| Reaction Details |
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 | Report a problem with these data |
| Target | Tyrosine-protein kinase JAK1 |
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| Ligand | BDBM50393751 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_856879 (CHEMBL2160360) |
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| Ki | 2±n/a nM |
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| Citation |  Zak, M; Mendonca, R; Balazs, M; Barrett, K; Bergeron, P; Blair, WS; Chang, C; Deshmukh, G; Devoss, J; Dragovich, PS; Eigenbrot, C; Ghilardi, N; Gibbons, P; Gradl, S; Hamman, C; Hanan, EJ; Harstad, E; Hewitt, PR; Hurley, CA; Jin, T; Johnson, A; Johnson, T; Kenny, JR; Koehler, MF; Bir Kohli, P; Kulagowski, JJ; Labadie, S; Liao, J; Liimatta, M; Lin, Z; Lupardus, PJ; Maxey, RJ; Murray, JM; Pulk, R; Rodriguez, M; Savage, S; Shia, S; Steffek, M; Ubhayakar, S; Ultsch, M; van Abbema, A; Ward, SI; Xiao, L; Xiao, Y Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. J Med Chem55:6176-93 (2012) [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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| BDBM50393751 |
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| n/a |
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| Name | BDBM50393751 |
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| Synonyms: | CHEMBL2159204 |
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| Type | Small organic molecule |
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| Emp. Form. | C14H15F2N5 |
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| Mol. Mass. | 291.2992 |
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| SMILES | Cc1nc2cnc3[nH]ccc3c2n1C1CCNCC1(F)F |
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| Structure | 
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