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Literature summary for 3.4.23.46 extracted from

  • Al-Tel, T.H.; Al-Qawasmeh, R.A.; Schmidt, M.F.; Al-Aboudi, A.; Rao, S.N.; Sabri, S.S.; Voelter, W.
    Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors (2009), J. Med. Chem., 52, 6484-6488.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
11-oxo-N-(pyridin-4-yl)-10,11-dihydro-5H-dibenzo[b,e][1,4]-diazepine-3-carboxamide
-
Homo sapiens
3-(3H-imidazo[4,5-c]pyridin-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
Homo sapiens
3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]diazepin-11(10H)-one
-
Homo sapiens
3-(5-(pyridin-4-yl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]-diazepin-11(10H)-one
-
Homo sapiens
3-(6-fluoro-1H-benzo[d]imidazol-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one
-
Homo sapiens
N-(4-fluorophenyl)-11-oxo-10,11-dihydro-5H-dibenzo[b,e]-[1,4]diazepine-3-carboxamide
-
Homo sapiens
N-[(2S,3S)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-N'-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)amino]benzene-1,3-dicarboxamide
-
Homo sapiens
OM99-2 i.e. Glu-Val-Asn-(S)-CH(OH)CH2-Leu-Ala-Glu-Phe-OH Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
amyloid precursor protein + H2O
-
Homo sapiens fragments of amyloid precursor protein
-
?
rhodamine-EVNLDAEFK-DABCYL + H2O
-
Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
BACE1
-
Homo sapiens
beta-secretase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000016
-
OM99-2 in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.00001
-
N-[(2S,3S)-4-(cyclopropylamino)-3-hydroxy-1-phenylbutan-2-yl]-N'-[(1R)-1-(4-fluorophenyl)ethyl]-5-[(methylsulfonyl)amino]benzene-1,3-dicarboxamide in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000211
-
N-(4-fluorophenyl)-11-oxo-10,11-dihydro-5H-dibenzo[b,e]-[1,4]diazepine-3-carboxamide in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000244
-
3-(6-fluoro-1H-benzo[d]imidazol-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000293
-
3-(5-(4-fluorophenyl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]diazepin-11(10H)-one in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000295
-
11-oxo-N-(pyridin-4-yl)-10,11-dihydro-5H-dibenzo[b,e][1,4]-diazepine-3-carboxamide in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000309
-
3-(3H-imidazo[4,5-c]pyridin-2-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens
0.000348
-
3-(5-(pyridin-4-yl)-1H-imidazol-2-yl)-5H dibenzo[b,e][1,4]-diazepin-11(10H)-one in 50 mM sodium acetate buffer, pH 4.5, at 25°C Homo sapiens