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Assay Detail

CHEMBL5588237

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

Binding
Inhibition of NLRP3 inflammasome activation in LPS/nigericin stimulated human PBMC assessed as reduction in IL-1beta release pretreated with LPS for 3 hrs followed by compound addition for 40 mins prior to nigericin stimulation for 40 mins by ELISA
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PBMC
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

Discovery of Potent, Specific, and Orally Available NLRP3 Inflammasome Inhibitors Based on Pyridazine Scaffolds for the Treatment of Septic Shock and Peritonitis.
Fu Z, Duan Y, Pei H, Zou Y, Tang M, Chen Y, Yang T, Ma Z, Yan W, Su K, Cai X, Guo T, Teng Y, Jia T, Chen L.
J Med Chem (2024) 67 : 15711 -15737
PubMed 39169676 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.54 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5597392 1 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5597392 IC50 = 2.88 nM 8.54