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Target
Tyrosine-protein kinase JAK1 [866-1154]
Ligand
BDBM264194
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
7.00±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  US11247983 Publication Date 2/15/2022
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:
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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