Ligand id: 8287

Name: EPZ015666

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 8
Hydrogen bond donors 3
Rotatable bonds 8
Topological polar surface area 99.61
Molecular weight 383.2
XLogP 1.31
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Mechanism Of Action and Pharmacodynamic Effects
EPZ015666 inhibits PRMT5, an arginine methyltransferase (RMT) of the histone methyltransferase (HMT) family. PRMT5 is the only PRMT reported to catalyse symmetrical methylation of arginine residues on histone tails [2], and acts to promote transcriptional silencing of target genes. Aberrant regulation of methylation is reported in disease [9], making the proteins controlling this modification attractive drug discovery targets. For example, PRMT5 is overexpressed in several malignancies [1,3,6,8,10], including mantle cell lymphoma (MCL) [4,7].