Literature summary for 3.4.21.73 extracted from

Frederickson, M.; Callaghan, O.; Chessari, G.; Congreve, M.; Cowan, S.R.; Matthews, J.E.; McMenamin, R.; Smith, D.M.; Vinkovic, M.; Wallis, N.G.
Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator (2008), J. Med. Chem., 51, 183-186.

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Crystallization (Commentary)

Crystallization (Comment)	Organism
in complex with inhibitors mexiletine and 4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide	Rattus norvegicus

Inhibitors

Inhibitors	Comment	Organism	Structure
4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide	inhibitor with moderate clearance level, high volume of distribution, and long half-life of 7.5 hours. More than 50 fold selective for uPA over all but one of the enzymes tested. Selectivity against trypsin is only 3- to 4fold	Rattus norvegicus
mexiletine	IC50 value above 1 mM, crystallographic data	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000072	-	-	Rattus norvegicus	4-(2-aminoethoxy)-N-(3-chloro-2-ethoxy-5-piperidin-1-ylphenyl)-3,5-dimethylbenzamide

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Release 2023.1 (January 2023)