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Literature summary for 3.4.21.37 extracted from

  • Crocetti, L.; Giovannoni, M.P.; Schepetkin, I.A.; Quinn, M.T.; Khlebnikov, A.I.; Cilibrizzi, A.; Piaz, V.D.; Graziano, A.; Vergelli, C.
    Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase (2011), Bioorg. Med. Chem., 19, 4460-4472.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.37

Inhibitors

Inhibitors Comment Organism Structure
(3-methylindazol-1-yl)-m-tolyl-methanone
-
 Homo sapiens
1-(2-methylbenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid methyl ester
-
 Homo sapiens
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid propyl ester
-
 Homo sapiens
1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid methyl ester
-
 Homo sapiens
1-(4-cyanobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid methyl ester
-
 Homo sapiens
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid propyl ester
-
 Homo sapiens
1-benzoyl-1H-indazole-3-carboxylic acid methyl ester
-
 Homo sapiens
1-benzoyl-1H-indazole-3-carboxylic acid phenylamide
-
 Homo sapiens
1-butyryl-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-cyclopentanecarbonyl-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-propionyl-1H-indazole-3-carboxylic acid ethyl ester
-
 Homo sapiens
1-[(3-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(3-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(3-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(3-nitrophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(4-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(4-cyanophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(4-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1-[(4-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
-
 Homo sapiens
1H-indazol-1-yl(3-methylphenyl)methanone
-
 Homo sapiens
2,2,2-trifluoroethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
2,2,2-trifluoroethyl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
2,2,2-trifluoroethyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
2,2,2-trifluoroethyl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
2,2,2-trifluoroethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-(1,3-benzodioxol-5-ylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-acetyl-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(2-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(3-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(3-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(4-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(4-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
ethyl 1-[(4-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
additional information not inhibited by 1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid, (3-methoxyphenyl)-(3-methylindazol-1-yl)-methanone, 1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(naphthalene-1-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(3,4,5-trimethoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(pyridine-4-carbonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(toluene-4-sulfonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorobenzenesulfonyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorobenzyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(4-chlorophenyl)-1H-indazole-3-carboxylic acid phenylamide, 1-(2-oxo-2-phenylethyl)-1H-indazole-3-carboxylic acid ethyl ester, 1-(4-chlorophenylcarbamoyl)-1H-indazole-3-carboxylic acid ethyl ester, and 1-(3-methoxyphenylcarbamoyl)-1H-indazole-3-carboxylic acid ethyl ester Homo sapiens
propan-2-yl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
propan-2-yl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
propan-2-yl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
propan-2-yl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
propan-2-yl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
propyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
-
 Homo sapiens
propyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
propyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
-
 Homo sapiens
sivelestat ONO-5046, competitive and selective inhibitor Homo sapiens

Organic Solvent Stability

Organic Solvent Comment Organism
DMSO 1% (v/v) DMSO has no effect on enzyme activity Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens N-methoxysuccinyl-L-Ala-L-Ala-L-Pro-L-Val + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
HNE
-
 Homo sapiens
neutrophil elastase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000089
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-benzoyl-1H-indazole-3-carboxylic acid methyl ester
0.00013
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-methylbenzoyl)-1H-indazole-3-carboxylic acid methyl ester
0.00018
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-butyryl-1H-indazole-3-carboxylic acid ethyl ester
0.00024
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propan-2-yl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
0.00026
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 2,2,2-trifluoroethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
0.00031
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid methyl ester
0.00034
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 2,2,2-trifluoroethyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
0.0004
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
0.0004
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propyl 1-(phenylcarbonyl)-1H-indazole-3-carboxylate
0.0004
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-propionyl-1H-indazole-3-carboxylic acid ethyl ester
0.00041
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
0.00042
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-benzoyl-1H-indazole-3-carboxylic acid phenylamide
0.00046
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 2,2,2-trifluoroethyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
0.00048
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-cyclopentanecarbonyl-1H-indazole-3-carboxylic acid ethyl ester
0.00051
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propan-2-yl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
0.00051
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 2,2,2-trifluoroethyl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
0.00055
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid methyl ester
0.00065
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propan-2-yl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
0.00069
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propan-2-yl 1-(thiophen-3-ylcarbonyl)-1H-indazole-3-carboxylate
0.0007
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propyl 1-[(3-aminophenyl)carbonyl]-1H-indazole-3-carboxylate
0.00076
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propan-2-yl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
0.00078
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens propyl 1-[(3-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
0.0008
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
0.00089
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 2,2,2-trifluoroethyl 1-[(3-methoxyphenyl)carbonyl]-1H-indazole-3-carboxylate
0.00093
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid ethyl ester
0.0016
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
0.0017
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(3-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
0.0017
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(3-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
0.0018
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid phenylamide
0.0019
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-methoxybenzoyl)-1H-indazole-3-carboxylic acid propyl ester
0.0019
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid propyl ester
0.0031
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(thiophene-3-carbonyl)-1H-indazole-3-carboxylic acid phenylamide
0.0031
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(3-aminobenzoyl)-1H-indazole-3-carboxylic acid phenylamide
0.0039
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(3-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.0048
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-acetyl-1H-indazole-3-carboxylate
0.0057
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(4-fluorophenyl)carbonyl]-1H-indazole-3-carboxylate
0.0059
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(3-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.0061
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(4-chlorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.0081
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(4-fluorophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.0093
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(3-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.01
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1H-indazol-1-yl(3-methylphenyl)methanone
0.011
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(3-nitrophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.019
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(4-chlorophenyl)carbonyl]-1H-indazole-3-carboxylate
0.022
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens (3-methylindazol-1-yl)-m-tolyl-methanone
0.028
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-(1,3-benzodioxol-5-ylcarbonyl)-1H-indazole-3-carboxylate
0.029
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(4-methylphenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.034
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(2-methylbenzoyl)-1H-indazole-3-carboxylic acid phenylamide
0.036
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(4-methylphenyl)carbonyl]-1H-indazole-3-carboxylate
0.038
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-[(4-cyanophenyl)carbonyl]-N-phenyl-1H-indazole-3-carboxamide
0.038
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens 1-(4-cyanobenzoyl)-1H-indazole-3-carboxylic acid ethyl ester
0.052
-
 in 200 mM Tris-HCl, pH 7.5, at 25°C Homo sapiens ethyl 1-[(2-methylphenyl)carbonyl]-1H-indazole-3-carboxylate