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Ligands
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960 1-[(6-chloroimidazo[1,2-B]pyridazin-3-yl)sulfonyl]-6-(1-methyl-1h-pyrazol-4-yl)-1h-pyrazolo[4,3-B]pyridine
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Code : 5Z0S   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal structure of FGFR1 kinase domain in complex with a novel inhibitor
Release Data : 2018-12-26
Compound :
mol_id molecule chains synonym
1 Fibroblast growth factor receptor 1 A,B FGFR-1,Basic fibroblast growth factor receptor 1,bFGF-R-1,Fms-like tyrosine kinase 2,FLT-2,N-sam,Proto-oncogene c-Fgr
ec: 2.7.10.1
fragment: 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 : Liu, Q., Xu, Y.
Keywords : FGFR1 inhibitor, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.4500 Å )
Citation :

Structure-Based Discovery of a Series of 5H-Pyrrolo[2,3-b]pyrazine FGFR Kinase Inhibitors

Jiang, A.,Liu, Q.,Wang, R.  et al.
(2018)  Molecules  23

PubMed: 29562726
DOI: 10.3390/molecules23030698

Chain : A, B
UniProt : P11362 (FGFR1_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 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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