Compound name
SGC0946
Protein family
HMT
Target name
DOT1L@Methyltransferase
Affinity biochemical (nM)
0.3
Affinity on-target cellular (nM)
2.6
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000216b
SMILES
CC(C)N(CCCNC(=O)Nc1ccc(C(C)(C)C)cc1)C[C@H]1O[C@@H](n2cc(Br)c3c(N)ncnc32)[C@H](O)[C@@H]1O
InChIKey
IQCKJUKAQJINMK-HUBRGWSESA-N
NCBI gene ID
84444
UniProt ID
Q8TEK3
Synonyms
KIAA1814, DOT1, KMT4
Mode of action
Inhibitor
Negative control
SGC0649
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioactive enzyme assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1038/ncomms2304
https://www.thesgc.org/chemical-probes/SGC0946
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Westen Blot (reduction of H3K79 dimethylation in A431 cells by DOT1L)
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
12
Selectivity remarks
Screened against G9a, EHMT1, PRMT3/5, SETDB1, SETD7/8, MLL, EZH2, SUV39H2, SUV420H2; Clean profile in Ricerca selectivity panel at 1 µM against 29 diverse receptors
Selectivity Source Knowledge
https://doi.org/10.1038/ncomms2304
https://www.thesgc.org/chemical-probes/SGC0946
Selectivity Number of Off-targets
0