3en5 Summary details

pdbe.org/3en5/summary_details
spacer Targeted polypharmacology: crystal structure of the c-Src kinase domain in complex with PP494, a multitargeted kinase inhibitor
Summary
Header TRANSFERASEsearch
Method X-RAY DIFFRACTION
Experiment Resolution: 2.66 Å, R-factor: 20.644%, Free R-factor: 24.788%, Spacegroup: P 1
Released 14/10/2008, deposition: 25/09/2008, last revision: 13/07/2011
Authors Blair, J.A.search; Apsel, B.search; Knight, Z.A.search; Shokat, K.M.search
Primary citation Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
NAT.CHEM.BIOL.search vol:4, pag:691-699 (2008) [PubMed 18849971 ]search
Keywords SRCsearch, tyrosinesearch, kinasesearch, polypharmacologysearch, inhibitorsearch, multitargetsearch, phosphoinositidesearch, transferasesearch, signalingsearch, pyrazolopyrimidinesearch, kinase-inhibitor complexsearch, ATP-bindingsearch, Lipoproteinsearch, Myristatesearch, Nucleotide-bindingsearch, Phosphoproteinsearch, Proto-oncogenesearch, SH2 domainsearch, SH3 domainsearch, Tyrosine-protein kinasesearch
EC 2.7.10.2 ExPASy BRENDA search (A B)
Organism Gallus gallus(chicken) 9031search(A B)
UniProt P00523search (A B)
Solvent A, B
Related entries 3en4, 3en6, 3en7
Polymers
Chain Id Name Type UniProt Residues in sample sequence % of sample sequence observed
A, B Proto-oncogene tyrosine-protein kinase Src Protein P00523 (SRC_CHICK)search
286 91%
Heterogens
Chain Id Name Ligands
A, B 1-CYCLOBUTYL-3-(3,4-DIMETHOXYPHENYL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE KS4 search
spacer