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Literature summary extracted from

  • Tanaka, T.; Muto, T.; Maruoka, H.; Imajo, S.; Fukami, H.; Tomimori, Y.; Fukuda, Y.; Nakatsuka, T.
    Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 3431-3434.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.39
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.39 (6E)-4-[(4-chlorophenyl)sulfonyl]-6-(phenylmethylidene)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 (6R)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 (6S)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione potent inhibitor Homo sapiens
3.4.21.39 2-[4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]-N-methylacetamide
-
 Homo sapiens
3.4.21.39 3-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)-4-methoxybenzonitrile
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(2,5-dimethoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(2-ethoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(2-fluorobenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(4,5-dichloro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(5-chloro-2-propoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(5-fluoro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(5-hydroxy-2-methoxybenzyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(cyclohexylmethyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(naphthalen-2-ylmethyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-3-ylmethyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-4-ylmethyl)-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(2-butoxy-5-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(2-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(3-chloro-5-fluoro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(3-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(4-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(5-chloro-2-ethoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 6-benzyl-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
-
 Homo sapiens
3.4.21.39 chymostatin
-
 Homo sapiens
3.4.21.39 [4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]acetic acid
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.39 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.39
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.39 mast cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.39 angiotensin I + H2O
-
 Homo sapiens angiotensin II + ?
-
 ?
3.4.21.39 succinyl-Ala-Ala-Pro-Phe-4-nitroanilide + H2O
-
 Homo sapiens succinyl-Ala-Ala-Pro-Phe + 4-nitroaniline
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.39 0.000018
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.000023
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(4,5-dichloro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.000026
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(5-fluoro-2-methoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.000027
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 3-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)-4-methoxybenzonitrile
3.4.21.39 0.000027
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens (6S)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.000034
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.000039
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens [4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]acetic acid
3.4.21.39 0.000042
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 2-[4-chloro-2-([1-[(4-chlorophenyl)sulfonyl]-3,7-dioxo-1,4-diazepan-6-yl]methyl)phenoxy]-N-methylacetamide
3.4.21.39 0.000043
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens chymostatin
3.4.21.39 0.000083
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(5-chloro-2-ethoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.00011
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(2-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.00014
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(2-methoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.00015
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(2-fluorobenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.00018
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(2-ethoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.00022
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(5-chloro-2-propoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.00028
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(2-butoxy-5-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.00031
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(3-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.00042
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-benzyl-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.00046
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(4-chlorobenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.0011
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(5-hydroxy-2-methoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.0015
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens (6E)-4-[(4-chlorophenyl)sulfonyl]-6-(phenylmethylidene)-1,4-diazepane-2,5-dione
3.4.21.39 0.0042
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 6-(3-chloro-5-fluoro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione
3.4.21.39 0.0074
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(2,5-dimethoxybenzyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.01
-
 IC50 above 0.01 mM, in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(cyclohexylmethyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.01
-
 IC50 above 0.01 mM, in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(naphthalen-2-ylmethyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.01
-
 IC50 above 0.01 mM, in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-3-ylmethyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.01
-
 IC50 above 0.01 mM, in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens 4-[(4-chlorophenyl)sulfonyl]-6-(pyridin-4-ylmethyl)-1,4-diazepane-2,5-dione
3.4.21.39 0.01
-
 in 50 mM Tris/HCl buffer (pH 7.5) containing 1 M NaCl and 0.01% Triton X-100 Homo sapiens (6R)-6-(5-chloro-2-methoxybenzyl)-4-[(4-chlorophenyl)sulfonyl]-1,4-diazepane-2,5-dione