| Assay ID | Title | Year | Journal | Article |
|---|
| AID708080 | Modulation of gamma-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in amyloid beta 42 level after overnight incubation by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID1578456 | Fraction unbound in Wistar Han rat plasma at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID627897 | Inhibition of gamma secretase in rat primary neurons assessed as reduction in amyloid beta-42 secretion | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| Aminothiazoles as γ-secretase modulators. |
| AID647494 | Antialzheimer activity in rat assessed as reduction in amyloid beta42 level in CSF at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID647491 | Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta42 production after 5 hrs by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID647492 | Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta level after 5 hrs by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID1503799 | Modulation of gamma-secretase (unknown origin) assessed as ratio of total amyloid beta to amyloid beta 42 level | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators. |
| AID715389 | Modulation of gamma-secretase assessed as reduction in amyloid beta 40 level by cell based assay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Optimization of a natural product-based class of γ-secretase modulators. |
| AID551699 | Selectivity ratio of IC50 for gamma secretase-mediated total amyloid beta production to IC50 for gamma secretase-mediated amyloid beta42 production in HEK293 cells | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators. |
| AID1578472 | Unbound tissue partition coefficient, ratio of drug level in skeletal muscle to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID551700 | Antialzheimer activity in CD rat assessed as decrease in amyloid beta42 level in CSF at 30 mg/kg, po after 3 hrs | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators. |
| AID1242095 | Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 42 production after 16 hrs by sandwich ELISA | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Potent benzoazepinone γ-secretase modulators with improved bioavailability. |
| AID1383010 | Inhibition of gamma-secretase (unknown origin) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead. |
| AID1578459 | Fraction unbound in Wistar Han rat heart at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1578471 | Unbound tissue partition coefficient, ratio of drug level in liver to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID647504 | Inhibition of human ERG by cell based voltage clamp assay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID708073 | Antialzheimer activity in CD1 mouse assessed as reduction in amyloid beta 42 level in brain at 30 mg/kg, po at 4 hrs by ELISA relative to control | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID647512 | Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as inhibition of amyloid beta40 production after 5 hrs by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID1578462 | Total plasma concentration in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1578466 | Drug concentration in total liver in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID656709 | Intrinsic clearance in human liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators. |
| AID1054419 | Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw assessed as inhibition of amyloid beta-42 production after 16 to 18 hrs by HTRF assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23
| Discovery of 2-methylpyridine-based biaryl amides as γ-secretase modulators for the treatment of Alzheimer's disease. |
| AID647515 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID504053 | AUC (0 to 6 hrs) in po dosed rat | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
| Iminoheterocycles as gamma-secretase modulators. |
| AID1578465 | Drug concentration in total heart in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID551701 | Antialzheimer activity in CD rat assessed as decrease in amyloid beta42 level in brain at 30 mg/kg, po after 3 hrs | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators. |
| AID1678955 | Modulation of gamma secretase in Wistar rat fetal brain-derived neuronal cell incubated for 3 days by ELISA | 2020 | RSC medicinal chemistry, Sep-01, Volume: 11, Issue:9
| Recent developments of small molecule γ-secretase modulators for Alzheimer's disease. |
| AID1578461 | Fraction unbound in Wistar Han rat skeletal muscle at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID551698 | Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay | 2011 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
| Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators. |
| AID1578463 | Drug concentration in total white adipose tissue in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID708066 | Inhibition of notch processing up to 10 uM | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID647495 | Antialzheimer activity in rat assessed as reduction in amyloid beta42 level in cortex at 30 mg/kg, po | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID708071 | Reduction in total amyloid beta level in CD1 mouse at 30 mg/kg, po at 4 hrs by ELISA relative to control | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID1578464 | Drug concentration in total brain in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID647514 | Permeability from apical to basolateral side of human Caco2 cells | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID656707 | Inhibition of gamma secretase expressed in CHO cells expressing APP assessed as amyloid beta42 production | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators. |
| AID715390 | Modulation of gamma-secretase assessed as increase in amyloid beta 38 level at 800 nM by cell based assay relative to control | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Optimization of a natural product-based class of γ-secretase modulators. |
| AID1578469 | Unbound tissue partition coefficient, ratio of drug level in brain to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID504052 | Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
| Iminoheterocycles as gamma-secretase modulators. |
| AID1578470 | Unbound tissue partition coefficient, ratio of drug level in adipose to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1242096 | Modulation of gamma-secretase in HEK293 cells expressing Swedish mutant APP assessed as inhibition of intracellular amyloid beta 40 production after 16 hrs by sandwich ELISA | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Potent benzoazepinone γ-secretase modulators with improved bioavailability. |
| AID1369083 | Inhibition of CYP3A4 in human liver microsomes assessed as residual activity at 5 uM using midazolam as substrate preincubated for 30 mins followed by substrate addition measured after 20 mins in presence of NADPH by LC-MS/MS analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Discovery of novel scaffolds for γ-secretase modulators without an arylimidazole moiety. |
| AID504054 | Selectivity ratio of drug level in brain to plasma in po dosed rat | 2010 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 20, Issue:18
| Iminoheterocycles as gamma-secretase modulators. |
| AID656708 | Efflux ratio of permeability in MDCK cells over expressing human MDR1 | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Design and synthesis of dihydrobenzofuran amides as orally bioavailable, centrally active γ-secretase modulators. |
| AID647652 | Cardiotoxicity in dog assessed as effect on electrocardiographic QTc interval at compound concentration required for pharmacological effect | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID1578468 | Unbound tissue partition coefficient, ratio of drug level in heart to plasma in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1442050 | Modulation of gamma-secretase (unknown origin) | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6
| Design, Synthesis, and Evaluation of a Novel Series of Oxadiazine Gamma Secretase Modulators for Familial Alzheimer's Disease. |
| AID715387 | Modulation of gamma-secretase assessed as reduction in amyloid beta 42 level by cell based assay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Optimization of a natural product-based class of γ-secretase modulators. |
| AID1578457 | Fraction unbound in Wistar Han rat white adipose tissue at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1669507 | Modulation of gamma secretase in HEK293 cells transfected with human APP with Swedish and London familial AD mutation assessed as reduction in Abeta42 levels incubated for 5 hrs by sandwich immuno-assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Generation of Leads for γ-Secretase Modulation. |
| AID1578458 | Fraction unbound in Wistar Han rat brain at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1578474 | Apparent permeability of the compound across dog RRCK cells by MDCK-LE assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1578460 | Fraction unbound in Wistar Han rat liver at 2 uM incubated for 6 hrs by equilibrium dialysis method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID1578467 | Drug concentration in total skeletal muscle in Wistar Han rat at 1 to 2 mg/kg, iv infused for 10 to 20 hrs by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Structural attributes influencing unbound tissue distribution. |
| AID708078 | Inhibition of beta-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in total amyloid beta level up to 10 uM after overnight incubation by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID1369082 | Inhibition of CYP3A4 in human liver microsomes assessed as residual activity at 5 uM using midazolam as substrate after 20 mins in presence of NADPH by LC-MS/MS analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 01-15, Volume: 26, Issue:2
| Discovery of novel scaffolds for γ-secretase modulators without an arylimidazole moiety. |
| AID647493 | Modulation of gamma-secretase-mediated cleavage of human APP Swedish and London mutation expressed in HEK293 cells assessed as reduction of total amyloid beta/amyloid beta42 ratio after 5 hrs by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Jan-12, Volume: 55, Issue:1
| Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo. |
| AID708079 | Inhibition of gamma-secretase in human SK-N-BE(2) cells expressing wild type APP 695 assessed as reduction in total amyloid beta level up to 10 uM after overnight incubation by sandwich immunoassay | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21
| Design and synthesis of a novel series of bicyclic heterocycles as potent γ-secretase modulators. |
| AID1503798 | Modulation of gamma-secretase (unknown origin) assessed as reduction in amyloid beta 42 level | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Discovery of a Tetrahydrobenzisoxazole Series of γ-Secretase Modulators. |
| AID1631517 | Modulation of human gamma-secretase assessed as inhibition of amyloid beta (1 to 42 residues) production by ELISA | 2016 | Journal of medicinal chemistry, Aug-25, Volume: 59, Issue:16
| Gamma Secretase Modulators: New Alzheimer's Drugs on the Horizon? |
| 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. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |