Reaction Details |
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Target | Tyrosine-protein kinase JAK1 |
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Ligand | BDBM50545945 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2013351 (CHEMBL4666929) |
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Ki | 0.210000±n/a nM |
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Citation | Zak, M; Hanan, EJ; Lupardus, P; Brown, DG; Robinson, C; Siu, M; Lyssikatos, JP; Romero, FA; Zhao, G; Kellar, T; Mendonca, R; Ray, NC; Goodacre, SC; Crackett, PH; McLean, N; Hurley, CA; Yuen, PW; Cheng, YX; Liu, X; Liimatta, M; Kohli, PB; Nonomiya, J; Salmon, G; Buckley, G; Lloyd, J; Gibbons, P; Ghilardi, N; Kenny, JR; Johnson, A Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling. Bioorg Med Chem Lett29:1522-1531 (2019) [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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BDBM50545945 |
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n/a |
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Name | BDBM50545945 |
Synonyms: | CHEMBL4777342 |
Type | Small organic molecule |
Emp. Form. | C18H13ClF2N6O2 |
Mol. Mass. | 418.785 |
SMILES | Cn1cc(NC(=O)c2cnn3cccnc23)c(n1)-c1cc(Cl)ccc1OC(F)F |
Structure |
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