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Assay Detail

CHEMBL750653

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

Binding
Inhibition of cloned (from RNA) human Neuronal nitric oxide synthase
22
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Nitric oxide synthase 1 (CHEMBL3568)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.
Hagen TJ, Bergmanis AA, Kramer SW, Fok KF, Schmelzer AE, Pitzele BS, Swenton L, Jerome GM, Kornmeier CM, Moore WM, Branson LF, Connor JR, Manning PT, Currie MG, Hallinan EA.
J Med Chem (1998) 41 : 3675 -3683
PubMed 9733492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.33 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552935 1 6.77
CHEMBL541081 1 6.41
CHEMBL227744 NITROARGININE 1.0 1 6.30
CHEMBL553119 1 6.07
CHEMBL542710 4 5.88
CHEMBL545059 4 5.60
CHEMBL545291 1 5.52
CHEMBL541090 1 5.33
CHEMBL543886 1 5.26
CHEMBL552936 2 5.08
CHEMBL555587 1 5.01
CHEMBL256147 TILARGININE 3.0 1 5.00
CHEMBL553678 2 4.92
CHEMBL543888 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552935 IC50 = 170.0 nM 6.77
CHEMBL541081 IC50 = 390.0 nM 6.41
CHEMBL227744 NITROARGININE IC50 = 500.0 nM 6.30
CHEMBL553119 IC50 = 850.0 nM 6.07
CHEMBL542710 IC50 = 1310.0 nM 5.88
CHEMBL545059 IC50 = 2530.0 nM 5.60
CHEMBL545291 IC50 = 3000.0 nM 5.52
CHEMBL542710 IC50 = 3200.0 nM 5.50
CHEMBL541090 IC50 = 4700.0 nM 5.33
CHEMBL542710 IC50 = 5370.0 nM 5.27
CHEMBL545059 IC50 = 5440.0 nM 5.26
CHEMBL543886 IC50 = 5460.0 nM 5.26
CHEMBL552936 IC50 = 8290.0 nM 5.08
CHEMBL545059 IC50 = 9050.0 nM 5.04
CHEMBL555587 IC50 = 9800.0 nM 5.01
CHEMBL256147 TILARGININE IC50 = 10000.0 nM 5.00
CHEMBL552936 IC50 = 11200.0 nM 4.95
CHEMBL553678 IC50 = 12100.0 nM 4.92
CHEMBL543888 IC50 = 20000.0 nM 4.70
CHEMBL542710 IC50 = 20600.0 nM 4.69
CHEMBL553678 IC50 = 38300.0 nM 4.42
CHEMBL545059 IC50 = 45700.0 nM 4.34