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Literature summary for 3.1.1.4 extracted from

  • Althaus, J.; Hake, T.; Hanekamp, W.; Lehr, M.
    1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2? and fatty acid amide hydrolase bioisosteric replacement of the carboxylic acid moiety (2016), J. Enzyme Inhib. Med. Chem., 31, 131-140 .
    View publication on PubMed
Search for more literature for 3.1.1.4

Inhibitors

Inhibitors Comment Organism Structure
1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
 Homo sapiens
1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
 Homo sapiens
1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid
-
 Homo sapiens
2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
 Homo sapiens
2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
 Homo sapiens
methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
 Homo sapiens
additional information indazole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 are reported to be potent dual inhibitors of cytosolic phospholipase A2alpha and fatty acid amide hydrolase. The carboxylic acid functionality of the lead compounds is of special importance for a pronounced inhibition of cytosolic phospholipase A2alpha and fatty acid amide hydrolase Homo sapiens
N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
 Homo sapiens
N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
-
 Homo sapiens
N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
-
 Homo sapiens
phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
phospholipase A2alpha
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens 1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazole-5-carboxylic acid
0.00013
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
0.00029
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens N-cyclohexyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
0.00055
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens phenyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
0.00059
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens 2-methoxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
0.00066
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens 2-hydroxy-N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]acetamide
0.0016
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens 1-(5-nitro-1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
0.0019
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens N-ethyl-N'-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]urea
0.0021
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens methyl [1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamate
0.0063
-
 37°C, pH 8.0, substrate 1-stearoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Homo sapiens 1-(1H-indazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one