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Literature summary for 3.4.14.5 extracted from

  • Liang, G.B.; Qian, X.; Feng, D.; Biftu, T.; Eiermann, G.; He, H.; Leiting, B.; Lyons, K.; Petrov, A.; Sinha-Roy, R.; Zhang, B.; Wu, J.; Zhang, X.; Thornberry, N.A.; Weber, A.E.
    Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes (2007), Bioorg. Med. Chem. Lett., 17, 1903-1907.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,3-dimethyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-(2-hydroxyethyl)-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-tert-butyl-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-[2-(benzyloxy)ethyl]-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-ethyl-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1-(2-oxopropyl)-1,4-diazepan-2-one
-
Homo sapiens
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-7-(trifluoromethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-(2-fluorobenzyl)-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-ethyl-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3R,S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6,6-trimethyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2-fluorobenzyl)-7-methyl-1,4-diazepan-2-one
-
Homo sapiens
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2-methylbenzyl)-1,4-diazepan-2-one
-
Homo sapiens
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(pyridin-2-ylmethyl)-1,4-diazepan-2-one
-
Homo sapiens
(3S,7S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
-
Homo sapiens
[(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-2-oxo-1,4-diazepan-1-yl]acetic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DPP-4
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000149
-
-
Homo sapiens (3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2-methylbenzyl)-1,4-diazepan-2-one
0.0000066
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
0.0000066
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,3-dimethyl-1,4-diazepan-2-one
0.000008
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
0.000009
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
0.0000096
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-tert-butyl-3-methyl-1,4-diazepan-2-one
0.0000097
-
-
Homo sapiens (3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
0.0000105
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-[2-(benzyloxy)ethyl]-3-methyl-1,4-diazepan-2-one
0.000011
-
-
Homo sapiens (3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(pyridin-2-ylmethyl)-1,4-diazepan-2-one
0.0000115
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
0.0000116
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1-(2-oxopropyl)-1,4-diazepan-2-one
0.0000151
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-(2-hydroxyethyl)-3-methyl-1,4-diazepan-2-one
0.0000151
-
-
Homo sapiens (3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
0.0000192
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
0.0000207
-
-
Homo sapiens (3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-ethyl-3-methyl-1,4-diazepan-2-one
0.0000246
-
-
Homo sapiens (3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
0.0000277
-
-
Homo sapiens (3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2-fluorobenzyl)-7-methyl-1,4-diazepan-2-one
0.000033
-
-
Homo sapiens (3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
0.0000343
-
-
Homo sapiens (3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
0.0000373
-
-
Homo sapiens (3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
0.0000603
-
-
Homo sapiens (3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
0.0000699
-
-
Homo sapiens [(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-2-oxo-1,4-diazepan-1-yl]acetic acid
0.000126
-
-
Homo sapiens (3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-(2-fluorobenzyl)-3-methyl-1,4-diazepan-2-one
0.000139
-
-
Homo sapiens (3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-7-(trifluoromethyl)-1,4-diazepan-2-one
0.000142
-
-
Homo sapiens (3S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6,6-trimethyl-1,4-diazepan-2-one
0.000143
-
-
Homo sapiens (3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
0.000296
-
-
Homo sapiens (3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-ethyl-3-methyl-1,4-diazepan-2-one
0.000397
-
-
Homo sapiens (3S,7S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
0.000765 0.00105 absolute configuration of 3-methyl group not determined Homo sapiens (3R,S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one