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Literature summary for 1.1.1.146 extracted from

  • Lepifre, F.; Christmann-Franck, S.; Roche, D.; Leriche, C.; Carniato, D.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
    Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold (2009), Bioorg. Med. Chem. Lett., 19, 3682-3685.
    View publication on PubMed
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
-
 Homo sapiens
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
-
 Homo sapiens
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
-
 Homo sapiens
1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
-
 Homo sapiens
2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
-
 Homo sapiens
6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000005
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[(1-phenylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
0.0000015
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(2-methyl-2-phenylpropanoyl)-2-azaspiro[4.5]decane
0.000003
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[[1-(4-fluorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
0.000006
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2-azaspiro[4.5]decane
0.000022
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-3,4-dihydro-2H-spiro[naphthalene-1,3'-pyrrolidine]
0.000025
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-pyrrolidine]
0.000092
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[(1-pyridin-2-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
0.000094
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]-2,3-dihydrospiro[indene-1,3'-piperidine]
0.000252
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[(1-pyridin-4-ylcyclopropyl)carbonyl]-2-azaspiro[4.5]decane
0.00045
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[(4-chlorophenyl)acetyl]-2-azaspiro[4.5]decane
0.00141
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[(4-fluorophenyl)acetyl]-2-azaspiro[4.5]decane
0.0021
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 1'-[[1-(4-chlorophenyl)cyclopropyl]carbonyl]spiro[indene-1,4'-piperidine]
0.0025
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 6-fluoro-4'-[(1-phenylcyclopropyl)methyl]spiro[chromene-2,1'-cyclohexan]-4(3H)-one