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Found 684 with Last Name = 'cuozzo' and Initial = 'jw'
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50568221(CHEMBL4854947)
Affinity DataKi:  1.25E+3nMAssay Description:Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected in Sf9 cells assessed as inhibitory constant incubated fo...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50568222(CHEMBL4867490)
Affinity DataKi:  1.93E+3nMAssay Description:Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected in Sf9 cells assessed as inhibitory constant incubated fo...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50568220(CHEMBL4873655)
Affinity DataKi:  9.27E+3nMAssay Description:Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected in Sf9 cells assessed as inhibitory constant incubated fo...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM225238(BTK inhibitor, 3)
Affinity DataIC50:  0.550nMT: 2°CAssay Description:The BTK time-resolved FRET-based competitive binding assay and cell-based BTK assays have been previously described.[Xu et al., J.Pharmacol. Exp. The...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM225238(BTK inhibitor, 3)
Affinity DataIC50:  0.550nMAssay Description:Inhibition of recombinant wild type human N-terminal His6-tagged BTK expressed in baculovirus incubated for 20 mins by TR-FRET based competitive bind...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetCollagenase 3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  0.900nMAssay Description:Inhibition of MMP-13 using 5-FAM-TPGPLGL[Dap- (DNP)]ARRK(5-TAMRA)-amide as substrate after 45 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
Google Research Applied Science, Mountain View, California 94043, United States.

Curated by ChEMBL
LigandPNGBDBM50559893(CHEMBL4749356)
Affinity DataIC50:  1nMAssay Description:Inhibition of His-tagged human recombinant soluble epoxide hydrolase pre-incubated for 15 mins before Epoxy-fluor7 substrate addition and measured af...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431093(CHEMBL2338810)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431121(CHEMBL2332037)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50540028(CHEMBL4635769)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of C-terminal FLAG-tagged human autotaxin expressed in Freestyle 293 cells using synthetic substrate FS-3 by fluorescence based assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDisintegrin and metalloproteinase domain-containing protein 17(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of TACE using Mca-PLAQAV-Dpa-RSSSR-NH2 as substrate preincubated 15 mins measured every 30 sec for 30 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50574409(CHEMBL4873534)
Affinity DataIC50:  1.60nMAssay Description:Binding affinity to recombinant His-tagged ERalpha LBD (307 to 554 residue) (unknown origin) expressed in Escherichia coli preincubated for 15 mins f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431118(CHEMBL2332041)
Affinity DataIC50:  1.80nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Praecis Pharmaceuticals

LigandPNGBDBM36463(3-(4-((3-(Aminomethyl)cyclohexyl)methylamino)-6-(3...)
Affinity DataIC50: <2nMpH: 9.5 T: 2°CAssay Description:Selection of DNA-encoded libraries (DELs), which are covalent attachment of encoding double stranded DNA to small-molecule created using a combinatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase 14(Homo sapiens (Human))
Praecis Pharmaceuticals

LigandPNGBDBM36462(3-(4-((3-(Aminomethyl)cyclohexyl)methylamino)-6-(3...)
Affinity DataIC50: <2nMpH: 9.5 T: 2°CAssay Description:Selection of DNA-encoded libraries (DELs), which are covalent attachment of encoding double stranded DNA to small-molecule created using a combinatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Wyeth Research

LigandPNGBDBM21922(8-chloro-4-[(3-chloro-4-fluorophenyl)amino]-6-[(2H...)
Affinity DataIC50:  2nMpH: 7.2 T: 2°CAssay Description:Tpl2/Cot activity was directly assayed using GST-MEK1 as a substrate. The phosphorylation on serine residues was detected by an ELISA. IC50 calculati...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50557619(CHEMBL4796239)
Affinity DataIC50:  2nMAssay Description:Inhibition of recombinant human full-length His-tagged TAK1-TAB1 fusion protein (437 to 504 residues) expressed in baculovirus expression system usin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBifunctional epoxide hydrolase 2(Homo sapiens (Human))
Google Research Applied Science, Mountain View, California 94043, United States.

Curated by ChEMBL
LigandPNGBDBM50559894(CHEMBL4793243)
Affinity DataIC50:  2nMAssay Description:Inhibition of His-tagged human recombinant soluble epoxide hydrolase pre-incubated for 15 mins before Epoxy-fluor7 substrate addition and measured af...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Wyeth Research

LigandPNGBDBM50173838(4-(4-benzylphenylamino)-6-(2-morpholinoethylamino)...)
Affinity DataIC50:  2nMAssay Description:Inhibitory activity against human Tpl2 kinase via quantification of MEK phosphorylationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50540030(CHEMBL4633392)
Affinity DataIC50:  2nMAssay Description:Inhibition of C-terminal FLAG-tagged human autotaxin expressed in Freestyle 293 cells using synthetic substrate FS-3 by fluorescence based assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50540025(CHEMBL4639517)
Affinity DataIC50:  2nMAssay Description:Inhibition of C-terminal FLAG-tagged human autotaxin expressed in Freestyle 293 cells using synthetic substrate FS-3 by fluorescence based assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50091691(CHEMBL3582356)
Affinity DataIC50:  2nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50574409(CHEMBL4873534)
Affinity DataIC50:  2.10nMAssay Description:Binding affinity to ERalpha S463P mutant (unknown origin) expressed in Escherichia coli preincubated for 15 mins followed by ligand addition and meas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50540029(CHEMBL4648587)
Affinity DataIC50:  2.20nMAssay Description:Inhibition of C-terminal FLAG-tagged human autotaxin expressed in Freestyle 293 cells using synthetic substrate FS-3 by fluorescence based assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50091689(CHEMBL3582354)
Affinity DataIC50:  2.60nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431097(CHEMBL2332039)
Affinity DataIC50:  2.70nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50168737((2R,3R)-1-[4-(2-Chloro-4-fluoro-benzyloxy)-benzene...)
Affinity DataIC50:  3nMAssay Description:Inhibition of ADAMTS-4 using WAAG-3R as substrate preincubated for 15 mins measured after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Wyeth Research

LigandPNGBDBM50194998(4-(3-chloro-4-fluorophenylamino)-6-((5-methyl-1H-i...)
Affinity DataIC50:  3nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM225238(BTK inhibitor, 3)
Affinity DataIC50:  3nMAssay Description:Inhibition of recombinant human N-terminal His-tagged BTK C481S mutant expressed in baculovirus infected in Sf9 cells incubated for 1 hr by TR-FRET a...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetMitogen-activated protein kinase kinase kinase 8(Homo sapiens (Human))
Wyeth Research

LigandPNGBDBM50194988(4-(3-chloro-4-fluorophenylamino)-6-((1,5-dimethyl-...)
Affinity DataIC50:  3nMAssay Description:Inhibition of Tpl2 kinase by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50574409(CHEMBL4873534)
Affinity DataIC50:  3.20nMAssay Description:Binding affinity to ERalpha Y537S mutant (unknown origin) expressed in Escherichia coli preincubated for 15 mins followed by ligand addition and meas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-3, mitochondrial(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431118(CHEMBL2332041)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of human His-tagged SIRT3 (102 to 399) expressed in Escherichia coli BL21(DE3) assessed as inhibition of deacetylation of Ac-RHKKAcW-NH2 s...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50540026(CHEMBL4645846)
Affinity DataIC50:  3.5nMAssay Description:Inhibition of C-terminal FLAG-tagged human autotaxin expressed in Freestyle 293 cells using synthetic substrate FS-3 by fluorescence based assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-1(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431097(CHEMBL2332039)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of His-tagged SIRT1 (1 to 747) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase BTK(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM225238(BTK inhibitor, 3)
Affinity DataIC50:  3.80nMAssay Description:Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected in Sf9 cells incubated for 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
LigandPNGBDBM50091692(CHEMBL3582357)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50091696(CHEMBL3582351)
Affinity DataIC50:  4nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-3, mitochondrial(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431097(CHEMBL2332039)
Affinity DataIC50:  4nMAssay Description:Inhibition of human His-tagged SIRT3 (102 to 399) expressed in Escherichia coli BL21(DE3) assessed as inhibition of deacetylation of Ac-RHKKAcW-NH2 s...More data for this Ligand-Target Pair
TargetNAD-dependent protein deacetylase sirtuin-1(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431093(CHEMBL2338810)
Affinity DataIC50:  4.30nMAssay Description:Inhibition of His-tagged SIRT1 (1 to 747) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after...More data for this Ligand-Target Pair
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431117(CHEMBL2332042)
Affinity DataIC50:  4.40nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50091695(CHEMBL3582350)
Affinity DataIC50:  4.40nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50574409(CHEMBL4873534)
Affinity DataIC50:  4.70nMAssay Description:Binding affinity to ERalpha D538G mutant (unknown origin) expressed in Escherichia coli preincubated for 15 mins followed by ligand addition and meas...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431119(CHEMBL2332040)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-3, mitochondrial(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431121(CHEMBL2332037)
Affinity DataIC50:  4.90nMAssay Description:Inhibition of human His-tagged SIRT3 (102 to 399) expressed in Escherichia coli BL21(DE3) assessed as inhibition of deacetylation of Ac-RHKKAcW-NH2 s...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50557620(CHEMBL4752978)
Affinity DataIC50:  5nMAssay Description:Inhibition of recombinant human full-length His-tagged TAK1-TAB1 fusion protein (437 to 504 residues) expressed in baculovirus expression system usin...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
X-Chem

Curated by ChEMBL
LigandPNGBDBM50574413(CHEMBL4873959)
Affinity DataIC50:  5.30nMAssay Description:Binding affinity to recombinant His-tagged ERalpha LBD (307 to 554 residue) (unknown origin) expressed in Escherichia coli preincubated for 15 mins f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-1(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431121(CHEMBL2332037)
Affinity DataIC50:  5.30nMAssay Description:Inhibition of His-tagged SIRT1 (1 to 747) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-2(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431115(CHEMBL2332044)
Affinity DataIC50:  5.40nMAssay Description:Inhibition of His-tagged SIRT2 (1 to 389) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate incubated for 20 mins prior to substrat...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNAD-dependent protein deacetylase sirtuin-1(Homo sapiens (Human))
Sirtris A Gsk

Curated by ChEMBL
LigandPNGBDBM50431116(CHEMBL2332043)
Affinity DataIC50:  5.80nMAssay Description:Inhibition of His-tagged SIRT1 (1 to 747) (unknown origin)-mediated deacetylation of Ac-RHKKAcW-NH2 substrate preincubated for 20 mins measured after...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetA disintegrin and metalloproteinase with thrombospondin motifs 4(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50122453(CHEMBL3622491)
Affinity DataIC50:  6nMAssay Description:Inhibition of recombinant human ADAMTS4 (213 to 575 amino acid residues) using WAAG-3R as substrate preincubated for 15 mins followed by substrate ad...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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