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Literature summary for 3.4.23.15 extracted from

  • Bezencon, O.; Bur, D.; Weller, T.; Richard-Bildstein, S.; Remen, L.; Sifferlen, T.; Corminboeuf, O.; Grisostomi, C.; Boss, C.; Prade, L.; Delahaye, S.; Treiber, A.; Strickner, P.; Binkert, C.; Hess, P.; Steiner, B.; Fischli, W.
    Design and preparation of potent, nonpeptidic, bioavailable renin inhibitors (dagger) (2009), J. Med. Chem., 52, 3689-3702.
    View publication on PubMed
Search for more literature for 3.4.23.15

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with the (+)- and (-)-enantiomer of inhibitor 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. The hydrophobic interactions dominate the positioning of the inhibitors with the pseudosymmetry of the central template being able to establish the necessary hydrogen bonds in either orientation. Substitution of either of the two nitrogen atoms abolishes this pseudosymmetry and completely abrogates this observed effect Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
 Homo sapiens
3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
-
 Rattus norvegicus
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 the (+)- and (-)-enantiomers are almost equally potent as renin inhibotrs in buffer and in plasma. crystallization data 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
-
 Rattus norvegicus
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-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 inhibitor is well absorbed and reduces the blood pressure by about 30 mm Hg at 10 mg/kg in vivo Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens P00797
-
-
Rattus norvegicus
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000002
-
 in buffer 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
0.0000004
-
 in buffer 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
0.00000055
-
 in buffer Homo sapiens 3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide
0.00019
-
 in buffer 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
0.00036
-
 in buffer 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
0.00056
-
 in buffer Homo sapiens 3-(5-amino-5-oxopentanoyl)-7-[4-[3-(2-bromo-5-fluorophenoxy)propyl]phenyl]-N-(2-chlorobenzyl)-N-cyclopropyl-3,9-diazabicyclo[3.3.1]non-6-ene-6-carboxamide