| Assay ID | Title | Year | Journal | Article |
|---|
| AID1796280 | Enzyme Inhibition Assay from Article 10.1021/jm010308g: \\Homodimeric tacrine congeners as acetylcholinesterase inhibitors.\\ | 2002 | Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
| Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
| AID1796323 | Enzyme Inhibition Assay from Article 10.1021/jm990224w: \\Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.\\ | 1999 | Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
| Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions. |
| AID1796464 | Measurement of FBSAChE/EqBuChE Inhibitory Activity from Article 10.1016/s0960-894x(01)00294-3: \\Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase.\\ | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. |
| AID1796269 | Measurement of FBSAChE/EqBuChE Inhibitory Activity from Article 10.1021/jm049510k: \\Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design o | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID733746 | Ratio of IC50 for BuChE in human plasma to IC50 for AChE in Wistar rat brain cortex | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors. |
| AID44129 | Inhibition of equine (Eq) Butyrylcholinesterase | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. |
| 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. |
| AID1487783 | Inhibition of Leishmania infantum trypanothione reductase | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID240985 | Inhibitory concentration against human acetylcholinesterase | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties. |
| AID743645 | Selectivity ratio of BuChE (unknown origin) to AChE (unknown origin) | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors. |
| AID1487767 | Inhibition of Trypanosoma cruzi trypanothione reductase at 5 uM using 100 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID404431 | Inhibition of fetal bovine serum AChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID1306828 | Cytotoxicity against mouse J774.1 cells after 24 hrs by AlamarBlue based cytotoxicity assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Bistacrine derivatives as new potent antimalarials. |
| AID30826 | Inhibition of fetal Bovine serum AChE | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. |
| 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. |
| AID743646 | Inhibition of AChE (unknown origin) | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors. |
| AID1593222 | Inhibition of nNOS in Wistar rat cortical homogenates incubated for 30 mins | 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. |
| AID484173 | Inhibition of electric eel AChE | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. |
| AID1378413 | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation at 50 uM relative to control | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | New tacrine dimers with antioxidant linkers as dual drugs: Anti-Alzheimer's and antiproliferative agents. |
| AID427195 | Inhibition of human recombinant BACE1 by fluorimetric assay | 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. |
| AID271343 | Partition coefficient, log P of the compound | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation. |
| AID1487763 | Inhibition of Trypanosoma brucei rhodesiense rhodesain at 20 uM using Cbz-Phe-Arg-AMC as substrate measured for 5 mins by spectrofluorometric analysis relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1378374 | Inhibition of human AChE | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | New tacrine dimers with antioxidant linkers as dual drugs: Anti-Alzheimer's and antiproliferative agents. |
| 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. |
| AID1058688 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity. |
| AID592640 | Inhibition of human AChE incubated with compounf for 5 mins before addition of substrate acetylthiocholine iodide by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
| Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors. |
| AID1411526 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID1058687 | Inhibition of equine serum BuChE using butylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity. |
| AID613944 | Inhibition of human serum recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers. |
| 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. |
| AID1564190 | Inhibition of human serum BuChe using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by susbtrate addition and measured for 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors. |
| AID484175 | Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. |
| AID1564174 | Selectivity index, ratio of IC50 for human recombinant AChE expressed in HEK293 cells to IC50 for human serum BuChE | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors. |
| AID1472411 | Competitive inhibition of recombinant human BChE assessed as dissociation rate constant using butyrylthiocholine iodide as substrate at pH 8 by stopped flow assay | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID1487784 | Antileishmanial activity against Leishmania infantum | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1306829 | Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as parasite viability after 72 hrs by malstat assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Bistacrine derivatives as new potent antimalarials. |
| AID733748 | Inhibition of AChE in Wistar rat brain cortex using acetylthiocholine iodide as substrate by Ellman's colorimetric method | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors. |
| AID654195 | Inhibition of human BACE-1 | 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. |
| AID30699 | Inhibition of acetylcholinesterase (AChE) of fetal bovine serum (FBS) | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. |
| AID271270 | Inhibition of rat serum BuChE | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge. |
| AID1472410 | Competitive inhibition of recombinant human BChE assessed as association rate constant using butyrylthiocholine iodide as substrate at pH 8 by stopped flow assay | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID613945 | Inhibition of human serum recombinant BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers. |
| AID404432 | Inhibition of horse BuChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID1422763 | Inhibition of AChE in Swiss Webster mouse cerebral homogenate using acetylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Design, synthesis, cholinesterase inhibition and molecular modelling study of novel tacrine hybrids with carbohydrate derivatives. |
| AID44133 | Inhibition of Equine Butyrylcholinesterase | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors. |
| AID1411532 | Octanol/water partition co-efficient, log P of the compound by RP-HPLC analysis | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID613950 | Inhibition of BACE1 expressed in baculovirus assessed as inhibition of amyloid beta-42 production after 60 mins by spectrofluorometric assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers. |
| AID404433 | Ratio of Ki for fetal bovine serum AChE to Ki for horse BuChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID1306830 | Selectivity index, ratio of IC50 for mouse J774.1 cells to IC50 for chloroquine-sensitive ring-stage Plasmodium falciparum 3D7 | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Bistacrine derivatives as new potent antimalarials. |
| AID44424 | Apparent selectivity for (AChE) measured as the ratio of IC50 Butyrylcholinesterase (BChE) / IC50 Acetylcholinesterase (AChE) | 2002 | Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
| Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
| AID733747 | Inhibition of BuChE in human plasma using butyrylthiocholine iodide as substrate by Ellman's colorimetric method | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | Synthesis of tacrine-lophine hybrids via one-pot four component reaction and biological evaluation as acetyl- and butyrylcholinesterase inhibitors. |
| AID304407 | Inhibition of human AChE-induced amyloid-beta (1-40) aggregation at 100 uM by thioflavin T fluorescene method | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease. |
| AID1318844 | Inhibition of Wistar rat brain AChE using acetylthiochloline iodide as substrate after 30 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach. |
| AID304408 | Inhibition of human AChE-induced amyloid-beta (1-40) aggregation by thioflavin T fluorescene method | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease. |
| AID235168 | Selectivity ratio for inhibitory potency of Acetylcholinesterase (AChE) and serum BChE | 1999 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 9, Issue:16
| Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors. |
| AID31961 | Concentration that causes 50% inhibition of Acetylcholinesterase (AChE) using rat cortex homogenate and ethopropazine | 2002 | Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
| Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
| AID1306827 | Antimalarial activity against chloroquine-sensitive ring-stage Plasmodium falciparum 3D7 assessed as parasite viability after 72 hrs by malstat assay | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Bistacrine derivatives as new potent antimalarials. |
| AID44283 | Concentration that causes 50% inhibition of Butyrylcholinesterase (BChE) using human serum and BW284c51 | 2002 | Journal of medicinal chemistry, May-23, Volume: 45, Issue:11
| Homodimeric tacrine congeners as acetylcholinesterase inhibitors. |
| AID304406 | Inhibition of human serum recombinant BChE by Ellman's method | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease. |
| AID1487764 | Inhibition of Trypanosoma brucei rhodesiense rhodesain using Cbz-Phe-Arg-AMC as substrate measured for 10 mins by spectrofluorometric analysis | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID407787 | Inhibition of rat BuChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID1593218 | Inhibition of human AChE-induced amyloid beta aggregation (1-40) (unknown origin) aggregation at 100 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. |
| AID271269 | Inhibition of rat brain AChE | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge. |
| AID1487777 | Inhibition of Trypanosoma brucei trypanothione reductase at 5 uM using 100 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1422764 | Inhibition of BuChE in Swiss Webster mouse whole blood serum using butyrylthiocholine iodide as substrate preincubated for 10 mins followed substrate addition measured after 10 mins by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Design, synthesis, cholinesterase inhibition and molecular modelling study of novel tacrine hybrids with carbohydrate derivatives. |
| AID1487770 | Inhibition of Trypanosoma cruzi trypanothione reductase at 2 uM using 40 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1564175 | Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation at 50 uM incubated for 48 hrs by thioflavin-T fluorescence method relative to control | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors. |
| AID1470887 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 8 mins in presence of BuChE inhibitor ethopropazine by Ellman's method | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Recent progress in the identification of selective butyrylcholinesterase inhibitors for Alzheimer's disease. |
| AID1879289 | Inhibition of AChE in rat brain cortex using acetylthiocholine iodide as substrate incubated for 8 mins by Ellman's method | 2022 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 61 | Design, synthesis, biological evaluation and molecular modeling of N-isobutyl-N-((2-(p-tolyloxymethyl)thiazol-4yl)methyl)benzo[d][1,3] dioxole-5-carboxamides as selective butyrylcholinesterase inhibitors. |
| AID1411531 | Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID1545273 | Inhibition of rat brain Acetylcholinesterase using acetylthiocholine as substrate in presence of BChE inhibitor ethopropazine by spectrophotometric 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). |
| AID44443 | Inhibitory potency against rat serum Butyrylcholinesterase with BW284c51 as AChE inhibitor | 1999 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 9, Issue:16
| Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors. |
| AID44438 | Compound was evaluated for its inhibitory activity against rat serum Butyrylcholinesterase | 2001 | Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
| Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. |
| AID1318846 | Selectivity ratio of IC50 for human plasma BuChE to IC50 for Wistar rat brain AChE | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach. |
| AID1472409 | Competitive inhibition of recombinant human BChE using butyrylthiocholine iodide as substrate at pH 8 by stopped flow assay | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity. |
| AID1306831 | Selectivity index, ratio of IC50 for mouse J774.1 cells to IC50 for ring-stage Plasmodium falciparum Dd2 | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16
| Bistacrine derivatives as new potent antimalarials. |
| AID1059719 | Inhibition of amyloid beta (1 to 42) aggregation (unknown origin) at 5 uM by ThT-based fluorescence assay | 2013 | ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
| Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation. |
| AID1487769 | Inhibition of Trypanosoma cruzi trypanothione reductase at 2 uM using 100 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID592642 | Selectivity index, ratio of IC50 for human AChE to IC50 for equine BChE | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
| Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors. |
| AID1422765 | Selectivity ratio of IC50 for BuChE in Swiss Webster mouse whole blood serum to IC50 for AChE in Swiss Webster mouse cerebral homogenate | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Design, synthesis, cholinesterase inhibition and molecular modelling study of novel tacrine hybrids with carbohydrate derivatives. |
| AID1411527 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID238665 | Dissociation constant for inhibition of fetal bovine serum Acetylcholinesterase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID1487778 | Inhibition of Trypanosoma brucei trypanothione reductase at 5 uM using 40 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID407786 | Inhibition of rat AChE | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. |
| AID592641 | Inhibition of equine BChE incubated with compounf for 5 mins before addition of substrate S-butyrylthiocholine iodide by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
| Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and Aβ-aggregation inhibitors. |
| AID310880 | Inhibition of AchE relative to tacrine | 2007 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
| Quantitative structure-activity relationship (QSAR) of tacrine derivatives against acetylcholinesterase (AChE) activity using variable selections. |
| AID613946 | Selectivity ratio of IC50 for human serum recombinant BuChE to IC50 for human serum recombinant AChE | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers. |
| AID1411529 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID1564197 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by susbtrate addition and measured for 5 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181 | Tacrine-O-protected phenolics heterodimers as multitarget-directed ligands against Alzheimer's disease: Selective subnanomolar BuChE inhibitors. |
| AID1318845 | Inhibition of human plasma BuChE using S-butyrylthiocholine iodide as substrate after 30 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach. |
| AID1500936 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation by thioflavin T-based fluorometric assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease. |
| AID1487768 | Inhibition of Trypanosoma cruzi trypanothione reductase at 5 uM using 40 uM trypanothione disulfide as substrate by spectrophotometric method relative to control | 2017 | Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16
| Bistacrines as potential antitrypanosomal agents. |
| AID1545274 | Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine as substrate in presence of AChE inhibitor BW284C51 by spectrophotometric 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). |
| AID271271 | Selectivity for AChE over BuChE | 2006 | Journal of medicinal chemistry, Sep-07, Volume: 49, Issue:18
| Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge. |
| AID613948 | Inhibition of human recombinant AChE-induced amyloid beta (1-40) aggregation assessed as inhibition of fibril formation at 100 uM by thioflavin T-based fluorescence method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers. |
| AID1058686 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2013 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
| Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity. |
| AID32102 | Inhibitory potency against acetylcholinesterase (AChE) of rat cortex homogenate with ethopropazine as BChE inhibitor | 1999 | Bioorganic & medicinal chemistry letters, Aug-16, Volume: 9, Issue:16
| Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors. |
| AID243067 | Inhibitory ratio for bovine acetylcholinesterase and equine butyrylcholinesterase | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID271341 | Antitubercular activity against Mycobacterium tuberculosis H37Ra | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation. |
| AID238704 | Dissociation constant for inhibition of equine Butyrylcholinesterase (BuChE) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Development of molecular probes for the identification of extra interaction sites in the mid-gorge and peripheral sites of butyrylcholinesterase (BuChE). Rational design of novel, selective, and highly potent BuChE inhibitors. |
| AID271342 | Antitubercular activity against Mycobacterium tuberculosis H37Rv | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
| Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation. |
| AID1411528 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate pretreated for 4.5 mins followed by substrate addition and measured after 2.5 mins by Ellman's method | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6
| Novel bipharmacophoric inhibitors of the cholinesterases with affinity to the muscarinic receptors M |
| AID72314 | Competitive antagonist activity against Gamma-aminobutyric acid A (GABA-A) receptor | 2000 | Journal of medicinal chemistry, Apr-20, Volume: 43, Issue:8
| GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology. |
| AID304405 | Inhibition of human serum recombinant AChE by Ellman's method | 2007 | Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
| Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease. |
| AID241442 | Inhibitory concentration against rat brain Acetylcholinesterase | 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. |
| 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. |
| AID484174 | Inhibition of equine serum BuChE | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12
| Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |