Literature summary for 3.4.22.52 extracted from

Abell, A.D.; Jones, M.A.; Coxon, J.M.; Morton, J.D.; Aitken, S.G.; McNabb, S.B.; Lee, H.Y.; Mehrtens, J.M.; Alexander, N.A.; Stuart, B.G.; Neffe, A.T.; Bickerstaffe, R.
Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors (2009), Angew. Chem. Int. Ed. Engl., 48, 1455-1458.

Search for more literature for 3.4.22.52

Inhibitors

Inhibitors	Comment	Organism	Structure
(6S,9S,16R)-6-(hydroxymethyl)-9-(2-methylpropyl)-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-8,11,14-trione	-	Ovis aries
(6S,9S,16R)-9-(2-methylpropyl)-8,11,14-trioxo-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-6-carbaldehyde	less potent inhibitor with greater than 2fold selectivity for ovine calpain 1 over calpain 2	Ovis aries
(7S,10S,17R)-10-(2-methylpropyl)-9,12,15-trioxo-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-7-carbaldehyde	potent inhibitor of calpain with greater than 7fold selectivity for ovine calpain 2 over ovine calpain 1	Ovis aries
(7S,10S,17R)-7-(hydroxymethyl)-10-(2-methylpropyl)-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-9,12,15-trione	-	Ovis aries
(8S,11S,18R)-11-(2-methylpropyl)-10,13,16-trioxo-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-8-carbaldehyde	-	Ovis aries
(8S,11S,18R)-8-(hydroxymethyl)-11-(2-methylpropyl)-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-10,13,16-trione	-	Ovis aries
(9R,12S,19R)-12-(2-methylpropyl)-11,14,17-trioxo-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-9-carbaldehyde	-	Ovis aries
(9R,12S,19R)-9-(hydroxymethyl)-12-(2-methylpropyl)-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-11,14,17-trione	-	Ovis aries
leupeptin	a naturally occurring calpain inhibitor	Ovis aries
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide	-	Ovis aries
N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-oxopentan-2-yl]-L-leucinamide	potent inhibitor with more than 2.5fold selectivity for ovine calpain 1 over ovine calpain 2	Ovis aries
SNJ1715	-	Ovis aries

Organism

Organism	UniProt	Comment	Textmining
Ovis aries	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
lens	-	Ovis aries	-

Synonyms

Synonyms	Comment	Organism
calpain 1	-	Ovis aries
CAPN1	-	Ovis aries

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.00005	-	pH and temperature not specified in the publication	Ovis aries	N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-oxopentan-2-yl]-L-leucinamide
0.00017	-	pH and temperature not specified in the publication	Ovis aries	(8S,11S,18R)-11-(2-methylpropyl)-10,13,16-trioxo-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-8-carbaldehyde
0.00022	-	pH and temperature not specified in the publication	Ovis aries	(7S,10S,17R)-10-(2-methylpropyl)-9,12,15-trioxo-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-7-carbaldehyde
0.0004	-	pH and temperature not specified in the publication	Ovis aries	(6S,9S,16R)-9-(2-methylpropyl)-8,11,14-trioxo-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-6-carbaldehyde
0.00134	-	pH and temperature not specified in the publication	Ovis aries	(8S,11S,18R)-8-(hydroxymethyl)-11-(2-methylpropyl)-18-phenyl-2,17-dioxa-9,12,15-triazabicyclo[18.2.2]tetracosa-1(22),20,23-triene-10,13,16-trione
0.00175	-	pH and temperature not specified in the publication	Ovis aries	(7S,10S,17R)-7-(hydroxymethyl)-10-(2-methylpropyl)-17-phenyl-2,16-dioxa-8,11,14-triazabicyclo[17.2.2]tricosa-1(21),19,22-triene-9,12,15-trione
0.00315	-	pH and temperature not specified in the publication	Ovis aries	(9R,12S,19R)-12-(2-methylpropyl)-11,14,17-trioxo-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-9-carbaldehyde
0.0032	-	pH and temperature not specified in the publication	Ovis aries	N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide
0.013	-	pH and temperature not specified in the publication	Ovis aries	(6S,9S,16R)-6-(hydroxymethyl)-9-(2-methylpropyl)-16-phenyl-2,15-dioxa-7,10,13-triazabicyclo[16.2.2]docosa-1(20),18,21-triene-8,11,14-trione
0.05	-	pH and temperature not specified in the publication	Ovis aries	(9R,12S,19R)-9-(hydroxymethyl)-12-(2-methylpropyl)-19-phenyl-2,18-dioxa-7-thia-10,13,16-triazabicyclo[19.2.2]pentacosa-1(23),21,24-triene-11,14,17-trione

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)