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Found 14 Enz. Inhib. hit(s) with Target = 'Caspase-3' and Monomerid = 10246
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataKi:  0.230nM ΔG°:  -55.0kJ/molepH: 7.5 T: 2°CAssay Description:The effectiveness of compounds against the activity of human recombinant caspase-1-8 was measured using fluorometric assays. Assays were carried out ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataKi:  77nMAssay Description:Enzyme activities with or without inhibitors were measured using a fluorescence assay. The formation of the cleavage product AFC was monitored for 90...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  0.200nMAssay Description:Inhibition of recombinant human caspase-3 using Ac-LDEVD-AMC as substrate assessed as accumulation of 7-AMC incubated for 10 mins followed by substra...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human recombinant caspase 3 assessed as fluorescent 7-amido-4-methylcoumarin releaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of His-tagged human recombinant caspase 3 expressed in Escherichia coli using acetyl-Asp-Glu-Val-Asp-7- amido-4-methylcoumarin (Ac-DEVD-AM...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  2.20nMAssay Description:The caspase enzymatic activity was determined by measuring the accumulation of a fluorogenic product. All assays were prepared in 96-well format. Rec...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  3.10nMpH: 7.5 T: 2°CAssay Description:The substrate peptides terminating in AMC are processed by caspases with or without inhibitors. The amount of AMC released was determined by using a ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  3.80nMpH: 7.4 T: 2°CAssay Description:The substrate peptides terminating in AMC are processed by caspases with or without inhibitors. The amount of AMC released was determined by using a ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  21nMpH: 7.5 T: 2°CAssay Description:The rate of chromogenic substrate hydrolysis was monitored by the change of absorbance at 405 nm for 3 min. Compounds were tested in duplicate. The I...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  27nMpH: 7.0 T: 2°CAssay Description:The substrate peptides terminating in AMC are processed by caspases with or without inhibitors, and the accumulation of AMC was assessed with a Cytof...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  27nMpH: 7.0 T: 2°CAssay Description:The substrate peptides terminating in AMC are processed by caspases with or without inhibitors, and the accumulation of AMC was assessed with a Cytof...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  43.9nMpH: 7.0 T: 2°CAssay Description:The substrate peptides terminating in AMC are processed by caspases with or without inhibitors, and the accumulation of AMC was assessed with a Cytof...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  76nMAssay Description:Inhibition of recombinant human caspase-3 activity using Ac-DEVD-AMC as substrate preincubated for 10 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed