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Found 886 with Last Name = 'filippakopoulos' and Initial = 'p'
TargetGlycogen synthase kinase-3 beta(Sus scrofa)
University Of Athens

Curated by ChEMBL
LigandPNGBDBM7401((2 Z,3 E)-6-Bromoindirubin-3 -oxime | (3E)-6-bromo...)
Affinity DataIC50:  5nMAssay Description:Inhibition of porcine brain GSK3beta using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrateMore data for this Ligand-Target Pair
TargetAurora kinase A(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM81552(Benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one, 1...)
Affinity DataIC50:  8nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChromatin remodeling regulator CECR2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50504160(CHEMBL3133807 | US11773085, Compound B25)
Affinity DataIC50:  9.40nMAssay Description:Inhibition of BAZ2A (unknown origin) after 30 mins by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSerine/threonine-protein kinase pim-3(Homo sapiens (Human))
Clermont Universit£

Curated by ChEMBL
LigandPNGBDBM50299249(1,10-Dihydropyrrolo[2,3-a]carbazole-3-carbaldehyde...)
Affinity DataIC50:  10nMAssay Description:Inhibition of Pim-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  10nMAssay Description:Inhibition of rat DYRK1A isolated from brain using KKISGRLSPIMTEQ as substrate and [gamma33P]ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  15nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase B(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM81552(Benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one, 1...)
Affinity DataIC50:  24nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50210164(CHEMBL2132936)
Affinity DataIC50:  25nMAssay Description:Inhibition of [3H]-Nalpha-methylhistamine binding to H3 receptor in guinea-pig brain membranesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  28nMAssay Description:Inhibition of human recombinant GST-tagged DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  34nMAssay Description:Inhibition of rat DYRK1A isolated from brain using KKISGRLSPIMTEQ as substrate and [gamma33P]ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  35nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-3(Homo sapiens (Human))
Clermont Universit£

Curated by ChEMBL
LigandPNGBDBM50299245(7-Bromo-1,10-dihydropyrrolo[2,3-a]carbazole-3-carb...)
Affinity DataIC50:  40nMAssay Description:Inhibition of Pim-3More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347748(CHEMBL1802356)
Affinity DataIC50:  40nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
University Hospital Basel

LigandPNGBDBM35053(K00486)
Affinity DataIC50:  40nMpH: 7.5 T: 2°CAssay Description:Phosphorylation reactions were monitored using a coupled-enzyme assay in which ADP production was coupled to NADH oxidation by pyruvate kinase and la...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  40nMAssay Description:Inhibition of rat recombinant GST-tagged DYRK1A using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  40nMAssay Description:Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAurora kinase C(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM81552(Benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one, 1...)
Affinity DataIC50:  41nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  44nMAssay Description:Inhibition of human recombinant GST-tagged DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by sc...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347744(CHEMBL1803083)
Affinity DataIC50:  47nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 9(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50504160(CHEMBL3133807 | US11773085, Compound B25)
Affinity DataIC50:  47nMAssay Description:Displacement of H3K14Ac from BAZ2B (unknown origin) preincubated for 30 mins with non-biotinylated peptide followed by addition of biotinylated pepti...More data for this Ligand-Target Pair
TargetChromatin remodeling regulator CECR2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50504160(CHEMBL3133807 | US11773085, Compound B25)
Affinity DataIC50:  48nMAssay Description:Inhibition of BAZ2A (unknown origin) after 30 mins by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
University Hospital Basel

LigandPNGBDBM81550(Furan thiazolidinediones, A47)
Affinity DataIC50:  49nM Kd:  40nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-2(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM81550(Furan thiazolidinediones, A47)
Affinity DataIC50:  49nM Kd:  23nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
University Hospital Basel

LigandPNGBDBM35052(K00152 | US10047093, 8-39 | US10392392, Example 8-...)
Affinity DataIC50:  50nMpH: 7.5 T: 2°CAssay Description:Phosphorylation reactions were monitored using a coupled-enzyme assay in which ADP production was coupled to NADH oxidation by pyruvate kinase and la...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK4(Mus musculus)
Cnrs

Curated by ChEMBL
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  50nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  55nMAssay Description:Inhibition of human recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]AT...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  56nMAssay Description:Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP ...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347746(CHEMBL1803085)
Affinity DataIC50:  60nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347746(CHEMBL1803085)
Affinity DataIC50:  60nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase pim-1(Homo sapiens (Human))
University Hospital Basel

LigandPNGBDBM50363167(CHEMBL1945559)
Affinity DataIC50:  60nMAssay Description:Inhibition of PIM1 using ATP as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  60nMAssay Description:Inhibition of human recombinant full length GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  60nMAssay Description:Inhibition of human recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]AT...More data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347745(CHEMBL1803084)
Affinity DataIC50:  61nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK4(Mus musculus)
Cnrs

Curated by ChEMBL
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  64nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50292406(CHEMBL485053 | leucettamine B)
Affinity DataIC50:  66nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50347748(CHEMBL1802356)
Affinity DataIC50:  66nMAssay Description:Inhibition of rat recombinant GST-tagged DYRK1A using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 beta(Sus scrofa)
University Of Athens

Curated by ChEMBL
LigandPNGBDBM50426336(CHEMBL2321952)
Affinity DataIC50:  70nMAssay Description:Inhibition of porcine brain GSK3beta using YRRAAVPPSPSLSRHSSPHQSpEDEEE as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  71nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM100152(7-methoxy-1-methyl-9H-beta-carboline;hydrochloride...)
Affinity DataIC50:  72nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347750(CHEMBL1802358)
Affinity DataIC50:  73nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by sci...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347769(CHEMBL1802852)
Affinity DataIC50:  73nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHomeodomain-interacting protein kinase 2(Homo sapiens (Human))
Harvard Medical School

LigandPNGBDBM81551(Furan thiazolidinediones, A64)
Affinity DataIC50:  74nM Kd:  9.5nMAssay Description:In vitro biochemical assays were performed in parallel to determine the most potent tool compound.More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50365262((+)-JQ1 | (S)-JQ1 (1) | CHEMBL1957266 | JQ1 | US10...)
Affinity DataIC50:  77nMAssay Description:Binding affinity to human BRD4 bromodomain 1 using H4Ac4 peptide by amplified luminescent proximity homogeneous assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50365262((+)-JQ1 | (S)-JQ1 (1) | CHEMBL1957266 | JQ1 | US10...)
Affinity DataIC50:  77nMAssay Description:Inhibition of recombinant His-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins follow...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetChromatin remodeling regulator CECR2(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM50504160(CHEMBL3133807 | US11773085, Compound B25)
Affinity DataIC50:  79nMAssay Description:Inhibition of BAZ2A (unknown origin) after 30 mins by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCREB-binding protein(Homo sapiens (Human))
University Of Oxford

Curated by ChEMBL
LigandPNGBDBM188519(SGC-CBP30)
Affinity DataIC50:  79nMAssay Description:Inhibition of human CREBBP by AlphaScreen assayMore data for this Ligand-Target Pair
TargetDual specificity tyrosine-phosphorylation-regulated kinase 2(Homo sapiens (Human))
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347747(CHEMBL1802355)
Affinity DataIC50:  80nMAssay Description:Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation countingMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDual specificity protein kinase CLK1(Mus musculus)
Universite£? De Rennes 1

Curated by ChEMBL
LigandPNGBDBM50347772(CHEMBL1802855)
Affinity DataIC50:  80nMAssay Description:Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 5(Homo sapiens (Human))
University Of Athens

Curated by ChEMBL
LigandPNGBDBM7401((2 Z,3 E)-6-Bromoindirubin-3 -oxime | (3E)-6-bromo...)
Affinity DataIC50:  83nMAssay Description:Inhibition of human recombinant CDK5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCalcium/calmodulin-dependent protein kinase type II subunit beta(Homo sapiens (Human))
Ludwig-Maximilians University Of Munich

Curated by ChEMBL
LigandPNGBDBM50363167(CHEMBL1945559)
Affinity DataIC50:  83nMAssay Description:Inhibition of CaMK2 using ATP as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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