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TitleDiscovery and optimization of 4-pyrazolyl-2-aminopyrimidine derivatives as potent spleen tyrosine kinase (SYK) inhibitors.
Journal, issue, pagesEur. J. Med. Chem., Vol. 270, Page 116375-116375, Year 2024
Publish dateJan 23, 2024 (structure data deposition date)
AuthorsCervi, G. / D'Alessio, R. / Bindi, S. / Buffa, L. / Burocchi, A. / Canevari, G. / Modugno, M. / Motto, I. / Saturno, G. / Orsini, P.
External linksEur. J. Med. Chem. / PubMed:38604095
MethodsX-ray diffraction
Resolution1.6 - 1.75 Å
Structure data

PDB-8rrq:
Crystal structure of human SYK in complex with compound 24
Method: X-RAY DIFFRACTION / Resolution: 1.6 Å

PDB-8rrz:
Crystal structure of SYK kinase in complex with compound 1
Method: X-RAY DIFFRACTION / Resolution: 1.75 Å

Chemicals

PDB-1h2w:
PROLYL OLIGOPEPTIDASE FROM PORCINE BRAIN

ChemComp-GOL:
GLYCEROL

ChemComp-HOH:
WATER

PDB-1h2y:
PROLYL OLIGOPEPTIDASE FROM PORCINE BRAIN, Y473F MUTANT WITH COVALENTLY BOUND INHIBITOR Z-PRO-PROLINAL

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / inhibitor / kinase

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