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TargetTyrosine-protein kinase JAK1
LigandBDBM391025
Substrate/Competitorn/a
Meas. Tech.Biochemical HTRF Assay
IC50 0.070±n/a nM
Citation Childers, MLFuller, PGuerin, DKatz, JDPu, QScott, METhompson, CFMartinez, MFalcone, DTorres, LDeng, YKurukulasuriya, RZeng, HBai, YKong, NLiu, YZheng, Z Geminally substituted cyanoethylpyrazolo pyridones as Janus kinase inhibitors US Patent US9957264 Publication Date 5/1/2018
More Info.:Get all data from this article,  Assay Method
 
Tyrosine-protein kinase JAK1
Name:Tyrosine-protein kinase JAK1
Synonyms:JAK-1 | JAK1 | JAK1A | JAK1B | JAK1_HUMAN | Janus kinase 1 | Janus kinase 1 (JAK1) | Janus kinase 1 JAK1
Type:Protein
Mol. Mass.:133293.73
Organism:Homo sapiens (Human)
Description:P23458
Residue:1154
Sequence:
MQYLNIKEDCNAMAFCAKMRSSKKTEVNLEAPEPGVEVIFYLSDREPLRLGSGEYTAEEL
CIRAAQACRISPLCHNLFALYDENTKLWYAPNRTITVDDKMSLRLHYRMRFYFTNWHGTN
DNEQSVWRHSPKKQKNGYEKKKIPDATPLLDASSLEYLFAQGQYDLVKCLAPIRDPKTEQ
DGHDIENECLGMAVLAISHYAMMKKMQLPELPKDISYKRYIPETLNKSIRQRNLLTRMRI
NNVFKDFLKEFNNKTICDSSVSTHDLKVKYLATLETLTKHYGAEIFETSMLLISSENEMN
WFHSNDGGNVLYYEVMVTGNLGIQWRHKPNVVSVEKEKNKLKRKKLENKHKKDEEKNKIR
EEWNNFSYFPEITHIVIKESVVSINKQDNKKMELKLSSHEEALSFVSLVDGYFRLTADAH
HYLCTDVAPPLIVHNIQNGCHGPICTEYAINKLRQEGSEEGMYVLRWSCTDFDNILMTVT
CFEKSEQVQGAQKQFKNFQIEVQKGRYSLHGSDRSFPSLGDLMSHLKKQILRTDNISFML
KRCCQPKPREISNLLVATKKAQEWQPVYPMSQLSFDRILKKDLVQGEHLGRGTRTHIYSG
TLMDYKDDEGTSEEKKIKVILKVLDPSHRDISLAFFEAASMMRQVSHKHIVYLYGVCVRD
VENIMVEEFVEGGPLDLFMHRKSDVLTTPWKFKVAKQLASALSYLEDKDLVHGNVCTKNL
LLAREGIDSECGPFIKLSDPGIPITVLSRQECIERIPWIAPECVEDSKNLSVAADKWSFG
TTLWEICYNGEIPLKDKTLIEKERFYESRCRPVTPSCKELADLMTRCMNYDPNQRPFFRA
IMRDINKLEEQNPDIVSEKKPATEVDPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDN
TGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICTEDGGNGIKLIMEFLP
SGSLKEYLPKNKNKINLKQQLKYAVQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIG
DFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLMQSKFYIASDVWSFGVTLHELLTYCDS
DSSPMALFLKMIGPTHGQMTVTRLVNTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRT
SFQNLIEGFEALLK
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  Blast E-value cutoff:
BDBM391025
n/a
NameBDBM391025
Synonyms:(2S,5S)-tert-butyl 5-(3-((4- ((1H-1,2,3-triazol-1- yl)methyl)phenyl)amino)- 4-oxo-4,5-dihydro-1H- pyrazolo[4,3-c]pyridin-1- yl)-5-(cyanomethyl) tetrahydro-2H-pyran-2- carboxylate (from I-14-1A) | US9957264, Example 5-96
TypeSmall organic molecule
Emp. Form.C27H30N8O4
Mol. Mass.530.5783
SMILESCC(C)(C)OC(=O)[C@@H]1CC[C@](CC#N)(CO1)n1nc(Nc2ccc(Cn3ccnn3)cc2)c2c1cc[nH]c2=O |r|
Structure
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