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Target
Tyrosine-protein kinase JAK2 [808-1132]
Ligand
BDBM264181
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Studies
IC50
10400±n/a nM
Citation
 Astrand, A; Grimster, N; 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  US10167276 Publication Date 1/1/2019 
Target
Name:
Tyrosine-protein kinase JAK2 [808-1132]
Synonyms:
JAK2 | JAK2 (aa 808-1132) | JAK2_HUMAN | Tyrosine-protein kinase JAK2 JH1 (808-1132)
Type:
Protein
Mol. Mass.:
39171.39
Organism:
Homo sapiens (Human)
Description:
O60674[808-1132]
Residue:
335
Sequence:
FRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
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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