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Assay Detail

CHEMBL3734236

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

Binding
Inhibition of human Nox2 expressed in COS7 cells co-transfected with human p22-phox,p47phox and p67-phox assessed as inhibition of PMA-induced H2O2 production by amplex red dye based fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Tetrahydroisoquinolines as selective nadph oxidase 2 inhibitors
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 4.44 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3347543 1 4.92
CHEMBL3347550 1 4.70
CHEMBL3347492 1 4.60
CHEMBL3347583 1 4.57
CHEMBL3347503 1 4.52
CHEMBL3733336 1 4.50
CHEMBL3347491 1 4.40
CHEMBL3347542 1 4.40
CHEMBL3347549 1 4.29
CHEMBL3347554 1 4.19
CHEMBL3347502 1 4.11
CHEMBL3347567 1 4.10
CHEMBL3347584 1 -
CHEMBL3347555 1 -
CHEMBL3347566 1 -
CHEMBL3347525 1 -
CHEMBL3347524 1 -
CHEMBL3347501 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3347543 IC50 = 12000.0 nM 4.92
CHEMBL3347550 IC50 = 20000.0 nM 4.70
CHEMBL3347492 IC50 = 25000.0 nM 4.60
CHEMBL3347583 IC50 = 27000.0 nM 4.57
CHEMBL3347503 IC50 = 30000.0 nM 4.52
CHEMBL3733336 IC50 = 32000.0 nM 4.50
CHEMBL3347491 IC50 = 40000.0 nM 4.40
CHEMBL3347542 IC50 = 40000.0 nM 4.40
CHEMBL3347549 IC50 = 51000.0 nM 4.29
CHEMBL3347554 IC50 = 64000.0 nM 4.19
CHEMBL3347502 IC50 = 78000.0 nM 4.11
CHEMBL3347567 IC50 = 79000.0 nM 4.10
CHEMBL3347584 IC50 > 100000.0 nM -
CHEMBL3347555 IC50 - -
CHEMBL3347566 IC50 > 100000.0 nM -
CHEMBL3347525 IC50 > 100000.0 nM -
CHEMBL3347524 IC50 > 100000.0 nM -
CHEMBL3347501 IC50 > 100000.0 nM -