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TargetTyrosine-protein kinase JAK1
LigandBDBM159749
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1672940
IC50 14±n/a nM
Citation Vazquez MLKaila NStrohbach JWTrzupek JDBrown MFFlanagan MEMitton-Fry MJJohnson TATenBrink REArnold EPBasak AHeasley SEKwon SLangille JParikh MDGriffin SHCasavant JMDuclos BAFenwick AEHarris TMHan SCaspers NDowty MEYang XBanker MEHegen MSymanowicz PTLi LWang LLin THJussif JClark JDTelliez JBRobinson RPUnwalla R Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem 61:1130-1152 (2018) [PubMed]  Article
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 | 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:
BDBM159749
n/a
NameBDBM159749
Synonyms:US9035074, 3
TypeSmall organic molecule
Emp. Form.C15H23N5O2S
Mol. Mass.337.44
SMILESCC(C)CS(=O)(=O)N[C@H]1C[C@H](C1)N(C)c1ncnc2[nH]ccc12 |r,wD:10.12,8.7,(5.44,2.67,;3.95,2.27,;3.55,.79,;2.86,3.36,;1.37,2.96,;1.37,4.5,;-.11,3.36,;.97,1.48,;-.51,1.08,;-1.85,1.85,;-2.62,.51,;-1.28,-.26,;-4.1,.12,;-5.19,1.2,;-4.1,-1.42,;-5.44,-2.19,;-5.44,-3.73,;-4.1,-4.5,;-2.77,-3.73,;-1.31,-4.21,;-.4,-2.96,;-1.31,-1.72,;-2.77,-2.19,)|
Structure
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