Reaction Details |
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Target | Tyrosine-protein kinase JAK2 [831-1132] |
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Ligand | BDBM264181 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Enzyme Inhibition Assay |
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IC50 | 10400±n/a nM |
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Citation | Astrand, AB; Grimster, NP; Kawatkar, S; Kettle, JG; Nilsson, MK; Ruston, L; Su, Q; Vasbinder, M; Winter-Holt, JJ; Woessner, RD; Chuaqui, CE; McCabe, J Compounds and methods for inhibiting JAK US Patent US10654835 Publication Date 5/19/2020 |
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More Info.: | Get all data from this article, Assay Method |
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Tyrosine-protein kinase JAK2 [831-1132] |
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Name: | Tyrosine-protein kinase JAK2 [831-1132] |
Synonyms: | JAK2 | JAK2 (aa 831-1132) | JAK2_HUMAN | Tyrosine-protein kinase JAK2 (aa 831-1132) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 35337.99 |
Organism: | Homo sapiens (Human) |
Description: | O60674[831-1132] |
Residue: | 302 |
Sequence: | GFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEE
HLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDH
IKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKV
KEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQ
GQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNM
AG
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BDBM264181 |
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n/a |
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Name | BDBM264181 |
Synonyms: | (2R)-2-[(3S)-3,4- dimethylpiperazin-1- yl]-N-(3-{5-fluoro-2- [(3-methoxy-1- methyl-1H-pyrazol-4- yl)amino]pyrimidin- 4-yl}-1H-indol-7- yl)propanamide | US10167276, Example 5 | US10654835, Example 5 | US11247983, Example 5 | US9714236, 5 |
Type | Small organic molecule |
Emp. Form. | C26H32FN9O2 |
Mol. Mass. | 521.5898 |
SMILES | COc1nn(C)cc1Nc1ncc(F)c(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)[C@@H](C)C3)cccc12 |r| |
Structure |
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