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Literature summary for 3.4.23.5 extracted from

  • Li, Z.; Bao, K.; Xu, H.; Wu, P.; Li, W.; Liu, J.; Zhang, W.
    Design, synthesis, and bioactivities of tasiamide B derivatives as cathepsin D inhibitors (2019), J. Pept. Sci., 25, e3154 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(5S,8S,11S,12S,16S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7-methyl-16-(2-methylpropyl)-3,6,9,14-tetraoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15-tetraazaheptadecan-17-oic acid
-
Homo sapiens
(5S,8S,11S,12S,16S,19S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7,19-dimethyl-16-(2-methylpropyl)-3,6,9,14,17-pentaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18-pentaazaicosan-20-oic acid
-
Homo sapiens
(5S,8S,11S,12S,16S,19S,22R)-8-(3-amino-3-oxopropyl)-11,22-dibenzyl-12-hydroxy-7,19,21-trimethyl-16-(2-methylpropyl)-3,6,9,14,17,20-hexaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18,21-hexaazatricosan-23-oic acid
-
Homo sapiens
(6S,9S,12S,13S,17S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8-trimethyl-17-(2-methylpropyl)-4,7,10,15-tetraoxo-6-(propan-2-yl)-3-oxa-5,8,11,16-tetraazaoctadecan-18-oic acid
-
Homo sapiens
(6S,9S,12S,13S,17S,20S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8,20-tetramethyl-17-(2-methylpropyl)-4,7,10,15,18-pentaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19-pentaazahenicosan-21-oic acid
-
Homo sapiens
(6S,9S,12S,13S,17S,20S,23R)-9-(3-amino-3-oxopropyl)-12,23-dibenzyl-13-hydroxy-2,2,8,20,22-pentamethyl-17-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19,22-hexaazatetracosan-24-oic acid
-
Homo sapiens
4-([N-[(benzyloxy)carbonyl]-L-valyl-N2-methyl-L-glutaminyl]amino)-2,4,5-trideoxy-5-phenyl-L-threo-pentonic acid
-
Homo sapiens
methyl (5S,8S,11S,12S,16S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7-methyl-16-(2-methylpropyl)-3,6,9,14-tetraoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15-tetraazaheptadecan-17-oate
-
Homo sapiens
methyl (5S,8S,11S,12S,16S,19S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7,19-dimethyl-16-(2-methylpropyl)-3,6,9,14,17-pentaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18-pentaazaicosan-20-oate
-
Homo sapiens
methyl (5S,8S,11S,12S,16S,19S,22R)-8-(3-amino-3-oxopropyl)-11,22-dibenzyl-12-hydroxy-7,19,21-trimethyl-16-(2-methylpropyl)-3,6,9,14,17,20-hexaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18,21-hexaazatricosan-23-oate
-
Homo sapiens
methyl (6S,9S,12S,13S,17S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8-trimethyl-17-(2-methylpropyl)-4,7,10,15-tetraoxo-6-(propan-2-yl)-3-oxa-5,8,11,16-tetraazaoctadecan-18-oate
-
Homo sapiens
methyl (6S,9S,12S,13S,17S,20S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8,20-tetramethyl-17-(2-methylpropyl)-4,7,10,15,18-pentaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19-pentaazahenicosan-21-oate
-
Homo sapiens
methyl (6S,9S,12S,13S,17S,20S,23R)-9-(3-amino-3-oxopropyl)-12,23-dibenzyl-13-hydroxy-2,2,8,20,22-pentamethyl-17-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19,22-hexaazatetracosan-24-oate
-
Homo sapiens
pepstatin A
-
Homo sapiens
tasiamide B
-
Homo sapiens
TB-11
-
Homo sapiens
Tb-9
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
Cath D
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000000783
-
at pH 3.5 and 25°C Homo sapiens Tb-9
0.000000126
-
at pH 3.5 and 25°C Homo sapiens TB-11
0.000000182
-
at pH 3.5 and 25°C Homo sapiens tasiamide B
0.000000693
-
at pH 3.5 and 25°C Homo sapiens pepstatin A
0.00000329
-
at pH 3.5 and 25°C Homo sapiens methyl (5S,8S,11S,12S,16S,19S,22R)-8-(3-amino-3-oxopropyl)-11,22-dibenzyl-12-hydroxy-7,19,21-trimethyl-16-(2-methylpropyl)-3,6,9,14,17,20-hexaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18,21-hexaazatricosan-23-oate
0.000027
-
at pH 3.5 and 25°C Homo sapiens (5S,8S,11S,12S,16S,19S,22R)-8-(3-amino-3-oxopropyl)-11,22-dibenzyl-12-hydroxy-7,19,21-trimethyl-16-(2-methylpropyl)-3,6,9,14,17,20-hexaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18,21-hexaazatricosan-23-oic acid
0.000102
-
at pH 3.5 and 25°C Homo sapiens methyl (5S,8S,11S,12S,16S,19S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7,19-dimethyl-16-(2-methylpropyl)-3,6,9,14,17-pentaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18-pentaazaicosan-20-oate
0.000108
-
at pH 3.5 and 25°C Homo sapiens (5S,8S,11S,12S,16S,19S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7,19-dimethyl-16-(2-methylpropyl)-3,6,9,14,17-pentaoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15,18-pentaazaicosan-20-oic acid
0.000131
-
at pH 3.5 and 25°C Homo sapiens (6S,9S,12S,13S,17S,20S,23R)-9-(3-amino-3-oxopropyl)-12,23-dibenzyl-13-hydroxy-2,2,8,20,22-pentamethyl-17-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19,22-hexaazatetracosan-24-oic acid
0.00019
-
at pH 3.5 and 25°C Homo sapiens methyl (6S,9S,12S,13S,17S,20S,23R)-9-(3-amino-3-oxopropyl)-12,23-dibenzyl-13-hydroxy-2,2,8,20,22-pentamethyl-17-(2-methylpropyl)-4,7,10,15,18,21-hexaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19,22-hexaazatetracosan-24-oate
0.000196
-
at pH 3.5 and 25°C Homo sapiens methyl (5S,8S,11S,12S,16S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7-methyl-16-(2-methylpropyl)-3,6,9,14-tetraoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15-tetraazaheptadecan-17-oate
0.000407
-
at pH 3.5 and 25°C Homo sapiens methyl (6S,9S,12S,13S,17S,20S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8,20-tetramethyl-17-(2-methylpropyl)-4,7,10,15,18-pentaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19-pentaazahenicosan-21-oate
0.000903
-
at pH 3.5 and 25°C Homo sapiens (6S,9S,12S,13S,17S,20S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8,20-tetramethyl-17-(2-methylpropyl)-4,7,10,15,18-pentaoxo-6-(propan-2-yl)-3-oxa-5,8,11,16,19-pentaazahenicosan-21-oic acid
0.005
-
IC50 above 0.005 mM, at pH 3.5 and 25°C Homo sapiens (6S,9S,12S,13S,17S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8-trimethyl-17-(2-methylpropyl)-4,7,10,15-tetraoxo-6-(propan-2-yl)-3-oxa-5,8,11,16-tetraazaoctadecan-18-oic acid
0.006384
-
at pH 3.5 and 25°C Homo sapiens (5S,8S,11S,12S,16S)-8-(3-amino-3-oxopropyl)-11-benzyl-12-hydroxy-7-methyl-16-(2-methylpropyl)-3,6,9,14-tetraoxo-1-phenyl-5-(propan-2-yl)-2-oxa-4,7,10,15-tetraazaheptadecan-17-oic acid
0.01
-
IC50 above 0.01 mM, at pH 3.5 and 25°C Homo sapiens 4-([N-[(benzyloxy)carbonyl]-L-valyl-N2-methyl-L-glutaminyl]amino)-2,4,5-trideoxy-5-phenyl-L-threo-pentonic acid
0.01
-
IC50 above 0.01 mM, at pH 3.5 and 25°C Homo sapiens methyl (6S,9S,12S,13S,17S)-9-(3-amino-3-oxopropyl)-12-benzyl-13-hydroxy-2,2,8-trimethyl-17-(2-methylpropyl)-4,7,10,15-tetraoxo-6-(propan-2-yl)-3-oxa-5,8,11,16-tetraazaoctadecan-18-oate