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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 20 hits in this display   

TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  8nMAssay Description:Inhibition of human recombinant N-terminal GST-tagged PI3K-gamma (39 to 1102 residues) expressed n baculovirus infected TN5 cells using phosphatidyli...More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  8nMAssay Description:Inhibition of PI3Kgamma (unknown origin)More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  8nMAssay Description:Biochemical assay using PI3Ks and diversification of tolyl quinazolinone series.More data for this Ligand-Target Pair
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  9nMAssay Description:Inhibition of human recombinant GST-tagged PI3Kgamma incubated for 180 mins using [33P]gamma-ATP by scintillation proximity assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  30nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged DYRK1A catalytic domain expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
University of California San Francisco

LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  60nMAssay Description:Biochemical assay using PI3Ks and diversification of tolyl quinazolinone series.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
University of California San Francisco

LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  60nMAssay Description:Inhibition of PI3Kalpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  70nMAssay Description:Inhibition of recombinant human GST-tagged CLK1 catalytic domain (129 to 484 residues) expressed in Escherichia coli using GRSRSRSRSRSRSRSR as substr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1B(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  80nMAssay Description:Inhibition of full length recombinant human GST-tagged DYRK1B expressed in insect cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins i...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  100nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged DYRK2 expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incub...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University of California San Francisco

LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  270nMAssay Description:Biochemical assay using PI3Ks and diversification of tolyl quinazolinone series.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  300nMAssay Description:Inhibition of PI3Kdelta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  300nMAssay Description:Biochemical assay using PI3Ks and diversification of tolyl quinazolinone series.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  1.60E+3nMAssay Description:Inhibition of tetracycline-inducible EGFP-DYRK1A (unknown origin) expressed in HEK293 cells coexpressing full length human EGFP-tau protein assessed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform(Homo sapiens (Human))
University of California San Francisco

LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  2.70E+3nMAssay Description:Inhibition of PI3Kbeta (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCDGSH iron-sulfur domain-containing protein 1(Homo sapiens (Human))
Northeast Ohio Medical University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  3.26E+3nMAssay Description:Displacement of [3H]-rosiglitazone from human recombinant C-terminal His-tagged cytosolic domain of mitoNEET (32-108) by scintillation proximity assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Saarland University

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of EGFR (unknown origin) incubated for 15 mins in presence of [gamma-32P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmine oxidase [flavin-containing] B(Homo sapiens (Human))
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  1.30E+4nMAssay Description:Inhibition of human recombinant MAOB by amplex red assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmine oxidase [flavin-containing] B(Homo sapiens (Human))
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  1.30E+4nMAssay Description:Inhibition of human recombinant MAO-B after 15 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAmine oxidase [flavin-containing] A(Homo sapiens (Human))
Northeastern Ohio Universities Colleges Of Medicine And Pharmacy

Curated by ChEMBL
LigandPNGBDBM50324735((5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE...)
Affinity DataIC50:  1.66E+5nMAssay Description:Inhibition of human recombinant MAOA assessed as inhibition of kynuramine conversion to fluorescent metabolite 4-hydroxyquinoline by fluorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed