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Literature summary for 3.4.21.59 extracted from

  • Schaschke, N.; Sommerhoff, C.
    Upgrading a natural product: Inhibition of human beta-tryptase by cyclotheonamide analogues (2010), ChemMedChem, 5, 367-370.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]butanamide
-
Homo sapiens
5-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]pentanamide
-
Homo sapiens
6-amino-N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
Homo sapiens
6-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
Homo sapiens
7-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]heptanamide
-
Homo sapiens
APC-366
-
Homo sapiens
cyclotheonamide E4
-
Homo sapiens
N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
Homo sapiens
N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
mast cell
-
Homo sapiens
-

Subunits

Subunits Comment Organism
homotetramer 2 * 000, SDS-PAGE Homo sapiens

Synonyms

Synonyms Comment Organism
beta-tryptase
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
6-amino-N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
Homo sapiens
0.000012
-
5-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]pentanamide
-
Homo sapiens
0.000016
-
6-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]hexanamide
-
Homo sapiens
0.000023
-
7-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]heptanamide
-
Homo sapiens
0.001
-
4-amino-N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]butanamide
-
Homo sapiens
0.04
-
N-[(9S,12R,16R)-12-[(2S)-butan-2-yl]-16-(3-carbamimidamidopropyl)-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
Homo sapiens
0.38
-
N-[(9S,12R,16R)-16-(4-aminobutyl)-12-[(2S)-butan-2-yl]-9-(4-hydroxybenzyl)-2,6,11,14,18-pentaoxo-1,5,10,13,17-pentaazabicyclo[17.2.1]docos-7-en-3-yl]acetamide
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000051
-
-
Homo sapiens cyclotheonamide E4