Kinases are likely the most well studied target class for discovery, and there are several breakthrough therapies targeting kinases in the oncology space. Two thirds of known kinases are serine-threonine kinases, and about 17% are tyrosine kinases with the remainder classified as atypical kinases. Signaling pathways downstream of various kinases have been well studied, but the challenge for precision drug targeting is the redundancy and overlap of signaling pathways, which can impede therapeutic efficacy. Additionally, loss and gain of function mutations have been identified as disease drivers for several diseases, including various types of cancers.

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At Charles River, we have developed over a hundred assays covering Ser/Thr, Tyr, and lipid kinases utilizing radiometric, fluorescence-based, and luminescent readouts. Our discovery teams have worked on many kinase targets across multiple therapeutic areas, delivering development candidates in inflammation, respiratory, metabolic, and oncology indications. In addition, our pioneering SoftFocus® kinase libraries have been utilized to successfully deliver several development candidates.

  • Discovery of LRRK2 Inhibitors by Using an Ensemble of Virtual Screening Methods. Bioorganic & Medicinal Chemistry Letters. 2017, 27 (11), 2520-2527. Abstract​.
  • The Rational Design of Selective Benzoxazepin Inhibitors of the ɑ-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326). J. Med. Chem. 2016, 59, 985-1002. Abstract.
  • Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1. J. Med. Chem. 2015, 58, 5053-5074. Abstract.
  • The Tyrosine Kinase Inhibitor Nilotinib Has Antineoplastic Activity in Prostate Cancer Cells but Up‐Regulates the ERK Survival Signal – Implications for Targeted Therapies. Urol Oncol. 2015, 33, 2, 72, 1‐7. Full Text.
  • Annotation of Human Cancers with EGFR Signaling – Associated Protein Complexes Using Proximity Ligation Assays. Sci Signal. 2015, 13, 8, 359. Full Text.

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SoftFocus® Compound Libraries

SoftFocus® compound libraries have delivered outstanding success to partners that have screened them and have led to several clinical candidates.