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tau aggregation inhibitor

A chemical that inhibits the aggregation of the tau protein (HGNC:MAPT) and its distinct morphological forms (e.g. paired helical fragments (PHFs), straight filaments (SFs), oligomers, or larger aggregates).

ChEBI ID: 142738

Members (2)

MemberDefinitionClass
2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrileA member of the class of hydroxyindoles that is 1H-indole substituted by hydroxy, 5-(morpholin-4-ylmethyl)pyridin-2-yl, and cyano groups at positions 2, 3 and 5, respectively. It is a potent, brain permeable inhibitor of human GSK3alpha and GSK3beta with Ki of 6.9 nM and 31 nM, respectively. The drug was being developed by AstraZeneca for the treatment of Alzheimer's disease (clinical trial now discontinued).AZD1080
chir 98014A member of the class of aminopyrimidines that is pyrimidine substituted by {2-[(6-amino-5-nitropyridin-2-yl)amino]ethyl}amino, 2,4-dichlorophenyl, and 1H-imidazol-1-yl groups at positions 2, 4 and 5, respectively. It is a potent ATP-competitive inhibitor of GSK3alpha and GSK3beta (IC50 values of 0.65 and 0.58 nM, respectively).CHIR-98014

Research

Studies (18)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (5.56)29.6817
2010's9 (50.00)24.3611
2020's8 (44.44)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1 (4.76%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other20 (95.24%)84.16%

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
cytochrome P450 2C9, partialHomo sapiens (human)Potency8.533812
cytochrome P450 2D6Homo sapiens (human)Potency6.807413
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency4.272213
EWS/FLI fusion proteinHomo sapiens (human)Potency3.406733
GVesicular stomatitis virusPotency8.533812
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency8.533812
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency8.533814
Interferon betaHomo sapiens (human)Potency12.257725
PPM1D proteinHomo sapiens (human)Potency14.740312

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiopoietin-1 receptorHomo sapiens (human)IC505.000011
Casein kinase I isoform epsilonHomo sapiens (human)IC505.000011
Cyclin-dependent kinase 1Homo sapiens (human)IC504.000011
Fibroblast growth factor receptor 1Homo sapiens (human)IC501.000011
Glycogen synthase kinase-3 alphaHomo sapiens (human)IC500.007011
Glycogen synthase kinase-3 betaHomo sapiens (human)IC500.010134
Glycogen synthase kinase-3 betaHomo sapiens (human)Ki0.031011
Insulin receptorHomo sapiens (human)IC502.000011
Insulin-like growth factor 1 receptorHomo sapiens (human)IC502.000011
LIM domain kinase 1Homo sapiens (human)IC5010.000044
LIM domain kinase 2Homo sapiens (human)IC5010.000044
Mitogen-activated protein kinase 1Homo sapiens (human)IC5010.000011
RAC-alpha serine/threonine-protein kinaseHomo sapiens (human)IC505.000011
Serine/threonine-protein kinase Chk1Homo sapiens (human)IC5010.000011
Vascular endothelial growth factor receptor 1 Homo sapiens (human)IC505.000011
Vascular endothelial growth factor receptor 2Homo sapiens (human)IC502.000011