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Literature summary for 3.4.22.53 extracted from

  • Ovat, A.; Li, Z.; Hampton, C.; Asress, S.; Fernandez, F.; Glass, J.; Powers, J.
    Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors (2010), J. Med. Chem., 53, 6326-6336.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
Cbz-Leu-DL-Abu-CONH-(CH2)3-(4-methylpiperazin-1-yl)
-
Sus scrofa
Cbz-Leu-DL-Abu-CONH-(CH2)3-2-methoxyadenin-9-yl
-
Sus scrofa
Cbz-Leu-DL-Abu-CONH-(CH2)3-adenin-9-yl
-
Sus scrofa
Cbz-Leu-DL-Abu-CONH-(CH2)3-cytosin-3-yl
-
Sus scrofa
Cbz-Leu-DL-Abu-CONH-(CH2)3-morpholine
-
Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)2-N-(CH3)2
-
Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)3-(4-methylpiperazin-1-yl)
-
Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)3-2-methoxyadenin-9-yl
-
Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)3-adenin-9-yl best inhibitor Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)3-cytosin-3-yl
-
Sus scrofa
CBZ-Leu-DL-Phe-CONH-(CH2)3-N-(CH3)2
-
Sus scrofa

Organism

Organism UniProt Comment Textmining
Sus scrofa
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Sus scrofa
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
succinyl-Leu-Tyr-7-amido-4-methylcoumarin + H2O
-
Sus scrofa succinyl-Leu-Tyr + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
Cal II
-
Sus scrofa
calpain II
-
Sus scrofa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000041
-
Cbz-Leu-DL-Abu-CONH-(CH2)3-morpholine in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000068
-
CBZ-Leu-DL-Phe-CONH-(CH2)3-adenin-9-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.00007
-
Cbz-Leu-DL-Abu-CONH-(CH2)3-adenin-9-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000077
-
Cbz-Leu-DL-Abu-CONH-(CH2)3-2-methoxyadenin-9-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000209
-
CBZ-Leu-DL-Phe-CONH-(CH2)3-2-methoxyadenin-9-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000286
-
Cbz-Leu-DL-Abu-CONH-(CH2)3-(4-methylpiperazin-1-yl) in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000438
-
CBZ-Leu-DL-Phe-CONH-(CH2)3-cytosin-3-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.000844
-
CBZ-Leu-DL-Phe-CONH-(CH2)3-N-(CH3)2 in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.00114
-
Cbz-Leu-DL-Abu-CONH-(CH2)3-cytosin-3-yl in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.00352
-
CBZ-Leu-DL-Phe-CONH-(CH2)2-N-(CH3)2 in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa
0.00636
-
CBZ-Leu-DL-Phe-CONH-(CH2)3-(4-methylpiperazin-1-yl) in 50 mM Tris-HCl, 50 mM NaCl, 1 mM EDTA, 1 mM EGTA, 0.1% CHAPS, pH 7.5, 10 mM dithiothreitol, 5 mM CaCl2, and less than 5% (v/v) DMSO, temperature not specified in the publication Sus scrofa