Compound name
TP-064
Protein family
HMT
Target name
CARM1
Affinity biochemical (nM)
10
Affinity on-target cellular (nM)
43
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000230b
SMILES
CNCCN1CCC(c2cc(CN(C)C(=O)c3cccc(Oc4ccccc4)c3)ccn2)CC1
InChIKey
VUIITYLFSAXKIQ-UHFFFAOYSA-N
NCBI gene ID
10498
UniProt ID
Q86X55
Synonyms
PRMT4
Mode of action
Inhibitor
Negative control
TP-064N
Affinity biochemical definition
IC50
Affinity biochemical assay type
Scintillation proximity assay (SPA)
Affinity Biochemical Source Knowledge
https://www.oncotarget.com/article/24883/text/
Affinity biochemical relation
<
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Western Blot (dimethylation of MED12, Med12me2a/Med12, in HEK293T cells)
Affinity on-target cellular source knowledge
https://www.oncotarget.com/article/24883/text/
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase screen (Scintillation proximity assays)
Selectivity platform number of targets
32
Selectivity remarks
In-vitro potencies of closest targets: IC50(PRMT6) = 1.3 µM, IC50(PRMT8) = 8.1 µM, IC50(PRMT4) <0.01 µM, IC50(PRMT1) >10 µM, IC50(PRMT3) >10 µM, IC50(PRMT5) >10 µM, IC50(PRMT7) >10 µM, IC50(PRMT9) >10 µM, IC50(G9a) >10 µM, IC50(GLP) >10 µM, IC50(SETDB1) >10 µM, IC50(SUV39H1) >10 µM, IC50(SUV39H2) >10 µM, IC50(PRDM9) >10 µM, IC50(SETD) >10 µM, IC50(SETD7) >10 µM, IC50(MLL1) >10 µM, IC50(MLL3) >10 µM, IC50(SETD2) >10 µM, IC50(PRC2) >10 µM, IC50(SUV420H1) >10 µM, IC50(SUV420H2) >10 µM, IC50(SMYD2) >10 µM, IC50(SMYD3) >10 µM, IC50(DNMT1) >10 µM, IC50(DNMT3A/3L) >10 µM, IC50(DNMT3B/3L) >10 µM, IC50(NSD1) >10 µM, IC50(NSD2) >10 µM, IC50(NSD3) >10 µM, IC50(ASH1L) >10 µM, IC50(DOT1L) >10 µM
Selectivity Source Knowledge
https://www.oncotarget.com/article/24883/text/