Reaction Details |
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Target | Tyrosine-protein kinase JAK1 |
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Ligand | BDBM50035810 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1441072 (CHEMBL3377594) |
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IC50 | 9.0±n/a nM |
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Citation | Duan, JJ; Lu, Z; Jiang, B; Yang, BV; Doweyko, LM; Nirschl, DS; Haque, LE; Lin, S; Brown, G; Hynes, J; Tokarski, JS; Sack, JS; Khan, J; Lippy, JS; Zhang, RF; Pitt, S; Shen, G; Pitts, WJ; Carter, PH; Barrish, JC; Nadler, SG; Salter-Cid, LM; McKinnon, M; Fura, A; Schieven, GL; Wrobleski, ST Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors. Bioorg Med Chem Lett24:5721-6 (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 |
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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BDBM50035810 |
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n/a |
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Name | BDBM50035810 |
Synonyms: | CHEMBL3359927 |
Type | Small organic molecule |
Emp. Form. | C14H17FN4O |
Mol. Mass. | 276.3094 |
SMILES | C[C@]1(F)CCC[C@H]1Nc1c(cnn2cccc12)C(N)=O |r| |
Structure |
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