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

CHEMBL693033

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

Functional
Ability to inhibit the conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by e-NOS from HUVEC cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HUVEC
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.
Beaton H, Boughton-Smith N, Hamley P, Ghelani A, Nicholls DJ, Tinker AC, Wallace AV.
Bioorg Med Chem Lett (2001) 11 : 1027 -1030
PubMed 11327581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.08 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8365 1 7.30
CHEMBL8292 1 7.10
CHEMBL8281 1 6.92
CHEMBL268521 1 6.55
CHEMBL256147 TILARGININE 3.0 1 6.52
CHEMBL8105 1 6.12
CHEMBL274405 1 6.04
CHEMBL8041 1 5.72
CHEMBL8106 1 5.40
CHEMBL8302 1 5.30
CHEMBL416696 1 5.02
CHEMBL8304 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8365 IC50 = 50.0 nM 7.30
CHEMBL8292 IC50 = 80.0 nM 7.10
CHEMBL8281 IC50 = 120.0 nM 6.92
CHEMBL268521 IC50 = 280.0 nM 6.55
CHEMBL256147 TILARGININE IC50 = 300.0 nM 6.52
CHEMBL8105 IC50 = 750.0 nM 6.12
CHEMBL274405 IC50 = 920.0 nM 6.04
CHEMBL8041 IC50 = 1900.0 nM 5.72
CHEMBL8106 IC50 = 4000.0 nM 5.40
CHEMBL8302 IC50 = 5000.0 nM 5.30
CHEMBL416696 IC50 = 9500.0 nM 5.02
CHEMBL8304 IC50 = 10000.0 nM 5.00