4RX7

SYK Catalytic Domain Complexed with a Potent Triazine Inhibitor

Summary for 4RX7

Entry DOI	10.2210/pdb4rx7/pdb
Related	4RX8 4RX9
Descriptor	Tyrosine-protein kinase SYK, FORMIC ACID, GLYCEROL, ... (5 entities in total)
Functional Keywords	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	34202.32
Authors	Lee, C.C. (deposition date: 2014-12-09, release date: 2015-03-18, Last modification date: 2024-02-28)
Primary citation	Thoma, G.,Smith, A.B.,van Eis, M.J.,Vangrevelinghe, E.,Blanz, J.,Aichholz, R.,Littlewood-Evans, A.,Lee, C.C.,Liu, H.,Zerwes, H.G. Discovery and profiling of a selective and efficacious syk inhibitor. J.Med.Chem., 58:1950-1963, 2015 Cited by PubMed Abstract: We describe the discovery of selective and potent Syk inhibitor 11, which exhibited favorable PK profiles in rat and dog and was found to be active in a collagen-induced arthritis model in rats. Compound 11 was selected for further profiling, but, unfortunately, in GLP toxicological studies it showed liver findings in rat and dog. Nevertheless, 11 could become a valuable tool compound to investigate the rich biology of Syk in vitro and in vivo. PubMed: 25633741 DOI: 10.1021/jm5018863 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.8 Å)

Structure validation