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Literature summary for 1.1.1.146 extracted from

  • Venier, O.; Pascal, C.; Braun, A.; Namane, C.; Mougenot, P.; Crespin, O.; Pacquet, F.; Mougenot, C.; Monseau, C.; Onofri, B.; Dadji-Faihun, R.; Leger, C.; Ben-Hassine, M.; Van-Pham, T.; Ragot, J.L.; Philippo, C.; Guessregen, S.; Engel, C.; Farjot, G.; Noah, L.; Maniani, K.; Nicolai, E.
    Pyrrolidine-pyrazole ureas as potent and selective inhibitors of 11beta-hydroxysteroid-dehydrogenase type 1 (2011), Bioorg. Med. Chem. Lett., 21, 2244-2251.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
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Homo sapiens
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Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability Homo sapiens
2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability Mus musculus
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability Homo sapiens
3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone good stability in liver microsomes, excellent potency on both human and mouse enzymes and good estimated intestinal permeability Mus musculus
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile high metabolic lability Homo sapiens
4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile high metabolic lability Mus musculus
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes Homo sapiens
[4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone potent inhibitor with a high permeability value, and low metabolic lability in mouse and human microsomes, significant inhibition of isoform 11beta-HSD1 in both the liver and fat tissue of mice, 2 h after oral administration at 30 mg/kg Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
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Mus musculus P50172
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-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisol + NAD+
-
Homo sapiens cortisone + NADH + H+
-
?
cortisol + NAD+
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Mus musculus cortisone + NADH + H+
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000007
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.000027
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.000037
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
0.000043
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens [4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.000049
-
pH not specified in the publication, temperature not specified in the publication Mus musculus [4-[5-(4-methoxyphenyl)pyrimidin-2-yl]-3,4-dihydroquinoxalin-1(2H)-yl][3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.000055
-
pH not specified in the publication, temperature not specified in the publication Mus musculus 3,4-dihydroquinoxalin-1(2H)-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone
0.000075
-
pH not specified in the publication, temperature not specified in the publication Mus musculus 4-[4-[[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]carbonyl]-3,4-dihydroquinoxalin-1(2H)-yl]benzonitrile
0.00049
-
pH not specified in the publication, temperature not specified in the publication Mus musculus 2,3-dihydro-4H-1,4-benzoxazin-4-yl[3-(1H-pyrazol-4-yl)pyrrolidin-1-yl]methanone