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Literature summary for 1.1.1.146 extracted from

  • Julian, L.D.; Wang, Z.; Bostick, T.; Caille, S.; Choi, R.; Degraffenreid, M.; Di, Y.; He, X.; Hungate, R.W.; Jaen, J.C.; Liu, J.; Monshouwer, M.; McMinn, D.; Rew, Y.; Sudom, A.; Sun, D.; Tu, H.; Ursu, S.; Walker, N.; Yan, X.; Ye, Q.; Powers, J.P.
    Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model (2008), J. Med. Chem., 51, 3953-3960.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
Homo sapiens
N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
Homo sapiens
N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
Homo sapiens
N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
Homo sapiens
N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
type I isoform
-
Homo sapiens P28845 type I isoform
-
Macaca fascicularis
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1,2-dehydrocortisone + NADPH
-
Homo sapiens 1,2-dehydrocortisol + NADP+
-
?
1,2-dehydrocortisone + NADPH
-
Macaca fascicularis 1,2-dehydrocortisol + NADP+
-
?
cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000007
-
pH and temperature not specified in the publication Homo sapiens N-[4(4-cyanophenyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
0.0000007
-
pH and temperature not specified in the publication Homo sapiens N-[4-(3-cyanopropyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
0.0000008
-
pH and temperature not specified in the publication Homo sapiens N-cyclohexyl-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
0.0000014
-
pH and temperature not specified in the publication Homo sapiens N-[4-(3-pyridyl)cyclohexyl]-N-cyclopropyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide
0.0000017
-
pH and temperature not specified in the publication Homo sapiens N-cyclohexyl-N-ethyl-4-[(2S)-1,1,1-trifluoro-2-hydroxypropan-2-yl]benzamide