Literature summary for 2.3.1.26 extracted from

Ohshiro, T.; Matsuda, D.; Nagai, K.; Doi, T.; Sunazuka, T.; Takahashi, T.; Rudel, L.L.; Omura, S.; Tomoda, H.
The selectivity of beauveriolide derivatives in inhibition toward the two isozymes of acyl-CoA: cholesterol acyltransferase (2009), Chem. Pharm. Bull., 57, 377-381.

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Cloned(Commentary)

Cloned (Comment)	Organism
expression of isoforms ACT1 and ACAT2 in CHO cell	Chlorocebus aethiops

Inhibitors

Inhibitors	Comment	Organism	Structure
(6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	inhibition of both isoforms ACAT1 and ACAT2; inhibition of both isoforms ACAT1 and ACAT2	Chlorocebus aethiops
(6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT1	Chlorocebus aethiops
(6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT2	Chlorocebus aethiops
(6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT1	Chlorocebus aethiops
(6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT1	Chlorocebus aethiops
(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT2	Chlorocebus aethiops
(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	selective inhibition of isoform ACAT2	Chlorocebus aethiops

Organism

Organism	UniProt	Comment	Textmining
Chlorocebus aethiops	O77759	isoform ACAT2	-
Chlorocebus aethiops	O77760	isoform ACAT1	-

Source Tissue

Source Tissue	Comment	Organism	Textmining

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00006	-	(6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.00009	-	(6R,9S,13S)-3-benzyl-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.0001	-	(6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.0001	-	(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.00015	-	(6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.00025	-	(6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.00027	-	(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.001	-	(6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.004	-	(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1R)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.004	-	(6S,9S,13S)-6-methyl-9-(4-methylbenzyl)-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.0065	-	(6S,9S,13S)-9-(3-chlorobenzyl)-6-methyl-13-[(1S)-1-methylbutyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops
0.01	-	(6S,9S,13S)-9-(diphenylmethyl)-6-methyl-13-[(1S)-1-methylpentyl]-3-[(1S)-1-methylpropyl]-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.02	-	(6S,9S,13S)-6-methyl-13-[(1S)-1-methylnonyl]-3-[(1S)-1-methylpropyl]-9-(naphthalen-2-ylmethyl)-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT1, 37°C	Chlorocebus aethiops
0.04	-	(6S,9S,13R)-9-(2-chlorobenzyl)-6-methyl-3-[(1S)-1-methylpropyl]-13-pentyl-1-oxa-4,7,10-triazacyclotridecane-2,5,8,11-tetrone	isoform ACAT2, 37°C	Chlorocebus aethiops

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Release 2023.1 (January 2023)