4RSS

Crystal structure of tyrosine-protein kinase SYK with an inhibitor

Summary for 4RSS

Entry DOI	10.2210/pdb4rss/pdb
Descriptor	Tyrosine-protein kinase SYK, 1-[(3-methyl-1-{2-[(1,2,3-trimethyl-1H-indol-5-yl)amino]pyrimidin-4-yl}-1H-pyrazol-4-yl)methyl]azetidin-3-ol (3 entities in total)
Functional Keywords	kinase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological source	Homo sapiens (human)
Cellular location	Cell membrane : P43405
Total number of polymer chains	1
Total formula weight	34318.47
Authors	Lee, B.I.,Lee, S.J.,Choi, J.-S. (deposition date: 2014-11-11, release date: 2015-10-21, Last modification date: 2024-03-20)
Primary citation	Choi, J.S.,Hwang, H.J.,Kim, S.W.,Lee, B.I.,Lee, J.,Song, H.J.,Koh, J.S.,Kim, J.H.,Lee, P.H. Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors. Bioorg.Med.Chem.Lett., 25:4441-4446, 2015 Cited by PubMed Abstract: A series of pyrazolylpyrimidine scaffold based Syk inhibitors were synthesized and evaluated for their biological activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymatic and TNF-α release assay. PubMed: 26384287 DOI: 10.1016/j.bmcl.2015.09.011 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.83 Å)

Structure validation