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Literature summary for 3.4.22.15 extracted from

  • Chowdhury, S.F.; Sivaraman, J.; Wang, J.; Devanathan, G.; Lachance, P.; Qi, H.; Menard, R.; Lefebvre, J.; Konishi, Y.; Cygler, M.; Sulea, T.; Purisima, E.O.
    Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides (2002), J. Med. Chem., 45, 5321-5329.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging drop vapor diffusion method, 1.9 A X-ray structure of the complex of cathepsin L with the inhibitor 13 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
biphenyl-4-yl-acetylasparagine-D-Arg-Phe-Phe-NH2
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Abu-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Arg-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-Phe-NH2
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Trp-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylcysteine-D-Arg-Tyr-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Leu-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Met-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide the inhibitor shows a 310fold and 210fold selectivity for cathepsin L over cathepsin K and B, respectively Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(3-phenylpropyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(benzyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-Phe-NH2
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-D-Orn-Phe-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylmethylcysteine-Gly-Phe-Phe-NH2
-
Homo sapiens
biphenyl-4-yl-acetylnorvaline-D-Arg-Phe-N-(2-phenylethyl)amide
-
Homo sapiens
biphenyl-4-yl-acetylserine-D-Arg-Phe-Phe-NH2
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P07711
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000019
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.000021
-
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.000045
-
biphenyl-4-yl-acetylcysteine-D-Arg-Tyr-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.000067
-
biphenyl-4-yl-acetylcysteine-D-Arg-Trp-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00007
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-Phe-NH2 pH 5.5, 25°C Homo sapiens
0.00017
-
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-Phe-NH2 pH 5.5, 25°C Homo sapiens
0.0002
-
biphenyl-4-yl-acetylmethylcysteine-D-Orn-Phe-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00021
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(3-phenylpropyl)amide pH 5.5, 25°C Homo sapiens
0.00021
-
biphenyl-4-yl-acetylcysteine-D-Arg-Abu-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00024
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Met-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00027
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Leu-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00049
-
biphenyl-4-yl-acetylnorvaline-D-Arg-Phe-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.00093
-
biphenyl-4-yl-acetylmethylcysteine-Gly-Phe-Phe-NH2 pH 5.5, 25°C Homo sapiens
0.0039
-
biphenyl-4-yl-acetylcysteine-D-Arg-Arg-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens
0.0066
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(benzyl)amide pH 5.5, 25°C Homo sapiens
0.03
-
biphenyl-4-yl-acetylasparagine-D-Arg-Phe-Phe-NH2 pH 5.5, 25°C Homo sapiens
0.07
-
biphenyl-4-yl-acetylserine-D-Arg-Phe-Phe-NH2 pH 5.5, 25°C Homo sapiens
0.081
-
biphenyl-4-yl-acetylcysteine-D-Arg-N-(2-phenylethyl)amide pH 5.5, 25°C Homo sapiens