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Target
Eukaryotic translation initiation factor 2-alpha kinase 3
Ligand
BDBM103857
Substrate
n/a
Meas. Tech.
Alpha Elisa Assay
IC50
<10.00±n/a nM
Citation
 Bifulco, Jr., N; DiPietro, LV; Miduturu, CV Inhibitors of the fibroblast growth factor receptor US Patent  US9695165 Publication Date 7/4/2017 
Target
Name:
Eukaryotic translation initiation factor 2-alpha kinase 3
Synonyms:
E2AK3_HUMAN | EIF2AK3 | HsPEK | PEK | PERK | Pancreatic eIF2-alpha kinase | Pancreatic endoplasmic reticulum kinase (PERK)
Type:
Enzyme
Mol. Mass.:
125190.66
Organism:
Homo sapiens (Human)
Description:
Q9NZJ5
Residue:
1116
Sequence:
MERAISPGLLVRALLLLLLLLGLAARTVAAGRARGLPAPTAEAAFGLGAAAAPTSATRVPAAGAVAAAEVTVEDAEALPAAAGEQEPRGPEPDDETELRPRGRSLVIISTLDGRIAALDPENHGKKQWDLDVGSGSLVSSSLSKPEVFGNKMIIPSLDGALFQWDQDRESMETVPFTVESLLESSYKFGDDVVLVGGKSLTTYGLSAYSGKVRYICSALGCRQWDSDEMEQEEDILLLQRTQKTVRAVGPRSGNEKWNFSVGHFELRYIPDMETRAGFIESTFKPNENTEESKIISDVEEQEAAIMDIVIKVSVADWKVMAFSKKGGHLEWEYQFCTPIASAWLLKDGKVIPISLFDDTSYTSNDDVLEDEEDIVEAARGATENSVYLGMYRGQLYLQSSVRISEKFPSSPKALESVTNENAIIPLPTIKWKPLIHSPSRTPVLVGSDEFDKCLSNDKFSHEEYSNGALSILQYPYDNGYYLPYYKRERNKRSTQITVRFLDNPHYNKNIRKKDPVLLLHWWKEIVATILFCIIATTFIVRRLFHPHPHRQRKESETQCQTENKYDSVSGEANDSSWNDIKNSGYISRYLTDFEPIQCLGRGGFGVVFEAKNKVDDCNYAIKRIRLPNRELAREKVMREVKALAKLEHPGIVRYFNAWLEAPPEKWQEKMDEIWLKDESTDWPLSSPSPMDAPSVKIRRMDPFATKEHIEIIAPSPQRSRSFSVGISCDQTSSSESQFSPLEFSGMDHEDISESVDAAYNLQDSCLTDCDVEDGTMDGNDEGHSFELCPSEASPYVRSRERTSSSIVFEDSGCDNASSKEEPKTNRLHIGNHCANKLTAFKPTSSKSSSEATLSISPPRPTTLSLDLTKNTTEKLQPSSPKVYLYIQMQLCRKENLKDWMNGRCTIEERERSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVGDFGLVTAMDQDEEEQTVLTPMPAYARHTGQVGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYPFSTQMERVRTLTDVRNLKFPPLFTQKYPCEYVMVQDMLSPSPMERPEAINIIENAVFEDLDFPGKTVLRQRSRSLSSSGTKHSRQSNNSHSPLPSN
  
Inhibitor
Name:
BDBM103857
Synonyms:
US9695165, 40
Type:
Small organic molecule
Emp. Form.:
C28H24Cl2FN3O4
Mol. Mass.:
556.412
SMILES:
COc1cc(OC)c(Cl)c(c1Cl)-c1cc2cnc(cc2n(C(C)C)c1=O)-c1cc(NC(=O)C=C)ccc1F |(-2,10.01,;-2,8.47,;-.67,7.7,;.67,8.47,;2,7.7,;3.33,8.47,;4.67,7.7,;2,6.16,;3.33,5.39,;.67,5.39,;-.67,6.16,;-2,5.39,;.67,3.85,;-.67,3.08,;-.67,1.54,;-2,.77,;-2,-.77,;-.67,-1.54,;.67,-.77,;.67,.77,;2,1.54,;3.33,.77,;4.67,1.54,;3.33,-.77,;2,3.08,;3.33,3.85,;-.67,-3.08,;-2,-3.85,;-2,-5.39,;-3.33,-6.16,;-3.33,-7.7,;-2,-8.47,;-4.67,-8.47,;-4.67,-10.01,;-.67,-6.16,;.67,-5.39,;.67,-3.85,;2,-3.08,)|
Structure:
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