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TargetTyrosine-protein kinase JAK2
LigandBDBM50031747
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1432585 (CHEMBL3388144)
IC50 138±n/a nM
Citation Menet, CJFletcher, SRVan Lommen, GGeney, RBlanc, JSmits, KJouannigot, NDeprez, Pvan der Aar, EMClement-Lacroix, PLepescheux, LGalien, RVayssiere, BNelles, LChristophe, TBrys, RUhring, MCiesielski, FVan Rompaey, L Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem57:9323-42 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase JAK2
Name:Tyrosine-protein kinase JAK2
Synonyms:JAK-2 | JAK2 | JAK2_HUMAN | Janus kinase 2 | Janus kinase 2 (JAK2) | Janus kinase 2 (a protein tyrosine kinase)
Type:Protein
Mol. Mass.:130684.68
Organism:Homo sapiens (Human)
Description:O60674
Residue:1132
Sequence:
MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSG
EYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYF
PRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLG
MAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQF
SQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSR
GKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLR
EALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQT
GLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNC
YQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKI
RNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASM
MSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWA
MHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVP
PECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAEL
ANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRD
PTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIE
ILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQI
CKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFW
YAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIE
LLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50031747
n/a
NameBDBM50031747
Synonyms:CHEMBL3360318
TypeSmall organic molecule
Emp. Form.C17H16N4O2
Mol. Mass.308.3345
SMILESCOc1ccc(cc1)-c1cccc2nc(NC(=O)C3CC3)nn12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: