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Assay Detail

CHEMBL665579

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

Functional
Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by inducible NOS (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

3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.
Beaton H, Hamley P, Nicholls DJ, Tinker AC, Wallace AV.
Bioorg Med Chem Lett (2001) 11 : 1023 -1026
PubMed 11327580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.47 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7889 L-NIL 1 6.89
CHEMBL256147 TILARGININE 3.0 1 6.52
CHEMBL414608 1 6.26
CHEMBL266226 1 5.92
CHEMBL7931 1 5.89
CHEMBL8065 1 5.57
CHEMBL8272 1 5.57
CHEMBL274402 1 5.38
CHEMBL225304 PIMAGEDINE 2.0 1 5.35
CHEMBL7969 1 5.33
CHEMBL8088 1 5.26
CHEMBL7946 1 5.05
CHEMBL7890 L-NAME 2.0 1 4.85
CHEMBL8390 1 4.75
CHEMBL7891 1 4.50
CHEMBL268403 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7889 L-NIL IC50 = 130.0 nM 6.89
CHEMBL256147 TILARGININE IC50 = 300.0 nM 6.52
CHEMBL414608 IC50 = 550.0 nM 6.26
CHEMBL266226 IC50 = 1200.0 nM 5.92
CHEMBL7931 IC50 = 1300.0 nM 5.89
CHEMBL8065 IC50 = 2700.0 nM 5.57
CHEMBL8272 IC50 = 2700.0 nM 5.57
CHEMBL274402 IC50 = 4200.0 nM 5.38
CHEMBL225304 PIMAGEDINE IC50 = 4500.0 nM 5.35
CHEMBL7969 IC50 = 4700.0 nM 5.33
CHEMBL8088 IC50 = 5500.0 nM 5.26
CHEMBL7946 IC50 = 9000.0 nM 5.05
CHEMBL7890 L-NAME IC50 = 14000.0 nM 4.85
CHEMBL8390 IC50 = 18000.0 nM 4.75
CHEMBL7891 IC50 = 32000.0 nM 4.50
CHEMBL268403 IC50 = 33000.0 nM 4.48