Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetEukaryotic translation initiation factor 2-alpha kinase 3
LigandBDBM50396540
Substrate/Competitorn/a
Meas. Tech.ChEMBL_862854 (CHEMBL2172956)
IC50 0.200000±n/a nM
Citation Axten, JMMedina, JRFeng, YShu, ARomeril, SPGrant, SWLi, WHHeerding, DAMinthorn, EMencken, TAtkins, CLiu, QRabindran, SKumar, RHong, XGoetz, AStanley, TTaylor, JDSigethy, SDTomberlin, GHHassell, AMKahler, KMShewchuk, LMGampe, 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 Chem55:7193-207 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Eukaryotic translation initiation factor 2-alpha kinase 3
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:
MERAISPGLLVRALLLLLLLLGLAARTVAAGRARGLPAPTAEAAFGLGAAAAPTSATRVP
AAGAVAAAEVTVEDAEALPAAAGEQEPRGPEPDDETELRPRGRSLVIISTLDGRIAALDP
ENHGKKQWDLDVGSGSLVSSSLSKPEVFGNKMIIPSLDGALFQWDQDRESMETVPFTVES
LLESSYKFGDDVVLVGGKSLTTYGLSAYSGKVRYICSALGCRQWDSDEMEQEEDILLLQR
TQKTVRAVGPRSGNEKWNFSVGHFELRYIPDMETRAGFIESTFKPNENTEESKIISDVEE
QEAAIMDIVIKVSVADWKVMAFSKKGGHLEWEYQFCTPIASAWLLKDGKVIPISLFDDTS
YTSNDDVLEDEEDIVEAARGATENSVYLGMYRGQLYLQSSVRISEKFPSSPKALESVTNE
NAIIPLPTIKWKPLIHSPSRTPVLVGSDEFDKCLSNDKFSHEEYSNGALSILQYPYDNGY
YLPYYKRERNKRSTQITVRFLDNPHYNKNIRKKDPVLLLHWWKEIVATILFCIIATTFIV
RRLFHPHPHRQRKESETQCQTENKYDSVSGEANDSSWNDIKNSGYISRYLTDFEPIQCLG
RGGFGVVFEAKNKVDDCNYAIKRIRLPNRELAREKVMREVKALAKLEHPGIVRYFNAWLE
APPEKWQEKMDEIWLKDESTDWPLSSPSPMDAPSVKIRRMDPFATKEHIEIIAPSPQRSR
SFSVGISCDQTSSSESQFSPLEFSGMDHEDISESVDAAYNLQDSCLTDCDVEDGTMDGND
EGHSFELCPSEASPYVRSRERTSSSIVFEDSGCDNASSKEEPKTNRLHIGNHCANKLTAF
KPTSSKSSSEATLSISPPRPTTLSLDLTKNTTEKLQPSSPKVYLYIQMQLCRKENLKDWM
NGRCTIEERERSVCLHIFLQIAEAVEFLHSKGLMHRDLKPSNIFFTMDDVVKVGDFGLVT
AMDQDEEEQTVLTPMPAYARHTGQVGTKLYMSPEQIHGNSYSHKVDIFSLGLILFELLYP
FSTQMERVRTLTDVRNLKFPPLFTQKYPCEYVMVQDMLSPSPMERPEAINIIENAVFEDL
DFPGKTVLRQRSRSLSSSGTKHSRQSNNSHSPLPSN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50396540
n/a
NameBDBM50396540
Synonyms:CHEMBL2171143
TypeSmall organic molecule
Emp. Form.C24H23N5O
Mol. Mass.397.4723
SMILESCc1ccccc1CC(=O)N1CCc2cc(ccc12)-c1cn(C)c2ncnc(N)c12
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: