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Literature summary for 3.4.24.71 extracted from

  • Brands, M.; Ergueden, J.K.; Hashimoto, K.; Heimbach, D.; Schroeder, C.; Siegel, S.; Stasch, J.P.; Weigand, S.
    Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis (2005), Bioorg. Med. Chem. Lett., 15, 4201-4205.
    View publication on PubMed
Search for more literature for 3.4.24.71

Inhibitors

Inhibitors Comment Organism Structure
1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide IC50: 0.00065 mM Homo sapiens
1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide IC50: 0.00012 mM Homo sapiens
1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide IC50: 0.00086 mM Homo sapiens
4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid IC50: 0.00039 mM Homo sapiens
5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.00066 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.00022 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.003 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide IC50: 0.0022 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide IC50: 0.0059 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide IC50: 0.0051 mM Homo sapiens
5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide IC50: 0.00017 mM Homo sapiens
5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.00074 mM Homo sapiens
5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.0003 mM Homo sapiens
5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.0064 mM Homo sapiens
5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid IC50: 0.074 mM Homo sapiens
5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide IC50: 0.0067 mM Homo sapiens
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide IC50: 0.01 mM Homo sapiens
N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-[(phenylamino)methyl]-1H-indole-5-carboxamide IC50: 0.01 mM Homo sapiens
N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.00022 mM Homo sapiens
N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.0012 mM Homo sapiens
N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.00017 mM Homo sapiens
N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.00044 mM Homo sapiens
N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.00021 mM Homo sapiens
N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.0002 mM Homo sapiens
N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide IC50: 0.00013 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide IC50: 0.00015 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide IC50: 0.0023 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide IC50: 0.01 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide IC50: 0.007 mM; IC50: 0.01 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide IC50: 0.00085 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide IC50: 0.000039 mM Homo sapiens
N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide IC50: 0.09 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
ECE-1
-
 Homo sapiens
endothelin-converting enzyme-1
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000039
-
 IC50: 0.000039 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[3-[(4-sulfamoylphenyl)carbamoyl]phenyl]-1H-indole-2,5-dicarboxamide
0.00012
-
 IC50: 0.00012 mM Homo sapiens 1-(2-fluorobenzyl)-5-[[(1-methylcyclopentyl)acetyl]amino]-N-phenyl-1H-indole-2-carboxamide
0.00013
-
 IC50: 0.00013 mM Homo sapiens N2-[6-(acetylamino)pyridin-3-yl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.00015
-
 IC50: 0.00015 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-(3-[[4-(methylsulfamoyl)phenyl]carbamoyl]phenyl)-1H-indole-2,5-dicarboxamide
0.00017
-
 IC50: 0.00017 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-[2-(trifluoromethyl)benzyl]-1H-indole-2-carboxamide
0.00017
-
 IC50: 0.00017 mM Homo sapiens N2-(6-aminopyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.0002
-
 IC50: 0.0002 mM Homo sapiens N2-[4-[(butylsulfonyl)amino]phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.00021
-
 IC50: 0.00021 mM Homo sapiens N2-[4-(dimethylcarbamoyl)phenyl]-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.00022
-
 IC50: 0.00022 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.00022
-
 IC50: 0.00022 mM Homo sapiens N2-(4-carbamoylphenyl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.0003
-
 IC50: 0.0003 mM Homo sapiens 5-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.00039
-
 IC50: 0.00039 mM Homo sapiens 4-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]benzoic acid
0.00044
-
 IC50: 0.00044 mM Homo sapiens N2-(6-chloropyridin-3-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.00065
-
 IC50: 0.00065 mM Homo sapiens 1-(2,6-difluorobenzyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
0.00066
-
 IC50: 0.00066 mM Homo sapiens 5-[(3,3-dimethylbutanethioyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.00074
-
 IC50: 0.00074 mM Homo sapiens 5-[(4,4-dimethylpentanoyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.00085
-
 IC50: 0.00085 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-pyridin-3-yl-1H-indole-2,5-dicarboxamide
0.00086
-
 IC50: 0.00086 mM Homo sapiens 1-(cyclohexylmethyl)-5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1H-indole-2-carboxamide
0.0012
-
 IC50: 0.0012 mM Homo sapiens N2-(5-aminopyridin-2-yl)-N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-1H-indole-2,5-dicarboxamide
0.0022
-
 IC50: 0.0022 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-1-[(2-methyl-1,3-thiazol-4-yl)methyl]-N-phenyl-1H-indole-2-carboxamide
0.0023
-
 IC50: 0.0023 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1,3,4-thiadiazol-2-yl-1H-indole-2,5-dicarboxamide
0.003
-
 IC50: 0.003 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-1-(2-methylbenzyl)-N-phenyl-1H-indole-2-carboxamide
0.0051
-
 IC50: 0.0051 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-N-phenyl-1-(2-phenylethyl)-1H-indole-2-carboxamide
0.0059
-
 IC50: 0.0059 mM Homo sapiens 5-[(3,3-dimethylbutanoyl)amino]-N,1-diphenyl-1H-indole-2-carboxamide
0.0064
-
 IC50: 0.0064 mM Homo sapiens 5-[(cyclopentylacetyl)amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.0067
-
 IC50: 0.0067 mM Homo sapiens 5-[[(2,2-dimethylpropyl)sulfonyl]amino]-1-(2-fluorobenzyl)-N-phenyl-1H-indole-2-carboxamide
0.007
-
 IC50: 0.007 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
0.01
-
 IC50: 0.01 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-phenyl-1H-indole-2,5-dicarboxamide
0.01
-
 IC50: 0.01 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-1H-pyrazol-3-yl-1H-indole-2,5-dicarboxamide
0.01
-
 IC50: 0.01 mM Homo sapiens N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-[(phenylamino)methyl]-1H-indole-5-carboxamide
0.01
-
 IC50: 0.01 mM Homo sapiens N-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-2-(3-phenyl-1,2,4-oxadiazol-5-yl)-1H-indole-5-carboxamide
0.074
-
 IC50: 0.074 mM Homo sapiens 5-[([5-[(2,2-dimethylpropyl)carbamoyl]-1-(2-fluorobenzyl)-1H-indol-2-yl]carbonyl)amino]pyridine-3-carboxylic acid
0.09
-
 IC50: 0.09 mM Homo sapiens N5-(2,2-dimethylpropyl)-1-(2-fluorobenzyl)-N2-[5-[(4-methylpiperazin-1-yl)carbonyl]pyridin-3-yl]-1H-indole-2,5-dicarboxamide