Assay ID | Title | Year | Journal | Article |
AID1151397 | Inhibition of human 11beta-HSD1 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID1151399 | Reduction in fasting blood glucose level in high fat diet-fed STZ-induced diabetes mouse model at 30 mg/kg bid for 9 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID1151402 | In vivo inhibition of 11beta-HSD1 in mouse assessed as inhibition of [3H]cortisone to [3H]cortisol conversion at 10 mg/kg, po measured after 4 hrs relative to control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID404230 | Inhibition of [3H]cortisone to [3H]cortisol conversion in mouse at 10 mg/kg, po administered as single dose after 4 hrs | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151404 | Reduction in cumulative food intake in diet-induced obese mouse model at 20 mg/kg bid for 11 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID404227 | Inhibition of human 11beta HSD2 | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151406 | Reduction in postprandial blood glucose level in high fat diet-fed STZ-induced diabetes mouse model at 30 mg/kg bid for 9 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID1151401 | In vivo inhibition of 11beta-HSD1 in mouse assessed as inhibition of [3H]cortisone to [3H]cortisol conversion at 10 mg/kg, po measured after 1 hr relative to control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID404225 | Inhibition of human 11beta HSD1 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID404228 | Inhibition of mouse 11beta HSD2 | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151407 | Reduction in aortic total cholesterol accumulation in high fat diet-fed mouse model at 30 mg/kg bid for 9 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID332063 | Inhibition of mouse 11-beta-HSD1 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID332067 | Inhibition of 11-beta-HSD1 in mouse pharmacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 1 hr | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID332068 | Inhibition of 11-beta-HSD1 in mouse pharmacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 4 hrs | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID758682 | Inhibition of human 11beta-HSD1 | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes. |
AID332065 | Inhibition of mouse 11-beta-HSD2 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151395 | Inhibition of human 11beta-HSD2 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID466259 | Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors. |
AID404229 | Inhibition of [3H]cortisone to [3H]cortisol conversion in mouse at 10 mg/kg, po administered as single dose after 1 hr | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID758683 | Inhibition of mouse 11beta-HSD1 | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11β-HSD1 inhibitors: potential impact in diabetes. |
AID404226 | Inhibition of mouse 11beta HSD1 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1873294 | Inhibition of human 11beta-HSD2 | 2022 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 69 | Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach. |
AID332064 | Inhibition of human 11-beta-HSD2 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151400 | Inhibition of mouse 11beta-HSD2 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID366737 | Inhibition of 11beta-HSD2 expressed in CHO-K1 cells assessed as conversion of [3H]cortisol to cortisone by SPA assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
AID366736 | Inhibition of 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to cortisol by SPA assay | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. |
AID1873296 | Inhibition of mouse 11beta-HSD1 | 2022 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 69 | Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach. |
AID1873295 | Inhibition of human 11beta-HSD1 | 2022 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 69 | Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach. |
AID1151403 | Reduction in body weight in diet-induced obese mouse model at 20 mg/kg bid for 11 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID332062 | Inhibition of human 11-beta-HSD1 by SPA assay | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I. |
AID1151405 | Reduction in fasting blood glucose level in diet-induced obese mouse model at 20 mg/kg bid for 11 days relative to vehicle-treated control | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
AID466260 | Displacement of [3H]cortisone from mouse 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5
| Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |