Compound name
SGC707
Protein family
HMT
Target name
PRMT3@Methyltransferase
Affinity biochemical (nM)
85
Affinity on-target cellular (nM)
91
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000197b
SMILES
O=C(NCC(=O)N1CCCC1)Nc1ccc2cnccc2c1
InChIKey
DMIDPTCQPIJYFE-UHFFFAOYSA-N
NCBI gene ID
10196
UniProt ID
O60678
Mode of action
Allosteric inhibitor
Negative control
XY1
Affinity biochemical definition
Kd
Affinity biochemical assay type
SPR
Affinity Biochemical Source Knowledge
https://doi.org/10.1002/anie.201412154
https://www.thesgc.org/chemical-probes/SGC707
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot assay (measuring H4R3me2a levels in HEK293 cells co-transfected with FLAG tagged PRMT3 (wt))
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
31
Selectivity remarks
Screened at 1 µM, 5 µM and 20 µM, closest target at 20 µM: METTL21a (60% of contr.); Selective against panel of 250 enzymes (kinases, GPCRs, ion channels, transporters) at 10 µM, closest targets as % of contr.: 5HT2B (69%, Ki >15 µM), BRSK1 (56%), DLK1 (60%), MSK2 (55%), PKG2 (58%), PRKX (61%);
Selectivity Source Knowledge
https://doi.org/10.1002/anie.201412154
https://www.thesgc.org/chemical-probes/SGC707
Selectivity Number of Off-targets
0