Target
Eukaryotic translation initiation factor 2-alpha kinase 3
Ligand
BDBM46492
Substrate
n/a
Meas. Tech.
Counterscreen assay for PERK inhibitors: Dose response cell-based high throughput screening assay to measure inhibition of PERK at 6 hours
EC50
>55700±n/a nM
Citation
 PubChem, PC Counterscreen assay for PERK inhibitors: Dose response cell-based high throughput screening assay to measure inhibition of PERK at 6 hours PubChem Bioassay (2009)[AID] 
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:
BDBM46492
Synonyms:
4-(4-keto-5,7-dimethyl-3-phenyl-pyrrolo[3,4-d]pyridazin-6-yl)-N-[2-(4-methylpiperazino)ethyl]butyramide | 4-(5,7-dimethyl-1-oxo-2-phenyl-1,2-dihydro-6H-pyrrolo[3,4-d]pyridazin-6-yl)-N-[2-(4-methylpiperazin-1-yl)ethyl]butanamide | 4-(5,7-dimethyl-4-oxidanylidene-3-phenyl-pyrrolo[3,4-d]pyridazin-6-yl)-N-[2-(4-methylpiperazin-1-yl)ethyl]butanamide | 4-(5,7-dimethyl-4-oxo-3-phenyl-6-pyrrolo[3,4-d]pyridazinyl)-N-[2-(4-methyl-1-piperazinyl)ethyl]butanamide | 4-(5,7-dimethyl-4-oxo-3-phenylpyrrolo[3,4-d]pyridazin-6-yl)-N-[2-(4-methylpiperazin-1-yl)ethyl]butanamide | MLS000660593 | SMR000310112 | cid_16193820
Type:
Small organic molecule
Emp. Form.:
C25H34N6O2
Mol. Mass.:
450.5765
SMILES:
CN1CCN(CCNC(=O)CCCn2c(C)c3cnn(-c4ccccc4)c(=O)c3c2C)CC1
Structure:
Search PDB for entries with ligand similarity: