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Literature summary for 1.1.1.146 extracted from

  • Stanetty, C.; Czollner, L.; Koller, I.; Shah, P.; Gaware, R.; Cunha, T.D.; Odermatt, A.; Jordis, U.; Kosma, P.; Classen-Houben, D.
    Synthesis of novel 3-amino and 29-hydroxamic acid derivatives of glycyrrhetinic acid as selective 11beta-hydroxysteroid dehydrogenase 2 inhibitors (2010), Bioorg. Med. Chem., 18, 7522-7541.
    View publication on PubMed
Search for more literature for 1.1.1.146

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
 Homo sapiens
(3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
-
 Homo sapiens
(3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid
-
 Homo sapiens
(3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
-
 Homo sapiens
(3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
-
 Homo sapiens
(3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
-
 Homo sapiens
(3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
-
 Homo sapiens
(3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
-
 Homo sapiens
(3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
-
 Homo sapiens
(3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
-
 Homo sapiens
3,11-dioxoolean-12-en-30-oic acid
-
 Homo sapiens
carbenoxolone
-
 Homo sapiens
glycyrrhetinic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

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-hydroxysteroid dehydrogenase 1
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADP+
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
 1% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-(2-methoxycarbonyl-ethylsulfonylamino)-11-oxo-olean-12-en-29-oic acid
additional information
-
 12% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens carbenoxolone
additional information
-
 15% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-amino-11-oxoolean-12-en-29-oic acid, diphenylmethyl ester
additional information
-
 32% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3alpha,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
additional information
-
 38% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-acetoxy-N-methoxy-11-oxo-olean-12-en-29-amide
additional information
-
 4% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3alpha,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oicacid
additional information
-
 5% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-(2-carboxy-ethylsulfonylamino)-11-oxoolean-12-en-29-oic acid
additional information
-
 58% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-methylsulfonylamino-11-oxo-olean-12-en-29-oic acid
additional information
-
 6% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-11-oxo-3-succinylamino-olean-12-en-29-oic acid
additional information
-
 71% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3,N-dihydroxy-N-methyl-11-oxo-olean-12-en-29-amide
additional information
-
 71% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-N-hydroxy-N-methyl-11-oxo-3-[(trifluoromethylsulfonyl)amino]-olean-12-en-29-amide
additional information
-
 72% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-acetylamino-N-hydroxy-N-methyl-11-oxoolean-12-en-29-amide
additional information
-
 87% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
additional information
-
 9% residual activity at 0,001 mM, pH not specified in the publication, 37°C Homo sapiens (3beta)-3-hydroxy-11-oxoolean-12-en-30-amide
additional information
-
 93% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-N-hydroxy-N-methyl-3-methoxyamino-11-oxo-olean-12-en-29-amide
additional information
-
 99% residual activity at 0,0002 mM, pH not specified in the publication, 37°C Homo sapiens (3alpha,18beta,20beta)-11-oxo-3-trifluoromethylsulfonylaminoolean-12-en-29-oic acid
0.0000427
-
 pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
0.0000619
-
 pH not specified in the publication, 37°C Homo sapiens (3alpha,18beta,20beta)-3-methoxyamino-11-oxo-olean-12-en-29-oic acid
0.000619
-
 pH not specified in the publication, 37°C Homo sapiens 3,11-dioxoolean-12-en-30-oic acid
0.000626
-
 pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-acetoxy-N-hydroxy-11-oxo-olean-12-en-29-amide
0.000778
-
 pH not specified in the publication, 37°C Homo sapiens glycyrrhetinic acid
0.000825
-
 pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-(acetylamino)-11-oxo-olean-12-en-29-oic acid
0.000929
-
 pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-hydroxy-N-methoxy-11-oxo-olean-12-en-29-amide
0.001012
-
 pH not specified in the publication, 37°C Homo sapiens (3beta,18beta,20beta)-3-acetoxy-N-methyl-N-hydroxy-11-oxoolean-12-en-29-amide
0.001157
-
 pH not specified in the publication, 37°C Homo sapiens (3beta)-N,3-dihydroxy-11-oxoolean-12-en-30-amide
0.001508
-
 pH not specified in the publication, 37°C Homo sapiens (3E)-3-(methoxyimino)-11-oxoolean-12-en-30-oic acid
0.007138
-
 pH not specified in the publication, 37°C Homo sapiens (3beta)-3-(acetyloxy)-11-oxoolean-12-en-30-oic acid