| Assay ID | Title | Year | Journal | Article |
|---|
| AID1721441 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1545293 | Inhibition of human plasma butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 15 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1656477 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate peincubated for 15 mins followed by substrate addition measured at 1 min interval by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3
| Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy. |
| AID1593220 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1721442 | Inhibition of recombinant human BChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1129463 | Neuroprotective activity in mouse HT22 cells assessed as protection against glutamate-induced oxidative damage after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
| Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species. |
| AID1384003 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1166376 | Inhibition of amyloid beta (1-42) self-mediated aggregation (unknown origin) at 10 uM after 24 hrs by thioflavin T fluorescence method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
| Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects. |
| AID1721515 | Drug level in human liver microsomes treated with N-{8-[(6-Chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl}-2-(6-hydroxy-7-methoxy-2-methylchroman-2-yl)acetamide at 5 uM measured up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1763919 | Inhibition of recombinant human nNOS assessed as maximum inhibition relative to control | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID1721455 | Inhibition of self-induced Amyloid beta (1 to 42 residues) (unknown origin) aggregation expressed in Escherichia coli BL21 (DE3) at 10 uM measured after overnight incubation by thioflavin-S based spectrophotometric method relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1129462 | Cytotoxicity against mouse HT22 cells after 24 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
| Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species. |
| AID1593210 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1193213 | Antioxidant activity assessed as Trolox equivalent per microM of compound after 15 mins by oxygen radical absorbance capacity fluorescein assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1256881 | Hepatotoxicity in human HepG2 cells assessed as cell viability after 24 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1183277 | Inhibition of aggregation of tau protein (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as amyloid fibril formation at 10 uM after 24 hrs by thioflavin S fluorescence method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies. |
| AID1256893 | Acute toxicity in im dosed albino Wistar rat assessed as mortality measured within 48 hrs | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1183276 | Inhibition of aggregation of amyloid beta-42 (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as amyloid fibril formation at 10 uM after 24 hrs by thioflavin S fluorescence method | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies. |
| AID243154 | Inhibitory activity against human erythrocyte acetylcholinesterase | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis. |
| AID1904772 | Inhibition of recombinant mouse sEH using CMNPC as substrate preincubated for 5 mins followed by substrate addition and measured every 30 sec for 10 mins for by fluorescence based assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease. |
| AID1487761 | Selectivity index, ratio of IC50 for mouse J774.1 cells to IC50 for Trypanosoma brucei brucei TC221 measured after 48 hrs | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1183275 | Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate by spectrophotometric analysis | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies. |
| AID1831860 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID1129464 | Ratio of EC50 for cytotoxicity against mouse HT22 cells to EC50 for neuroprotective activity in glutamate-induced mouse HT22 cells | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
| Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species. |
| AID1763916 | Selectivity index, ratio of IC50 for human BuchE to IC50 for human Ache | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID1545292 | Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1437793 | Inhibition of amyloid beta 42 (unknown origin) self aggregation at 50 uM by ThT-based fluorometric method relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease. |
| AID1511116 | Inhibition of human recombinant amyloid beta (1 to 42) aggregation expressed in Escherichia coli BL21 (DE3) at 10 uM by Thioflavin S steady state fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1166375 | Selectivity ratio of IC50 for human plasmatic BChE to human recombinant AChE | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
| Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects. |
| AID1193211 | Inhibition of equine serum BChE using acetylthiocholine chloride as substrate after 15 mins by Ellman spectrophotometric method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1511118 | Permeability of the compound measured after compound dilution in PBS/EtOH buffer (70:30) by PAMPA-BBB assay | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1256880 | Inhibition of human recombinant AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1193209 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman spectrophotometric method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1256878 | Selectivity ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1593211 | Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured over 2 mins by UV-Vis spectrophotometric analysis based Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1904773 | Inhibition of recombinant mouse AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 240 sec by Ellman's method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease. |
| AID1545294 | Selectivity index, ratio of IC50 for human plasma butyrylcholinesterase to IC50 for human erythrocyte acetylcholinesterase | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID1166373 | Inhibition of human recombinant AChE after 5 mins by Ellman method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
| Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects. |
| AID31017 | Inhibitory activity against human erythrocyte acetylcholinesterase | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. |
| AID1193212 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1721454 | Inhibition human BACE1 expressed in baculovirus expression system at 5 uM using Panvera peptide as substrate measured after 60 mins by fluorescence assay relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1593213 | Inhibition of HFIP pretreated amyloid beta (1-42) (unknown origin) self aggregation at 50 uM incubated for 24 hrs by thioflavin T based fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1721453 | Inhibition human BACE1 expressed in baculovirus expression system using Panvera peptide as substrate measured after 60 mins by fluorescence assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1721447 | Potency index, ratio of 6-chlorotacrine IC50 to test compound IC50 for recombinant human BChE | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1193214 | Inhibition of self-induced Abeta(1 to 42) (unknown origin) aggregation at 25 uM after 24 hrs by Thioflavin T-based fluorometric assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1511113 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by spectrophotometry analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID654174 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins prior substrate addition measured after 5 mins by spectrophotometry | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases. |
| AID1487758 | Antitrypanosomal activity against Trypanosoma brucei brucei TC221 after 72 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1721516 | Drug level in mouse liver microsomes treated with N-{8-[(6-Chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl}-2-(6-hydroxy-7-methoxy-2-methylchroman-2-yl)acetamide at 5 uM measured up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1763914 | Inhibition of recombinant human AChE using acetylthiocholine as substrate by DTNB-reagent based Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID31767 | Experimental pIC50 values for the inhibition of acetylcholinesterase | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. |
| AID1721457 | Permeability of compound in PBS/EtOH buffer (7:3) PAMPA-BBB assay | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID482894 | Inhibition of AChE | 2010 | European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
| Prediction of acetylcholinesterase inhibitors and characterization of correlative molecular descriptors by machine learning methods. |
| AID1593219 | Cytotoxicity against CHOK1 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1129472 | Antioxidant activity assessed as trolox equivalent of ABTS radical scavenging activity | 2014 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
| Functionalized acridin-9-yl phenylamines protected neuronal HT22 cells from glutamate-induced cell death by reducing intracellular levels of free radical species. |
| AID1763917 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID1721456 | Inhibition of tau aggregation (unknown origin) expressed in Escherichia coli BL21 (DE3) at 10 uM measured after overnight incubation by thioflavin-S based spectrophotometric method relative to control | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1511117 | Inhibition of tau aggregation (unknown origin) expressed in Escherichia coli BL21 (DE3) at 10 uM by Thioflavin S steady state fluorescence assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1721452 | Antioxidant activity assessed as DPPH radical scavenging activity incubated for 1 hr under dark condition | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1256875 | Antioxidant activity assessed as DPPH radical scavenging activity after 30 mins by microplate reader analysis | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1763918 | Inhibition of recombinant human nNOS | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID1511112 | Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by spectrophotometry analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1384011 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1487760 | Cytotoxicity against mouse J774.1 cells after 24 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1193210 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman spectrophotometric method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID214657 | The competitive inhibitory activity against trypanothione reductase was evaluated from Lineweaver Burk plots | 1999 | Journal of medicinal chemistry, Dec-30, Volume: 42, Issue:26
| Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationships. |
| AID243159 | In vitro inhibitory activity against human erythrocyte acetylcholinesterase | 2004 | Journal of medicinal chemistry, Aug-26, Volume: 47, Issue:18
| Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis. |
| AID1904769 | Inhibition of recombinant human sEH using CMNPC as substrate preincubated for 5 mins followed by substrate addition and measured every 30 sec for 10 mins for by fluorescence based assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease. |
| AID1593212 | Selectivity index, ratio of IC50 for recombinant human BChE to IC50 for recombinant human AChE | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1256879 | Inhibition of human plasmatic BChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured every 2 mins by Ellman's method | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity. |
| AID1763915 | Inhibition of recombinant human BuChE using butyrylthiocholine as substrate by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 43 | Huprine Y - Tryptophan heterodimers with potential implication to Alzheimer's disease treatment. |
| AID1166374 | Inhibition of human plasmatic BChE after 5 mins by Ellman method | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
| Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects. |
| AID1511114 | Antagonist activity at NMDA receptor in rat CGN cells assessed as increase in intracellular calcium level incubated for 30 mins in presence of Fura-2AM followed by NMDA/glycine stimulation by fluorescence spectrometer analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1904771 | Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 240 sec by Ellman's method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease. |
| AID1384004 | Inhibition of human plasmatic BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 2 mins time interval by Ellman's method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1511121 | Inhibition of human recombinant BACE-1 expressed in baculovirus expression system at 5 uM using panvera peptide as substrate measured after 1 hr by FRET assay relative to control | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | A novel class of multitarget anti-Alzheimer benzohomoadamantane‒chlorotacrine hybrids modulating cholinesterases and glutamate NMDA receptors. |
| AID1384006 | Antagonist activity at human M1 mAChR expressed in CHO cells assessed as inhibition of oxotremorine M-stimulated calcium influx preincubated for 10 mins followed by oxotremorine M addition by Fluo-4 NW dye based fluorescence assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1593215 | Effective permeability of the compound in PBS buffer at pH 7.4 at 100 uM after 3 to 6 hrs by PAMPA | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Novel tacrine-tryptophan hybrids: Multi-target directed ligands as potential treatment for Alzheimer's disease. |
| AID1384005 | Selectivity ratio of IC50 for human plasmatic BuChE to IC50 for human erythrocyte AChE | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | The concept of hybrid molecules of tacrine and benzyl quinolone carboxylic acid (BQCA) as multifunctional agents for Alzheimer's disease. |
| AID1183274 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate by spectrophotometric analysis | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targeting β-amyloid, tau, and cholinesterase pathologies. |
| AID1904770 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 240 sec by Ellman's method | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
| Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease. |
| AID1487759 | Antitrypanosomal activity against Trypanosoma brucei brucei TC221 after 48 hrs by alamar blue assay | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1831859 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
| Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID1721517 | Drug level in rat liver microsomes treated with N-{8-[(6-Chloro-1,2,3,4-tetrahydroacridin-9-yl)amino]octyl}-2-(6-hydroxy-7-methoxy-2-methylchroman-2-yl)acetamide at 5 uM measured up to 60 mins by UPLC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
| Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6. |
| AID1799184 | AChE Inhibition Assay from Article 10.1021/jm900859q: \\Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds.\\ | 2009 | Journal of medicinal chemistry, Sep-10, Volume: 52, Issue:17
| Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. |
| AID1796272 | AChE Inhibition Assay from Article 10.1021/jm990971t: \\SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues.\\ | 2000 | Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
| SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analogues. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |