Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties

Mathieu Bibian, Ronald J. Rahaim, Jun Yong Choi, Yoshihiko Noguchi, Stephan Schürer, Weimin Chen, Shima Nakanishi, Konstantin Licht, Laura H. Rosenberg, Lin Li, Yangbo Feng, Michael D. Cameron, Derek R. Duckett, John L. Cleveland, William R. Roush

Research output: Contribution to journalArticlepeer-review

40 Scopus citations


The development of a series of potent and highly selective casein kinase 1δ/ε (CK1δ/ε) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC50 ≤ 50 nM versus CK1δ. The two lead compounds have ≤100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human cancer cell lines.

Original languageEnglish (US)
Pages (from-to)4374-4380
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Issue number15
StatePublished - Aug 1 2013


  • Antiproliferative agent
  • Casein kinase 1δ/ε inhibitor
  • Potent growth inhibitor of A375 melanoma cell line
  • Purine scaffold kinase inhibitor
  • Selective CK1δ/ε inhibitor

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry


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