Target
Tyrosine-protein kinase JAK1 [866-1154]
Ligand
BDBM264209
Substrate
n/a
Meas. Tech.
JAK Enzymatic Assay
pH
7.3±n/a
IC50
304±n/a nM
Comments
extracted
Citation
 Grimster, NKawatkar, SKettle, JGSu, QVasbinder, MChuaqui, CE Compounds and methods for inhibiting JAK US Patent  US9714236 Publication Date 7/25/2017 
Target
Name:
Tyrosine-protein kinase JAK1 [866-1154]
Synonyms:
JAK1 | JAK1 (aa 866-1154) | JAK1A | JAK1B | JAK1_HUMAN | Tyrosine-protein kinase JAK1 | Tyrosine-protein kinase JAK1 (aa 866-1154)
Type:
Protein
Mol. Mass.:
33185.74
Organism:
Homo sapiens (Human)
Description:
P23458[866-1154]
Residue:
289
Sequence:
DPTHFEKRFLKRIRDLGEGHFGKVELCRYDPEGDNTGEQVAVKSLKPESGGNHIADLKKEIEILRNLYHENIVKYKGICTEDGGNGIKLIMEFLPSGSLKEYLPKNKNKINLKQQLKYAVQICKGMDYLGSRQYVHRDLAARNVLVESEHQVKIGDFGLTKAIETDKEYYTVKDDRDSPVFWYAPECLMQSKFYIASDVWSFGVTLHELLTYCDSDSSPMALFLKMIGPTHGQMTVTRLVNTLKEGKRLPCPPNCPDEVYQLMRKCWEFQPSNRTSFQNLIEGFEALLK
  
Inhibitor
Name:
BDBM264209
Synonyms:
(2R)-2-[(3R)-3,4- dimethylpiperazin-1- yl]-N-(3-{2-[(3-methoxy- 1-methyl-1H- pyrazol-4-yl)amino] pyrimidin-4-yl}- 1H-indol-7-yl)propanamide | US10167276, Example 30 | US10654835, Example 30 | US11247983, Example 30 | US9714236, 30
Type:
Small organic molecule
Emp. Form.:
C26H33N9O2
Mol. Mass.:
503.5993
SMILES:
COc1nn(C)cc1Nc1nccc(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)[C@H](C)C3)cccc12 |r|
Structure:
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