Literature summary for 2.3.1.26 extracted from

Ban, H.; Muraoka, M.; Ioriya, K.; Ohashi, N.
Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubility (2006), Bioorg. Med. Chem. Lett., 16, 44-48.

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Inhibitors

Inhibitors	Comment	Organism	Structure
1-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]-3-{4-[(ethylamino)methyl]-2,6-bis(1-methylethyl)phenyl}urea	IC50: 680 nM	Rattus norvegicus
1-[2,4-bis(1-methylethyl)pyridin-3-yl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea	IC50: 5.4 nM	Rattus norvegicus
1-[3-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea	IC50: 43 nM	Rattus norvegicus
1-[4-(aminomethyl)-2,6-bis(1-methylethyl)phenyl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea	IC50: 382 nM	Rattus norvegicus
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-(1-butyl-4-{3-[3-(ethylamino)propoxy]phenyl}-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl)urea	IC50: 452 nM	Rattus norvegicus
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-piperidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea	IC50: 540 nM	Rattus norvegicus
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-pyrrolidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea	IC50: 427 nM	Rattus norvegicus
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea	i.e. SMP-797, possessing a potent ACAT inhibitory activity and significantly enhanced aqueous solubility under acidic conditions. The compound is a promising agent for oral treatment of hypercholesterolemia.IC50: 21 nM	Rattus norvegicus
1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(4-hydroxybutoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea	IC50: 61 nM	Rattus norvegicus
SM-32504	IC50: 11 nM	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000054	-	IC50: 5.4 nM	Rattus norvegicus	1-[2,4-bis(1-methylethyl)pyridin-3-yl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea
0.000011	-	IC50: 11 nM	Rattus norvegicus	SM-32504
0.000021	-	i.e. SMP-797, possessing a potent ACAT inhibitory activity and significantly enhanced aqueous solubility under acidic conditions. The compound is a promising agent for oral treatment of hypercholesterolemia.IC50: 21 nM	Rattus norvegicus	1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
0.000043	-	IC50: 43 nM	Rattus norvegicus	1-[3-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(3-hydroxypropoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
0.000061	-	IC50: 61 nM	Rattus norvegicus	1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-4-[3-(4-hydroxybutoxy)phenyl]-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
0.000382	-	IC50: 382 nM	Rattus norvegicus	1-[4-(aminomethyl)-2,6-bis(1-methylethyl)phenyl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]urea
0.000427	-	IC50: 427 nM	Rattus norvegicus	1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-pyrrolidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
0.000452	-	IC50: 452 nM	Rattus norvegicus	1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-(1-butyl-4-{3-[3-(ethylamino)propoxy]phenyl}-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl)urea
0.00054	-	IC50: 540 nM	Rattus norvegicus	1-[4-amino-2,6-bis(1-methylethyl)phenyl]-3-{1-butyl-2-oxo-4-[3-(3-piperidin-1-ylpropoxy)phenyl]-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl}urea
0.00068	-	IC50: 680 nM	Rattus norvegicus	1-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,2,4a,8a-tetrahydro-1,8-naphthyridin-3-yl]-3-{4-[(ethylamino)methyl]-2,6-bis(1-methylethyl)phenyl}urea

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Release 2023.1 (January 2023)