Compound name
LLY-284
Target name
PRMT5
Affinity biochemical (nM)
1074
Affinity on-target cellular (nM)
30000
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001484a
SMILES
Nc1ncnc2c1ccn2[C@@H]1O[C@H]([C@@H](O)c2ccccc2)[C@@H](O)[C@H]1O
InChIKey
WWOOWAHTEXIWBO-CNUKPYSBSA-N
NCBI gene ID
10419
UniProt ID
O14744
Synonyms
HRMT1L5, HSL7, IBP72, JBP1, SKB1, SKB1Hs
Mode of action
Negative control for LLY-283
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://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00014
Affinity biochemical relation
0
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 source knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00014
Affinity on-target cellular relation
>
Selectivity platform
Methyltransferase panel
Selectivity platform number of targets
32
Selectivity remarks
Screened at 1 µM, highly selective with all targets >55% remaining activity, PRMT5 (55%), other targets >90%
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00014
Selectivity Number of Off-targets
0