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Target
Eukaryotic translation initiation factor 2-alpha kinase 3
Ligand
BDBM50336292
Substrate
n/a
Meas. Tech.
ChEMBL_716579 (CHEMBL1670303)
IC50
102±n/a nM
Citation
 Ren, L; Wenglowsky, S; Miknis, G; Rast, B; Buckmelter, AJ; Ely, RJ; Schlachter, S; Laird, ER; Randolph, N; Callejo, M; Martinson, M; Galbraith, S; Brandhuber, BJ; Vigers, G; Morales, T; Voegtli, WC; Lyssikatos, J Non-oxime inhibitors of B-Raf(V600E) kinase. Bioorg Med Chem Lett 21:1243-7 (2011) [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:
BDBM50336292
Synonyms:
CHEMBL1667909 | N-(2-(dimethylamino)vinyl)-3-(5-hydroxynaphthalen-2-ylamino)furo[2,3-c]pyridine-2-carboxamide
Type:
Small organic molecule
Emp. Form.:
C22H20N4O3
Mol. Mass.:
388.4192
SMILES:
CN(C)\C=C\NC(=O)c1oc2cnccc2c1Nc1ccc2c(O)cccc2c1
Structure:
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