Table 1.
Current inhibition assays performed for different epigenetic factors.
| Type of inhibitor | Epigenetic Factor | Acronym | CHEMBL ID | Inhibitor molecules | |
|---|---|---|---|---|---|
| DNMTi | DNA (cytosine-5)-methyltransferase 1 | DNMT1 | CHEMBL1993 | 841 | |
| DNA (cytosine-5)-methyltransferase 3A | DNMT3A | CHEMBL1992 | 258 | ||
| DNA (cytosine-5)-methyltransferase 3B | DNMT3B | CHEMBL6095 | 80 | ||
| HDACi | HDACi (Zn dependent) | Histone deacetylase 1 | HDAC1 | CHEMBL325 | 6434 |
| Histone deacetylase 6 | HDAC6 | CHEMBL1865 | 4701 | ||
| Histone deacetylase 8 | HDAC8 | CHEMBL3192 | 2420 | ||
| Histone deacetylase 3 | HDAC3 | CHEMBL1829 | 2043 | ||
| Histone deacetylase 2 | HDAC2 | CHEMBL1937 | 2003 | ||
| Histone deacetylase 4 | HDAC4 | CHEMBL3524 | 1279 | ||
| Histone deacetylase 7 | HDAC7 | CHEMBL2716 | 521 | ||
| Histone deacetylase 11 | HDAC11 | CHEMBL3310 | 503 | ||
| Histone deacetylase 5 | HDAC5 | CHEMBL2563 | 460 | ||
| Histone deacetylase 10 | HDAC10 | CHEMBL5103 | 419 | ||
| Histone deacetylase 9 | HDAC9 | CHEMBL4145 | 348 | ||
| SIRTi (NAD+ dependent) | NAD-dependent deacetylase sirtuin 1 | SIRT 1 | CHEMBL4506 | 2073 | |
| NAD-dependent deacetylase sirtuin 2 | SIRT 2 | CHEMBL4462 | 2839 | ||
| NAD-dependent deacetylase sirtuin 3 | SIRT 3 | CHEMBL4461 | 634 | ||
| NAD-dependent deacetylase sirtuin 5 | SIRT 5 | CHEMBL2163183 | 250 | ||
| NAD-dependent deacetylase sirtuin 6 | SIRT 6 | CHEMBL2163182 | 221 | ||
| NAD-dependent deacetylase sirtuin 7 | SIRT 7 | CHEMBL2163184 | 10 | ||
| HMTi | KMTi | Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 | KMT1D | CHEMBL6031 | 238 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 | G9A | CHEMBL6032 | 92523 | ||
| Histone-lysine N-methyltransferase MLL | MLL1 | CHEMBL1293299 | 17219 | ||
| Histone-lysine N-methyltransferase EZH2 | EZH2 | CHEMBL2189110 | 1243 | ||
| Histone-lysine N-methyltransferase, H3 lysine-79 specific | DOT1L | CHEMBL1795117 | 344 | ||
| Histone-lysine N-methyltransferase SETD7 | SETD7 | CHEMBL5523 | 204 | ||
| Histone-lysine N-lysine methyltransferase SETD8 | SETD8 | CHEMBL1795176 | 98 | ||
| Histone-lysine N-lysine methyltransferase SMYD2 | SMYD2 | CHEMBL2169716 | 84 | ||
| Histone-lysine N-methyltransferase SMYD3 | SMYD3 | CHEMBL2321643 | 54 | ||
| Histone-lysine N-methyltransferase SUV39H1 | SMYD2 | CHEMBL2169716 | 84 | ||
| Histone-lysine N-methyltransferase EZH1 | EZH1 | CHEMBL2189116 | 32 | ||
| Histone-lysine N-methyltransferase SUV39H2 | SUV39H2 | CHEMBL1795177 | 21 | ||
| Histone-lysine N-methyltransferase NSD2 | NSD2 | CHEMBL3108645 | 20 | ||
| Histone-lysine N-methyltransferase SETDB1 | SETDB1 | CHEMBL2321646 | 14 | ||
| Histone-lysine N-methyltransferase SUV420H2 | SUV420H2 | CHEMBL2321644 | 12 | ||
| Histone-lysine N-methyltransferase SETD2 | SETD2 | CHEMBL3108647 | 11 | ||
| Histone-lysine N-methyltransferase, H3 lysine-36 and H4 lysine-20 specific | NSD1 | CHEMBL3588738 | 10 | ||
| Histone-lysine N-methyltransferase PRDM9 | PRDM9 | CHEMBL3588737 | 10 | ||
| Histone-lysine N-methyltransferase SUV420H1 | SUV420H1 | CHEMBL2321645 | 9 | ||
| Histone-lysine N-methyltransferase MLL3 | MLL3 | CHEMBL2189113 | 7 | ||
| Histone-lysine N-methyltransferase NSD3 | NSD3 | CHEMBL3108646 | 7 | ||
| Histone-lysine N-methyltransferase ASH1L | ASH1L | CHEMBL3588739 | 6 | ||
| Histone-lysine N-methyltransferase SETMAR | SETMAR | CHEMBL2189111 | 3 | ||
| Histone-lysine N-methyltransferase MLL2 | MLL2 | CHEMBL2189114 | 2 | ||
| Histone-lysine N-methyltransferase MLL4 | MLL4 | CHEMBL2189112 | 2 | ||
| Histone-lysine N-methyltransferase SETD1B | SET1B | CHEMBL4105837 | 1 | ||
| Histone-lysine N-methyltransferase SETD1A | SETD1A | CHEMBL4105954 | 1 | ||
| RMTi | Histone-arginine methyltransferase CARM1 | CARM1 | CHEMBL5406 | 201 | |
| Protein-arginine N-methyltransferase 1 | PRMT1 | CHEMBL5524 | 528 | ||
| Protein arginine N-methyltransferase 6 | PRMT6 | CHEMBL1275221 | 139 | ||
| Protein arginine N-methyltransferase 3 | PRMT3 | CHEMBL5891 | 138 | ||
| Protein arginine N-methyltransferase 5 | PRMT5 | CHEMBL1795116 | 91 | ||
| Protein arginine N-methyltransferase 7 | PRMT7 | CHEMBL3562175 | 25 | ||
| HDMi | JmjC | Probable JmjC domain-containing histone demethylation protein 2C | JHDM2C | CHEMBL3792271 | 1 |
| Histone lysine demethylase PHF8 | PHF8 | CHEMBL1938212 | 136 | ||
| Lysine-specific demethylase 2A | KDM2A | CHEMBL1938210 | 128 | ||
| Lysine-specific demethylase 2B | KDM2B | CHEMBL3779760 | 333 | ||
| Lysine-specific demethylase 3A | KDM3A | CHEMBL1938209 | 87 | ||
| Lysine-specific demethylase 3B | KDM3B | CHEMBL3784906 | 9 | ||
| Lysine-specific demethylase 4A | KDM4A | CHEMBL5896 | 51948 | ||
| Lysine-specific demethylase 4B | KDM4B | CHEMBL3313832 | 73 | ||
| Lysine-specific demethylase 4C | KDM4C | CHEMBL6175 | 878 | ||
| Lysine-specific demethylase 4D | KDM4D | CHEMBL6138 | 53 | ||
| Lysine-specific demethylase 4D-like | KDM4E | CHEMBL1293226 | 110 | ||
| Lysine-specific demethylase 5A | KDM5A | CHEMBL2424504 | 621 | ||
| Lysine-specific demethylase 5B | KDM5B | CHEMBL3774295 | 469 | ||
| Lysine-specific demethylase 5C | KDM5C | CHEMBL2163176 | 147 | ||
| Lysine-specific demethylase 6A | KDM6A | CHEMBL2069164 | 29 | ||
| Lysine-specific demethylase 6B | KDM6B | CHEMBL1938211 | 203 | ||
| Lysine-specific demethylase 7 | KDM7A | CHEMBL2163177 | 35 | ||
| LSD | Lysine-specific histone demethylase 1 | KDM1A | CHEMBL6136 | 1710 | |
| Lysine-specific histone demethylase 1B | KDM1B | CHEMBL1938208 | 62 | ||
| BETi | Bromo and Extra terminal Domain | Bromodomain-containing protein 1 | BRD1 | CHEMBL2176774 | 121 |
| Bromodomain-containing protein 2 | BRD2 | CHEMBL1293289 | 570 | ||
| Bromodomain-containing protein 3 | BRD3 | CHEMBL1795186 | 474 | ||
| Bromodomain-containing protein 4 | BRD4 | CHEMBL1163125 | 4864 | ||
| Bromodomain testis-specific protein | BRDT | CHEMBL1795185 | 119 | ||