Compound name
UNC1999
Protein family
HMT
Target name
EZH2@Methyltransferase
Affinity biochemical (nM)
2
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
2146
UniProt ID
Q15910
Synonyms
EZH1, ENX-1, KMT6, KMT6A
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