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Ligands
Code Name Link
C4F 3-(3-methoxybenzyl)-1h-pyrrolo[2,3-B]pyridine
Code : 3C4F   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE
Title : FGFR TYROSINE KINASE DOMAIN IN COMPLEX WITH 3-(3-methoxybenzyl)-7-azaindole
Release Data : 2008-02-26
Compound :
mol_id molecule chains synonym
1 Basic fibroblast growth factor receptor 1 A,B FGFR-1, bFGF-R, Fms-like tyrosine kinase 2, c-fgr, CD331 antigen
ec: 2.7.10.1
fragment: KINASE DOMAIN
mutation: C488A
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Escherichia coli  (taxid:562)
gene: FGFR1, FGFBR, FLG, FLT2
expression_system_strain: BL21(DE3)RIL
expression_system_vector_type: vector
expression_system_vector: pET29a
Authors : Zhang, K.Y.J., Wang, W.
Keywords : FIBROBLAST GROWTH FACTOR RECEPTOR, TYROSINE KINASE DOMAIN, RECEPTOR TYROSINE KINASE, FGFR1, FGFR, Alternative splicing, ATP-binding, Chromosomal rearrangement, Disease mutation, Dwarfism, Glycoprotein, Heparin-binding, Immunoglobulin domain, Kallmann syndrome, Membrane, Nucleotide-binding, Phosphoprotein, Polymorphism, Transferase, Transmembrane, Tyrosine-protein kinase
Exp. method : X-RAY DIFFRACTION ( 2.07 Å )
Citation :

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

Tsai, J.,Lee, J.T.,Wang, W.  et al.
(2008)  Proc.Natl.Acad.Sci.Usa  105 : 3041 - 3046

PubMed: 18287029
DOI: 10.1073/pnas.0711741105

Chain : A, B
UniProt : P11362 (FGFR1_HUMAN)
Reaction : Reaction=ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein]; Xref=Rhea:RHEA:10596, Rhea:RHEA-COMP:10136, Rhea:RHEA- COMP:10137, ChEBI:CHEBI:15378, ChEBI:CHEBI:30616, ChEBI:CHEBI:46858, ChEBI:CHEBI:82620, ChEBI:CHEBI:456216; EC=2.7.10.1; Evidence={ECO:0000255|PROSITE-ProRule:PRU10028, ECO:0000269|PubMed:1379697, ECO:0000269|PubMed:15117958, ECO:0000269|PubMed:18480409, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:19665973, ECO:0000269|PubMed:20133753, ECO:0000269|PubMed:8622701};