Compile Data Set for Download or QSAR
Found 2019 Enz. Inhib. hit(s) with Target = 'Glycogen synthase kinase-3 alpha'
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8336(N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-...)
Affinity DataKi:  0.0800nM ΔG°:  -57.1kJ/molepH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8337(N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyrida...)
Affinity DataKi:  0.110nM ΔG°:  -56.3kJ/molepH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8339(N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyrida...)
Affinity DataKi:  0.190nM ΔG°:  -54.9kJ/molepH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8338(N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-c]pyrida...)
Affinity DataKi:  0.950nM ΔG°:  -51.0kJ/molepH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8296(3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-...)
Affinity DataKi:  9nMAssay Description:Competitive inhibition of full length recombinant human GSK-3alpha expressed in baculovirus infected insect Sf9 cells using GS-2 peptide as substrate...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8296(3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-...)
Affinity DataKi:  9.10nM ΔG°:  -45.4kJ/mole IC50:  34.3nMpH: 7.0 T: 2°CAssay Description:In vitro kinase inhibition assay using purified GSK-3 alpha from insect cells, was incubated at room temperature with substrate, and test compounds i...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50563322(CHEMBL4777349)
Affinity DataKi:  13nMAssay Description:Inhibition of human GSKalpha S449A mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50402020(CHEMBL2205426)
Affinity DataKi:  21nMAssay Description:Inhibition of recombinant GSK3A after 1 hr by scintillation counter analysis in presence of gamma-[33P]ATPMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8297(3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophen...)
Affinity DataKi:  30.8nM ΔG°:  -42.4kJ/mole IC50:  77.5nMpH: 7.0 T: 2°CAssay Description:In vitro kinase inhibition assay using purified GSK-3 alpha from insect cells, was incubated at room temperature with substrate, and test compounds i...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM350085(3-[3-[4-[dideuterio(methylamino)methyl]phenyl]isox...)
Affinity DataKi:  33nMAssay Description:ATP competitive inhibition of human GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50563323(CHEMBL4791586)
Affinity DataKi:  43nMAssay Description:Inhibition of human GSKalpha S449A mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50073190(CHEMBL3408213 | US11471446, Compound DBA-11)
Affinity DataKi:  231nMAssay Description:Inhibition of human GSKalpha S449A mutant (2 to 3nd residues) using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE as substrate incubated for 40 mins in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50224883(7-chloro-3-oxo-8-[(thiazol-5-ylmethyl)-amino]-11,1...)
Affinity DataKi:  911nMAssay Description:Inhibition of GSK3 alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50277583(2-amino-4-methyl-1,3-thiazol-5-yl)-N-[4-(morpholin...)
Affinity DataKi: >1.00E+4nMAssay Description:Inhibition of GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118096(US8664219, I-16 | US8664219, I-8)
Affinity DataIC50:  0.300nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM188514(4,7,7-trimethyl-4-phenyl-3-(trifluoromethyl)-2,4,6...)
Affinity DataIC50:  0.400nMAssay Description:Inhibition of GSK3alpha (unknown origin) by ADP-glo analysisMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM188514(4,7,7-trimethyl-4-phenyl-3-(trifluoromethyl)-2,4,6...)
Affinity DataIC50:  0.400nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118098(US8664219, I-10)
Affinity DataIC50:  0.5nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50573930(CHEMBL4856177)
Affinity DataIC50:  0.600nMAssay Description:Inhibition of human GSK3A using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate incubated for 2 hrs by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM122537(US8735593, I-5)
Affinity DataIC50:  0.600nMpH: 7.5 T: 2°CAssay Description:Compounds of the present invention were screened for their ability to inhibit GSK-3β (AA 1-420) activity using a standard coupled enzyme system ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50313013(CHEMBL1080901 | CT-98024 | N2-(2-(4-(2,4-dichlorop...)
Affinity DataIC50:  0.650nMAssay Description:Inhibition of GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118093(US8664219, I-3)
Affinity DataIC50:  0.700nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8349(6-aryl-pyrazolo[3,4-b]pyridine analogue 13 | CHEMB...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8349(6-aryl-pyrazolo[3,4-b]pyridine analogue 13 | CHEMB...)
Affinity DataIC50:  0.800nMpH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8350(6-aryl-pyrazolo[3,4-b]pyridine analogue 14 | N-[5-...)
Affinity DataIC50:  1nMpH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8359(6-aryl-pyrazolo[3,4-b]pyridine analogue 23 | N-[5-...)
Affinity DataIC50:  1nMAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118102(US8664219, I-18)
Affinity DataIC50:  1nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8350(6-aryl-pyrazolo[3,4-b]pyridine analogue 14 | N-[5-...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50150699(3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetr...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human GSK-3alpha S449A mutant (2 to end residues) using phospho GS2 peptide as substrate after 40 mins in presence of [gamma-33ATP] by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118094(US8664219, I-4)
Affinity DataIC50:  1nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50150699(3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetr...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of human GSK-3alpha using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate measured in presence of [gamma-33P]ATP by radiometric assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50601417(CHEMBL5178166)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of GSK3alpha (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50150699(3-(9-fluoro-2-(piperidine-1-carbonyl)-1,2,3,4-tetr...)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of GSK3alpha (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50389083(CHEMBL2064535)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118097(US8664219, I-9)
Affinity DataIC50:  2nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118103(US8664219, I-19)
Affinity DataIC50:  2nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50389079(CHEMBL2064532)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM122535(US8735593, I-3)
Affinity DataIC50:  2nMpH: 7.5 T: 2°CAssay Description:Compounds of the present invention were screened for their ability to inhibit GSK-3β (AA 1-420) activity using a standard coupled enzyme system ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50325983(6-(2-(4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidaz...)
Affinity DataIC50:  2nMAssay Description:A selection of compounds was screened against a selected panel of kinases based on single point inhibitory ability to determine absolute inhibitory a...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118105(US8664219, I-23)
Affinity DataIC50:  2nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM2579((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of human GSK3A using YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM188512((R)-4-(2-methoxyphenyl)-7,7-dimethyl-3-(trifluorom...)
Affinity DataIC50:  3nMpH: 7.5 T: 2°CAssay Description:Purified GSK3beta was incubated with tested compounds in doses in the presence of 4.3 uM of ATP and 1.5uM peptide substrate (Peptide 15, Caliper, MA)...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118096(US8664219, I-16 | US8664219, I-8)
Affinity DataIC50:  3nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM122533(US8735593, I-1)
Affinity DataIC50:  3nMpH: 7.5 T: 2°CAssay Description:Compounds of the present invention were screened for their ability to inhibit GSK-3β (AA 1-420) activity using a standard coupled enzyme system ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118104(US8664219, I-21)
Affinity DataIC50:  3nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM118101(US8664219, I-17)
Affinity DataIC50:  3nMAssay Description:Compounds are screened for their ability to inhibit the phosphorylation of tyrosine (TYR) residues through the use of western blotting of Jurkat cell...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8330(N-{5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl}butan...)
Affinity DataIC50:  4nMpH: 7.0 T: 2°CAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8357(6-aryl-pyrazolo[3,4-b]pyridine analogue 21 | CHEMB...)
Affinity DataIC50:  4nMAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM8357(6-aryl-pyrazolo[3,4-b]pyridine analogue 21 | CHEMB...)
Affinity DataIC50:  4nMAssay Description:The biochemical activity of compounds was determined by incubation with specific enzyme and substrate in the presence 10 uM ATP/ [gamma-33P] ATP. Aft...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlycogen synthase kinase-3 alpha(Homo sapiens (Human))
GlaxoSmithKline

LigandPNGBDBM50291370(CHEMBL4172418)
Affinity DataIC50:  4nMAssay Description:Inhibition of human GSK3alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Displayed 1 to 50 (of 2019 total ) | Next | Last >>
Jump to: