Compound name
GSK343
Protein family
HMT
Target name
EZH2@Methyltransferase
Affinity biochemical (nM)
1.2
Affinity on-target cellular (nM)
174
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000215b
SMILES
CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(-c2ccnc(N3CCN(C)CC3)c2)cc2c1cnn2C(C)C
InChIKey
ULNXAWLQFZMIHX-UHFFFAOYSA-N
NCBI gene ID
2146
UniProt ID
Q15910
Synonyms
EZH1, ENX-1, KMT6, KMT6A
Mode of action
Inhibitor
Affinity biochemical definition
Ki,app
Affinity biochemical assay type
Enzyme inhibition assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/ml3003346
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Immunofluorescence (inhibition of H3K27 methylation in HCC1806 cells)
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel (HotSpot screen, Reaction Biology)
Selectivity platform number of targets
19
Selectivity remarks
Selective over other methyltransferases (radioisotope-based filter binding assays), closest target: IC50(EZH1) = 240 nM, others <60 µM; Screened against 44 receptors and enzymes (internal screening at GSK), closest target: IC50(A1b) = 10 µM, others >10 µM, >100-fold selective
Selectivity Source Knowledge
https://doi.org/10.1021/ml3003346
https://www.thesgc.org/chemical-probes/GSK343
Selectivity Number of Off-targets
0