Literature summary for 3.4.21.105 extracted from

Yang, J.; Barniol-Xicota, M.; Nguyen, M.T.N.; Ticha, A.; Strisovsky, K.; Verhelst, S.H.L.
Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases (2018), Bioorg. Med. Chem. Lett., 28, 1423-1427 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one	covalent, but slow reversible inhibition mechanism	Bacillus subtilis
2-(benzyloxy)-5-chloro-4H-3,1-benzoxazin-4-one	covalent, but slow reversible inhibition mechanism	Escherichia coli
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one	covalent, but slow reversible inhibition mechanism	Bacillus subtilis
2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one	covalent, but slow reversible inhibition mechanism	Escherichia coli
additional information	an alkoxy substituent at the 2-position of enzoxazin-4-one inhibitors is crucial for potency and results in low micromolar inhibitors of rhomboid proteases	Bacillus subtilis
additional information	an alkoxy substituent at the 2-position of enzoxazin-4-one inhibitors is crucial for potency and results in low micromolar inhibitors of rhomboid proteases	Escherichia coli

Organism

Organism	UniProt	Comment	Textmining
Bacillus subtilis	-	-	-
Escherichia coli	-	-	-

Synonyms

Synonyms	Comment	Organism
GlpG	-	Escherichia coli
Yqgp	-	Bacillus subtilis

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.001	-	pH not specified in the publication, temperature not specified in the publication	Escherichia coli	2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
0.0012	-	pH not specified in the publication, temperature not specified in the publication	Escherichia coli	2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
0.0016	-	pH not specified in the publication, temperature not specified in the publication	Bacillus subtilis	2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one
0.015	-	pH not specified in the publication, temperature not specified in the publication	Bacillus subtilis	2-(benzyloxy)-5-methyl-4H-3,1-benzoxazin-4-one

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Release 2023.1 (January 2023)