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Literature summary for 3.4.23.46 extracted from

  • Azimi, S.; Zonouzi, A.; Firuzi, O.; Iraji, A.; Saeedi, M.; Mahdavi, M.; Edraki, N.
    Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors Design, synthesis and SAR analysis (2017), Eur. J. Med. Chem., 138, 729-737 .
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
2-(2-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 34.28% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)-5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 87.94% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)-6-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 63.7% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione complete inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)-8-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 69.43% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione 69.49% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione less than 10% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl)isoindoline-1,3-dione 37.9% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(tert-butylamino)-6-chloroimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 32.95% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(3-(tert-butylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 24.24% inhibition at 0.01 mM Homo sapiens
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione 43.17% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(6-bromo-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 45.3% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(6-bromo-3-(tert-butylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione 48.72% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione 88.097% inhibition at 0.05 mM Homo sapiens
2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione 19.6% inhibition at 0.05 mM Homo sapiens
OM99-2
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
amyloid-beta precursor protein + H2O Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid-beta precursor protein + H2O
-
 Homo sapiens ?
-
 ?
Rh-EVNLDAEFK-quencher + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
BACE1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
 at pH 4.5 and 23°C Homo sapiens OM99-2
0.00284
-
 at pH 4.5 and 23°C Homo sapiens 2-(3-(4-(3-(cyclohexylamino)-7-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
0.00593
-
 at pH 4.5 and 23°C Homo sapiens 2-(3-(4-(3-(cyclohexylamino)-5-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione
0.0149
-
 at pH 4.5 and 23°C Homo sapiens 2-(3-(4-(6-chloro-3-(cyclohexylamino)imidazo[1,2-a]pyridin-2-yl)-2-methoxyphenoxy)propyl) isoindoline-1,3-dione
0.02942
-
 at pH 4.5 and 23°C Homo sapiens 2-(3-(4-(3-(cyclohexylamino)-6-methylimidazo[1,2-a]pyridin-2-yl)phenoxy)propyl)isoindoline-1,3-dione