Literature summary for 1.1.1.146 extracted from

Rew, Y.; McMinn, D.L.; Wang, Z.; He, X.; Hungate, R.W.; Jaen, J.C.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Villemure, E.; Walker, N.P.; Yan, X.; Ye, Q.; Powers, J.P.
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 1797-1801.

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in HEK-293 cells	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	potent 11beta-HSD1 inhibitor	Homo sapiens
N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens
N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide	-	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P28845	-	-

Synonyms

Synonyms	Comment	Organism
11beta-HSD1	-	Homo sapiens
11beta-hydroxysteroid dehydrogenase type 1	-	Homo sapiens
HSD1	-	Homo sapiens

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000006	-	-	Homo sapiens	N-[trans-4-(2-cyano-2-cyclopropylethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000007	-	-	Homo sapiens	N-[trans-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.00000088	-	-	Homo sapiens	N-[trans-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000014	-	-	Homo sapiens	N-cyclopropyl-N-(trans-4-pyridin-3-ylcyclohexyl)-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000017	-	-	Homo sapiens	N-[trans-4-[(1-carbamoylcyclopropyl)methyl]cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.000002	-	-	Homo sapiens	N-[cis-4-(2-cyano-2-methylpropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000024	-	-	Homo sapiens	N-[trans-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000028	-	-	Homo sapiens	N-[cis-4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000038	-	-	Homo sapiens	N-[trans-4-(3-amino-2,2-dimethyl-3-oxopropyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000055	-	-	Homo sapiens	N-[trans-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.0000076	-	-	Homo sapiens	N-[cis-4-(cyanomethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.000011	-	-	Homo sapiens	N-[cis-4-(4-amino-4-oxobutyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.000011	-	-	Homo sapiens	N-[1-[(1-cyanocyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.000014	-	-	Homo sapiens	N-[1-[(1-carbamoylcyclopropyl)methyl]piperidin-4-yl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide
0.000036	-	-	Homo sapiens	N-[4-(2-amino-2-oxoethyl)cyclohexyl]-N-cyclopropyl-4-[(1S)-2,2,2-trifluoro-1-hydroxy-1-methylethyl]benzamide

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Release 2023.1 (January 2023)