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Literature summary for 1.1.1.146 extracted from

  • Wang, H.; Ruan, Z.; Li, J.J.; Simpkins, L.M.; Smirk, R.A.; Wu, S.C.; Hutchins, R.D.; Nirschl, D.S.; Van Kirk, K.; Cooper, C.B.; Sutton, J.C.; Ma, Z.; Golla, R.; Seethala, R.; Salyan, M.E.; Nayeem, A.; Krystek, S.R.; Sheriff, S.; Camac, D.M.; Morin, P.E.; Carpenter, B.; Robl, J.A.; Zahler, R.; Gordon, D.A.; Hamann, L.G.
    Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (2008), Bioorg. Med. Chem. Lett., 18, 3168-3172.
    View publication on PubMed
Search for more literature for 1.1.1.146

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitor 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine. The carbonyl oxygen of the inhibitor is within hydrogen bonding distance to active site residues S170 and Y183, the inhibitor also forms hydrophobic interactions with the protein Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
-
 Homo sapiens
2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
 Homo sapiens
2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
 Homo sapiens
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
-
 Homo sapiens
2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
-
 Homo sapiens
2-[[(2,6-dichlorophenyl)thio]methyl]-6-[(4-methylpiperidin-1-yl)carbonyl]pyridine
-
 Homo sapiens
azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
-
 Homo sapiens
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
-
 Homo sapiens
[5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 type I isoform
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000001
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
0.0000011
-
 pH and temperature not specified in the publication Homo sapiens 2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
0.0000011
-
 pH and temperature not specified in the publication Homo sapiens 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
0.0000017
-
 pH and temperature not specified in the publication Homo sapiens [5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][(1R,5S)-1,3,3-trimethyl-6-azabicyclo[3.2.1]oct-6-yl]methanone
0.000002
-
 pH and temperature not specified in the publication Homo sapiens 1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
0.000002
-
 pH and temperature not specified in the publication Homo sapiens [5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
0.0000025
-
 pH and temperature not specified in the publication Homo sapiens azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
0.0000029
-
 pH and temperature not specified in the publication Homo sapiens 2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine