Compound name
LLY-283
Protein family
HMT
Target name
PRMT5
Affinity biochemical (nM)
22
Affinity on-target cellular (nM)
25
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000226b
SMILES
Nc1ncnc2c1ccn2[C@@H]1O[C@H]([C@H](O)c2ccccc2)[C@@H](O)[C@H]1O
InChIKey
WWOOWAHTEXIWBO-QFRSUPTLSA-N
NCBI gene ID
10419
UniProt ID
O14744
Synonyms
HRMT1L5, HSL7, IBP72, JBP1, SKB1, SKB1Hs
Mode of action
Inhibitor
Negative control
LLY-284
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioactivity-based assay (measuring transfer of the methyl group from 3H-SAM to peptide substrate)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acsmedchemlett.8b00014
https://www.thesgc.org/chemical-probes/LLY-283
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot (monitoring SmBB-Rme2s levels in MCF7 cells)
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
32
Selectivity remarks
Screened at 1 µM and 10 µM, selective over other targets including closely related arginine methyltransferases PRMT4, PRMT6, PRMT7;
Selectivity Source Knowledge
https://doi.org/10.1021/acsmedchemlett.8b00014
Selectivity Number of Off-targets
0