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Literature summary for 4.4.1.20 extracted from

  • Kleinschmidt, T.K.; Haraldsson, M.; Basavarajappa, D.; Lundeberg, E.; Thulasingam, M.; Ekoff, M.; Fauland, A.; Lehmann, C.; Kahnt, A.S.; Lindbom, L.; Haeggstroem, J.Z.
    Tandem benzophenone amino pyridines, potent and selective inhibitors of human leukotriene C4 synthase (2015), J. Pharmacol. Exp. Ther., 355, 108-116 .
    View publication on PubMed
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
molecular docking of inhibitors 2-benzoyl-5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]benzoic acid, 5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid, 5-[5-[(4-chlorophenyl)(cyclopropylmethyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid. Inhibitors interact with catalytic residues R104 and R31 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-benzoyl-5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]benzoic acid potent and selective inhibitor, potently inhibits cysteinyl leukotriene biosynthesis in immune cells Homo sapiens
5-[5-[(4-chlorophenyl)(cyclopropylmethyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid compound at 6 mg/kg body weight reduces LTE4 levels in peritoneal lavage fluid by 88%and significantly decreases vascular permeability in vivo. Potent and selective inhibitor, potently inhibits cysteinyl leukotriene biosynthesis in immune cells Homo sapiens
5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid potent and selective inhibitor, potently inhibits cysteinyl leukotriene biosynthesis in immune cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16873
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000095
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[5-[(4-chlorophenyl)(cyclopropylmethyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid
0.000116
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-benzoyl-5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]benzoic acid
0.000124
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[5-[(4-chlorophenyl)(methyl)amino]pyridine-2-carbonyl]-2-(4-methoxybenzoyl)benzoic acid

General Information

General Information Comment Organism
physiological function in coincubations of platelets and polymorphonuclear leukocytes, inhibition of LTC4S leads to shunting of LTA4 toward anti-inflammatory lipoxin A4, which is significantly enhanced by simultaneous inhibition of LTA4H Homo sapiens