5EAK

Optimization of Microtubule Affinity Regulating Kinase (MARK) Inhibitors with Improved Physical Properties

Summary for 5EAK

Entry DOI	10.2210/pdb5eak/pdb
Descriptor	Serine/threonine-protein kinase MARK2, N-[(1S,2R)-2-aminocyclohexyl]-4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]thiophene-2-carboxamide (3 entities in total)
Functional Keywords	catalytic domain, protein-serine-threonine kinases, kinase inhibitor, serine-threonine kinases, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (Human)
Cellular location	Cell membrane; Peripheral membrane protein: Q7KZI7
Total number of polymer chains	2
Total formula weight	76508.48
Authors	Su, H.P. (deposition date: 2015-10-16, release date: 2016-02-17, Last modification date: 2024-03-06)
Primary citation	Sloman, D.L.,Noucti, N.,Altman, M.D.,Chen, D.,Mislak, A.C.,Szewczak, A.,Hayashi, M.,Warren, L.,Dellovade, T.,Wu, Z.,Marcus, J.,Walker, D.,Su, H.P.,Edavettal, S.C.,Munshi, S.,Hutton, M.,Nuthall, H.,Stanton, M.G. Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties. Bioorg.Med.Chem.Lett., 26:4362-4366, 2016 Cited by PubMed: 27491711 DOI: 10.1016/j.bmcl.2016.02.003 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.8 Å)

Structure validation