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Target
Tyrosine-protein kinase JAK2 [808-1132]
Ligand
BDBM264224
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Studies
IC50
1950±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:
BDBM264224
Synonyms:
(2R)-N-(3-{2-[(3- Methoxy-1-methyl- 1H-pyrazol-4-yl)amino]-5- methylpyrimidin-4-yl}- 1H-indol-7-yl)- 2-(4-methylpiperazin-1- yl)butanamide | US10167276, Example 44 | US10654835, Example 44 | US11247983, Example 44 | US9714236, 44
Type:
Small organic molecule
Emp. Form.:
C27H35N9O2
Mol. Mass.:
517.6259
SMILES:
CC[C@@H](N1CCN(C)CC1)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cn(C)nc2OC)ncc1C |r|
Structure:
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