| Reaction Details |
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 | Report a problem with these data |
| Target | Tyrosine-protein kinase JAK1 |
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| Ligand | BDBM50315244 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_625434 (CHEMBL1116983) |
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| IC50 | 390±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 |
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| Synonyms: | JAK-1 | JAK1 | JAK1A | JAK1B | JAK1_HUMAN | Janus kinase 1 | Janus kinase 1 (JAK1) | Janus kinase 1 JAK1 |
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| Type: | Protein |
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| Mol. Mass.: | 133293.73 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P23458 |
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| Residue: | 1154 |
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| 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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| BDBM50315244 |
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| n/a |
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| Name | BDBM50315244 |
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| Synonyms: | CHEMBL1091565 | morpholino(4-(3-(3,4,5-trimethoxyphenyl)quinoxalin-5-yl)phenyl)methanone |
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| Type | Small organic molecule |
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| Emp. Form. | C28H27N3O5 |
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| Mol. Mass. | 485.5311 |
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| SMILES | COc1cc(cc(OC)c1OC)-c1cnc2cccc(-c3ccc(cc3)C(=O)N3CCOCC3)c2n1 |
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| Structure | 
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