2h8h Summary

pdbe.org/2h8h
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Src kinase in complex with a quinazoline inhibitor

The structure was published by Hennequin, L.F., Allen, J., Breed, J., et al., Ple, P.A., Warin, N., and Costello, G., in 2006 in a paper entitled "N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor." (abstract).

This crystal structure was determined using X-ray diffraction at a resolution of 2.2 Å and deposited in 2006.

The experimental data on which the structure is based was also deposited.

The PDB entry contains the structure of Proto-oncogene tyrosine-protein kinase Src. This molecule has the UniProt identifier P12931 (SRC_HUMAN)search. The sample contained 535 residues which is 100% of the natural sequence. Out of 535 residues 444 were observed and are deposited in the PDB.

It also contains one or more heterogenic compounds (e.g., ligands, co-factors, ions, modified amino acids, etc.); see here for a complete list.

The molecule is most likely monomeric.

The following tables show cross-reference information to other databases (to obtain a list of all PDB entries sharing the same property or classification, click on the magnifying glass icon):


Chain Name UniProt Name of source organism % of UniProt sequence present in the sample Residues in the sample molecules % of residues observed
A Proto-oncogene tyrosine-protein kinase Src P12931 (2-536) (SRC_HUMAN)search Homo sapienssearch 100% 535 83%


This entry contains 1 unique UniProt protein:

UniProt accession Name Organism PDB
P12931 (2 - 536) Proto-oncogene tyrosine-protein kinase Src Homo sapiens

Chain Structural classification (SCOP) Structural classification (CATH) Sequence family (Pfam)
A (P12931) SH3-domainsearch, SH2 domainsearch, Protein kinases, catalytic subunitsearch SH3 Domainssearch, SHC Adaptor Proteinsearch, Phosphorylase Kinase; domain 1search, Transferase(Phosphotransferase) domain 1search PF00017: SH2 domainsearch, PF00018: SH3 domainsearch, PF07714: Protein tyrosine kinasesearch

Chain ID Biological process (GO) Molecular function (GO) Cellular component (GO)
A (P12931) protein phosphorylationsearch regulation of intracellular estrogen receptor signaling pathwaysearch Ras protein signal transductionsearch leukocyte migrationsearch neurotrophin TRK receptor signaling pathwaysearch oogenesissearch regulation of vascular permeabilitysearch axon guidancesearch T cell costimulationsearch bone resorptionsearch regulation of protein bindingsearch viral processsearch negative regulation of cysteine-type endopeptidase activity involved in apoptotic processsearch signal transductionsearch forebrain developmentsearch immune system processsearch platelet activationsearch negative regulation of anoikissearch cellular response to progesterone stimulussearch blood coagulationsearch peptidyl-tyrosine phosphorylationsearch positive regulation of ERK1 and ERK2 cascadesearch response to interleukin-1search epidermal growth factor receptor signaling pathwaysearch protein autophosphorylationsearch positive regulation of integrin activationsearch positive regulation of podosome assemblysearch intracellular signal transductionsearch fibroblast growth factor receptor signaling pathwaysearch positive regulation of canonical Wnt signaling pathwaysearch negative regulation of mitochondrial depolarizationsearch signal complex assemblysearch membrane organizationsearch innate immune responsesearch cell cyclesearch negative regulation of focal adhesion assemblysearch phosphorylationsearch regulation of bone resorptionsearch progesterone receptor signaling pathwaysearch negative regulation of apoptotic processsearch negative regulation of extrinsic apoptotic signaling pathwaysearch negative regulation of protein homooligomerizationsearch branching involved in mammary gland duct morphogenesissearch positive regulation of protein kinase B signalingsearch negative regulation of intrinsic apoptotic signaling pathwaysearch cell adhesionsearch uterus developmentsearch Fc-gamma receptor signaling pathway involved in phagocytosissearch cell migrationsearch protein tyrosine kinase activitysearch ATP bindingsearch protein kinase activitysearch non-membrane spanning protein tyrosine kinase activitysearch protein bindingsearch nucleotide bindingsearch protein domain specific bindingsearch kinase activitysearch receptor bindingsearch identical protein bindingsearch SH3/SH2 adaptor activitysearch ion channel bindingsearch transferase activity, transferring phosphorus-containing groupssearch transferase activitysearch heme bindingsearch growth factor receptor bindingsearch phosphoprotein bindingsearch ephrin receptor bindingsearch integrin bindingsearch SH2 domain bindingsearch mitochondrionsearch cytosolsearch plasma membranesearch nucleussearch mitochondrial inner membranesearch cytoplasmsearch membranesearch late endosomesearch cytoskeletonsearch lysosomesearch caveolasearch extracellular vesicular exosomesearch

Chain InterPro annotation
A Protein kinase domainsearch SH2 domainsearch Serine-threonine/tyrosine-protein kinase catalytic domainsearch SH3 domainsearch Tyrosine-protein kinase, active sitesearch Protein kinase-like domainsearch Protein kinase, ATP binding sitesearch Tyrosine-protein kinase, catalytic domainsearch