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Literature summary for 1.1.1.146 extracted from

  • Roche, D.; Carniato, D.; Leriche, C.; Lepifre, F.; Christmann-Franck, S.; Graedler, U.; Charon, C.; Bozec, S.; Doare, L.; Schmidlin, F.; Lecomte, M.; Valeur, E.
    Discovery and structure-activity relationships of pentanedioic acid diamides as potent inhibitors of 11beta-hydroxysteroid dehydrogenase type I (2009), Bioorg. Med. Chem. Lett., 19, 2674-2678.
    View publication on PubMed
Search for more literature for 1.1.1.146

Inhibitors

Inhibitors Comment Organism Structure
(1-[2-oxo-2-[(pyridin-3-ylmethyl)amino]ethyl]cyclopentyl)acetic acid 11% inhibition at 0.001 mM Homo sapiens
(1-[2-[(2,4-dichlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 27% inhibition at 0.001 mM Homo sapiens
(1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
-
 Homo sapiens
(1-[2-[(2-chlorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 22% inhibition at 0.001 mM Homo sapiens
(1-[2-[(4-methoxypyridin-3-yl)amino]-2-oxoethyl]cyclopentyl)acetic acid 7% inhibition at 0.001 mM Homo sapiens
(1-[2-[(cyclohexylmethyl)amino]-2-oxoethyl]cyclopentyl)acetic acid 7% inhibition at 0.001 mM Homo sapiens
(1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
-
 Homo sapiens
2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
-
 Homo sapiens
3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
 Homo sapiens
3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
 Homo sapiens
4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
 Homo sapiens
4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
-
 Homo sapiens
N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
 Homo sapiens
N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
-
 Homo sapiens
N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
 Homo sapiens
N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
-
 Homo sapiens
N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
-
 Homo sapiens
[1-[2-(cyclohexylamino)-2-oxoethyl]cyclopentyl]acetic acid 13% inhibition at 0.001 mM Homo sapiens
[1-[2-(octahydroisoquinolin-2(1H)-yl)-2-oxoethyl]cyclopentyl]acetic acid 34% inhibition at 0.001 mM Homo sapiens
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethyl]cyclopentyl]acetic acid 8% inhibition at 0.001 mM Homo sapiens
[1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 3,3-dimethyl-4-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
0.000008
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens N-[(2s,5r)-5-carbamoyltricyclo[3.3.1.13,7]dec-2-yl]-N'-cyclopropyl-3,3-dimethylpentanediamide
0.000008
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens N-cyclopropyl-N'-[(2r,5s)-5-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
0.000009
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-[(2-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000009
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-[(2-methylpropyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000012
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 4-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
0.000016
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-oxo-2-[(pyridin-2-ylmethyl)amino]ethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000017
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-[(4-fluorophenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000018
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-[(4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000019
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[1-[2-(benzylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000048
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-(1-[2-[(4-methoxyphenyl)amino]-2-oxoethyl]cyclopentyl)-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000048
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[1-(2-oxo-2-pyrrolidin-1-ylethyl)cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.000057
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 3,3-dimethyl-4-(3-pyridin-2-yl-1,2,4-oxadiazol-5-yl)-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
0.00006
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.00015
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens N-cyclopropyl-3,3-dimethyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
0.00016
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[1-[2-(4-ethylpiperazin-1-yl)-2-oxoethyl]cyclopentyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.0002
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 4-[3-(4-chlorophenyl)-1,2,4-oxadiazol-5-yl]-3,3-dimethyl-N-tricyclo[3.3.1.13,7]dec-2-ylbutanamide
0.00034
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens 2-[1-[2-(cyclopropylamino)-2-oxoethyl]cyclohexyl]-N-tricyclo[3.3.1.13,7]dec-2-ylacetamide
0.00055
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens N-cyclopropyl-N'-[(2R)-1-hydroxytricyclo[3.3.1.13,7]dec-2-yl]-3,3-dimethylpentanediamide
0.001
-
 IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens N-cyclopropyl-N'-tricyclo[3.3.1.13,7]dec-2-ylpentanediamide
0.001
-
 IC50 above 0.001 mM, in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens (1r,4s)-4-[[5-(cyclopropylamino)-3,3-dimethyl-5-oxopentanoyl]amino]tricyclo[3.3.1.13,7]decane-1-carboxylic acid
0.0012
-
-
 Homo sapiens (1-[2-[(2-chloro-4-fluorobenzyl)amino]-2-oxoethyl]cyclopentyl)acetic acid
0.0018
-
 in 30 mM HEPES buffer, pH 7.4, at 37°C Homo sapiens [1-[2-oxo-2-(tricyclo[3.3.1.13,7]dec-2-ylamino)ethyl]cyclopentyl]acetic acid