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Literature summary 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.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 (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
3.4.22.52 leupeptin a naturally occurring calpain inhibitor Ovis aries
3.4.22.52 N-[[(1R)-1-phenyl-2-(4-propoxyphenyl)ethoxy]carbonyl]glycyl-N-[(2S)-1-hydroxypentan-2-yl]-L-leucinamide
-
 Ovis aries
3.4.22.52 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
3.4.22.52 SNJ1715
-
 Ovis aries

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.52 Ovis aries
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.52 lens
-
 Ovis aries
-

Synonyms

EC Number Synonyms Comment Organism
3.4.22.52 calpain 1
-
 Ovis aries
3.4.22.52 CAPN1
-
 Ovis aries

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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
3.4.22.52 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