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Literature summary for 3.4.14.5 extracted from

  • Backes, B.J.; Longenecker, K.; Hamilton, G.L.; Stewart, K.; Lai, C.; Kopecka, H.; von Geldern, T.W.; Madar, D.J.; Pei, Z.; Lubben, T.H.; Zinker, B.A.; Tian, Z.; Ballaron, S.J.; Stashko, M.A.; Mika, A.K.; Beno, D.W.; Kempf-Grote, A.J.; Black-Schaefer, C.; Sham, H.L.; Trevillyan, J.M.
    Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit (2007), Bioorg. Med. Chem. Lett., 17, 2005-2012.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-acetyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine efficacious in vivo, lowering blood glucose in ZDF rats that were allowed to feed freely on a mixed meal Homo sapiens
(3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-[6-[3-(morpholin-4-ylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-1-[6-[3-fluoro-5-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-fluorobenzyl)pyrrolidine-1-carboxamide
-
Homo sapiens
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-methoxybenzyl)-N-methylpyrrolidine-1-carboxamide
-
Homo sapiens
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethyl-N-methylpyrrolidine-1-carboxamide
-
Homo sapiens
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethylpyrrolidine-1-carboxamide
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-(6-phenylpyridin-2-yl)pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyridin-2-ylpyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyrimidin-2-ylpyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-[2-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-[4-(3-thienyl)pyrimidin-2-yl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-[5-(4-methoxyphenyl)pyrimidin-2-yl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2,4-dichlorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2-chloro-4,5-difluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
Homo sapiens
(3R,4S)-4-(2-chloro-4-fluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
Homo sapiens
(6-methylpyridin-2-yl)methyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
-
Homo sapiens
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]-N,N-dimethylbenzamide
-
Homo sapiens
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
-
Homo sapiens
4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
-
Homo sapiens
ethyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27487
-
-
Rattus norvegicus P14740
-
-

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
dipeptidyl peptidase IV
-
Rattus norvegicus
DPP4
-
Homo sapiens
DPP4
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000017
-
-
Homo sapiens (3R,4S)-1-[6-[3-(morpholin-4-ylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.0000018
-
-
Homo sapiens 3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
0.0000021
-
-
Homo sapiens (3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.0000035
-
-
Homo sapiens (3R,4S)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000006
-
-
Homo sapiens (3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000007
-
-
Homo sapiens 3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]-N,N-dimethylbenzamide
0.000009
-
-
Homo sapiens (3R,4S)-1-[6-[3-fluoro-5-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000015
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
0.000017
-
-
Homo sapiens (3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.00002
-
-
Homo sapiens (3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000034
-
-
Homo sapiens (3R,4S)-4-(2-chloro-4-fluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
0.000035
-
-
Homo sapiens (3R,4S)-4-(2-chloro-4,5-difluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
0.000076
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-[4-(3-thienyl)pyrimidin-2-yl]pyrrolidin-3-amine
0.000085
-
-
Homo sapiens 4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
0.00014
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-(6-phenylpyridin-2-yl)pyrrolidin-3-amine
0.00019
-
-
Homo sapiens (3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-fluorobenzyl)pyrrolidine-1-carboxamide
0.00021
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-pyrimidin-2-ylpyrrolidin-3-amine
0.00022
-
-
Homo sapiens (3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-methoxybenzyl)-N-methylpyrrolidine-1-carboxamide
0.00024
-
-
Homo sapiens (6-methylpyridin-2-yl)methyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
0.00028
-
-
Homo sapiens (3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethylpyrrolidine-1-carboxamide
0.00043
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-[5-(4-methoxyphenyl)pyrimidin-2-yl]pyrrolidin-3-amine
0.00049
-
-
Homo sapiens ethyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
0.00061
-
-
Homo sapiens (3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethyl-N-methylpyrrolidine-1-carboxamide
0.00079
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-pyridin-2-ylpyrrolidin-3-amine
0.002
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-[2-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
0.0027
-
-
Homo sapiens (3R,4S)-1-acetyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
0.0028
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine
0.0034
-
-
Homo sapiens (3R,4S)-1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
0.013
-
-
Homo sapiens (3R,4S)-4-(2,4-dichlorophenyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidin-3-amine