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Target
Tyrosine-protein kinase JAK1 [866-1154]
Ligand
BDBM264229
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
<4.00±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 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:
BDBM264229
Synonyms:
(2R)-N-(3-{2-[(1,3- dimethyl-1H-pyrazol- 4-yl)amino]-5- fluoropyrimidin-4-yl}- 1H-indol-7-yl)-2- (4-methylpiperazin- 1-yl)butanamide | US10167276, Example 49 | US10654835, Example 49 | US11247983, Example 49 | US9714236, 49
Type:
Small organic molecule
Emp. Form.:
C26H32FN9O
Mol. Mass.:
505.5904
SMILES:
CC[C@@H](N1CCN(C)CC1)C(=O)Nc1cccc2c(c[nH]c12)-c1nc(Nc2cn(C)nc2C)ncc1F |r|
Structure:
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