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Assay Detail

CHEMBL690699

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 endothelial NOS (e NOS) from HUVEC cells
24
Total Activities
24
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

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 24 5.06 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7945 1 6.80
CHEMBL256147 TILARGININE 3.0 1 6.52
CHEMBL8272 1 6.05
CHEMBL7891 1 5.70
CHEMBL7889 L-NIL 1 5.62
CHEMBL7890 L-NAME 2.0 1 5.57
CHEMBL7931 1 5.44
CHEMBL8390 1 5.40
CHEMBL266226 1 5.30
CHEMBL267075 1 5.30
CHEMBL7934 1 5.22
CHEMBL8065 1 5.10
CHEMBL440270 1 5.05
CHEMBL273659 1 5.05
CHEMBL268668 1 4.92
CHEMBL274402 1 4.72
CHEMBL8088 1 4.40
CHEMBL7969 1 4.36
CHEMBL268403 1 4.36
CHEMBL275955 1 4.26
CHEMBL225304 PIMAGEDINE 2.0 1 4.14
CHEMBL414608 1 4.10
CHEMBL7873 1 4.07
CHEMBL7946 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7945 IC50 = 160.0 nM 6.80
CHEMBL256147 TILARGININE IC50 = 300.0 nM 6.52
CHEMBL8272 IC50 = 900.0 nM 6.05
CHEMBL7891 IC50 = 2000.0 nM 5.70
CHEMBL7889 L-NIL IC50 = 2400.0 nM 5.62
CHEMBL7890 L-NAME IC50 = 2700.0 nM 5.57
CHEMBL7931 IC50 = 3600.0 nM 5.44
CHEMBL8390 IC50 = 4000.0 nM 5.40
CHEMBL266226 IC50 = 5000.0 nM 5.30
CHEMBL267075 IC50 = 5000.0 nM 5.30
CHEMBL7934 IC50 = 6000.0 nM 5.22
CHEMBL8065 IC50 = 8000.0 nM 5.10
CHEMBL440270 IC50 = 9000.0 nM 5.05
CHEMBL273659 IC50 = 9000.0 nM 5.05
CHEMBL268668 IC50 = 12000.0 nM 4.92
CHEMBL274402 IC50 = 19000.0 nM 4.72
CHEMBL8088 IC50 = 40000.0 nM 4.40
CHEMBL7969 IC50 = 44000.0 nM 4.36
CHEMBL268403 IC50 = 44000.0 nM 4.36
CHEMBL275955 IC50 = 55000.0 nM 4.26
CHEMBL225304 PIMAGEDINE IC50 = 72000.0 nM 4.14
CHEMBL414608 IC50 = 80000.0 nM 4.10
CHEMBL7873 IC50 = 86000.0 nM 4.07
CHEMBL7946 IC50 = 100000.0 nM 4.00