Brand  (β version)

PDB ID: 4F65

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Ligands
Code Name Style Show Link
0S9 5-bromo-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]-N~4~-[3-(2-phenylethyl)-1h-pyrazol-5-yl]pyrimidine-2,4-diamine PoSSuM
EDO 1,2-ethanediol PoSSuM
SO4 Sulfate ion PoSSuM
Non-standard Residues
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Glycosylation
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Structure summary

Code : 4F65   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8
Release Data : 2012-06-06
Compound :
mol_id molecule chains synonym
1 Fibroblast growth factor receptor 1 A,B FGFR-1, Basic fibroblast growth factor receptor 1, BFGFR, bFGF-R-1, Fms-like tyrosine kinase 2, FLT-2, N-sam, Proto-oncogene c-Fgr
ec: 2.7.10.1
fragment: kinase domain (UNP residues 458-765)
mutation: C488A, C584S
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FGFR1, BFGFR, CEK, FGFBR, FLG, FLT2, HBGFR
Authors : Norman, R.A., Breed, J., Ogg, D.
Keywords : kinase, ATP binding, phosphorylation, trans-membrane, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.260 Å )
Citation :

Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.

Norman, R.A.,Schott, A.K.,Andrews, D.M.  et al.
(2012)  J.Med.Chem.  55 : 5003 - 5012

PubMed: 22612866
DOI: 10.1021/jm3004043

Reaction

Chain : A, B
UniProt : P11362 (FGFR1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H(+) 2.7.10.1 PROSITE-ProRule:PRU10028, PubMed:1379697, PubMed:15117958, PubMed:18480409, PubMed:19224897, PubMed:19665973, PubMed:20133753, PubMed:8622701
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