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Literature summary for 1.1.1.146 extracted from

  • Boudon, S.; Heidl, M.; Vuorinen, A.; Wandeler, E.; Campiche, R.; Odermatt, A.; Jackson, E.
    Design, synthesis, and biological evaluation of novel selective peptide inhibitors of 11beta-hydroxysteroid dehydrogenase 1 (2018), Bioorg. Med. Chem., 26, 5128-5139 .
    View publication on PubMed
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
(R)-1-((S)-2-acetamido-3-(2-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-((S)-2-acetamido-3-(4-methoxyphenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-((S)-3-([1,1'-biphenyl]-3-yl)-2-aminopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-(3-acetamidopropanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-(acetyl-L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-(acetylglycyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-(L-tryptophyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-aminoacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-N-(adamantan-2-yl)-1-((S)-2-(2-hydroxyacetamido)-3-(4-methoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(3-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
 Homo sapiens
(R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
-
 Homo sapiens
4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
 Homo sapiens
4-((S)-2-acetamido-3-((R)-2-(adamantan-2-ylcarbamoyl)piperidin-1-yl)-3-oxopropyl)phenyl acetate
-
 Homo sapiens
4-((S)-2-acetamido-3-((R)-2-(azepane-1-carbonyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
 Homo sapiens
4-((S)-2-acetamido-3-((S)-2-(adamantan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
-
 Homo sapiens
4-[3-(4-methoxyphenoxy)-3-methyl-2-oxobutyl]adamantane-1-carboxamide
-
 Homo sapiens
glycyrrhetinic acid
-
 Homo sapiens
additional information not inhibited by (R)-1-(l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-histidyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide trifluoroacetate, (R)-1-(l-lysyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide bis trifluoroacetate, (R)-1-(acetylglycyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-prolyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, (R)-1-(acetyl-l-tyrosyl)-N-(adamantan-1-yl)pyrrolidine-2-carboxamide, and (R)-1-(acetyl-l-prolyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide Homo sapiens
N-acetyl-beta-alanyl-N-adamantan-1-yl-D-prolinamide
-
 Homo sapiens
PF-877423
-
 Homo sapiens
PF-915275
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
cortisone + NADPH + H+ Homo sapiens
-
 cortisol + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisone + NADPH + H+
-
 Homo sapiens cortisol + NADP+
-
 ?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000197
-
 at pH 7.4 and 37°C Homo sapiens (R)-1-((S)-2-acetamido-3-(4-cyanophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
0.000266
-
 at pH 7.4 and 37°C Homo sapiens (R)-1-((S)-2-acetamido-3-(4-fluorophenyl)propanoyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide
0.000373
-
 at pH 7.4 and 37°C Homo sapiens (R)-N-(adamantan-2-yl)-1-((S)-2-amino-3-(4-ethoxyphenyl)propanoyl)pyrrolidine-2-carboxamide
0.000496
-
 at pH 7.4 and 37°C Homo sapiens 4-((S)-2-acetamido-3-((R)-2-((adamantan-2-yl)carbamoyl)pyrrolidin-1-yl)-3-oxopropyl)phenyl acetate
0.000902
-
 at pH 7.4 and 37°C Homo sapiens (R)-1-(L-tyrosyl)-N-(adamantan-2-yl)pyrrolidine-2-carboxamide