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Assay Detail

CHEMBL5374273

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

Binding
Inhibition of NOX2 (unknown origin) transfected in COS cells assessed as reduction in PMA-stimulated H2O2 production preincubated for 15 mins followed by PMA stimulation and measured for 1 hr by amplex red dye based fluorescence analysis
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome b-245 heavy chain (CHEMBL1287627)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting NOX2 with Bivalent Small-Molecule p47phox-p22phox Inhibitors.
Zang J, Peters F, Cambet Y, Cifuentes-Pagano E, Hissabu MMS, Dustin CM, Svensson LH, Olesen MM, Poulsen MFL, Jacobsen S, Tuelung PS, Narayanan D, Langkilde AE, Gajhede M, Pagano PJ, Jaquet V, Vilhardt F, Bach A.
J Med Chem (2023) 66 : 14963 -15005
PubMed 37857466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.20 5.48
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419067 1 5.48
CHEMBL5410142 1 4.92
CHEMBL5408659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419067 IC50 = 3300.0 nM 5.48
CHEMBL5410142 IC50 = 12000.0 nM 4.92
CHEMBL5408659 Inhibition - % -