Threonine tyrosine kinase (TTK), a dual-specificity protein kinase, acts as a core component of the spindle assembly checkpoint and plays a crucial role in accurate separation of sister chromatids during mitosis to avoid aneuploidy. TTK inhibition is an attractive wide-spectrum strategy for cancer therapy. Researchers designed and synthesized a series of pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable TTK inhibitors. All the pharmacokinetic studies were carried out by Medicilon.
Compounds 5o exhibits strong binding affinity to TTK with a Kd value of 0.15 nM. Compound 5o demonstrates good oral pharmacokinetic properties.
Reference:
Relevant News
marketing@medicilon.com
