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Literature summary for 3.4.23.46 extracted from

  • Al-Tel, T.; Semreen, M.; Al-Qawasmeh, R.; Schmidt, M.; El-Awadi, R.; Ardah, M.; Zaarour, R.; Rao, S.; El-Agnaf, O.
    Design, synthesis, and qualitative structure-activity evaluations of novel beta-secretase inhibitors as potential Alzheimers drug leads (2011), J. Med. Chem., 54, 8373-8385.
    View publication on PubMed
Search for more literature for 3.4.23.46

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular modeling using PDB-structures 2B8L and 3FKT, with inhibitor 6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole inhibitor of BACE1, EC 3.4.23.46. 150fold more effective on BACE1 than BACE2 Homo sapiens
6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole inhibitor of BACE1, EC 3.4.23.46. 200fold more effective on BACE1 than BACE2 Homo sapiens
6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole inhibitor of BACE1, EC 3.4.23.46. 100fold more effective on BACE1 than BACE2 Homo sapiens

Organic Solvent Stability

Organic Solvent Comment Organism
dimethyl sulfoxide assay in 3.3% final concentration Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
rhodamine-EVNLDAEFK-quencher + H2O FRET-substrate Homo sapiens ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000017
-
 6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole pH 4.5, 25°C Homo sapiens
0.000025
-
 2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole pH 4.5, 25°C Homo sapiens
0.000034
-
 6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole pH 4.5, 25°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000026
-
 pH 4.5, 25°C Homo sapiens 2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-6-methoxy-1Hbenzo[d]imidazole
0.000035
-
 pH 4.5, 25°C Homo sapiens 6-fluoro-2-(3-(imidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo-[d]imidazole
0.0018
-
 pH 4.5, 25°C Homo sapiens 6-fluoro-2-(3-(7-fluoroimidazo[1,2-a]pyridin-2-yl)phenyl)-1H-benzo[d]imidazole