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Literature summary for 1.1.1.146 extracted from

  • Gillespie, P.; Pietranico-Cole, S.; Myers, M.; Bilotta, J.A.; Conde-Knape, K.; Fotouhi, N.; Goodnow, R.A.; Guertin, K.R.; Hamilton, M.M.; Haynes, N.E.; Liu, B.; Qi, L.; Ren, Y.; Scott, N.R.; So, S.S.; Spence, C.; Taub, R.; Thakkar, K.; Tilley, J.W.; Zwingelstein, C.
    Discovery of camphor-derived pyrazolones as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 2707-2711.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(4R,7S)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
-
Rattus norvegicus
(4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-2-(2'-methyl[1,1'-biphenyl]-3-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-2-(4-methylphenyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-2-(pyridin-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-2-[2-(trifluoromethyl)phenyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1,7,8,8-tetramethyl-2-[[2-(trifluoromethyl)phenyl]methyl]-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1-benzyl-2-(2,4-difluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1-benzyl-2-(2-fluorophenyl)-7,8,8-trimethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1-benzyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
1-ethyl-7,8,8-trimethyl-2-phenyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2,4-difluorophenyl)-7,8,8-trimethyl-1-(2-phenylethyl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2,5-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2,6-dichlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2-chlorophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(prop-2-en-1-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2-fluorophenyl)-7,8,8-trimethyl-1-(propan-2-yl)-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(2-fluorophenyl)-7,8,8-trimethyl-1-propyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(3-iodophenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-(3-methoxyphenyl)-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
2-benzyl-1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-3H-4,7-methanoindazol-3-one
-
Rattus norvegicus
3-methoxy-7,8,8-trimethyl-2-(4-methylphenyl)-4,5,6,7-tetrahydro-2H-4,7-methanoindazole
-
Rattus norvegicus
ABT-384
-
Rattus norvegicus
AMG-221
-
Rattus norvegicus
AZD-8329
-
Rattus norvegicus
BMS-770767
-
Rattus norvegicus
BVT.2733
-
Rattus norvegicus
PF-915275
-
Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
-
Rattus norvegicus 5783
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
34000
-
x * 34000, SDS-PAGE Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
adipose tissue
-
Rattus norvegicus
-
brain
-
Rattus norvegicus
-
liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

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

Subunits

Subunits Comment Organism
? x * 34000, SDS-PAGE Rattus norvegicus

Synonyms

Synonyms Comment Organism
11beta-hydroxysteroid dehydrogenase type 1
-
Rattus norvegicus
11betaHSD1
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Rattus norvegicus
NADPH
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000116
-
pH and temperature not specified in the publication Rattus norvegicus (4R,7S)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one
0.000138
-
pH and temperature not specified in the publication Rattus norvegicus (4S,7R)-1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methanoindazol-3-one