419955 1 10.15
CHEMBL5404792 1 8.36
CHEMBL5431968 1 8.27
CHEMBL5402007 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419955 IC50 = 0.07 nM 10.15
CHEMBL5404792 IC50 = 4.34 nM 8.36
CHEMBL5431968 IC50 = 5.32 nM 8.27
CHEMBL5402007 IC50 = 36.5 nM 7.44