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Literature summary for 1.1.1.146 extracted from

  • Ye, X.Y.; Yoon, D.; Chen, S.Y.; Nayeem, A.; Golla, R.; Seethala, R.; Wang, M.; Harper, T.; Sleczka, B.G.; Apedo, A.; Li, Y.X.; He, B.; Kirby, M.; Gordon, D.A.; Robl, J.A.
    Synthesis and structure-activity relationship of 2-adamantylmethyl tetrazoles as potent and selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) (2014), Bioorg. Med. Chem. Lett., 24, 654-660.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
(1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
(1S)-4-([1-[(4-bromophenyl)methyl]-1H-tetrazol-5-yl]methyl)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
-
Homo sapiens
4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
-
Homo sapiens
4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
-
Homo sapiens
5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
-
Homo sapiens
5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
-
Homo sapiens
5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
Homo sapiens
5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
-
Homo sapiens
5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
-
Homo sapiens
6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
-
Homo sapiens
methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
-
Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
pH and temperature not specified in the publication Homo sapiens 5-[[1-([1,1'-biphenyl]-4-yl)-3a-methoxyoctahydro-2,5-methanopentalen-1-yl]methyl]-1H-tetrazole
0.000002
-
pH and temperature not specified in the publication Homo sapiens 4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.0000023
-
pH and temperature not specified in the publication Homo sapiens 4-[(1H-tetrazol-5-yl)methyl]-4-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
0.0000026
-
pH and temperature not specified in the publication Homo sapiens 4-(2'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.0000037
-
pH and temperature not specified in the publication Homo sapiens (1R)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.0000048
-
pH and temperature not specified in the publication Homo sapiens 5-[2-[1-([1,1'-biphenyl]-4-yl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
0.000005
-
pH and temperature not specified in the publication Homo sapiens methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
0.000006
-
pH and temperature not specified in the publication Homo sapiens 4-(3'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000008
-
pH and temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-4-yl)-1-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-3a(1H)-ol
0.000008
-
pH and temperature not specified in the publication Homo sapiens 4-(4'-methoxy[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000008
-
pH and temperature not specified in the publication Homo sapiens 4-[(1H-tetrazol-5-yl)methyl]-4-[3'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]octahydro-2,5-methanopentalen-1-ol
0.00001
-
pH and temperature not specified in the publication Homo sapiens 4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000014
-
pH and temperature not specified in the publication Homo sapiens 4-[4-(pyridin-4-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000015
-
pH and temperature not specified in the publication Homo sapiens (1S)-4-(4'-fluoro[1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.00002
-
pH and temperature not specified in the publication Homo sapiens methyl 4'-[4-hydroxy-1-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-yl][1,1'-biphenyl]-4-sulfinate
0.000026
-
pH and temperature not specified in the publication Homo sapiens 4-(4-phenoxyphenyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000052
-
pH and temperature not specified in the publication Homo sapiens 5-[2-[1-(4-fluorophenyl)octahydro-2,5-methanopentalen-1-yl]ethyl]-1H-tetrazole
0.000085
-
pH and temperature not specified in the publication Homo sapiens 5-[2-(1-phenyloctahydro-2,5-methanopentalen-1-yl)ethyl]-1H-tetrazole
0.000102
-
pH and temperature not specified in the publication Homo sapiens 4-[4-(pyridin-3-yl)phenyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000107
-
pH and temperature not specified in the publication Homo sapiens 4-(phenylethynyl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000152
-
pH and temperature not specified in the publication Homo sapiens 4-([1,1'-biphenyl]-4-yl)-4-[(1H-tetrazol-5-yl)methyl]hexahydro-2,5-methanopentalen-2(1H)-ol
0.00019
-
pH and temperature not specified in the publication Homo sapiens 4-phenyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000282
-
pH and temperature not specified in the publication Homo sapiens 4-[([1,1'-biphenyl]-4-yl)methyl]-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.000449
-
pH and temperature not specified in the publication Homo sapiens 5-(2-[1-[(3-chlorophenyl)methyl]octahydro-2,5-methanopentalen-1-yl]ethyl)-1H-tetrazole
0.00064
-
pH and temperature not specified in the publication Homo sapiens 4-([1,1'-biphenyl]-3-yl)-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol
0.001929
-
pH and temperature not specified in the publication Homo sapiens 6-([1,1'-biphenyl]-4-yl)-6-[(1H-tetrazol-5-yl)methyl]tetrahydro-2,5-methanopentalene-2,3a(1H,3H)-diol
0.00408
-
pH and temperature not specified in the publication Homo sapiens 4-benzyl-4-[(1H-tetrazol-5-yl)methyl]octahydro-2,5-methanopentalen-1-ol