| Assay ID | Title | Year | Journal | Article |
|---|
| AID1151430 | Elimination half life in healthy human by 14 day test | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID375569 | Inhibition of 11beta-HSD1 | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID744015 | Oral bioavailability in rat at 0.5 mg/kg | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID1151443 | Drug excretion in healthy human urine | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID1151431 | Clearance in healthy human by 14 day test | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID744016 | Volume of distribution at steady state in rat at 0.1 mg/kg, iv and 0.5 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID744014 | Drug metabolism in human liver microsomes assessed as GSH adduct formation by GSH assay in presence of NADPH | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID375575 | Displacement of [125I]2-iodomelatonin from hamster brain melatonin MT3 receptor by scintillation counting | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID375581 | Inhibition of mouse 11beta-HSD1 | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1151433 | Reduction in 5alpha/5beta-tetrahydrocortisol to tetrahydrocortisone ratio in healthy human at 15 mg qd 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). |
| AID375580 | Bioavailability in rat at 0.1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1151432 | Inhibition of prednisone to prednisolone conversion in healthy human at 15 mg qd 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). |
| AID366738 | Inhibition of cynomolgus monkey 11beta-HSD1 mediated conversion of prednisone to prednisolone | 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. |
| AID1151409 | Reduction in plasma insulin level in cynomolgus monkey at 0.1 to 3 mg/kg | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID744019 | Inhibition of 11beta-HSD2 (unknown origin) at 10 uM | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID375585 | Inhibition of 11beta-HSD1 in dog hepatocytes | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1151429 | Tmax in healthy human by 14 day test | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
| Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). |
| AID375583 | Inhibition of 11beta-HSD1 in human hepatocytes | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID375584 | Inhibition of 11beta-HSD1 in monkey hepatocytes | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID375574 | Inhibition of rat choline transporter | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID744017 | Half life in rat at 0.1 mg/kg, iv and 0.5 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID375577 | Volume of distribution at steady state in rat at 0.1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1516423 | Inhibition of N-terminal MKHQHQHQHQHQHQQPL-tagged 11beta-HSD1 C272S mutant (unknown origin) expressed in Escherichia coli BL21 (DE3) using cortisol as substrate measured for 1 hr in presence of NADPH by fluorescence assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Mechanistic Insight on the Mode of Action of Colletoic Acid. |
| AID375582 | Inhibition of 11beta-HSD1 in rat hepatocytes | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID744008 | Oral bioavailability in rat at 0.5 mg/kg administered as suspension in 0.5 % methylcellulose | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID1516424 | Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Mechanistic Insight on the Mode of Action of Colletoic Acid. |
| AID427218 | Reduction of plasma insulin level in normal cynomolgus monkey at 3 mg/kg after 8 hrs | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model. |
| AID366732 | Inhibition of 11beta-HSD2 at 10 uM | 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. |
| AID744018 | Clearance in rat at 0.1 mg/kg, iv and 0.5 mg/kg, po | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID375573 | Inhibition of human 11beta-HSD2 in HEK293 cells at 10 uM | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID375576 | Plasma clearance in rat at 0.1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID375579 | AUC in rat at 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID427217 | Reduction of plasma insulin level in normal cynomolgus monkey at 1 mg/kg after 8 hrs | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model. |
| AID375578 | Half life in rat at 0.1 mg/kg, iv and 1 mg/kg, po | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1516425 | Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
| Mechanistic Insight on the Mode of Action of Colletoic Acid. |
| AID744020 | Inhibition of 11beta-HSD1 in human HEK293 cells | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites. |
| AID375572 | Inhibition of human 11beta-HSD1 in HEK293 cells | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| AID1151408 | In vivo inhibition of 11beta-HSD1 in cynomolgus monkey assessed as inhibition of prednisone to prednisolone conversion at 0.1 to 3 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). |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1799041 | Measurement of 11beta-HSD1 Activity from Article 10.1016/j.bmcl.2009.05.011: \\N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.\\ | 2009 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 19, Issue:13
| N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |