4RX9: SYK Catalytic Domain Complexed with a Potent Pyrimidine Inhibitor

Citation:
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.
PDB ID: 4RX9Download
MMDB ID: 127887
PDB Deposition Date: 2014/12/9
Updated in MMDB: 2017/12
Experimental Method:
x-ray diffraction
Resolution: 1.75  Å
Source Organism:
Similar Structures:
Biological Unit for 4RX9: monomeric; determined by author and by software (PISA)
Molecular Components in 4RX9
Label Count Molecule
Protein (1 molecule)
1
Tyrosine-protein Kinase SYK(Gene symbol: SYK)
Molecule annotation
Chemicals (2 molecules)
1
1
2
1
* Click molecule labels to explore molecular sequence information.

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