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Target
Tyrosine-protein kinase JAK2 [831-1132]
Ligand
BDBM264225
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
790±n/a nM
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  US11247983 Publication Date 2/15/2022 
Target
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:
GFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG
  
Inhibitor
Name:
BDBM264225
Synonyms:
(2R)-3-methoxy-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)propanamide | US10167276, Example 45 | US10654835, Example 45 | US11247983, Example 45 | US9714236, 45
Type:
Small organic molecule
Emp. Form.:
C27H35N9O3
Mol. Mass.:
533.6253
SMILES:
COC[C@@H](N1CCN(C)CC1)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cn(C)nc2OC)ncc1C |r|
Structure:
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