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TargetTyrosine-protein kinase JAK2
LigandBDBM50337334
Substrate/Competitorn/a
Meas. Tech.ChEMBL_726514 (CHEMBL1685409)
IC50 1±n/a nM
Citation Harikrishnan, LSKamau, MGWan, HInghrim, JAZimmermann, KSang, XMastalerz, HAJohnson, WLZhang, GLombardo, LJPoss, MATrainor, GLTokarski, JSLorenzi, MVYou, DGottardis, MMBaldwin, KFLippy, JNirschl, DSQiu, RMiller, AVKhan, JSack, JSPurandare, AV Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3. Bioorg Med Chem Lett21:1425-8 (2011) [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:
BDBM50337334
n/a
NameBDBM50337334
Synonyms:2-(4-chloro-2,6-difluorophenyl)-1-(4-(4-(5-methyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)piperazin-1-yl)ethanone | CHEMBL1682388
TypeSmall organic molecule
Emp. Form.C22H21ClF2N8O
Mol. Mass.486.905
SMILESCc1cc(Nc2nc(nn3cccc23)N2CCN(CC2)C(=O)Cc2c(F)cc(Cl)cc2F)[nH]n1
Structure
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