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Found 460 Enz. Inhib. hit(s) with Target = 'Caspase-8'
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM225((S)-5-5-(1-Carboxymethyl-2-oxo-ethylcarbamoyl)-thi...)
Affinity DataKi:  50nM ΔG°:  -41.7kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM220(5-{[(4-{[(2S)-1-carboxy-3-oxopropan-2-yl]carbamoyl...)
Affinity DataKi:  150nM ΔG°:  -38.9kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM226((S)-5-({5-[1-Carboxymethyl-3-(2-chloro-benzylsulfa...)
Affinity DataKi:  330nM ΔG°:  -37.0kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM227((S)-5-({5-[1-Carboxymethyl-3-(2-chloro-benzylsulfa...)
Affinity DataKi:  710nM ΔG°:  -35.1kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM222((S)-5-({5-[1-Carboxymethyl-3-(2-chloro-benzylsulfa...)
Affinity DataKi:  810nM ΔG°:  -34.8kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM221(5-{[(5-{[(2S)-1-carboxy-3-oxopropan-2-yl]carbamoyl...)
Affinity DataKi:  880nM ΔG°:  -34.6kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM219(5-({[(5-{[(2S)-1-carboxy-4-{[(2-chlorophenyl)methy...)
Affinity DataKi:  4.00E+3nM ΔG°:  -30.8kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM224((S)-5-({5-[1-Carboxymethyl-3-(2-chloro-benzylsulfa...)
Affinity DataKi:  1.90E+4nM ΔG°:  -26.9kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM223((S)-5-({5-[1-Carboxymethyl-3-(2-chloro-benzylsulfa...)
Affinity DataKi:  2.80E+4nM ΔG°:  -26.0kJ/molepH: 7.4 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29570(isatin sulfonamide, 9c)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29571(isatin sulfonamide, 10a)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29572(isatin Michael acceptor (IMA) analogue, 11a)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29573(isatin Michael acceptor (IMA) analogue, 11b)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29574(isatin Michael acceptor (IMA) analogue, 11c)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29575(isatin Michael acceptor (IMA) analogue, 12a)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29576(isatin Michael acceptor (IMA) analogue, 12b)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29577(isatin Michael acceptor (IMA) analogue, 12c)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29569(acs.jmedchem.1c00409_ST.540 | isatin sulfonamide, ...)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM29578(isatin Michael acceptor (IMA) analogue, 13a)
Affinity DataIC50: >5.00E+4nMpH: 7.4 T: 2°CAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM50116260((R)-2-({(2S,5S)-5-[(S)-2-(Acetyl-methyl-amino)-3-(...)
Affinity DataKi:  350nMAssay Description:Compound was tested for its inhibition against Caspase-8More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM50200932((3S)-3-[(2S)-6-(6-{5-[(3aS,6aR)-2-oxo-hexahydro-1H...)
Affinity DataKi:  540nMAssay Description:Inhibition of human caspase 8More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10215(2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4-[3-(trifluo...)
Affinity DataKi:  2.70E+3nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10323((S)-1-Benzyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]s...)
Affinity DataKi: >5.00E+3nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10305((S)-5-[1-(2-Methoxymethyl)pyrrolidinylsulfonyl]isa...)
Affinity DataKi: >2.50E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10216(BI-7E7 | Burnham Institute Compound 2 | ethyl 2-(2...)
Affinity DataKi:  3.00E+4nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10298(1-benzyl-5-nitro-2,3-dihydro-1H-indole-2,3-dione |...)
Affinity DataKi:  3.10E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10318((S)-5-{1-[2-(Phenoxymethyl)pyrrolidinyl]sulfonyl}i...)
Affinity DataKi:  4.90E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10297(1-methyl-5-nitro-2,3-dihydro-1H-indole-2,3-dione |...)
Affinity DataKi: >5.00E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10316((R)-5-{1-[2-(Anilinomethyl)pyrrolidinyl]sulfonyl}i...)
Affinity DataKi: >5.00E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10309(5-(pyrrolidine-1-sulfonyl)-2,3-dihydro-1H-indole-2...)
Affinity DataKi: >5.00E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10315((S)-5-{1-[2-(Anilinomethyl)pyrrolidinyl]sulfonyl}i...)
Affinity DataKi:  8.00E+4nMAssay Description:The substrate peptides terminating in AMC/AFC are processed by caspases with or without inhibitors, and the accumulation of AMC/AFC was assessed with...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10217(2-(2,3-dihydro-1,4-benzodioxin-2-yl)-N-(furan-2-yl...)
Affinity DataIC50:  6.00E+4nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10218(BI-9C3 | Burnham Institute Compound 4 | phenyl 2-(...)
Affinity DataIC50:  6.00E+4nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10219(BI-9B11 | Burnham Institute Compound 5 | [2-(2,3-d...)
Affinity DataIC50:  6.20E+4nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10220(2-(2,3-dihydro-1,4-benzodioxin-2-yl)-1,3-thiazole-...)
Affinity DataIC50:  7.50E+4nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10221(2-(2,3-dihydro-1,4-benzodioxin-2-yl)-N,N-dimethyl-...)
Affinity DataIC50: >2.00E+5nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10222(4-chlorophenyl 2-(2,3-dihydro-1,4-benzodioxin-2-yl...)
Affinity DataIC50: >2.00E+5nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10223(BI-9C5 | Burnham Institute Compound 9 | ethyl 2-(2...)
Affinity DataIC50: >2.00E+5nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10224(4-{[2-(2,3-dihydro-1,4-benzodioxin-2-yl)-1,3-thiaz...)
Affinity DataIC50: >2.00E+5nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10225(2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4-methyl-1,3-...)
Affinity DataIC50: >2.00E+5nMAssay Description:Fluorescent assays were carried out in black 96-well plates. Caspase activity was monitored using a Labsystem Fluoroskan II spectrofluorometer with a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10247(1,2,3,4-tetrahydroisoquinoline-1,3,4-trione | Isoq...)
Affinity DataIC50:  1.91E+3nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10264(2-oxo-1-phenyl-2-[(1,3,4-trioxo-1,2,3,4-tetrahydro...)
Affinity DataIC50:  425nMAssay 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
Ligand InfoPC cidPC sidPDB
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10278(3-Chloro-N-(1,2,3,4-tetrahydro-1,3,4-trioxoisoquin...)
Affinity DataIC50:  575nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10280(3-[(1,3,4-trioxo-1,2,3,4-tetrahydroisoquinolin-6-y...)
Affinity DataIC50:  1.12E+3nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10284(4-Oxo-4-piperidin-1-yl-N-(1,3,4-trioxo-1,2,3,4-tet...)
Affinity DataIC50:  288nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10287(Isoquinoline-1,3,4-trione 13f | N-(2-Methoxy-pheny...)
Affinity DataIC50:  835nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10295(4-nitro-N-(1,3,4-trioxo-1,2,3,4-tetrahydroisoquino...)
Affinity DataIC50:  2.47E+4nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10318((S)-5-{1-[2-(Phenoxymethyl)pyrrolidinyl]sulfonyl}i...)
Affinity DataIC50: >5.00E+4nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10320((S)-1-Methyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]s...)
Affinity DataIC50: >5.00E+4nMAssay 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-8(Homo sapiens (Human))
Sunesis Pharmaceuticals

LigandPNGBDBM10323((S)-1-Benzyl-5-{1-[2-(phenoxymethyl)pyrrolidinyl]s...)
Affinity DataIC50: >5.00E+4nMAssay 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
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