Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL831101

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

Binding
Inhibitory activity against human Endothelial nitric oxide synthase (eNOS)
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bicyclic amidine inhibitors of nitric oxide synthase: discovery of perhydro-iminopyrindine and perhydro-iminoquinoline as potent, orally active inhibitors of inducible nitric oxide synthase.
Guthikonda RN, Shah SK, Pacholok SG, Humes JL, Mumford RA, Grant SK, Chabin RM, Green BG, Tsou N, Ball R, Fletcher DS, Luell S, Euan MacIntyre D, Maccoss M.
Bioorg Med Chem Lett (2005) 15 : 1997 -2001
PubMed 15808455 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.67 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6808 1 6.84
CHEMBL191242 2 6.44
CHEMBL269058 1 6.20
CHEMBL191675 1 6.08
CHEMBL433589 1 6.06
CHEMBL365804 1 5.70
CHEMBL190655 1 5.35
CHEMBL193007 1 5.26
CHEMBL364230 1 4.90
CHEMBL192033 1 4.82
CHEMBL6656 1 4.07
CHEMBL370922 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6808 IC50 = 146.0 nM 6.84
CHEMBL191242 IC50 = 360.0 nM 6.44
CHEMBL191242 IC50 = 470.0 nM 6.33
CHEMBL269058 IC50 = 630.0 nM 6.20
CHEMBL191675 IC50 = 830.0 nM 6.08
CHEMBL433589 IC50 = 870.0 nM 6.06
CHEMBL365804 IC50 = 2000.0 nM 5.70
CHEMBL190655 IC50 = 4500.0 nM 5.35
CHEMBL193007 IC50 = 5500.0 nM 5.26
CHEMBL364230 IC50 = 12500.0 nM 4.90
CHEMBL192033 IC50 = 15300.0 nM 4.82
CHEMBL6656 IC50 = 85000.0 nM 4.07
CHEMBL370922 IC50 > 5000.0 nM -