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TargetTyrosine-protein kinase JAK1
LigandBDBM50243909
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1672940
IC50 11±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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BDBM50243909
n/a
NameBDBM50243909
Synonyms:CHEMBL4066876
TypeSmall organic molecule
Emp. Form.C16H23N5O2S
Mol. Mass.349.451
SMILESCN([C@@H]1C[C@H](CS(=O)(=O)NCC2CC2)C1)c1ncnc2[nH]ccc12 |r,wD:2.1,4.4,(6.35,-12.54,;7.68,-13.31,;9.01,-12.53,;9.41,-11.04,;10.9,-11.43,;12.23,-10.66,;13.56,-11.42,;14.32,-12.75,;12.79,-12.74,;14.89,-10.65,;16.23,-11.42,;17.56,-10.65,;19.1,-10.65,;18.33,-9.31,;10.5,-12.92,;7.69,-14.85,;6.36,-15.62,;6.36,-17.16,;7.69,-17.93,;9.03,-17.15,;10.5,-17.62,;11.4,-16.37,;10.49,-15.13,;9.02,-15.61,)|
Structure
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