| Assay ID | Title | Year | Journal | Article |
|---|
| AID1173449 | Effective permeability of the compound by PAMPA assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID1161578 | Permeability of the compound by PAMPA-BBB assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID243153 | In vitro inhibitory activity against bovine 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. |
| AID30682 | Compound was evaluated for the inhibition of acetylcholinesterase of bovine erythrocytes | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID30680 | Compound was evaluated for the inhibition of acetylcholinesterase activity from bovine erythrocytes after 0 minutes of incubation | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID231472 | Ratio between IC50 of bovine AChE and human AChE | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1161575 | Antioxidant activity assessed as total polyphenolics measured as gallic acid equivalent after 30 mins by Folin-Ciocalteu assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID1545296 | Antagonist activity at Acetylcholinesterase in Sprague-Dawley rat phrenic nerve-hemidiaphragm assessed as reversal of d-tubocurarine induced neuromuscular blockade after 15 mins | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
| Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID231475 | Ratio between IC50 of human BChE and human AChE | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1173446 | Cytotoxicity against rat L6 cells after 6 days by resazurin assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID1161577 | Inhibition of aggregation of TAU (unknown origin) expressed in Escherichia coli BL21 (DE3) at 10 uM after 24 hrs by thioflavin S fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID44455 | Inhibition of butyrylcholinesterase (BChE) in human serum | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1707538 | Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins under dark condition by UV-Vis spectrophotometric analysis | | | |
| AID30681 | Compound was evaluated for the inhibition of acetylcholinesterase activity from bovine erythrocytes after 30 minutes of incubation | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1161573 | Antioxidant activity assessed as ABTS free radical scavenging activity measured as trolox equivalent after 1 hr by spectrophotometry | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID31024 | Inhibition of acetylcholinesterase isolated from Human erythrocytes. | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1784491 | Inhibition of human recombinant AChE using acetylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1784492 | Inhibition of human serum BChE using butyrylthiocholine iodide as a substrate preincubated for 20 mins followed by substrate addition by spectrophotometric analysis | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1784499 | Inhibition of tau aggregation (unknown origin) in Escherichia coli BL21 (DE3) at 10 uM incubated overnight by thioflavin S based fluorescence analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1237960 | Inhibition of beta-haematin formation by microplate reader analysis relative to hemin | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity. |
| AID31794 | Ex Vivo evaluation of the Compound for the percentage of inhibition of brain acetylcholinesterase activity of drug-treated mice vs untreated controls (10 uM/Kg was used) | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| 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. |
| AID1161571 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins before substrate addition by Ellman method | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID1707536 | Selectivity index, ratio of IC50 for human serum BChE using butyrylthiocholineiodide as substrate to IC50 for recombinant human AChE using acetylthiocholine iodide as substrate | | | |
| AID1545298 | Inhibition of human Acetylcholinesterase using acetylthiocholine as substrate incubated for 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). |
| AID1173447 | Selectivity index, ratio of IC50 for rat L6 cells to IC50 for bloodstream forms of Trypanosoma brucei 221 | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID1784498 | Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation in Escherichia coli BL21 (DE3) at 10 uM incubated overnight by thioflavin S based fluorescence analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1545300 | Inhibition of human serum butyrylcholinesterase using butyrylthiocholine iodide as substrate incubated for 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). |
| AID437318 | Inhibition of human recombinant AChE in erythrocytes by Ellman's assay | 2009 | Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
| Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors. |
| AID227157 | Compound was evaluated for the antagonism index | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1784513 | Acute toxicity in zebra fish embryos assessed as lethality measured every 24 hrs for 72 hrs | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1161572 | Inhibition of human serum BChE using butyrylthiocholine iodide preincubated for 20 mins before substrate addition by Ellman method | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID1173445 | Trypanocidal activity against bloodstream forms of Trypanosoma brucei 221 assessed as growth inhibition after 48 hrs by resazurin assay | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID1707539 | Permeability of the compound in PBS/EtOH buffer (70:30) by PAMPA-BBB assay | | | |
| AID1161574 | Antioxidant activity assessed as DPPH free radical scavenging activity measured as trolox equivalent after 30 mins by spectrophotometry | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID1784512 | Acute toxicity in zebra fish embryos assessed as lowest observed adverse effect concentration measured every 24 hrs for 72 hrs | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1237959 | Inhibition of Trypanosoma brucei recombinant Trypanothione reductase assessed as decrease in (T[SH]2) formation using trypanothione disulfide as substrate after 15 mins by colorimetric analysis | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity. |
| AID1237961 | Selectivity index, ratio of IC50 for inhibition of Trypanosoma brucei recombinant Trypanothione reductase to IC50 for trypanocidal activity against bloodstream form of Trypanosoma brucei 221 | 2015 | Bioorganic & medicinal chemistry, Aug-15, Volume: 23, Issue:16
| Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity. |
| AID1161576 | Inhibition of aggregation of amyloid beta (1 to 42) (unknown origin) expressed in Escherichia coli BL21 (DE3) at 10 uM after 24 hrs by thioflavin S fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
| Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents with β-amyloid and tau anti-aggregating properties. |
| AID1707535 | Inhibition of human serum BChE using butyrylthiocholineiodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | | | |
| AID227404 | Compound was evaluated for the antagonism index at 1 uM | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24
| New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease. |
| AID1545299 | Inhibition of bovine erythrocyte acetylcholinesterase using acetylthiocholine as substrate incubated for 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). |
| AID1784531 | Inhibition of human recombinant BACE-1 expressed in Escherichia coli at 5 uM using panvera peptide as a substrate incubated for 1 hr by fluorescence analysis relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects. |
| AID1707534 | Inhibition of recombinant human AChE using acetylthiocholineiodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | | | |
| AID1173450 | Antiplamodial activity against chloroquine-resistant bloodstream forms of Plasmodium falciparum K1 infected in human A+ erythrocytes assessed as growth inhibition after 48 hrs by spectrophotometry | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID1707583 | Inhibition of recombinant human BACE-1 at 5 uM using methoxycoumarin-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-Lys-dinitrophenyl as substrate preincubated for 1 hr followed by substrate addition and measured after 15 mins by fluorescence based assay relative to | | | |
| AID1173448 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman method | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
| Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines. |
| AID272365 | Inhibition of bovine erythrocyte AChE | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole. |
| AID1796478 | Enzyme Inhibition Assay from Article 10.1021/jm0496741: \\Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors.\\ | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |