Reaction Details |
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Target | Eukaryotic translation initiation factor 2-alpha kinase 3 |
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Ligand | BDBM50072027 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1467748 (CHEMBL3412174) |
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EC50 | 130±n/a nM |
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Citation | Smith, AL; Andrews, KL; Beckmann, H; Bellon, SF; Beltran, PJ; Booker, S; Chen, H; Chung, YA; D'Angelo, ND; Dao, J; Dellamaggiore, KR; Jaeckel, P; Kendall, R; Labitzke, K; Long, AM; Materna-Reichelt, S; Mitchell, P; Norman, MH; Powers, D; Rose, M; Shaffer, PL; Wu, MM; Lipford, JR Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J Med Chem58:1426-41 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Eukaryotic translation initiation factor 2-alpha kinase 3 |
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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
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BDBM50072027 |
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n/a |
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Name | BDBM50072027 |
Synonyms: | CHEMBL3407852 |
Type | Small organic molecule |
Emp. Form. | C33H27FN6O3 |
Mol. Mass. | 574.6043 |
SMILES | CNc1ncc2c(F)cc(Oc3c(C)ccc(C(=O)c4c(-c5ccccc5)n(C)n(-c5ccccc5)c4=O)c3N)cc2n1 |
Structure |
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