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Literature summary for 1.13.11.34 extracted from

  • Hiesinger, K.; Kramer, J.S.; Beyer, S.; Eckes, T.; Brunst, S.; Flauaus, C.; Wittmann, S.K.; Weizel, L.; Kaiser, A.; Kretschmer, S.B.M.; George, S.; Angioni, C.; Heering, J.; Geisslinger, G.; Schubert-Zsilavecz, M.; Schmidtko, A.; Pogoryelov, D.; Pfeilschifter, J.; Hofmann, B.; Steinhilber, D.; Sch, S.c.h.w.
    Design, synthesis, and structure-activity relationship studies of dual inhibitors of soluble epoxide hydrolase and 5-lipoxygenase (2020), J. Med. Chem., 63, 11498-11521 .
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(R)-N-(2-(diphenylamino)ethyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
(R)-N-(3,3-bis(4-fluorophenyl)propyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(3-phenyl-3-(4-(trifluoromethoxy)phenyl)propyl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(4-methoxy-2-(trifluoromethyl)benzyl)-benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
3-(3-(1-hydroxyureido)hex-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens
4-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor, displays cellular activity in human polymorphonuclear leukocytes, oral bioavailability, and target engagement in vivo and demonstrates anti-inflammatory and anti-fibrotic efficiency in a kidney injury model caused by unilateral ureteral obstruction in mice Homo sapiens
N-(3-(4-chlorophenyl)-3-phenylpropyl)-3-(3-(1-hydroxyureido)-but-1-yn-1-yl)benzamide dual 5-LOX/soluble epoxide hydrolase inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09917
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00011
-
 pH 7.4, 37°C Homo sapiens (R)-N-(2-(diphenylamino)ethyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
0.00011
-
 pH 7.4, 37°C Homo sapiens (R)-N-(3,3-bis(4-fluorophenyl)propyl)-3-(3-(1-hydroxyureido)but-1-yn-1-yl)benzamide
0.00011
-
 pH 7.4, 37°C Homo sapiens 3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(3-phenyl-3-(4-(trifluoromethoxy)phenyl)propyl)benzamide
0.00012
-
 pH 7.4, 37°C Homo sapiens N-(3-(4-chlorophenyl)-3-phenylpropyl)-3-(3-(1-hydroxyureido)-but-1-yn-1-yl)benzamide
0.0003
-
 pH 7.4, 37°C Homo sapiens 3-(3-(1-hydroxyureido)hex-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
0.0007
-
 pH 7.4, 37°C Homo sapiens 3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
0.001
-
 pH 7.4, 37°C Homo sapiens 4-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(2-(trifluoromethyl)-benzyl)benzamide
0.0017
-
 pH 7.4, 37°C Homo sapiens 3-(3-(1-hydroxyureido)but-1-yn-1-yl)-N-(4-methoxy-2-(trifluoromethyl)benzyl)-benzamide