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Target
Eukaryotic translation initiation factor 2 subunit 1
Ligand
BDBM50570947
Substrate
n/a
Meas. Tech.
ChEMBL_2113376 (CHEMBL4822226)
IC50
3340±n/a nM
Citation
 Calvo, V; Surguladze, D; Li, AH; Surman, MD; Malibhatla, S; Bandaru, M; Jonnalagadda, SK; Adarasandi, R; Velmala, M; Singireddi, DRP; Velpuri, M; Nareddy, BR; Sastry, V; Mandati, C; Guguloth, R; Siddiqui, S; Patil, BS; Chad, E; Wolfley, J; Gasparek, J; Feldman, K; Betzenhauser, M; Wiens, B; Koszelak-Rosenblum, M; Zhu, G; Du, H; Rigby, AC; Mulvihill, MJ Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors. Bioorg Med Chem Lett 43:0 (2021) [PubMed]  Article 
Target
Name:
Eukaryotic translation initiation factor 2 subunit 1
Synonyms:
EIF2A | EIF2S1 | Eukaryotic translation initiation factor 2 subunit alpha | IF2A_HUMAN | eIF-2-alpha | eIF-2A | eIF-2alpha
Type:
PROTEIN
Mol. Mass.:
36100.17
Organism:
Homo sapiens
Description:
ChEMBL_103542
Residue:
315
Sequence:
MPGLSCRFYQHKFPEVEDVVMVNVRSIAEMGAYVSLLEYNNIEGMILLSELSRRRIRSINKLIRIGRNECVVVIRVDKEKGYIDLSKRRVSPEEAIKCEDKFTKSKTVYSILRHVAEVLEYTKDEQLESLFQRTAWVFDDKYKRPGYGAYDAFKHAVSDPSILDSLDLNEDEREVLINNINRRLTPQAVKIRADIEVACYGYEGIDAVKEALRAGLNCSTENMPIKINLIAPPRYVMTTTTLERTEGLSVLSQAMAVIKEKIEEKRGVFNVQMEPKVVTDTDETELARQMERLERENAEVDGDDDAEEMEAKAED
  
Inhibitor
Name:
BDBM50570947
Synonyms:
CHEMBL4854364
Type:
Small organic molecule
Emp. Form.:
C25H28N4O3
Mol. Mass.:
432.5148
SMILES:
CO[C@@H](C(=O)Nc1ccc(c(C)c1)-c1cnc(N)c(c1)C(=O)NC(C)C)c1ccccc1 |r|
Structure:
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