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TargetTyrosine-protein kinase JAK1
LigandBDBM246853
Substrate/Competitorn/a
Meas. Tech.JAK1 Assay
IC50<300±0 nM
Citation Li, YBurns, DM Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors US Patent US9708333 Publication Date 7/18/2017
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:
BDBM246853
n/a
NameBDBM246853
Synonyms:4-[3-(cyanomethyl)- 3-(3',5'-dimethyl- 1H,1'H-4,4'- bipyrazol-1- yl)azetidin-1-yl]-2,5- difluoro-N-[(1S)- 2,2,2-trifluoro-1- methylethyl] benzamide | US10053465, 2 | US10065963, Compound 2 | US10125150, Example 2 | US10336759, # 2 | US10435392, Example 17 | US10479803, Example 2D | US10519163, Example 2 | US10675284, Example 2 | US11084822, Example 2 | US11130767, # 2 | US11136326, Example 2 | US11304949, Compound 4 | US11324749, Comp. No. 4 | US11591318, Example 7 | US11596632, Comp. No. 4 | US20240058343, Compound 4 | US9732097, Example 2 | US9926301, Example 17
TypeSmall organic molecule
Emp. Form.C23H22F5N7O
Mol. Mass.507.4591
SMILESC[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(cn1)-c1c(C)n[nH]c1C)C(F)(F)F |r|
Structure
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