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Literature summary 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

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.1.1.146 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

EC Number Inhibitors Comment Organism Structure
1.1.1.146 1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
-
Homo sapiens
1.1.1.146 2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
Homo sapiens
1.1.1.146 2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
-
Homo sapiens
1.1.1.146 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-(3-fluoro-4-methylphenyl)pyridine
-
Homo sapiens
1.1.1.146 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
-
Homo sapiens
1.1.1.146 2-[[(2,6-dichlorophenyl)thio]methyl]-6-[(4-methylpiperidin-1-yl)carbonyl]pyridine
-
Homo sapiens
1.1.1.146 azonan-1-yl(6-[[(2,6-dichlorophenyl)sulfonyl]methyl]pyridin-2-yl)methanone
-
Homo sapiens
1.1.1.146 [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
1.1.1.146 [5-[(2,4-dichlorophenoxy)methyl]pyridin-3-yl][2-(pyridin-3-yl)piperidin-1-yl]methanone
-
Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.1.1.146 microsome
-
Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.146 Homo sapiens
-
type I isoform
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.146 HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.146 1,2-dehydrocortisone + NADPH
-
Homo sapiens 1,2-dehydrocortisol + NADP+
-
?
1.1.1.146 cortisone + NADPH + H+
-
Homo sapiens cortisol + NADP+
-
?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.146 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
1.1.1.146 0.0000011
-
pH and temperature not specified in the publication Homo sapiens 2-(4-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine
1.1.1.146 0.0000011
-
pH and temperature not specified in the publication Homo sapiens 2-[(3,3-dimethylpiperidin-1-yl)carbonyl]-6-[4-(trifluoromethoxy)phenyl]pyridine
1.1.1.146 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
1.1.1.146 0.000002
-
pH and temperature not specified in the publication Homo sapiens 1-[[6-(4-nitrophenyl)pyridin-2-yl]carbonyl]decahydroquinoline
1.1.1.146 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
1.1.1.146 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
1.1.1.146 0.0000029
-
pH and temperature not specified in the publication Homo sapiens 2-(2-chlorophenyl)-6-[(3,3-dimethylpiperidin-1-yl)carbonyl]pyridine