Compound name
UNC1999
Protein family
HMT
Target name
EZH1@Methyltransferase
Affinity biochemical (nM)
45
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000209b
SMILES
CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(-c2ccc(N3CCN(C(C)C)CC3)nc2)cc2c1cnn2C(C)C
InChIKey
DPJNKUOXBZSZAI-UHFFFAOYSA-N
NCBI gene ID
2145
UniProt ID
Q92800
Synonyms
KIAA0388, KMT6B
Mode of action
Inhibitor
Negative control
UNC2400
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric kinase assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/cb400133j
https://www.thesgc.org/chemical-probes/UNC1999
Affinity biochemical relation
=
Selectivity platform
HMT panel, literature
Selectivity platform number of targets
16
Selectivity remarks
Selective over 15 other lysine, arginine, and DNA methyltransferases; Less than 20% inhibition on 50 kinase targets at 10 µM; Tested in PDSP screen: less than 50% inhibition on 40 7TM targets at 10 µM, greater than 50% inhibition of 4 7TM targets at 10 µM, closest targets: Ki(H3) = 300 nM, Ki(NET) = 1500nM, Ki(Sigma 1) =4700 nM, Ki(Sigma 2) = 65 nM (Radioligand binding assay);
Selectivity Source Knowledge
https://doi.org/10.1021/cb400133j
Selectivity Number of Off-targets
0