oral PRMT5 inh. for treating cancers
projected human dose of 15 mg QD w/ 6 HBD
SBDD from SAM cofactor
J. Med. Chem., Mar. 23, 2021
Merck & Co, Boston, MA
“Compound 72”
1 min read
The Merck protein arginine methyltransferase 5 (PRMT5) inhibitor (“compound 72”) is a SAM cofactor-mimetic with a novel 5,5-fused carbon-based bicyclic scaffold. PRMT5 is an actively pursued epigenetic target for cancer with a flurry of research programs being published recently and several trials being initiated. Remarkably, compound 72 has an excellent oral PK profile in higher species with a low predicted human dose of 15 mg QD, despite having 6 hydrogen bond donors and 6 rings.
Search By Structure
- LSN3318839
- GLPG1972
- APJ compound 14
- Encequidar
- S62798 (Servier)
- CVN424
- ABBV-167
- GDC-0310
- “Compound 72”
- “Compound 20”
- TAK-418
- Compound 13 (GSK716)
- RBN-012759
- Sisunatovir
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