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 The p38αMAPK (MAPK14, mitogen-activated protein kinase 14, CSBP, CSBP1, CSBP2, CSPB1, EXIP, Mxi2, PRKM14, PRKM15, RK, SAPK2A, p38, p38ALPHA) is a serine/threonine protein kinase which plays a key role in the intracellular signaling networks that transduce and amplify stress signals into physiological changes. This kinase is a brain drug discovery target. It is involved in neuroinflammatory responses and synaptic dysfunction in multiple degenerative and neuropsychiatric brain disorders.
We offer the chemical optimization service - synthesis of p38αMAPK targeted set of arylpyridazine derivatives for developing of drugs for neurological disorders. These novel compounds will be selected from a set of 2,000+ virtual arylpyridazines using our company’s proprietary molecular modeling platform ODDA™, synthesized and provided for your biological projects.
This set of novel analogs will be synthesized exclusively upon your request.
See also: p38 MAP Kinase Alpha Targeted Library
This is referred to a paper from Journal of Medicinal Chemistry* which showed that authors discovered p38αMAPK inhibitors. Compound mw150 (6-(4-methylpiperazin-1-yl)-3-(naphthalen-2-yl)-4-(pyridin-4-yl)pyridazine) possess the best inhibition activity against this enzyme and efficacious in diverse animal models of neurologic disorders:
MW150, p38αMAPK Ki = 100 nM
Design and synthesis of inhibitors p38αMAPK is a promising direction in neurologic diseases treatment.
* Saktimayee M Roy, George Minasov, Ottavio Arancio, Laura W Chico, Linda J. Van Eldik, Wayne F Anderson, Jeffrey C Pelletier, and D. Martin Watterson. A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction. J. Med. Chem. 2019, Vol. 62(11), pp. 5298−5311, DOI: 10.1021/acs.jmedchem.9b00058.
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