Target
Tyrosine-protein kinase JAK1 [866-1154]
Ligand
BDBM264206
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
IC50
575±n/a nM
Citation
 Astrand, ABGrimster, NPKawatkar, SKettle, JGNilsson, MKRuston, LSu, QVasbinder, MWinter-Holt, JJWoessner, RDChuaqui, CEMcCabe, 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:
BDBM264206
Synonyms:
(2R)-2-[4-(2- methoxyethyl)piperazin- 1-yl]-N-(3-{2-[(3- methoxy-1-methyl- 1H-pyrazol-4-yl)amino] pyrimidin-4-yl}-1H- indol-7-yl)propanamide | US10167276, Example 27 | US10654835, Example 27 | US11247983, Example 27 | US9714236, 27
Type:
Small organic molecule
Emp. Form.:
C27H35N9O3
Mol. Mass.:
533.6253
SMILES:
COCCN1CCN(CC1)[C@H](C)C(=O)Nc1cccc2c(c[nH]c12)-c1ccnc(Nc2cn(C)nc2OC)n1 |r|
Structure:
Search PDB for entries with ligand similarity: