| Reaction Details |
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 | Report a problem with these data |
| Target | Tyrosine-protein kinase JAK1 |
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| Ligand | BDBM103737 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1432584 (CHEMBL3388143) |
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| IC50 | 27±n/a nM |
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| Citation |  Menet, CJ; Fletcher, SR; Van Lommen, G; Geney, R; Blanc, J; Smits, K; Jouannigot, N; Deprez, P; van der Aar, EM; Clement-Lacroix, P; Lepescheux, L; Galien, R; Vayssiere, B; Nelles, L; Christophe, T; Brys, R; Uhring, M; Ciesielski, F; Van Rompaey, L Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634. J Med Chem57:9323-42 (2014) [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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| BDBM103737 |
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| n/a |
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| Name | BDBM103737 |
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| Synonyms: | US10206907, Compound 234 | US11000528, Cpd # 11 | US8563545, 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H23F2N5O |
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| Mol. Mass. | 411.4477 |
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| SMILES | FC1(F)CCN(Cc2ccc(cc2)-c2cccc3nc(NC(=O)C4CC4)nn23)CC1 |
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| Structure | 
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