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Found 578 with Last Name = 'rothfuss' and Initial = 'j'
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM10351(1-(4-Methoxybenzyl)-5-(2-(pyridin-3-yl-oxymethyl)-...)
Affinity DataKi:  4.40nM IC50:  3.90nMAssay 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
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Washington University

Curated by ChEMBL
LigandPNGBDBM31592(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Affinity DataIC50:  0.180nMAssay Description:Inhibition of rat PDE10AMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496801(CHEMBL3222273)
Affinity DataIC50:  0.240nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50391056(CHEMBL2088421)
Affinity DataIC50:  0.280nMAssay Description:Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496803(CHEMBL3218037)
Affinity DataIC50:  0.280nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Washington University

Curated by ChEMBL
LigandPNGBDBM31596(substituted pyrazole, 13)
Affinity DataIC50:  0.300nMAssay Description:Inhibition of rat PDE10AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496811(CHEMBL3222274)
Affinity DataIC50:  0.360nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496800(CHEMBL3218036)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50099491(2-(4-(2-(3-cyclohexyl-1-(4-cyclohexylbutyl)ureido)...)
Affinity DataIC50:  0.460nMAssay Description:Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assayMore data for this Ligand-Target Pair
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50391057(CHEMBL2088422)
Affinity DataIC50:  0.590nMAssay Description:Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496812(CHEMBL3222276)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Washington University School Of Medicine

Curated by ChEMBL
LigandPNGBDBM50496802(CHEMBL3218039)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of human recombinant PDE10A catalytic domain assessed reduction in [3H]cAMP hydrolysis preincubated with enzyme for 5 mins prior to substr...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPeroxisome proliferator-activated receptor alpha(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50099489(2-(4-{2-[1-(4-Cyclohexyl-butyl)-3-(2-methoxy-pheny...)
Affinity DataIC50:  1.90nMAssay Description:Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

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))
Washington University

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-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of caspase 7 by fluorometric assayMore data for this Ligand-Target Pair
TargetCaspase-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  2.95nMAssay 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
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340533((S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-((pyridin-3-...)
Affinity DataIC50:  3.10nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340530((S)-1-(4-methoxybenzyl)-5-(2-((pyridin-3-yloxy)met...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340529((S)-1-(4-(2-fluoroethoxy)benzyl)-5-(2-((pyridin-3-...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50216416(1-(4-bromo-benzyl)-5-[2-(pyridin-3-yl-oxymethyl)-p...)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

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-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50340543((S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)me...)
Affinity DataIC50:  3.80nMAssay Description:Inhibition of caspase 7 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50216421(1-(4-hydroxy-benzyl)-5-[2-(pyridin-3-yl-oxymethyl)...)
Affinity DataIC50:  3.90nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50340547((4S,7S,10S,13S)-4-sec-butyl-7-(2-carboxyethyl)-13-...)
Affinity DataIC50:  4.20nMAssay Description:Inhibition of caspase 8 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10357((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  4.20nMAssay 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))
Washington University

LigandPNGBDBM10352(1-(4-Methylthiobenzyl)-5-(2-(pyridin-3-yl-oxymethy...)
Affinity DataIC50:  4.40nMAssay 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))
Washington University

LigandPNGBDBM50340543((S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)me...)
Affinity DataIC50:  4.5nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-8(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10357((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  4.70nMAssay 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))
Washington University

LigandPNGBDBM50216418(2-{1-(4-bromo-benzyl)-2-oxo-5-[2-(pyridine-3-yloxy...)
Affinity DataIC50:  5.10nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM10350(1-Benzyl-5-(2-(pyridin-3-yl-oxymethyl)-pyrrolidine...)
Affinity DataIC50:  5.20nMAssay 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))
Washington University

LigandPNGBDBM50340542((S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)me...)
Affinity DataIC50:  5.60nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM10347((S)-1-(6-Fluoropyridin-2-yl-methyl)-5-(2-phenoxyme...)
Affinity DataIC50:  5.80nMAssay 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
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Rattus norvegicus (rat))
Washington University

Curated by ChEMBL
LigandPNGBDBM50351893(CHEMBL1825071)
Affinity DataIC50:  6nMAssay Description:Inhibition of rat PDE10AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340537((S)-2-(1-(4-methoxybenzyl)-2-oxo-5-(2-((pyridin-3-...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50340542((S)-1-((1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl)me...)
Affinity DataIC50:  6.10nMAssay Description:Inhibition of caspase 7 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50216416(1-(4-bromo-benzyl)-5-[2-(pyridin-3-yl-oxymethyl)-p...)
Affinity DataIC50:  6.60nMAssay Description:Inhibition of human recombinant caspase 7More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340536((S)-2-(1-(4-(2-fluoroethoxy)benzyl)-2-oxo-5-(2-((p...)
Affinity DataIC50:  7.10nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50340540((S)-2-(1-(4-(2-fluoroethoxy)benzyl)-2-oxo-5-(2-((p...)
Affinity DataIC50:  7.5nMAssay Description:Inhibition of human caspase 3 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50216415(2-{1-benzyl-2-oxo-5-[2-(pyridine-3-yloxymethyl)-py...)
Affinity DataIC50:  7.60nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50216419(2-{1-(4-methoxy-benzyl)-2-oxo-5-[2-(pyridin-3-ylox...)
Affinity DataIC50:  7.80nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM50216417(2-{1-(4-hydroxy-benzyl)-2-oxo-5-[2-(pyridine-3-ylo...)
Affinity DataIC50:  7.80nMAssay Description:Inhibition of human recombinant caspase 3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-6(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM50340548((4S,7S,10S,13S)-10-sec-butyl-7-(2-carboxyethyl)-13...)
Affinity DataIC50:  8nMAssay Description:Inhibition of caspase 6 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-6(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10356((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  8nMAssay 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-1(Homo sapiens (Human))
Washington University

LigandPNGBDBM10355((3S)-3-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-(4-hydr...)
Affinity DataIC50:  8.10nMAssay 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-1(Homo sapiens (Human))
Washington University

LigandPNGBDBM10355((3S)-3-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-(4-hydr...)
Affinity DataIC50:  8.40nMpH: 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-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM10341((S)-1-(4-Methoxybenzyl)-5-(2-phenoxymethyl-azetidi...)
Affinity DataIC50:  8.40nMAssay 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-1(Homo sapiens (Human))
Washington University

LigandPNGBDBM10355((3S)-3-[(2S)-2-[(2S)-2-[(2S)-2-acetamido-3-(4-hydr...)
Affinity DataIC50:  8.40nMAssay Description:Inhibition of caspase 1 by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-3(Homo sapiens (Human))
Washington University

LigandPNGBDBM10353(1-(4-Fluorobenzyl)-5-(2-(pyridin-3-yl-oxymethyl)-p...)
Affinity DataIC50:  8.40nMAssay 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-7(Homo sapiens (Human))
Washington University

Curated by ChEMBL
LigandPNGBDBM10246((4S)-4-{[(1S)-1-{[(2S)-1-carboxy-3-oxopropan-2-yl]...)
Affinity DataIC50:  8.5nMAssay 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
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