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Target
Tyrosine-protein kinase JAK2 [831-1132]
Ligand
BDBM264194
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
2530±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  US10654835 Publication Date 5/19/2020 
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:
BDBM264194
Synonyms:
(2R)-2-[4-(2- hydroxyethyl)piperazin- 1-yl]-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-yl) amino]-5-methylpyrimidin- 4-yl}-1H-indol-7- yl)propanamide | US10167276, Example 15 | US10654835, Example 15 | US11247983, Example 15 | US9714236, 15
Type:
Small organic molecule
Emp. Form.:
C27H35N9O3
Mol. Mass.:
533.6253
SMILES:
COc1nn(C)cc1Nc1ncc(C)c(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(CCO)CC3)cccc12 |r|
Structure:
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