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TargetTyrosine-protein kinase JAK3
LigandBDBM26369
Substrate/CompetitorBDBM17296
Meas. Tech.HTRF Kinase Inhibition Assay
IC50>25000±n/a nM
Citation DiMauro, EFNewcomb, JNunes, JJBemis, JEBoucher, CChai, LChaffee, SCDeak, HLEpstein, LFFaust, TGallant, PGore, AGu, YHenkle, BHsieh, FHuang, XKim, JLLee, JHMartin, MWMcGowan, DCMetz, DMohn, DMorgenstern, KAOliveira-dos-Santos, APatel, VFPowers, DRose, PESchneider, STomlinson, SATudor, YYTurci, SMWelcher, AAZhao, HZhu, LZhu, X Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. J Med Chem51:1681-94 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Tyrosine-protein kinase JAK3
Name:Tyrosine-protein kinase JAK3
Synonyms:JAK-3 | JAK3 | JAK3_HUMAN | Janus kinase 3 | Janus kinase 3 (JAK3) | Janus kinase 3 JAK3 | L-JAK | Leukocyte janus kinase
Type:Protein
Mol. Mass.:125111.08
Organism:Homo sapiens (Human)
Description:P52333
Residue:1124
Sequence:
MAPPSEETPLIPQRSCSLLSTEAGALHVLLPARGPGPPQRLSFSFGDHLAEDLCVQAAKA
SGILPVYHSLFALATEDLSCWFPPSHIFSVEDASTQVLLYRIRFYFPNWFGLEKCHRFGL
RKDLASAILDLPVLEHLFAQHRSDLVSGRLPVGLSLKEQGECLSLAVLDLARMAREQAQR
PGELLKTVSYKACLPPSLRDLIQGLSFVTRRRIRRTVRRALRRVAACQADRHSLMAKYIM
DLERLDPAGAAETFHVGLPGALGGHDGLGLLRVAGDGGIAWTQGEQEVLQPFCDFPEIVD
ISIKQAPRVGPAGEHRLVTVTRTDNQILEAEFPGLPEALSFVALVDGYFRLTTDSQHFFC
KEVAPPRLLEEVAEQCHGPITLDFAINKLKTGGSRPGSYVLRRSPQDFDSFLLTVCVQNP
LGPDYKGCLIRRSPTGTFLLVGLSRPHSSLRELLATCWDGGLHVDGVAVTLTSCCIPRPK
EKSNLIVVQRGHSPPTSSLVQPQSQYQLSQMTFHKIPADSLEWHENLGHGSFTKIYRGCR
HEVVDGEARKTEVLLKVMDAKHKNCMESFLEAASLMSQVSYRHLVLLHGVCMAGDSTMVQ
EFVHLGAIDMYLRKRGHLVPASWKLQVVKQLAYALNYLEDKGLPHGNVSARKVLLAREGA
DGSPPFIKLSDPGVSPAVLSLEMLTDRIPWVAPECLREAQTLSLEADKWGFGATVWEVFS
GVTMPISALDPAKKLQFYEDRQQLPAPKWTELALLIQQCMAYEPVQRPSFRAVIRDLNSL
ISSDYELLSDPTPGALAPRDGLWNGAQLYACQDPTIFEERHLKYISQLGKGNFGSVELCR
YDPLGDNTGALVAVKQLQHSGPDQQRDFQREIQILKALHSDFIVKYRGVSYGPGRQSLRL
VMEYLPSGCLRDFLQRHRARLDASRLLLYSSQICKGMEYLGSRRCVHRDLAARNILVESE
AHVKIADFGLAKLLPLDKDYYVVREPGQSPIFWYAPESLSDNIFSRQSDVWSFGVVLYEL
FTYCDKSCSPSAEFLRMMGCERDVPALCRLLELLEEGQRLPAPPACPAEVHELMKLCWAP
SPQDRPSFSALGPQLDMLWSGSRGCETHAFTAHPEGKHHSLSFS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM26369
BDBM17296
NameBDBM26369
Synonyms:4-methyl-3-N-(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-5-yl)-1-N-[3-(trifluoromethyl)benzene]benzene-1,3-dicarboxamide | Aminopyrimidine amide, 13b
TypeSmall organic molecule
Emp. Form.C31H30F3N7O2
Mol. Mass.589.6108
SMILESCN1CCN(CC1)c1ccc(Nc2ncc(NC(=O)c3cc(NC(=O)c4cccc(c4)C(F)(F)F)ccc3C)cn2)cc1
Structure
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