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Assay Detail

CHEMBL3391327

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

Binding
Inhibition of full length human NOX2 transfected in COS 22 cells assessed as inhibition of Phorbol 12-myristate 13-acetate-stimulated ROS generation by measuring H2O2 production by fluorescence assay in presence of superoxide dismutase
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS 22
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
Cifuentes-Pagano E, Saha J, Csányi G, Ghouleh IA, Sahoo S, Rodríguez A, Wipf P, Pagano PJ, Skoda EM.
Medchemcomm (2013) 4 : 1085 -1092
PubMed 24466406 · DOI

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
CHEMBL3347551 1 4.50
CHEMBL3347542 1 4.40
CHEMBL3347491 1 4.40
CHEMBL3347549 1 4.29
CHEMBL3347554 1 4.19
CHEMBL3347502 1 4.11
CHEMBL3347567 1 4.10
CHEMBL3347555 1 -
CHEMBL3347566 1 -
CHEMBL3347525 1 -
CHEMBL3347524 1 -
CHEMBL3347501 1 -
CHEMBL3347584 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
CHEMBL3347551 IC50 = 32000.0 nM 4.50
CHEMBL3347542 IC50 = 40000.0 nM 4.40
CHEMBL3347491 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
CHEMBL3347555 IC50 - -
CHEMBL3347566 IC50 > 100000.0 nM -
CHEMBL3347525 IC50 > 100000.0 nM -
CHEMBL3347524 IC50 > 100000.0 nM -
CHEMBL3347501 IC50 > 100000.0 nM -
CHEMBL3347584 IC50 > 100000.0 nM -