Reaction Details |
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Target | Tyrosine-protein kinase JAK1 |
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Ligand | BDBM246877 |
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Substrate/Competitor | n/a |
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Meas. Tech. | PI3K Enzyme Assay |
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IC50 | <10±n/a nM |
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Citation | Qiao, L; Weng, L; Meloni, D; Jia, Z; Wang, J; Zhou, J Salts and processes of preparing a PI3K inhibitor US Patent US10336759 Publication Date 7/2/2019 |
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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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BDBM246877 |
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n/a |
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Name | BDBM246877 |
Synonyms: | 4-{3-(cyanomethyl)- 3-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)- 1H-pyrazol-1- yl]azetidin-1-yl}-2,5- difluoro-N-[(1S)- 2,2,2-trifluoro-1- methylethyl] benzamide | US10053465, 16 | US10065963, Compound 16 | US10125150, Example 16 | US10336759, # 16 | US10479803, Example 16 | US10519163, Example 16 | US10675284, Example 16 | US11084822, Example 16 | US11130767, # 16 | US11136326, Example 16 | US11214573, Example 28 | US11304949, Compound 16 | US11324749, Comp. No. 16 | US11406640, Comp. No. 16 | US11918581, Compound 16 | US20240058343, Compound 16 | US9611269, Example 28 | US9732097, Example 16 |
Type | Small organic molecule |
Emp. Form. | C24H19F5N8O |
Mol. Mass. | 530.4527 |
SMILES | C[C@H](NC(=O)c1cc(F)c(cc1F)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12)C(F)(F)F |r| |
Structure |
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