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Assay Detail

CHEMBL5384036

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

Binding
Inhibition of NLRP3 inflammasome activation in LPS-treated mouse BMDM cells assessed as inhibition of ATP-stimulated IL-1beta release incubated for 30 mins followed by ATP stimulation for 1 hr by ELISA method
3
Total Activities
3
Compounds Tested
1
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

Novel Aryl Sulfonamide Derivatives as NLRP3 Inflammasome Inhibitors for the Potential Treatment of Cancer.
Albanese V, Missiroli S, Perrone M, Fabbri M, Boncompagni C, Pacifico S, De Ventura T, Ciancetta A, Dondio G, Kricek F, Pinton P, Guerrini R, Preti D, Giorgi C.
J Med Chem (2023) 66 : 5223 -5241
PubMed 36972104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.98 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5421905 1 8.16
CHEMBL5422387 1 8.07
CHEMBL5436366 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5421905 IC50 = 6.88 nM 8.16
CHEMBL5422387 IC50 = 8.58 nM 8.07
CHEMBL5436366 IC50 = 19.9 nM 7.70