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Found 134 with Last Name = 'tisi' and Initial = 'd'
TargetBcl2-associated agonist of cell death(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50270877((R)-4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex...)
Affinity DataKi: <0.5nMAssay Description:Binding affinity to BH3 binding groove of BclXLMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50221972((2S,3S)-2-(4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)p...)
Affinity DataKi:  4.30nMAssay Description:Binding affinity to DPP4More data for this Ligand-Target Pair
TargetReceptor-type tyrosine-protein phosphatase beta(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50270587(5-(3-Cyclohexyl-4'-fluoro-2'-trifluoromethyl-biphe...)
Affinity DataKi:  220nMAssay Description:Inhibition of PtpBMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50178428((S)-2-amino-3-methyl-1-(pyrrolidin-1-yl)butan-1-on...)
Affinity DataKi:  2.00E+3nMAssay Description:Binding affinity to DPP4More data for this Ligand-Target Pair
TargetQueuine tRNA-ribosyltransferase catalytic subunit 1(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50240341(2-AMINOQUINAZOLIN-4(3H)-ONE | 2-Amino-quinazolin-4...)
Affinity DataKi:  2.10E+3nMAssay Description:Inhibition of TGTMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetQueuine tRNA-ribosyltransferase catalytic subunit 1(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50271082(4-(4-methoxyphenethyl)-6-amino-3H-imidazo[4,5-g]qu...)
Affinity DataKi:  3.70E+3nMAssay Description:Inhibition of TGTMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNitric oxide synthase, brain(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50226527(CHEMBL107251 | N-(3-(AMINOMETHYL)BENZYL)ACETAMIDIN...)
Affinity DataKi:  7.30E+3nMAssay Description:Binding affinity nNOSMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedMMDB

TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM13534(CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl...)
Affinity DataIC50:  1.40nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27083(1-(2,6-difluorophenyl)-3-{3-[5-(morpholin-4-ylmeth...)
Affinity DataIC50:  1.5nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27083(1-(2,6-difluorophenyl)-3-{3-[5-(morpholin-4-ylmeth...)
Affinity DataIC50:  2.60nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27082(1-(2-fluorophenyl)-3-{3-[5-(morpholin-4-ylmethyl)-...)
Affinity DataIC50:  2.80nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhenylethanolamine N-methyltransferase(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM13014(7,8-Dichloro-1,2,3,4-tetrahydro-isoquinoline; hydr...)
Affinity DataIC50:  3nMAssay Description:Inhibition of PNMTMore data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27079(N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  3.5nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProthrombin(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM12589((2R,3S)-3-({[5-chloro-2-(1H-1,2,3,4-tetrazol-1-yl)...)
Affinity DataIC50:  4nMAssay Description:Inhibition of thrombinMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-1(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50176510((S)-4-oxo-3-(2-((4-(quinoxalin-2-ylamino)benzamido...)
Affinity DataIC50:  5nMAssay Description:Inhibition of caspase 1More data for this Ligand-Target Pair
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27084(1-cyclohexyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3...)
Affinity DataIC50:  5.20nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27084(1-cyclohexyl-3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3...)
Affinity DataIC50:  5.70nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27078(N-[3-(1H-1,3-benzodiazol-2-yl)-1H-pyrazol-4-yl]ben...)
Affinity DataIC50:  5.90nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27080(4-fluoro-N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-ben...)
Affinity DataIC50:  10nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27082(1-(2-fluorophenyl)-3-{3-[5-(morpholin-4-ylmethyl)-...)
Affinity DataIC50:  10nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27086(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  10nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27081(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  12nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27085(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  13nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27079(N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  15nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDNA ligase(Staphylococcus aureus)
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50444582(CHEMBL3099715)
Affinity DataIC50:  15nMAssay Description:Inhibition of C-terminal 6xHis-tagged full length recombinant Staphylococcus aureus DNA ligase (1 to 312) expressed in Escherichia coli BL21 (DE3) us...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM13534(CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl...)
Affinity DataIC50:  17nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
TargetMethionine aminopeptidase 2(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM17462(1,2,3-triazole analogue, 18 | 5-(3-methylphenyl)-1...)
Affinity DataIC50:  18nMAssay Description:Inhibition of MetAp2More data for this Ligand-Target Pair
TargetDipeptidyl peptidase 4(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM11558((3S)-2-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-1...)
Affinity DataIC50:  23nMAssay Description:Binding affinity to DPP4More data for this Ligand-Target Pair
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27085(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  24nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27086(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  26nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhenylethanolamine N-methyltransferase(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50240934(3-(hydroxymethyl)-N-(3,3,3-trifluoropropyl)-1,2,3,...)
Affinity DataIC50:  28nMAssay Description:Inhibition of PNMTMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Astex

LigandPNGBDBM27078(N-[3-(1H-1,3-benzodiazol-2-yl)-1H-pyrazol-4-yl]ben...)
Affinity DataIC50:  52nMAssay Description:CDK2/cyclinA activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27081(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  54nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Astex

LigandPNGBDBM13344(N-[4-Chloro-3-(3-pyridinyloxymethyl)phenyl]-3-fluo...)
Affinity DataIC50:  65nMpH: 7.4 T: 2°CAssay Description:IC50 is the inhibitor concentration, which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-33P] lab...More data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM27077(N-[3-(1H-1,3-benzodiazol-2-yl)-1H-pyrazol-4-yl]ace...)
Affinity DataIC50:  70nMpH: 7.0 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUrokinase-type plasminogen activator(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50231528(4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-(piperidi...)
Affinity DataIC50:  72nMAssay Description:Inhibition of uPAMore data for this Ligand-Target Pair
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27080(4-fluoro-N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-ben...)
Affinity DataIC50:  75nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase A(Homo sapiens (Human))
Astex

LigandPNGBDBM50270611(4-(6,7-Dimethoxy-9H-pyrimido[4,5-b]indol-4-yl)-pip...)
Affinity DataIC50:  94nMAssay Description:Inhibition of aurora kinase AMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Astex

LigandPNGBDBM27079(N-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  140nMAssay Description:CDK2/cyclinA activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Astex

LigandPNGBDBM27083(1-(2,6-difluorophenyl)-3-{3-[5-(morpholin-4-ylmeth...)
Affinity DataIC50:  160nMAssay Description:CDK2/cyclinA activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Astex

LigandPNGBDBM27085(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  160nMAssay Description:CDK2/cyclinA activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Astex

LigandPNGBDBM27078(N-[3-(1H-1,3-benzodiazol-2-yl)-1H-pyrazol-4-yl]ben...)
Affinity DataIC50:  180nMpH: 8.5 T: 2°CAssay Description:Assays for Aurora kinase was performed in a DELFIA format. Aurora enzyme was incubated with test compound and cross-tide substrate in the reaction bu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCaspase-1(Homo sapiens (Human))
Astex Therapeutics

Curated by ChEMBL
LigandPNGBDBM50176515((S)-4-oxo-3-(6-(4-(quinoxalin-2-ylamino)benzamido)...)
Affinity DataIC50:  190nMAssay Description:Inhibition of caspase 1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Astex

LigandPNGBDBM13354(3-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-1-(4-chl...)
Affinity DataIC50:  196nMpH: 7.4 T: 2°CAssay Description:IC50 is the inhibitor concentration, which inhibits 50% of kinase activity that catalyzes the transfer of the terminal phosphate from [gamma-33P] lab...More data for this Ligand-Target Pair
TargetDNA ligase(Staphylococcus aureus)
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50444581(CHEMBL3099713)
Affinity DataIC50:  220nMAssay Description:Inhibition of C-terminal 6xHis-tagged full length recombinant Staphylococcus aureus DNA ligase (1 to 312) expressed in Escherichia coli BL21 (DE3) us...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDNA ligase(Staphylococcus aureus)
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50444580(CHEMBL3099714)
Affinity DataIC50:  230nMAssay Description:Inhibition of C-terminal 6xHis-tagged full length recombinant Staphylococcus aureus DNA ligase (1 to 312) expressed in Escherichia coli BL21 (DE3) us...More data for this Ligand-Target Pair
TargetCyclin-A2/Cyclin-dependent kinase 2(Homo sapiens (Human))
Astex

LigandPNGBDBM27082(1-(2-fluorophenyl)-3-{3-[5-(morpholin-4-ylmethyl)-...)
Affinity DataIC50:  230nMAssay Description:CDK2/cyclinA activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM27078(N-[3-(1H-1,3-benzodiazol-2-yl)-1H-pyrazol-4-yl]ben...)
Affinity DataIC50:  230nMAssay Description:CDK1/cyclinB activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM27083(1-(2,6-difluorophenyl)-3-{3-[5-(morpholin-4-ylmeth...)
Affinity DataIC50:  290nMAssay Description:CDK1/cyclinB activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM27085(3-{3-[5-(morpholin-4-ylmethyl)-1H-1,3-benzodiazol-...)
Affinity DataIC50:  290nMAssay Description:CDK1/cyclinB activity was determined using a radiometric assay to measure the incorporation of gamma-phosphate from [gamma-33P]-ATP into histone H1. ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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