Cloned (Comment) | Organism |
---|---|
- |
Homo sapiens |
- |
Mus musculus |
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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P28845 | - |
- |
Mus musculus | P50172 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
cortisol + NAD+ | - |
Homo sapiens | cortisone + NADH + H+ | - |
? | |
cortisol + NAD+ | - |
Mus musculus | cortisone + NADH + H+ | - |
? |
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 |