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Target
Eukaryotic translation initiation factor 2-alpha kinase 3 [540-1115]
Ligand
BDBM482207
Substrate
n/a
Meas. Tech.
PERK enzyme assays
IC50
<16±n/a nM
Citation
 Bindi, S; Carenzi, D; Motto, I; Pulici, M N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors US Patent  US11491158 Publication Date 11/8/2022 
Target
Name:
Eukaryotic translation initiation factor 2-alpha kinase 3 [540-1115]
Synonyms:
E2AK3_HUMAN | EIF2AK3 | PEK | PERK
Type:
Enzyme
Mol. Mass.:
65443.31
Organism:
Homo sapiens (Human)
Description:
Q9NZJ5 [540-1115]
Residue:
576
Sequence:
VRRLFHPHPHRQRKESETQCQTENKYDSVSGEANDSSWNDIKNSGYISRYLTDFEPIQCLGRGGFGVVFEAKNKVDDCNYAIKRIRLPNRELAREKVMREVKALAKLEHPGIVRYFNAWLEAPPEKWQEKMDEIWLKDESTDWPLSSPSPMDAPSVKIRRMDPFATKEHIEIIAPSPQRSRSFSVGISCDQTSSSESQFSPLEFSGMDHEDISESVDAAYNLQDSCLTDCDVEDGTMDGNDEGHSFELCPSEASPYVRSRERTSSSIVFEDSGCDNASSKEEPKTNRLHIGNHCANKLTAFKPTSSKSSSEATLSISPPRPTTLSLDLTKNTTEKLQPSSPKVYLYIQMQLCRKENLKDWMNGRCTIEERERSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVGDFGLVTAMDQDEEEQTVLTPMPAYARHTGQVGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYPFSTQMERVRTLTDVRNLKFPPLFTQKYPCEYVMVQDMLSPSPMERPEAINIIENAVFEDLDFPGKTVLRQRSRSLSSSGTKHSRQSNNSHSPLPS
  
Inhibitor
Name:
BDBM482207
Synonyms:
N-[3-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-fluoro-phenyl]-4-bromo-3-methyl-benzenesulfonamide | US10918642, Cmpd # 52 | US11491158, Cmpd 52
Type:
Small organic molecule
Emp. Form.:
C20H17BrFN5O2S
Mol. Mass.:
490.349
SMILES:
Cc1cc(ccc1Br)S(=O)(=O)Nc1cccc(-c2cn(C)c3ncnc(N)c23)c1F
Structure:
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