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TargetTyrosine-protein kinase JAK1
LigandBDBM50243842
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1672940
IC50 19±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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BDBM50243842
n/a
NameBDBM50243842
Synonyms:CHEMBL4066404
TypeSmall organic molecule
Emp. Form.C17H27N5O2S
Mol. Mass.365.494
SMILESCCCCN(C)S(=O)(=O)C[C@H]1C[C@H](C1)N(C)c1ncnc2[nH]ccc12 |r,wD:12.14,10.9,(20.04,-11.87,;18.7,-12.63,;17.37,-11.86,;16.03,-12.62,;14.69,-11.84,;14.7,-10.3,;13.35,-12.61,;14.12,-13.94,;12.58,-13.93,;12.02,-11.85,;10.69,-12.62,;9.2,-12.23,;8.81,-13.72,;10.3,-14.11,;7.48,-14.5,;6.15,-13.73,;7.49,-16.04,;6.16,-16.81,;6.15,-18.35,;7.49,-19.12,;8.83,-18.34,;10.3,-18.81,;11.2,-17.56,;10.29,-16.31,;8.82,-16.8,)|
Structure
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