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Assay Detail

CHEMBL4256752

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

Binding
Inhibition of NLRP3 in mouse J774A.1 cells assessed as reduction in LPS-stimulated IL-1beta levels pre-incubated with LPS for 4.5 hrs followed by incubation for 30 mins in presence of ATP and measured after 30 mins by ELISA
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
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

Structural Insights of Benzenesulfonamide Analogues as NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
Fulp J, He L, Toldo S, Jiang Y, Boice A, Guo C, Li X, Rolfe A, Sun D, Abbate A, Wang XY, Zhang S.
J Med Chem (2018) 61 : 5412 -5423
PubMed 29877709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.49 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4278966 1 6.38
CHEMBL4277889 1 6.26
CHEMBL4289639 1 6.20
CHEMBL4293687 1 6.09
CHEMBL4285824 1 6.01
CHEMBL4286218 1 5.88
CHEMBL4293025 1 5.85
CHEMBL4277518 1 5.82
CHEMBL4282420 1 5.79
CHEMBL4283094 1 5.78
CHEMBL4291357 1 5.76
CHEMBL4288157 1 5.72
CHEMBL4284271 1 5.70
CHEMBL4283514 1 5.69
CHEMBL4294115 1 5.68
CHEMBL4277456 1 5.49
CHEMBL4286869 1 5.47
CHEMBL4294769 1 5.46
CHEMBL4290279 1 5.45
CHEMBL4279617 1 5.30
CHEMBL4280865 1 5.23
CHEMBL4292588 1 4.98
CHEMBL4281291 1 4.87
CHEMBL4289169 1 4.77
CHEMBL4277453 1 4.74
CHEMBL4288097 1 4.50
CHEMBL4294904 1 4.49
CHEMBL4291505 1 4.35
CHEMBL4284698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4278966 IC50 = 420.0 nM 6.38
CHEMBL4277889 IC50 = 550.0 nM 6.26
CHEMBL4289639 IC50 = 630.0 nM 6.20
CHEMBL4293687 IC50 = 810.0 nM 6.09
CHEMBL4285824 IC50 = 970.0 nM 6.01
CHEMBL4286218 IC50 = 1310.0 nM 5.88
CHEMBL4293025 IC50 = 1400.0 nM 5.85
CHEMBL4277518 IC50 = 1500.0 nM 5.82
CHEMBL4282420 IC50 = 1640.0 nM 5.79
CHEMBL4283094 IC50 = 1660.0 nM 5.78
CHEMBL4291357 IC50 = 1740.0 nM 5.76
CHEMBL4288157 IC50 = 1900.0 nM 5.72
CHEMBL4284271 IC50 = 2010.0 nM 5.70
CHEMBL4283514 IC50 = 2030.0 nM 5.69
CHEMBL4294115 IC50 = 2080.0 nM 5.68
CHEMBL4277456 IC50 = 3250.0 nM 5.49
CHEMBL4286869 IC50 = 3400.0 nM 5.47
CHEMBL4294769 IC50 = 3440.0 nM 5.46
CHEMBL4290279 IC50 = 3530.0 nM 5.45
CHEMBL4279617 IC50 = 5010.0 nM 5.30
CHEMBL4280865 IC50 = 5830.0 nM 5.23
CHEMBL4292588 IC50 = 10480.0 nM 4.98
CHEMBL4281291 IC50 = 13360.0 nM 4.87
CHEMBL4289169 IC50 = 17100.0 nM 4.77
CHEMBL4277453 IC50 = 18031.0 nM 4.74
CHEMBL4288097 IC50 = 31780.0 nM 4.50
CHEMBL4294904 IC50 = 32750.0 nM 4.49
CHEMBL4291505 IC50 = 44420.0 nM 4.35
CHEMBL4284698 IC50 = 146560.0 nM -