4RX8: SYK Catalytic Domain Complexed with a Potent Triazine Inhibitor2

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: 4RX8Download
MMDB ID: 127886
PDB Deposition Date: 2014/12/9
Updated in MMDB: 2017/12
Experimental Method:
x-ray diffraction
Resolution: 1.59  Å
Source Organism:
Similar Structures:
Biological Unit for 4RX8: monomeric; determined by author and by software (PISA)
Molecular Components in 4RX8
Label Count Molecule
Protein (1 molecule)
Tyrosine-protein Kinase SYK(Gene symbol: SYK)
Molecule annotation
Chemicals (3 molecules)
* Click molecule labels to explore molecular sequence information.

Citing MMDB