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Assay Detail

CHEMBL678075

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

Binding
Inhibitory concentration against recombinant human Endothelial nitric oxide synthase
11
Total Activities
11
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

Dihydroquinolines with amine-containing side chains as potent n-NOS inhibitors.
Jaroch S, Hölscher P, Rehwinkel H, Sülzle D, Burton G, Hillmann M, McDonald FM.
Bioorg Med Chem Lett (2003) 13 : 1981 -1984
PubMed 12781178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.39 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL227744 NITROARGININE 1.0 1 6.50
CHEMBL256147 TILARGININE 3.0 1 6.27
CHEMBL7890 L-NAME 2.0 1 5.82
CHEMBL61969 1 5.48
CHEMBL293212 1 5.46
CHEMBL292099 1 5.21
CHEMBL542132 1 5.17
CHEMBL552822 1 5.06
CHEMBL545441 1 5.03
CHEMBL544514 1 5.02
CHEMBL538997 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL227744 NITROARGININE IC50 = 320.0 nM 6.50
CHEMBL256147 TILARGININE IC50 = 540.0 nM 6.27
CHEMBL7890 L-NAME IC50 = 1500.0 nM 5.82
CHEMBL61969 IC50 = 3300.0 nM 5.48
CHEMBL293212 IC50 = 3500.0 nM 5.46
CHEMBL292099 IC50 = 6200.0 nM 5.21
CHEMBL542132 IC50 = 6700.0 nM 5.17
CHEMBL552822 IC50 = 8700.0 nM 5.06
CHEMBL545441 IC50 = 9400.0 nM 5.03
CHEMBL544514 IC50 = 9600.0 nM 5.02
CHEMBL538997 IC50 = 52000.0 nM 4.28