Compound name
MS023
Protein family
HMT
Target name
PRMT3@Methyltransferase
Affinity biochemical (nM)
119
Affinity on-target cellular (nM)
1000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000034d
SMILES
CC(C)Oc1ccc(-c2c[nH]cc2CN(C)CCN)cc1
InChIKey
FMTVWAGUJRUAKE-UHFFFAOYSA-N
NCBI gene ID
10196
UniProt ID
O60678
Mode of action
Inhibitor
Negative control
MS094
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation proximity assay (SPA)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acschembio.5b00839
https://www.thesgc.org/chemical-probes/MS023
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot (inhibition of PRMT3 methyltransferase activity in MCF7 cells)
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
25
Selectivity remarks
Screened at 1 µM and 10 µM, highly selective within methyltransferase family; Selective over 9 reader proteins (UHRF1, BRPF1, WDR5, HGDF2, TDRD3, RBBP1, FXR1, EED, and SND1) in DSF assays: all enzymes dTm <2 K;
Selectivity Source Knowledge
https://doi.org/10.1021/acschembio.5b00839
Selectivity Number of Off-targets
0