Reaction Details |
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Target | Tyrosine-protein kinase JAK1 |
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Ligand | BDBM50315235 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_625434 (CHEMBL1116983) |
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IC50 | 190±n/a nM |
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Citation | Pissot-Soldermann, C; Gerspacher, M; Furet, P; Gaul, C; Holzer, P; McCarthy, C; Radimerski, T; Regnier, CH; Baffert, F; Drueckes, P; Tavares, GA; Vangrevelinghe, E; Blasco, F; Ottaviani, G; Ossola, F; Scesa, J; Reetz, J Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors. Bioorg Med Chem Lett20:2609-13 (2010) [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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BDBM50315235 |
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n/a |
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Name | BDBM50315235 |
Synonyms: | (4-(8-(3-fluoro-4-(morpholinomethyl)phenyl)quinoxalin-2-yl)-2-methylphenyl)(morpholino)methanone | CHEMBL1092840 |
Type | Small organic molecule |
Emp. Form. | C31H31FN4O3 |
Mol. Mass. | 526.6012 |
SMILES | Cc1cc(ccc1C(=O)N1CCOCC1)-c1cnc2cccc(-c3ccc(CN4CCOCC4)c(F)c3)c2n1 |
Structure |
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