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Target
Eukaryotic translation initiation factor 2-alpha kinase 3
Ligand
BDBM50396540
Substrate
n/a
Meas. Tech.
ChEMBL_862854 (CHEMBL2172956)
IC50
0.200000±n/a nM
Citation
 Axten, JM; Medina, JR; Feng, Y; Shu, A; Romeril, SP; Grant, SW; Li, WH; Heerding, DA; Minthorn, E; Mencken, T; Atkins, C; Liu, Q; Rabindran, S; Kumar, R; Hong, X; Goetz, A; Stanley, T; Taylor, JD; Sigethy, SD; Tomberlin, GH; Hassell, AM; Kahler, KM; Shewchuk, LM; Gampe, RT Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J Med Chem 55:7193-207 (2012) [PubMed]  Article 
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:
BDBM50396540
Synonyms:
CHEMBL2171143
Type:
Small organic molecule
Emp. Form.:
C24H23N5O
Mol. Mass.:
397.4723
SMILES:
Cc1ccccc1CC(=O)N1CCc2cc(ccc12)-c1cn(C)c2ncnc(N)c12
Structure:
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