Any feedback?
Please rate this page
(enzyme.php)
(0/150)

BRENDA support

BRENDA Home
show all | hide all No of entries

Information on EC 2.7.11.26 - tau-protein kinase and Organism(s) Homo sapiens and UniProt Accession P49841

for references in articles please use BRENDA:EC2.7.11.26
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
EC Tree
IUBMB Comments
Activated by tubulin. Involved in the formation of paired helical filaments, which are the main fibrous component of all fibrillary lesions in brain and are associated with Alzheimer's disease.
Specify your search results
Select one or more organisms in this record: ?
This record set is specific for:
Homo sapiens
UNIPROT: P49841
Show additional data
Do not include text mining results
Include (text mining) results
Include results (AMENDA + additional results, but less precise)
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms
Synonyms
amp-activated protein kinase, glycogen synthase kinase, protein kinase 1, gsk3b, extracellular-regulated kinase, gsk-3 beta, protein kinase-a, srpk2, gsk-3alpha, ttbk2, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycogen synthase kinase 3-beta
-
glycogen synthase kinase 3beta
-
glycogen synthase kinase-3
-
glycogen synthase kinase-3 alpha
-
glycogen synthase kinase-3beta
-
glycogen synthase kinase-3beta1
-
glycogen synthase kinase-3beta2
-
glycogen synthetase kinase-3 beta
-
GSK-3beta1
-
GSK-3beta2
-
tau protein kinase
-
cAMP-dependent protein kinase A
-
-
casein kinase 1 delta
-
cyclin-dependent kinase 5
-
-
Gasket protein
-
-
-
-
glycogen synthase kinase
-
-
-
-
glycogen synthase kinase 3
-
-
glycogen synthase kinase 3 beta
-
-
glycogen synthase kinase 3beta
-
-
glycogen synthase kinase-3
glycogen synthase kinase-3alphabeta
-
-
glycogen synthase kinase-3beta
GSK 3-beta
-
-
GSK-3
GSK-3 alpha
-
-
-
-
GSK-3 beta
-
-
-
-
GSK-3alpha
GSK-3beta
GSK-3beta1
-
isoform
GSK-3beta2
-
neuron-specific isoform
GSK3alpha
-
p25-Cdk5 kinase complex
-
-
protein kinase 1
-
-
protein kinase-A
-
-
protein tau kinase
-
-
-
-
serine-threonine kinase
-
-
serum- and glucocorticoid-induced protein kinase 1
-
-
SGK1
-
-
Syk
-
common tyrosine kinase of tau and alpha-synuclein
tau factor protein kinase (phosphorylating)
-
-
-
-
tau kinase
tau protein kinase
tau protein kinase I
-
-
-
-
tau protein kinase I/glycogen synthase kinase 3beta
-
-
tau protein kinase I/GSK-3beta/kinaseFA
-
-
tau protein kinase II (cdk5/p20)
-
-
Tau tubulin kinase 1
-
tau tubulin kinase 2
-
tau-protein kinase I
-
-
tau-tubulin kinase
-
Tau-tubulin kinase 1
tau-tubulin kinase 2
-
-
tauprotein kinase
-
-
TPK I
-
-
TPKI/GSK-3beta
-
-
TPKI/GSK-3beta/FA
-
-
TTBK1
TTBK2
additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [tau-protein] = ADP + O-phospho-[tau-protein]
show the reaction diagram
activation loop structure, substrate binding structure, and catalytic site structure and mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:[tau-protein] O-phosphotransferase
Activated by tubulin. Involved in the formation of paired helical filaments, which are the main fibrous component of all fibrillary lesions in brain and are associated with Alzheimer's disease.
CAS REGISTRY NUMBER
COMMENTARY hide
111694-09-8
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + beta-catenin
ADP + beta-catenin phosphate
show the reaction diagram
-
-
-
?
ATP + DIWKKFELLPTPPLSPSRRSG
ADP + DIWKKFELLP(P)TPPL(P)SPSRRSG
show the reaction diagram
c-Myc
-
?
ATP + DIWKKFELVPSPPTSPPWGL
ADP + DIWKKFELVP(P)SPPT(P)SPPWGL
show the reaction diagram
L-myc
-
?
ATP + EEPQTVPEMPGETPPLSPIDMESQER
ADP + EEPQTVPEMPGE(P)TPPL(P)SPIDMESQER
show the reaction diagram
c-Jun
-
?
ATP + FXVEXTPXCFSRXSSLSSLS
ADP + ?
show the reaction diagram
-
-
-
?
ATP + LLNASGSTSTPAPSRTASFSESR
ADP + LLNASGSTS(P)TPAP(P)SRTASFSESR
show the reaction diagram
ATP-citrate lyase
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
-
-
-
?
ATP + SPPLSPIDMETQER
ADP + (P)SPPLSPIDME(P)TQER
show the reaction diagram
JunD
-
?
ATP + SPVVSGDT(P)SPR
ADP + ?
show the reaction diagram
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
show the reaction diagram
ATP + TPPKSPSAAK
ADP + TPPK(P)SPSAAK
show the reaction diagram
protein tau
-
?
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
show the reaction diagram
phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
show the reaction diagram
protein tau + ATP
phosphorylated protein tau + ADP
show the reaction diagram
the microtubule-associated protein tau is the principal component of the paired helical filaments - PHFs - found in the brains of patients with Alzheimer disease, and PHF-tau is hyperphosphorylated
-
-
?
ATP + alpha-actin
ADP + p35
show the reaction diagram
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
-
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + cAMP response element-binding protein
ADP + phosphorylated cAMP response element-binding protein
show the reaction diagram
-
-
-
-
?
ATP + CCDC92
ADP + phosphorylated CCDC92
show the reaction diagram
-
-
-
?
ATP + CEP164
ADP + phospho-CEP164
show the reaction diagram
-
-
-
?
ATP + CEP164
ADP + phosphorylated CEP164
show the reaction diagram
TTBK2-induced phosphorylations of CEP164 modulate its function, which in turn seems relevant for the process of cilia formation
-
-
?
ATP + CEP83
ADP + phosphorylated CEP83
show the reaction diagram
-
-
-
?
ATP + CEP89
ADP + phosphorylated CEP89
show the reaction diagram
-
-
-
?
ATP + CEP97
ADP + phospho-CEP97
show the reaction diagram
-
-
-
?
ATP + coronavirus nucleocapsid protein
ADP + phosphorylated coronavirus nucleocapsid protein
show the reaction diagram
-
phosphorylation sites are at Ser177, Ser181, Ser184, Ser185, Ser187, Ser189, Ser191, Ser203, and Ser207
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
-
-
-
-
?
ATP + cyclin D1
ADP + phosphorylated cyclin D1
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
-
-
-
-
?
ATP + DVL3
ADP + phosphorylated DVL3
show the reaction diagram
-
-
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
show the reaction diagram
-
-
-
-
?
ATP + FITC-GSRSRTPSLP
ADP + FITC-GSRSRTP-phosphoserine-LP
show the reaction diagram
-
synthetic fluorescence-labeled peptide substrate derived from residues 207-216 of tau protein, phosphorylation of S214 by SGK1
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + heat shock factor-1
ADP + phosphorylated heat shock factor-1
show the reaction diagram
-
-
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
show the reaction diagram
-
-
-
?
ATP + JHMV-N protein
ADP + phosphorylated JHMV-N protein
show the reaction diagram
-
phosphorylation sites are at Ser197, Ser201, Ser-205, and Ser-209
-
-
?
ATP + Jun
ADP + phosphorylated Jun
show the reaction diagram
-
-
-
-
?
ATP + KRREILSRRPpSYR
ADP + ?
show the reaction diagram
-
KRREILSRRPpSYR is selectively phosphorylated by GSK-3 and therefore acts as a competitive inhibitor of other GSK-3 substrates
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
show the reaction diagram
-
isoenzyme TPKII
-
-
?
ATP + mu-calpain
ADP + calpastatin
show the reaction diagram
-
-
-
?
ATP + Myc
ADP + phosphorylated Myc
show the reaction diagram
-
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + p53 phosphate
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
ATP + pyruvate dehydrogenase
ADP + pyruvate dehydrogenase phosphate
show the reaction diagram
-
PDH is phosphorylated and inactivated in vitro and also in betaA-treated hippocampal cultures, resulting in mitochondrial dysfunction which will contribute to neuronal death
-
-
?
ATP + Rabin8
ADP + phosphorylated Rabin8
show the reaction diagram
-
-
-
?
ATP + RSRSRSRSRSRSPPPVSK
ADP + phosphorylated RSRSRSRSRSRSPPPVSK
show the reaction diagram
-
SC35-derived peptide 180-197, recombinant GSK-3beta
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
ATP + tau-protein
ADP + O-phospho-tau-protein
show the reaction diagram
ATP + TDP-43
ADP + phospho-TDP-43
show the reaction diagram
-
-
-
?
ATP + TDP-43
ADP + phosphorylated TDP-43
show the reaction diagram
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
show the reaction diagram
-
-
-
?
ATP + [FRAT-2 protein]
ADP + phosphorylated [FRAT-2 protein]
show the reaction diagram
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, phosphorylation by GSK3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + tau-protein
ADP + O-phospho-tau-protein
show the reaction diagram
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
show the reaction diagram
phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
ATP + alpha-actin
ADP + p35
show the reaction diagram
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
show the reaction diagram
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
show the reaction diagram
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
show the reaction diagram
-
-
-
-
?
ATP + CCDC92
ADP + phosphorylated CCDC92
show the reaction diagram
-
-
-
?
ATP + CEP164
ADP + phosphorylated CEP164
show the reaction diagram
TTBK2-induced phosphorylations of CEP164 modulate its function, which in turn seems relevant for the process of cilia formation
-
-
?
ATP + CEP83
ADP + phosphorylated CEP83
show the reaction diagram
-
-
-
?
ATP + CEP89
ADP + phosphorylated CEP89
show the reaction diagram
-
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
show the reaction diagram
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
show the reaction diagram
-
-
-
-
?
ATP + DVL3
ADP + phosphorylated DVL3
show the reaction diagram
-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
show the reaction diagram
-
-
-
-
?
ATP + mu-calpain
ADP + calpastatin
show the reaction diagram
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
show the reaction diagram
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
show the reaction diagram
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
show the reaction diagram
ATP + Rabin8
ADP + phosphorylated Rabin8
show the reaction diagram
-
-
-
?
ATP + SC35
ADP + phosphorylated SC35
show the reaction diagram
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
show the reaction diagram
-
tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
show the reaction diagram
ATP + TDP-43
ADP + phosphorylated TDP-43
show the reaction diagram
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
show the reaction diagram
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
show the reaction diagram
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Zn2+
-
high zinc concentrations (0.1-0.5 mM) increase glycogen synthase kinase-3beta phosphorylation on tyrosine 216, a phosphorylation associated with increased activity of this tau kinase, whereas the phosphorylation of GSK-3alpha at Y279 and the level of total GSK-3beta are not affected
additional information
-
not activated by K+, Ca2+ or Zn2+
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone
enzyme binding structure analysis
(5,6-dibromo-1H-indol-3-yl)methanol
-
(5,6-dichloro-1H-indol-3-yl)methanol
-
(5,6-difluoro-1H-indol-3-yl)methanol
-
(5-bromo-6-chloro-1H-indol-3-yl)methanol
-
(5-bromo-6-fluoro-1H-indol-3-yl)methanol
-
(6-bromo-5-chloro-1H-indol-3-yl)methanol
-
(6-bromo-5-fluoro-1H-indol-3-yl)methanol
-
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
1-(5,6-dibromo-1H-indol-3-yl)methanamine
-
1-(5,6-dibromo-1H-indol-3-yl)propan-2-one
-
1-(5,6-dichloro-1H-indol-3-yl)methanamine
-
1-(5,6-dichloro-1H-indol-3-yl)propan-2-one
-
1-(5,6-difluoro-1H-indol-3-yl)methanamine
-
1-(5,6-difluoro-1H-indol-3-yl)propan-2-one
-
1-(5-bromo-6-chloro-1H-indol-3-yl)methanamine
-
1-(5-bromo-6-chloro-1H-indol-3-yl)propan-2-one
-
1-(5-bromo-6-fluoro-1H-indol-3-yl)methanamine
-
1-(5-bromo-6-fluoro-1H-indol-3-yl)propan-2-one
-
1-(6-bromo-5-chloro-1H-indol-3-yl)methanamine
-
1-(6-bromo-5-chloro-1H-indol-3-yl)propan-2-one
-
1-(6-bromo-5-fluoro-1H-indol-3-yl)methanamine
-
1-(6-bromo-5-fluoro-1H-indol-3-yl)propan-2-one
-
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
-
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
2-(5,6-dibromo-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-dibromo-1H-indol-3-yl)ethanamine
-
2-(5,6-dichloro-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-dichloro-1H-indol-3-yl)ethanamine
-
2-(5,6-difluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-difluoro-1H-indol-3-yl)ethanamine
-
2-(5-bromo-6-chloro-1H-indol-3-yl)-N-methylethanamine
-
2-(5-bromo-6-chloro-1H-indol-3-yl)ethanamine
-
2-(5-bromo-6-fluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(5-bromo-6-fluoro-1H-indol-3-yl)ethanamine
-
2-(6-bromo-5-chloro-1H-indol-3-yl)-N-methylethanamine
-
2-(6-bromo-5-chloro-1H-indol-3-yl)ethanamine
-
2-(6-bromo-5-fluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(6-bromo-5-fluoro-1H-indol-3-yl)ethanamine
-
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
-
3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
-
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
3-(imidazo[1,2-a]pyridin-3-yl)-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl]-1H-pyrrole-2,5-dione
an imidazo[1,2-a]pyridinylindolylmaleimide
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
-
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
-
3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione
enzyme binding structure analysis
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
-
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
-
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
-
4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
enzyme binding structure analysis
5,6-dibromo-3-methyl-1H-indole
-
5,6-dibromo-3-phenyl-1H-indole
best inhibitor for glycogen synthetase kinase-3 beta
5,6-dichloro-3-methyl-1H-indole
-
5,6-dichloro-3-phenyl-1H-indole
-
5,6-difluoro-3-methyl-1H-indole
-
5,6-difluoro-3-phenyl-1H-indole
-
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
-
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
-
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
-
5-bromo-6-chloro-3-methyl-1H-indole
-
5-bromo-6-chloro-3-phenyl-1H-indole
-
5-bromo-6-fluoro-3-methyl-1H-indole
-
5-bromo-6-fluoro-3-phenyl-1H-indole
-
5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine
enzyme binding structure analysis
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
-
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
-
6-bromo-5-chloro-3-methyl-1H-indole
-
6-bromo-5-chloro-3-phenyl-1H-indole
-
6-bromo-5-fluoro-3-methyl-1H-indole
-
6-bromo-5-fluoro-3-phenyl-1H-indole
-
7-methoxy-1-methyl-9h-betacarboline
enzyme binding structure analysis
convolutamine I
-
-
convolutamine J
-
-
CT99021
inhibition of GSK3 with CT99021 has little effect on the relative level of phosphorylation of Ser199 or Ser404 of human tau, but inhibition of GSK3beta using CT99021 results in dephosphorylation of endogenous c-Jun, Inh-2 and beta-catenin and dramatically increased c-Myc and beta-catenin expression
GF 109203X
a benzofuranylindolylmaleimide
kororamide A
-
-
kororamide B
-
-
KRM-189
74% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-191
84% inhibition at 0.01 mM, competes with ATP for GSK-3beta, leading to decreased Vmax and constant Km with increasing concentrations of ATP
KRM-192
75% inhibition at 0.01 mM
KRM-195
80% inhibition at 0.01 mM
KRM-296
65% inhibition at 0.01 mM
KRM-7777
65% inhibition at 0.01 mM
LiCl
71% inhibition at 0.01 mM
meridianin F
-
-
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide
enzyme binding structure analysis
Ro 31-8220
a benzofuranylindolylmaleimide
SB-415286
-
staurosporine
tideglusib
irreversible inhibitor
-
[3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine
enzyme binding structure analysis
(2'Z,3'E)-6-bromoindirubin-3'-oxime
-
-
(2S)-3-cyclohexyl-2-(9H-purin-6-ylamino)propan-1-ol
ZINC00012956
(5,6-dibromo-1H-indol-3-yl)methanol
-
(5,6-dichloro-1H-indol-3-yl)methanol
-
(5,6-difluoro-1H-indol-3-yl)methanol
-
(5-bromo-6-chloro-1H-indol-3-yl)methanol
-
(5-bromo-6-fluoro-1H-indol-3-yl)methanol
-
(6-bromo-5-chloro-1H-indol-3-yl)methanol
-
(6-bromo-5-fluoro-1H-indol-3-yl)methanol
-
1-(5,6-dibromo-1H-indol-3-yl)methanamine
-
1-(5,6-dibromo-1H-indol-3-yl)propan-2-one
-
1-(5,6-dichloro-1H-indol-3-yl)methanamine
-
1-(5,6-dichloro-1H-indol-3-yl)propan-2-one
-
1-(5,6-difluoro-1H-indol-3-yl)methanamine
-
1-(5,6-difluoro-1H-indol-3-yl)propan-2-one
-
1-(5-bromo-6-chloro-1H-indol-3-yl)methanamine
-
1-(5-bromo-6-chloro-1H-indol-3-yl)propan-2-one
-
1-(5-bromo-6-fluoro-1H-indol-3-yl)methanamine
-
1-(5-bromo-6-fluoro-1H-indol-3-yl)propan-2-one
-
1-(6-bromo-5-chloro-1H-indol-3-yl)methanamine
-
1-(6-bromo-5-chloro-1H-indol-3-yl)propan-2-one
-
1-(6-bromo-5-fluoro-1H-indol-3-yl)methanamine
-
1-(6-bromo-5-fluoro-1H-indol-3-yl)propan-2-one
-
1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
-
-
1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
1-[3-(6-amino-9H-purin-9-yl)propyl]-3-methylpyridin-2(1H)-one
ZINC91332506
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
-
-
2-(5,6-dibromo-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-dibromo-1H-indol-3-yl)ethanamine
-
2-(5,6-dichloro-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-dichloro-1H-indol-3-yl)ethanamine
-
2-(5,6-difluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(5,6-difluoro-1H-indol-3-yl)ethanamine
-
2-(5-bromo-6-chloro-1H-indol-3-yl)-N-methylethanamine
-
2-(5-bromo-6-chloro-1H-indol-3-yl)ethanamine
-
2-(5-bromo-6-fluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(5-bromo-6-fluoro-1H-indol-3-yl)ethanamine
-
2-(6-bromo-5-chloro-1H-indol-3-yl)-N-methylethanamine
-
2-(6-bromo-5-chloro-1H-indol-3-yl)ethanamine
-
2-(6-bromo-5-fluoro-1H-indol-3-yl)-N-methylethanamine
-
2-(6-bromo-5-fluoro-1H-indol-3-yl)ethanamine
-
2-amino-N-(2'-(cyclohex-2''-enyl)acetyl)acetimide
-
-
2-amino-N-(2'-(phenyl)acetyl)propanimide
-
-
2-bromo-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)benzoate
-
-
2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
3-((5-((4-amino-4-methylcyclohexyl)amino)-pyrrolo[2,1-f][1,2,4] triazin-4-yl)amino)-5-bromophenol
-
-
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
-
-
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
-
-
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
-
-
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
-
-
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
-
-
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
-
-
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
-
-
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[(5E)-5-methyl-4-oxo-2-hydroxy-5-octenyl]glutarimide
-
-
3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol
-
-
3-[5-[((4-amino-4-methylpiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl]amino)-5-bromophenol
-
-
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
-
-
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
-
-
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
4-(2-amino-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohept[1,2-b]indol-11-yl)-2-methyl-3-butyn-2-ol
-
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
4-[3-hydroxyanilino]-6,7-dimethoxyquinazoline
-
-
4-{(2R)-2-[(1R,3R,5S)-3,5-dimethyl-2-oxocyclohexyl]-2-hydroxyethyl}piperidine-2,6-dione
-
-
5,6-dibromo-3-methyl-1H-indole
-
5,6-dibromo-3-phenyl-1H-indole
best inhibitor for glycogen synthetase kinase-3 beta
5,6-dichloro-3-methyl-1H-indole
-
5,6-dichloro-3-phenyl-1H-indole
-
5,6-difluoro-3-methyl-1H-indole
-
5,6-difluoro-3-phenyl-1H-indole
-
5,6-dihydroxy-2-(4-hydroxy-3-methoxycyclohexa-1,5-dien-1-yl)-7-methoxy-4H-chromen-4-one
ZINC14644839
5-bromo-6-chloro-3-methyl-1H-indole
-
5-bromo-6-chloro-3-phenyl-1H-indole
-
5-bromo-6-fluoro-3-methyl-1H-indole
-
5-bromo-6-fluoro-3-phenyl-1H-indole
-
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
-
-
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
-
-
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
-
-
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
-
-
6-bromo-5-chloro-3-methyl-1H-indole
-
6-bromo-5-chloro-3-phenyl-1H-indole
-
6-bromo-5-fluoro-3-methyl-1H-indole
-
6-bromo-5-fluoro-3-phenyl-1H-indole
-
6-O-methyl-7-O-alpha-L-rhamnopyranosyldaidzein
-
-
7-O-alpha-L-rhamnopyranosyldaidzein
-
-
AMP-PNP
-
ATP analogue adenosine 5'-(beta,gamma-imino)triphosphate
convolutamine I
-
-
convolutamine J
-
-
cycloheximide
-
-
disheveled protein
-
-
-
DMSO
-
complete inhibition at 0.4% (v/v)
enzastaurin
-
activation-related phosphorylation of Y216/Y276 is dramatically decreased following exposure to enzastaurin whereas the inhibitory phosphorylation of S21 is significantly up-regulated in glioma cells. GSK3 inhibition results in glioma cell death and reduced tumorigenicity
GF 109203X
-
-
GSK-3 inhibitor IX
-
-
kenpaullone
-
-
kororamide A
-
-
kororamide B
-
-
leptin
-
-
-
lithium
meridianin F
-
-
methyl 2-bromo-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)benzoate
-
-
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
-
-
N-(4-ethoxy-3-fluorobenzyl)-9H-purin-6-amine
ZINC69775110
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
-
-
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-(5-phenyl-1H-indazol-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
-
-
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
-
-
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
-
-
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
-
-
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
-
-
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
-
-
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
-
-
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
-
-
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
-
-
naramycin B
-
-
Ro 31-8220
-
-
roscovitine
-
complete inhibition of T231 phosphorylation by 25-Cdk5 kinase complex
SB-216763
-
specific inhibitor of GSK-3beta
SB-415286
-
complete inhibition at 0.005 mM
SB415286
-
-
SRN-003-556
-
-
staurosporine
-
-
trans-activating transcriptor-eIF2B
-
acts as a competitive inhibitor of GSK-3
-
ZM336372
-
inhibits GSK-3beta through phosphorylation at Ser9, a dose-dependent increase in phosphorylation of GSK-3beta occurs after treatment with ZM336372 (0.025-0.1 mM)
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
14-3-3
protein 14-3-3 recognises GSK-3 phosphorylated at Ser9, and the association of tau with this complex is believed to regulate its phosphorylation by GSK-3, since in human embryonic kidney cells, tau phosphorylation by GSK-3 is suppressed in the absence of 14-3-3, but GSK-3 is active and phosphorylates tau if 14-3-3 is present
-
AMP
AMP binding induces a conformational change in the ? -subunit activation loop of the kinase that allows phosphorylation of the activating residue Thr172 by AMPK upstream kinases
heparansulfate
heparin is more effective than heparan sulfate at lower concentrations in inducing the hyperphosphorylation of tau by GSK3beta
heparin
heparin is more effective than heparan sulfate at lower concentrations in inducing the hyperphosphorylation of tau by GSK3beta
AT7519
-
0.0005 mM AT7519 inhibits glycogen synthase kinase 3beta phosphorylation, AT7519 dephosphorylates GSK-3beta independent of inhibition of transcription
cAMP
-
required for PKA activation
forskolin
-
forskolin specifically induces tau hyperphosphorylation by PKA at Ser214 resulting in increased phosphorylation at Ser199, Ser22, Ser396, and Ser404 in N2a/tau441 cells, forskolin has no effect on GSK-3
FRAT-2
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, activates phosphorylation of primed sites of tau protein about 8fold, no effect on unprimed site phosphorylation
-
heparin
-
-
L-Dopa
-
activates GSK-3beta at high dose
p25
-
inducible cytotoxic expression factor required for Cdk5 activity, formation of a complex with Cdk5, p25 overexpression increases tau phosphorylation rate
-
protein 14-3-3
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization
-
soluble beta-amyloid oligomers
-
activate GSK-3beta mediated tau phosphorylation and increase toxicity, reduced content of soluble, not insoluble, amyloid oligomers reduces the tau phosphorylation activity, specific antibodies can inhibit the activation, overview
-
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.002
(4-amino-2-((4-chlorophenyl)amino)thiazol-5-yl)(3-nitrophenyl)methanone
Homo sapiens
pH and temperature not specified in the publication
0.0000025
1-(4-methoxyphenyl)-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000086
1-(4-methoxyphenyl)-6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000125 - 0.000131
1-(cyclopropylmethyl)-3-[4-(5,6-difluoro-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indole-5-carbonitrile
0.0000094
1-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000065
2-(1,3-benzodioxol-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000049
2-(1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000044
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluoro-4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000054
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00022
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(4-methoxybenzyl)sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00034
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[2-(3-fluorophenyl)ethyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00068
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[(3-fluorophenyl)sulfanyl]methyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000068
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000057
2-(2,3-dihydro-1-benzofuran-5-yl)-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00021
2-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000094
2-[(2-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000013
2-[(3-chloro-4-methoxybenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0002
2-[(3-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00028
2-[(4-chlorobenzyl)sulfanyl]-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000084
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000025
2-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00645
3-(1-(2-morpholinoethyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00021
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00129
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00015
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.0116
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-1,2,4-triazol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.0001
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00053
3-(1-(4-morpholinobutyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.000035
3-(1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00022
3-(1-benzofuran-3-yl)-4-(1-methyl-7-phenoxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000007
3-(1-benzofuran-3-yl)-4-(5-bromo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000235
3-(1-benzofuran-3-yl)-4-(5-cyclopropyl-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000026
3-(1-benzofuran-3-yl)-4-(5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00036
3-(1-benzofuran-3-yl)-4-(5-fluoro-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00069
3-(1-benzofuran-3-yl)-4-(5-hydroxy-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000345
3-(1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000184
3-(1-benzofuran-3-yl)-4-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00044
3-(1-benzofuran-3-yl)-4-(6-chloro-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000015
3-(1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000223
3-(1-benzofuran-3-yl)-4-(6-iodo-5-methoxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000055
3-(1-benzofuran-3-yl)-4-(7-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00022
3-(1-benzofuran-3-yl)-4-[1-(3-hydroxypropyl)-5-phenoxy-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.001304
3-(1-benzofuran-3-yl)-4-[1-methyl-5-(morpholin-4-yl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00165
3-(1-benzofuran-3-yl)-4-[5-(benzyloxy)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000016
3-(1-benzofuran-3-yl)-4-[5-bromo-1-(3-hydroxypropyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0009
3-(1-benzofuran-3-yl)-4-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000054
3-(1-benzofuran-3-yl)-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00000012
3-(1-benzofuran-3-yl)-4-[7-(methoxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00026
3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00204
3-(1H-imidazol-1-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00192
3-(1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.000314
3-(5,6-difluoro-1-benzofuran-3-yl)-4-(1-methyl-1H-benzo[g]indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000887
3-(5,7-dibromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00055
3-(5-bromo-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000075
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000335
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(4-methoxyphenoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00000051
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000483
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-en-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000253
3-(5-bromo-1-methyl-1H-indol-3-yl)-4-[6-(prop-2-yn-1-yloxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000042
3-(5-chloro-1-methyl-1H-indol-3-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00067
3-(5-fluoro-1-benzofuran-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00018
3-(5-fluoro-1-benzofuran-3-yl)-4-(5-iodo-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000014
3-(5-fluoro-1-benzofuran-3-yl)-4-(6-hydroxy-1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000035
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-hydroxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00000035
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000238
3-(5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(methoxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000247
3-(5-fluoro-6-iodo-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00057
3-(5-methoxy-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.000708
3-(5H-[1,3]dioxolo[4,5-f]indol-7-yl)-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00101
3-(6-bromo-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00036
3-(6-chloro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.000866
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(6-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000114
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.004092
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclobutylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00104
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(cyclopropylmethoxy)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00000095
3-(6-chloro-5-fluoro-1-methyl-1H-indol-3-yl)-4-[6-(hydroxymethyl)-1-benzofuran-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00016
3-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00018
3-(7-methoxy-1-benzofuran-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.000831
3-(7-methoxy-1-benzofuran-3-yl)-4-[1-methyl-6-(trifluoromethyl)-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.01186
3-(naphthalen-1-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.000091
3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzo-nitrile
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00424
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.0000023
3-[([5-[1-(4-methoxyphenyl)-1H-benzimidazol-6-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000035
3-[([5-[3-(4-methoxyphenyl)-1-benzofuran-5-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)methyl]benzonitrile
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000021
3-[1H-indol-3-yl]-4-[2-[4-methylpiperazin-1-yl]quinazolin-4-yl]-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.0000132
3-[4-(6-ethyl-1-benzofuran-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1-methyl-1H-indole-5-carbonitrile
Homo sapiens
-
0.0000226
3-[5-(cyclopropylethynyl)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.007
3-[6-(4-chlorophenyl)-5-fluoro-1-methyl-1H-indol-3-yl]-4-(7-methoxy-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00016
3-[6-(benzyloxy)-1-methyl-1H-indol-3-yl]-4-(5-fluoro-1-benzofuran-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
0.0000051
3-[6-(hydroxymethyl)-1-benzofuran-3-yl]-4-[7-(hydroxymethyl)-1-methyl-1H-indol-3-yl]-1H-pyrrole-2,5-dione
Homo sapiens
-
0.00013
4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
Homo sapiens
pH and temperature not specified in the publication
0.00033
5-(2,3-dihydro-1-benzofuran-5-yl)-N-(3-fluorobenzyl)-1,3,4-oxadiazol-2-amine
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000016
5-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-indazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000028
5-([ [5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)-2-methoxybenzonitrile
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0019
5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
pH and temperature not specified in the publication
0.0000031
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1,3-benzothiazole
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0000065
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)imidazo[1,2-a]pyridine
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.000018
6-(5-[[4-methoxy-3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)quinoline
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.00035
7-methoxy-1-methyl-9h-betacarboline
Homo sapiens
pH and temperature not specified in the publication
0.000548
KRM-189
Homo sapiens
-
0.000467
KRM-191
Homo sapiens
-
0.001012
KRM-192
Homo sapiens
-
0.001863
KRM-195
Homo sapiens
-
0.000539
KRM-296
Homo sapiens
-
0.007149
KRM-7777
Homo sapiens
-
0.000071
LiCl
Homo sapiens
-
0.00063
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
Homo sapiens
in 25 mM HEPES, pH 7.5, 10 mM magnesium acetate, 1 mM dithiothreitol, and 0.01% bovine serum albumin
0.0032
N-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000028
staurosporine
Homo sapiens
pH and temperature not specified in the publication
0.0032
[3R]-1-[5-methyl-7Hpyrrolo[2,3-d]pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
pH and temperature not specified in the publication
0.00281
1-ethyl-3-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)urea
Homo sapiens
-
-
0.023
1-methyl-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.000021
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
Homo sapiens
-
-
0.000143
2-chloro-5-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
Homo sapiens
-
-
0.000074
2-chloro-5-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000028
2-chloro-5-[[4-(2-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000076
2-chloro-5-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000085
2-chloro-5-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000026
2-chloro-5-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000109
2-chloro-5-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000019
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
Homo sapiens
-
-
0.00012
3-((5-((4-amino-4-methylcyclohexyl)amino)-pyrrolo[2,1-f][1,2,4] triazin-4-yl)amino)-5-bromophenol
Homo sapiens
isoform TTBK1, pH and temperature not specified in the publication
-
0.00026
3-(1-(2-(1H-imidazol-1-yl)ethyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.07334
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-1-phenyl-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00066
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00055
3-(1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01358
3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01245
3-(1-(3-(piperidin-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00114
3-(1-(3-hydroxypropyl)-1H-indol-3-yl)-4-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00179
3-(1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00085
3-(1-(4-(1H-imidazol-1-yl)butyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0009
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(2-morpholinoethyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00076
3-(1-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-4-(1-(3-morpholinopropyl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.0306
3-(1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000187
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000131
3-(2,3-dihydro-1H-indol-1-yl)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000161
3-(2,3-dihydro-1H-indol-1-yl)-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000694
3-(2,3-dihydro-1H-indol-1-yl)-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000337
3-(2-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000216
3-(2-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000093
3-(2-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000195
3-(2-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000374
3-(2-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000161
3-(2-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000216
3-(2-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00011
3-(2-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00046
3-(3-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000058
3-(3-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001478
3-(3-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000532
3-(3-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000203
3-(3-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000141
3-(3-nitrophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001412
3-(4-chlorophenyl)-4-(2,3-dihydro-1H-indol-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000514
3-(4-chlorophenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000091
3-(4-chlorophenyl)-4-[(3,5-dichloro-4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000447
3-(4-chlorophenyl)-4-[(3-chlorophenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000407
3-(4-chlorophenyl)-4-[(3-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000317
3-(4-chlorophenyl)-4-[(4-hydroxyphenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.002285
3-(4-chlorophenyl)-4-[methyl(phenyl)amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000529
3-(4-chlorophenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00039
3-(4-methoxyphenyl)-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000243
3-(4-methoxyphenyl)-4-[[4-(methylsulfanyl)phenyl]amino]-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00014
3-(5-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00048
3-(5-methoxy-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.02246
3-(5-methoxy-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00095
3-(6-bromo-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00226
3-(6-bromo-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00031
3-(6-fluoro-1-(3-(1H-imidazol-1-yl)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.01244
3-(6-fluoro-1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-pyrrolo[3,2-b]pyridin-1-yl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000014
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
Homo sapiens
-
-
0.00059
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000291
3-[(2,5-dioxo-4-phenyl-2,5-dihydro-1H-pyrrol-3-yl)amino]benzoic acid
Homo sapiens
-
-
0.000082
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000052
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000142
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00002
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000083
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000071
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000149
3-[(3,5-dichloro-4-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000152
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000139
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000104
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000094
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000059
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000173
3-[(3-chloro-4-hydroxyphenyl)amino]-4-(4-chlorophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000114
3-[(3-chlorophenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000104
3-[(3-chlorophenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000257
3-[(3-chlorophenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00007
3-[(3-chlorophenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000156
3-[(3-chlorophenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000301
3-[(3-chlorophenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000259
3-[(3-hydroxyphenyl)amino]-4-(2-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000251
3-[(3-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000472
3-[(3-hydroxyphenyl)amino]-4-(3-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000236
3-[(3-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000481
3-[(3-hydroxyphenyl)amino]-4-(4-methoxyphenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000704
3-[(3-hydroxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000123
3-[(4-hydroxyphenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.001398
3-[methyl(phenyl)amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.002613
3-[methyl(phenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000136
3-[[4-(2-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000134
3-[[4-(3-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000195
3-[[4-(3-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000079
3-[[4-(3-nitrophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000186
3-[[4-(4-chlorophenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000214
3-[[4-(4-methoxyphenyl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]amino]benzoic acid
Homo sapiens
-
-
0.000152
3-[[4-(methylsulfanyl)phenyl]amino]-4-(3-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000392
3-[[4-(methylsulfanyl)phenyl]amino]-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.000404
3-[[4-(methylsulfanyl)phenyl]amino]-4-phenyl-1H-pyrrole-2,5-dione
Homo sapiens
-
-
0.00025
4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
-
-
0.000738 - 0.000801
4-(2-amino-5,6,7,8-tetrahydropyrimido[4',5':3,4]cyclohept[1,2-b]indol-11-yl)-2-methyl-3-butyn-2-ol
-
0.023
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.00043
5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
Homo sapiens
-
-
0.00053
5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-amine
Homo sapiens
-
-
0.00126
5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-amine
Homo sapiens
-
-
0.023
5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-amine
Homo sapiens
-
-
0.023
5-phenyl[1,2]oxazolo[5,4-b]pyridin-3-amine
Homo sapiens
-
-
0.002343
N-(1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.000691
N-(4,5-diphenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl)butanamide
Homo sapiens
-
-
0.000415
N-(5,6-diphenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000383
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.000075
N-(5-bromo-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000234
N-(5-chloro-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000087
N-(5-cyano-6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000099
N-(5-phenyl-1H-indazol-3-yl)butanamide
Homo sapiens
-
-
0.000291
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide
Homo sapiens
-
-
0.000056
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.000005
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopentanecarboxamide
Homo sapiens
-
-
0.003572
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)methanesulfonamide
Homo sapiens
-
-
0.000043
N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
Homo sapiens
-
-
0.000007
N-(5-phenyl-1H-pyrazolo[3,4-c]pyridin-3-yl)butanamide
Homo sapiens
-
-
0.002697
N-(5-phenyl-1H-pyrazolo[4,3-d]pyrimidin-3-yl)butanamide
Homo sapiens
-
-
0.000498
N-(6-phenyl-1H-indazol-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000425
N-(6-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)cyclopropanecarboxamide
Homo sapiens
-
-
0.000007
N-[4-[3-(4-ethylpiperazin-1-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000022
N-[4-[3-(dimethylamino)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[4-[3-(morpholin-4-yl)propyl]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[4-[ethyl(piperidin-1-ylmethyl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000009
N-[4-[methyl(piperidin-1-yl)amino]-5-phenyl-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000007
N-[5-(2,3-difluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000027
N-[5-(2-chlorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000018
N-[5-(2-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.00002
N-[5-(3-fluorophenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000356
N-[5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000005
N-[5-(6,6-difluorocyclohexa-1,3-dien-1-yl)-4-[3-(dimethylamino)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000851
N-[5-(biphenyl-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000241
N-[5-(naphthalen-1-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000169
N-[5-(naphthalen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000011
N-[5-(pyridin-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000443
N-[5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]butanamide
Homo sapiens
-
-
0.000004
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-(4-ethylpiperazin-1-yl)butanamide
Homo sapiens
-
-
0.000001
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.0000008
N-[5-bromo-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000007
N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000016
N-[5-bromo-6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000018
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-2-(4-methylpiperidin-1-yl)acetamide
Homo sapiens
-
-
0.000007
N-[5-bromo-6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000001
N-[5-chloro-6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000011
N-[5-phenyl-4-[3-(pyrrolidin-1-yl)propyl]-1H-pyrazolo[3,4-c]pyridazin-3-yl]butanamide
Homo sapiens
-
-
0.000042
N-[6-(1H-indol-5-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.001
N-[6-(2,5-difluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000036
N-[6-(2-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.001593
N-[6-(2-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.00032
N-[6-(2H-pyrrol-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000008
N-[6-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000005
N-[6-(3-bromo-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000007
N-[6-(3-chloro-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000828
N-[6-(3-fluorophenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000012
N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000125
N-[6-(3-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000481
N-[6-(3-sulfamoylphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000015
N-[6-(4-hydroxyphenyl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000012
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-methylpiperidine-1-carboxamide
Homo sapiens
-
-
0.000008
N-[6-(4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000006
N-[6-(4-hydroxyphenyl)-5-methyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000024
N-[6-(4-hydroxyphenyl)-5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.023
N-[6-(4-methoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000141
N-[6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000035
N-[6-(furan-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000099
N-[6-(tetrahydrothiophen-3-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000215
N-[6-(thiophen-2-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000039
N-[6-(thiophen-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.000329
N-[6-(thiophen-3-yl)-1H-indazol-3-yl]cyclopropanecarboxamide
Homo sapiens
-
-
0.0002
staurosporine
Homo sapiens
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
0.26
-
in the presence of Mg2+
0.57
-
in the presence of Mn2+
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
purified recombinant GSK-3beta
Manually annotated by BRENDA team
-
U251, T98, U87, U373, U118, A172
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
-
weak expression
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
-
mainly
Manually annotated by BRENDA team
additional information
TTBK2 localization sites include the centriole/basal body, the midbody, and possibly the mitotic spindles. Localization at the base of primary cilia
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
sequence comparisons of diverse protein kinases, phylogenetic tree of tau protein kinases and analysis
malfunction
physiological function
evolution
TTBK2 is a serine/threonine protein kinase of the CK1 superfamily
malfunction
metabolism
isoform TTBK2 influences the function of the glutamate receptor GluK2. The enzyme down-regulates GluK2 activity by decreasing the receptor protein abundance in the cell membrane via RAB5-dependent endocytosis
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
GSK3B_HUMAN
420
0
46744
Swiss-Prot
Mitochondrion (Reliability: 5)
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
100000
-
immunoprecipitation, lysosomal degradation product of full-length TTBK1
142700
-
predicted
23000
-
1 * 30000 + 1 * 23000, catalytic and regulatory subunit, SDS-PAGE
230000
-
immunoprecipitation, full-length TTBK1 migrates to 230 kDa because of the negative charge of the polyglutamate sequence and the protein modification
30000
35000
-
gel filtration
38620
-
calculated
39000
-
1 * 39000, SDS-PAGE
45000
47000
-
SDS-PAGE
72000
-
SDS-PAGE
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
dimer
GSK3beta enzyme is composed of three domains: an N-terminal domain consisting of a closed beta-barrel structure, a C-terminal domain containing a kinase fold structure, and a small extradomain subsequent to the C-terminal domain. The catalytic site is between the two major domains and has an ATP analogue molecule in its ATP binding site
heterodimer
-
1 * 30000 + 1 * 23000, catalytic and regulatory subunit, SDS-PAGE
monomer
additional information
TTBK2 possesses a casein kinase 1 (CK1) kinase domain followed by a about 900 amino acid segment, potentially responsible for its localization and substrate recruitment
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
phosphoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
by hanging-drop vapour-diffusion method, crystals belong to space group P212121, with unit-cell parameters a = 55.6, b = 113.7, c = 117.3 A, alpha = beta = gamma = 90.0°, to 2.9 A resolution
-
enzyme complexed with the Cdk2 inhibitor WHI-P180, using 0.1 M Tris pH 8.5, 10% (v/v) glycerol, 2.0 M sodium/potassium phosphate at 4°C
hanging drop vapour-diffusion method, prismatic crystals, orthorhombic space group P2(1)2(1)2(1), unit cell parameters a = 82.9, b = 86.1, c = 178.1 A
-
isoform TTBK2 kinase domain with ADP, using 0.1 M Tris pH 8.5, 10% (v/v) glycerol and 2 M Na/K phosphate
purified recombinant Leu-Glu-His6-tagged GSK3beta in complex with ATP or ATP analogue AMP-PNP, 10 mg/ml protein, 2 mM ATP or AMP-PNP, 12-14% w/v PEG 6000, 100 mM NaCl, 5 mM MgCl2, 10% v/v glycerol, in 100 mM HEPES-NaOH, pH 7.5, hanging drop vapor diffusion method, 4°C, several days, soaking in 0.1 mM ethylmercuric thiosalicylate at pH 7.5 for 1 h, cryoprotection by 30% w/v D-sorbitol, X-ray diffraction structure determination and analysis at 1.7-2.6 A resolution
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
K85A
kinase-dead mutant
K85R
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type
P379A/P380A
site-directed mutagenesis, the mutant shows rediuced activity compared to the wild-type
R96A
site-directed mutagenesis, the mutant activity is similar to the wild-type
S9A
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type
T390A
site-directed mutagenesis, the mutant activity is similar to the wild-type
Y216F
site-directed mutagenesis, the mutant activity is similar to the wild-type
D163A
K148R
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type
K50A
kinase-dead mutant
K63A
kinase-dead mutant
K85R
-
dead-kinase mutant of GSK-3beta
P442A/P443A
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type
R159A
site-directed mutagenesis, the mutant shows reduced activity compared to the wild-type
S9A
-
site-directed mutagenesis, mutant cannot be inhibited by phosphorylation at position 9 and is thus constitutively active
Y279F
site-directed mutagenesis, the mutant activity is similar to the wild-type
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
95
-
10 min, inactivation
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant GST-tagged enzyme from Escherichia coli strain BL21-CodonPlus(DE3) by glutathione affinity chromatography and tag cleavage by thrombin
recombinant GST-tagged enzyme from HEK-293 cells by glutathione affinity chromatography
recombinant GST-tagged GSK3beta1 and GSKbeta2 from HEK-293 cells by glutathione affinity chromatography
centrifugation, sonication, gel filtration, metal affinity chromatography, to homogeneity
-
GSTrap affinity chromatography
-
Ni-NTA agarose resin column chromatography and Superdex 75 gel filtration
Ni-NTA resin and by gel filtration
-
nickel resin column chromatography and Superdex 75 gel filtration
recombinant GST-tagged enzyme from HEK-293 cells by glutathione affinity chromatography
recombinant isoenzyme TPHII
-
recombinant Leu-Glu-His6-tagged GSK3beta from Escherichia coli
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
GSK-3 exists as two isoforms, alpha and beta, which share 85% sequence identity and are encoded by distinct genes located on chromosomes 19 and 3, respectively. Isozyme GSK-3beta occurs in two splicing variants, GSK-3beta1 and GSK-3beta2, that differ by the presence of an additional insertion of 13 amino acids
GSK-3beta consists of two splice variants, the major short form (GSK-3beta1) and the minor long form (GSK-3beta2), whose structural difference is the insert of only 13 amino acid residues to the C-terminal side of the catalytic site of GSK-3beta1, recombinant expression of isozymes GSK-3beta1 and GSK-3beta2 in HEK-293T cells
phylogenetic tree
recombinant expression of GST-tagged enzyme in Escherichia coli strain BL21-CodonPlus(DE3)
recombinant expression of GST-tagged GSK3beta1 and GSKbeta2 in HEK-293 cells, coepression with FLAG-tagged tau protein isoform 2
transient transfection of GST-tagged enzyme into HEK-293 cells coexpression with recombinant tau, coexpression of wild-type GSK-3alpha and wild-type GSK-3beta enhances Tau phosphorylation at Ser396 and Ser404
using a baculovirus expression system
after cloning and cDNA analysis TPKI is found to be identical with glycogen synthase kinase 3beta, the catalytic subunit of TPKII is identical with cdc2-related kinase, PSSALRE/Cdk5
-
cDNA cloned and expressed in Escherichia coli BL21(DE3)
-
expressed in CHO cells
-
expressed in Escherichia coli BL21-CodonPlus (DE3) cells
-
expressed in Mus musculus line 141
expressed in Neuro2a cells
-
expressed in Saccharomyces cerevisiae
-
expressed in Xenopus laevis oocytes
expression of GSK3beta in Escherichia coli in fusion with a Leu-Glu-His6-tag at the C-terminus
-
expression of GST-fusion SGK1 in COS-1 cells in the cytoplasm, coexpression with protein 14-3-3 or addition of serum leads to relocation of the enzyme in the nucleus
-
HA- and myc-tagged full-length TTBK1 expressed in COS-7 cells, HA-TTBK1 expressed in HEK293 cells and in mock-transfected cells, recombinant full length TTBK1 expressed in Escherichia coli or baculovirus-infected Sf-9 insect cells
-
isoform TTBK2 kinase domain is expressed in Escherichia coli strain NEB2523
recombinant overexpression of myc-tagged human TTBK1 in HEK-293 cells
recombinant TPKII cdk5/p20
-
tau protein kinase II, full length human cdk5 gene inserted into baculovirus genome
-
the tau tubulin kinase 2 kinase domain is expressed in Escherichia coli C2523 cells
TPKI/GSK-3beta-interacting proteins from a human brain cDNA library in a yeast two-hybrid system
-
transient co-expression of human tau long isoform, HA-tagged GSK3beta, and GST-tagged GFP-fusion FRAT-2 protein in HEK-293 cells
-
transient expression of HA-tagged wild-type and mutant enzymes in CHO cells
-
transient transfection of GST-tagged enzyme into HEK-293 cells coexpression with recombinant tau, coexpression of wild-type GSK-3alpha and wild-type GSK-3beta enhances Tau phosphorylation at Ser396 and Ser404
TTBK2 kinase domain (residues 1-331) of TTBK2 subcloned into pBiEx-3 vector, expressed in insect cells with a baculovirus overexpression system
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
isoform TTBK1 is upregulated in the frontal cortex of patients with Alzheimer's disease
the reduction of tau phosphorylation by treatment with 100 nM leptin is mimicked by the downregulation of GSK-3beta
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
drug development
glycogen synthase kinase-3 activity and substrate phosphorylation, e.g. glycogen synthase, tau, CRMP2 and amyloid precursor protein, are reported to be abnormally high in both Type 2 diabetes and Alzheimer's disease. The enzyme GSK3 is a target for development of isozyme-selective inhibitors
medicine
pharmacology
-
anti-bodies highly specific for toxic amyloid oligomer subspecies may reduce toxicity via reduction of GSK-3beta amount in Alzheimer's disease therapeutic strategy
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Delcommenne, M.; Tan, C.; Gray, V.; Rue, L.; Woodgett, J.; Dedhar, S.
Phosphoinositide-3-OH kinase-dependent regulation of glycogen synthase kinase 3 and protein kinase B/AKT by the integrin-linked kinase
Proc. Natl. Acad. Sci. USA
95
11211-11216
1998
Homo sapiens (P49841)
Manually annotated by BRENDA team
Lau, K.F.; Miller, C.C.; Anderton, B.H.; Shaw, P.C.
Molecular cloning and characterization of the human glycogen synthase kinase-3beta promoter
Genomics
60
121-128
1999
Homo sapiens (P49841)
Manually annotated by BRENDA team
Rhoads, A.R.; Karkera, J.D.; Detera-Wadleigh, S.D.
Radiation hybrid mapping of genes in the lithium-sensitive wnt signaling pathway
Mol. Psychiatry
4
437-442
1999
Homo sapiens (P49841)
Manually annotated by BRENDA team
Stambolic, V.; Woodgett, J.R.
Mitogen inactivation of glycogen synthase kinase-3 beta in intact cells via serine 9 phosphorylation
Biochem. J.
303
701-704
1994
Homo sapiens (P49841)
Manually annotated by BRENDA team
Ali, A.; Hoeflich, K.P.; Woodgett, J.R.
Glycogen synthase kinase-3: properties, functions, and regulation
Chem. Rev.
101
2527-2540
2001
Homo sapiens (P49841)
Manually annotated by BRENDA team
Song, J.S.; Yang, S.D.
tau Protein kinase I/GSK-3b/kinase FA in heparin phosphorylates Tau on Ser199, Thr231, Ser235, Ser262, Ser369, and Ser400 sites phosphorylated in Alzheimer disease brain
J. Protein Chem.
14
95-105
1995
Homo sapiens
Manually annotated by BRENDA team
Hoshi, M.; Takashima, A.; Noguchi, K.; Murayama, M.; Sato, M.; Kondo, S.; Saitoh, Y.; Ishiguro, K.; Hoshino, T.; Imahori, K.
Regulation of mitochondrial pyruvate dehydrogenase activity by tau protein kinase I/glycogen synthase kinase 3beta in brain
Proc. Natl. Acad. Sci. USA
93
2719-2723
1996
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Imahori, K.; Uchida, T.
Physiology and pathology of tau protein kinases in relation to Alzheimer's disease
J. Biochem.
121
179-188
1997
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Aoki, M.; Iwamoto-Sugai, M.; Sugiura, I.; Sasaki, C.; Hasegawa, T.; Okumura, C.; Sugio, S.; Kohno, T.; Matsuzaki, T.
Expression, purification and crystallization of human tau-protein kinase I/glycogen synthase kinase-3beta
Acta Crystallogr. Sect. D
56
1464-1465
2000
Homo sapiens
Manually annotated by BRENDA team
Evans, D.B.; Rank, K.B.; Bhattacharya, K.; Thomsen, D.R.; Gurney, M.E.; Sharma, S.K.
tau Phosphorylation at serine 396 and serine 404 by human recombinant tau protein kinase II inhibits tau's ability to promote microtubule assembly
J. Biol. Chem.
275
24977-24983
2000
Homo sapiens
Manually annotated by BRENDA team
Lund, E.T.; McKenna, R.; Evans, D.B.; Sharma, S.K.; Mathews, W.R.
Characterization of the in vitro phosphorylation of human tau by tau protein kinase II (cdk5/p20) using mass spectrometry
J. Neurochem.
76
1221-1232
2001
Homo sapiens
Manually annotated by BRENDA team
Mukai, F.; Ishiguro, K.; Sano, Y.; Fujita, S.C.
Alternative splicing isoform of tau protein kinase I/glycogen synthase kinase 3beta
J. Neurochem.
81
1073-1083
2002
Homo sapiens, Mus musculus, Rattus norvegicus
Manually annotated by BRENDA team
Rank, K.B.; Pauley, A.M.; Bhattacharya, K.; Wang, Z.; Evans, D.B.; Fleck, T.J.; Johnston, J.A.; Sharma, S.K.
Direct interaction of soluble human recombinant tau protein with Abeta 1-42 results in tau aggregation and hyperphosphorylation by tau protein kinase II
FEBS Lett.
514
263-268
2002
Homo sapiens
Manually annotated by BRENDA team
Aoki, M.; Yokota, T.; Sugiura, I.; Sasaki, C.; Hasegawa, T.; Okumura, C.; Ishiguro, K.; Kohno, T.; Sugio, S.; Matsuzaki, T.
Structural insight into nucleotide recognition in tau-protein kinase I/glycogen synthase kinase 3 beta
Acta Crystallogr. Sect. D
60
439-446
2004
Homo sapiens
Manually annotated by BRENDA team
Cho, J.H.; Johnson, G.V.
Glycogen synthase kinase 3beta phosphorylates tau at both primed and unprimed sites. Differential impact on microtubule binding
J. Biol. Chem.
278
187-193
2003
Homo sapiens
Manually annotated by BRENDA team
Hamdane, M.; Sambo, A.V.; Delobel, P.; Begard, S.; Violleau, A.; Delacourte, A.; Bertrand, P.; Benavides, J.; Buee, L.
Mitotic-like tau phosphorylation by p25-Cdk5 kinase complex
J. Biol. Chem.
278
34026-34034
2003
Homo sapiens
Manually annotated by BRENDA team
Hernandez, F.; Perez, M.; Lucas, J.J.; Mata, A.M.; Bhat, R.; Avila, J.
Glycogen synthase kinase-3 plays a crucial role in tau exon 10 splicing and intranuclear distribution of SC35. Implications for Alzheimer's disease
J. Biol. Chem.
279
3801-3806
2004
Homo sapiens
Manually annotated by BRENDA team
Cho, J.H.; Johnson, G.V.
Glycogen synthase kinase 3 beta induces caspase-cleaved tau aggregation in situ
J. Biol. Chem.
279
54716-54723
2004
Homo sapiens
Manually annotated by BRENDA team
Stoothoff, W.H.; Cho, J.H.; McDonald, R.P.; Johnson, G.V.
FRAT-2 preferentially increases glycogen synthase kinase 3 beta-mediated phosphorylation of primed sites, which results in enhanced tau phosphorylation
J. Biol. Chem.
280
270-276
2005
Homo sapiens
Manually annotated by BRENDA team
Zhang, Y.; Li, H.L.; Wang, D.L.; Liu, S.J.; Wang, J.Z.
A transitory activation of protein kinase-A induces a sustained tau hyperphosphorylation at multiple sites in N2a cells-imply a new mechanism in Alzheimer pathology
J. Neural Transm.
2
1-11
2006
Homo sapiens
Manually annotated by BRENDA team
Ma, Q.L.; Lim, G.P.; Harris-White, M.E.; Yang, F.; Ambegaokar, S.S.; Ubeda, O.J.; Glabe, C.G.; Teter, B.; Frautschy, S.A.; Cole, G.M.
Antibodies against beta-amyloid reduce abeta oligomers, glycogen synthase kinase-3beta activation and tau phosphorylation in vivo and in vitro
J. Neurosci. Res.
83
374-384
2006
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Lambourne, S.L.; Sellers, L.A.; Bush, T.G.; Choudhury, S.K.; Emson, P.C.; Suh, Y.H.; Wilkinson, L.S.
Increased tau phosphorylation on mitogen-activated protein kinase consensus sites and cognitive decline in transgenic models for Alzheimer's disease and FTDP-17: evidence for distinct molecular processes underlying tau abnormalities
Mol. Cell. Biol.
25
278-293
2005
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Chun, J.; Kwon, T.; Lee, E.J.; Kim, C.H.; Han, Y.S.; Hong, S.K.; Hyun, S.; Kang, S.S.
14-3-3 Protein mediates phosphorylation of microtubule-associated protein tau by serum- and glucocorticoid-induced protein kinase 1
Mol. Cells
18
360-368
2004
Homo sapiens
Manually annotated by BRENDA team
Hanger, D.P.; Byers, H.L.; Wray, S.; Leung, K.Y.; Saxton, M.J.; Seereeram, A.; Reynolds, C.H.; Ward, M.A.; Anderton, B.H.
Novel phosphorylation sites in tau from Alzheimer brain support a role for casein kinase 1 in disease pathogenesis
J. Biol. Chem.
282
23645-23654
2007
Homo sapiens
Manually annotated by BRENDA team
Kitano-Takahashi, M.; Morita, H.; Kondo, S.; Tomizawa, K.; Kato, R.; Tanio, M.; Shirota, Y.; Takahashi, H.; Sugio, S.; Kohno, T.
Expression, purification and crystallization of a human tau-tubulin kinase 2 that phosphorylates tau protein
Acta Crystallogr. Sect. F
63
602-604
2007
Homo sapiens
Manually annotated by BRENDA team
Sato, S.; Cerny, R.L.; Buescher, J.L.; Ikezu, T.
Tau-tubulin kinase 1 (TTBK1), a neuron-specific tau kinase candidate, is involved in tau phosphorylation and aggregation
J. Neurochem.
98
1573-1584
2006
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Lebouvier, T.; Scales, T.M.; Hanger, D.P.; Geahlen, R.L.; Lardeux, B.; Reynolds, C.H.; Anderton, B.H.; Derkinderen, P.
The microtubule-associated protein tau is phosphorylated by Syk
Biochim. Biophys. Acta
1783
188-192
2008
Homo sapiens
Manually annotated by BRENDA team
Kotliarova, S.; Pastorino, S.; Kovell, L.C.; Kotliarov, Y.; Song, H.; Zhang, W.; Bailey, R.; Maric, D.; Zenklusen, J.C.; Lee, J.; Fine, H.A.
Glycogen synthase kinase-3 inhibition induces glioma cell death through c-MYC, nuclear factor-kappaB, and glucose regulation
Cancer Res.
68
6643-6651
2008
Homo sapiens
Manually annotated by BRENDA team
Yamauchi, K.; Kurosaka, A.
Expression and function of glycogen synthase kinase-3 in human hair follicles
Arch. Dermatol. Res.
302
263-270
2010
Homo sapiens
Manually annotated by BRENDA team
Boom, A.; Authelet, M.; Dedecker, R.; Frederick, C.; Van Heurck, R.; Daubie, V.; Leroy, K.; Pochet, R.; Brion, J.P.
Bimodal modulation of tau protein phosphorylation and conformation by extracellular Zn2+ in human-tau transfected cells
Biochim. Biophys. Acta
1793
1058-1067
2009
Homo sapiens
Manually annotated by BRENDA team
Kang, N.S.; Lee, G.N.; Kim, C.H.; Bae, M.A.; Kim, I.; Cho, Y.S.
Identification of small molecules that inhibit GSK-3beta through virtual screening
Bioorg. Med. Chem. Lett.
19
533-537
2009
Homo sapiens (P49841)
Manually annotated by BRENDA team
Saitoh, M.; Kunitomo, J.; Kimura, E.; Hayase, Y.; Kobayashi, H.; Uchiyama, N.; Kawamoto, T.; Tanaka, T.; Mol, C.D.; Dougan, D.R.; Textor, G.S.; Snell, G.P.; Itoh, F.
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta
Bioorg. Med. Chem.
17
2017-2029
2009
Homo sapiens (P49841)
Manually annotated by BRENDA team
Ye, Q.; Xu, G.; Lv, D.; Cheng, Z.; Li, J.; Hu, Y.
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors
Bioorg. Med. Chem.
17
4302-4312
2009
Homo sapiens
Manually annotated by BRENDA team
Song, S.; Mazurek, N.; Liu, C.; Sun, Y.; Ding, Q.Q.; Liu, K.; Hung, M.C.; Bresalier, R.S.
Galectin-3 mediates nuclear beta-catenin accumulation and Wnt signaling in human colon cancer cells by regulation of glycogen synthase kinase-3beta activity
Cancer Res.
69
1343-1349
2009
Homo sapiens
Manually annotated by BRENDA team
Koh, S.H.; Kim, S.H.; Kim, H.T.
Role of glycogen synthase kinase-3 in L-DOPA-induced neurotoxicity
Expert. Opin. Drug Metab. Toxicol.
5
1359-1368
2009
Homo sapiens
Manually annotated by BRENDA team
Gimenez-Cassina, A.; Lim, F.; Cerrato, T.; Palomo, G.M.; Diaz-Nido, J.
Mitochondrial hexokinase II promotes neuronal survival and acts downstream of glycogen synthase kinase-3
J. Biol. Chem.
284
3001-3011
2009
Homo sapiens
Manually annotated by BRENDA team
Wu, C.H.; Yeh, S.H.; Tsay, Y.G.; Shieh, Y.H.; Kao, C.L.; Chen, Y.S.; Wang, S.H.; Kuo, T.J.; Chen, D.S.; Chen, P.J.
Glycogen synthase kinase-3 regulates the phosphorylation of severe acute respiratory syndrome coronavirus nucleocapsid protein and viral replication
J. Biol. Chem.
284
5229-5239
2009
Homo sapiens
Manually annotated by BRENDA team
Dobocan, M.C.; Sadvakassova, G.; Congote, L.F.
Chaperonin 10 as an endothelial-derived differentiation factor: role of glycogen synthase kinase-3
J. Cell. Physiol.
219
470-476
2009
Homo sapiens
Manually annotated by BRENDA team
Goodarzi, M.; Freitas, M.P.; Jensen, R.
Feature selection and linear/nonlinear regression methods for the accurate prediction of glycogen synthase kinase-3beta inhibitory activities
J. Chem. Inf. Model.
49
824-832
2009
Homo sapiens
Manually annotated by BRENDA team
Chan, M.M.; Cheung, B.K.; Li, J.C.; Chan, L.L.; Lau, A.S.
A role for glycogen synthase kinase-3 in antagonizing mycobacterial immune evasion by negatively regulating IL-10 induction
J. Leukoc. Biol.
86
283-291
2009
Homo sapiens
Manually annotated by BRENDA team
Kim, K.H.; Gaisina, I.; Gallier, F.; Holzle, D.; Blond, S.Y.; Mesecar, A.; Kozikowski, A.P.
Use of molecular modeling, docking, and 3D-QSAR studies for the determination of the binding mode of benzofuran-3-yl-(indol-3-yl)maleimides as GSK-3beta inhibitors
J. Mol. Model.
15
1463-1479
2009
Homo sapiens (P49841)
Manually annotated by BRENDA team
Cheenpracha, S.; Zhang, H.; Mar, A.M.; Foss, A.P.; Foo, S.H.; Lai, N.S.; Jee, J.M.; Seow, H.F.; Ho, C.C.; Chang, L.C.
Yeast glycogen synthase kinase-3beta pathway inhibitors from an organic extract of Streptomyces sp.
J. Nat. Prod.
72
1520-1523
2009
Homo sapiens
Manually annotated by BRENDA team
van Eersel, J.; Bi, M.; Ke, Y.D.; Hodges, J.R.; Xuereb, J.H.; Gregory, G.C.; Halliday, G.M.; Goetz, J.; Kril, J.J.; Ittner, L.M.
Phosphorylation of soluble tau differs in Picks disease and Alzheimers disease brains
J. Neural Transm.
116
1243-1251
2009
Homo sapiens
Manually annotated by BRENDA team
Castano, Z.; Gordon-Weeks, P.R.; Kypta, R.M.
The neuron-specific isoform of GSK-3beta is required for axon growth
J. Neurochem.
113
117-130
2010
Homo sapiens
Manually annotated by BRENDA team
LaPointe, N.E.; Morfini, G.; Pigino, G.; Gaisina, I.N.; Kozikowski, A.P.; Binder, L.I.; Brady, S.T.
The amino terminus of tau inhibits kinesin-dependent axonal transport: implications for filament toxicity
J. Neurosci. Res.
87
440-451
2009
Homo sapiens
Manually annotated by BRENDA team
Miura, T.; Nishihara, M.; Miki, T.
Drug development targeting the glycogen synthase kinase-3beta (GSK-3beta)-mediated signal transduction pathway: role of GSK-3beta in myocardial protection against ischemia/reperfusion injury
J. Pharmacol. Sci.
109
162-167
2009
Homo sapiens
Manually annotated by BRENDA team
Osakada, F.; Takahashi, M.
Drug development targeting the glycogen synthase kinase-3beta (GSK-3beta)-mediated signal transduction pathway: targeting the Wnt pathway and transplantation therapy as strategies for retinal repair
J. Pharmacol. Sci.
109
168-173
2009
Homo sapiens
Manually annotated by BRENDA team
Takahashi-Yanaga, F.; Sasaguri, T.
Drug development targeting the glycogen synthase kinase-3beta (GSK-3beta)-mediated signal transduction pathway: Inhibitors of the Wnt/beta-catenin signaling pathway as novel anticancer drugs
J. Pharmacol. Sci.
109
179-183
2009
Homo sapiens
Manually annotated by BRENDA team
Deming, D.; Geiger, P.; Chen, H.; Kunnimalaiyaan, M.; Holen, K.
ZM336372 induces apoptosis associated with phosphorylation of GSK-3beta in pancreatic adenocarcinoma cell lines
J. Surg. Res.
161
28-32
2009
Homo sapiens
Manually annotated by BRENDA team
Jahnke, H.G.; Rothermel, A.; Sternberger, I.; Mack, T.G.; Kurz, R.G.; Paenke, O.; Striggow, F.; Robitzki, A.A.
An impedimetric microelectrode-based array sensor for label-free detection of tau hyperphosphorylation in human cells
Lab Chip
9
1422-1428
2009
Homo sapiens
Manually annotated by BRENDA team
Voss, K.; Gamblin, T.C.
GSK-3beta phosphorylation of functionally distinct tau isoforms has differential, but mild effects
Mol. Neurodegener.
4
18
2009
Homo sapiens
Manually annotated by BRENDA team
Manceur, A.P.; Driscoll, B.D.; Sun, W.; Audet, J.
Selective enhancement of the uptake and bioactivity of a TAT-conjugated peptide inhibitor of glycogen synthase kinase-3
Mol. Ther.
17
500-507
2009
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Greco, S.J.; Sarkar, S.; Casadesus, G.; Zhu, X.; Smith, M.A.; Ashford, J.W.; Johnston, J.M.; Tezapsidis, N.
Leptin inhibits glycogen synthase kinase-3beta to prevent tau phosphorylation in neuronal cells
Neurosci. Lett.
455
191-194
2009
Homo sapiens
Manually annotated by BRENDA team
Santo, L.; Vallet, S.; Hideshima, T.; Cirstea, D.; Ikeda, H.; Pozzi, S.; Patel, K.; Okawa, Y.; Gorgun, G.; Perrone, G.; Calabrese, E.; Yule, M.; Squires, M.; Ladetto, M.; Boccadoro, M.; Richardson, P.G.; Munshi, N.C.; Anderson, K.C.; Raje, N.
AT7519, a novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition
Oncogene
29
2325-2336
2010
Homo sapiens
Manually annotated by BRENDA team
Thompson, A.J.; Williamson, R.; Schofield, E.; Stephenson, J.; Hanger, D.; Anderton, B.
Quantitation of glycogen synthase kinase-3 sensitive proteins in neuronal membrane rafts
Proteomics
9
3022-3035
2009
Homo sapiens
Manually annotated by BRENDA team
Nehme, H.; Chantepie, S.; Defert, J.; Morin, P.; Papy-Garcia, D.; Nehme, R.
New methods based on capillary electrophoresis for in vitro evaluation of protein tau phosphorylation by glycogen synthase kinase 3-beta
Anal. Bioanal. Chem.
407
2821-2828
2015
Homo sapiens (P49841)
Manually annotated by BRENDA team
Ye, Q.; Li, M.; Zhou, Y.B.; Cao, J.Y.; Xu, L.; Li, Y.J.; Han, L.; Gao, J.R.; Hu, Y.Z.; Li, J.
Design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3beta inhibitors
Arch. Pharm.
346
349-358
2013
Homo sapiens (P49841)
Manually annotated by BRENDA team
Saeki, K.; Machida, M.; Kinoshita, Y.; Takasawa, R.; Tanuma, S.
Glycogen synthase kinase-3beta2 has lower phosphorylation activity to tau than glycogen synthase kinase-3beta1
Biol. Pharm. Bull.
34
146-149
2011
Homo sapiens (P49841)
Manually annotated by BRENDA team
Liao, J.C.; Yang, T.T.; Weng, R.R.; Kuo, C.T.; Chang, C.W.
TTBK2: a tau protein kinase beyond tau phosphorylation
BioMed Res. Int.
2015
575170
2015
Mus musculus (Q3UVR3), Homo sapiens (Q6IQ55)
Manually annotated by BRENDA team
Lund, H.; Cowburn, R.F.; Gustafsson, E.; Stroemberg, K.; Svensson, A.; Dahllund, L.; Malinowsky, D.; Sunnemark, D.
Tau-tubulin kinase 1 expression, phosphorylation and co-localization with phospho-Ser422 tau in the Alzheimers disease brain
Brain Pathol.
23
378-389
2012
Homo sapiens (Q5TCY1), Homo sapiens
Manually annotated by BRENDA team
Xu, J.; Sato, S.; Okuyama, S.; Swan, R.J.; Jacobsen, M.T.; Strunk, E.; Ikezu, T.
Tau-tubulin kinase 1 enhances prefibrillar tau aggregation and motor neuron degeneration in P301L FTDP-17 tau-mutant mice
FASEB J.
24
2904-2915
2010
Homo sapiens (Q5TCY1)
Manually annotated by BRENDA team
Hanger, D.P.; Noble, W.
Functional implications of glycogen synthase kinase-3-mediated tau phosphorylation
Int. J. Alzheimers Dis.
2011
352805
2011
Homo sapiens (P49841)
Manually annotated by BRENDA team
Kumar Dasappa, J.; Nagendra, H.G.
Preferential selectivity of inhibitors with human tau protein kinase gsk3beta elucidates their potential roles for off-target Alzheimers therapy
Int. J. Alzheimers Dis.
2013
809386
2013
Homo sapiens (P49841), Homo sapiens
Manually annotated by BRENDA team
Buescher, J.L.; Phiel, C.J.
A noncatalytic domain of glycogen synthase kinase-3 (GSK-3) is essential for activity
J. Biol. Chem.
285
7957-7963
2010
Homo sapiens (P49840), Homo sapiens (P49841)
Manually annotated by BRENDA team
Soutar, M.P.; Kim, W.Y.; Williamson, R.; Peggie, M.; Hastie, C.J.; McLauchlan, H.; Snider, W.D.; Gordon-Weeks, P.R.; Sutherland, C.
Evidence that glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain
J. Neurochem.
115
974-983
2010
Homo sapiens (P49840), Homo sapiens (P49841)
Manually annotated by BRENDA team
Ranganadha Reddy, A.; Venkateswarulu, T.; John Babu, D.; Shyamala Devi, N.
Homology modeling, simulation and docking studies of Tau-protein kinase
Res. J. Pharm. Technol.
7
376-388
2014
Homo sapiens
-
Manually annotated by BRENDA team
Jiang, J.; Wang, Z.H.; Qu, M.; Gao, D.; Liu, X.P.; Zhu, L.Q.; Wang, J.Z.
Stimulation of EphB2 attenuates tau phosphorylation through PI3K/Akt-mediated inactivation of glycogen synthase kinase-3beta
Sci. Rep.
5
11765
2015
Homo sapiens (P49841), Homo sapiens, Mus musculus (Q9WV60), Mus musculus
Manually annotated by BRENDA team
Marcotte, D.J.; Spilker, K.A.; Wen, D.; Hesson, T.; Patterson, T.A.; Kumar, P.R.; Chodaparambil, J.V.
The crystal structure of the catalytic domain of tau tubulin kinase 2 in complex with a small-molecule inhibitor
Acta Crystallogr. Sect. F
76
103-108
2020
Homo sapiens (Q6IQ55), Homo sapiens
Manually annotated by BRENDA team
Ikezu, S.; Ingraham Dixie, K.L.; Koro, L.; Watanabe, T.; Kaibuchi, K.; Ikezu, T.
Tau-tubulin kinase 1 and amyloid-beta peptide induce phosphorylation of collapsin response mediator protein-2 and enhance neurite degeneration in Alzheimer disease mouse models
Acta Neuropathol. Commun.
8
12
2020
Homo sapiens (Q5TCY1), Homo sapiens
Manually annotated by BRENDA team
Bao, C.; Bajrami, B.; Marcotte, D.J.; Chodaparambil, J.V.; Kerns, H.M.; Henderson, J.; Wei, R.; Gao, B.; Dillon, G.M.
Mechanisms of regulation and diverse activities of tau-tubulin kinase (TTBK) isoforms
Cell. Mol. Neurobiol.
41
669-685
2021
Mus musculus (Q3UVR3), Mus musculus (Q6PCN3), Homo sapiens (Q5TCY1), Homo sapiens (Q6IQ55)
Manually annotated by BRENDA team
Nieding, K.; Matschke, V.; Meuth, S.G.; Lang, F.; Seebohm, G.; Strutz-Seebohm, N.
Tau tubulin kinase TTBK2 sensitivity of glutamate receptor GluK2
Cell. Physiol. Biochem.
39
1444-1452
2016
Homo sapiens (Q6IQ55), Homo sapiens
Manually annotated by BRENDA team
Nozal, V.; Martinez, A.
Tau tubulin kinase 1 (TTBK1), a new player in the fight against neurodegenerative diseases
Eur. J. Med. Chem.
161
39-47
2019
Homo sapiens (Q5TCY1)
Manually annotated by BRENDA team
Jana, S.; Singh, S.K.
Identification of human tau-tubulin kinase 1 inhibitors an integrated e-pharmacophore-based virtual screening and molecular dynamics simulation
J. Biomol. Struct. Dyn.
38
886-900
2020
Homo sapiens (Q5TCY1), Homo sapiens
Manually annotated by BRENDA team
Cortes-Gomez, M.; Llorens-Alvarez, E.; Alom, J.; del Ser, T.; Avila, J.; Saez-Valero, J.; Garcia-Ayllon, M.
Tau phosphorylation by glycogen synthase kinase 3beta modulates enzyme acetylcholinesterase expression
J. Neurochem.
157
2091-2105
2020
Homo sapiens (P49841), Homo sapiens
Manually annotated by BRENDA team
Llorach-Pares, L.; Nonell-Canals, A.; Avila, C.; Sanchez-Martinez, M.
Kororamides, convolutamines, and indole derivatives as possible tau and dual-specificity kinase inhibitors for Alzheimer's disease A computational study
Mar. Drugs
16
386
2018
Homo sapiens (P48730), Homo sapiens (P49841)
Manually annotated by BRENDA team
Bernatik, O.; Pejskova, P.; Vyslouzil, D.; Hanakova, K.; Zdrahal, Z.; Cajanek, L.
Phosphorylation of multiple proteins involved in ciliogenesis by tau tubulin kinase 2
Mol. Biol. Cell
31
1032-1046
2020
Homo sapiens (Q6IQ55), Homo sapiens
Manually annotated by BRENDA team