Reaction Details |
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Target | Tyrosine-protein kinase JAK1 |
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Ligand | BDBM50131843 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1526612 (CHEMBL3635831) |
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Kd | 2800±n/a nM |
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Citation | Wurz, RP; Pettus, LH; Ashton, K; Brown, J; Chen, JJ; Herberich, B; Hong, FT; Hu-Harrington, E; Nguyen, T; St Jean, DJ; Tadesse, S; Bauer, D; Kubryk, M; Zhan, J; Cooke, K; Mitchell, P; Andrews, KL; Hsieh, F; Hickman, D; Kalyanaraman, N; Wu, T; Reid, DL; Lobenhofer, EK; Andrews, DA; Everds, N; Guzman, R; Parsons, AT; Hedley, SJ; Tedrow, J; Thiel, OR; Potter, M; Radinsky, R; Beltran, PJ; Tasker, AS Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett6:987-92 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase JAK1 |
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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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BDBM50131843 |
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n/a |
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Name | BDBM50131843 |
Synonyms: | CHEMBL3633152 |
Type | Small organic molecule |
Emp. Form. | C28H30N6O4 |
Mol. Mass. | 514.5756 |
SMILES | COc1cc(OCCN(C)C)ccc1Nc1ncc2c(C)cc(=O)n(-c3cccc(NC(=O)C=C)c3)c2n1 |
Structure |
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