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Literature summary for 3.4.23.15 extracted from

  • Chen, A.; Bayly, C.; Bezencon, O.; Richard-Bildstein, S.; Dube, D.; Dube, L.; Gagne, S.; Gallant, M.; Gaudreault, M.; Grimm, E.; Houle, R.; Lacombe, P.; Laliberte, S.; Levesque, J.F.; Liu, S.; MacDonald, D.; Mackay, B.; Martin, D.; McKay, D.; Powell, D.; Remen, L.; Soisson, S.; Toulmond, S.
    Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension (2010), Bioorg. Med. Chem. Lett., 20, 2204-2209.
    View publication on PubMed
Search for more literature for 3.4.23.15

Inhibitors

Inhibitors Comment Organism Structure
(1R,5S)-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-8-azabicyclo[3.2.1]oct-2-ene-2-carboxamide
-
 Homo sapiens
(2R)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]-N-[3-(2-methoxyethoxy)-5-(3-methoxypropyl)benzyl]propanamide
-
 Homo sapiens
(2S)-6-(2,4-diamino-6-ethylpyrimidin-5-yl)-2-(3,5-difluorophenyl)-4-(3-methoxypropyl)-2-methyl-2H-1,4-benzoxazin-3(4H)-one
-
 Homo sapiens
2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
-
 Homo sapiens
3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
 Homo sapiens
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
-
 Homo sapiens
3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
-
 Homo sapiens
3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[2-chloro-5-[3-(dimethylamino)propyl]benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[[5-chloro-2-(3-methoxypropyl)-1-oxidopyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
3-amino-N-[[5-chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
5-amino-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)pentanamide
-
 Homo sapiens
7-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
 Homo sapiens
aliskiren
-
 Homo sapiens
N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
-
 Homo sapiens
N-cyclopropyl-7-[4-[3-(2,6-dichloro-4-methylphenoxy)propyl]phenyl]-N-(2,3-dimethylbenzyl)-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
 Homo sapiens
N-cyclopropyl-N-[[1-(3-methoxypropyl)-1H-indol-3-yl]methyl]morpholine-2-carboxamide
-
 Homo sapiens
N-[2-[7-([[(3R,4R)-4-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperidin-3-yl]oxy]methyl)-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
N-[2-[7-[[(2R)-1-(4-[3-[(2-methoxybenzyl)oxy]propoxy]phenyl)piperazin-2-yl]methoxy]-3,4-dihydroquinolin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
remikiren RO 42-5892 Homo sapiens
tetrahydro-2H-pyran-4-yl cyclopropyl[[(3S,4S)-4-[(2R)-2-[4-methoxy-3-(3-methoxypropoxy)benzyl]-3-methylbutyl]pyrrolidin-3-yl]methyl]carbamate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
angiotensinogen + H2O Homo sapiens
-
 angiotensin I + angiotensinogen propeptide
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
angiotensinogen + H2O
-
 Homo sapiens angiotensin I + angiotensinogen propeptide
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000002
-
 at pH 7.4 and 37°C Homo sapiens (2R)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]-N-[3-(2-methoxyethoxy)-5-(3-methoxypropyl)benzyl]propanamide
0.00000009
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(3-hydroxypropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000011
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(3-cyanopropyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000019
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(4-methoxybutyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000019
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[[5-chloro-2-(3-methoxypropyl)pyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000021
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(4-methoxybutoxy)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000026
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-cyclopropyl-N-[2,3-dichloro-5-(3-methoxypropyl)benzyl]-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000026
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(6-methoxyhexyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000027
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-(2-cyanoethyl)benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.0000003
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[[5-chloro-2-(3-methoxypropyl)-1-oxidopyridin-4-yl]methyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.0000004
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00000079
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
0.0000015
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-N-[2-chloro-5-[3-(dimethylamino)propyl]benzyl]-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.0000019
-
 at pH 7.4 and 37°C Homo sapiens 2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-3-(methylamino)propanamide
0.0000029
-
 at pH 7.4 and 37°C Homo sapiens N-(5-[[acetyl(methyl)amino]methyl]-2-chlorobenzyl)-3-amino-N-cyclopropyl-2-[4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]benzyl]propanamide
0.00021
-
 at pH 7.4 and 37°C Homo sapiens 3-amino-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)-2-methylpropanamide
0.00026
-
 at pH 7.4 and 37°C Homo sapiens 3-(benzylamino)-2-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]benzyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)propanamide
0.00065
-
 at pH 7.4 and 37°C Homo sapiens 5-amino-3-[4-[3-(2-chloro-3,6-difluorophenoxy)propyl]phenyl]-N-cyclopropyl-N-(2,3-dichlorobenzyl)pentanamide