Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + alpha-actin
ADP + p35
-
-
-
?
ATP + alpha-casein
ADP + alpha-casein phosphate
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
-
-
-
-
?
ATP + axin
ADP + phosphorylated axin
ATP + beta-casein
ADP + beta-casein phosphate
-
isoenzyme TPKII
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
ATP + beta-catenin
ADP + phosphorylated beta-catenin
ATP + c-Jun
ADP + phosphorylated c-Jun
-
substrate of isoform GSK-3alpha
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
-
-
-
-
?
ATP + cAMP response element-binding protein
ADP + phosphorylated cAMP response element-binding protein
-
-
-
-
?
ATP + casein
ADP + phosphorylated casein
ATP + CCDC92
ADP + phosphorylated CCDC92
-
-
-
?
ATP + CEP164
ADP + phospho-CEP164
ATP + CEP164
ADP + phosphorylated CEP164
TTBK2-induced phosphorylations of CEP164 modulate its function, which in turn seems relevant for the process of cilia formation
-
-
?
ATP + CEP83
ADP + phosphorylated CEP83
-
-
-
?
ATP + CEP89
ADP + phosphorylated CEP89
-
-
-
?
ATP + CEP97
ADP + phospho-CEP97
ATP + coronavirus nucleocapsid protein
ADP + phosphorylated coronavirus nucleocapsid protein
-
phosphorylation sites are at Ser177, Ser181, Ser184, Ser185, Ser187, Ser189, Ser191, Ser203, and Ser207
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
-
-
-
-
?
ATP + cyclin D1
ADP + phosphorylated cyclin D1
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
-
-
-
-
?
ATP + dephospho-beta-tubulin
ADP + beta-tubulin phosphate
-
isoenzyme tau-tubulin kinase
-
-
?
ATP + DIWKKFELLPTPPLSPSRRSG
ADP + DIWKKFELLP(P)TPPL(P)SPSRRSG
c-Myc
-
?
ATP + DIWKKFELVPSPPTSPPWGL
ADP + DIWKKFELVP(P)SPPT(P)SPPWGL
L-myc
-
?
ATP + DVL3
ADP + phosphorylated DVL3
-
-
-
?
ATP + EEPQTVPEMPGETPPLSPIDMESQER
ADP + EEPQTVPEMPGE(P)TPPL(P)SPIDMESQER
c-Jun
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
ATP + FITC-GSRSRTPSLP
ADP + FITC-GSRSRTP-phosphoserine-LP
-
synthetic fluorescence-labeled peptide substrate derived from residues 207-216 of tau protein, phosphorylation of S214 by SGK1
-
-
?
ATP + FXVEXTPXCFSRXSSLSSLS
ADP + ?
-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
-
-
-
-
?
ATP + glycogen synthase
ADP + phosphorylated glycogen synthase
-
-
-
?
ATP + H-Arg-Arg-Arg-Ala-Ala-Glu-Glu-Leu-Asp-Ser-Arg-Ala-Gly-pSer-Pro-Gln-Leu-OH
ADP + ?
-
-
-
-
?
ATP + heat shock factor-1
ADP + phosphorylated heat shock factor-1
-
-
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
ATP + histone H2a
ADP + histone H2a phosphate
-
isoenzyme TPKII
-
-
?
ATP + histone H2b
ADP + histone H2b phosphate
-
isoenzyme TPKII
-
-
?
ATP + histone H3
ADP + histone H3 phosphate
-
isoenzyme TPKII
-
-
?
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
ATP + HSPB6
ADP + phosphorylated HSPB6
-
phosphorylation at Ser16
-
-
?
ATP + JHMV-N protein
ADP + phosphorylated JHMV-N protein
-
phosphorylation sites are at Ser197, Ser201, Ser-205, and Ser-209
-
-
?
ATP + Jun
ADP + phosphorylated Jun
-
-
-
-
?
ATP + KAUSSPTVSRKTD
ADP + KAUSSPTVSRKTD phosphate
-
synthetic peptide p25/F3
-
-
?
ATP + KRREILSRRPpSYR
ADP + ?
-
KRREILSRRPpSYR is selectively phosphorylated by GSK-3 and therefore acts as a competitive inhibitor of other GSK-3 substrates
-
-
?
ATP + LLNASGSTSTPAPSRTASFSESR
ADP + LLNASGSTS(P)TPAP(P)SRTASFSESR
ATP-citrate lyase
-
?
ATP + MADSRPKPANKTPPK
ADP + MADSRPKPANKTPPK phosphate
-
synthetic peptide F5f
-
-
?
ATP + mammalian histone H1
ADP + phosphorylated mammalian histone H1
ATP + MAP2
ADP + MAP2 phosphate
ATP + MARSRPK
ADP + MARSRPK phosphate
-
synthetic peptide F5h
-
-
?
ATP + mu-calpain
ADP + calpastatin
-
-
-
?
ATP + Myc
ADP + phosphorylated Myc
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
-
-
-
-
?
ATP + p53
ADP + p53 phosphate
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
ATP + PANKTPPKSPGEPAKDPAAK
ADP + PANKTPPKSPGEPAKDPAAK phosphate
-
synthetic peptide p25/F5a
-
-
?
ATP + phospho-glycogen synthase peptide-2
ADP + phosphorylated phospho-glycogen synthase peptide-2
-
GSK3 substrate
-
-
?
ATP + protein
ADP + phosphoprotein
autophosphorylation at Tyr and Ser
-
-
?
ATP + protein PHF-1
ADP + protein PHF-1 phosphate
-
-
-
-
?
ATP + protein PHF-1 (Ser396/404)
ADP + protein PHF-1 (Ser396/404) phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
ATP + protein tau-1
ADP + protein tau-1 phosphate
-
-
-
-
?
ATP + pyruvate dehydrogenase
ADP + pyruvate dehydrogenase phosphate
-
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
-
-
-
?
ATP + RADSRPK
ADP + RADSRPK phosphate
-
synthetic peptide F5g
-
-
?
ATP + RKRSRAE
ADP + RKRSRAE phosphate
-
synthetic peptide 8659
-
-
?
ATP + RKRSRKE
ADP + RKRSRKE phosphate
-
synthetic peptide 8655
-
-
?
ATP + RRREEETEEE
ADP + RRREEETEEE phosphate
-
synthetic peptide CKII substrate
-
-
?
ATP + RRRPASVPPSPSLSRHSpSHQRR
ADP + ?
-
-
-
-
?
ATP + RSRSRSRSRSRSPPPVSK
ADP + phosphorylated RSRSRSRSRSRSPPPVSK
-
SC35-derived peptide 180-197, recombinant GSK-3beta
-
-
?
ATP + SC35
ADP + phosphorylated SC35
ATP + SPPLSPIDMETQER
ADP + (P)SPPLSPIDME(P)TQER
JunD
-
?
ATP + SPVVSGDT(P)SPR
ADP + ?
-
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
ATP + tau-protein
ADP + O-phospho-tau-protein
ATP + TDP-43
ADP + phospho-TDP-43
ATP + TDP-43
ADP + phosphorylated TDP-43
-
-
-
?
ATP + TPPKSPSAAK
ADP + TPPK(P)SPSAAK
protein tau
-
?
ATP + tubulin
ADP + phospho-tubulin
ATP + YRRAAVPPSPSLSRHSSPHQSpEDEEE
ADP + ?
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
-
-
?
ATP + [FRAT-2 protein]
ADP + phosphorylated [FRAT-2 protein]
-
i.e. frequently rearranged in advanced T-cell lymphoma protein 2, phosphorylation by GSK3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
protein tau + ATP
phosphorylated protein tau + ADP
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
-
-
?
additional information
?
-
ATP + alpha-casein
ADP + alpha-casein phosphate
-
-
-
-
?
ATP + alpha-casein
ADP + alpha-casein phosphate
-
isoenzyme TPKI
-
-
?
ATP + axin
ADP + phosphorylated axin
-
-
-
-
?
ATP + axin
ADP + phosphorylated axin
-
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
-
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
-
-
-
?
ATP + beta-catenin
ADP + beta-catenin phosphate
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
-
substrate of isoform GSK-3beta
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
-
-
-
-
?
ATP + casein
ADP + phosphorylated casein
-
-
-
-
?
ATP + casein
ADP + phosphorylated casein
-
-
-
-
?
ATP + CEP164
ADP + phospho-CEP164
-
-
-
?
ATP + CEP164
ADP + phospho-CEP164
-
-
-
?
ATP + CEP97
ADP + phospho-CEP97
-
-
-
?
ATP + CEP97
ADP + phospho-CEP97
-
-
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
-
-
-
-
?
ATP + eIF2B peptide
ADP + phosphorylated eIF2B peptide
-
-
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
-
isoenzyme TPKII
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
-
isoenzyme TPKII
-
-
?
ATP + histone H1
ADP + histone H1 phosphate
-
Cdk5 substrate
-
-
?
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
-
-
-
?
ATP + HLSNVSSTGSIDMVDSPQLATLADEVSASLAK
ADP + HLSNVSSTGSIDMVDpSPQLATLADEVSASLAK
-
-
-
?
ATP + mammalian histone H1
ADP + phosphorylated mammalian histone H1
-
-
-
-
?
ATP + mammalian histone H1
ADP + phosphorylated mammalian histone H1
-
-
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
-
-
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
-
isoenzyme TPKI and TPKII
-
-
?
ATP + MAP2
ADP + MAP2 phosphate
-
isoenzyme TPKII
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
-
-
-
?
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylates tau and forms paired helical filament epitopes, tau/K1, K2, K3 and tau/4 repeat
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylates tau on S202, T231, S396, and S400 but not on S262, S235, and S404. Phosphorylates tau directly at S202 but requires the previous phosphorylation on S235 to phosphorylate T231, once a priming kinase phosphorylates S404, GSK3beta sequentially phosphorylates S400 and then S396
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
Drosophila sp. (in: flies)
-
GSK-3beta-mediated hyperphosphorylated forms of tau are degradable by the proteasomal machinery
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
691083, 702438, 702646, 703599, 704555, 705246, 705263, 705280, 705440, 705916, 706016, 706672 -
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
enzyme can also phosphorylate bovine tau
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylates tau protein into Alzheimer disease-like forms, resulting in neuronal death
-
?
ATP + protein tau
ADP + protein tau phosphate
-
when a beta-mediated aggregated tau is used as a substrate for TPKII, an 8fold increase in the rate of TPKII-mediated tau phosphorylation is observed
-
?
ATP + protein tau
ADP + protein tau phosphate
-
6 isoforms of human tau expressed in adult human brain
-
?
ATP + protein tau
ADP + protein tau phosphate
-
prior phosphorylation of tau by isoenzyme TPKII strongly enhances the action of TPKI
-
?
ATP + protein tau
ADP + protein tau phosphate
-
regulates PDH and participates in energy metabolism and acetylcholine synthesis
-
?
ATP + protein tau
ADP + protein tau phosphate
-
direct tau phosphorylation by TTBK1 at Ser198, Ser199, Ser202 and Ser422
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
TTBK2 (1-331) phosphorylates residues Ser208 and Ser210
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
in vitro, GSK-3beta phosphorylates protein tau at 14 sites, all tau protein isoforms are phosphorylated by GSK-3beta which changes filament polymerization levels and filament morphology
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylation at Ser9
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
role of GSK3 as a key mediator of tau hyperphosphorylation, whereas Cdk5 acts as a modulator of tau hyperphosphorylation via the inhibitory regulation of GSK3
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
T231 is the primary phosphorylation site for GSK3beta, the tau227-237 (AVVRTPPKSPS) derived from tau containing T231P232 motif is the GSK3beta binding site with high affinity (Kd = 0.00082 mmol/L), tau mutant T231A completely abolishes tau phosphorylation by GSK3beta
-
-
?
ATP + protein tau
ADP + protein tau phosphate
the antagonist of GSK-3beta in protein tau phosphorylation is the phosphatase PP2A
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylation occurs at Ser-396/Ser-404
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
PKA transfers about 2 mol of phosphate per mole of the shortest protein tau isoform and phosphorylates Ser156, 235, 267, 320 and 327 (corresponding to Ser214, 324, 356, 409 and 416 of the longest protein tau isoform)
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylation at Ser9
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
protein tau primed by CK1 functions as an effective phosphate acceptor for GSK-3beta
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
microtubule-associated protein, enzyme can also phosphorylate human tau
-
?
ATP + protein tau
ADP + protein tau phosphate
-
microtubule-associated protein
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + SC35
ADP + phosphorylated SC35
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
-
-
?
ATP + SC35
ADP + phosphorylated SC35
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors, recombinant GSK-3beta
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
-
tau in Alzheimer disease brain is highly phosphorylated and aggregates into paired helical filaments comprising characteristic neurofibrillary tangles, overview
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
-
determination of several phosphorylation sites, e.g. Ser258, Ser289, Ser262, and Ser356 within the microtubule-binding repeats or at Ser184 and Ser185 of the central region, for casein kinase I, casein kinase 2, and glycogen synthase kinase-3beta in insoluble tau, PHF-tau, extracted from Alzheimer brain and of tau from control healthy brain by mass spectrometry, overview
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
phosphorylation at Ser-422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 phosphorylates tau-protein at Ser198, Ser199, Ser202 and Ser422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
phosphorylation on Ser198, Ser199, Ser202, and Ser422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
tau tubulin kinase 2 phosphorylates tau-protein at Ser208 and Ser210
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
good substrate for protein kinase A which phosphorylates several key residues (Ser156, Ser235, Ser267, Ser320, Ser327) of tau-protein and induces its tight interaction with 14-3-3 proteins
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
ERK2 phosphorylates Thr-50, Thr-153, Thr-175, Thr-181, Thr-205, Thr-231, Ser-235, Ser-404, and Ser-422 in tau-protein
-
-
?
ATP + TDP-43
ADP + phospho-TDP-43
-
-
-
?
ATP + TDP-43
ADP + phospho-TDP-43
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
-
-
-
?
ATP + YRRAAVPPSPSLSRHSSPHQSpEDEEE
ADP + ?
-
-
-
-
?
ATP + YRRAAVPPSPSLSRHSSPHQSpEDEEE
ADP + ?
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
14-3-3 connects glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
cdk5 associated with p25
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation of tau, especially at the primed epitope T231 negatively regulates tau-microtubule interactions, different effects of phosphorylation on primed T231 and unprimed S396/S404 epitopes of tau, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
protein 14-3-3 mediates phosphorylation of microtubule-associated protein tau by serum- and glucocorticoid-induced protein kinase 1 SGK1, which forms an activated ternary complex with protein 14-3-3theta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau is primarily found in neurons, regulation of tau phosphorylation by GSK3beta via interaction with FRAT-1 and FRAT-2, i.e. frequently rearranged in advanced T-cell lymphoma proteins
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
cdk5 associated with p25, recombinant bacterially expressed human tau protein as substrate, phosphorylation of the AT8 and AT180 epitopes, and at T231 of the Alzheimer's mitotic epitope TG-3
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation at the C-terminus, lower activity with C-terminally truncated tau D421 compared to the wild-type tau, the truncated tau protein forms sarcosyl-insoluble aggregates
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation of primed and unprimed sites by GSK3beta, wild-type and recombinant tau, recombinant GSK3beta S9A
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation of S214 by SGK1, recombinant tau S214A is no substrate
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phoshorylation at residues Ser404, Ser199, Ser202 and Thr231
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation at Ser208 and Ser210
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
tau isoforms in the human central nervous system and GSK-3 phosphorylation sites. Isozymes GSK-3alpha and GSK-3beta1/2 differentially phosphorylate tau, e.g. Ser396 in tau is phosphorylated by both splice variants, whereas Ser199 is a significant target of GSK-3beta1, but not of GSK-3beta2 activity
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation at Ser422, no phosphorylation at Ser231
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation level of tau at Thr205, Thr231, Ser396 and tau-1 sites
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
the enzyme is a serine/threonine protein kinase
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
the enzyme phosphorylates in tau residues S46, T50, S69, and T71 at the N-terminus, residues T149, T153, T175, T181, S184, S195, S198, S199, S202, T205, S210, T212, S214, T217, T220, T231, S235, S237, S241, and T245 in the central, proline-rich domain, residues S258 and S262 in the repeat domain R1 domain, residues S285, S289, and S324 in the repeat domain R2 domain, and residues S352, S356, T373, S396, S400, S404, S409, and S413 in the repeat domain R4 domain, there are no phosphorylation sites of GSK-3 in the repeat domain R3 domain, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
activity in organisms with mutated APP and tau, not in wild-type, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
cdk5 substrate in brain, cdk5 associated with p39, tau is a microtubule-associated and developmentally regulated protein involved in axonal development in neurons, tau phosphorylation by cyclin-dependent kinase 5/p39 during brain development reduces its affinity for microtubules
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
hyperphosphorylation of tau by CDK5 is involved in apoptosis and neurodegeneration in Alzheimer's disease, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
regulation, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation in vivo is stimulated by extracellular signal-regulated kinase Erk phosphorylation and apolipoprotein isozyme E4, to a lesser extent by isozyme apoE3, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation of the PHF-1 epitope at Ser396 and Ser404 by CDK5
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
preferred substrate of cdk5 associated with p39, recombinant bacterially expressed human tau protein as substrate, phosphorylation at Ser202 and Thr205
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK is one of the main tau kinase phosphorylating tau at the epitopes Ser262/356 and Thr231 at basal conditions in neurons
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
recombinant human tau protein expressed in transgenic mice
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK phosphorylate tau in vitro at several epitopes including Thr231, Ser262/356, Ser396, Ser409 and Ser422, whereas Ser199, Ser202, Ser235, Ser400, and Ser404 are not phosphorylated by AMPK
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation level of tau at Thr205, Thr231, Ser396 and tau-1 sites
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK is one of the main tau kinase phosphorylating tau at the epitopes Ser262/356 and Thr231 at basal conditions in neurons
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK phosphorylate tau in vitro at several epitopes including Thr231, Ser262/356, Ser396, Ser409 and Ser422, whereas Ser199, Ser202, Ser235, Ser400, and Ser404 are not phosphorylated by AMPK
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
abnormal hyperphosphorylation of tau by PKA and GSK-3 is associated with Alzheimer's disease and other tauopaties leading to neuronal degeneration
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau is microtubule-associated, phopshorylation at T231 by CDK5 causes its release into the cytoplasm
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation at T231, no activity with tau mutant T231A
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation by PKA at Ser214, and by GSK-3 at Ser404, Ser396, Ser198, Ser199, and Ser202
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation of tau at various sites
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation at Ser198, Ser199, Ser202, Ser396, and Ser404
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
tau phosphorylation at GSK-3beta sensitive but AMPK insensitive residues Ser202/Thr205
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
tau phosphorylation at GSK-3beta sensitive but AMPK insensitive residues Ser202/Thr205
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
-
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
proline-directed kinase
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
-
-
-
?
glycogen synthase + ATP
phosphorylated glycogen synthase + ADP
-
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
-
TPKI cannot phosphorylate K1, K2 and K3 peptides, histones H1, H2A, H2B and H3 and beta casein
-
-
?
additional information
?
-
-
novel isoenzyme, distinct from TPKI, TPKII CKI and CKII, no activity toward beta-casein and neurofilament, no reaction with synthetic peptides F5a PANKTPPKSPGEPAKDPAAK, F5n MADSRPK, F5d MADSRKPAN, F5e MADSRPAE and 8656 RKRARKE, only weak activity with histones H1, H2a and H2b as substrates
-
-
?
additional information
?
-
-
glycogen synthase kinase-3beta also performs serine/threonine protein kinase reaction, EC 2.7.11.1, with other substrates than tau, e.g. it phosphorylates the glycogen synthase
-
-
?
additional information
?
-
enzyme regulates cell fate in Dictyostelium
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
possible role of the sgg protein in a signal transduction pathway necessary for intercellular communication at different stages of development
-
-
?
additional information
?
-
enzyme acts as a repressor of engrailed autoregulation
-
-
?
additional information
?
-
implicated in cell-fate determination and differentiation, phosphorylates several regulatory proteins that are activated by dephosphorylation in response to hormones or growth factors
-
-
?
additional information
?
-
enzyme of the lithium-sensitive wnt signaling pathway
-
-
?
additional information
?
-
enzyme forms part of the wingless signalling pathway. GSK-3beta activity is negatively regulated by phosphorylation on serine 9 and positively regulated by phosphorylation on tyrosine 216. Enzyme may also be regulated at the transcriptional level
-
-
?
additional information
?
-
-
abnormal phosphorylation of tau in dividing cells leads to its accumulation in the cytosol as microtubule-free form, Cdk5 is involved in neurodegenerative mechanisms
-
-
?
additional information
?
-
-
GSK-3 affects the tau-mRNA splicing of exon 10 via phosphorylation of the splicing factors of the serine/arginine-rich splicing factor SR family, e.g. SC35, leading to priming and dislocation of the splicing factor, aberrant tau splicing contributes to tauopathies including Alzheimer's disease, overview
-
-
?
additional information
?
-
-
GSK3beta and PKA work coordinatedly on tau phosphorylation
-
-
?
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of organisms with Alzheimer's disease leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of patients suffering from Alzheimer's disease leads to age-dependent memory deficits
-
-
?
additional information
?
-
-
phosphorylated tau is important in cytoskeleton assembly
-
-
?
additional information
?
-
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization in the nucleus or cytoplasm, overview
-
-
?
additional information
?
-
-
the enzyme participates in Alzheimer's disease
-
-
?
additional information
?
-
-
GSK3beta catalyzes tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins, EC 2.7.11.1, in different tissues
-
-
?
additional information
?
-
-
GSK3beta catalyzes tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins, EC 2.7.11.1, in different tissues
-
-
?
additional information
?
-
-
GSK3beta catalyzes tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins, EC 2.7.11.1, in different tissues
-
-
?
additional information
?
-
-
GSK3beta, EC 2.7.11.1, and PKA, EC 2.7.11.11, catalyze tau phosphorylation in brain, but phosphorylation of glycogen synthase and other proteins in different tissues
-
-
?
additional information
?
-
-
substrate specificity of GSK3beta
-
-
?
additional information
?
-
the enzyme performs autophosphorylation
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain. There are GSK3 substrates with preference for GSK3beta1 over GSK3beta2, and others that hold no distinction, suggesting different modes of interaction with GSK3, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain. There are GSK3 substrates with preference for GSK3beta1 over GSK3beta2, and others that hold no distinction, suggesting different modes of interaction with GSK3, overview
-
-
?
additional information
?
-
in addition to autophosphorylation, known phosphorylation substrates of TTBK2 include tau, tubulin, CEP164, CEP97, and TDP-43, a neurodegeneration-associated protein. The enzyme binds to CEP164, a centriolar protein, and EB1, a microtubule plus-end tracking protein
-
-
?
additional information
?
-
development and evaluation of a capillary electrophoresis-based method for in vitro determination of protein tau phosphorylation by GSK3beta. When the GSK3beta-dependent phosphorylation reaction is carried out in the presence of heparin or heparan sulfate, an increase in the maximum phosphorylation levels is clearly observed, suggesting the appearance of new phosphorylatable sites on protein tau generated by the presence of sulfated polysaccharides
-
-
?
additional information
?
-
GSK-3alpha-specific requirement for priming of tau protein
-
-
?
additional information
?
-
GSK-3alpha-specific requirement for priming of tau protein
-
-
?
additional information
?
-
recombinant splicing variant GSK-3beta2 has lower phosphorylation activity to tau than splicing variant GSK-3beta1 in vitro, although the phosphorylation activities of the two variants to a synthetic peptide substrate pGS-2 are comparable
-
-
?
additional information
?
-
tau possesses 80 phosphorylatable serine and threonine residues
-
-
?
additional information
?
-
amyloid beta induces collapsin response mediator protein-2 phosphorylation at threonine 514 in a tau-tubulin kinase 1-dependent manner, and tau-tubulin kinase 1 enhances amyloid beta-induced collapsin response mediator protein-2 phosphorylation in Rho kinase-dependent manner in vitro
-
-
-
additional information
?
-
-
amyloid beta induces collapsin response mediator protein-2 phosphorylation at threonine 514 in a tau-tubulin kinase 1-dependent manner, and tau-tubulin kinase 1 enhances amyloid beta-induced collapsin response mediator protein-2 phosphorylation in Rho kinase-dependent manner in vitro
-
-
-
additional information
?
-
isoform TTBK1 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK1 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK2 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK2 is autophosphorylated
-
-
-
additional information
?
-
no activity with Rab8a
-
-
-
additional information
?
-
-
no activity with Rab8a
-
-
-
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of mutants leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of mutants leads to age-dependent memory deficits
-
-
?
additional information
?
-
-
rapid, reversible cold-water stress-induced hyperphosphorylation of tau S199, S202, T205, T231, and S235 in hippocampal and cerebral region of the brain, hyperphosphorylation of tau is associated to the Alzheimer's disease
-
-
?
additional information
?
-
-
cdk5 also performs the kinase reaction of EC 2.7.11.22
-
-
?
additional information
?
-
the enzyme performs autophosphorylation
-
-
?
additional information
?
-
isoform TTBK1 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK1 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK2 is autophosphorylated
-
-
-
additional information
?
-
isoform TTBK2 is autophosphorylated
-
-
-
additional information
?
-
-
often protein kinase A works in pair with 14-3-3 since it phosphorylates target proteins at (R/K)RX(S/T) sequences (where X is any amino acid)
-
-
-
additional information
?
-
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
?
additional information
?
-
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
?
additional information
?
-
implicated in the hormonal control of several regulatory proteins including glycogen synthase and the transcription factor c-jun
-
-
?
additional information
?
-
-
activation and deregulation of GSK-3, e.g. by wortmannin or GF-109203X, induces Alzheimer-like tau hyperphosphorylation in hippocampus, the hyperphosphorylated tau forms neurofibrillary tangle
-
-
?
additional information
?
-
-
CDK5-dependent clustering of endoplasmic reticulum ER and mitochondria during ceramide-mediated neuronal death: neurotoxic calcium transfer from ER to mitochondria is regulated by cyclin-dependent kinase 5-dependent phosphorylation of tau, inhibition of the process leads to cell death
-
-
?
additional information
?
-
-
tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain, inhibition of tau hyperphosphorylation inhibits an associated loss in spatial memory
-
-
?
additional information
?
-
-
does not phosphorylate tau at epitope Ser 262
-
-
?
additional information
?
-
MDS1 is not essential during normal vegetative growth but appears to be required for meiosis
-
-
?
additional information
?
-
enzyme is involved in the induction of meiosis
-
-
?
additional information
?
-
MCK1 encodes a positive regulator of meiosis and spore formation. MCK1 is required in vegetative cells for basal IME1 expression, it is also required for efficient ascus maturation. MCK1 plays a role in governing centromere function during vegetative growth as well as sporulation
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + alpha-actin
ADP + p35
-
-
-
?
ATP + amyloid precursor protein
ADP + phosphorylated amyloid precursor protein
-
-
-
-
?
ATP + beta-catenin
ADP + phosphorylated beta-catenin
-
-
-
-
?
ATP + c-Myc
ADP + phosphorylated c-Myc
-
-
-
-
?
ATP + CCDC92
ADP + phosphorylated CCDC92
-
-
-
?
ATP + CEP164
ADP + phosphorylated CEP164
TTBK2-induced phosphorylations of CEP164 modulate its function, which in turn seems relevant for the process of cilia formation
-
-
?
ATP + CEP83
ADP + phosphorylated CEP83
-
-
-
?
ATP + CEP89
ADP + phosphorylated CEP89
-
-
-
?
ATP + cyclin D
ADP + phosphorylated cyclin D
-
-
-
-
?
ATP + cyclin E
ADP + phosphorylated cyclin E
-
-
-
-
?
ATP + DVL3
ADP + phosphorylated DVL3
-
-
-
?
ATP + glycogen synthase
ADP + glycogen synthase phosphate
-
-
-
-
?
ATP + mu-calpain
ADP + calpastatin
-
-
-
?
ATP + nuclear factor-kappaB
ADP + phosphorylated nuclear factor-kappaB
-
-
-
-
?
ATP + p53
ADP + phosphorylated p53
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
ATP + Rabin8
ADP + phosphorylated Rabin8
-
-
-
?
ATP + SC35
ADP + phosphorylated SC35
-
substrate prephosphorylated SC35, SC35 is a member of the SR family of serine/arginine-rich splicing factors
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
-
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
ATP + TDP-43
ADP + phosphorylated TDP-43
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
ATP + [amyloid precursor protein]
ADP + O-phospho-[amyloid precursor protein]
phosphorylation of the intracellular domain Thr668 of APP by GSK-3beta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
additional information
?
-
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
phosphorylates tau on S202, T231, S396, and S400 but not on S262, S235, and S404. Phosphorylates tau directly at S202 but requires the previous phosphorylation on S235 to phosphorylate T231, once a priming kinase phosphorylates S404, GSK3beta sequentially phosphorylates S400 and then S396
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
prior phosphorylation of tau by isoenzyme TPKII strongly enhances the action of TPKI
-
?
ATP + protein tau
ADP + protein tau phosphate
-
regulates PDH and participates in energy metabolism and acetylcholine synthesis
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
microtubule-associated protein
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + protein tau
ADP + protein tau phosphate
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
phosphorylation at Ser-422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 phosphorylates tau-protein at Ser198, Ser199, Ser202 and Ser422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
phosphorylation on Ser198, Ser199, Ser202, and Ser422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
tau tubulin kinase 2 phosphorylates tau-protein at Ser208 and Ser210
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
isoform TTBK1 is the isoform responsible for tau phosphorylation at epitopes enriched in tauopathies such as serine 422
-
-
?
ATP + tau-protein
ADP + O-phospho-tau-protein
-
ERK2 phosphorylates Thr-50, Thr-153, Thr-175, Thr-181, Thr-205, Thr-231, Ser-235, Ser-404, and Ser-422 in tau-protein
-
-
?
ATP + tubulin
ADP + phospho-tubulin
-
-
-
?
ATP + tubulin
ADP + phospho-tubulin
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
14-3-3 connects glycogen synthase kinase-3 beta to tau within a brain microtubule-associated tau phosphorylation complex
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
cdk5 associated with p25
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
phosphorylation of tau, especially at the primed epitope T231 negatively regulates tau-microtubule interactions, different effects of phosphorylation on primed T231 and unprimed S396/S404 epitopes of tau, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
protein 14-3-3 mediates phosphorylation of microtubule-associated protein tau by serum- and glucocorticoid-induced protein kinase 1 SGK1, which forms an activated ternary complex with protein 14-3-3theta
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau is primarily found in neurons, regulation of tau phosphorylation by GSK3beta via interaction with FRAT-1 and FRAT-2, i.e. frequently rearranged in advanced T-cell lymphoma proteins
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phoshorylation at residues Ser404, Ser199, Ser202 and Thr231
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation at Ser208 and Ser210
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
tau isoforms in the human central nervous system and GSK-3 phosphorylation sites. Isozymes GSK-3alpha and GSK-3beta1/2 differentially phosphorylate tau, e.g. Ser396 in tau is phosphorylated by both splice variants, whereas Ser199 is a significant target of GSK-3beta1, but not of GSK-3beta2 activity
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
activity in organisms with mutated APP and tau, not in wild-type, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
cdk5 substrate in brain, cdk5 associated with p39, tau is a microtubule-associated and developmentally regulated protein involved in axonal development in neurons, tau phosphorylation by cyclin-dependent kinase 5/p39 during brain development reduces its affinity for microtubules
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
hyperphosphorylation of tau by CDK5 is involved in apoptosis and neurodegeneration in Alzheimer's disease, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
regulation, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation by GSK-3beta is involved in development of neurodegenerative Alzheimer's disease, the tau phosphorylation activity by GSK-3beta is further increased by soluble toxic beta-amyloid oligomers, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau phosphorylation in vivo is stimulated by extracellular signal-regulated kinase Erk phosphorylation and apolipoprotein isozyme E4, to a lesser extent by isozyme apoE3, overview
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK is one of the main tau kinase phosphorylating tau at the epitopes Ser262/356 and Thr231 at basal conditions in neurons
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
recombinant human tau protein expressed in transgenic mice
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
AMPK is one of the main tau kinase phosphorylating tau at the epitopes Ser262/356 and Thr231 at basal conditions in neurons
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
abnormal hyperphosphorylation of tau by PKA and GSK-3 is associated with Alzheimer's disease and other tauopaties leading to neuronal degeneration
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
tau is microtubule-associated, phopshorylation at T231 by CDK5 causes its release into the cytoplasm
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
phosphorylation of tau at various sites
-
-
?
ATP + [tau-protein]
ADP + O-phospho-[tau-protein]
-
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
AtK-1 kinase is involved in reproduction-specific processes
-
-
?
additional information
?
-
-
glycogen synthase kinase-3beta also performs serine/threonine protein kinase reaction, EC 2.7.11.1, with other substrates than tau, e.g. it phosphorylates the glycogen synthase
-
-
?
additional information
?
-
enzyme regulates cell fate in Dictyostelium
-
-
?
additional information
?
-
-
-
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
possible role of the sgg protein in a signal transduction pathway necessary for intercellular communication at different stages of development
-
-
?
additional information
?
-
enzyme acts as a repressor of engrailed autoregulation
-
-
?
additional information
?
-
implicated in cell-fate determination and differentiation, phosphorylates several regulatory proteins that are activated by dephosphorylation in response to hormones or growth factors
-
-
?
additional information
?
-
enzyme of the lithium-sensitive wnt signaling pathway
-
-
?
additional information
?
-
enzyme forms part of the wingless signalling pathway. GSK-3beta activity is negatively regulated by phosphorylation on serine 9 and positively regulated by phosphorylation on tyrosine 216. Enzyme may also be regulated at the transcriptional level
-
-
?
additional information
?
-
-
abnormal phosphorylation of tau in dividing cells leads to its accumulation in the cytosol as microtubule-free form, Cdk5 is involved in neurodegenerative mechanisms
-
-
?
additional information
?
-
-
GSK-3 affects the tau-mRNA splicing of exon 10 via phosphorylation of the splicing factors of the serine/arginine-rich splicing factor SR family, e.g. SC35, leading to priming and dislocation of the splicing factor, aberrant tau splicing contributes to tauopathies including Alzheimer's disease, overview
-
-
?
additional information
?
-
-
GSK3beta and PKA work coordinatedly on tau phosphorylation
-
-
?
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of organisms with Alzheimer's disease leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of patients suffering from Alzheimer's disease leads to age-dependent memory deficits
-
-
?
additional information
?
-
-
phosphorylated tau is important in cytoskeleton assembly
-
-
?
additional information
?
-
-
protein 14-3-3 facilitates tau phosphorylation by SGK1 and regulates its subcellular localization in the nucleus or cytoplasm, overview
-
-
?
additional information
?
-
-
the enzyme participates in Alzheimer's disease
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain. There are GSK3 substrates with preference for GSK3beta1 over GSK3beta2, and others that hold no distinction, suggesting different modes of interaction with GSK3, overview
-
-
?
additional information
?
-
glycogen synthase kinase-3 isoforms have distinct substrate preference in the brain. There are GSK3 substrates with preference for GSK3beta1 over GSK3beta2, and others that hold no distinction, suggesting different modes of interaction with GSK3, overview
-
-
?
additional information
?
-
in addition to autophosphorylation, known phosphorylation substrates of TTBK2 include tau, tubulin, CEP164, CEP97, and TDP-43, a neurodegeneration-associated protein. The enzyme binds to CEP164, a centriolar protein, and EB1, a microtubule plus-end tracking protein
-
-
?
additional information
?
-
-
naturally occurring V717I mutation of the amyloid precursor protein APP in a CT100 fragment of mutants leads to augmented age-dependent tau phosphorylation, followed by increased activation status of mitogen-activated protein kinase family members, e.g. ERK1/2, p38, and c-Jun NH2-terminal kinase, compared to the wild-type organism, naturally occurring V337M mutation of tau protein of mutants leads to age-dependent memory deficits
-
-
?
additional information
?
-
-
rapid, reversible cold-water stress-induced hyperphosphorylation of tau S199, S202, T205, T231, and S235 in hippocampal and cerebral region of the brain, hyperphosphorylation of tau is associated to the Alzheimer's disease
-
-
?
additional information
?
-
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
?
additional information
?
-
enzyme is involved in the cellular response to insulin, the enzyme is highly phosphorylated on tyrosine and thus active in resting cells
-
-
?
additional information
?
-
implicated in the hormonal control of several regulatory proteins including glycogen synthase and the transcription factor c-jun
-
-
?
additional information
?
-
-
activation and deregulation of GSK-3, e.g. by wortmannin or GF-109203X, induces Alzheimer-like tau hyperphosphorylation in hippocampus, the hyperphosphorylated tau forms neurofibrillary tangle
-
-
?
additional information
?
-
-
CDK5-dependent clustering of endoplasmic reticulum ER and mitochondria during ceramide-mediated neuronal death: neurotoxic calcium transfer from ER to mitochondria is regulated by cyclin-dependent kinase 5-dependent phosphorylation of tau, inhibition of the process leads to cell death
-
-
?
additional information
?
-
-
tau becomes a more favorable substrate for GSK-3 when it is prephosphorylated by PKA in rat brain, inhibition of tau hyperphosphorylation inhibits an associated loss in spatial memory
-
-
?
additional information
?
-
MDS1 is not essential during normal vegetative growth but appears to be required for meiosis
-
-
?
additional information
?
-
enzyme is involved in the induction of meiosis
-
-
?
additional information
?
-
MCK1 encodes a positive regulator of meiosis and spore formation. MCK1 is required in vegetative cells for basal IME1 expression, it is also required for efficient ascus maturation. MCK1 plays a role in governing centromere function during vegetative growth as well as sporulation
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(2'Z,3'E)-6-bromoindirubin-3'-oxime
(2S)-3-cyclohexyl-2-(9H-purin-6-ylamino)propan-1-ol
ZINC00012956
(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
-
(Rp)-adenosine 3',5'-cyclic monophosphorothionate triethyl ammonium salt
-
inhibitor of PKA
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-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-methyl-6-(5-[[3-(trifluoromethyl)benzyl]sulfanyl]-1,3,4-oxadiazol-2-yl)-1H-benzimidazole
-
1-[3-(6-amino-9H-purin-9-yl)propyl]-3-methylpyridin-2(1H)-one
ZINC91332506
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-(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-(benzylsulfanyl)-5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazole
-
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-cyanoethyl alsterpaullone
-
-
2-methyl-N-(5-phenyl-1H-pyrazolo[3,4-b]pyridin-3-yl)propanamide
-
-
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-((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-(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)-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-pyrrol-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-pyrrol-3-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-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-(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-(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-(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-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-(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-(5,6-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-(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-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-(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-(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-(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-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-(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-(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-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
-
-
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
-
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-[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-[5-[((4-amino-4-methylpiperidin-1-yl)methyl]pyrrolo[2,1-f][1,2,4]triazin-4-yl]amino)-5-bromophenol
-
-
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
-
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
-
-
3alpha,5alpha-tetrahydroprogesterone
-
decreases only expression of GSK-3 beta in the cerebellum but not in the hypothalamus
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
-
TDZD-8
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
4-phenyl-1H-pyrazolo[3,4-b]pyridin-3-amine
-
-
4-[1-cyclohexyl-4-[4-fluorophenyl]-1H-imidazol-5-yl]pyrimidin-2-amine
enzyme binding structure analysis
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; 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-(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-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
-
-
5-[2-phenylpyrazolo[1,5-a]pyridin-3-yl]-1h-pyrazolo[3,4-c]pyridazin-3-amine
enzyme binding structure analysis
5alpha-dihydroprogesterone
-
decreases only expression of GSK-3 beta in the cerebellum but not in the hypothalamus
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
-
6-bromo-5-methylindirubin-3'-oxime
-
potent inhibitor
6-bromo-indirubin-3'-acetoxime
-
potent inhibitor
6-bromo-indirubin-3'-oxime
6-bromoindirubin-3'-oxim
-
-
6-bromoindirubin-3'-oxime
-
-
6-O-methyl-7-O-alpha-L-rhamnopyranosyldaidzein
-
-
7-methoxy-1-methyl-9h-betacarboline
enzyme binding structure analysis
7-O-alpha-L-rhamnopyranosyldaidzein
-
-
A-582941
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
alpha-bungarotoxin
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
AMP-PNP
-
ATP analogue adenosine 5'-(beta,gamma-imino)triphosphate
AR-A014418
-
selective ATP-competitive inhibitor of GSK3
Butyrolactone
-
cdk5 inhibitor, isoenzyme TPKII
caffeic acid
-
0.02 mg/ml caffeic acid decreases the activating phosphorylation of GSK-3beta
carteriosulfonic acid A
-
low micromolar inhibitor of GSK-3beta
carteriosulfonic acid B
-
low micromolar inhibitor of GSK-3beta
carteriosulfonic acid C
-
low micromolar inhibitor of GSK-3beta
CHIR98023
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
compound C
inhibits tau protein phosphorylation by AMPK
dantrolene
-
in the presence of dantrolene, GSK-3beta activation and tau phosphorylation are decreased
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
Insulin
-
insulin induces phosphorylation of the Ser9 residue, thereby inactivating GSK-3beta
-
insulin-like growth factor-I
-
-
-
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
methyl 2-bromo-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)benzoate
-
-
methyl 3-([[5-(2,3-dihydro-1-benzofuran-5-yl)-1,3,4-oxadiazol-2-yl]sulfanyl]methyl)benzoate
-
methyllycaconitine
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
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-[3-cyano-6-[3-[1-piperidinyl]propanoyl]-4,5,6,7-tetrahydrothieno[2,3-c]pyridin-2-yl]1-naphthalenecarboxamide
enzyme binding structure analysis
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
-
-
Nicotine
-
attenuates beta-amyloid peptide 1-42-induced activation of GSK-3beta
p25
-
p25 overexpressing mice have reduced GSK3beta activity
-
progesterone
-
decreases expression and phosphorylation of GSK-3 beta in the cerebellum but not in the hypothalamus, regulation of tau expression and phosphorylation by progesterone may contribute to the hormonal regulation of cerebellar function by the modification of neuronal cytoskeleton
Protein kinase C
-
protein kinase C inhibits GSK-3beta by phosphorylating its auto-inhibitory domain at Ser9
-
TDZD-8
-
selective GSK-3beta inhibitor, induces phosphorylation of the Ser9 residue, thereby inactivating GSK-3beta
tideglusib
irreversible inhibitor
-
trans-activating transcriptor-eIF2B
-
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)
[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
-
-
(2'Z,3'E)-6-bromoindirubin-3'-oxime
-
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
-
-
6-bromo-indirubin-3'-oxime
-
potent inhibitor
6-bromo-indirubin-3'-oxime
-
-
6-bromo-indirubin-3'-oxime
-
selective and potent GSK3beta inhibitor
ATP
-
strongly inhibited by elevated concentrations of ATP uncomplexed with magnesium
ATP
-
strongly inhibited by elevated concentrations of ATP uncomplexed with magnesium
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
-
-
GF 109203X
a benzofuranylindolylmaleimide
kenpaullone
-
-
LiCl
-
slight inhibition of T231 phosphorylation by p25-Cdk5 kinase complex
LiCl
71% inhibition at 0.01 mM
LiCl
-
complete inhibition at 2 mM
LiCl
-
a dose-dependent increase in phosphorylation of GSK-3beta occurs after treatment with LiCl (5-20 mM)
LiCl
-
pharmacological inhibition of GSK3 in old transgenic mice by chronic treatment with lithium, leads to a reduction of the age-dependent increase in tau hyperphosphorylation
LiCl
-
GSK-3-specific inhibitor
LiCl
-
lithium is a weak inhibitor of GSK3beta, lithium dose-dependently inhibits GSK3beta through the phosphorylation of serine 9 residue
lithium
-
after inhibition of GSK-3 in cortical neurons, the splicing factor SC35 is nuclearly redistributed and enriched in nuclear speckles and colocalizes with the kinase
lithium
selective inhibition of GSK-3, blocks tau hyperphosphorylation either in cultured neurons or in rat brain
lithium chloride
15 mM
Ro 31-8220
-
-
Ro 31-8220
a benzofuranylindolylmaleimide
roscovitine
-
complete inhibition of T231 phosphorylation by 25-Cdk5 kinase complex
roscovitine
-
Cdk5 inhibitor
roscovitine
-
inhibition of CDK5
SB 216763
-
GSK-3-specific inhibitor
SB-216763
-
specific inhibitor of GSK-3beta
SB-216763
-
selective ATP-competitive inhibitor of GSK3
SB-415286
-
complete inhibition at 0.005 mM
SB216763
-
SB216763
-
specific GSK-3 inhibitor
SB216763
-
potent and selective cell permeable ATP-competitive inhibitor of GSK3
staurosporine
-
-
staurosporine
a benzofuranylindolylmaleimide
trans-activating transcriptor-eIF2B
-
acts as a competitive inhibitor of GSK-3
-
trans-activating transcriptor-eIF2B
-
acts as a competitive inhibitor of GSK-3
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme
-
additional information
-
no inhibition of the p25-Cdk5 kinase complex by PD98059 and SB203580
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme
-
additional information
-
inhibition of GSK3 activity results in c-MYC activation, leading to the induction of Bax, Bim, DR4/DR5, and tumor necrosis factor-related apoptosis-inducing ligand expression and subsequent cytotoxicity. inhibition of GSK3 activity causes a dramatic decrease in intracellular nuclear factor-kappaB activity. Inhibition of GSK3 activity results in c-MYC-dependent glioma cell death through multiple mechanisms, all of which converge on the apoptotic pathways
-
additional information
not inhibited by 2-(2,3-dihydro-1-benzofuran-5-yl)-5-[(3-fluorobenzyl)oxy]-1,3,4-oxadiazole
-
additional information
-
galectin-3 regulates GSK-3beta activity/phosphorylation via the PI3K/AKT pathway
-
additional information
-
treatment with 1 CFU/cell bacillus Calmette-Guerin increases the phosphorylation of GSK3beta at serine 9 and therefore inhibits the activity to about 40% 1 h after stimulation
-
additional information
-
the crude organic extract of fermentation cultures of Streptomyces sp. strain H7667 inhibits growth of a yeast transformant (with cloned human GSK-3beta) at 37°C, but shows no inhibition at 25°C
-
additional information
design, synthesis, and evaluation of 3-aryl-4-pyrrolyl-maleimides as glycogen synthase kinase-3beta inhibitors. Compounds 3-(1-(3-morpholinopropyl)-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-(6-fluoro-1-(3-morpholinopropyl)-1H-indol-3-yl)-4-(1Hpyrrol-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, and 3-(1-methyl-1H-indol-3-yl)-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione significantly reduce amyloidbeta-induced Tau hyperphosphorylation, showing the inhibition of GSK-3beta at the cellular level. Structure-activity relationships, in silico molecular modeling study, overview
-
additional information
inhibitor development using seven different scaffolds, scaffold 3-aminopyrrolidine exhibits high preferential affinity with GSK3beta. Interaction analysis of inhibitor scaffolds with different protein kinases, overview
-
additional information
-
inhibitor development using seven different scaffolds, scaffold 3-aminopyrrolidine exhibits high preferential affinity with GSK3beta. Interaction analysis of inhibitor scaffolds with different protein kinases, overview
-
additional information
activation of EphB2 receptor kinase arrests tau hyperphosphorylation through PI3K-/Akt-mediated GSK-3beta inhibition. EphrinB1/Fc treatment induces tyrosine phosphorylation (activation) of EphB2, while deletion of the tyrosine kinase domain (VM) of EphB2 eliminates the receptor stimulation-induced GSK-3beta inhibition and tau dephosphorylation
-
additional information
-
activation of EphB2 receptor kinase arrests tau hyperphosphorylation through PI3K-/Akt-mediated GSK-3beta inhibition. EphrinB1/Fc treatment induces tyrosine phosphorylation (activation) of EphB2, while deletion of the tyrosine kinase domain (VM) of EphB2 eliminates the receptor stimulation-induced GSK-3beta inhibition and tau dephosphorylation
-
additional information
-
not inhibited by indirubin, indirubin-3'-oxime, 5-bromo-indirubin, 5-aminoindirubin-3'-oxime, 6-bromo-indirubin, 6-bromo-N-methyl-indirubin-3'-oxime, 6-bromo-N-methyl-indirubin-3'-acetoxime, 6-bromo-indirubin-3'diethyl phosphatoxime, indirubin-3'-methoxime, 6-bromo-5-nitroindirubin, 6-bromo-5-nitroindirubin-3'-oxime, and 6-bromo-5-methylindirubin
-
additional information
-
inactivating phosphorylation of Ser9 of TPKI/GSK3beta in close correspondence with tau phosphorylation
-
additional information
-
Cdk5 over-activation leads to inhibition of GSK3 in young transgenic mice, in old transgenic animals the inhibition of GSK3 is lost
-
additional information
-
N-terminus negatively regulates tau phosphorlyation by blocking GSK3beta access, local conformational change induced by T231 phosphorylation is required for the phosphorylation of the C-terminus and hyperphosphorylation of tau
-
additional information
-
cdk5 can negatively regulate GSK3beta activity through neuregulin/ErbB signaling, phosphorylation at the inhibitory GSK3beta-Ser9 site activates GSK3beta
-
additional information
-
the 3-nitropropionic acid treatment induces GSK-3beta truncation, calpeptin prevents GSK-3beta cleavage and cell death induced by 3-nitropropionic acid
-
additional information
stimulation of EphB2 upregulates PI3K and Akt causing inhibition of GSK-3beta
-
additional information
-
stimulation of EphB2 upregulates PI3K and Akt causing inhibition of GSK-3beta
-
additional information
-
protein tau-associated novel protein kinase Cepsilon suppresses the GSK-3beta-mediated phosphorylation of protein tau through the phosphorylation of GSK-3beta by the kinase in vitro
-
additional information
-
desacyl-carteriosulfonic acid shows no GSK-3beta inhibitory activity at concentrations up to 0.05 mM
-
additional information
-
phosphorylation of GSK3beta at S9 inhibits the enzyme, the phosphorylation at Ser9 is inhibited by wortmannin or GF-109203X, this inhibition is eliminated by inhibition of GSK-3 by a different inhibitor
-
additional information
GSK-3 is inactivated by phosphorylation of serine 9 in GSK-3beta and serine 21 in GSK-3alpha subunits by mainly Akt. Hyperglycemia induces strong activity of GSK-3 in rat brain
-
additional information
-
Galphaq protein inhibits GSK-3beta via activation of protein kinase C
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
0.00281
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
-
-
0.0000094
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
0.000021
2-(3-ethylpiperazin-1-yl)-N-[6-(3-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]acetamide
Homo sapiens
-
-
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
0.000143
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
-
-
0.000094
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
0.00012
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
-
-
0.00645
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
0.07334
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
-
-
0.00021
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
0.00055
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
-
-
0.00129
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
0.01245
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
-
-
0.00015
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
0.00179
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
-
-
0.00053
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
0.0009
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
-
-
0.00204
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
0.0306
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
-
-
0.000314
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
-
0.00014
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
-
-
0.00055
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
-
0.00048
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
-
-
0.00057
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
-
0.00095
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
-
-
0.00101
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
-
0.00031
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
-
-
0.00016
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
0.000014
3-benzyl-N-[5-bromo-6-(furan-2-yl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrrolidine-1-carboxamide
Homo sapiens
-
-
0.00424
3-phenyl-4-(1H-pyrrol-3-yl)-1H-pyrrole-2,5-dione
Homo sapiens
pH and temperature not specified in the publication
0.00059
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
-
-
0.0000023
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
-
0.001398
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
-
-
0.00013
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
0.00043
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
-
-
0.0019
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
0.0000095
BIIB-TTBKi-284
Mus musculus
isoform TTBK1, pH and temperature not specified in the publication
-
0.0125
carteriosulfonic acid A
Oryctolagus cuniculus
-
at 37°C
0.0068
carteriosulfonic acid B
Oryctolagus cuniculus
-
at 37°C
0.0068
carteriosulfonic acid C
Oryctolagus cuniculus
-
at 37°C
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
0.002343
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
-
-
0.0032
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
0.000007
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
-
-
0.000034
SB216763
Rattus norvegicus
-
-
0.000028 - 0.0002
staurosporine
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
0.000125
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
Homo sapiens
-
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
Homo sapiens
-
0.000738
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
Homo sapiens
isoform TTBK1, pH and temperature not specified in the publication
-
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
Homo sapiens
isoform TTBK1, pH and temperature not specified in the publication
-
0.000028
staurosporine
Homo sapiens
pH and temperature not specified in the publication
0.0002
staurosporine
Homo sapiens
-
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
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
evolution
sequence comparisons of diverse protein kinases, phylogenetic tree of tau protein kinases and analysis
evolution
TTBK2 is a serine/threonine protein kinase of the CK1 superfamily
evolution
TTBK2 is a serine/threonine protein kinase of the CK1 superfamily
malfunction
-
chronic inhibition of GSK-3 enhances glycolysis
malfunction
-
GSK-3beta heterozygote mice, which express GSK-3beta at 50% wild type levels, have impaired memory reconsolidation but normal memory consolidation
malfunction
-
inactivation of glycogen synthase kinase-3beta suppresses mitochondrial permeability transition pore opening and protects cardiomyocytes
malfunction
-
inhibition of glycogen synthase kinase-3 increases beta-catenin concentration in the cytoplasm
malfunction
-
inhibition of GSK-3beta abolishes Abeta-induced spine alterations
malfunction
-
inhibition of GSK-3beta abrogates glucocorticoid-induced bone loss by increasing beta-catenin- and Runx2-mediated osteoblast differentiation
malfunction
-
inhibition of GSK-3beta mediates Nrf2 activation by the M1 receptor
malfunction
abnormal tau phosphorylation (p-tau) occurs after hypoxic damage to the brain associated with traumatic brain injury and stroke
malfunction
AMPK inhibition leads to a rapid decrease of tau phosphorylation. AMP-activated protein kinase (AMPK) is deregulated in the Alzheimer's disease brain where it co-localized with phosphorylated tau in pre-tangle and tangle bearing neurons. AMPK mice deficient for one of the catalytic alpha subunits display reduced endogenous tau phosphorylation. AMPK deficiency reduces tau pathology in the PS19 mouse model of tauopathy
malfunction
comparison of phosphorylation sites in human Alzheimer and control brain with recombinant tau phosphorylated by GSK-3 in vitro, several sites are not phosphrylated in Alzheimer's disease samples, overview. Inhibiting GSK-3 with SB-415286 also protects cultured neurons from cell death induced by reduced phosphatidylinositol 3-kinase activity, and this protection is paralleled by decreased tau phosphorylation
malfunction
deletion of the C-terminus alphaDELTACT-4 leads to loss of nearly all activity of the GSK-3 isoform and abolishes suppression of Wnt signaling, GSK-3 C-terminal deletions mutants fail to interact with axin GID
malfunction
deletion of the C-terminus betaDELTACT-4 leads to loss of nearly all activity of the GSK-3 isoform and abolishes suppression of Wnt signaling, GSK-3 C-terminal deletions mutants fail to interact with axin GID
malfunction
functional status of glycogen synthase kinase-3 and correlated appearance of distinct tau phospho-epitopes: neurons displaying increases in activation of phosphorylation of glycogen synthase kinase-3alpha/beta at tyrosine 279/216 also show an intense rather than moderate AT8 (phospho-Ser202/Thr205 tau) immunoreactivity, and immunoreactivity for AT100 (phospho-Ser212/Thr214 tau) and phosphorylated Ser422, phospho-epitopes associated with fibrillar tau pathology. These neurons are rare in 8.5-month-old, but numerous in 18.5- and 28-month-old pR5 mice. Tau- rather than an amyloid-beta peptide-induced pathology is associated with increased neuronal tyrosine phosphorylation. Tyrosine phosphorylation only increases in neurons with fibrillar tau pathology
malfunction
knockout TTBK2fmly1/fmly1 mice with homozygous mutants of truncated TTBK2 at residue 450 are embryonic lethal at embryonic day 10, with indistinct brain subdivisions, distorted caudal bodies, and delayed body and brain development. Heterozygous mutant TTBK2fmly1/+ mice are completely normal and exhibit a regular lifespan
malfunction
mutations of TTBK2 are associated with spinocerebellar ataxia type 11. Mutation of TTBK2 may potentially be more serious than mutations of other proteins involved in ciliopathies. Upregulated TTBK2 in kidney carcinoma and melanoma cell lines is correlated with resistance of the target therapeutic drug Sunitinib, while knockdown of TTBK2 in these cells increases Sunitinib sensitivity. Reduction of TTBK2 also increases Sunitinib inhibition of cancer cell migration. The enzyme phosphorylates transactive response (TAR) DNA-binding protein 43, or TDP-43, a DNA/RNA binding protein responsible for transcriptional repression, pre-mRNA splicing, and translational regulation. Hyperphosphorylation-associated aggregation of TDP-43 is a signature of two neurodegenerative diseases: amyotrophic sclerosis (ALS) and frontotemporal lobar degeneration (FTLD-TDP). Phosphorylation of TDP-43 by both TTBK1 and TTBK2 overexpression results in relocalization of TDP-43 from the nucleus to the cytosol. TTBK1/TTBK2 colocalize with phospho-TDP-43 in the frontal cortex of FTLD-TDP patients and in the spinal cord of ALS patients, suggesting that phosphorylation of TDP-43 by both TTBK1 and TTBK2 likely plays a role in progression of these diseases
malfunction
phosphorylation of CRMP2, CRMP4, beta-catenin, c-Myc, c-Jun and some residues on tau associated with Alzheimer's disease, is altered in cortical tissue lacking both isoforms of GSK3
malfunction
Stimulation of EphB2 attenuates tau phosphorylation through PI3K/Akt-mediated inactivation of glycogen synthase kinase-3beta
malfunction
Stimulation of EphB2 attenuates tau phosphorylation through PI3K/Akt-mediated inactivation of glycogen synthase kinase-3beta
malfunction
tau-tubulin kinase 1 enhances prefibrillar tau aggregation, forming small oligomers, and motor neuron degeneration in P301L FTDP-17 tau-mutant mice. TTBK1 up-regulation enhances tau phosphorylation and oligomerization, whose toxicity results in enhanced neurodegeneration and locomotor dysfunction in a tauopathy animal model, overview. The bigenic mice show enhanced tau phosphorylation at multiple sites, i.e. AT8, 12E8, PHF-1, and pS422, and they show significant locomotor dysfunction as determined by both rotorod and grip strength tests, as well as enhanced loss of motor neurons in the L4-L5 spinal cord. The neuronal dysfunction and degeneration is associated with increased levels of tau oligomers, cyclin-dependent protein kinase 5 activators p35 and p25, and pY216 phosphorylated glycogen synthase kinase 3-beta
malfunction
the abnormal phosphorylation of tau leads to the formation of neurofibrillary tangles produced by the action of tau kinases, resulting in the loss of neurons and synapse, leading to dementia
malfunction
the deletion of the C-terminal tail of slicing variant GSK-3beta2 results in considerable reduction of tau phosphorylation activity as compared with GSK-3beta1
malfunction
-
disrupting expression of isoform TTBK-d results in loss of spermatozoa, but not spermatids. In the soma, isoform TTBK-d RNAi impairs the function of multiciliated epidermal cells in propelling planarian movement, as well as the osmoregulatory function of protonephridia. Decreased density and structural defects of motile cilia are observed in the epidermis
malfunction
inhibition of tau tubulin kinase 2 may lead to the movement disorder spinocerebellar ataxia type 11
malfunction
-
abnormal tau phosphorylation (p-tau) occurs after hypoxic damage to the brain associated with traumatic brain injury and stroke
-
malfunction
-
functional status of glycogen synthase kinase-3 and correlated appearance of distinct tau phospho-epitopes: neurons displaying increases in activation of phosphorylation of glycogen synthase kinase-3alpha/beta at tyrosine 279/216 also show an intense rather than moderate AT8 (phospho-Ser202/Thr205 tau) immunoreactivity, and immunoreactivity for AT100 (phospho-Ser212/Thr214 tau) and phosphorylated Ser422, phospho-epitopes associated with fibrillar tau pathology. These neurons are rare in 8.5-month-old, but numerous in 18.5- and 28-month-old pR5 mice. Tau- rather than an amyloid-beta peptide-induced pathology is associated with increased neuronal tyrosine phosphorylation. Tyrosine phosphorylation only increases in neurons with fibrillar tau pathology
-
malfunction
-
AMPK inhibition leads to a rapid decrease of tau phosphorylation. AMP-activated protein kinase (AMPK) is deregulated in the Alzheimer's disease brain where it co-localized with phosphorylated tau in pre-tangle and tangle bearing neurons. AMPK mice deficient for one of the catalytic alpha subunits display reduced endogenous tau phosphorylation. AMPK deficiency reduces tau pathology in the PS19 mouse model of tauopathy
-
physiological function
-
activation of GSK-3beta results in the inhibition of the Wnt signaling pathway
physiological function
-
cisplatin-induced cytotoxicity may be associated with modulation of GSK-3 activation
physiological function
-
glycogen synthase kinase-3 regulates the phosphorylation of severe acute respiratory syndrome coronavirus nucleocapsid protein and viral replication
physiological function
-
GSK-3 activity is required for tau filaments to inhibit kinesin-dependent FAT
physiological function
-
GSK-3 is necessary and sufficient for cardiomyocyte differentiation in mesenchymal stem cells, GSK-3beta in the cytosol induces cardiomyocyte differentiation of mesenchymal stem cells through down-regulation of beta-catenin. In contrast, GSK-3alpha in the nucleus inhibits cardiomyocyte differentiation through down-regulation of c-Jun
physiological function
-
GSK-3-regulated signal transduction pathways are important for stem cell maintenance and may be involved in events controlling cell differentiation
physiological function
-
GSK-3beta activation is required for memory reconsolidation in the adult brain
physiological function
-
GSK-3beta is a critical mediator of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine/1-methyl-4-phenylpyridinium iodide-induced neurotoxicity through its ability to regulate mitochondrial functions
physiological function
-
GSK-3beta is a multifunctional Ser/Thr kinase that plays important roles in necrosis and apoptosis of cardiomyocytes
physiological function
-
GSK3 negatively regulates mycobacteria-induced interleukin-10 production in human monocytes
physiological function
-
GSK3beta regulates both tau phosphorylation and total tau levels through protein phosphatase-2A
physiological function
-
increased GSK-3 correlates with increased cell death, GSK-3 plays a very important role in L-DOPA neurotoxicity, as well as in neurodegeneration
physiological function
-
mitochondrial hexokinase II is a promoter of neuronal survival under the regulation of GSK-3
physiological function
-
protein tau phosphorylation plays an essential role in adult hippocampal neurogenesis and GSK-3 facilitates neurogenesis only in the presence of tau proteins, tau hyperphosphorylation induced by activating GSK-3 promotes neurogenesis
physiological function
-
the GSK-3beta-mediated high phosphorylation of protein tau induces synapse loss and neuronal death
physiological function
-
the neuron-specific isoform GSK-3beta2 is required for axon growth by phosphorylating microtubule-associated proteins including protein tau
physiological function
AMP-activated protein kinase modulates tau phosphorylation and tau pathology in vivo. Tau functions, which include the regulation of microtubules dynamics, are dependent on its phosphorylation status, any changes in tau phosphorylation can have major impacts on synaptic plasticity and memory. Endogenous AMPK activation in mouse primary neurons induces an increase of tau at multiple sites. AMPK regulates tau phosphorylation in mouse primary neurons as well as in vivo, and thus suggest that AMPK could be a key player in the development of Alzheimer's disease pathology. The two alpha subunits of AMPK can have distinct roles. AMPKalpha2, which is the most highly expressed of the catalytic subunit in the brain, is responsible for the detrimental effects observed following ischemic stroke in mice. AMPK activation increases tau phosphorylation in primary neurons and affects tau binding to microtubules. AMPK controls basal tau phosphorylation levels
physiological function
glycogen synthase kinase-3 (GSK-3) isoforms, GSK-3alpha and GSK-3beta, are serine/threonine kinases involved in numerous cellular processes and diverse diseases, including Alzheimer disease, cancer, and diabetes. GSK-3 isoforms function redundantly in some settings, while, in others, they exhibit distinct activities. In the canonical Wnt signaling pathway, GSK-3 phosphorylation of beta-catenin is regulated via interactions with the scaffold protein axin
physiological function
glycogen synthase kinase-3 (GSK-3beta) and protein phosphatase 2A (PP2A) are thought to control the levels of tau phosphorylation. No alteration in the activities of GSK-3beta and PP2A during episodes of ischaemia of up to 8 min and reperfusion of up to 2 h, and 4 weeks recovery. Tau dephosphorylation following ischaemia is not dependent on GSK-3beta or PP2A activity, but is associated with AMPK dephosphorylation
physiological function
glycogen synthase kinase-3 plays an important role in the pathogenesis of Diabetes mellitus and Alzheimer's disease. Diabetic rats display an increased GSK-3 activity, and decreased activity and expression of Akt. And Abeta40 and Abeta42 are overproduced and the microtubule-associated protein tau is hyperphosphorylated in the hippocampus. Selective inhibition of GSK-3 attenuates the conditions of Abeta overproduction and tau hyperphosphorylation. GSK-3 regulates both the production of Amyloidbeta and the phosphorylation of tau in rat brain and may therefore contribute to Diabetes mellitus caused Alzheimer disease-like neurological defects. Hyperglycemia induces strong activity of GSK-3 and lowers activity of Akt in rat brain. The production of Abeta40 and Abeta42 is increased significantly while activation of GSK-3 and inhibition of Akt are induced in Diabetes mellitus
physiological function
glycogen synthase kinase-3beta (GSK-3beta) is a serine/threonine kinase that phosphorylate protein substrates involved in Alzheimer's disease (AD), such as microtubule-associated protein tau and amyloid precursor protein (APP). Splicing variant GSK-3beta2 has lower phosphorylation activity to tau at Alzheimer disease-relevant epitope Ser396 than GSK-3b 1 in cells, whereas the two variants exhibit equivalent levels of phosphorylation activities to amyloid precursor protein. Tau is an unfavorable substrate of GSK-3beta2. Changes in the balance of GSK-3beta2/-3beta1 in neurons underlie tau hyperphosphorylation in Alzheimer's disease. The intracellular domain Thr668 of APP is phosphorylated by GSK-3beta, the phosphorylation regulates APP function and metabolism
physiological function
in the canonical Wnt signaling pathway, GSK-3 phosphorylation of beta-catenin is regulated via interactions with the scaffold protein axin. Glycogen synthase kinase-3 (GSK-3) isoforms, GSK-3alpha and GSK-3beta, are serine/threonine kinases involved in numerous cellular processes and diverse diseases, including Alzheimer disease, cancer, and diabetes. GSK-3 isoforms function redundantly in some settings, while, in others, they exhibit distinct activities. In the canonical Wnt signaling pathway, GSK-3 phosphorylation of beta-catenin is regulated via interactions with the scaffold protein axin
physiological function
role for TTBK1 in pre-tangle formation prior to the formation of fibrillar tau. Tau is phosphorylated at Ser422 at an early/intermediate stage in neurofibrillary tangle formation
physiological function
stimulation of GSK-3beta both in vitro and in vivo induces tau hyperphosphorylation with impairments of the cognitive functions, whereas inhibition of GSK-3beta improves tau pathologies and memory deficits. Activation of EphB2 receptor kinase arrests tau hyperphosphorylation through PI3K-/Akt-mediated GSK-3beta inhibition. Activation of GSK-3beta inhibits long-term potentiation and impairs synaptic function
physiological function
stimulation of GSK-3beta both in vitro and in vivo induces tau hyperphosphorylation with impairments of the cognitive functions, whereas inhibition of GSK-3beta improves tau pathologies and memory deficits. Stimulation of EphB2 upregulates PI3K and Akt with inhibition of GSK-3beta. Stimulation of EphB2 attenuates tau phosphorylation both in vitro and in hippocampus of human tau transgenic mice
physiological function
tau is primarily a neuronal microtubule-associated protein that has functions related to the stabilisation of microtubules. Phosphorylation of tau is usually a very rapid and reversible process, which is mediated by the opposing actions of several protein kinases and phosphatases. Tau phosphorylation is increased during embryonic development, and in neurodegenerative conditions. Phosphorylation of tau is an important dynamic and regulatory element involved in the binding of tau to tubulin, ole for GSK-3 activity on physiological tau function and on tau dysfunction in neurodegenerative disease, glycogen synthase kinase-3 activity and tau function in normal and diseased brain, detailed overview. In neurons, the primary location of tau is in axons, where it is presumed to act as a stabilising protein for the microtubule cytoskeleton. Tau has an important function in maintaining microtubule dynamic instability, through dual processes that result in the lengthening and shortening of microtubules in response to external signals. Increased tau phosphorylation leads to its detachment from tubulin, thereby, enhancing microtubule disassembly and reducing microtubule stability. Highly phosphorylated forms of tau bind less well to microtubules, resulting in a loss of the microtubule-stabilising properties of tau and ultimately the collapse of the neuronal cytoskeleton. Tau phosphorylation also influences the positioning of tau in dendrites, and the association of tau with plasma membranes and nuclei. Elevated phosphorylation results in the relocalisation of tau fromaxons into the somatodendritic region of neurons. 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. The phosphorylation of tau by GSK-3 reduces the ability of tau to promote microtubule assembly in vitro and in cells. Priming of tau for GSK-3 phosphorylation is frequently provided by the activity of PKA, CK1, or CK2 on unphosphorylated substrates, although other kinases, such as members of the mitogen-activated protein kinase family, or cdk5, can also initiate priming on some GSK-3 substrates. GSK-3 remains a principal candidate kinase for both physiological and pathological tau phosphorylation, overview. GSK-3 in cells is important for the maintenance of healthy functional neurons, and changes in tau phosphorylation are likely be indicative of reduced neuronal viability
physiological function
the enzyme phosphhorylates some residues on tau associated with Alzheimer's disease
physiological function
the enzyme phosphhorylates some residues on tau associated with Alzheimer's disease, phosphorylation of the microtubule associated protein tau. Inhibitor-2 phosphorylation is differentially regulated by GSK3beta1 and GSK3beta2, overview
physiological function
-
the pathogenesis of Alzheimer's disease includes hyperphosphorylation of tau protein which results in the self-assembly of tangles of paired helical fragments and straight filaments. Defective tau protein causes the dementia leading to Alzheimer's disease
physiological function
TTBK2 is a multifunctional kinase. TTBK2 is essential for regulating the growth of axonemal microtubules in ciliogenesis. It also plays roles in resistance of cancer target therapies and in regulating glucose and GABA transport. The enzyme binds to CEP164, a centriolar protein, and EB1, a microtubule plus-end tracking protein. The TTBK2 pathway may be independent of the biogenesis of the ciliary transition zone. TTBK2 can also bind to EB1 through its SxIP motifs, where EB1 is a microtubule plus-end tracking protein required for ciliogenesis
physiological function
TTBK2 is a multifunctional kinase. TTBK2 is essential for regulating the growth of axonemal microtubules in ciliogenesis. It also plays roles in resistance of cancer target therapies and in regulating glucose and GABA transport. The enzyme binds to CEP164, a centriolar protein, and EB1, a microtubule plus-end tracking protein. The TTBK2 pathway may be independent of the biogenesis of the ciliary transition zone. TTBK2 can also bind to EB1 through its SxIP motifs, where EB1 is a microtubule plus-end tracking protein required for ciliogenesis
physiological function
-
ERK2 dysregulation in Alzheimer's disease can lead to abnormal phosphorylation of Tau resulting in the pathology of the disease
physiological function
-
isoform TTBK-d is specifically required in postmeiotic regulation of spermatogenesis. Isoform TTBK-d is required for the structural integrity of planarian motile cilia and protonephridial units
physiological function
over-expression the enzyme and tau-protein provokes an imbalance in cholinergic activity with a decrease in the neurotransmitter acetylcholine in the cell. An increased phosphorylation of tau by the kinase GSK3beta can modulate the levels of the cholinergic acetylcholinesterase. These changes may consequently compromise cholinergic neurotransmission
physiological function
phosphorylation of isoform TTBK1 is linked to neurodegenerative diseases like Alzheimer's disease, amyotrophic lateral sclerosis, and spinocerebellar ataxia type 11
physiological function
tau tubulin kinase 2 is a key player in the cilium assembly pathway, controlling the final step of cilia initiation
physiological function
tau-tubulin kinase 1 reduces the neurite length of primary cultured neurons in Rho kinase-dependent manner in vitro
physiological function
-
the tau-kinases MARK1, TTBK1, TTBK2 reduce lifespan of Drosophila melanogaster, and the effects are increased by co expression with human tau-protein
physiological function
-
glycogen synthase kinase-3 (GSK-3beta) and protein phosphatase 2A (PP2A) are thought to control the levels of tau phosphorylation. No alteration in the activities of GSK-3beta and PP2A during episodes of ischaemia of up to 8 min and reperfusion of up to 2 h, and 4 weeks recovery. Tau dephosphorylation following ischaemia is not dependent on GSK-3beta or PP2A activity, but is associated with AMPK dephosphorylation
-
physiological function
-
AMP-activated protein kinase modulates tau phosphorylation and tau pathology in vivo. Tau functions, which include the regulation of microtubules dynamics, are dependent on its phosphorylation status, any changes in tau phosphorylation can have major impacts on synaptic plasticity and memory. Endogenous AMPK activation in mouse primary neurons induces an increase of tau at multiple sites. AMPK regulates tau phosphorylation in mouse primary neurons as well as in vivo, and thus suggest that AMPK could be a key player in the development of Alzheimer's disease pathology. The two alpha subunits of AMPK can have distinct roles. AMPKalpha2, which is the most highly expressed of the catalytic subunit in the brain, is responsible for the detrimental effects observed following ischemic stroke in mice. AMPK activation increases tau phosphorylation in primary neurons and affects tau binding to microtubules. AMPK controls basal tau phosphorylation levels
-
additional information
amino acids 345367 of GSK-3beta are essential for enzyme activity with tau protein, structure-function analysis of GSK-3alpha and GSK-3beta in mammalian cells
additional information
amino acids 345367 of GSK-3beta are essential for enzyme activity with tau protein, structure-function analysis of GSK-3alpha and GSK-3beta in mammalian cells
additional information
amino acids 417-430 of GSK-3alpha are essential for enzyme activity with tau protein, structure-function analysis of GSK-3alpha and GSK-3beta in mammalian cells
additional information
amino acids 417-430 of GSK-3alpha are essential for enzyme activity with tau protein, structure-function analysis of GSK-3alpha and GSK-3beta in mammalian cells
additional information
compared to GSK3beta1, the GSK3b2 isoform contains a 13 amino acid insert, which lies within the catalytic domain (between residues 303 and 304 of GSK3beta1), in a linker region flanked by a-helices (between domain X and XI)
additional information
compared to GSK3beta1, the GSK3b2 isoform contains a 13 amino acid insert, which lies within the catalytic domain (between residues 303 and 304 of GSK3beta1), in a linker region flanked by a-helices (between domain X and XI)
additional information
glycogen synthase kinase-3beta2 has lower phosphorylation activity to tau than glycogen synthase kinase-3beta1. The lower tau phosphorylation activity of GSK-3beta2 is due to the weak interaction of its C-terminal tail with tau
additional information
-
homology modeling, simulation and docking studies with L-glutamic acid, memantine, tacrine, and ropinirol ligands, of Tau-protein kinase, overview
additional information
isozymes GSK-3alpha and GSK-3beta share many substrates and appear to be able to compensate partially for each other, although they also appear to have distinct functions
additional information
structure and sequence analysis of TTBK2, potential homologues of the TTBK2 noncatalytic region, detailed overview
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.