| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3421227 | Binding | Inhibition of human DOT1L using oligo-nucleosome/[3H]-SAM as substrate preincubated for 30 mins followed by substrate addition measured after 120 mins by Morrison plot analysis | Homo sapiens | 2 | ALA3414551 | single protein format | Scientific Literature | |
| 2. | ALA3421228 | Binding | Selectivity ratio of IC50 for human G9a to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 3. | ALA3421229 | Binding | Selectivity ratio of IC50 for human GLP to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 4. | ALA3421230 | Binding | Selectivity ratio of IC50 for human SETD7 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 5. | ALA3421231 | Binding | Selectivity ratio of IC50 for human SMYD2 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 6. | ALA3421232 | Binding | Selectivity ratio of IC50 for human SMYD3 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 7. | ALA3421233 | Binding | Selectivity ratio of IC50 for human MMSET to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 8. | ALA3421234 | Binding | Selectivity ratio of IC50 for human WHSC1L1 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 9. | ALA3421235 | Binding | Selectivity ratio of IC50 for human PRMT1 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 10. | ALA3421236 | Binding | Selectivity ratio of IC50 for human PRMT3 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 11. | ALA3421237 | Binding | Selectivity ratio of IC50 for human PRMT4 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 12. | ALA3421238 | Binding | Selectivity ratio of IC50 for human PRMT5 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 13. | ALA3421239 | Binding | Selectivity ratio of IC50 for human PRMT6 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 14. | ALA3421240 | Binding | Selectivity ratio of IC50 for human PRMT8 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 15. | ALA3421241 | Binding | Selectivity ratio of IC50 for human EZH1 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 16. | ALA3421242 | Binding | Selectivity ratio of IC50 for human EZH2 to IC50 for human DOT1L | Homo sapiens | 1 | ALA3414551 | assay format | Scientific Literature | |
| 17. | ALA3421243 | Binding | Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level after 4 days by ELISA method | Homo sapiens | 1 | ALA3414551 | cell-based format | Scientific Literature | |
| 18. | ALA3421244 | Binding | Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as reduction of H3K79me2 level at 1 uM after 3 to 4 days by immunoblot analysis relative to control | Homo sapiens | 1 | ALA3414551 | cell-based format | Scientific Literature | |
| 19. | ALA3421462 | Binding | Inhibition of DOT1L in human MV4-11 cells expressing MLL-AF4 assessed as cell growth inhibition after 14 days by Guava Viacount assay | Homo sapiens | 1 | ALA3414551 | cell-based format | Scientific Literature | |
| 20. | ALA3888978 | Binding | In Vitro Biological Assay: An in vitro biological assay that can be used includes the steps of (1) mixing a histone substrate (e.g., an isolated histone sample for a histone or modified histone of interest, or an isolated oligonucleosome substrate) with recombinant DOT1L enzyme (e.g., recombinant protein containing amino acids 1-416); (2) adding a candidate compound of the invention to this mixture; (3) adding non-radioactive and 3H-labeled S-Adenosyl methionine (SAM) to start the reaction; (4) adding excessive amount of non-radioactive SAM to stop the reaction; (4) washing off the free non-incorporated 3H-SAM; and (5) detecting the quantity of 3H-labeled histone substrate by any methods known in the art (e.g., by a PerkinElmer TopCount platereader). | 9 | ALA3886905 | single protein format | BindingDB Database |
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