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Assay Detail

CHEMBL675569

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Binding
Inhibition of human endothelial Nitric Oxide Synthase expressed in Sf-21 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Expert

Target

Nitric oxide synthase 3 (CHEMBL4803)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of orally bioavailable inhibitors of inducible nitric oxide synthase. Part 1: synthesis and biological evaluation of dihydropyridin-2-imines.
Kawanaka Y, Kobayashi K, Kusuda S, Tatsumi T, Murota M, Nishiyama T, Hisaichi K, Fujii A, Hirai K, Naka M, Komeno M, Nakai H, Toda M.
Bioorg Med Chem Lett (2002) 12 : 2291 -2294
PubMed 12161118 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.04 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75304 1 6.64
CHEMBL74919 1 6.62
CHEMBL75484 1 6.50
CHEMBL72316 1 6.44
CHEMBL76342 1 6.36
CHEMBL75428 1 6.29
CHEMBL75905 1 6.28
CHEMBL75496 1 6.24
CHEMBL260277 1 5.82
CHEMBL308310 1 5.68
CHEMBL74679 1 5.13
CHEMBL75794 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75304 IC50 = 230.0 nM 6.64
CHEMBL74919 IC50 = 240.0 nM 6.62
CHEMBL75484 IC50 = 320.0 nM 6.50
CHEMBL72316 IC50 = 360.0 nM 6.44
CHEMBL76342 IC50 = 440.0 nM 6.36
CHEMBL75428 IC50 = 510.0 nM 6.29
CHEMBL75905 IC50 = 520.0 nM 6.28
CHEMBL75496 IC50 = 580.0 nM 6.24
CHEMBL260277 IC50 = 1500.0 nM 5.82
CHEMBL308310 IC50 = 2100.0 nM 5.68
CHEMBL74679 IC50 = 7400.0 nM 5.13
CHEMBL75794 IC50 = 31000.0 nM 4.51