Compound name
SGC3027
Protein family
Methyltransferase
Target name
PRMT7
Affinity biochemical (nM)
294
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000235b
SMILES
CC1=C(C)C(=O)C(C(C)(C)CC(=O)N(CCCCSC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)Cc2cccc(-c3ccc(Cl)cc3)c2)=C(C)C1=O
InChIKey
MLJVGAYSVYMPSB-MSUKGTQXSA-N
Mode of action
Pro-drug of SGC8158
Negative control
SGC3027N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioactive activity assay (PRMT methylation of HSPA8, values for active compound SGC8158)
Affinity Biochemical Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7224190/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (TR-FRET assays), literature
Selectivity platform number of targets
342
Selectivity remarks
Screened at 0.1 µM and 1 µM, all values determined for active compound SGC8158, closest targets: IC50(PRMT4) = 3.6 nM, IC50(PRMT5-MEP50) = 44 nM, IC50(PRMT9) = 138 nM; Clean in radiometric assays against 35 methyltransferases including PRMTs: IC50(PRMT5) = 0.15 µM, IC50(PRMT4) = 0.14 µM, IC50 (PRMT9) = 0.16 µM, IC50(BCDIN3D) = 1.1 µM, IC50(PRMT3) = 1.6 µM, IC50(DOT1L) = 1.7 µM, IC50(PRMT8) = 15 µM, IC50(PRMT6) = 15 µM, IC50(PRMT1) = 12 µM
Selectivity Source Knowledge
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7224190/
Selectivity Number of Off-targets
3