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Found 8 Enz. Inhib. hit(s) with Target = 'Glutaminyl-peptide cyclotransferase' and Ligand = 'BDBM50299853'
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataKi:  6nMAssay Description:This novel assay was used to determine the kinetic parameters for most of the QC substrates. QC activity was analyzed spectrophotometrically using a ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataKi:  6.30nMAssay Description:Inhibition of human glutaminyl cyclase expressed in Pichia pastoris by pGAP coupled enzyme assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminyl-peptide cyclotransferase(Mus musculus (mouse))
Seoul National University

Curated by ChEMBL
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  22nMAssay Description:Inhibition of mouse glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  29nMAssay Description:Inhibition of human glutaminyl cyclase using L-glutamine-7-amido-4-methylcoumarin as substrate incubated for 10 mins in presence of pyroglutamyl pept...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  29nMAssay Description:Inhibition of human glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 m...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  29nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect ce...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  29nMAssay Description:Inhibition of human recombinant glutaminyl cyclase using H-Gln-AMC hydrobromide as substrate measured after 15 mins by fluorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutaminyl-peptide cyclotransferase(Homo sapiens (Human))
Probiodrug

US Patent
LigandPNGBDBM50299853(1-(3,4-Dimethoxyphenyl)-3-(3-(5-methyl-1H-imidazol...)
Affinity DataIC50:  119nMAssay Description:Inhibition of human glutaminyl cyclase expressed in HEK293 cells using L-glutaminyl-beta-naphthylamine as substrate after 1 hr by fluorometric analys...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed