An EC 2.1.1.* (methyltransferases) inhibitor that interferes with the action of Enhancer of zeste homolog 2 (EZH2), a histone-lysine N-methyltransferase (EC 2.1.1.43).
ChEBI ID: 167694
| Member | Definition | Class |
|---|---|---|
| gsk343 | A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM). | GSK343 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 28 (65.12) | 24.3611 |
| 2020's | 15 (34.88) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (4.65%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 41 (95.35%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 13.4504 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 23.9185 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 5.3547 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 13.4504 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 13.4504 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 13.4504 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 25.4206 | 2 | 4 |
| PPM1D protein | Homo sapiens (human) | Potency | 29.4107 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| DNA (cytosine-5)-methyltransferase 1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| DNA (cytosine-5)-methyltransferase 3A | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| DNA (cytosine-5)-methyltransferase 3B | Mus musculus (house mouse) | IC50 | 100.0000 | 1 | 1 |
| Histone-arginine methyltransferase CARM1 | Homo sapiens (human) | IC50 | 128.0000 | 1 | 1 |
| Histone-binding protein RBBP4 | Homo sapiens (human) | IC50 | 0.1220 | 2 | 2 |
| Histone-binding protein RBBP4 | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| Histone-binding protein RBBP7 | Homo sapiens (human) | IC50 | 0.0040 | 1 | 1 |
| Histone-binding protein RBBP7 | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| Histone-lysine N-methyltransferase 2A | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase 2B | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase 2C | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase 2D | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase EHMT2 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase EZH1 | Homo sapiens (human) | IC50 | 0.2400 | 2 | 2 |
| Histone-lysine N-methyltransferase EZH2 | Homo sapiens (human) | IC50 | 1.0255 | 6 | 6 |
| Histone-lysine N-methyltransferase EZH2 | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| Histone-lysine N-methyltransferase SETD7 | Homo sapiens (human) | IC50 | 63.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase SETMAR | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase SUV39H1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase SUV39H2 | Homo sapiens (human) | IC50 | 123.0000 | 1 | 1 |
| Histone-lysine N-methyltransferase, H3 lysine-79 specific | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Polycomb protein EED | Homo sapiens (human) | IC50 | 0.1220 | 2 | 2 |
| Polycomb protein EED | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| Polycomb protein SUZ12 | Homo sapiens (human) | IC50 | 0.1220 | 2 | 2 |
| Polycomb protein SUZ12 | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| Protein arginine N-methyltransferase 1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Protein arginine N-methyltransferase 3 | Homo sapiens (human) | IC50 | 74.0000 | 1 | 1 |
| Protein arginine N-methyltransferase 5 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Zinc finger protein AEBP2 | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Histone-lysine N-methyltransferase EZH2 | Homo sapiens (human) | Ki,app | 0.0012 | 1 | 1 |