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Target
Tyrosine-protein kinase JAK1 [866-1154]
Ligand
BDBM264238
Substrate
n/a
Meas. Tech.
JAK Enzymatic Assay
pH
7.3±n/a
IC50
17.0±n/a nM
Comments
extracted
Citation
 Grimster, N; Kawatkar, S; Kettle, JG; Su, Q; Vasbinder, M; Chuaqui, 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:
BDBM264238
Synonyms:
(2R)-N-(3-{2-[(1- ethyl-3-methoxy-1H- pyrazol-4-yl)amino]-5- methylpyrimidin-4- yl}-1H-indol-7-yl)- 2-(4-methylpiperazin-1- yl)propanamide | US10167276, Example 58 | US10654835, Example 58 | US11247983, Example 58 | US9714236, 58
Type:
Small organic molecule
Emp. Form.:
C27H35N9O2
Mol. Mass.:
517.6259
SMILES:
CCn1cc(Nc2ncc(C)c(n2)-c2c[nH]c3c(NC(=O)[C@@H](C)N4CCN(C)CC4)cccc23)c(OC)n1 |r|
Structure:
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