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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)
| Member | Definition | Class |
|---|---|---|
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | A 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 98014 | A 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)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (5.56) | 29.6817 |
| 2010's | 9 (50.00) | 24.3611 |
| 2020's | 8 (44.44) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (4.76%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 20 (95.24%) | 84.16% |
Protein Targets (24)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.5338 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 6.8074 | 1 | 3 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 4.2722 | 1 | 3 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 3.4067 | 3 | 3 |
| G | Vesicular stomatitis virus | Potency | 8.5338 | 1 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.5338 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.5338 | 1 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 12.2577 | 2 | 5 |
| PPM1D protein | Homo sapiens (human) | Potency | 14.7403 | 1 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Angiopoietin-1 receptor | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Casein kinase I isoform epsilon | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | IC50 | 0.0070 | 1 | 1 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | IC50 | 0.0101 | 3 | 4 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | Ki | 0.0310 | 1 | 1 |
| Insulin receptor | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Insulin-like growth factor 1 receptor | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| LIM domain kinase 1 | Homo sapiens (human) | IC50 | 10.0000 | 4 | 4 |
| LIM domain kinase 2 | Homo sapiens (human) | IC50 | 10.0000 | 4 | 4 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |