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Target
Eukaryotic translation initiation factor 2-alpha kinase 3
Ligand
BDBM384212
Substrate
n/a
Meas. Tech.
pERK AlphaScreen Protocol
IC50
122±n/a nM
Citation
 Jones, P; Czako, B; Cross, J; Leonard, P; Mseeh, F; Parker, CA Heterocyclic inhibitors of PTPN11 US Patent  US10280171 Publication Date 5/7/2019 
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:
BDBM384212
Synonyms:
4-[6-(4-amino-4- ethylpiperidin-1-yl)- 1H-pyrazolo[3,4-b]- pyrazin-3-yl]-3- chloropyridin-2- amine | US10280171, Example 135 | US10851110, Example 135 | US11466017, Example 135
Type:
Small organic molecule
Emp. Form.:
C17H21ClN8
Mol. Mass.:
372.855
SMILES:
CCC1(N)CCN(CC1)c1cnc2c(n[nH]c2n1)-c1ccnc(N)c1Cl
Structure:
Search PDB for entries with ligand similarity: