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Ligands
Code Name Style Show Link
JAK 2-methyl-1-(piperidin-4-yl)-1,6-dihydroimidazo[4,5-D]pyrrolo[2,3-B]pyridine
Non-standard Residues
Code Name Show
PTR O-phosphotyrosine
Glycosylation
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Modification
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Code : 4F09   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Discovery and Optimization of C-2 Methyl Imidazo-pyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2
Release Data : 2012-07-04
Compound :
mol_id molecule chains synonym
1 Tyrosine-protein kinase JAK2 A Janus kinase 2, JAK-2
ec: 2.7.10.2
fragment: UNP residues 833-1132
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human Spodoptera frugiperda  (taxid:7108)
gene: JAK2 kinase domain
expression_system_common: Fall armyworm
expression_system_vector_type: plasmid
Authors : Murray, J.M.
Keywords : JAK2, kinase domain, JH1 domain, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 2.40 Å )
Citation :

Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2.

Zak, M.,Mendonca, R.,Balazs, M.  et al.
(2012)  J.Med.Chem.  55 : 6176 - 6193

PubMed: 22698084
DOI: 10.1021/jm300628c

Chain : A
UniProt : O60674 (JAK2_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein] 2.7.10.2 PROSITE-ProRule:PRU10028, PubMed:7615558, PubMed:9618263
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