| Assay ID | Title | Year | Journal | Article |
|---|
| AID1501001 | Inhibition of human full-length 11beta-HSD1 expressed in HEK293 cells at 10 uM using cortisone as substrate after 2 hrs by LC-MS analysis relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction. |
| AID1501002 | Inhibition of human full-length 11beta-HSD2 expressed in HEK293 cells at 10 uM using cortisol as substrate after 2 hrs by LC-MS analysis relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction. |
| AID480481 | Inhibition of human 11-beta-HSD1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID1501000 | Inhibition of 11beta-HSD1 in human liver microsomes using [3H]cortisone as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by scintillation proximity assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction. |
| AID480487 | Inhibition of 11-beta-HSD1 in C57BL mouse assessed as reduction of plasma cortisol level at 1 mg/kg, po administered 30 mins before cortisone challenge measured after 60 mins by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID480491 | Inhibition of 11-beta-HSD1 in C57BL mouse assessed as reduction of plasma cortisol level at 100 mg/kg, po administered 30 mins before cortisone challenge measured after 60 mins by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID1151411 | In vivo inhibition of 11beta-HSD1 in mouse assessed as inhibition of cortisone to cortisol conversion at 5 mg/kg 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). |
| AID1151410 | In vivo inhibition of 11beta-HSD1 in mouse assessed as inhibition of cortisone to cortisol conversion at 100 mg/kg 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). |
| AID480486 | Intrinsic clearance in human liver microsomes | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID1501004 | Stability in human liver microsomes at 10 uM after 30 mins by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Design, synthesis and in vivo study of novel pyrrolidine-based 11β-HSD1 inhibitors for age-related cognitive dysfunction. |
| AID480484 | Inhibition of human 11-beta-HSD1 expressed in HEK293 cells co-transfected with GRE-luciferase after 6 hrs by luciferase reporter gene assay | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID480488 | Inhibition of 11-beta-HSD1 in C57BL mouse assessed as reduction of plasma cortisol level at 3 mg/kg, po administered 30 mins before cortisone challenge measured after 60 mins by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID1265864 | Inhibition of 11beta-HSD1 in human liver microsomes assessed as conversion of [3H]-cortisone to [3H]-cortisol at 10 uM after 30 mins by scintillation proximity assay relative to control | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors. |
| AID692679 | Inhibition of 11betaHSD1 expressed in HEK cells | 2012 | ACS medicinal chemistry letters, Oct-11, Volume: 3, Issue:10
| Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors. |
| AID480490 | Inhibition of 11-beta-HSD1 in C57BL mouse assessed as reduction of plasma cortisol level at 30 mg/kg, po administered 30 mins before cortisone challenge measured after 60 mins by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID1265865 | Inhibition of 11beta-HSD1 in human liver microsomes assessed as conversion of [3H]-cortisone to [3H]-cortisol after 30 mins by scintillation proximity assay | 2015 | Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
| Searching for novel applications of the benzohomoadamantane scaffold in medicinal chemistry: Synthesis of novel 11β-HSD1 inhibitors. |
| AID480489 | Inhibition of 11-beta-HSD1 in C57BL mouse assessed as reduction of plasma cortisol level at 10 mg/kg, po administered 30 mins before cortisone challenge measured after 60 mins by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| AID480492 | Inhibition of 11-beta-HSD1 in po dosed C57BL mouse assessed as reduction of plasma cortisol level administered 30 mins before cortisone challenge measured after 60 mins by ELISA | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |