Compound name
UNC0642
Protein family
HMT
Target name
EHMT1/GLP@Methyltransferase
Affinity biochemical (nM)
2.5
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000194b
SMILES
COc1cc2c(NC3CCN(C(C)C)CC3)nc(N3CCC(F)(F)CC3)nc2cc1OCCCN1CCCC1
InChIKey
RNAMYOYQYRYFQY-UHFFFAOYSA-N
NCBI gene ID
79813
UniProt ID
Q9H9B1
Synonyms
Eu-HMTase1, FLJ12879, KIAA1876, bA188C12.1, KMT1D, FLJ40292
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic activity assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/jm401480r
https://www.thesgc.org/chemical-probes/UNC0642
Affinity biochemical relation
<
Selectivity platform
HMT panel, literature
Selectivity platform number of targets
16
Selectivity remarks
>100-fold selective against other HMTs, selective against 44 GPCRS, ion channels and transporters at 1 µM, closest targets as % of contr.: H3 (93%, Ki = 45 nM), µ opioid (74%, Ki >10 µM), a2C (67%, Ki > 10 µM), a1D (59%, Ki = 4.5 µM); Selective against 50 kinases at 10 µM
Selectivity Source Knowledge
https://doi.org/10.1021/jm401480r
Selectivity Number of Off-targets
0