Target
Eukaryotic translation initiation factor 2 subunit 1
Ligand
BDBM50570955
Substrate
n/a
Meas. Tech.
ChEMBL_2113376 (CHEMBL4822226)
IC50
45±n/a nM
Citation
 Calvo, VSurguladze, DLi, AHSurman, MDMalibhatla, SBandaru, MJonnalagadda, SKAdarasandi, RVelmala, MSingireddi, DRPVelpuri, MNareddy, BRSastry, VMandati, CGuguloth, RSiddiqui, SPatil, BSChad, EWolfley, JGasparek, JFeldman, KBetzenhauser, MWiens, BKoszelak-Rosenblum, MZhu, GDu, HRigby, ACMulvihill, 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:
BDBM50570955
Synonyms:
CHEMBL4863698
Type:
Small organic molecule
Emp. Form.:
C23H22F2N4O3
Mol. Mass.:
440.4426
SMILES:
CCNC(=O)c1cc(cnc1N)-c1ccc(NC(=O)[C@H](O)c2cc(F)cc(F)c2)cc1C |r|
Structure:
Search PDB for entries with ligand similarity: