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Assay Detail

CHEMBL665580

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 i-NOS from human DLD-1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type DLD-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Nitric oxide synthase, inducible (CHEMBL4481)
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 16 6.20 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8292 1 7.40
CHEMBL8365 1 7.29
CHEMBL274405 1 7.05
CHEMBL8281 1 6.96
CHEMBL8041 1 6.82
CHEMBL8302 1 6.82
CHEMBL8105 1 6.72
CHEMBL256147 TILARGININE 3.0 1 6.52
CHEMBL268521 1 6.14
CHEMBL274207 1 5.80
CHEMBL416696 1 5.57
CHEMBL412901 1 5.55
CHEMBL8304 1 5.46
CHEMBL8288 1 5.44
CHEMBL8106 1 5.08
CHEMBL269162 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8292 IC50 = 40.0 nM 7.40
CHEMBL8365 IC50 = 51.0 nM 7.29
CHEMBL274405 IC50 = 89.0 nM 7.05
CHEMBL8281 IC50 = 110.0 nM 6.96
CHEMBL8041 IC50 = 150.0 nM 6.82
CHEMBL8302 IC50 = 150.0 nM 6.82
CHEMBL8105 IC50 = 190.0 nM 6.72
CHEMBL256147 TILARGININE IC50 = 300.0 nM 6.52
CHEMBL268521 IC50 = 730.0 nM 6.14
CHEMBL274207 IC50 = 1600.0 nM 5.80
CHEMBL416696 IC50 = 2700.0 nM 5.57
CHEMBL412901 IC50 = 2800.0 nM 5.55
CHEMBL8304 IC50 = 3500.0 nM 5.46
CHEMBL8288 IC50 = 3600.0 nM 5.44
CHEMBL8106 IC50 = 8300.0 nM 5.08
CHEMBL269162 IC50 = 28000.0 nM 4.55