Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 1935 |
| CHEMBL ID | 95 |
| CHEBI ID | 45980 |
| SCHEMBL ID | 2828 |
| MeSH ID | M0021008 |
| Synonym |
|---|
| BIDD:GT0090 |
| AB00053524-17 |
| BRD-K81473089-003-04-8 |
| BRD-K81473089-003-03-0 |
| acridine, 1,2,3,4-tetrahydro-9-amino- |
| 9-acridinamine, 1,2,3,4-tetrahydro- |
| 1,2,3,4-tetrahydro-acridin-9-ylamine |
| DIVK1C_000936 |
| KBIO1_000936 |
| cognex |
| SPECTRUM_000416 |
| tocris-0965 |
| lopac-a-3773 |
| NCGC00024908-01 |
| NCGC00015054-01 |
| BSPBIO_000337 |
| BSPBIO_003298 |
| BPBIO1_000371 |
| PRESTWICK3_000329 |
| PRESTWICK2_000329 |
| IDI1_000936 |
| LOPAC0_000036 |
| PDSP1_000330 |
| PDSP2_000328 |
| SPECTRUM5_001402 |
| STK101308 |
| 1,2,3,4-tetrahydroacridin-9-amine |
| tetrahydroaminacrine |
| 1,2,3,4-tetrahydro-9-acridineamine |
| EU-0010966 |
| AB00053524 |
| tacrina [inn-spanish] |
| cs 12602 |
| tacrinum [inn-latin] |
| einecs 206-291-2 |
| tetrahydroaminocrine |
| tetrahydroaminocrin |
| tacrine [inn:ban] |
| brn 0147610 |
| 5-amino-6,7,8,9-tetrahydroacridine (european) |
| 321-64-2 |
| C01453 |
| tacrine |
| tetrahydroaminoacridine |
| 1,2,3,4-tetrahydro-9-aminoacridine |
| 1,2,3,4-tetrahydro-9-acridinamine |
| 9-amino-1,2,3,4-tetrahydroacridine |
| CHEBI:45980 , |
| 5-amino-6,7,8,9-tetrahydroacridine |
| tracine |
| 9-amino-1,2,3,4-tetrahydroacridine (tha) |
| chembl95 , |
| 2AOX |
| 1MX1 |
| bdbm8961 |
| cid_1935 |
| 2AOW |
| DB00382 |
| tacrine.hcl |
| 9-tha |
| OPREA1_008681 |
| NCGC00024908-05 |
| NCGC00024908-03 |
| KBIOSS_000896 |
| KBIO3_002518 |
| KBIO2_000896 |
| KBIOGR_001337 |
| KBIO2_006032 |
| KBIO2_003464 |
| SPBIO_002258 |
| NINDS_000936 |
| SPECTRUM3_001709 |
| SPECTRUM4_000819 |
| PRESTWICK1_000329 |
| PRESTWICK0_000329 |
| NCIOPEN2_003667 |
| SPBIO_001823 |
| SPECTRUM2_001812 |
| NCGC00024908-04 |
| HMS2089F19 |
| NCGC00015054-07 |
| AKOS000277493 |
| tacrinal |
| tacrinal (tn) |
| tacrine (inn) |
| D08555 |
| NCGC00015054-06 |
| 5,6,7,8-tetrahydroacridin-9-amine |
| A18628 |
| 1,2,3,4-tetrahydro-acridin-9-yl-amine |
| unii-4vx7ynb537 |
| tacrina |
| 4vx7ynb537 , |
| tacrinum |
| tox21_302277 |
| dtxsid1037272 , |
| dtxcid9017272 |
| cas-321-64-2 |
| NCGC00255540-01 |
| BCP9000019 |
| tox21_110073 |
| CCG-204132 |
| SR-01000075593-13 |
| NCGC00015054-09 |
| NCGC00015054-02 |
| NCGC00015054-03 |
| NCGC00015054-10 |
| NCGC00015054-04 |
| NCGC00015054-08 |
| NCGC00015054-05 |
| FT-0631953 |
| tacrine [vandf] |
| tacrine [inn] |
| tacrine [mi] |
| tacrine [who-dd] |
| 1ACJ |
| gtpl6687 |
| C-110 |
| SCHEMBL2828 |
| tox21_110073_1 |
| NCGC00015054-12 |
| 1,2,3,4-tetra -hydro-9-acridinamine |
| T3994 |
| AE-641/00604043 |
| acridine, 9-aminotetrahydro- |
| romotal (salt/mix) |
| acridine, 9-amino-1,2,3,4-tetrahydro- |
| AB00053524_19 |
| AB00053524_18 |
| mfcd00046923 |
| SBI-0050025.P003 |
| Z56790573 |
| BCP03564 |
| Q421076 |
| BRD-K81473089-003-15-4 |
| SDCCGSBI-0050025.P004 |
| HMS3743C11 |
| BS-28027 |
| HY-111338 |
| AB89727 |
| SY138494 |
| EN300-02105 |
Tacrine (THA) is a drug used in the treatment of Alzheimer's disease as a cognitive enhancer and inhibitor of the enzyme acetylcholinesterase (AChE) Tacrine is a small organic compound that was discovered to mimic the functions of the neural cell adhesion molecule L1.
Tacrine has a sensitizing effect on M-cholinergic receptors. It occurs after a long incubation of the gastric smooth muscles with the drug and is manifested as a secondary contraction which is shifted in time and is significantly inhibited by atropine.
Tacrine has been on the French market for four years for symptomatic treatment of Alzheimer's disease. Tacrine has a sensitizing effect on M-cholinergic receptors; it occurs after a long incubation of the gastric smooth muscles with the drug.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tacrine has a biliary excretion in SCHs with maximum BEI% value of 22.9±1.9% at 10 min of incubation." | ( Tacrine sinusoidal uptake and biliary excretion in sandwich-cultured primary rat hepatocytes. Kaddoumi, A; Mohamed, LA, 2014) | 2.57 |
| "Tacrine has a sensitizing effect on M-cholinergic receptors; it occurs after a long incubation of the gastric smooth muscles with the drug and is manifested as a secondary contraction which is shifted in time and is significantly inhibited by atropine." | ( Sensitizing effect of tacrine on M-cholinergic receptors in gastric smooth muscle of rats. Ardasheva, RG; Argirova, MD; Getova, DP; Krustev, AD; Prisadova, NA; Turiiski, VI, ) | 1.89 |
| "Tacrine has a biliary excretion in SCHs with maximum BEI% value of 22.9±1.9% at 10 min of incubation." | ( Tacrine sinusoidal uptake and biliary excretion in sandwich-cultured primary rat hepatocytes. Kaddoumi, A; Mohamed, LA, 2014) | 2.57 |
| "Tacrine has a sensitizing effect on M-cholinergic receptors; it occurs after a long incubation of the gastric smooth muscles with the drug and is manifested as a secondary contraction which is shifted in time and is significantly inhibited by atropine." | ( Sensitizing effect of tacrine on M-cholinergic receptors in gastric smooth muscle of rats. Ardasheva, RG; Argirova, MD; Getova, DP; Krustev, AD; Prisadova, NA; Turiiski, VI, ) | 1.89 |
| "Tacrine has been shown to accumulate within mitochondria, and it particularly targets mtDNA." | ( Tacrine inhibits topoisomerases and DNA synthesis to cause mitochondrial DNA depletion and apoptosis in mouse liver. Berson, A; Demeilliers, C; Descatoire, V; Feldmann, G; Fromenty, B; Haouzi, D; Mansouri, A; Pessayre, D; Sutton, A; Vadrot, N, 2003) | 2.48 |
| "Tacrine has been shown to have efficacy in mildly to moderately impaired Alzheimer's patients on both psychometric testing and a clinician's structured interview." | ( Tacrine: first drug approved for Alzheimer's disease. Crismon, ML, 1994) | 2.45 |
| "Tacrine dosages have been studied in 5 protocols that used either enrichment or parallel designs." | ( The effect of tacrine and lecithin in Alzheimer's disease. A population pharmacodynamic analysis of five clinical trials. Holford, NH; Peace, K, 1994) | 1.37 |
| "Tacrine has also been shown to block ionic currents, including many types of potassium (K+) currents, calcium currents, and sodium currents." | ( Selective blockade of the delayed rectifier potassium current by tacrine in Drosophila. Kraliz, D; Singh, S, 1997) | 1.26 |
| "(1) Tacrine has been on the French market for four years for symptomatic treatment of Alzheimer's disease. " | ( Tacrine: a second look. An outdated drug to be discarded. , 1999) | 2.3 |
| "Tacrine has been studied in two clinical trials of identical design in patients with probable Alzheimer disease. " | ( Results and validation of a population pharmacodynamic model for cognitive effects in Alzheimer patients treated with tacrine. Holford, NH; Peace, KE, 1992) | 1.94 |
Tacrine did not activate whole-cell currents in KXα3β4R2 cells but inhibited receptor activity at submicromolar concentration. Tacrine induced increase of nicotinic receptors in SH-SY5Y cells, was not blocked by tubocurarine or mecamylamine.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tacrine did not activate whole-cell currents in KXα3β4R2 cells but inhibited receptor activity at submicromolar concentration." | ( Inhibition mechanism of rat α₃β₄ nicotinic acetylcholine receptor by the Alzheimer therapeutic tacrine. Cheffer, A; Ulrich, H, 2011) | 1.31 |
| "Tacrine can produce modest dose-related improvements in cognitive function and global measures of patient function." | ( Maximizing function in Alzheimer's disease: what role for tacrine? Smucker, WD, 1996) | 1.26 |
| "The tacrine-induced increase in number of nAChRs was significantly blocked by the antagonist mecamylamine (10(-4) M), while tubocurarine (10(-4) M) had no effect." | ( Tacrine interacts with an allosteric activator site on alpha 4 beta 2 nAChRs in M10 cells. Nordberg, A; Svensson, AL, 1996) | 2.22 |
| "Tacrine therapy could generate savings up to 17% of the current costs of AD, or a total of $3.6 billion annually for the estimated 1.6 million persons with mild-to-moderate AD." | ( Potential effect of tacrine on expenditures for Alzheimer's disease. Bowe, T; Lubeck, DP; Mazonson, PD, 1994) | 1.33 |
| "The tacrine induced increase of nicotinic receptors in SH-SY5Y cells, was not blocked in the presence of the nicotinic antagonists tubocurarine or mecamylamine." | ( Tacrine interacts with different sites on nicotinic receptor subtypes in SH-SY5Y neuroblastoma and M10 cells. Svensson, AL, 2000) | 2.23 |
| "Tacrine was found to inhibit the specific binding of [3H]quinuclidinyl benzilate (QNB) in rat brain cortex with IC50 values of 11 microM both in the absence and in the presence of 100 microM eserine, which had been added to ensure complete inhibition of cholinesterases at all concentrations of tacrine; in the cerebellum, the IC50 value was 10 microM in the absence and 14 microM in the presence of eserine; Hill slope factors (nH) were in the range of 1.55-1.79 and were not significantly affected by the presence of eserine." | ( The binding of cholinesterase inhibitors tacrine (tetrahydroaminoacridine) and 7-methoxytacrine to muscarinic acetylcholine receptors in rat brain in the presence of eserine. Musílková, J; Tucek, S, 1991) | 1.27 |
Tacrine hydrochloride, a reversible inhibitor of acetylcholinesterase, finds limited use in Alzheimer's disease due to frequent dosing, hepatotoxicity and extensive pre-systemic metabolism. Tacrine treatment increased the uptake of 11C-nicotine to the brain.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Tacrine treatment upregulated the expression of L1.1 (a homolog of the mammalian recognition molecule L1) and enhanced the L1.1-mediated intracellular signaling cascades in the injured spinal cords." | ( A Small Organic Compound Mimicking the L1 Cell Adhesion Molecule Promotes Functional Recovery after Spinal Cord Injury in Zebrafish. Hu, J; Li, R; Loers, G; Sahu, S; Schachner, M; Shen, H; Shen, Y; Zhang, Z, 2018) | 1.2 |
| "Tacrine treatment at a dose of 40 micro mol/kg caused a significant increase in serum alanine aminotransferase activity in 17- and 30-day-old mice at 6 h post-dosing, with the extent of stimulation in 30-day-old mice being more prominent." | ( Evaluation of acute tacrine treatment on passive-avoidance response, open-field behavior, and toxicity in 17- and 30-day-old mice. Dong, H; Han, YF; Ko, KM; Pan, SY; Yang, R; Yu, ZL, 2006) | 1.38 |
| "Oral tacrine treatment (80 mg daily) restore nicotinic receptors in AD patients as visualized by PET and 11C-nicotine." | ( In vivo detection of neurotransmitter changes in Alzheimer's disease. Nordberg, A, 1993) | 0.74 |
| "Tacrine treatment did not alter the level of HSP-70 in cell extracts and tacrine affected mildly the secretion of PN-1." | ( Tacrine alters the secretion of the beta-amyloid precursor protein in cell lines. Farlow, MR; Lahiri, DK; Lewis, S, 1994) | 2.45 |
| "Tacrine-treated rats showed a slight increase in the average initiation time for fast responses (i.e., a slight decrease in the local rate of responding), and also showed a substantial increase in the average length of pauses greater than 2.5 s." | ( Motor dysfunction produced by tacrine administration in rats. Aberman, J; Carriero, DL; Gianutsos, G; Mayorga, AJ; Outslay, G; Salamone, JD, 1997) | 1.31 |
| "Tacrine treatment increased the uptake of 11C-nicotine to the brain." | ( Tacrine restores cholinergic nicotinic receptors and glucose metabolism in Alzheimer patients as visualized by positron emission tomography. Amberla, K; Bjurling, P; Hartvig, P; Hellström-Lindahl, E; Johansson, M; Lilja, A; Lundqvist, H; Nordberg, A; Viitanen, M; Warpman, U, ) | 2.3 |
| "Oral treatment with tacrine hydrochloride; a reversible inhibitor of acetylcholinesterase, finds limited use in Alzheimer's disease due to frequent dosing, hepatotoxicity and extensive pre-systemic metabolism." | ( Design and Development of Novel Transdermal Nanoemulgel for Alzheimer's Disease: Pharmacokinetic, Pharmacodynamic and Biochemical Investigations. Farswan, M; Madaan, T; Razdan, BK; Setya, S; Talegaonkar, S, 2019) | 0.83 |
| "Pre-treatment with tacrine (RR = 0.29) was significantly more efficacious than pre-treatment with ranitidine, but the difference between tacrine and pyridostigmine was not significant." | ( Reversible cholinesterase inhibitors as pre-treatment for exposure to organophosphates: assessment using azinphos-methyl. Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA, 2015) | 0.74 |
| "Treatment with tacrine had no statistically significant effect on plasma Abeta42 and Abeta40 either at 2 weeks or at 6 weeks of administration compared to baseline levels." | ( Plasma levels of Abeta42 and Abeta40 in Alzheimer patients during treatment with the acetylcholinesterase inhibitor tacrine. Basun, H; Eckman, C; Lannfelt, L; Nilsberth, C; Younkin, S, 2002) | 0.86 |
| "Treatment with tacrine at a low dose (5 micro mol/kg) significantly prolonged the retention latency in 17-day-old mice only, but it shortened the retention latency at high doses of 20 and 40 micro mol/kg in 17- and 30-day-old, respectively." | ( Evaluation of acute tacrine treatment on passive-avoidance response, open-field behavior, and toxicity in 17- and 30-day-old mice. Dong, H; Han, YF; Ko, KM; Pan, SY; Yang, R; Yu, ZL, 2006) | 1 |
| "Treatment with tacrine in cells resulted in the drastic inhibition of secretion of the major isoforms of beta APP into the medium." | ( Reversibility of the effect of tacrine on the secretion of the beta-amyloid precursor protein in cultured cells. Lahiri, DK, 1994) | 0.91 |
| "Treatment with tacrine costs about $1,000 to $1,500 per year (Anderson, 1993)." | ( Tacrine: a pharmacological approach to Alzheimer's disease. Keltner, NL, 1994) | 2.07 |
| "Treatment with tacrine at doses > 80 mg/d was associated with a reduced likelihood of NHP. " | ( Long-term tacrine (Cognex) treatment: effects on nursing home placement and mortality, Tacrine Study Group. Davis, K; Gracon, S; Hoover, T; Knopman, D; Schneider, L; Smith, F; Talwalker, S, 1996) | 1.05 |
| "Treatment with tacrine or NIK-247 increased acetylcholine content of the striatum, but this effect was not enhanced by pindolol, which per se did not affect basal acetylcholine content." | ( Role of adrenergic neuronal activity in the yawning induced by tacrine and NIK-247 in rats. Fujii, K; Furukawa, T; Ishii, Y; Kimura, H; Matsumoto, S; Nagashima, M; Yamada, K; Yoshida, S, 1992) | 0.86 |
Tacrine was unable to significantly protect rat thymocytes against the toxic effects of sulphur mustard. The toxic effect of tacrine on hepatocytes was assayed by the reduction of methyl thiazolyl tetrazolium (MTT) and intracellular glutathione (GSH)
| Excerpt | Reference | Relevance |
|---|---|---|
| " To assess adverse events in relation to dosage and plasma drug levels, 24 hospitalized AD subjects were randomly assigned to receive placebo or HP 029 for 10 days in a double-blind, sequential escalation study." | ( Clinical safety, tolerance, and plasma levels of the oral anticholinesterase 1,2,3,4-tetrahydro-9-aminoacridin-1-oL-maleate (HP 029) in Alzheimer's disease: preliminary findings. Cutler, NR; De Luna, DM; Murphy, MF; Nash, RJ; Prior, PL, 1990) | 0.28 |
| " Treatment-related adverse clinical events occurred in 36%, 28%, and 30% of patients in the groups that received placebo, velnacrine maleate (150 mg), and velnacrine maleate (225 mg), respectively." | ( Effectiveness and safety of velnacrine for the treatment of Alzheimer's disease. A double-blind, placebo-controlled study. Mentane Study Group. Antuono, PG, 1995) | 0.29 |
| " In contrast, tacrine was unable to significantly protect rat thymocytes against the toxic effects of sulphur mustard." | ( Modulation of mustard toxicity by tacrine. Gray, P; Lewis, K; Masta, A; Phillips, D, 1994) | 0.93 |
| " Direct liver injury, possibly associated with the production of a toxic metabolite, would be consistent with reports of aberrant xenobiotic metabolism in Alzheimer's disease patients." | ( Clinical trials with velnacrine: (PROPP) the physician reference of predicted probabilities--a statistical model for the estimation of hepatotoxicity risk with velnacrine maleate. Hardiman, S; Miller, K; Murphy, M, 1993) | 0.29 |
| "Clinical trials with tacrine (THA) and its principal (1-OH) metabolite (velnacrine) for the treatment of Alzheimer's disease have been hampered by adverse hepatic events that were undetected in preclinical studies." | ( Cytotoxicity of tacrine and velnacrine metabolites in cultured rat, dog and human hepatocytes. Curren, RD; Viau, CJ; Wallace, K, 1993) | 0.95 |
| "To assess the value of serum measurements of tacrine hydrochloride and its metabolite in predicting risk of adverse reaction in Alzheimer's disease." | ( Serum concentrations of tacrine hydrochloride predict its adverse effects in Alzheimer's disease. Ford, JM; Roberts, CJ; Truman, CA; Wilcock, GK, 1993) | 0.85 |
| "Tacrine hydrochloride concentration is valuable in predicting the development of adverse effects, and its measurement may improve the use of the drug." | ( Serum concentrations of tacrine hydrochloride predict its adverse effects in Alzheimer's disease. Ford, JM; Roberts, CJ; Truman, CA; Wilcock, GK, 1993) | 2.04 |
| " A common side effect of this drug in humans is major hepatotoxicity." | ( Noninterference of cytochrome P4501A2 in the cytotoxicity of tacrine using genetically engineered V79 Chinese hamster cells for stable expression of the human or rat isoform and two human hepatocyte cell lines. Astier, AL; Benoit, GG; Naud, CF; Simard, MA, 1997) | 0.54 |
| " These results strongly suggest that THA-induced cytotoxicity is not mediated by CYP1A2 indicating that THA could be toxic by direct inhibition at the ribosomial level." | ( [No relationship between tacrine cytotoxicity and its metabolisation by cytochrome P4501A2]. Astier, A; Benoit, G; Naud, C; Simard, M, 1997) | 0.6 |
| " The most common tacrine-associated adverse events were elevated liver transaminase levels [alanine aminotransferase (ALT) and, to a lesser degree, aspartate aminotransferase] and peripheral cholinergic events involving primarily the digestive system (nausea, vomiting, diarrhea, dyspepsia, anorexia, and weight loss)." | ( Safety of tacrine: clinical trials, treatment IND, and postmarketing experience. Berghoff, WG; DeJong, R; Dombey, SL; Gracon, SI; Knapp, MJ; Kraemer, D; Lobbestael, SJ; Luscombe, FA; Pierce, M; Symons, J, 1998) | 1.04 |
| " THA induced dose-dependent toxic effects in liver parenchymal and nonparenchymal cells, with human hepatocytes being less sensitive." | ( Toxic effects of tacrine on primary hepatocytes and liver epithelial cells in culture. Guillouzo, A; Lagadic-Gossmann, D; Le Bot, MA; Rissel, M, 1998) | 0.64 |
| "The toxic effect of THA on mice liver was significantly reduced by DDB." | ( [Effect of dimethyl diphenyl bicarboxylate (DDB) on 9-amino-1,2,3,4-tetrahydroacridine-induced hepatotoxicity in mice]. Li, Y, 2001) | 0.31 |
| "5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects." | ( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004) | 0.32 |
| " The toxic effect of tacrine on hepatocytes was assayed by the reduction of methyl thiazolyl tetrazolium (MTT) and intracellular glutathione (GSH), as well as by albumin synthesis." | ( Re-evaluation of tacrine hepatotoxicity using gel entrapped hepatocytes. Bader, A; Meng, Q; Ru, J; Schmitmeier, S; Shen, C; Zhang, G, 2007) | 1 |
| " Genetic polymorphism of cytochrome P450 enzymes is probably responsible for balance between a number of stable and non-toxic metabolites and highly protein-reactive and toxic ones." | ( Possible role of hydroxylated metabolites of tacrine in drug toxicity and therapy of Alzheimer's disease. Jun, D; Kuca, K; Patocka, J, 2008) | 0.61 |
| " An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems." | ( Developing structure-activity relationships for the prediction of hepatotoxicity. Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010) | 0.36 |
| " However, tacrine was removed from the market due to its hepatotoxicity concerns as it undergoes metabolism to toxic quinonemethide species through the cytochrome P450 enzyme CYP1A2." | ( Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. Edginton, AN; McEneny-King, A; Osman, W; Rao, PPN, 2017) | 1.12 |
In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of tacrine (tetrahydroaminoacridine, THA) were found. The aim of the present work was to develop and validate an LC-MS/MS method with electrospray ionization for the quantification of T6FA in rat plasma.
| Excerpt | Reference | Relevance |
|---|---|---|
| " A population pharmacodynamic model has been developed that allows the use of all observations from one or more trials to be combined." | ( Methodologic aspects of a population pharmacodynamic model for cognitive effects in Alzheimer patients treated with tacrine. Holford, NH; Peace, KE, 1992) | 0.49 |
| " A population pharmacodynamic model has been used to describe the cognitive component of the Alzheimer disease assessment scale (ADASC) using mixed effects nonlinear regression." | ( Results and validation of a population pharmacodynamic model for cognitive effects in Alzheimer patients treated with tacrine. Holford, NH; Peace, KE, 1992) | 0.49 |
| " Pharmacokinetic parameters were related to clinical and biochemical effects in patients who, in a separate study, participated in a clinical trial of oral THA." | ( Pharmacokinetics of tetrahydroaminoacridine: relations to clinical and biochemical effects in Alzheimer patients. Adem, A; Ahlin, A; Junthé, T; Nybäck, H; Ohman, G, 1992) | 0.28 |
| " Forty-eight young male volunteers divided into six dosage groups were included into a single-dose pharmacokinetic study with either oral (p." | ( Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers. Albrecht, V; Dvorák, I; Dvoráková, J; Filip, V; Fusek, J; Havlůj, J; Vachek, J, 1991) | 0.54 |
| " The pharmacokinetic data were compared to the degree of sedation and pain relief." | ( Pharmacokinetics and effects of 9-amino-1,2,3,4-tetrahydroacridine in the immediate postoperative period in neurosurgical patients. Hartvig, P; Lindström, B; Pettersson, E; Wiklund, L, ) | 0.13 |
| "The duration of the effects of THA as an antagonist of postoperative sedation was only about double that seen previously after the IV administration of physostigmine in a similar group of patients, although the elimination half-life of THA was six times longer than that of physostigmine." | ( Pharmacokinetics and effects of 9-amino-1,2,3,4-tetrahydroacridine in the immediate postoperative period in neurosurgical patients. Hartvig, P; Lindström, B; Pettersson, E; Wiklund, L, ) | 0.13 |
| " Blood and urine samples were collected for the pharmacokinetic assessment." | ( Multiple dose pharmacokinetics, safety, and tolerance of velnacrine (HP 029) in healthy elderly subjects: a potential therapeutic agent for Alzheimer's disease. Ho, I; Hsu, R; Lassman, HB; Puri, SK, 1990) | 0.28 |
| " Dose-normalized Cmax and AUC values after administration of the 20 mg and 30 mg doses of tacrine were comparable to each other but were significantly greater (p less than ." | ( Steady-state pharmacokinetics of tacrine in patients with Alzheimer's disease. Balogh, L; Cutler, NR; Gamzu, ER; Gracon, SI; Kinkel, AW; Prior, P; Sedman, AJ; Selen, A; Underwood, BA, 1990) | 0.78 |
| " There were no consistent pharmacokinetic differences that could explain the effect on intravenous THA on muscle strength in these two patients." | ( Functional and pharmacokinetic studies of tetrahydroaminoacridine in patients with amyotrophic lateral sclerosis. Aquilonius, SM; Askmark, H; Gillberg, PG; Hartvig, P; Hilton-Brown, P; Lindström, B; Nilsson, D; Stålberg, E; Winkler, T, 1990) | 0.28 |
| " Tacrine is associated with large pharmacokinetic interindividual variation within both patient and control groups." | ( Clinical pharmacokinetics of tacrine. Madden, S; Park, BK; Spaldin, V, 1995) | 1.49 |
| "In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of the cholinesterase inhibitor tacrine (tetrahydroaminoacridine, THA) were found." | ( Tacrine in Alzheimer's disease: pharmacokinetic and clinical comparison of oral and rectal administration. Ahlin, A; Hassan, M; Junthé, T; Nybäck, H, 1994) | 1.93 |
| " We have used a population pharmacodynamic model to describe the response to tacrine and placebo in the 3 trials that used the enrichment design." | ( The effect of tacrine and lecithin in Alzheimer's disease. A population pharmacodynamic analysis of five clinical trials. Holford, NH; Peace, K, 1994) | 0.88 |
| "The pharmacokinetic of some centrally acting cholinesterase inhibitors that have been used to improve memory in patients with dementia of Alzheimer's type, was compared." | ( Pharmacokinetic studies of cholinesterase inhibitors. Johansson, M; Nordberg, A, 1993) | 0.29 |
| " Mean tacrine oral clearance was reduced by 30%; however, mean absorption rate and elimination half-life values were not affected by cimetidine." | ( Inhibition of tacrine oral clearance by cimetidine. deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996) | 1.14 |
| " The mean elimination half-life was estimated at 5-7 h and remained unchanged when the tacrine dose was increased." | ( Steady-state pharmacokinetics of tacrine in long-term treatment of Alzheimer patients. Hellström-Lindahl, E; Johansson, M; Nordberg, A, ) | 0.64 |
| "The pharmacokinetic disposition of intravenous and oral doses of tacrine was determined in 5 elderly patients (aged 64 to 96 y) with the clinical diagnosis of Alzheimer's disease." | ( Bioavailability and pharmacokinetic disposition of tacrine in elderly patients with Alzheimer's disease. Lou, G; Montgomery, PR; Sitar, DS, 1996) | 0.78 |
| " Drug interactions with cholinesterase inhibitors may occur by pharmacokinetic or pharmacodynamic mechanisms." | ( Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer's disease. Crismon, ML, ) | 0.13 |
| " Its long duration of action, coupled with its short pharmacokinetic half-life, reduces dosing frequency, decreases body drug exposure and minimizes the dependence of drug action on the individual variations of drug metabolism commonly found in the elderly." | ( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics. Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000) | 0.31 |
| " This article presents the latest information on their pharmacokinetic properties and pharmacodynamic activity." | ( Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors. Jann, MW; Shirley, KL; Small, GW, 2002) | 0.31 |
| " A comparison is also presented between several methods based on animal pharmacokinetic data, using the same set of proprietary compounds, and it lends further support for the use of this method, as opposed to methods that require the gathering of pharmacokinetic data in laboratory animals." | ( Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. Gao, F; Lombardo, F; Obach, RS; Shalaeva, MY, 2004) | 0.32 |
| " pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data." | ( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008) | 0.35 |
| " Intravenous and oral 6-h blood sampling profiles in old (30 months old) and young (7 months old) rats revealed pharmacokinetic changes similar to those in humans with an approximately 40% increase in C(max) of galantamine and prolonged t(1/2) (1." | ( Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats. Aw, CC; Browne, ER; Chen, CP; Goh, CW; Lee, JH, 2011) | 0.59 |
| " Pharmacokinetic study demonstrated that tacrine could be quickly absorbed and extensively metabolized to its monohydroxylated metabolites in vivo." | ( Pharmacokinetics and brain dispositions of tacrine and its major bioactive monohydroxylated metabolites in rats. Qian, S; Wo, SK; Zuo, Z, 2012) | 0.91 |
| " In Part II, there were no significant differences in Cmax, AUC0-tn or tmax between 4 mg single dose fasting group and fed group (p=0." | ( A single-center, randomized, open-label, dose-escalation study to evaluate the pharmacokinetics of tacrine analogue octahydrogenacridine succinate tablets in healthy Chinese subjects. Cui, Y; Gu, J; Liang, Y; Wang, D; Xu, J; Zhang, D; Zhao, X, 2012) | 0.6 |
| "To investigate the pharmacokinetic differences between the common nasal delivery models." | ( Pharmacokinetic comparison between the long-term anesthetized, short-term anesthetized and conscious rat models in nasal drug delivery. Qian, S; Wong, YC; Zuo, Z, 2014) | 0.4 |
| " Regarding the pharmacokinetic parameters (Cmax, Tmax, AUC, bioavailability) of tacrine and its metabolites, short-term anesthetized model resembled closer to conscious model than long-term anesthetized model." | ( Pharmacokinetic comparison between the long-term anesthetized, short-term anesthetized and conscious rat models in nasal drug delivery. Qian, S; Wong, YC; Zuo, Z, 2014) | 0.63 |
| " The aim of the present work was to develop and validate an LC-MS/MS method with electrospray ionization for the quantification of T6FA in rat plasma using tacrine-3-ferulic acid (T3FA) as internal standard and to examine its application for pharmacokinetic study in rats." | ( Determination of tacrine-6-ferulic acid in rat plasma by LC-MS/MS and its application to pharmacokinetics study. Deng, X; Liao, Q; Pi, R; Sun, X; Xie, Z; Zhang, P; Zhou, Y, 2014) | 0.94 |
| " This novel method has been applied to a pharmacokinetic study in rats." | ( Highly Sensitive LC-MS-MS Method for the Determination of Tacrine in Rat Plasma: Application to Pharmacokinetic Studies in Rats. Mullangi, R; Ponnayyan Sulochana, S; Ravichandiran, V; Sukumaran, SK, 2016) | 0.68 |
| "This work is aimed to synthesize and evaluate the effect of chalcones on the AChE activity, as well as anti-oxidant activity and predict their pharmacokinetic profile." | ( Effect on Acetylcholinesterase and Anti-oxidant Activity of Synthetic Chalcones having a Good Predicted Pharmacokinetic Profile. Almeida, WP; Figueiro, M; Kawano, DF; Sakata, RP, 2017) | 0.46 |
| " Considering the prediction of pharmacokinetic parameters being a useful tool for selecting potential drug candidates, our study results suggest that the majority of chalcones, including the most active one, have a promising pharmacokinetic profile and blood-brain barrier permeability." | ( Effect on Acetylcholinesterase and Anti-oxidant Activity of Synthetic Chalcones having a Good Predicted Pharmacokinetic Profile. Almeida, WP; Figueiro, M; Kawano, DF; Sakata, RP, 2017) | 0.46 |
The brain bioavailability of tacrine after intranasal TMME was found to be 2-fold higher. The results showed that tacrine could be directly transported into the brain from the nasal cavity.
| Excerpt | Reference | Relevance |
|---|---|---|
| " The bioavailability of THA was low and varied considerably between subjects." | ( Pharmacokinetics of tetrahydroaminoacridine: relations to clinical and biochemical effects in Alzheimer patients. Adem, A; Ahlin, A; Junthé, T; Nybäck, H; Ohman, G, 1992) | 0.28 |
| " The plasma clearance of THA was high and the oral bioavailability low with large interindividual differences (6-36%)." | ( Functional and pharmacokinetic studies of tetrahydroaminoacridine in patients with amyotrophic lateral sclerosis. Aquilonius, SM; Askmark, H; Gillberg, PG; Hartvig, P; Hilton-Brown, P; Lindström, B; Nilsson, D; Stålberg, E; Winkler, T, 1990) | 0.28 |
| " Oral bioavailability showed large interindividual differences and ranged 6-36% in the four subjects studied." | ( Clinical pharmacokinetics of intravenous and oral 9-amino-1,2,3,4-tetrahydroacridine, tacrine. Aquilonius, SM; Askmark, H; Hartvig, P; Lindström, B; Wiklund, L, 1990) | 0.5 |
| " In this open, randomized, crossover study, 24 healthy, elderly men were given 100 mg of velnacrine on two different study days to assess the influence of food on the bioavailability of velnacrine." | ( The effect of food on the bioavailability of velnacrine (HP 029) in healthy elderly men: a potential Alzheimer agent. Ho, I; Hsu, RS; Lassman, HB; Puri, SK, 1989) | 0.28 |
| " After intravenous administration, clearance was above 600 ml/min in both patients, and oral bioavailability was calculated at below 5%." | ( Pharmacokinetics of tacrine hydrochloride in Alzheimer's disease. Ford, JM; Forsyth, DR; Morgan, RA; Roberts, CJ; Truman, CA; Wilcock, GK, 1989) | 0.6 |
| " Pharmacokinetic investigations showed that the oral bioavailability of tacrine was low and greatly varying between subjects." | ( Clinical experiences and biochemical findings with tacrine (THA). Ahlin, A; Hassan, M; Junthé, T; Nybäck, H, 1993) | 0.77 |
| "In a previous pharmacokinetic study in Alzheimer patients great inter-individual variation and low oral bioavailability of the cholinesterase inhibitor tacrine (tetrahydroaminoacridine, THA) were found." | ( Tacrine in Alzheimer's disease: pharmacokinetic and clinical comparison of oral and rectal administration. Ahlin, A; Hassan, M; Junthé, T; Nybäck, H, 1994) | 1.93 |
| " Following oral administration of [14C]velnacrine maleate, drug-related material was well absorbed in all three species, with the majority of the dose recovered in the urine." | ( Disposition of [14C]velnacrine maleate in rats, dogs, and humans. Coe, RA; Gilbert, PJ; Hartley, TE; Hillbeck, D; Troke, JA; Turcan, RG; Vose, CW, ) | 0.13 |
| " It has a mean bioavailability after oral administration of about 17 percent and an elimination half-life of approximately three hours." | ( Tacrine: first drug approved for Alzheimer's disease. Crismon, ML, 1994) | 1.73 |
| " Mean tacrine oral clearance was reduced by 30%; however, mean absorption rate and elimination half-life values were not affected by cimetidine." | ( Inhibition of tacrine oral clearance by cimetidine. deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996) | 1.14 |
| " The bioavailability of the oral formulation was low (9." | ( Bioavailability and pharmacokinetic disposition of tacrine in elderly patients with Alzheimer's disease. Lou, G; Montgomery, PR; Sitar, DS, 1996) | 0.55 |
| " The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus." | ( Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities. Cheng, DH; Tang, XC, 1998) | 0.56 |
| "The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents." | ( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000) | 0.31 |
| " doses provided an estimate of oral bioavailability of 100%." | ( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics. Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000) | 0.31 |
| " The rate of absorption of 7-MEOTA during luminal perfusion with single 7-MEOTA was compared with rate of absorption during simultaneous perfusion with 7-MEOTA and CRT and with absorption rate after the premedication with CRT for period of three days before beginning of perfusion." | ( Intestinal single-pass in situ perfusion technique in rat: the influence of L-carnitine on absorption of 7-methoxytacrine. Bajgar, J; Herink, J; Herout, V; Kunes, M; Kvĕtina, J; Svoboda, Z, 2005) | 0.54 |
| "The mechanism associated with the increased bioavailability of tacrine as a result of a 24-h period of fasting was examined in rats." | ( Mechanism for increased bioavailability of tacrine in fasted rats. Ahn, SH; Chung, SJ; Hong, SS; Li, H; Park, BS; Park, CH; Seo, SY; Sung, JH, 2006) | 0.84 |
| " The results showed that tacrine could be directly transported into the brain from the nasal cavity and intranasal administration resulted in higher bioavailability of drug with reduced distribution into non-targeted tissues." | ( Nose-to-brain delivery of tacrine. Jogani, VV; Mishra, AK; Mishra, P; Misra, AR; Shah, PJ, 2007) | 0.94 |
| " In conclusion, B7T is expected to have a low oral bioavailability in vivo, which may be due to its poor intestinal permeability, significant tissue binding and hepatic hydroxylation metabolism." | ( Preclinical characterization of intestinal absorption and metabolism of promising anti-Alzheimer's dimer bis(7)-tacrine. Chan, K; Cheung, MC; Gu, ZM; Han, YF; Li, WM; Pang, YP; Wang, YT; Yu, H; Zhang, L; Zuo, Z, 2008) | 0.56 |
| " The brain bioavailability of tacrine after intranasal TMME compared with intranasal tacrine solution was found to be 2-fold higher indicating larger extent of distribution of the drug to brain with intranasal TMME." | ( Intranasal mucoadhesive microemulsion of tacrine to improve brain targeting. Jogani, VV; Mishra, AK; Mishra, P; Misra, AR; Shah, PJ, ) | 0.69 |
| "7%, whereas intranasal administration demonstrated an absolute bioavailability of 28." | ( Intranasal delivery of a novel acetylcholinesterase inhibitor HLS-3 for treatment of Alzheimer's disease. Han, Y; He, L; Ho, CY; Mak, M; Qian, S; Wang, Q; Wong, YC; Zuo, Z, 2018) | 0.48 |
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| "The objective of the study was to evaluate pharmacokinetic, pharmacodynamic, safety and stability profile of transdermal w/o nanoemulsion gel of tacrine hydrochloride and determine its relative bioavailability from transdermal nanogel in contrast to marketed capsule and conventional hydrogel." | ( Design and Development of Novel Transdermal Nanoemulgel for Alzheimer's Disease: Pharmacokinetic, Pharmacodynamic and Biochemical Investigations. Farswan, M; Madaan, T; Razdan, BK; Setya, S; Talegaonkar, S, 2019) | 0.71 |
| " In silico predicted ADME and physicochemical properties of conjugates showed good CNS bioavailability and safety parameters." | ( Piperazine-2-carboxylic acid derivatives as MTDLs anti-Alzheimer agents: Anticholinesterase activity, mechanistic aspect, and molecular modeling studies. Abd El-Wahab, HAA; Akincioglu, H; Gülçin, İ; Omar, FA; Soliman, AM, 2024) | 1.44 |
Tacrine treatment of AD patients with high dosage or in the long term may have effects on the process of amyloidogensis. Alteration of warfarin dosage should not be required in patients receiving concurrent tacrine therapy.
| Excerpt | Relevance | Reference |
|---|---|---|
| " The common dosage was 150 to 200 mg (3 to 4 of 50 mg dosing capsules per day)." | ( [Comparison of tacrine hepatotoxicity in patients with Alzheimer disease or AIDS]. Barbier, G; Beugre, T; Bonhomme, L; Dietlin, F; Esctein, S; Fredj, G; Jasmin, C; Kalifa, D; Meyer, P; Misset, JL, ) | 0.48 |
| " This dosage was well tolerated for 28 days." | ( Alzheimer's patients should be included in phase I clinical trials to evaluate compounds for Alzheimer's disease. Cutler, NR; Murphy, MF; Nash, RJ; Sramek, JJ, ) | 0.13 |
| "The tolerable dosage predicted by studies performed in healthy elderly subjects was 300 mg/d." | ( Implications of the study population in the early evaluation of anticholinesterase inhibitors for Alzheimer's disease. Cutler, NR; Murphy, MF; Nash, RJ; Sramek, JJ, 1992) | 0.28 |
| "A velnacrine dosage of 300 mg/d that was tolerated in healthy elderly subjects was not tolerated by AD patients." | ( Implications of the study population in the early evaluation of anticholinesterase inhibitors for Alzheimer's disease. Cutler, NR; Murphy, MF; Nash, RJ; Sramek, JJ, 1992) | 0.28 |
| " The dose-response curves for NIK-247 and tacrine were biphasic bell-shaped." | ( Effects of NIK-247 on CO-induced impairment of passive avoidance in mice. Kameyama, T; Kinbara, K; Nabeshima, T; Yoshida, S, 1992) | 0.55 |
| " Acute tetrahydroaminoacridine (THA) dosing caused lower brain (68%) and higher plasma (90%) ChE inhibition than the other drugs studied and increased levels of brain dihydroxyphenylacetic acid (DOPAC) (236%), homovanillic acid (HVA) (197%) and 5-hydroxyindoleacetic acid (5-HIAA) (130%)." | ( Effect of acute and chronic cholinesterase inhibition on biogenic amines in rat brain. Shillcutt, S; Soininen, H; Unni, L, 1990) | 0.28 |
| " The results suggest that 1) the insult to cholinergic neurons in the NBM may be involved in the PA memory consolidation deficit induced by nonselective quisqualic acid lesioning; 2) the beneficial effects of THA on NBM lesion-induced PA retention deficit occur in a narrow dose range; 3) the alleviating effects of THA on NBM lesion-induced PA memory deficits are blocked by frontal cortex lesions; and 4) the dose-response window for THA-induced PA retention performance improvement is broadened by repeated treatment." | ( Effects of THA on passive avoidance retention performance of intact, nucleus basalis, frontal cortex and nucleus basalis + frontal cortex-lesioned rats. Riekkinen, M; Riekkinen, P; Sirviö, J, 1991) | 0.28 |
| " Forty-eight young male volunteers divided into six dosage groups were included into a single-dose pharmacokinetic study with either oral (p." | ( Pharmacokinetics and tolerance of 7-methoxytacrine following the single dose administration in healthy volunteers. Albrecht, V; Dvorák, I; Dvoráková, J; Filip, V; Fusek, J; Havlůj, J; Vachek, J, 1991) | 0.54 |
| "Multicentre double blind, placebo controlled, random order crossover trial with individual determination of maximum tolerated dosage and four month follow up." | ( Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial. Groupe Français d'Etude de la Tetrahydroaminoacridine. Chatellier, G; Lacomblez, L, 1990) | 1.72 |
| " The tmax and t1/2 were not affected by dosage nor multiple dosing." | ( Multiple dose pharmacokinetics, safety, and tolerance of velnacrine (HP 029) in healthy elderly subjects: a potential therapeutic agent for Alzheimer's disease. Ho, I; Hsu, R; Lassman, HB; Puri, SK, 1990) | 0.28 |
| "4 hours for all dosing regimens." | ( Steady-state pharmacokinetics of tacrine in patients with Alzheimer's disease. Balogh, L; Cutler, NR; Gamzu, ER; Gracon, SI; Kinkel, AW; Prior, P; Sedman, AJ; Selen, A; Underwood, BA, 1990) | 0.56 |
| "A selective and stability-indicating high-performance liquid chromatographic assay with diazepam as the internal standard was developed for simultaneously analyzing physostigmine and tetrahydroaminoacridine in skin samples, permeation diffusates and dosage form." | ( Simultaneous determination of physostigmine and tetrahydroaminoacridine in a transdermal permeation study by high-performance liquid chromatography. Chow, D; Feldman, S; Lau, SW, 1990) | 0.28 |
| " To assess adverse events in relation to dosage and plasma drug levels, 24 hospitalized AD subjects were randomly assigned to receive placebo or HP 029 for 10 days in a double-blind, sequential escalation study." | ( Clinical safety, tolerance, and plasma levels of the oral anticholinesterase 1,2,3,4-tetrahydro-9-aminoacridin-1-oL-maleate (HP 029) in Alzheimer's disease: preliminary findings. Cutler, NR; De Luna, DM; Murphy, MF; Nash, RJ; Prior, PL, 1990) | 0.28 |
| " A two-phase experiment was performed: initially, one animal was used and served as his own control in a multiple dose, crossover, placebo controlled trial, designed to establish a dose-response curve and an optimal dose range based on THA serum concentrations." | ( Oral tacrine administration in middle-aged monkeys: effects on discrimination learning. Fitten, LJ; Kling, A; Perryman, K; Tachiki, K, ) | 0.65 |
| " Some combinations of cholinergic drugs enhance retention even though the total drug dosage is reduced by as much as 97% compared to the dose needed to improve retention when the same drugs are administered singly." | ( Two-drug combinations of memory enhancers: effect of dose ratio upon potency and therapeutic window, in mice. Cherkin, A; Flood, JF; Smith, GE, 1988) | 0.27 |
| " A dose-response curve was determined for each of four drugs (arecoline, edrophonium, oxotremorine, tacrine) and for each of the six possible two-drug combinations." | ( Memory enhancement: supra-additive effect of subcutaneous cholinergic drug combinations in mice. Cherkin, A; Flood, JF; Smith, GE, 1985) | 0.49 |
| " There was a significant dose-response relationship up to 160 mg/day." | ( Tacrine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in Alzheimer's disease. McTavish, D; Wagstaff, AJ, 1994) | 1.73 |
| " Alteration of warfarin dosage should not be required in patients receiving concurrent tacrine therapy." | ( Lack of effect of tacrine administration on the anticoagulant activity of warfarin. Garnett, WR; Rajagopalan, R; Reece, PA; Rock, WL; Sedman, AJ; Taylor, JR; Underwood, B, 1995) | 0.85 |
| " A reliable caregiver is essential to ensure compliance with frequent dosing and weekly blood testing." | ( Alzheimer's disease: how to give and monitor tacrine therapy. Lantz, MS; Woo, JK, 1995) | 0.55 |
| " Pharmacokinetic parameters for the elimination of radioactivity from the plasma of rats and dogs were similar after oral dosing compared with intravenous dosing." | ( Disposition of [14C]velnacrine maleate in rats, dogs, and humans. Coe, RA; Gilbert, PJ; Hartley, TE; Hillbeck, D; Troke, JA; Turcan, RG; Vose, CW, ) | 0.13 |
| " The time-course of the response and its relation to tacrine dosage obtained from the enrichment design analysis were used to define the parallel design." | ( The effect of tacrine and lecithin in Alzheimer's disease. A population pharmacodynamic analysis of five clinical trials. Holford, NH; Peace, K, 1994) | 0.9 |
| " The two drugs are special as the dosage of them is guided mainly by side effects and not by therapeutic effects in contrast to most drugs used for psychiatric disorders." | ( Side effects of long acting cholinesterase inhibitors. Beermann, B, 1993) | 0.29 |
| " Group 3 remained on a dosage of 120 mg/d for a total of 18 weeks; after 6 weeks at 120 mg/d, group 4 titrated to 160 mg/d for the last 12 weeks." | ( A 30-week randomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. The Tacrine Study Group. Davis, CS; Gracon, SI; Knapp, MJ; Knopman, DS; Pendlebury, WW; Solomon, PR, 1994) | 0.54 |
| "05) dose-response trends and between-group comparisons on CIBI and ADAS-Cog." | ( A 30-week randomized controlled trial of high-dose tacrine in patients with Alzheimer's disease. The Tacrine Study Group. Davis, CS; Gracon, SI; Knapp, MJ; Knopman, DS; Pendlebury, WW; Solomon, PR, 1994) | 0.54 |
| " In new rats, a dose-response assessment revealed that 60 and 30 nmol, but not 10 nmol, CDP infused into the medial septum impaired spatial learning, but not cue learning or swim speed." | ( Effects of intracranial infusions of chlordiazepoxide on spatial learning in the Morris water maze. II. Neuropharmacological specificity. McNamara, RK; Skelton, RW, 1993) | 0.29 |
| " We report age-related changes in the drug dosage needed to improve 1 week retention in the P/8 but not R/1 line." | ( Age-related changes in the pharmacological improvement of retention in senescence accelerated mouse (SAM). Flood, JF; La Reginna, M; Morley, JE, ) | 0.13 |
| " Clinical considerations may dictate a reduction in tacrine dosage when tacrine is coadministered with cimetidine." | ( Inhibition of tacrine oral clearance by cimetidine. deVries, TM; Forgue, ST; Reece, PA; Sedman, AJ, 1996) | 0.91 |
| "mandomized assignment to placebo or one of three ascending dosage regimens of tacrine over 30 weeks, followed by open label treatment for all patients who began the double-blind trial." | ( Long-term tacrine (Cognex) treatment: effects on nursing home placement and mortality, Tacrine Study Group. Davis, K; Gracon, S; Hoover, T; Knopman, D; Schneider, L; Smith, F; Talwalker, S, 1996) | 0.92 |
| " In addition, zinc or tacrine treatment of AD patients with high dosage or in the long term may have effects on the process of amyloidogensis." | ( Amyloidogenic processing of Alzheimer's amyloid precursor protein in vitro and its modulation by metal ions and tacrine. Chong, YH; Suh, YH, 1996) | 0.82 |
| " The reversal of scopolamine-induced impairment was characterized by the presence of an inverted U-shaped dose-response curve." | ( An inverted U-shaped curve for heptylphysostigmine on radial maze performance in rats: comparison with other cholinesterase inhibitors. Braida, D; Griffini, P; Lamperti, M; Maggi, A; Paladini, E; Sala, M, 1996) | 0.29 |
| " Dosing was initiated at 40 mg/day and increased in increments of 40 mg/day every 6 weeks until the target dose was achieved." | ( Mixed-model analysis of incomplete longitudinal data from a high-dose trial of tacrine (Cognex) in Alzheimer's patients. Smith, F, 1996) | 0.52 |
| " Using last tacrine dose, the analyses demonstrated a dose-response relationship where patients on higher tacrine doses were less likely to enter a nursing home or die than patients on lower doses." | ( The use of survival analysis techniques in evaluating the effect of long-term tacrine (Cognex) treatment on nursing home placement and mortality in patients with Alzheimer's disease. Gracon, S; Smith, F; Srirama, M; Talwalker, S, 1996) | 0.9 |
| " Six groups of adult rats were given 10 mg/kg THA twice daily by gavage for 1, 2, 4, or 8 wk (chronic THA groups), or 1 mL of saline twice daily by gavage for 1-8 wk (control), or IV THA approximately 20 min before (acute), and the cumulative dose-response curves of dTC at the tibialis and soleus muscles were determined during indirect train-of-four stimulation in the anesthetized, mechanically ventilated rat." | ( The effects of chronic tacrine therapy on d-tubocurarine blockade in the soleus and tibialis muscles of the rat. Donati, F; Eshelby, D; Fox, GS; Ibebunjo, C; Tchervenkov, JI, 1997) | 0.61 |
| " Twelve to 18 hr after the last gavage of tacrine or saline, and -20 min after iv tacrine, cumulative dose-response curves of succinylcholine were determined in the tibialis and soleus muscles in anaesthetized, ventilated rats during monitoring of evoked twitch response to indirect (nerve) train-of-four stimulation." | ( Tacrine does not alter the potency of succinylcholine in the rat. Donati, F; Eshelby, D; Fox, GS; Ibebunjo, C; Tchervenkov, JI, 1997) | 2 |
| " Approximately half the patients treated with tacrine have liver enzyme abnormalities develop, primarily in the first 12 weeks of therapy, that resolve with discontinuation of drug or dosage adjustment." | ( Tacrine. A cause of fatal hepatotoxicity? Blackard, WG; Crowe, DR; Fallon, MB; Sood, GK, 1998) | 2 |
| " The reversal of scopolamine-induced impairment was characterized by an inverted U-shaped dose-response curve." | ( Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268). Braida, D; Colibretti, L; Griffini, P; Lamperti, M; Paladini, E; Sala, M, 1998) | 0.3 |
| " Cholinergic events were manageable with dosage adjustment." | ( Safety of tacrine: clinical trials, treatment IND, and postmarketing experience. Berghoff, WG; DeJong, R; Dombey, SL; Gracon, SI; Knapp, MJ; Kraemer, D; Lobbestael, SJ; Luscombe, FA; Pierce, M; Symons, J, 1998) | 0.7 |
| " Tacrine, the first drug marketed for Alzheimer's disease (AD), induces an elevation of serum liver transaminase prohibiting an effective dosage in many patients." | ( Aminotransferase levels and silymarin in de novo tacrine-treated patients with Alzheimer's disease. Allain, H; Braun, W; Brissot, P; Gandon, JM; Lebreton, S; Schück, S; Strenge-Hesse, A, ) | 1.3 |
| " Patients were treated blindly in relation to the ApoE phenotype, with incremental tacrine dosages ranging from 40 mg/day up to the highest dosage (160 mg) tolerated without side-effects." | ( The apolipoprotein E epsilon4 allele and the response to tacrine therapy in Alzheimer's disease. Boller, F; Caputo, L; Couderc, R; de Rotrou, J; Forette, F; Guelfi, MC; Latour, F; Moulin, F; Rigaud, AS; Traykov, L, 2000) | 0.78 |
| " The present study investigated the dose-response characteristics of donepezil, tacrine, rivastigmine and metrifonate in inducing tremor, lacrimation, salivation and hypothermia and the duration of action of these compounds in Lister hooded rats." | ( Comparison of donepezil-, tacrine-, rivastigmine- and metrifonate-induced central and peripheral cholinergically mediated responses in the rat. Dronfield, S; Egan, K; Green, AR; Marsden, CA, 2000) | 0.83 |
| " In order to maximize and prolong positive drug effects, it is important to start early and adjust dosage during the treatment." | ( Cholinesterase inhibitors stabilize Alzheimer's disease. Giacobini, E, 2000) | 0.31 |
| " Its long duration of action, coupled with its short pharmacokinetic half-life, reduces dosing frequency, decreases body drug exposure and minimizes the dependence of drug action on the individual variations of drug metabolism commonly found in the elderly." | ( The experimental Alzheimer drug phenserine: preclinical pharmacokinetics and pharmacodynamics. Brossi, A; De Micheli, E; Deutsch, J; Greig, NH; Holloway, HW; Ingram, DK; Lahiri, DK; Perry, TA; Soncrant, TT; Utsuki, T; Yu, QS, 2000) | 0.31 |
| "The features of apoptotic dose responses typically have been evaluated over a broad dose-response continuum to differentiate apoptotic and necrotic responses." | ( Apoptosis: biphasic dose responses. Calabrese, EJ, 2001) | 0.31 |
| " Improvement in behavioural symptoms also occurs, but without a dose-response relationship." | ( Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors. Jann, MW; Shirley, KL; Small, GW, 2002) | 0.31 |
| "1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg." | ( Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors. Albuquerque, EX; Christner, C; Fehrenbacher, A; Höffle, A; Jostock, R; Lübbert, H; Ludwig, J; Maelicke, A; Pereira, EF; Radina, M; Samochocki, M; Ullmer, C; Zerlin, M, 2003) | 0.32 |
| " Dose-response curves for tremor (central effect) and salivation (peripheral effect) showed that donepezil and icopezil possess a more favourable therapeutic index than the nonselective inhibitors, tacrine and heptylphysostigmine." | ( Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease. Chapin, D; Hubbard, ST; Jones, SB; Liston, DR; Nason, D; Nielsen, JA; Ramirez, A; Shalaby, IA; Villalobos, A; White, WF, 2004) | 0.51 |
| " In the random trials, tacrine dosage ranged from 25 to 200 mg/day, with a duration of 3-36 weeks." | ( Methodology, results and quality of clinical trials of tacrine in the treatment of Alzheimer's disease: a systematic review of the literature. Arrieta, JL; Artalejo, FR, 1998) | 0.86 |
| " Use of controlled-release dosage forms to deliver drugs for chronic administration, by taking advantage of their rate-controlling drug delivery features, has gained increasing popularity in recent years." | ( A potent and selective tacrine analog--biomembrane permeation and physicochemical characterization. Chien, YW; Pang, YP; Patani, GA, 2005) | 0.64 |
| " The type of inhibition (competitive, uncompetitive, or mixed), the dissociation constants for the inhibitors, and the inhibitor dose-response curves were also determined." | ( Automated method, based on micro-sequential injection, for the study of enzyme kinetics and inhibition. Carroll, AD; Chen, Y; Ruzicka, J; Scampavia, L, 2006) | 0.33 |
| " Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
| " This selective localization of tacrine in the brain may be helpful in reducing dose, frequency of dosing and dose-dependent side effects, and may prove an interesting new approach in delivery of the drug to the brain for the treatment of Alzheimer's disease." | ( Nose-to-brain delivery of tacrine. Jogani, VV; Mishra, AK; Mishra, P; Misra, AR; Shah, PJ, 2007) | 0.92 |
| " The role of acute dosing rodent models in identifying candidate genes associated with drug-induced liver injury in man deserves further study." | ( Molecular and genetic association of interleukin-6 in tacrine-induced hepatotoxicity. Alfirevic, A; Barratt, BJ; Carr, DF; Park, BK; Pirmohamed, M; Sherwood, J; Smith, J; Tugwood, JD, 2007) | 0.59 |
| " We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
| " We have assessed in vivo the mortality-reducing efficacy of a group of known AChE inhibitors, when given in equitoxic dosage before exposure to the OPC paraoxon." | ( Usefulness of administration of non-organophosphate cholinesterase inhibitors before acute exposure to organophosphates: assessment using paraoxon. Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA; Shafiullah, M, 2013) | 0.39 |
| " Protection was quantified using Cox analysis by determining the relative risk (RR) of death in rats that were administered these AChE inhibitors in equitoxic dosage (25% of LD01) 30 min before azinphos-methyl exposure." | ( Reversible cholinesterase inhibitors as pre-treatment for exposure to organophosphates: assessment using azinphos-methyl. Hasan, MY; Kuča, K; Lorke, DE; Nurulain, SM; Petroianu, GA, 2015) | 0.42 |
| " To evaluate the protocol, brain sections from mice dosed intraperitoneally with donepezil, tacrine, clozapine, haloperidol, and aripiprazole were used." | ( Development of an Integrated Tissue Pretreatment Protocol for Enhanced MALDI MS Imaging of Drug Distribution in the Brain. Chen, Y; Gordon, A; Li, B; Tang, W, 2020) | 0.78 |
| Role | Description |
|---|---|
| EC 3.1.1.7 (acetylcholinesterase) inhibitor | An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of enzyme acetylcholinesterase (EC 3.1.1.7), which helps breaking down of acetylcholine into choline and acetic acid. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| acridines | |
| aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Pathway | Proteins | Compounds |
|---|---|---|
| histamine degradation | 4 | 24 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 39.8107 | 0.0251 | 20.2376 | 39.8107 | AID886 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 15.8489 | 0.1778 | 14.3909 | 39.8107 | AID2147 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 3.2617 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395; AID1347397; AID1347398; AID1347399 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 7.5193 | 0.1000 | 20.8793 | 79.4328 | AID488772; AID588456 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 12.5893 | 0.0126 | 10.6917 | 88.5700 | AID887 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 61.6448 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 14.5750 | 0.0041 | 10.8903 | 31.5287 | AID493107 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0282 | 7.0559 | 15.8489 | AID895; AID928 |
| GLS protein | Homo sapiens (human) | Potency | 28.1838 | 0.3548 | 7.9355 | 39.8107 | AID624146 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 61.6448 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
| TDP1 protein | Homo sapiens (human) | Potency | 25.2291 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 8.6644 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
| AR protein | Homo sapiens (human) | Potency | 45.7540 | 0.0002 | 21.2231 | 8,912.5098 | AID743035; AID743042; AID743054; AID743063 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 19.9526 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 26.2000 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 22.3294 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 1.8888 | 0.5318 | 15.4358 | 37.6858 | AID504845 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 16.2855 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 21.8870 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 56.6987 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 15.9197 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 38.5708 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 41.8020 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743080; AID743091 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.7717 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| arylsulfatase A | Homo sapiens (human) | Potency | 3.3808 | 1.0691 | 13.9551 | 37.9330 | AID720538 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 37.6858 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 26.5949 | 0.0007 | 23.0674 | 1,258.9301 | AID743085; AID743122 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 61.1306 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 0.0525 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 0.0020 | 7.5337 | 39.8107 | AID891 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 15.8489 | 0.0025 | 5.8400 | 31.6228 | AID899 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 49.1692 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 34.3762 | 0.0006 | 27.2152 | 1,122.0200 | AID743219 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 0.1901 | 0.4256 | 12.0591 | 28.1838 | AID504536 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 28.1838 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 18.1056 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 15.8489 | 0.0316 | 10.2792 | 39.8107 | AID884; AID885 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 13.8914 | 0.0010 | 6.0009 | 35.4813 | AID943; AID944 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 31.6228 | 0.0200 | 10.7869 | 31.6228 | AID912 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.1623 | 0.3162 | 12.7657 | 31.6228 | AID881 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 45.4900 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 32.0647 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 45.4900 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.1623 | 0.0063 | 8.2350 | 39.8107 | AID881 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| Ataxin-2 | Homo sapiens (human) | Potency | 15.8489 | 0.0119 | 12.2221 | 68.7989 | AID588378 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 15.8489 | 1.0000 | 12.2248 | 31.6228 | AID885 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| mu-type opioid receptor isoform MOR-1 | Homo sapiens (human) | EC50 (µMol) | 92.4700 | 0.1320 | 3.3004 | 9.5690 | AID720642 |
| 5-hydroxytryptamine receptor 2A | Mus musculus (house mouse) | EC50 (µMol) | 76.0830 | 0.0038 | 1.3621 | 8.3930 | AID720643 |
| Acetylcholinesterase | Electrophorus electricus (electric eel) | Kd | 0.0160 | 0.0160 | 0.8065 | 2.2000 | AID1396208 |
| Muscarinic acetylcholine receptor M2 | Sus scrofa (pig) | EC50 (µMol) | 6.3048 | 0.0135 | 1.8625 | 6.3096 | AID303074 |
| Fatty acid-binding protein, liver | Homo sapiens (human) | Kd | 900.0000 | 0.2000 | 0.5500 | 0.9000 | AID1632106 |
| Acetylcholinesterase | Mus musculus (house mouse) | Kd | 0.0180 | 0.0180 | 0.5590 | 1.1000 | AID31795 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Histamine N-methyltransferase | Homo sapiens (human) | Activity | 0.0100 | 0.0100 | 0.0100 | 0.0100 | AID387771 |
| Carboxylic ester hydrolase | Rattus norvegicus (Norway rat) | INH | 0.0810 | 0.0810 | 0.0810 | 0.0810 | AID1545288 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1632107 | Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP6 expressed in Escherichia coli NEB cells at 200 uM by surface plasmon resonance method | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). |
| AID1271538 | Hepatotoxicity in ICR mouse assessed as serum aspartate aminotransferase level at 30 mg/kg, ig after 22 hrs by spectrophotometry analysis (Rvb = 113.9 +/- 31.1 U/L) | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| 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. |
| AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID331669 | Inhibition of equine BChE by Ellman's assay | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates. |
| AID1810884 | Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins by spectrophotometric analysis | |||
| AID692189 | Therapeutic index, ratio of Cmax in human to IC50 for human OCT2 A270S mutant | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
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| AID1651267 | Antioxidant activity assessed as hydroxyl radical scavenging activity incubated for 30 mins in water bath | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis and anti-Alzheimer's disease activity study of xanthone derivatives based on multi-target strategy. |
| AID1406253 | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 1 min by Ellman's assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID303069 | Inhibition of Electrophorus electricus Acetylcholinesterase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| AID1202689 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain. |
| AID1674222 | Inhibition of rat brain Acetylcholinesterase using acetylthiocholine as substrate in presence of BChE inhibitor ethopropazine | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Fragment Linking Strategies for Structure-Based Drug Design. |
| AID257806 | Inhibition of BuChE from horse serum | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
| AID43581 | Inhibition of beta-lactamase at 100 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID714533 | Cytotoxicity against human HepG2 cells assessed as cell viability at 3 uM after 24 hrs by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1057010 | Inhibition of human erythrocytic AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman method | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID44441 | Inhibitory concentration against rat brain butyrylcholinesterase (BuChE) was determined using Ellman's method | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors. |
| AID1886721 | Inhibition of human AChE assesses as inhibitory rate at 10 uM using acetylthiocholine iodide iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method relative to control | |||
| AID1271533 | Hepatotoxicity in ICR mouse assessed as serum alanine aminotransferase level at 30 mg/kg, ig after 36 hrs by spectrophotometry analysis (Rvb = 38.1 +/- 8.2 U/L) | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1450072 | Inhibition of recombinant human CYP1A2 expressed in insect cells at 0.01 uM using EOMCC as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
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| AID1332147 | Inhibition of human recombinant microsomal MAO-A expressed in baculovirus-infected insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by amplex red assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents. |
| AID1070084 | Inhibition of electric eel acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID657793 | Selectivity ratio of IC50 for mitochondrial MAO-B in rat liver homogenates to IC50 for mitochondrial MAO-A in rat liver homogenates | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID118346 | Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 2.5 mg/kg sc | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1311919 | Inhibition of human erythrocyte ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1054516 | Inhibition of human recombinant BuChE by Ellman's assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer's disease. |
| AID656043 | Antioxidant activity assessed as trolox equivalent of peroxyl radical scavenging activity in phosphate buffer at pH 7.4 by ORAC assay | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID1077104 | Toxicity in Wistar rat assessed as total glutathione level in kidney at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
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| AID31496 | Inhibitory activity against Acetylcholinesterase | 1996 | Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26 | Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors. |
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| AID1480846 | Inhibition of human erythrocyte AChE at 5 uM using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1831861 | Cytotoxicity against human HepG2 cells assessed as cell viability at 0.1 uM after 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID303074 | Inhibition of [3H]NMS dissociation from porcine muscarinic M2 receptor | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| AID1399485 | Inhibition of porcine liver carboxylesterase at 20 uM using 4-nitrophenol acetate as substrate incubated for 10 mins followed by substrate addition by spectrophotometric method relative to control | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics. |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID455416 | Inhibition of human AChE by Ellman's method | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives. |
| AID1077117 | Toxicity in Wistar rat assessed as GSSG level in brain at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1077116 | Toxicity in Wistar rat assessed as GSSG level in brain at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1728609 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 1 min in presence of H2O2 by Ellman's method | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID1435914 | Cytotoxicity against human primary hepatocytes assessed as cell viability at 0.1 uM measured after 2 hrs by trypan blue assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
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| AID628415 | Inhibition of human recombinant AChE after 5 mins using spectrophotometer by Ellman's method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties. |
| AID1351140 | Hepatotoxicity in Kunming mouse assessed as increase in serum ASAT level at 35 mg/kg, ig after 48 hrs by colorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1501663 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 0.23 uM after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
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| AID1728644 | Cognitive enhancing effect in Sprague-Dawley rat model of amyloid beta (25 to 35) peptide-induced memory impairment assessed as reduction in escape latency time at 0.2 mg per 100 g, ip qd for 4 weeks administered via gavage and measured after 4 to 5 days | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
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| AID1152333 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Novel aromatic-polyamine conjugates as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. |
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| AID1831868 | Antineuroinflammatory activity in mouse BV-2 cells assessed as suppression of LPS-induced COX-2 mRNA expression at 0.1 uM preincubated for 24 hrs followed by LPS stimulation and measured after 24 hrs by RT-PCR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
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| 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. |
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| AID1686242 | Toxicity in human HepG2 cells assessed as cell viability at 300 uM by MTT assay relative to control | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID170963 | Ameliorating effects on diazepam-induced memory impairment of passive avoidance response (no of rats) by peroral administration | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
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| AID1542239 | Toxicity in mouse neuronal cells assessed as safe dose that maintains 100% cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1351116 | Inhibition of human self-induced amyloid beta (1 to 42) aggregation at 20 uM after 48 hrs by ThT fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
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| AID1077102 | Toxicity in Wistar rat assessed as lipidperoxidation product level in kidney at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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| AID469399 | Selectivity ratio of IC50 for human AChE to IC50 for human BuChE | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease. |
| AID540235 | Phospholipidosis-negative literature compound | |||
| AID240819 | Inhibitory concentration against rat serum Butyrylcholinesterase | 2004 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18 | Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID240813 | Inhibitory concentration against butyrylcholinesterase | 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. |
| AID690970 | Antioxidant activity of the compound assessed as DPPH radical scavenging activity after 60 mins | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. |
| 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. |
| AID1379213 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured for 6 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID480450 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID482855 | Inhibition of AChE in human erythrocytes by Ellman's method | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID729967 | Inhibition of horse serum BChE using butyrylthiocholine chloride as substrate after 15 mins by Ellman's method | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease. |
| AID1140643 | Displacement of propidium iodide from AchE in bovine erythrocytes at 0.3 uM after 15 mins by fluorescence microplate reader analysis | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | New melatonin-N,N-dibenzyl(N-methyl)amine hybrids: potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID781329 | pKa (acid-base dissociation constant) as determined by other workers | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID1198133 | Hepatotoxicity in Sprague-Dawley rat assessed as increase in alanine aminotransferase activity in serum at 6 umol/100g body weight, ip measured after 24 to 36 hrs | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID716203 | Inhibition of horse AChE by colorimetric Ellman assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1891150 | Inhibition of BChE (unknown origin) using acetylcholine iodide as substrate incubated for 10 mins by Ellman's method | 2022 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 65 | Polyphenolic compounds: Synthesis, assessment of antimicrobial effect and enzymes inhibition against important medicinal enzymes with computational details. |
| AID1435911 | Cytotoxicity against human HepG2 cells at 100 uM measured after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID302147 | Inhibition of human recombinant AChE by Ellman's method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
| AID1409648 | Inhibition of self-induced aggregation of HFIP-treated human amyloid beta (1 to 42 residues) at 20 uM by thioflavin T-based fluorescence assay relative to control | |||
| AID1071763 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1382544 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| AID118339 | Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 0.63 mg/kg sc | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1409662 | Hepatotoxicity in ICR mouse assessed as serum AST activity at 30 mg/kg, administered intragastrically measured 36 hrs post dose (Rvb = 120 +/- 13 U/L) | |||
| AID244095 | Selectivity for Acetylcholinesterase and butyrylcholinesterase | 2004 | Bioorganic & medicinal chemistry letters, Sep-20, Volume: 14, Issue:18 | Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1886723 | Inhibition of human BChE using acetylthiocholine iodide or butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | |||
| 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. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
| AID1627647 | Displacement of [3H]Nalpha-methylhistamine from human full length recombinant histamine H3 receptor expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID1399482 | Inhibition of equine serum BChE using butylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics. |
| AID552182 | Inhibition of electric eel AChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation. |
| AID567063 | Selectivity ratio of IC50 for horse serum BChE to IC50 for electric eel AChE | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists. |
| AID349873 | Inhibition of human serum AChE by Ellman's method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1075982 | Inhibition of scopolamine-induced cognitive deficit in ICR mouse assessed as spontaneous alternation behaviour at 1 mg/kg, ip administered 1 hr prior to scopolamine challenge measured after 30 mins by Y-maze test (Rvb = 40.22 +/-3.54%) | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1167624 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1389654 | Reversal of scopolamine-induced cognitive function impairment in ICR mouse assessed as escape latency at 15 mg/kg, po dosed 30 mins before scopolamine challenge by Morris water maze test | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
| AID1456265 | Antioxidant activity assessed as trolox equivalent of AAPH-induced peroxyl radical scavenging activity at 0.1 to 10 uM preincubated for 15 mins followed by AAPH addition measured every min for 90 mins by ORAC-FL assay | |||
| AID274657 | Viability of SH-SY5Y cells measured as neuroprotection activity in presence of H2O2 at 0.3 uM relative to control | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| AID621448 | Inhibition of human AChE by Ellman's assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation. |
| AID1435912 | Cytotoxicity against human HepG2 cells at 300 uM measured after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| 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. |
| AID421518 | Inhibition of human recombinant AChE-mediated amyloid beta aggregation at 100 uM | 2009 | European journal of medicinal chemistry, Jun, Volume: 44, Issue:6 | Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase. |
| AID1235033 | Inhibition of mouse recombinant AChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents. |
| AID240779 | Inhibitory concentration against acetylcholinesterase | 2005 | Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11 | Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors. |
| 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. |
| AID1866876 | Inhibition of Electrophorus electricus AchE using acetylcholine iodide as substrate incubated for 10 mins followed by substrate addition measured at 0 to 180 secs by Ellman's method | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID1057004 | Inhibition of human recombinant MAO-A using p-tyramine as substrate assessed as formation of H2O2 at 100 uM preincubated for 15 mins under dark condition followed by substrate addition measured after 20 mins by fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID1075986 | Neuroprotective activity against Abeta1-42 peptide-induced neurotoxicity in rat C6 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1882053 | Inhibition of recombinant bovine mitochondrial MAO-B using benzylamine or serotonin as substrate incubated for 60 mins by fluorimetry assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID659697 | Inhibition of equine serum BuChE using butyrylcholine as substrate by Ellman's method | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids. |
| AID1057011 | Selectivity ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID765127 | Inhibition of horse serum BChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors. |
| AID1071755 | Hepatotoxicity in human HepG2 cells assessed as ALT level at 10 uM after 24 hrs (Rvb = 11.7 +/- 0.88 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1816809 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by DTNB-reagent based Ellman's method | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection. |
| AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1190807 | Inhibition of horse serum BuChE pre-incubated for 20 mins before butylthicoline iodide substrate addition by Ellman's assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD. |
| AID1653238 | Inhibition of electric eel AChE | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines. |
| AID1351151 | Cognition enhancing effect in ICR mouse model of scopalamine-induced memory impairment assessed as reversal of lowered spontaneous alteration at 20 umol equiv/kg, po pretreated for 30 mins followed by scopalamine treatment Y-maze test | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1592449 | Selectivity index, ratio of IC50 for human serum BChE to IC50 for human recombinant AChE | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. |
| AID315743 | Hepatotoxicity in Wistar rat serum assessed as lactate dehydrogenase level at 5.93 umol, ip after 12 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1077132 | Toxicity in Wistar rat assessed as total glutathione level in liver at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1378368 | Competitive inhibition of equine serum BuChE assessed as enzyme-inhibitor complex using p-nitrophenyl butyrate as substrate by Lineweaver-Burk plot analysis | 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. |
| 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). |
| AID412867 | Inhibition of BuChE from equine serum | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity. |
| AID1856387 | Solubility of the compound in PBS buffer incubated overnight at room temperature by HPLC based continuous shake-flask method | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8 | Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model. |
| AID1693559 | Inhibition of human BChE using butyrylthiocholineiodide as substrate incubated for 10 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1465115 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | 9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment. |
| AID1409660 | Hepatotoxicity in ICR mouse assessed as serum AST activity at 30 mg/kg, administered intragastrically measured 8 hrs post dose (Rvb = 120 +/- 20 U/L) | |||
| AID1542240 | Permeability of the compound at 30 to 50 uM at pH 7.4 measured up to 6 hrs by PAMPA-BBB assay method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| 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. |
| AID1335243 | Inhibition of human recombinant AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
| AID1738199 | Inhibition of equine BChE at 9 uM using acetylthiocholine as substrate measured for 0.5 to 1.5 mins by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation. |
| AID443743 | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
| AID1738200 | Inhibition of equine BChE at 0.9 uM using acetylthiocholine as substrate measured for 0.5 to 1.5 mins by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation. |
| AID1054514 | Inhibition of amyloid beta (1 to 42) aggregation (unknown origin) at 50 uM by thioflavin T fluorescence method | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer's disease. |
| AID462834 | Inhibition of equine serum BChE by Ellman's method | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus. |
| AID511767 | Antidementia against scopolamine-induced cognitive impairment in Swiss albino mouse assessed as improvement in latency to transfer from bright to dark compartment at 20 umol/kg, po by passive avoidance test | 2010 | Journal of medicinal chemistry, Sep-09, Volume: 53, Issue:17 | Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology. |
| AID1330801 | Cytotoxicity against human HepG2 cells assessed as cell viability at 5 uM after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID1240922 | Inhibition of electric eel AChE using ATC iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1184617 | Inhibition of electric eel AChE | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode. |
| AID1686243 | Toxicity in human HepG2 cells assessed as cell viability at 1000 uM by MTT assay relative to control | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID604025 | Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID469396 | Inhibition of BuChE in horse serum by Ellman method | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease. |
| AID480449 | Inhibition of equine serum BChE by modified Ellman's method | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID1174272 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | New tetracyclic tacrine analogs containing pyrano[2,3-c]pyrazole: efficient synthesis, biological assessment and docking simulation study. |
| AID1459904 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Novel tacrine-1,2,3-triazole hybrids: In vitro, in vivo biological evaluation and docking study of cholinesterase inhibitors. |
| 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. |
| AID480454 | Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release at 25 uM after 30 mins | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID1382564 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| AID1351126 | Cytotoxicity against rat PC12 cells assessed as inhibition of cell viability at 1 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1351125 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability at 50 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID302144 | Inhibition of human serum BuChE by Ellman's method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
| AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1190761 | Inhibition of human recombinant AchE using acetylthiocholine iodide as substrate by Ellman method | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Iminosugars as a new class of cholinesterase inhibitors. |
| AID118349 | Antagonistic activity against Scopolamine induced behavioral deficits in mice at dose 5.0 mg/kg sc | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID621449 | Inhibition of equine BuChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation. |
| AID1168965 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation at 500 uM after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | Discovery of 3-Arylcoumarin-tetracyclic Tacrine Hybrids as Multifunctional Agents against Parkinson's Disease. |
| AID1328981 | Hepatotoxicity in human HepG2 cells assessed as cell viability at 100 uM by MTT assay relative to control | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease. |
| 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. |
| 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. |
| AID480455 | Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release after 30 mins | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID491973 | Inhibition of human serum BChE by Ellman's reaction | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties. |
| AID696204 | Inhibition of Swiss albino mouse RBC AChE after 30 mins by Ellman method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Lead optimization studies towards the discovery of novel carbamates as potent AChE inhibitors for the potential treatment of Alzheimer's disease. |
| AID1486124 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, molecular docking, and biological activity of polyfluoroalkyl dihydroazolo[5,1-c][1,2,4]triazines as selective carboxylesterase inhibitors. |
| AID1704819 | Inhibition of human BuChE by spectrophotometric based Ellman's method | |||
| AID1184619 | Inhibition of equine serum BChE | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode. |
| AID1077134 | Toxicity in Wistar rat assessed as GSSG level in liver at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID612152 | Selectivity ratio of IC50 for BChE to IC50 for AChE | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors. |
| AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1632105 | Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP6 expressed in Escherichia coli NEB cells at 250 uM by surface plasmon resonance method | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). |
| AID1667718 | Inhibition of human AchE | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening. |
| AID629638 | Selectivity ratio of IC50 for Electrophorus electricus AChE to IC50 for equine serum BuChE | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues. |
| AID1193152 | Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID656040 | Inhibition of horse serum BChE by Ellman's method | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| 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. |
| AID1406257 | Antioxidant activity assessed as DPPH free radical scavenging activity after 90 mins dark incubation | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID229535 | Ratio of IC50 values obtained for BChE/ AChE | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID759422 | Inhibition of human AChE using acetylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Selective inhibition of human acetylcholinesterase by xanthine derivatives: in vitro inhibition and molecular modeling investigations. |
| AID265948 | Inhibition of human AChE | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites. |
| AID1311918 | Antioxidant activity assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition measured every min for 120 mins by ORAC-FL assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1330803 | Cytotoxicity against human HepG2 cells assessed as cell viability at 25 uM after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID238797 | Competitive inhibition constant for Acetylcholinesterase | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation. |
| AID170962 | Ameliorating effects on diazepam-induced memory impairment of passive avoidance response (no of rats) | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID666573 | Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1495953 | Agonist activity at human 5-HT1A receptor expressed in HEK293 cells after 60 mins by Eu-cAMP solution based ultra LANCE assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
| 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. |
| AID1057267 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and evaluation of novel 4-dimethylamine flavonoid derivatives as potential multi-functional anti-Alzheimer agents. |
| AID32103 | Inhibition of acetylcholinesterase (AChE) | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID282009 | Selectivity for human BChE over human AChE | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID603188 | Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate after 10 mins by Ellman's spectrophotometric method | 2011 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13 | New class of acetylcholinesterase inhibitors from the stem bark of Knema laurina and their structural insights. |
| AID1399488 | Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalent antioxidant capacity at 20 uM after 1 hr by UV/Vis spectrophotometric analysis | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics. |
| AID604021 | Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID349872 | Inhibition of human serum BChE by Ellman's method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1075992 | Inhibition of electric eel acetylcholinesterase type VI-S using acetylthiocholine iodide as substrate measured every 30s for 5 mins by Ellman's spectrophotometric method | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of 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. |
| AID1651629 | Inhibition of electric eel AchE using acetylthiocholine as substrate measured for 6 mins by Ellman's method | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Bioactive Azepine-Indole Alkaloids from |
| AID1578227 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| 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. |
| AID1389635 | Hepatotoxicity in ICR mouse assessed as serum ALT activity at 15 mg/kg, ig after 8 hrs (Rvb = 31.9 +/- 2.1 U/L) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
| AID282826 | Selectivity for human BChE over bovine AChE | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
| AID1866878 | Selectivity index, ratio of IC50 for equine serum BchE to IC50 for Electrophorus electricus AchE | 2022 | European journal of medicinal chemistry, Apr-15, Volume: 234 | Development of 5-hydroxyl-1-azabenzanthrone derivatives as dual binding site and selective acetylcholinesterase inhibitors. |
| AID1071753 | Hepatotoxicity in human HepG2 cells assessed as ALT level at 100 uM after 24 hrs (Rvb = 11.7 +/- 0.88 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1869216 | Cytotoxicity against human HL-60 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | |||
| AID1728646 | Cognitive enhancing effect in Sprague-Dawley rat model of amyloid beta (25 to 35) peptide-induced memory impairment assessed as time spent in target platform at 0.2 mg per 100 g, ip qd for 4 weeks administered via gavage and measured after 5 days by Morri | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID1635491 | Neuroprotective activity against H2O2-induced oxidative damage in human SH-SY5Y cells assessed as increase in cell viability at 20 uM incubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1317859 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 25 uM measured after 48 hrs by ThT-assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID692188 | Therapeutic index, ratio of Cmax in human to IC50 for human OCT2 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID658006 | Inhibition of amyloid beta (1 to 42) self-aggregation after 24 hrs by thioflavin T fluorescence method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID1503607 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID30868 | In vitro inhibition of electric eel acetylcholinesterase | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID552790 | Inhibition of bovine erythrocytes AChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Cholinergic and neuroprotective drugs for the treatment of Alzheimer and neuronal vascular diseases. II. Synthesis, biological assessment, and molecular modelling of new tacrine analogues from highly substituted 2-aminopyridine-3-carbonitriles. |
| AID1686241 | Toxicity in human HepG2 cells assessed as cell viability at 100 uM by MTT assay relative to control | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID1140640 | Inhibition of human recombinant AchE using acetylthiocholine iodide as substrate incubated for 5 mins prior to substrate addition measured after 5 mins by Ellman method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | New melatonin-N,N-dibenzyl(N-methyl)amine hybrids: potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID1771809 | Inhibition of BuChE in human plasma using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID1700051 | Inhibition of human serum BuChe by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation. |
| AID629589 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis, biological evaluation of 9-N-substituted berberine derivatives as multi-functional agents of antioxidant, inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID1209581 | Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
| AID690972 | Inhibition of HFIP pretreated AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin-T based fluorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID658005 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID1632108 | Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP6 expressed in Escherichia coli NEB cells at 200 uM in presence of taurocholate by surface plasmon resonance method | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). |
| AID1077133 | Toxicity in Wistar rat assessed as total glutathione level in liver at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1693558 | Inhibition of human recombinant AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate incubated for 10 mins by Ellman's method | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
| AID1201737 | Inhibition of horse serum BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease. |
| AID31964 | In vitro inhibitory effect on rat Acetylcholinesterase | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation. |
| AID1421882 | Inhibition of human AChE using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors. |
| AID716206 | Selectivity index, ratio of IC50 for electric eel AChE to horse BChE | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID552789 | Inhibition of Electrophorus electricus AChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Cholinergic and neuroprotective drugs for the treatment of Alzheimer and neuronal vascular diseases. II. Synthesis, biological assessment, and molecular modelling of new tacrine analogues from highly substituted 2-aminopyridine-3-carbonitriles. |
| AID1771842 | Inhibition of BuChE in human plasma using BTC as substrate at 10 uM preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method relative to control | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID1542236 | Cytotoxicity against human HepG2 cell assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID469397 | Inhibition of human AChE in erythrocyte | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease. |
| AID654685 | Selectivity ratio of IC50 for equine serum butyrylcholinesterase to IC50 for electric eel acetylcholinesterase | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Design, synthesis and evaluation of isaindigotone derivatives as dual inhibitors for acetylcholinesterase and amyloid beta aggregation. |
| AID725909 | Inhibition of AChE in Sprague-Dawley rat cortices using acetylthiocholine iodide as substrate by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
| AID604024 | Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID404439 | Inhibition of bovine 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. |
| AID184797 | Toxicity was evaluated in rats, after intraperitoneal administration;Value ranges from (10-20) | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID234643 | Selectivity at AChE and BChE | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID315734 | Inhibition of BuChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1077142 | Toxicity in ip dosed Wistar rat measured per 100 g body weight | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID30663 | Inhibition of activity against Torpedo Ray acetylcholinesterase. | 2001 | Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20 | A structure-based design approach to the development of novel, reversible AChE inhibitors. |
| 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. |
| AID1125767 | Inhibition of BuChE in equine serum using butyrylthiocholine iodide as substrate preincubated with enzyme for 10 mins prior to substrate challenge measured after 15 mins by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease. |
| AID491969 | Selectivity ratio of IC50 for bovine erythrocyte AChE to IC50 for human erythrocyte AChE | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties. |
| AID1279141 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID395327 | Dissociation constant, pKa by capillary electrophoresis | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID1352329 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Tetrahydroacridine derivatives with dichloronicotinic acid moiety as attractive, multipotent agents for Alzheimer's disease treatment. |
| AID1591865 | Selectivity ratio of IC50 for equine serum BuchE to IC50 for electric eel AchE | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids. |
| AID1077122 | Toxicity in Wistar rat assessed as ethoxyresorufin-O-deethylation activity in liver measured as resorufin level at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1486123 | Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, molecular docking, and biological activity of polyfluoroalkyl dihydroazolo[5,1-c][1,2,4]triazines as selective carboxylesterase inhibitors. |
| AID1271508 | Inhibition of HFIP pretreated Amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM incubated for 24 hrs by Thioflavin T-based fluorometric assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1195130 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins by Ellman method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Synthesis of new N-benzylpiperidine derivatives as cholinesterase inhibitors with β-amyloid anti-aggregation properties and beneficial effects on memory in vivo. |
| AID298279 | Inhibition of human recombinant butyrylcholinesterase | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease. |
| AID1738198 | Inhibition of electric eel AchE at 0.9 uM using acetylthiocholine as substrate measured for 0.5 to 1.5 mins by Ellman's method relative to control | 2020 | European journal of medicinal chemistry, Jul-15, Volume: 198 | New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation. |
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| AID1406255 | Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured for 1 min by Ellman's assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID539464 | Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
| AID569583 | Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors. |
| AID404428 | Inhibition of human recombinant 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. |
| AID1816811 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 2 mins by DTNB-reagent based Ellman's method | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Highly Potent and Selective Butyrylcholinesterase Inhibitors for Cognitive Improvement and Neuroprotection. |
| AID1480843 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity at 5 uM pretreated for 15 mins followed by APPH challenge measured every minute for 240 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| 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. |
| AID1564171 | Competitive inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate measured for 125 secs by Lineweaver-burk plot analysis | 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. |
| AID1542250 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 10 mins by spectrophotometry based Ellman's method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1335237 | Inhibition of electric eel AChE preincubated for 5 mins followed by acetylthiocholine iodide substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT |
| AID1882051 | Selectivity ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin) | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| 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. |
| AID1360335 | Inhibition of human BchE (unknown origin)-induced amyloid beta (1 to 42) aggregation at 10 uM after 48 hrs by thioflavin T fluorescence method relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| 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. |
| AID482862 | Displacement of propidium iodide from AChE in bovine erythrocytes at 1 uM after 15 mins by fluorescence plate reader | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1815195 | Ratio of IC50 for cytotoxicity against human HepG2 cells to ratio of IC50 for inhibition of rat cortex AChE | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1240924 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1545285 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID289395 | Inhibition of beta amyloid protein 1-42 aggregation by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID1138648 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured up to 1 hr by spectrophotometric analysis relative to control | 2014 | Journal of natural products, Apr-25, Volume: 77, Issue:4 | Biologically active dichapetalins from Dichapetalum gelonioides. |
| AID1486134 | Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalent antioxidant capacity after 1 hr by UV/Vis spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, molecular docking, and biological activity of polyfluoroalkyl dihydroazolo[5,1-c][1,2,4]triazines as selective carboxylesterase inhibitors. |
| AID31495 | Inhibition of Acetylcholinesterase in human red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID1168967 | Cytotoxicity against HEK293 cells assessed as inhibition of cell proliferation at 500 uM after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | Discovery of 3-Arylcoumarin-tetracyclic Tacrine Hybrids as Multifunctional Agents against Parkinson's Disease. |
| AID1317853 | Inhibition of equine serum BuChE preincubated for 5 mins followed by addition of butyrylthiocholine iodide as substrate measured after 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1468630 | Inhibition of human BChE using BTC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method | |||
| AID690969 | Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID230724 | Ratio of the IC50 values of BuChE and AcHe | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID274652 | Selectivity for human AChE over BuChE | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| AID1831863 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID265949 | Inhibition of human BuChE | 2006 | Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11 | Discovery of huperzine A-tacrine hybrids as potent inhibitors of human cholinesterases targeting their midgorge recognition sites. |
| AID349045 | Inhibition of human recombinant AChE | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity. |
| AID1450068 | Inhibition of recombinant human CYP3A4 expressed in insect cells using DBOMF as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1406256 | Selectivity ratio of IC50 for human AChE to IC50 for human BChE | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities. |
| AID1435904 | Permeability of the compound at 100 uM at pH 7.4 measured after 6 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID171712 | ED50/MED ratio | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID1631819 | Inhibition of equine BuChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16 | Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening. |
| AID1759908 | Inhibition of human GluN1a/GluN2B receptor expressed in HEK293 cells assessed as relative inhibition of glycine/glutamate-induced current measured at +40 mV holding potential by whole-cell patch clamp method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
| AID1468646 | Displacement of [3H]-CP55950 from human CB1 receptor expressed in CHO cell membranes after 3 hrs by scintillation counting method | |||
| AID235837 | Safety index is the ratio of acute lethality LD50 to extracellular AchE ED50. | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID256692 | Inhibitory activity AChE from Electrophorus electricus using ATCh substrate and DTNB by spectrophotometry | 2005 | Journal of medicinal chemistry, Dec-29, Volume: 48, Issue:26 | Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition. |
| AID175557 | Effect after an intraperitoneal dose of 0.3 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
| AID1846082 | Inhibition of electric eel AChE preincubated for 15 mins followed by substrate addition using acetylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Apr-05, Volume: 215 | A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease. |
| AID517226 | Selectivity index, ratio of IC50 for human plasmatic BChE to IC50 for human recombinant AChE | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20 | Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease. |
| AID272367 | Inhibition of human serum BChE | 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. |
| AID1271548 | Cognition improving effect in scopolamine-induced ICR mouse memory impairment model assessed as escape latency at 20 umol/kg, po qd pretreated for 30 mins measured 30 mins post scopolamine challenge measured on day 5 by Morris water maze test | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID692195 | Inhibition of human MATE1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID1682163 | Inhibition of rat cortex homogenate BuChE by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1466563 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis | |||
| AID1810376 | Inhibition of human recombinant GSK-3beta using prephosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by Kinase-Glo luminescence assay | |||
| AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1416887 | Inhibition of electric eel AChE at 100 uM after 15 mins by DTNB reagent based assay relative to control | 2018 | MedChemComm, Jan-01, Volume: 9, Issue:1 | Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors. |
| AID1686234 | Inhibition of Electrophorus electricus AChE pre-incubated for 10 mins before addition of acetylthiocholine iodide substrate and further incubated for 15 mins by Ellman's method | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID1257000 | Reversible inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholineiodide as substrate assessed as enzyme recovery at 52 uM incubated for 30 mins by Ellman's colorimetric assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents. |
| 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. |
| AID604020 | Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID1632104 | Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP6 expressed in Escherichia coli NEB cells by surface plasmon resonance method | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). |
| AID314093 | Inhibition of human AchE-induced amyloid beta aggregation at 100 uM | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Multi-target-directed ligands to combat neurodegenerative diseases. |
| AID1193154 | Selectivity index, ratio of IC50 for BuChE in horse serum to IC50 for Electrophorus electricus AChE | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID1167622 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins by spectrophotometric method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID44423 | Inhibition of Butyrylcholinesterase (BChE) of human erythrocytes [-log IC50 (uM)] | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease. |
| AID716202 | Inhibition of electric eel AChE by colorimetric Ellman assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1435919 | Cytotoxicity against human primary hepatocytes assessed as cell viability at 100 uM measured after 2 hrs by trypan blue assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID1311914 | Inhibition of electric eel ACHE preincubated for 6 mins followed by addition of acetylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID654176 | Inhibition of human recombinant AChE-induced Abeta1-40 aggregation at 100 uM by thioflavin T fluorescence method | 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. |
| AID349883 | Inhibition of amyloid beta (1-42) self-aggregation at 50 uM after 24 hrs by thioflavin T fluorescence method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1635483 | Inhibition of human erythrocyte AChE using ATCI as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by Ellman assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID482861 | Displacement of propidium iodide from AChE in bovine erythrocytes after 15 mins by fluorescence plate reader | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID1167542 | Selectivity ratio of IC50 for equine BChE to IC50 for electric eel AChE | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1351130 | Cytotoxicity against human HL7702 cells assessed as reduction in cell viability at 10 uM by MTT assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1055216 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID197592 | Inhibition of circling behavior, percentage of control was reported | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID31627 | Inhibition against Acetylcholinesterase (AChE) | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors. |
| AID600978 | Inhibition of human erythrocytes AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID407147 | Inhibition of equine serum BuchE | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13 | Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID744314 | Inhibition of acetylcholinesterase (unknown origin)-induced amyloid beta(1 to 42) aggregation at 25 uM after 48 hrs by ThT fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID44422 | Inhibitory concentration against butyrylcholinesterase from human serum | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine. |
| AID1351131 | Induction of apoptosis in human HL7702 cells at 10 uM by FITC staining based flow cytometry relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1888431 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
| AID1077121 | Toxicity in Wistar rat assessed as brain weight at 1 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID716440 | Hepatotoxicity against Wistar rat assessed as increase in tissue content of oxidised glutathione at 6 uM/100 gram of body weight, ip after 24 hrs | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1338124 | Permeability of the compound at 100 uM up to 6 hrs by PAMPA | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID656049 | Inhibition of human recombinant BChE using panvera peptide as substrate at 10 uM preincubated for 60 mins before substrate addition by FRET assay | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID759421 | Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate treated 5 mins before substrate addition measured up to 4 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Selective inhibition of human acetylcholinesterase by xanthine derivatives: in vitro inhibition and molecular modeling investigations. |
| AID1379223 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID1631830 | Inhibition of electric eel AChE using ACTI as substrate preincubated for 29 mins followed by substrate addition measured at 1 min intervals for 10 mins by Ellman's assay | 2016 | Journal of medicinal chemistry, 08-25, Volume: 59, Issue:16 | Discovery and Structure-Activity Relationships of a Highly Selective Butyrylcholinesterase Inhibitor by Structure-Based Virtual Screening. |
| AID443746 | Inhibition of human recombinant AChE expressed in HEK293 cells by photometry | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
| AID1810883 | Antioxidant activity of compound assessed as trolox equivalent of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every 2 mins for 90 mins by ORAC fluorescein assay | |||
| AID654181 | Inhibition of human recombinant BACE-1 using M-2420 as substrate at 5 uM preincubated for 1 hr prior substrate addition measured after 15 mins by spectrofluorimetry | 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. |
| AID612150 | Inhibition of AChE by Ellman's method | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors. |
| AID1310670 | Neurotoxicity in human SH-SY5Y cells assessed as cell viability at 50 uM after 24 hrs by XTT assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Potent anticholinesterasic and neuroprotective pyranotacrines as inhibitors of beta-amyloid aggregation, oxidative stress and tau-phosphorylation for Alzheimer's disease. |
| AID1330795 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID1869217 | Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | |||
| AID137448 | Reversal of scopolamine-induced memory impairment in mice, after subcutaneous administration of 0.63 mg/kg | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | (+/-)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity. |
| AID27167 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| 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. |
| AID1240932 | Inhibition of acetylcholinesterase in human erythrocytes using acetylthiocholine iodide substrate by spectrophotometric Ellman's method | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1153518 | Inhibition of BChE in horse serum using butyrylthiocholine iodide as substrate after 120 mins by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13 | Preparation, anticholinesterase activity and molecular docking of new lupane derivatives. |
| AID1564162 | Inhibition of electric eel AChE assessed as dissociation constant for enzyme-inhibitor complex using acetylthiocholine iodide as substrate measured for 125 secs 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. |
| AID1635493 | Antioxidant activity assessed as DPPH free radical scavenging activity at 20 uM after 30 secs by spectrophotometry | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1077129 | Toxicity in Wistar rat assessed as protein content in liver at 1 umol/100 g body weight, ip by Biuret method relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID491968 | Antioxidant activity against AAPH-induced peroxyl radicals assessed as trolox equivalents measured for 80 mins by ORAC-FL method | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties. |
| AID134237 | Acute toxicity in mice was determined after oral administration | 1988 | Journal of medicinal chemistry, Jul, Volume: 31, Issue:7 | (+/-)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity. |
| AID752021 | Inhibition of electric eel AChE preincubated for 30 mins prior to horseradish peroxidase, H2O2 and DETAPAC addition measured for 20 mins under ROS condition by Muraoka and Miura method | 2013 | Bioorganic & medicinal chemistry, Jun-15, Volume: 21, Issue:12 | Investigation of the role of linker moieties in bifunctional tacrine hybrids. |
| AID1297713 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1501658 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by UV-Vis spectrophotometric analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID31775 | Inhibition of acetylcholinesterase (AChE) of human erythrocytes | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease. |
| AID1271527 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 10 uM after 48 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID289394 | Selectivity for human BChE over Electrophorus electricus AchE | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID1071760 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 300 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1542235 | Selectivity index, ratio of IC50 of recombinant human AChE to IC50 of human serum BChE | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1592448 | Inhibition of human serum BChE using BTCh as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. |
| AID1324829 | Selectivity index, ratio of IC50 for horse serum BChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents. |
| AID629635 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 10 mins before substrate addition by Ellman's method | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues. |
| AID1439218 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | New tacrine-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates. |
| AID714539 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 0.01 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1856383 | Inhibition of human BChE using butyrylthiocholineiodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 sec for 3 mins by DTNB-based UV analysis | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8 | Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model. |
| AID1495954 | Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 20 mins by by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
| AID1704818 | Inhibition of recombinant human AChE using ATCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method | |||
| AID663255 | Hepatotoxicity in Sprague-Dawley rat assessed increase in alanine aminotransferase level in serum at 6 umol/100g of body weight, ip after 36 hrs | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID8002 | Observed volume of distribution | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
| AID480448 | Inhibition of electric eel AChE by modified Ellman's method | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
| AID1382573 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by addition of substrate measured after 5 mins | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Novel Tacrine-Hydroxyphenylbenzimidazole hybrids as potential multitarget drug candidates for Alzheimer's disease. |
| AID1332149 | Inhibition of human recombinant BuChe using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents. |
| AID1152331 | Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate by spectrophotometer analysis | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Novel aromatic-polyamine conjugates as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. |
| AID1437807 | Hepatotoxicity against human HepG2 cells assessed as decrease in cell viability at 50 uM after 24 hrs by MTT assay 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. |
| AID1330748 | Inhibition of equine serum BuChE using s-butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID139927 | Percent change in brain Acetylcholine content in the mouse brain using GC/MS methodology. | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1570268 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition measured after 6 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships. |
| AID1739253 | Inhibition of AChE (unknown origin) preincubated for 30 mins followed by substrate addition acetylthiocholineiodide measured after 40 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Aug-15, Volume: 200 | Simple analogues of natural product chelerythrine: Discovery of a novel anticholinesterase 2-phenylisoquinolin-2-ium scaffold with excellent potency against acetylcholinesterase. |
| AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID716430 | Hepatotoxicity against human HSC cells assessed as reduction in cell number at 75 uM after 24 hrs by fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1635489 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 80 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1311921 | Selectivity index, ratio of IC50 for human serum BCHE to IC50 for human erythrocyte ACHE | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID482854 | Inhibition of equine serum BuChE by Ellman's method | 2010 | Journal of medicinal chemistry, Jul-22, Volume: 53, Issue:14 | Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1700048 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human erythrocytes AChE | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Novel deoxyvasicinone and tetrahydro-beta-carboline hybrids as inhibitors of acetylcholinesterase and amyloid beta aggregation. |
| AID1624339 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2019 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 29, Issue:6 | Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity. |
| 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. |
| AID1503611 | Inhibition of amyloid beta 42 (unknown origin) self aggregation at 50 uM after 24 hrs by thioflavin T-based fluorometric assay relative to control | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID1164690 | Inhibition of recombinant human BChE by Ellman method | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. |
| AID1545271 | Inhibition of human 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). |
| AID1810411 | Antialzheimer activity against scopolamine-induced ICR mouse model of memory impairment assessed as improved memory and cognition by measuring escape latency time at 15 mg/kg, ip treated with scopolamine for 10 days followed by compound addition for 15 da | |||
| AID1564173 | Inhibition of human serum BuChe 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. |
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| AID694075 | Selectivity ratio of Ki for human recombinant BChE to Ki for human recombinant AChE | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase. |
| AID639366 | Inhibition of AChE in bovine erythrocytes using acetylthiocholine as substrate by Ellman method | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease. |
| AID1686239 | Antioxidant activity assessed as AAPH radical scavenging activity incubated for 15 mins by ORAC-FL method relative to Trolox | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID517222 | Inhibition of human recombinant AChE after 5 mins | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20 | Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease. |
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| AID184454 | Acute toxicity in rat by peroral administration | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID707700 | Inhibition of human recombinant GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1578224 | Antagonist activity at histamine H3 receptor (unknown origin) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1682335 | Inhibition of rat cortex homogenate acetylcholinesterase by spectrophotometric method | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1468635 | Inhibition of human erythrocyte AChE using ATC iodide as substrate preincubated for 4.5 mins followed by substrate addition measured after 2.5 mins by Ellman's method | |||
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| AID1236872 | Inhibition of human recombinant BACE1 using M-2420 as substrate up to 5 uM preincubated with enzyme for 1 hr by FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14 | From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold. |
| AID1815197 | Ratio of IC50 for Inhibition of hERG (unknown origin) expressed in CHO-K1 cells to ratio of IC50 for Inhibition of rat cortex AChE | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID726766 | Non-competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method | 2013 | Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5 | Acetylcholinesterase immobilized capillary reactors-tandem mass spectrometry: an on-flow tool for ligand screening. |
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| AID629645 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 3 uM after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues. |
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| AID1416239 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM by MTT assay relative to control | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | 5-Methyl- |
| AID716445 | Antiamnesic activity against scopolamine-induced cognitive impairment in Wistar rat assessed as reduction in number of error made at 2 umol/100 g body weight after 20 to 120 mins by eight arm radial maze test | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID716433 | Hepatotoxicity against human HSC cells assessed as mitochondrial swelling at 25 uM after 24 hrs by fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
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| AID1271502 | Cognition improving effect in scopolamine-induced ICR mouse memory impairment model assessed as improvement in pathlength in target quadrant at 20 umol/kg, po qd pretreated for 30 mins measured 30 mins post scopolamine challenge measured on day 6 by Morri | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID282008 | Inhibition of human recombinant BChE | 2004 | Journal of medicinal chemistry, Dec-16, Volume: 47, Issue:26 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties. |
| AID1480848 | Inhibition of human serum BuChE at 5 uM using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1711761 | Inhibition of electric eel AchE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID350220 | Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
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| AID714535 | Cytotoxicity against human HepG2 cells assessed as cell viability at 30 uM after 24 hrs by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
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| AID341424 | Inhibition of self-induced Abeta (1 to 42) aggregation at 10 uM thioflavin T-based fluorescence assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush. |
| AID1400877 | Induction of necrosis in human MDA-MB-231 cells at 2 uM after 24 hrs by acridine orange/ethidium bromide staining-based flow cytometric method | 2017 | MedChemComm, Apr-01, Volume: 8, Issue:4 | Design and synthesis of cenocladamide analogues and their evaluation against breast cancer cell lines. |
| AID589212 | Mechanism based inhibition of human cytochrome P450 1A2 measured by 7-ethoxyresorufin O-deethylation (EROD) | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
| AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1186578 | Inhibition of human AChE assessed as acetylthiocholine hydrolysis | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase. |
| AID241692 | Inhibitory concentration against human erythrocyte Acetylcholinesterase | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. |
| AID1768736 | Antioxidant activity assessed as hydroxyl radical scavenging activity | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1382551 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 0.1 mM measured after 4 days by atomic force microscopic method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
| AID1271511 | Inhibition of recombinant human AChE assessed as reduction in AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by thioflavin T fluorescence-based fluorimetric method relative to control | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1071756 | Hepatotoxicity in human HepG2 cells assessed as ALT level at 30 uM after 24 hrs (Rvb = 11.7 +/- 0.88 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID111987 | Reversal of scopolamine-induced memory impairment in mice at 5 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| 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. |
| AID1077128 | Toxicity in Wistar rat assessed as protein content in liver at 6 umol/100 g body weight, ip by Biuret method relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1351133 | Hepatotoxicity in Kunming mouse assessed as cellular edema in liver at 35 mg/kg, ig after 48 hrs by H and E staining based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID754041 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease. |
| AID1271530 | Cognition improving effect in scopolamine-induced ICR mouse memory impairment model assessed as escape latency at 20 umol/kg, po qd pretreated for 30 mins measured 30 mins post scopolamine challenge measured on day 1 by Morris water maze test | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1503610 | Selectivity index, ratio of IC50 for human serum AChE to IC50 for human serum BChE | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
| AID44284 | Concentration required to inhibit 50% of Butyrylcholinesterase obtained from human serum was determined in vitro | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors. |
| AID620402 | Selectivity ratio of IC50 for equine serum BChE to IC50 for Electrophorus electricus AChE | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. |
| AID181681 | Inhibition of serotonin reuptake in rat whole brains without cerebellum | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1831866 | Antineuroinflammatory activity in mouse BV-2 cells assessed as suppression of LPS-induced TNF-alpha mRNA expression at 0.1 uM preincubated for 24 hrs followed by LPS stimulation and measured after 24 hrs by RT-PCR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| 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. |
| AID1435901 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine iodide as substrate pretreated for 5 mins followed by substrate addition measured after 5 mins by spectrophotometry based Ellman method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID1439217 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method | 2017 | European journal of medicinal chemistry, Mar-10, Volume: 128 | New tacrine-derived AChE/BuChE inhibitors: Synthesis and biological evaluation of 5-amino-2-phenyl-4H-pyrano[2,3-b]quinoline-3-carboxylates. |
| AID1545288 | Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine as substrate incubated for 20 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). |
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| AID462839 | Inhibition of Electrophorus electricus AChE-induced amyloid beta (1-40) aggregation at 25 uM by thioflavin T fluorescence assay | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus. |
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| AID1886722 | Inhibition of horse serum BChE using acetylthiocholine iodide or butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | |||
| AID123386 | Effect on brain acetylcholine concentration in mice after intraperitoneal administration of 80% lethal dose (20 mg/kg) | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
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| AID629590 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis, biological evaluation of 9-N-substituted berberine derivatives as multi-functional agents of antioxidant, inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID692194 | Inhibition of human OCT1 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
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| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID44306 | Ratio of inhibitory activity against acetylcholinesterase (AChE) to that of butyrylcholinesterase (BChE) | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Synthesis and structure-activity relationships of open D-Ring galanthamine analogues. |
| AID1578226 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Search for new multi-target compounds against Alzheimer's disease among histamine H |
| AID1873185 | Inhibition of AChE (unknown origin) using S-Acetylthiocholine iodide as substrate at 50 mg/ml incubated for 1 hr by Ellman's method relative to control | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Occurrence, synthesis and biological activity of 2-(2-phenyethyl)chromones. |
| AID282831 | Inhibition of beta amyloid protein 40 aggregation at 100 uM by thioflavin T-based fluorometric assay | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
| AID658004 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID1201749 | Inhibition of human BuChE using S-butyrylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease. |
| AID289392 | Inhibition of human BChE by Ellman's method | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| 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 |
| AID1450067 | Inhibition of recombinant human CYP1A2 expressed in insect cells using EOMCC as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1267380 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents. |
| AID1071758 | Hepatotoxicity in human HepG2 cells assessed as AST level at 30 uM after 24 hrs (Rvb = 50.3 +/- 2.90 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
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| AID412872 | Hepatotoxicity in Wistar rat liver assessed as serum albumin level after 24 to 36 hrs | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity. |
| AID1077113 | Toxicity in Wistar rat assessed as lipidperoxidation product level in brain at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1077135 | Toxicity in Wistar rat assessed as GSSG level in liver at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1768734 | Inhibition of equine serum BuChE by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID663256 | Hepatotoxicity in Sprague-Dawley rat assessed increase in aminotransferase level in serum at 6 umol/100g of body weight, ip after 3 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
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| AID663243 | Neuroprotective activity in Sprague-Dawley rat hippocampal CA1 region assessed as enhancement of high frequency stimulation-induced long-term potentiation by measuring field excitatory postsynaptic potentials incubated for 5 mins prior to HFS-induction me | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID31781 | Inhibitory activity against acetylcholinesterase | 1995 | Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24 | Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. |
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| AID1379220 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID714723 | Neuroprotective activity in 20 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as increase in cell viability after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1241463 | Inhibition of human NR1-1a/NR2B expressed in mouse L13-E6 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders. |
| AID1853195 | Inhibition of human acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12 | Pyrazolines as potential anti-Alzheimer's agents: DFT, molecular docking, enzyme inhibition and pharmacokinetic studies. |
| AID600979 | Inhibition of human plasma AChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
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| AID714543 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 5 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1542238 | Toxicity in mouse neuronal cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
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| AID227159 | Drug concentration that reaches 50% of antagonism index (AI). | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease. |
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| AID537384 | Inhibition of Electrophorus electricus AChE after 120 secs by Ellman spectroscopic method | 2010 | Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22 | 4-Phenylcoumarins from Mesua elegans with acetylcholinesterase inhibitory activity. |
| AID1071759 | Hepatotoxicity in human HepG2 cells assessed as AST level at 10 uM after 24 hrs (Rvb = 50.3 +/- 2.90 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| 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. |
| AID1558576 | Inhibition of human AChE | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID1815194 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID716210 | Neurotoxicity in mouse hippocampal HT22 cells assessed as cell viability at 50 uM after 24 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1399480 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 10 mins followed by substrate addition by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16 | Synthesis, molecular docking, and biological activity of 2-vinyl chromones: Toward selective butyrylcholinesterase inhibitors for potential Alzheimer's disease therapeutics. |
| AID1077131 | Toxicity in Wistar rat assessed as lipidperoxidation product level in liver at 1 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1389638 | Hepatotoxicity in ICR mouse assessed as serum AST activity at 15 mg/kg, ig after 8 hrs (Rvb = 96.5 +/- 9.3 U/L) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
| AID1075988 | Neuroprotective activity against H2O2-induced oxidative stress in mouse/rat NG108-15 cells assessed as cell viability at 100 uM incubated for 2 hrs prior to H2O2 challenge for 2 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1271537 | Hepatotoxicity in ICR mouse assessed as serum aspartate aminotransferase level at 30 mg/kg, ig after 8 hrs by spectrophotometry analysis (Rvb = 113.3 +/- 30 U/L) | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1198123 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID648660 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for Electrophorus electricus AChE | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Novel oxoisoaporphine-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1351120 | Inhibition of equine serum BuChE at 100 nM using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every minute by Ellman's method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1810881 | Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition by Ellman's method | |||
| AID1071762 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID404845 | Inhibition of rat cortex AChE | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID716439 | Hepatotoxicity against Wistar rat assessed as increase in tissue content of oxidised glutathione at 2 uM/100 gram of body weight after 24 hrs | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1882049 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID272364 | Inhibition of human 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. |
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| AID1917490 | Inhibition of equine serum BuChE using S-butyrylthiocholine as substrate at by DTNB reagent based spectrophotometric analysis | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Isatoic anhydrides as novel inhibitors of monoamine oxidase. |
| AID1882052 | Inhibition of recombinant bovine mitochondrial MAO-A using benzylamine or serotonin as substrate incubated for 60 mins by fluorimetry assay | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID1653243 | Inhibition of BuChE (unknown origin) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines. |
| AID1140645 | Displacement of propidium iodide from AchE in bovine erythrocytes at 3 uM after 15 mins by fluorescence microplate reader analysis | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | New melatonin-N,N-dibenzyl(N-methyl)amine hybrids: potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
| AID30692 | Inhibition of acetylcholinesterase (AChE)activity in bovine erythrocytes | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease. |
| AID1352330 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Tetrahydroacridine derivatives with dichloronicotinic acid moiety as attractive, multipotent agents for Alzheimer's disease treatment. |
| AID232649 | Ratio of inhibitory activity of ocmpound towards acetylcholinesterase from human erythrocytes over acetylcholinesterase from human serum | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID190325 | LD50/MED ratio | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID1201748 | Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease. |
| AID1077103 | Toxicity in Wistar rat assessed as lipidperoxidation product level in kidney at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID635890 | Inhibition of human AChE-induced amyloid beta (1 to 40) aggregation | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's di |
| AID1127132 | Inhibition of human erythrocyte AChE | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase. |
| AID1558582 | Inhibition of HFIP-pretreated amyloid beta (1 to 42 residues) (unknown origin) self aggregation at 50 uM incubated for 24 hrs by thioflavin F fluorescence method relative to control | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID1379230 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition measured every 2 mins for 20 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation. |
| AID694780 | Inhibition of electric eel AChE using acetylthiocholine chloride substrate incubated for 5 mins before substrate addition measured at 3 min interval by Ellman method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca²⁺ overload. |
| AID315736 | Vasorelaxation activity in PGF2-alpha-precontracted pig pulmonary artery | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID663979 | Selectivity ratio of IC50 for Equus caballus BChE to IC50 for electric eel AChE | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and pharmacological assessment of diversely substituted pyrazolo[3,4-b]quinoline, and benzo[b]pyrazolo[4,3-g][1,8]naphthyridine derivatives. |
| AID1271528 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 30 uM after 48 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1466565 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | |||
| AID1666038 | Improvement in cognition in ICR mouse model of scopolamine-induced cognition-impairment assessed as escape latency time at 15 mg/kg, po dosed 30 mins before scopolamine challenge for 10 days by Morris water maze test (Rvb = 37.5 secs) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Discovery and Biological Evaluation of a Novel Highly Potent Selective Butyrylcholinsterase Inhibitor. |
| AID141669 | Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the presence of Zn | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID366582 | Neuroprotective effect against human SH-SY5Y cells assessed as extracellular LDH release at 0.3 uM after 24 hrs in presence of 60 uM H2O2 | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID754043 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease. |
| AID1167540 | Inhibition of electric eel AChE preincubated for 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1678497 | Permeability of the compound on PBS buffer pH 7.4 at 100 uM by PAMPA-BBB assay | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | α-Linolenic Acid-Valproic Acid Conjugates: Toward Single-Molecule Polypharmacology for Multiple Sclerosis. |
| AID781328 | pKa (acid-base dissociation constant) as determined by Luan ref: Pharm. Res. 2005 | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| 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. |
| AID656039 | Inhibition of bovine erythrocytes AChE by Ellman's method | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID751999 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease. |
| AID30659 | Inhibition of Acetylcholinesterase in monkey red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID1272539 | Cytotoxicity against rat PC12 cells at 10 uM after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities. |
| AID1667724 | Inhibition of equine BuchE using butyrylthiocholine as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening. |
| AID1632106 | Binding affinity to recombinant human N-terminal His6 and Avi-tagged FABP1 expressed in Escherichia coli NEB cells by surface plasmon resonance method | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Identification and Investigation of Novel Binding Fragments in the Fatty Acid Binding Protein 6 (FABP6). |
| AID298278 | Inhibition of human recombinant acetylcholinesterase | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease. |
| AID1143497 | Inhibition of electric eel acetylcholinesterase type VI-S using acetylthiocholine iodide as substrate preincubated for 35 mins followed by enzyme addition measured after 3 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity. Investigation of AChE-ligand interactions by docking calculations and molecular dynamics simulations. |
| AID1351136 | Hepatotoxicity in Kunming mouse assessed as inflammatory cell infiltration in liver at 35 mg/kg, ig after 48 hrs by H and E staining based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1125768 | Selectivity ratio of IC50 for BuChE in equine serum to IC50 for electric eel AChE | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease. |
| AID1869221 | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells incubated for 24 hrs by Griess reagent assay | |||
| 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. |
| AID1651261 | Selectivity index, ratio of IC50 for equine serum BChE using butyrylthiocholine as substrate by Ellman's method to IC50 for electric eel AChE using acetylthiocholine as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis and anti-Alzheimer's disease activity study of xanthone derivatives based on multi-target strategy. |
| AID1465117 | Antioxidant activity assessed as ABTS radical cation scavenging activity by measuring trolox equivalents at 20 uM after 1 hr by UV/Vis spectrophotometric method-based ABTS radical cation decolorization assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | 9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment. |
| AID229811 | Ratio of Ki of [3H]NMS binding to that of [3H]-OXO-M binding. | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1071765 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 3 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1070082 | Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1611459 | Inhibition of BChE (unknown origin) incubated for 10 mins by Ellman's method | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24 | Discovery of potent and selective butyrylcholinesterase inhibitors through the use of pharmacophore-based screening. |
| AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
| AID1653683 | Antialzheimer activity against scopolamine-induced cognition impairment ICR mouse model assessed as mean escape latency time at 20 umol/kg, po treated 30 mins prior to scopolamine challenge and measured at 30 mins post-scopolamine challenge for 4 days of | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis, in vitro and in vivo biological evaluation of novel graveolinine derivatives as potential anti-Alzheimer agents. |
| AID106806 | Inhibition of malate dehydrogenase (MDH) at 400 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID694781 | Inhibition of equine serum BuChE using butyrylthiocholine chloride substrate incubated for 5 mins before substrate addition measured at 3 min interval by Ellman method | 2012 | Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21 | Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca²⁺ overload. |
| AID526834 | Selectivity ratio of IC50 for equine BChE to IC50 for electric eel AChE | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase. |
| AID1663426 | Antialzheimer activity in scopolamine-induced impairment in ICR mouse assessed as total entries at 15 mg/kg, ip administered once a day for 10 days pretreated with scopolamine for 30 mins and measured at 5th day of training session by Morris water maze te | 2020 | Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12 | Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity. |
| AID302143 | Inhibition of Electrophorus electricus AChE by Ellman's method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
| AID747766 | Induction of nitrite release in phosphate buffer at pH 7.4 at 10'-4 M after 4 hrs by Griess method | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. |
| 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. |
| AID707699 | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| AID1164693 | Selectivity ratio of IC50 for recombinant mouse AChE to IC50 for recombinant human BChE | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. |
| AID232238 | Selectivity was defined as the ratio between M2-IC50/M1-IC50 | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID747765 | Vasorelaxant activity against norepinephrine-induced contraction in rat aortic rings at 100 uM | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. |
| AID247942 | Inhibitory concentration against amyloid-beta aggregation; Not active | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation. |
| AID663253 | Hepatotoxicity in Sprague-Dawley rat assessed increase in alanine aminotransferase level in serum at 6 umol/100g of body weight, ip after 24 hrs | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID350218 | Octanol-water partition coefficient, log PC of the compound | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
| AID692192 | Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID1328954 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease. |
| AID1351147 | Cognition enhancing effect in ICR mouse model of scopalamine-induced memory impairment assessed as mean escape latency time at 20 umol equiv/kg, po pretreated for 30 mins followed by scopalamine treatment measured on 4 th day of training trial session by | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1057266 | Inhibition of equine serum BChE using butylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and evaluation of novel 4-dimethylamine flavonoid derivatives as potential multi-functional anti-Alzheimer agents. |
| AID1330796 | Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition measured for 1 min by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID654190 | Selectivity ratio of IC50 for human recombinant AChE to IC50 for human serum BChE | 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. |
| AID776474 | Hepatotoxicity in ICR mouse assessed as increase in serum ASAT level at 11.86 umol/100 g, id measured at 8 to 30 hrs | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease. |
| AID1382560 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| 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. |
| AID404842 | Inhibition of bovine erythrocyte AChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID315745 | Hepatotoxicity in Wistar rat serum assessed as lactate dehydrogenase level at 5.93 umol, ip after 36 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1236869 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins prior to substrate addition by Ellman's method | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14 | From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold. |
| AID31035 | Concentration required to inhibit 50% of Acetylcholinesterase obtained from human erythrocytes was determined in vitro | 1995 | Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7 | Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors. |
| AID716434 | Hepatotoxicity against human HSC cells assessed as mitochondrial swelling at 50 uM after 24 hrs by fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1450071 | Inhibition of recombinant human CYP1A2 expressed in insect cells at 20 uM using EOMCC as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1696522 | Inhibition of Sprague-Dawley rat acetylcholinesterase using acetylthiocholine iodide as substrate measured at 30 secs for 5 mins by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Isolation, reactivity, pharmacological activities and total synthesis of hispanolone and structurally related diterpenes from Labiatae plants. |
| AID654175 | Inhibition of human serum BChE using butyrylthiocholine 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. |
| AID1330752 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1627646 | Inhibition of equine serum BChE using butyrylthiocholine chloride as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
| AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
| AID1882050 | Inhibition of BuChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 5 mins by Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID257809 | Selectivity for human AChE over human BuChE | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
| AID600120 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate by spectroscopic Ellmans method | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation. |
| AID315737 | Hepatotoxicity in Wistar rat serum assessed as aspartate aminotransferase level at 5.93 umol, ip after 12 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1292252 | Inhibition of AChE (unknown origin) using acetylcholine iodate as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID1324824 | Inhibition of electric eel AChE using ATC as substrate preincubated for 15 mins followed by substrate addition by UV-spectrophotometric analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents. |
| AID771357 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, docking study and biological evaluation of some novel tetrahydrochromeno [3',4':5,6]pyrano[2,3-b]quinolin-6(7H)-one derivatives against acetyl- and butyrylcholinesterase. |
| AID477065 | inhibition of equine serum BuChE by Ellman's method | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors. |
| AID1389640 | Hepatotoxicity in ICR mouse assessed as serum AST activity at 15 mg/kg, ig after 36 hrs (Rvb = 85.0 +/- 7.2 U/L) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
| AID1077105 | Toxicity in Wistar rat assessed as total glutathione level in kidney at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
| AID1762425 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1054517 | Inhibition of human recombinant AChE by Ellman's assay | 2013 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 23, Issue:23 | Quinones bearing non-steroidal anti-inflammatory fragments as multitarget ligands for Alzheimer's disease. |
| AID31969 | In vitro inhibition of acetylcholinesterase, isolated from rat brain. | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. |
| AID1310668 | Neurotoxicity in human SH-SY5Y cells assessed as cell viability at 10 uM after 24 hrs by XTT assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Potent anticholinesterasic and neuroprotective pyranotacrines as inhibitors of beta-amyloid aggregation, oxidative stress and tau-phosphorylation for Alzheimer's disease. |
| AID1058685 | Inhibition of human 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. |
| AID1297712 | Inhibition of equine serum BuChE using butylthiocholine chloride as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1057013 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman method | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
| AID1201736 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman method | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease. |
| AID1167544 | Mixed-type inhibition of human erythrocyte AChE by Lineweaver-Burk reciprocal plot method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID1198136 | Hepatotoxicity in Sprague-Dawley rat assessed as increase in inflammatory cells in portal fields at 6 umol/100g body weight, ip measured after 24 hrs by histomorphological study | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID1815190 | Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| AID1831867 | Antineuroinflammatory activity in mouse BV-2 cells assessed as suppression of LPS-induced IL-1beta mRNA expression at 0.1 uM preincubated for 24 hrs followed by LPS stimulation and measured after 24 hrs by RT-PCR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID1437806 | Hepatotoxicity against human HepG2 cells assessed as decrease in cell viability at 5 uM after 24 hrs by MTT assay 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. |
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| AID112003 | Antagonistic activity against Scopolamine induced behavioral deficits in mice; 3/6 | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
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| AID117242 | Toxicity was evaluated in mice, after intraperitoneal administration | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
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| AID1435905 | Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation at 0.1 to 1 uM measured as trolox equivalent preincubated for 15 mins followed by AAPH addition measured evey 60 secs for 60 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID716437 | Hepatotoxicity against Wistar rat assessed as liver cell apoptosis at 2 uM/100 gram of body weight, ip by histopathological analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1198132 | Hepatotoxicity in Sprague-Dawley rat assessed as increase in aspartate aminotransferase activity in serum at 6 umol/100g body weight, ip measured after 24 to 36 hrs | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
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| AID1456268 | Inhibition of Torpedo californica AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min interval for 3 mins by Ellman's method | |||
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| AID1480845 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1152330 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate by spectrophotometer analysis | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Novel aromatic-polyamine conjugates as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. |
| AID552183 | Inhibition of equine BChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation. |
| AID1704814 | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI cells at 1 uM using p-tyramine as substrate by fluorometric assay relative to control | |||
| AID366355 | Inhibition of Electrophorus electricus AChE by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
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| AID1486128 | Inhibition of porcine liver carboxylesterase at 20 uM using 4-nitrophenol acetate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis relative to control | 2017 | Bioorganic & medicinal chemistry, 08-01, Volume: 25, Issue:15 | Synthesis, molecular docking, and biological activity of polyfluoroalkyl dihydroazolo[5,1-c][1,2,4]triazines as selective carboxylesterase inhibitors. |
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| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
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| AID231042 | NMS/OXO-M values are calculated from the ratio of the respective apparent Ki values | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| 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. |
| AID298281 | Inhibition of self-induced amyloid beta (1-40) aggregation at 10 uM by thioflavin T based fluorometric assay | 2007 | Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20 | Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease. |
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| AID1400276 | Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17 | Design, synthesis, and biological evaluation of selective and potent Carbazole-based butyrylcholinesterase inhibitors. |
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| AID714532 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1895839 | Inhibition of AChE (unknown origin) | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Inhibition of Histone Deacetylase 6 (HDAC6) as a therapeutic strategy for Alzheimer's disease: A review (2010-2020). |
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| AID1728618 | Induction of apoptosis in human SH-SY5Y cells assessed as viable cells at 5 uM incubated for 24 hrs by annexin V FITC/propidium iodide staining based flow cytometry (Rvb = 96.7 %) | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
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| AID1389636 | Hepatotoxicity in ICR mouse assessed as serum ALT activity at 15 mg/kg, ig after 22 hrs (Rvb = 34.7 +/- 2.0 U/L) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
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| AID1077140 | Toxicity in Wistar rat assessed as body weight at 6 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
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| AID117435 | Compound was evaluated for the approximate lethal dose when mice were administered increasing or decreasing doses of compound intraperitoneally until one fatality was observed | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
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| AID1351135 | Hepatotoxicity in Kunming mouse assessed as focal necrosis in liver at 35 mg/kg, ig after 48 hrs by H and E staining based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
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| AID1759903 | Inhibition of human GluN1a/GluN2B receptor expressed in HEK293 cells assessed as inhibition of glycine/glutamate-induced current measured at -60 mV holding potential by whole-cell patch clamp method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
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| AID1351128 | Cytotoxicity against rat PC12 cells assessed as inhibition of cell viability at 50 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1297715 | Inhibition of amyloid beta (1 to 42) (unknown origin) fibril formation at 50 uM after 24 hrs by phosphomolybdic acid staining-based transmission electron microscopic analysis | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1416241 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM by MTT assay relative to control | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | 5-Methyl- |
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| AID1545287 | Inhibition of rat cortex acetylcholinesterase using acetylthiocholine iodide as substrate incubated for 20 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). |
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| AID725912 | Selectivity ratio of IC50 for BuChE in Sprague-Dawley rat serum to IC50 for AChE in Sprague-Dawley rat cortices | 2013 | Bioorganic & medicinal chemistry, Feb-01, Volume: 21, Issue:3 | Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors. |
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| AID1075983 | Inhibition of scopolamine-induced cognitive deficit in ICR mouse assessed as increase in time spent swimming in Q1 quadrant at 1 mg/kg, ip administered 1 hr prior to scopolamine challenge measured after 30 mins by morris water maze test | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID612153 | Selectivity ratio of IC50 for AChE to IC50 for BChE | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID1869219 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | |||
| AID1378363 | Competitive inhibition of electric eel AChE assessed as enzyme-inhibitor complex using p-nitrophenyl acetate as substrate by Lineweaver-Burk plot analysis | 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. |
| AID1330806 | Cytotoxicity against human HepG2 cells assessed as cell viability at 300 uM after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID1759905 | Inhibition of human GluN1a/GluN2B receptor expressed in HEK293 cells assessed as relative inhibition of glycine/glutamate-induced current at 100 uM measured at +40 mV holding potential by whole-cell patch clamp method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
| AID1409646 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition measured after 2 mins by Ellman's method | |||
| AID1442004 | Competitive inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by Lineweaver-Burk plot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID1435917 | Cytotoxicity against human primary hepatocytes assessed as cell viability at 10 uM measured after 2 hrs by trypan blue assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID714527 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 10 mins prior to substrate addition measured after 15 mins by Ellman's method | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID31608 | Inhibition of human acetylcholinesterase-I | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1831869 | Antineuroinflammatory activity in mouse BV-2 cells assessed as suppression of LPS-induced iNOS mRNA expression at 0.1 uM preincubated for 24 hrs followed by LPS stimulation and measured after 24 hrs by RT-PCR analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID289397 | Inhibition of Electrophorus electricus AchE-induced beta amyloid protein 1-42 co-aggregation at 1 uM by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID232756 | Selectivity index is the ratio of salivation ED50 to extracellular AchE ED50. | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
| AID1292351 | Selectivity ratio of IC50 for horse serum BChE to IC50 for electric eel AChE | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID613949 | Inhibition of BACE1 expressed in baculovirus assessed as inhibition of amyloid beta-42 production at 5 uM 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. |
| AID1663424 | Antialzheimer activity in scopolamine-induced impairment in ICR mouse assessed as latency time at 15 mg/kg, ip administered once a day for 10 days pretreated with scopolamine for 30 mins and measured at 5th day of training session by Morris water maze tes | 2020 | Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12 | Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity. |
| AID689063 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-β aggregation. |
| AID282824 | Inhibition of AchE in bovine erythrocytes | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for 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. |
| 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. |
| AID747769 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. |
| AID32285 | Inhibitory concentration required against acetylcholinesterase activity | 2001 | Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23 | Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil. |
| AID1409663 | Hepatotoxicity in ICR mouse liver assessed as effect on hepatic cell gap after 22 hrs by hematoxylin/eosin staining based immunohistochemical method | |||
| AID1498899 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-30, Volume: 26, Issue:13 | Developing hybrid molecule therapeutics for diverse enzyme inhibitory action: Active role of coumarin-based structural leads in drug discovery. |
| AID1558583 | 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 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID407146 | Inhibition of electric eel AchE | 2008 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 18, Issue:13 | Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID443599 | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
| AID744315 | Inhibition of amyloid beta(1 to 42) (unknown origin) self-aggregation at 25 uM after 48 hrs by ThT fluorescence assay relative to control | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1075987 | Neuroprotective activity against Abeta1-42 peptide-induced neurotoxicity in rat C6 cells assessed as reduction in cell viability loss after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| 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. |
| AID1686238 | Selectivity index, ratio of IC50 for inhibition of AChE in human erythrocyte hemolyzates to IC50 for IC50 for inhibition of BuChE in human erythrocyte hemolyzates | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID781330 | pKa (acid-base dissociation constant) as determined by potentiometric titration | 2014 | Pharmaceutical research, Apr, Volume: 31, Issue:4 | Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds. |
| AID1771808 | Inhibition of equine serum BuChE using BTC as substrate preincubated with enzyme for 5 mins followed by substrate addition for 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Development and crystallography-aided SAR studies of multifunctional BuChE inhibitors and 5-HT |
| AID28681 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1335934 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-5 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID552791 | Inhibition of horse serum BuChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Cholinergic and neuroprotective drugs for the treatment of Alzheimer and neuronal vascular diseases. II. Synthesis, biological assessment, and molecular modelling of new tacrine analogues from highly substituted 2-aminopyridine-3-carbonitriles. |
| AID1705960 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 1 min followed by substrate addition and measured after 10 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. |
| AID1077119 | Toxicity in Wistar rat assessed as GSH level in brain at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| 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. |
| AID628416 | Inhibition of human plasmatic BChE after 5 mins using spectrophotometer by Ellman's method | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21 | Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties. |
| AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1459559 | Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinolone production using kynuramine as substrate after 20 mins by fluorescence assay | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID547804 | Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID729968 | Selectivity index, ratio of IC50 for horse serum BChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
| AID1352327 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 10 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Tetrahydroacridine derivatives with dichloronicotinic acid moiety as attractive, multipotent agents for Alzheimer's disease treatment. |
| AID1705962 | Inhibition of recombinant human N-terminal His6-tagged GSK-3beta H350L mutant expressed in baculovirus infected Sf21 cells using GSM as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. |
| AID262755 | Anticholinesterase activity against human plasma BChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1186587 | Inhibition of human recombinant AChE assessed as dissociation constant for enzyme-inhibitor-substrate complex by Lineweaver-Burk plot | 2014 | Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16 | Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. |
| AID663237 | Inhibition of equine serum butyrylcholine esterase using butyrylcholine chloride as substrate incubated for 5 mins prior to substrate addition measured every 3 mins by Ellman's assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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. |
| AID274650 | Inhibition of human erythrocyte AChE | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| AID1752235 | Inhibition of human amyloid beta 42 aggregation assessed as decreasing in fluorescence intensity for 3 hrs by ThT fluorescence assay | 2021 | Bioorganic & medicinal chemistry, 09-15, Volume: 46 | Development of curcumin-based amyloid β aggregation inhibitors for Alzheimer's disease using the SAR matrix approach. |
| AID31962 | In vitro inhibition against acetylcholinesterase in rat striata. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID30544 | In vitro inhibitory activity against acetylcholinesterase (AChE) in Electrophorus electricus | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Synthesis and structure-activity relationships of open D-Ring galanthamine analogues. |
| AID139843 | Compound was evaluated for the binding affinity by displacing [3H]methylscopolamine ([3H]-NMS) from mouse cerebral cortex tissue. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID548340 | Inhibition of horse serum BChE preincubated for 5 mins by Ellman's method | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Novel alkyl- and arylcarbamate derivatives with N-benzylpiperidine and N-benzylpiperazine moieties as cholinesterases inhibitors. |
| AID1762427 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
| AID1555976 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID257807 | Inhibition of human AChE | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
| AID1167541 | Inhibition of equine BChE preincubated for 15 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| 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. |
| AID736934 | Mixed-type inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate by Lineweaver-Burk plot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | Synthesis, biological evaluation and molecular modeling of aloe-emodin derivatives as new acetylcholinesterase inhibitors. |
| 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. |
| AID366354 | Selectivity ratio of IC50 for human serum BuChE to IC50 for human erythrocyte AChE | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID262757 | Selectivity for BChE over AChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID114804 | Compound was evaluated for the cholinergic activity in vivo in mice by administering the compound intraperitoneally and observation of the tremors was made after 30 min | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
| AID714726 | Neurotoxicity in Wistar rat primary cortical neurons assessed as decrease in cell viability at 25 to 100 uM by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1077106 | Toxicity in Wistar rat assessed as GSSG level in kidney at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1379221 | Cytotoxicity against human HepG2 cells assessed as cell viability at 25 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID1421884 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for human AChE | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors. |
| AID1831862 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
| AID1077110 | Toxicity in Wistar rat assessed as kidney weight at 6 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID761301 | Inhibition of electric eel AChE using acetylcholine iodide as substrate preincubated for 15 mins prior to substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Design, synthesis and neuroprotective evaluation of novel tacrine-benzothiazole hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1379218 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID130225 | Evaluated for the percentage change from control in mouse brain ACh concentrations | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1143744 | Inhibition of horse serum BuChE using butyrylthiocholine as substrate by UV spectroscopic analysis | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Dibenzo[1,4,5]thiadiazepine: a hardly-known heterocyclic system with neuroprotective properties of potential usefulness in the treatment of neurodegenerative diseases. |
| AID32093 | Inhibitory activity against rat brain total Acetylcholinesterase (AChE) was determined using Ellman's method | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors. |
| AID744310 | Antioxidant activity of the compound assessed as trolox equivalent of APPH-induced radical scavenging activity at 5 uM incubated for 15 mins measured every 1 min for 240 mins by ORAC-FL assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| 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 |
| AID1379217 | Inhibition of amyloid beta (1 to 42) (unknown origin) self -induced aggregation at 10 uM after 48 hrs by ThT-based fluorescence method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID1501678 | Induction of neuronal differentiation in human SH-SY5Y cells assessed as neurite bearing cells at 0.23 uM followed by culture medium replacement for every three days for 10 days by inverted-phase microscopic analysis relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID1592447 | Inhibition of human recombinant AChE using ATCh as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by Ellman method | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. |
| AID477066 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors. |
| AID1071757 | Hepatotoxicity in human HepG2 cells assessed as AST level at 100 uM after 24 hrs (Rvb = 50.3 +/- 2.90 IU/L) | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1651632 | Inhibition of recombinant human MAO-B at 10 uM incubated for 30 mins by fluorescence-based method | 2020 | Journal of natural products, 04-24, Volume: 83, Issue:4 | Bioactive Azepine-Indole Alkaloids from |
| AID134211 | Binding affinity against mouse Muscarinic acetylcholine receptor M2 using heart tissue and [3H]N-methylscopolamine | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| 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. |
| AID1179993 | Inhibition of AChE (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Coumarin hybrids as novel therapeutic agents. |
| AID1888435 | Inhibition of NO production in LPS-induced mouse BV-2 cells pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1698852 | Inhibition of equine serum BuChE | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Rapid discovery of a selective butyrylcholinesterase inhibitor using structure-based virtual screening. |
| AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
| AID1330797 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for human recombinant BChE | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID31965 | Inhibition of Acetylcholinesterase in rat red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID30543 | Compound was assessed for in vitro inhibition of Acetylcholinesterase isolated from Electrophorus electricus | 2000 | Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7 | Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1057012 | Inhibition of horse serum BuChE using butylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman method | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID1361162 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by CellTiter-Glo luminescence assay relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease. |
| AID1480852 | Inhibition of human erythrocyte AChE-induced amyloid beta (1 to 42) aggregation at 20 uM after 6 hrs by thioflavin T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| 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. |
| AID1324830 | Antioxidant activity assessed as inhibition of AAPH-induced peroxyl radical generation measured as trolox equivalent preincubated for 15 mins followed by AAPH addition measured evey 60 secs for 120 mins by ORAC-FL assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents. |
| AID139720 | Approximate lethal dose in mice. | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1545281 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate pretreated followed by substrate addition and measured after 2 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). |
| AID1198122 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID1555978 | Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 2 hrs under dark condition relative to control | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID26362 | Ionization constant (pKa) | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Prediction of human volume of distribution values for neutral and basic drugs. 2. Extended data set and leave-class-out statistics. |
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| AID227796 | Concentration required to potentiate the contraction of isolated rat ileum produced by 1 x 10 e -7 M Ach by 20 % | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
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| AID141322 | Compound was evaluated for the competitive inhibition of [3H]pirenzepine binding to Muscarinic acetylcholine receptor M1 of mouse cerebral cortex | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1901726 | Inhibition of human plasma BuChE using butyrylthiocholine as substrate preincubated for 5 mins followed by substrate addition by Ellman's method | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Synthesis, biological evaluation, and molecular modeling simulations of new heterocyclic hybrids as multi-targeted anti-Alzheimer's agents. |
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| AID170019 | Effect of compound on peripheral cholinergic effects in male wistar rats when administered orally at a dose of 10 mg/Kg; No significant change | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
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| AID1168968 | Cytotoxicity against HEK293 cells assessed as inhibition of cell proliferation at 2 mM after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | Discovery of 3-Arylcoumarin-tetracyclic Tacrine Hybrids as Multifunctional Agents against Parkinson's Disease. |
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| AID315739 | Hepatotoxicity in Wistar rat serum assessed as aspartate aminotransferase level at 5.93 umol, ip after 36 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
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| AID619268 | Inhibition of self-mediated amyloid beta (1 to 42) aggregation at 10 uM after 48 hrs by thioflavin T fluorescence method | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. |
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| 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. |
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| AID1382562 | Cytotoxicity against human HepG2 cells assessed as cell viability at 2.5 uM after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
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| AID663977 | Inhibition of Equus caballus BChE preincubated for 10 mins measured after 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and pharmacological assessment of diversely substituted pyrazolo[3,4-b]quinoline, and benzo[b]pyrazolo[4,3-g][1,8]naphthyridine derivatives. |
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| AID1593223 | Toxicity in intramuscularly dosed Wistar rat assessed as maximum tolerated dose measured during first 2 hrs then periodically for 48 hrs | 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. |
| AID1693557 | Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kin | 2021 | Bioorganic & medicinal chemistry, 01-15, Volume: 30 | Discovery of potent glycogen synthase kinase 3/cholinesterase inhibitors with neuroprotection as potential therapeutic agent for Alzheimer's disease. |
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| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1435900 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate pretreated for 10 mins followed by substrate addition measured after 15 mins by spectrophotometry based Ellman method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID366581 | Neuroprotective effect against human SH-SY5Y cells assessed as extracellular LDH release at 0.3 uM after 24 hrs in presence of 70 mM K+ relative to basal level | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| 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. |
| AID1686235 | Inhibition of horse serum BuChE pre-incubated for 10 mins before addition of butyrylthiocholine iodide substrate and further incubated for 15 mins by Ellman's method | 2016 | Journal of medicinal chemistry, 11-10, Volume: 59, Issue:21 | The Antioxidant Additive Approach for Alzheimer's Disease Therapy: New Ferulic (Lipoic) Acid Plus Melatonin Modified Tacrines as Cholinesterases Inhibitors, Direct Antioxidants, and Nuclear Factor (Erythroid-Derived 2)-Like 2 Activators. |
| AID1627645 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellmans method | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Cholinesterase inhibitory activity of chlorophenoxy derivatives-Histamine H3 receptor ligands. |
| AID692185 | Cmax in human | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID195551 | Inhibition of neuronal uptake of 5 - Hydroxytryptamine in rat brain homogenate | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. |
| AID752022 | Inhibition of electric eel AChE using acetylthiocholine as substrate preincubated for 10 mins prior to substrate addition measured every 30 seconds for 30 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Jun-15, Volume: 21, Issue:12 | Investigation of the role of linker moieties in bifunctional tacrine hybrids. |
| AID1317862 | Antioxidant activity assessed as AAPH radical scavenging activity measured as trolox equivalents preincubated for 15 mins followed by AAPH challenge measured every min for 80 mins by ORAC-FL assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID663252 | Hepatotoxicity in Sprague-Dawley rat assessed increase in aminotransferase level in serum at 6 umol/100g of body weight, ip after 24 hrs | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID175558 | Effect after an intraperitoneal dose of 1.0 mg/kg on amnesia induced in passive avoidance test in rats by Scopolamine | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
| AID315748 | Hepatotoxicity in Wistar rat liver assessed as tissue protein concentration at 5.93 umol, ip after 36 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1378385 | Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay | 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. |
| AID1435910 | Cytotoxicity against human HepG2 cells at 30 uM measured after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID658003 | Selectivity ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID694074 | Inhibition of human recombinant BChE using acetylthiocholine as substrate | 2012 | Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22 | Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aβ aggregation, and β-secretase. |
| AID1465121 | Inhibition of pig liver carboxylesterase at 20 uM using 4-nitrophenol acetate as substrate by spectrophotometric analysis | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | 9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment. |
| AID1542237 | Cytotoxicity against human HepG2 cell assessed as safe dose that maintains 100% cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1332148 | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus-infected insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by amplex red assay | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents. |
| AID289396 | Inhibition of Electrophorus electricus AchE-induced beta amyloid protein 1-42 co-aggregation at 100 uM by thioflavin T assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID657795 | Inhibition of mitochondrial MAO-B in rat liver homogenates using [14C]-phenylethylamine as substrate preincubated for 30 mins by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID648658 | Inhibition of Electrophorus electricus AChE using acetylthiocholine chloride as substrate after 15 mins incubation by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 22, Issue:6 | Novel oxoisoaporphine-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1459563 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Synthesis and evaluation of 7-substituted coumarin derivatives as multimodal monoamine oxidase-B and cholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID714540 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 0.1 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1057000 | Inhibition of human recombinant MAO-B using benzylamine as substrate at 100 uM preincubated for 15 mins under dark condition followed by substrate addition measured after 20 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Inhibition of cholinesterase and monoamine oxidase-B activity by Tacrine-Homoisoflavonoid hybrids. |
| AID594991 | Inhibition of amyloid beta (1-40) aggregation at 100 uM by thioflavin-T based spectrofluorometric assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity. |
| AID752001 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 6 mins prior to substrate addition measured after 60 to 180 secs by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, May-01, Volume: 23, Issue:9 | Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease. |
| AID714541 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 1 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1409645 | Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 20 mins followed by substrate addition measured after 2 mins by Ellman's method | |||
| AID1711762 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition and measured after 2 mins by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID629634 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 10 mins before substrate addition by Ellman's method | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues. |
| AID1575665 | Inhibition of amyloid beta (1 to 42 ) (unknown origin) self aggregation at 10 uM after 24 hrs by thioflavin-T fluorescence method | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | Synthesis of novel vanillin derivatives: novel multi-targeted scaffold ligands against Alzheimer's disease. |
| AID1186584 | Inhibition of human BuChE pre-incubated for 5 mins before butylthiocholine substrate addition by Ellman's method | 2014 | Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16 | Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. |
| AID1575667 | Antioxidant activity assessed as ferric-tripyridyltriazine complex reducing activity up to 250 uM at pH 3.5 after 30 mins under dark condition by FRAP assay | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | Synthesis of novel vanillin derivatives: novel multi-targeted scaffold ligands against Alzheimer's disease. |
| AID657790 | Selectivity ratio of IC50 for human serum BuChE to IC50 for human recombinant AChE | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| 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. |
| AID1784743 | Inhibition of equine serum BuChE using butyrylthiocholine as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT |
| 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. |
| AID232627 | Ratio of inhibitory activity against [3H]quinuclidinyl benzilate (QNB) binding in the absence of Zn to in the presence of Zn | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1379235 | Hepatotoxicity against human HepG2 cells up to 50 uM after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation. |
| AID1077126 | Toxicity in Wistar rat assessed as ethylmorphine-N-demethylation activity in liver measured as formaldehyde level at 6 umol/100 g body weight, ip by photometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1273121 | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated followed by substrate addition by Ellman's method | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors. |
| AID1297714 | Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation after 24 hrs by thioflavin T fluorescence assay | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID44286 | In vitro Butyrylcholinesterase inhibitory activity to determine its ability to reverse the cholinergic deficit characteristic of AD | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID229560 | Ratio of IC50(BChE-I) to IC50(AChE-I) | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1378387 | Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay | 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. |
| AID1310648 | Inhibition of electric eel AChE using acetylcholine as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Potent anticholinesterasic and neuroprotective pyranotacrines as inhibitors of beta-amyloid aggregation, oxidative stress and tau-phosphorylation for Alzheimer's disease. |
| AID1126620 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins by Ellman's method | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease. |
| AID1360334 | Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 10 uM after 48 hrs by thioflavin-T fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and β-secretase inhibition activities. |
| AID1815196 | Inhibition of hERG expressed in CHO-K1 cells assessed as reduction in thallium influx incubated for 30 minutes by FLIPR | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | A tacrine-tetrahydroquinoline heterodimer potently inhibits acetylcholinesterase activity and enhances neurotransmission in mice. |
| 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. |
| AID1635492 | Antioxidant activity assessed as DPPH free radical scavenging activity at 10 uM after 30 secs by spectrophotometry | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID744316 | Mixed-type inhibition of electric eel AChE using acetylthiocholine as substrate after 15 mins by Lineweaver-Burk plot analysis | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID289398 | Neuroprotective effect against beta amyloid protein 1-42 treated human IMR32 cells at 0.1 umol/ml after 48 hrs by MTT assay | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID315738 | Hepatotoxicity in Wistar rat serum assessed as aspartate aminotransferase level at 5.93 umol, ip after 20 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1382574 | Antioxidant activity assessed as DPPH radical scavenging activity incubated for 30 mins | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Novel Tacrine-Hydroxyphenylbenzimidazole hybrids as potential multitarget drug candidates for Alzheimer's disease. |
| AID1480847 | Inhibition of human serum BuChE using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1077109 | Toxicity in Wistar rat assessed as GSH level in kidney at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1728648 | Cognitive enhancing effect in Sprague-Dawley rat model of amyloid beta (25 to 35) peptide-induced memory impairment assessed as number of platform crossing at 0.2 mg per 100 g, ip qd for 4 weeks administered via gavage and measured after 5 days by Morris | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID366580 | Neuroprotective effect against human SH-SY5Y cells assessed as extracellular LDH release at 0.3 uM after 24 hrs in presence of 70 mM K+ | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID1382545 | Inhibition of human serum BCHE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID1501666 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by XTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| 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. |
| 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. |
| AID349879 | Antioxidant activity in human SH-SY5Y cells assessed as protection against H2O2-induced oxidative stress at 0.3 uM pretreated for 24 hrs before H2O2 challenge by lactate dehydrogenase assay relative to control | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID491976 | Inhibition of bovine erythrocyte AChE by Ellman's reaction | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties. |
| AID1557952 | Inhibition of Acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate by Ellman's spectrophotometric method | 2019 | Bioorganic & medicinal chemistry, 09-15, Volume: 27, Issue:18 | Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review. |
| AID716436 | Hepatotoxicity against Wistar rat assessed as fatty degeneration of hepatocyte at 6 uM/100 gram of body weight, ip after 24 hrs by histopathological analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID761299 | Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins by spectrophotometric analysis | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Design, synthesis and neuroprotective evaluation of novel tacrine-benzothiazole hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1592450 | Inhibition of native porcine brain GSK-3alpha/beta using GS-1 as substrate incubated for 30 mins in presence of [gamma-33P]ATP by liquid scintillation counting assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. |
| 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. |
| AID604023 | Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID690968 | Inhibition of electric eel AChE using acetylcholine iodide as substrate preincubated for 20 mins by Ellman's method | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1888432 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured after 5 mins by DTNB-reagent based Ellman's method | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease. |
| 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. |
| AID548338 | Inhibition of electric eel AChE preincubated for 5 mins by Ellman's method | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Novel alkyl- and arylcarbamate derivatives with N-benzylpiperidine and N-benzylpiperazine moieties as cholinesterases inhibitors. |
| AID621450 | Selectivity index, ratio of IC50 for human AChE to IC50 for equine BuChE | 2011 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 21, Issue:19 | Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aβ-aggregation inhibitors: Synthesis and biological evaluation. |
| AID1271544 | Hepatotoxicity in ICR mouse assessed as elevation in serum aspartate aminotransferase level at 30 mg/kg, ig after 8 hrs by spectrophotometry analysis relative to control | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1335935 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-6 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1759901 | Inhibition of human GluN1a/GluN2A receptor expressed in HEK293 cells assessed as inhibition of glycine/glutamate-induced current measured at -60 mV holding potential by whole-cell patch clamp method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
| AID1240487 | Inhibition of Electrophorus electricus AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate addition by Ellman's method | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17 | Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening. |
| 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. |
| AID620400 | Inhibition of Electrophorus electricus AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. |
| AID657796 | Inhibition of mitochondrial MAO-A in rat liver homogenates using [14C]-(5-hydroxy-triptamine) as substrate preincubated for 30 mins by liquid scintillation counting | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID1759896 | Inhibition of human recombinant AChE assessed as reduction in cholinesterase activity using acetylthiocholine iodide as substrate by Ellman's method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
| AID349881 | Inhibition of electric eel AChE by Ellman's method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID302145 | Inhibition of Torpedo californica AChE by Ellman's method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
| AID754042 | Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins prior to substrate addition measured at 60 to 180 seconds by Ellman's method | 2013 | European journal of medicinal chemistry, Jun, Volume: 64 | Design, synthesis and evaluation of novel tacrine-coumarin hybrids as multifunctional cholinesterase inhibitors against Alzheimer's disease. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1501670 | Cytoprotection against amyloid beta (1 to 42) peptide induced cell death in human SH-SY5Y cells assessed as increase in clonogenic survival at 0.23 uM after 24 hrs by Giemsa staining-based inverted microscopic analysis | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | From dual binding site acetylcholinesterase inhibitors to allosteric modulators: A new avenue for disease-modifying drugs in Alzheimer's disease. |
| AID656044 | Permeability of the compound in phosphate buffer at pH 7.4 by PAMPA | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
| AID303073 | Selectivity for human butyrylcholinesterase over human butyrylcholinesterase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| 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. |
| AID744320 | Selectivity index, ratio of IC50 for horse serum butyrylcholinesterase to IC50 for electric eel acetylcholinesterase | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1077143 | Antialzheimer activity in Wistar rat scopolamine-induced cognition impairment model assessed as decrease in amount of errors plus baits not found during exploration at 1 umol/100 g body weight, ip treated for 5 mins prior to scopolamine-challenge measured | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1167545 | Antioxidant activity assessed as oxygen radical absorbance capacity preincubated for 10 mins by fluorescence assay relative to trolox | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Discovery of indanone derivatives as multi-target-directed ligands against Alzheimer's disease. |
| AID569581 | Inhibition of electric eel AChE by Ellman's method | 2011 | Bioorganic & medicinal chemistry, Feb-01, Volume: 19, Issue:3 | Probing the mid-gorge of cholinesterases with spacer-modified bivalent quinazolinimines leads to highly potent and selective butyrylcholinesterase inhibitors. |
| AID1450070 | Inhibition of recombinant human CYP1A2 expressed in insect cells at 10 uM using EOMCC as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1077120 | Toxicity in Wistar rat assessed as brain weight at 6 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1273122 | Inhibition of human carboxylesterase 1 using o-nitrophenylacetate as substrate by spectrophotometry analysis | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors. |
| AID714534 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1077139 | Toxicity in Wistar rat assessed as liver weight at 1 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1416890 | Inhibition of horse serum BChE after 15 mins by DTNB reagent based assay | 2018 | MedChemComm, Jan-01, Volume: 9, Issue:1 | Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
| AID1055213 | Inhibition of human recombinant AChE-induced amyloid beta (1 to 40) aggregation at 100 uM after 48 hrs by thioflavin T fluorescence assay relative to control | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID443600 | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of [3H]arachidonic acid release | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
| AID1070083 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of a new series of ebselen derivatives as glutathione peroxidase (GPx) mimics and cholinesterase inhibitors against Alzheimer's disease. |
| AID1379224 | Cytotoxicity against human HepG2 cells assessed as cell viability at 300 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID1389645 | Reversal of scopolamine-induced cognitive function impairment in ICR mouse assessed as escape latency time at 15 mg/kg, po dosed 30 mins prior to scopolamine treatment by Morris water maze test (Rvb = 40.5 sec) | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease. |
| AID1409658 | Hepatotoxicity in ICR mouse assessed as serum ALT activity at 30 mg/kg, administered intragastrically measured 22 hrs post dose (Rvb = 39 +/- 9.4 U/L) | |||
| AID714722 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 100 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID716427 | Hepatotoxicity against human HSC cells assessed as reduction in cell number at 75 uM after 24 hrs using crystal violet staining by photometry | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID765128 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins before substrate addition by Ellman's method | 2013 | Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17 | Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors. |
| AID1435902 | Inhibition of horse serum BuChE using butyrylthiocholine as substrate pretreated for 10 mins followed by substrate addition measured after 15 mins by spectrophotometry based Ellman method | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID1667722 | Inhibition of electric eel AchE using acetylthiocholine as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening. |
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| AID1199519 | Inhibition of equine serum BuChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID196925 | Ability to inhibit after-hyperpolarization (AHP) in cultured rat sympathetic neurons. (number of neurons tested, n=3). Insufficient activity at this concentration | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle. |
| AID412866 | Inhibition of Electric eel AChE | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity. |
| AID714537 | Cytotoxicity against human HepG2 cells assessed as cell viability at 300 uM after 24 hrs by MTT assay relative to control | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1378371 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by Ellman's method | 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. |
| AID1564191 | Neuroprotective activity against serum/K+ deprivation induced cytotoxicity in rat primary neuronal cells at 1 to 25 uM by MTT assay | 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. |
| AID776491 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition by Ellmans method | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease. |
| AID1328977 | Neurotoxicity in rat primary cortical neurons assessed as decrease in cell viability at 25 uM by XTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease. |
| AID1543542 | Inhibition of human serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured at 1 min time interval by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Synthesis and evaluation of tetrahydroisoquinoline-benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID771360 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, docking study and biological evaluation of some novel tetrahydrochromeno [3',4':5,6]pyrano[2,3-b]quinolin-6(7H)-one derivatives against acetyl- and butyrylcholinesterase. |
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| AID1077123 | Toxicity in Wistar rat assessed as ethoxyresorufin-O-deethylation activity in liver measured as resorufin level at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1273500 | Inhibition of human erythrocyte AChE using acetylthiocholine as substrate assessed as substrate hydrolysis preincubated for 20 mins followed by substrate addition measured after 30 mins by Ellman's assay | 2015 | Journal of natural products, Dec-24, Volume: 78, Issue:12 | 1,9-seco-Bicyclic Polyprenylated Acylphloroglucinols from Hypericum uralum. |
| AID714544 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 10 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
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| AID1751083 | Inhibition of electric eel AChE by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of novel deoxyvasicinone-indole as multi-target agents for Alzheimer's disease. |
| AID241118 | Inhibitory concentration against Butyrylcholinesterase activity | 2005 | Bioorganic & medicinal chemistry letters, Jan-17, Volume: 15, Issue:2 | Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus. |
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| AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1055218 | Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
| AID1555977 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1361163 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by CellTiter-Glo luminescence assay relative to control | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease. |
| AID600981 | Inhibition of human plasma BChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease. |
| AID1328951 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins followed by substrate addition by Ellman's method | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Avarol derivatives as competitive AChE inhibitors, non hepatotoxic and neuroprotective agents for Alzheimer's disease. |
| AID366353 | Inhibition of human serum BuChE by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID1591863 | Inhibition of electric eel AchE using acetylthiocholine as substrate by Ellman's method | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids. |
| AID690971 | Inhibition of HFIP pretreated self-mediated amyloid beta (1 to 40) aggregation at 20 uM after 24 hrs by thioflavin-T based fluorimetric assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20 | Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID657791 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate by Ellman's method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID1674981 | Protection against amyloid beta oligomer-induced cytotoxicity in human SH-SY5Y cells expressing wild-type Tau assessed as cell viability at 10 uM by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 30, Issue:17 | Discovery of biphenyl pyrazole scaffold for neurodegenerative diseases: A novel class of acetylcholinesterase-centered multitargeted ligands. |
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| AID1751085 | Inhibition of self-induced amyloid beta(1 to 42) (unknown origin) aggregation by thioflavin-T fluorescence assay | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of novel deoxyvasicinone-indole as multi-target agents for Alzheimer's disease. |
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| 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. |
| AID90048 | Inhibition of rat kidney Histamine N-Methyltransferase (HMT) activity determined by the formation of N-methyl-histamine | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity. |
| AID141320 | Binding affinity against mouse Muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID229262 | Ratio of IC50 for BuChE to AChE | 1995 | Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24 | Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. |
| 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. |
| AID458980 | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in binary complex by EATCM analysis | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors. |
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| AID366583 | Neuroprotective effect against human SH-SY5Y cells assessed as extracellular LDH release at 0.3 uM after 24 hrs in presence of 60 uM H2O2 relative to basal level | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID443747 | Selectivity for human CB1 receptor over human CB2 receptor | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism. |
| AID594821 | Inhibition of BChE | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | (+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase. |
| AID666578 | Selectivity ratio of IC50 for equine serum butyrylcholinesterase to IC50 for electric eel acetylcholine esterase | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1635485 | Selectivity ratio of IC50 for human erythrocyte AChE to IC50 for equine serum BuChE | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1379216 | Inhibition of electric eel AchE-induced amyloid beta (1 to 40) aggregation at 100 uM after 24 hrs by ThT-based fluorescence method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
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| AID1466564 | Inhibition of equine serum BuChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by spectrophotometric analysis | |||
| AID1217709 | Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID589181 | Mechanism based inhibition of human cytochrome P450 1A2, partition ratio | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
| AID1198138 | Hepatotoxicity in Sprague-Dawley rat assessed as fatty degeneration of hepatocytes at 6 umol/100g body weight, ip measured after 24 hrs by histomorphological study | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| 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 |
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| 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. |
| AID480453 | Inhibition of dexamethasone-induced human NR1-1a/NR2A receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L12-G10 cells assessed as LDH release after 30 mins | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
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| AID52790 | Inhibition of chymotrypsin at 250 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
| AID1209582 | Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods. |
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| AID1071752 | Inhibition of electric eel AchE using acetylcholine as substrate preincubated for 15 mins followed by substrate addition measured for 5 mins by Ellman method | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID44289 | In vitro inhibitory activity against Butyrylcholinesterase (BChE) in human serum | 2003 | Bioorganic & medicinal chemistry letters, Jul-21, Volume: 13, Issue:14 | Synthesis and structure-activity relationships of open D-Ring galanthamine analogues. |
| AID1508032 | Inhibition of horse serum BChE | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Azaphenothiazines - promising phenothiazine derivatives. An insight into nomenclature, synthesis, structure elucidation and biological properties. |
| AID1241461 | Inhibition of human NR1-1a/NR2A expressed in mouse L12-G10 cells assessed as inhibition of glutamate-induced excitotoxicity incubated for 16 hrs by LDH release assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders. |
| AID1202688 | Inhibition of equine serum BuChE pre-incubated for 3 mins before butyrylthiocholine substrate addition by Ellman's reagent based spectrophotometry | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain. |
| AID1543541 | Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition and measured at 1 min time interval by Ellman's method relative to control | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Synthesis and evaluation of tetrahydroisoquinoline-benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID1728620 | Induction of apoptosis in human SH-SY5Y cells assessed as late apoptotic cells at 5 uM incubated for 24 hrs by annexin V FITC/propidium iodide staining based flow cytometry (Rvb = 1.2 %) | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID1352649 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by Ellman's method | 2018 | European journal of medicinal chemistry, Feb-25, Volume: 146 | Design, synthesis and biological evaluation of new coumarin-dithiocarbamate hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID387771 | Inhibition of histamine N-methyl-transferase | 2008 | Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19 | Design, synthesis, and docking studies of novel benzopyrone derivatives as H(1)-antihistaminic agents. |
| AID142248 | Antagonistic potency of compound towards Muscarinic acetylcholine receptor M2 in guinea pig left atrium. | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine. |
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| AID692183 | Protein binding in human plasma | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| 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. |
| AID1581645 | Inhibition of recombinant human BACE1 using Rh-EVNLDAEFK-Quencher as substrate measured after 60 mins by FRET based spectrofluorometric assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease. |
| AID141667 | Inhibition of [3H]quinuclidinyl benzilate (QNB) binding from rat forebrain membranes in the absence of Zn | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1271531 | Hepatotoxicity in ICR mouse assessed as serum alanine aminotransferase level at 30 mg/kg, ig after 8 hrs by spectrophotometry analysis (Rvb = 38.8 +/- 10.1 U/L) | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1186579 | Inhibition of human BChE assessed as acetylthiocholine hydrolysis | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase. |
| AID1152332 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BChE | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Novel aromatic-polyamine conjugates as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. |
| AID600118 | Selectivity ratio of IC50 for recombinant human AChE to IC50 for recombinant human serum BChE | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation. |
| AID656042 | Inhibition of human serum BChE by Ellman's method | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID341421 | Inhibition of human recombinant AChE by Ellman's method | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush. |
| AID1186585 | Selectivity index, ratio of IC50 for human BuChE to IC50 for human recombinant AChE | 2014 | Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16 | Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. |
| AID195552 | Inhibition of neuronal uptake of Noradrenaline in rat brain homogenate | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. |
| AID692193 | Inhibition of human OCT2 A270S mutant expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID1311917 | Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) at 20 uM measured after 46 to 48 hrs by ThT-based fluorometric assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1335937 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-8 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID1468641 | Displacement of [3H]-CP55950 from human CB2 receptor expressed in HEK cell membranes after 3 hrs by scintillation counting method | |||
| AID1077138 | Toxicity in Wistar rat assessed as liver weight at 6 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID114183 | Effective dose against administration in mice | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1542248 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate pre-incubated for 20 mins before substrate addition and measured for 180 secs by spectrophotometry based Ellman's method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID1075979 | Selectivity index, ratio of IC50 for human serum BuChE to IC50 for electric eel acetylcholinesterase type VI-S | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1184620 | Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode. |
| AID31500 | Inhibitory concentration against acetylcholinesterase (AChE) from human erythrocytes | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID1435913 | Cytotoxicity against human HepG2 cells at 1000 uM measured after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID604022 | Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID459730 | Inhibition of electric eel AChE by Ellman's method | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors. |
| AID44452 | Compound was evaluated for the in vitro inhibition of the Butyrylcholinesterase from horse serum | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID1256999 | Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholineiodide as substrate measured at 30 secs intervals over 9 mins by Ellman's colorimetric assay | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents. |
| AID257808 | Inhibition of human BuChE | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2 | Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties. |
| AID184491 | Ameliorating effects on diazepam-induced memory impairment of passive avoidance response (no of rats) | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID666575 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13 | Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents. |
| AID1351123 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability at 1 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1190763 | Selectivity ratio of IC50 for human recombinant AchE to IC50 for human recombinant serum BuchE | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Iminosugars as a new class of cholinesterase inhibitors. |
| AID1465118 | Antioxidant activity assessed as ABTS radical cation scavenging activity after 1 hr by UV/Vis spectrophotometric method-based ABTS radical cation decolorization assay | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | 9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment. |
| AID1558586 | Displacement of [3H]-CP55940 from human recombinant cannabinoid CB2 receptor expressed in human HEK cells at 10 uM by radioligand binding assay relative to control | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
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| AID142654 | Compound was evaluated for the competitive inhibition of [3H]methylscopolamine binding to Muscarinic acetylcholine receptor M2 of mouse cerebral cortex | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
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| AID1762431 | Inhibition of recombinant human BACE1 expressed in baculovirus expression system using Rh-EVNLDAEFK-quencher as substrate incubated for 60 mins by FRET assay | 2021 | European journal of medicinal chemistry, Jun-05, Volume: 218 | Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and γ-aminobutyric acid transporters. |
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| AID1240923 | Inhibition of equine serum BChE using ATC iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of 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. |
| AID1351115 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
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| AID1450076 | Inhibition of recombinant human CYP3A4 expressed in insect cells at 100 uM using DBOMF as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
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| AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1351134 | Hepatotoxicity in Kunming mouse assessed as vacuolar degeneration in the perivascular tissue at 35 mg/kg, ig after 48 hrs by H and E staining based assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1711764 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every minute for 80 mins by ORAC-FL assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Development of cyanopyridine-triazine hybrids as lead multitarget anti-Alzheimer agents. |
| AID747768 | Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. |
| AID1869215 | Inhibition of AChE in human Erythrocyte incubated for 20 mins by Ellman reagent based spectrophotometry | |||
| AID1184616 | Inhibition of human AChE | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode. |
| AID1896375 | Inhibition of electric eel AChE by Ellman's method | 2022 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 77 | Selective butyrylcholinesterase inhibition by isatin dimers and 3-indolyl-3-hydroxy-2-oxindole dimers. |
| AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1190809 | Antioxidant activity assessed as DPPH radical scavenging activity at 10 uM after 60 mins by spectrophotometry | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD. |
| AID1633668 | Permeability of the compound at pH 7.4 PBS buffer at 100 uM measured upto 6 hrs by PAMPA-BBB assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4 | Novel Sustainable-by-Design HDAC Inhibitors for the Treatment of Alzheimer's Disease. |
| 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. |
| AID315740 | Hepatotoxicity in Wistar rat serum assessed as albumin level at 5.93 umol, ip after 12 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1183481 | Inhibition of Torpedo californica AChE by spectrophotometry based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Synthesis and cholinesterase inhibition of cativic acid derivatives. |
| 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. |
| AID29359 | Ionization constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID526832 | Inhibition of equine BChE after 15 mins by Ellman's method using acetylcholine as substrate | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase. |
| AID716435 | Hepatotoxicity against Wistar rat assessed as liver cell apoptosis at 6 uM/100 gram of body weight, ip after 24 hrs by histopathological analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1311920 | Inhibition of human serum BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
| AID1564168 | Competitive inhibition of electric eel AChE using acetylthiocholine iodide as substrate measured for 125 secs by Lineweaver-burk plot analysis | 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. |
| 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. |
| AID1545272 | Inhibition of human Cholinesterase | 2019 | Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6 | Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018). |
| AID111985 | Reversal of scopolamine-induced memory impairment in mice at 1.25 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID1705939 | Cognitive enhancing effect in ICR mouse model of scopolamine-induced memory impairment assessed as reduction in distance travelled to found target at 15 mg/kg, po administered 30 mins prior to scopolamine injection by Morris water maze test | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1576566 | Selectivity index, ratio of IC50 for inhibition of AChE in Swiss mouse brain to IC50 for inhibition of BuChE in Swiss mouse serum | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling. |
| AID274654 | Viability of SH-SY5Y cells measured as reduction in LDH release in presence of hypertonic potassium at 0.3 uM relative to control | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| AID526831 | Inhibition of electric eel AChE after 15 mins by Ellman's method using acetylcholine as substrate | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase. |
| AID491974 | Inhibition of human erythrocyte AChE by Ellman's reaction | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties. |
| AID1409659 | Hepatotoxicity in ICR mouse assessed as serum ALT activity at 30 mg/kg, administered intragastrically measured 36 hrs post dose (Rvb = 30 +/- 8 U/L) | |||
| AID1445546 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every minute for 10 mins by Ellman's spectrophotometric method | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a "Bio-Oxidizable" Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. |
| AID1617641 | Inhibition of human erythrocyte BuChE using S-butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 secs for 1 hr by Ellman's method | 2019 | Journal of natural products, 12-27, Volume: 82, Issue:12 | Alkaloids from the Branches and Leaves of |
| AID1409664 | Hepatotoxicity in ICR mouse liver assessed as effect on liver cell number after 22 hrs by hematoxylin/eosin staining based immunohistochemical method | |||
| AID1442001 | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID1435915 | Cytotoxicity against human primary hepatocytes assessed as cell viability at 1 uM measured after 2 hrs by trypan blue assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID1058681 | Antioxidant activity assessed as hydrogen peroxide radical scavenging activity at 100 uM after 10 hrs by horseradish peroxidase assay | 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. |
| AID274655 | Viability of SH-SY5Y cells measured as neuroprotection activity in presence of hypertonic potassium at 0.3 uM relative to control | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| AID1330805 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID659698 | Selectivity ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids. |
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| 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. |
| AID1503606 | Inhibition of human serum AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 3 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Dec-01, Volume: 141 | New pyridine derivatives as inhibitors of acetylcholinesterase and amyloid aggregation. |
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| AID111984 | Reversal of scopolamine-induced memory impairment in mice at 0.63 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
| AID480456 | Inhibition of dexamethasone-induced human NR1-1a/NR2B receptor-mediated excitotoxicity in (S)-glutamate/glycine-stimulated mouse L13-E6 cells assessed as LDH release at 25 uM after 30 mins | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. |
| AID395324 | Lipophilicity, log D at pH 7.4 by liquid chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
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| AID331668 | Inhibition of electric eel AchE by Ellman's assay | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates. |
| AID1241459 | Inhibition of BChE in equine serum using butyrylthiocholine iodide substrate by Ellman assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders. |
| AID1409661 | Hepatotoxicity in ICR mouse assessed as serum AST activity at 30 mg/kg, administered intragastrically measured 22 hrs post dose (Rvb = 120 +/- 20 U/L) | |||
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| AID716429 | Hepatotoxicity against human HSC cells assessed as reduction in cell number at 50 uM after 24 hrs by fluorescence microscopic analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1501308 | Metal chelating activity assessed as inhibition of Cu2+ mediated amyloid beta (1 to 42) (unknown origin) aggregation at 25 uM after 2 hrs by turbidity assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
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| AID724167 | Inhibition of butyrylcholinesterase (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID620401 | Inhibition of equine serum BChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Hybrids of oxoisoaporphine-tacrine congeners: novel acetylcholinesterase and acetylcholinesterase-induced β-amyloid aggregation inhibitors. |
| AID714720 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 25 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1311209 | Effective permeability of the compound at 100 uM at pH 7.4 after 3 to 6 hrs by PAMPA | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | Design, synthesis and in vitro evaluation of benzothiazole-based ureas as potential ABAD/17β-HSD10 modulators for Alzheimer's disease treatment. |
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| AID1869218 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | |||
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| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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| AID1351139 | Hepatotoxicity in Kunming mouse assessed as increase in serum ALT level at 35 mg/kg, ig after 48 hrs by colorimetric method relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID594254 | Inhibition of electric eel AChE by Ellman's method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Syntheses and characterization of novel oxoisoaporphine derivatives as dual inhibitors for cholinesterases and amyloid beta aggregation. |
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| AID1351124 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability at 10 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1256998 | Antiinflammatory activity in CD1 mouse ear inflammation model assessed as suppression of TPA-induced ear edema at 1.5 micromol/20 microL of vehicle after 5 hrs | 2015 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 25, Issue:23 | Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents. |
| AID1379219 | Cytotoxicity against human HepG2 cells assessed as cell viability at 5 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
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| AID1077141 | Toxicity in Wistar rat assessed as body weight at 1 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
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| AID1856386 | Selectivity index, ratio of IC50 for inhibition of human AChE using acetylthiocholine iodide as substrate to IC50 for inhibition of human BChE using butyrylthiocholineiodide as substrate | 2022 | RSC medicinal chemistry, Aug-17, Volume: 13, Issue:8 | Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model. |
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| AID1831854 | Effective permeability of compound in PBS at pH 7.4 incubated upto 6 hrs by HPLC-MS analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Sustainable Drug Discovery of Multi-Target-Directed Ligands for Alzheimer's Disease. |
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| AID1140644 | Displacement of propidium iodide from AchE in bovine erythrocytes at 1 uM after 15 mins by fluorescence microplate reader analysis | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | New melatonin-N,N-dibenzyl(N-methyl)amine hybrids: potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease. |
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| AID1382554 | Cytotoxicity against NGF-differentiated rat PC12 cells assessed as decrease in cell viability at 1.25 to 10 uM after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
| AID1379562 | Selectivity index, ratio of IC50 for human AChE to IC50 for human BChE | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Novel deoxyvasicinone derivatives as potent multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation. |
| AID458978 | Selectivity ratio of pIC50 for electric eel AChE to pIC50 for equine BChE | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors. |
| AID88631 | Affinity for displacement of [125I]iodoproxyfan from human histamine H3 receptors stably expressed in CHO cells; ND is No Data. | 2002 | Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5 | Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity. |
| AID1495955 | Inhibition of rat serum BChE using butyrylthiocholine iodide as substrate after 20 mins by by Ellman's method | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Design, synthesis and evaluation of vilazodone-tacrine hybrids as multitarget-directed ligands against depression with cognitive impairment. |
| AID1682160 | In vivo inhibition of acetylcholinesterase in Sprague-Dawley rat cortex at 60 micromol/kg, IG administered once daily for 8 days and measured 30 mins post 8th dose by spectrophotometric method relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID696908 | Inhibition of Electrophorus electricus C2888 AChE using acetylthiocholine iodide as substrate by Ellman's spectroscopic method | 2012 | Journal of natural products, Nov-26, Volume: 75, Issue:11 | Acetylcholinesterase inhibitors from the leaves of Macaranga kurzii. |
| AID342535 | Inhibition of bovine AChE by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors. |
| AID412868 | Selectivity ratio of IC50 for Electric eel AChE to IC50 for equine serum BChE | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity. |
| AID1379561 | Inhibition of human BChE pre-incubated for 6 mins before ATCI substrate addition and measured after 12 mins by DTNB reagent dependent UV-Vis spectrophotometry based Ellman's method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Novel deoxyvasicinone derivatives as potent multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation. |
| AID1409655 | Cognition enhancing effect in scopolamine-induced ICR mouse assessed as mean escape latency time at 15 mg/kg, po administered 30 mins prior to scopolamine injection for 10 consecutive days followed by testing on day 11 post 30 mins scopolamine treatment b | |||
| AID303072 | Inhibition of human butyrylcholinesterase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| AID315735 | Selectivity ratio of IC50 for AChE to IC50 for BuChE | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID469398 | Inhibition of human BuChE in serum | 2009 | Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22 | Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease. |
| AID1338115 | Inhibition of Electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured after 5 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID31171 | In vitro inhibition of acetylcholinesterase from human erythrocytes | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID341422 | Inhibition of human serum BChE by Ellman's method | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush. |
| AID1271526 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 3 uM after 48 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1682107 | Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate incubated for 30 mins by Ellman's coupled enzyme assay | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID1235031 | Inhibition of human recombinant BChE using butyrylthiocholine iodide as substrate after 5 mins by Ellman's method | 2015 | Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15 | Structure-based development of nitroxoline derivatives as potential multifunctional anti-Alzheimer agents. |
| AID1317861 | Inhibition of electric eel AChE-mediated amyloid beta (1 to 42) (unknown origin) co-aggregation at 100 uM measured after 48 hrs by ThT-assay | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1077112 | Toxicity in Wistar rat assessed as lipidperoxidation product level in brain at 6 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1416238 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 10 uM measured for 300 secs by thioflavin T fluorometric assay relative to control | 2017 | MedChemComm, Jun-01, Volume: 8, Issue:6 | 5-Methyl- |
| AID1768733 | Inhibition of electric eel AChE by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID315747 | Hepatotoxicity in Wistar rat liver assessed as tissue protein concentration at 5.93 umol, ip after 20 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID776475 | Hepatotoxicity in ICR mouse assessed as increase in serum ALT level at 11.86 umol/100 g, id measured at 8 to 30 hrs | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease. |
| AID654180 | Inhibition of self-induced Abeta1-42 aggregation at 10 uM after 24 hrs by thioflavin T fluorescence method | 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. |
| 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. |
| AID1297711 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2016 | European journal of medicinal chemistry, Jun-30, Volume: 116 | Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID1077115 | Toxicity in Wistar rat assessed as total glutathione level in brain at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1272538 | Cytotoxicity against rat PC12 cells at 1 uM after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities. |
| AID1071355 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured after 5 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | 1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies. |
| AID1202687 | Inhibition of electric eel AChE pre-incubated for 3 mins before acetylthiocholine substrate addition by Ellman's reagent based spectrophotometry | 2015 | European journal of medicinal chemistry, Jun-05, Volume: 97 | Design, synthesis and anticholinesterase activity of novel benzylidenechroman-4-ones bearing cyclic amine side chain. |
| AID1164699 | Inhibition of AChE (unknown origin) | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. |
| AID25333 | Apparent dissociation constant of compound was evaluated; n.d. indicates not determined | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine. |
| AID44272 | In vitro inhibition of Butyrylcholinesterase from human plasma. | 1997 | Journal of medicinal chemistry, Oct-24, Volume: 40, Issue:22 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1784745 | Irreversible inhibition of recombinant equine serum BChE using butyrylthiocholine as substrate preincubated up to 120 mins by DTNB-reagent based 100-fold dilution assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT |
| AID350219 | Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10 | Lipophilicity of basic drugs measured by hydrophilic interaction chromatography. |
| AID1705940 | Cognitive enhancing effect in ICR mouse model of scopolamine-induced memory impairment assessed as reduction in time spent to found target at 15 mg/kg, po administered 30 mins prior to scopolamine injection by Morris water maze test | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Rational design and biological evaluation of a new class of thiazolopyridyl tetrahydroacridines as cholinesterase and GSK-3 dual inhibitors for Alzheimer's disease. |
| AID1198126 | Selectivity ratio of IC50 for human serum BuChE to IC50 for human erythrocyte AChE | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID1058678 | Cytotoxicity against human HSC assessed as cell viability at 20 uM after 24 hrs by MTT assay | 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. |
| AID241560 | Inhibitory concentration against human plasma Butyrylcholinesterase | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4 | Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine. |
| AID1480844 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity at 1 uM pretreated for 15 mins followed by APPH challenge measured every minute for 240 mins by ORAC-FL assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1075993 | Antioxidant activity assessed as inhibition of ABTS radical cation formation after 15 mins by ABTS radical scavenging method | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID1435918 | Cytotoxicity against human primary hepatocytes assessed as cell viability at 30 uM measured after 2 hrs by trypan blue assay relative to control | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy. |
| AID235632 | Selectivity index expressed as ratio (IC50 of BuChE) / (IC50 of total ChE) | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7 | Design, synthesis, and pharmacological profile of novel fused pyrazolo[4,3-d]pyridine and pyrazolo[3,4-b][1,8]naphthyridine isosteres: a new class of potent and selective acetylcholinesterase inhibitors. |
| AID1292349 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID241298 | Inhibition of Butyrylcholinesterase | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1 | Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation. |
| AID1186580 | Selectivity ratio of Ki for human BChE to Ki for human AChE | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aβ aggregation, and β-secretase. |
| AID1071761 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 30 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID1501299 | Metal chelating activity assessed as inhibition of Cu2+ mediated human amyloid beta (1 to 40) aggregation at 25 uM after 2 hrs by turbidity assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | A novel class of thiosemicarbazones show multi-functional activity for the treatment of Alzheimer's disease. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
| AID594990 | Inhibition of human BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity. |
| AID663257 | Hepatotoxicity in Sprague-Dawley rat assessed increase in alanine aminotransferase level in serum at 6 umol/100g of body weight, ip after 3 days | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID349046 | Inhibition of human recombinant BChE | 2008 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19 | Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity. |
| AID1442006 | Ratio of Kii for human OCT1-ASP+-inhibitor complex to Kis for human OCT1-inhibitor complex by Lineweaver-Burk plot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID1703582 | Permeability of the compound at pH 7.4 measured after 6 hrs by PAMPA method | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile. |
| 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). |
| AID315746 | Hepatotoxicity in Wistar rat liver assessed as tissue protein concentration at 5.93 umol, ip after 12 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1667721 | Selectivity index, ratio of IC50 for electric eel AchE using acetylthiocholine as substrate by Ellman's method to IC50 for equine BuchE using butyrylthiocholine as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening. |
| AID612151 | Inhibition of BChE by Ellman's method | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8 | Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors. |
| 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. |
| AID567064 | Inhibition of electric eel AChE after 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Synthesis, biological assessment and molecular modeling of new dihydroquinoline-3-carboxamides and dihydroquinoline-3-carbohydrazide derivatives as cholinesterase inhibitors, and Ca channel antagonists. |
| AID139844 | Compound was evaluated for the binding affinity by displacing [3H]oxotremorine from mouse cerebral cortex tissue. | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
| AID1869220 | Cytotoxicity against human SW480 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay | |||
| AID1168966 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation at 2 mM after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10 | Discovery of 3-Arylcoumarin-tetracyclic Tacrine Hybrids as Multifunctional Agents against Parkinson's Disease. |
| AID1201738 | Selectivity index, ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease. |
| AID729969 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate after 15 mins by Ellman's method | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease. |
| AID1311916 | Selectivity index, ratio of IC50 for equine BCHE to IC50 for electric eel ACHE | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID303071 | Inhibition of human Acetylcholinesterase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| AID1271543 | Hepatotoxicity in ICR mouse assessed as elevation in serum alanine aminotransferase level at 30 mg/kg, ig after 8 hrs by spectrophotometry analysis relative to control | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| 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. |
| AID1055219 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every 1 min by Ellman's method | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Synthesis and evaluation of multi-target-directed ligands against Alzheimer's disease based on the fusion of donepezil and ebselen. |
| AID1143504 | Inhibition of horse serum BChE using butyrylthiocholine iodide as substrate preincubated for 35 mins followed by enzyme addition measured after 3 mins by Ellman's method | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Structural modifications of 4-aryl-4-oxo-2-aminylbutanamides and their acetyl- and butyrylcholinesterase inhibitory activity. Investigation of AChE-ligand interactions by docking calculations and molecular dynamics simulations. |
| AID1351127 | Cytotoxicity against rat PC12 cells assessed as inhibition of cell viability at 10 uM by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1504318 | Inhibition of Electrophorus electricus AChE at 0.1 uM using acetylthiocholine iodide as substrate measured after 10 mins by Ellman's method relative to control | 2017 | Journal of natural products, 11-22, Volume: 80, Issue:11 | Targeted Isolation of Monoterpene Indole Alkaloids from Palicourea sessilis. |
| AID1378386 | Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay | 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. |
| AID1075991 | Inhibition of BuChE in human serum using butyrylthiocholine iodide as substrate measured every 30s for 5 mins by Ellman's spectrophotometric method | 2014 | European journal of medicinal chemistry, Mar-21, Volume: 75 | Synthesis, biological evaluation and molecular modeling study of novel tacrine-carbazole hybrids as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID729966 | Inhibition of recombinant human MAO-A using p-tyramine substrate preincubated for 15 mins before substrate addition measured after 20 mins by fluorescence assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease. |
| AID629646 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability at 30 uM after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12 | Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues. |
| AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1465116 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2017 | Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21 | 9-Substituted acridine derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors possessing antioxidant activity for Alzheimer's disease treatment. |
| AID1311915 | Inhibition of equine BCHE preincubated for 6 mins followed by addition of S-butyrylcholine iodide as substrate by Ellman's method | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin. |
| AID1279142 | Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins followed by substrate addition measured up to 180 secs by spectrophotometric-based Ellman's method | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7 | Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease. |
| AID366351 | Inhibition of Electrophorus electricus AChE by spectrophotometry | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID1292350 | Inhibition of horse serum BChE using butrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured for 10 mins by modified Ellman's method | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Biological evaluation of synthetic α,β-unsaturated carbonyl based cyclohexanone derivatives as neuroprotective novel inhibitors of acetylcholinesterase, butyrylcholinesterase and amyloid-β aggregation. |
| AID1330802 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID378483 | Inhibition of human AChE by Ellman's assay | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9 | Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana. |
| AID1653244 | Inhibition of VGCC (unknown origin) | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines. |
| AID724168 | Inhibition of acetylcholinesterase (unknown origin) | 2013 | Bioorganic & medicinal chemistry, Jan-01, Volume: 21, Issue:1 | Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase. |
| AID366352 | Inhibition of human erythrocyte AChE by Ellman's method | 2008 | Bioorganic & medicinal chemistry, Aug-15, Volume: 16, Issue:16 | New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties. |
| AID1241458 | Inhibition of electric eel AChE using acetylthiocholine iodide substrate by Ellman assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
| AID716438 | Hepatotoxicity against Wistar rat assessed as fatty degeneration of hepatocyte at 2 uM/100 gram of body weight, ip by histopathological analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID1456267 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured at 1 min interval for 3 mins by Ellmans method | |||
| AID1273118 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2016 | Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5 | Synthesis, molecular docking and biological evaluation of N,N-disubstituted 2-aminothiazolines as a new class of butyrylcholinesterase and carboxylesterase inhibitors. |
| AID1199520 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for Electrophorus electricus AChE | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID1077111 | Toxicity in Wistar rat assessed as kidney weight at 1 umol/100 g body weight, ip relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID349878 | Neuroprotective activity in human SH-SY5Y cells assessed as protection against KCl-induced cell death at 0.3 uM pretreated for 24 hrs before KCl challenge by lactate dehydrogenase assay relative to control | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1635490 | Neuroprotective activity against H2O2-induced oxidative damage in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID1382575 | Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation at 80 uM measured after 24 hrs by ThT fluorescence assay relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Novel Tacrine-Hydroxyphenylbenzimidazole hybrids as potential multitarget drug candidates for Alzheimer's disease. |
| AID1379222 | Cytotoxicity against human HepG2 cells assessed as cell viability at 50 uM after 24 hrs by MTT assay relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | New racemic annulated pyrazolo[1,2-b]phthalazines as tacrine-like AChE inhibitors with potential use in Alzheimer's disease. |
| AID31022 | Compound was evaluated for the in vitro inhibition of the Acetylcholinesterase (AChE) from human erythrocytes, | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID32720 | Inhibition acetylcholinesterase (AChE) enzyme. | 1997 | Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26 | Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications. |
| AID177101 | ED50 for salivation was defined as the dose required to produce a level 2 rating on a 0-4 point scale after treatment. | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID1635488 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 40 uM after 24 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID131755 | Tested for effective dose for elevation of Acetylcholinesterase (AChE) in mouse forebrain | 1994 | Journal of medicinal chemistry, Aug-19, Volume: 37, Issue:17 | Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase. |
| AID654684 | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholine chloride as substrate preincubated for 15 mins before substrate addition by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Design, synthesis and evaluation of isaindigotone derivatives as dual inhibitors for acetylcholinesterase and amyloid beta aggregation. |
| AID1338119 | Inhibition of recombinant human BACE1 expressed in baculovirus expression system at 50 uM using Rh-EVNLDAEFK-quencher as substrate after 60 mins by spectrofluorometric method relative to control | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation. |
| AID1851405 | Inhibition of human serum recombinant BChE using butyrylthiocholine iodide as a substrate incubated for 20 mins by DTNB reagent based Ellman's method | |||
| AID1558587 | Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells at 10 uM by radioligand binding assay relative to control | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID1555975 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by Ellman's method | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Design, synthesis, and biological evaluation of rutacecarpine derivatives as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| 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. |
| AID1698853 | Inhibition of human BuChE at 10 uM | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Rapid discovery of a selective butyrylcholinesterase inhibitor using structure-based virtual screening. |
| AID183622 | Concentration required to potentiate the contraction of isolated rat ileum produced by 1*10e-7 M ACh by 20 percent | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1635486 | Inhibition of human erythrocyte AChE-induced Abeta (1 to 42) aggregation at 10 uM incubated for 24 hrs by thioflavin-T fluorescence assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Benzylpiperidine-Linked Diarylthiazoles as Potential Anti-Alzheimer's Agents: Synthesis and Biological Evaluation. |
| AID142658 | Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1271532 | Hepatotoxicity in ICR mouse assessed as serum alanine aminotransferase level at 30 mg/kg, ig after 22 hrs by spectrophotometry analysis (Rvb = 40.1 +/- 9.9 U/L) | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1728635 | Hepatotoxicity in human HepG2 cells assessed as increase in ROS accumulation by measuring increase in green fluorescence at 50 uM measured after 24 hrs by ROS tracker based laser confocal microscopic analysis | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID692186 | Therapeutic index, ratio of Cmax in human to IC50 for human OCT1 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13 | Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. |
| AID1651259 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis and anti-Alzheimer's disease activity study of xanthone derivatives based on multi-target strategy. |
| AID31637 | Selectivity towards acetylcholinesterase over butyrylcholinesterase | 2003 | Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine. |
| AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
| 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. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
| AID1361156 | Inhibition of recombinant human serum BChE using butyrylthiocholine as substrate pretreated for 20 mins followed by substrate addition by Ellman's method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease. |
| AID1199518 | Inhibition of Electrophorus electricus AChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID44299 | IC50 (hBuChE/hAChE) ratio of the compound | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
| AID1480842 | Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation at 20 uM after 48 hrs by thioflavin T fluorescence assay relative to control | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment. |
| AID1879291 | Inhibition of BuchE (unknown origin) at 10 uM relative to control | 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. |
| AID547622 | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID1167623 | Inhibition of equine serum BChE using S-butyrylthiocholine chloride as substrate incubated for 6 mins by spectrophotometric method | 2014 | Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21 | Design, synthesis and evaluation of novel tacrine-(β-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease. |
| AID141204 | Antagonistic potency against Muscarinic acetylcholine receptor M3 (10 uM); nd= Not determined | 1998 | Journal of medicinal chemistry, Oct-22, Volume: 41, Issue:22 | Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease. |
| AID600117 | Inhibition of human recombinant AChE-induced amyloid beta (1-40) aggregation assessed as fibril formation at 100 uM by thioflavin T-based fluorometric assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation. |
| AID1751084 | Inhibition of equine serum BuChE by Ellman's method | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of novel deoxyvasicinone-indole as multi-target agents for Alzheimer's disease. |
| AID1682154 | In vivo inhibition of acetylcholinesterase in rat at 0.068 micromol/kg, icv relative to control | 2020 | Bioorganic & medicinal chemistry, 12-15, Volume: 28, Issue:24 | Pyridine alkaloids with activity in the central nervous system. |
| AID31783 | Inhibition of Acetylcholinesterase in mouse red blood cell | 1996 | Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15 | Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology. |
| AID656041 | Inhibition of human erythrocytes AChE by Ellman's method | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and β-amyloid-reducing properties. |
| AID1292255 | Inhibition of AChE (unknown origin) using acetylcholine iodate as substrate preincubated for 10 mins followed by substrate addition by Lineweaver-Burk plot analysis | 2016 | Bioorganic & medicinal chemistry, 05-15, Volume: 24, Issue:10 | Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds. |
| AID404844 | Inhibition of human serum BChE by Ellman's assay | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12 | Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation. |
| AID1728619 | Induction of apoptosis in human SH-SY5Y cells assessed as early apoptotic cells at 5 uM incubated for 24 hrs by annexin V FITC/propidium iodide staining based flow cytometry (Rvb = 1.3 %) | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
| AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1557447 | Inhibition of electric eel AChE using acetylthiocholine preincubated for 10 mins followed by addition of substrate and measured every 30 secs for 20 mins | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Current and emerging therapeutic targets of alzheimer's disease for the design of multi-target directed ligands. |
| AID761300 | Inhibition of amyloid beta (1 to 42) (unknown origin) aggregation at 50 uM after 24 hrs by thioflavin-T dye-based fluorescence assay relative to control | 2013 | Bioorganic & medicinal chemistry, Aug-01, Volume: 21, Issue:15 | Design, synthesis and neuroprotective evaluation of novel tacrine-benzothiazole hybrids as multi-targeted compounds against Alzheimer's disease. |
| AID654683 | Inhibition of electric eel acetylcholinesterase using acetylcholine chloride as substrate preincubated for 15 mins before substrate addition by Ellman's method | 2012 | Bioorganic & medicinal chemistry, Apr-15, Volume: 20, Issue:8 | Design, synthesis and evaluation of isaindigotone derivatives as dual inhibitors for acetylcholinesterase and amyloid beta aggregation. |
| AID716201 | Hepatotoxicity activity in Wistar rat assessed as increase in tissue content of TBARS at 6 uM/100 gram of body weight, ip after 24 hrs | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID31010 | In vitro inhibition of Torpedo californica acetylcholinesterase. | 1999 | Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4 | Aminopyridazines as acetylcholinesterase inhibitors. |
| AID1077125 | Toxicity in Wistar rat assessed as ethoxycoumarin-O-deethylation activity in liver measured as 7-hydroxycoumarin level at 1 umol/100 g body weight, ip by fluorometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID302146 | Inhibition of bovine erythrocytes AChE by Ellman's method | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | New potent acetylcholinesterase inhibitors in the tetracyclic triterpene series. |
| AID747770 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 5 mins by Ellman's method | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11 | NO-donating tacrine derivatives as potential butyrylcholinesterase inhibitors with vasorelaxation activity. |
| 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. |
| AID679752 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Tacrine: 100 uM) in MDR1-expressing MDCKII cells | 2002 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3 | Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. |
| AID1542249 | Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate pre-incubated for 20 mins before substrate addition and measured for 180 secs by spectrophotometry based Ellman's method | 2019 | European journal of medicinal chemistry, Apr-01, Volume: 167 | Tackling neuroinflammation and cholinergic deficit in Alzheimer's disease: Multi-target inhibitors of cholinesterases, cyclooxygenase-2 and 15-lipoxygenase. |
| AID539470 | Solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
| AID1077127 | Toxicity in Wistar rat assessed as ethylmorphine-N-demethylation activity in liver measured as formaldehyde level at 1 umol/100 g body weight, ip by photometric analysis relative to control | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Design, synthesis and biological evaluation of D-ring opened galantamine analogs as multifunctional anti-Alzheimer agents. |
| AID1198124 | Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID1570273 | Inhibition of AChE (unknown origin) by spectrophotometric analysis | 2019 | European journal of medicinal chemistry, Oct-15, Volume: 180 | Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships. |
| AID1882054 | Selectivity ratio of IC50 for recombinant bovine mitochondrial MAO-B to IC50 for recombinant bovine mitochondrial MAO-A | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Research progress in pharmacological activities and structure-activity relationships of tetralone scaffolds as pharmacophore and fluorescent skeleton. |
| AID44285 | Ex vivo inhibition of human plasma Butyrylcholinesterase. | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17 | Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines. |
| AID1217727 | Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
| AID1581642 | Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | 1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease. |
| AID1558577 | Inhibition of human BChE | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID378482 | Inhibition of electric eel AChE by Ellman's assay | 2006 | Journal of natural products, Sep, Volume: 69, Issue:9 | Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana. |
| AID776490 | Selectivity index, ratio of IC50 for equine serum BuChE to IC50 for electric eel AChE | 2013 | European journal of medicinal chemistry, Nov, Volume: 69 | Multifunctional tacrine-flavonoid hybrids with cholinergic, β-amyloid-reducing, and metal chelating properties for the treatment of Alzheimer's disease. |
| AID283051 | Inhibition of acetylcholinesterase | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Random chemistry as a new tool for the generation of small compound libraries: development of a new acetylcholinesterase inhibitor. |
| AID18767 | LD50 for actute lethality is defined as the dose that resulted in the death of 50% of the animals 1 hr after treatment. | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID349882 | Selectivity ratio of IC50 for human serum BChE to IC50 for human serum AChE | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1324825 | Inhibition of horse serum BChE using BTC as substrate preincubated for 15 mins followed by substrate addition by UV-spectrophotometric analysis | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents. |
| AID262754 | Anticholinesterase activity against human erythrocyte AChE | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7 | Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. |
| AID1656480 | Inhibition of Torpedo californica AChE using acetylthiocholine chloride as substrate peincubated for 15 mins followed by substrate addition measured after 5 mins 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. |
| AID1317852 | Inhibition of electric eel AChE preincubated for 5 mins followed by addition of acetylthiocholine iodide as substrate measured after 2 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Aug-25, Volume: 119 | Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies. |
| AID1442005 | Competitive inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of metformin after 2 mins by Lineweaver-Burk plot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID44304 | Inhibition ratio, (IC50 for human BChE activity) / (IC50 for bovine AChE activity) | 1999 | Journal of medicinal chemistry, Aug-26, Volume: 42, Issue:17 | Synthesis, in vitro pharmacology, and molecular modeling of very potent tacrine-huperzine A hybrids as acetylcholinesterase inhibitors of potential interest for the treatment of Alzheimer's disease. |
| AID657789 | Inhibition of human AChE-induced amyloid beta 40 aggregation at 100 uM after 24 hrs by thioflavin T fluorescence method | 2012 | European journal of medicinal chemistry, Jun, Volume: 52 | Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine. |
| AID412871 | Hepatotoxicity in Wistar rat liver assessed as aspartate aminotransferase activity after 24 to 36 hrs | 2008 | Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24 | NO-donating tacrine hybrid compounds improve scopolamine-induced cognition impairment and show less hepatotoxicity. |
| AID744300 | Cytotoxicity against human SH-SY5Y cells assessed as cell viability after 48 hrs by MTT assay | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Synthesis and evaluation of 7,8-dehydrorutaecarpine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
| AID303070 | Inhibition of Torpedo californica Acetylcholinesterase | 2007 | Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23 | First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. |
| AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID526833 | Inhibition of equine BChE after 15 mins by Ellman's method using butyrylcholine as substrate | 2010 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22 | Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase. |
| AID1414493 | Permeability of the compound at 100 uM after 3 to 6 hrs by PAMPA assay | 2018 | Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23 | Pyridinium Oximes with Ortho-Positioned Chlorine Moiety Exhibit Improved Physicochemical Properties and Efficient Reactivation of Human Acetylcholinesterase Inhibited by Several Nerve Agents. |
| AID1164695 | Inhibition of amyloid beta (1-42) self-mediated aggregation (unknown origin) at 10 uM after 8 to 48 hrs by thioflavin T fluorescence method | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor. |
| AID1199521 | Inhibition of human recombinant AChE after 5 mins by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase and β-amyloid aggregation inhibitors with neuroprotective properties. |
| AID1071751 | Hepatotoxicity against human HepG2 cells assessed as LDH release | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID404434 | Inhibition of Torpedo californica 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. |
| AID689066 | Antioxidant activity assessed as trolox equivalents of peroxyl radical scavenging activity at 0.5 to 10 uM after 10 mins by ORAC-FL assay | 2012 | Bioorganic & medicinal chemistry, Oct-01, Volume: 20, Issue:19 | O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-β aggregation. |
| 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. |
| AID1198125 | Inhibition of human serum BuChE using S-butyrylthiocholine iodide as substrate preincubated for 6 mins before substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID663236 | Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 5 mins prior to substrate addition measured every 3 mins by Ellman's assay | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID1704813 | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI cells using p-tyramine as substrate by fluorometric assay | |||
| AID1071764 | Hepatotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by MTT assay relative to control | 2014 | European journal of medicinal chemistry, Mar-03, Volume: 74 | Toxicological and pharmacological evaluation, antioxidant, ADMET and molecular modeling of selected racemic chromenotacrines {11-amino-12-aryl-8,9,10,12-tetrahydro-7H-chromeno[2,3-b]quinolin-3-ols} for the potential prevention and treatment of Alzheimer's |
| AID272366 | Inhibition of bovine erythrocyte AChE after 45 mins | 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. |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID384079 | Inhibition of horse serum butyrylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay | 2008 | European journal of medicinal chemistry, Mar, Volume: 43, Issue:3 | Chemiluminescent high-throughput microassay applied to imidazo[2,1-b]thiazole derivatives as potential acetylcholinesterase and butyrylcholinesterase inhibitors. |
| AID1558570 | Inhibition of human BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured for 3 mins by spectrophotometry based Ellman's method | 2019 | Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20 | Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo. |
| AID639367 | Inhibition of BuChE in horse serum using butyrylthiocholine as substrate by Ellman method | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6 | N-acylaminophenothiazines: neuroprotective agents displaying multifunctional activities for a potential treatment of Alzheimer's disease. |
| AID590994 | Inhibition of Electrophorus electricus acetylcholinesterase preincubated with compound for 10 mins using acetylcholine iodide as substrate after 15 mins by spectrophotometric analysis | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Synthesis, biological assessment and molecular modeling of 14-aryl-10,11,12,14-tetrahydro-9H-benzo[5,6]chromeno[2,3-b]quinolin-13-amines. |
| AID44437 | Butyrylcholinesterase | 1995 | Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24 | Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. |
| AID663976 | Inhibition of electric eel AChE preincubated for 10 mins measured after 15 mins by Ellman's method | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and pharmacological assessment of diversely substituted pyrazolo[3,4-b]quinoline, and benzo[b]pyrazolo[4,3-g][1,8]naphthyridine derivatives. |
| AID1729625 | Inhibition of human BuChE using butyrylthiocholine iodide as substrate peincubated for 5 mins followed by substrate addition by DTNB-reagent based Ellman's method | 2021 | European journal of medicinal chemistry, Jan-15, Volume: 210 | Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT |
| AID458979 | Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO cells in ternary complex by EATCM analysis | 2010 | Journal of medicinal chemistry, Mar-11, Volume: 53, Issue:5 | Hybrid molecules from xanomeline and tacrine: enhanced tacrine actions on cholinesterases and muscarinic M1 receptors. |
| AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
| AID458511 | Inhibition of horse serum BChE by Ellman's method | 2010 | Bioorganic & medicinal chemistry, Feb, Volume: 18, Issue:3 | 4-Aryl-4-oxo-N-phenyl-2-aminylbutyramides as acetyl- and butyrylcholinesterase inhibitors. Preparation, anticholinesterase activity, docking study, and 3D structure-activity relationship based on molecular interaction fields. |
| AID289391 | Inhibition of Electrophorus electricus AChE by Ellman's method | 2007 | Bioorganic & medicinal chemistry, Oct-15, Volume: 15, Issue:20 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abeta1-42 aggregation for Alzheimer's disease therapeutics. |
| AID1183482 | Inhibition of horse serum BChE by spectrophotometry based Ellman's method | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Synthesis and cholinesterase inhibition of cativic acid derivatives. |
| AID315741 | Hepatotoxicity in Wistar rat serum assessed as albumin level at 5.93 umol, ip after 20 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1267382 | Selectivity ratio of IC50 for horse serum BuChE to IC50 for electric eel AChE | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents. |
| AID139999 | Percent elevation of ACh level in mouse forebrain following intraperitoneal administration at a dose of 3.4 mg/kg | 1992 | Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8 | Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues. |
| AID1759897 | Inhibition of human plasmatic BuChE assessed as reduction in cholinesterase activity by Ellman's method | 2021 | European journal of medicinal chemistry, Jul-05, Volume: 219 | Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors. |
| AID1190808 | Selectivity index, ratio of horse serum BuChE to IC50 for electric eel AChE | 2015 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4 | Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of AD. |
| AID1450069 | Inhibition of recombinant human CYP1A2 expressed in insect cells at 1 uM using EOMCC as substrate pretreated for 10 mins followed by substrate addition measured every minute for 15 mins in presence of NADP+ by fluorescence assay relative to control | 2017 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 27, Issue:11 | Cytochrome P450 binding studies of novel tacrine derivatives: Predicting the risk of hepatotoxicity. |
| AID1917488 | Inhibition of human recombinant AChE using S-acetylthiocholine as substrate by DTNB reagent based spectrophotometric analysis | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Isatoic anhydrides as novel inhibitors of monoamine oxidase. |
| AID729965 | Inhibition of recombinant human MAO-B using p-benzylamine substrate preincubated for 15 mins before substrate addition measured after 20 mins by fluorescence assay | 2013 | European journal of medicinal chemistry, Apr, Volume: 62 | A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease. |
| AID1651260 | Inhibition of equine serum BChE using butyrylthiocholine as substrate by Ellman's method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis and anti-Alzheimer's disease activity study of xanthone derivatives based on multi-target strategy. |
| AID714721 | Neuroprotective activity in 30 uM rotenone and 10 uM oligomycin-treated Wistar rat primary cortical neurons assessed as cell viability at 50 uM after 24 hrs by XTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID1272540 | Cytotoxicity against human HepG2 cells at 1 uM after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | Design, synthesis and evaluation of novel 7-aminoalkyl-substituted flavonoid derivatives with improved cholinesterase inhibitory activities. |
| AID282825 | Inhibition of human serum BChE | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23 | Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease. |
| AID1335931 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-3 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID314091 | Inhibition of human AchE | 2008 | Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3 | Multi-target-directed ligands to combat neurodegenerative diseases. |
| 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. |
| AID1575666 | Antioxidant activity assessed as DPPH radical scavenging activity up to 250 uM after 30 mins under dark condition by spectrophotometric analysis | 2019 | MedChemComm, May-01, Volume: 10, Issue:5 | Synthesis of novel vanillin derivatives: novel multi-targeted scaffold ligands against Alzheimer's disease. |
| AID1310667 | Neurotoxicity in human SH-SY5Y cells assessed as cell viability at 5 uM after 24 hrs by XTT assay relative to control | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Potent anticholinesterasic and neuroprotective pyranotacrines as inhibitors of beta-amyloid aggregation, oxidative stress and tau-phosphorylation for Alzheimer's disease. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
| AID771359 | Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins prior to substrate addition by Ellman's method | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Design, synthesis, docking study and biological evaluation of some novel tetrahydrochromeno [3',4':5,6]pyrano[2,3-b]quinolin-6(7H)-one derivatives against acetyl- and butyrylcholinesterase. |
| AID1324822 | Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation at 20 uM after 48 hrs by thioflavin T fluorescence assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | Design, synthesis and evaluation of 4-dimethylamine flavonoid derivatives as potential multifunctional anti-Alzheimer agents. |
| AID1379560 | Inhibition of human AChE pre-incubated for 6 mins before ATCI substrate addition and measured after 12 mins by DTNB reagent dependent UV-Vis spectrophotometry based Ellman's method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Novel deoxyvasicinone derivatives as potent multitarget-directed ligands for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation. |
| AID142799 | Binding affinity against mouse M2 muscarinic receptor using heart tissue and [3H]N-methylscopolamine | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID1193155 | Inhibition of human recombinant AChE pre-incubated for 5 mins before addition of acetylthiocholine iodide substrate by Ellman's assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7 | Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents. |
| AID1335936 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10'-7 M preincubated for 15 mins followed by substrate addition and measured for 5 mins by Ellmans method | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis of new donepezil analogues and investigation of their effects on cholinesterase enzymes. |
| AID188755 | Number of circlings observed for 30 min at 3 mg/kg orally administered dose in rats | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID1459903 | Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by Ellman's method | 2017 | European journal of medicinal chemistry, Jan-05, Volume: 125 | Novel tacrine-1,2,3-triazole hybrids: In vitro, in vivo biological evaluation and docking study of cholinesterase inhibitors. |
| AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
| AID1653242 | Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate by Ellman's methods | 2019 | European journal of medicinal chemistry, Mar-15, Volume: 166 | Tacrines for Alzheimer's disease therapy. III. The PyridoTacrines. |
| AID44287 | In vitro inhibition of Butyrylcholinesterase from human erythrocytes | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID229561 | Ratio of IC50(M2 Receptor) to IC50(M1 Receptor) | 1992 | Journal of medicinal chemistry, Aug-21, Volume: 35, Issue:17 | Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
| AID116900 | Compound was evaluated for the cholinergic activity by the induction of amnesia at high toxic doses and lethal dose was determined | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
| AID1609489 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate by Ellman's method | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Neurobehavioral investigation and acetylcholinesterase inhibitory activity study for some new coumarin derivatives. |
| AID32094 | Inhibitory activity against acetylcholinesterase in rat striatal preparation | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID707698 | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| 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. |
| AID32279 | In vitro inhibitory activity against acetylcholinesterase | 1992 | Journal of medicinal chemistry, Feb-07, Volume: 35, Issue:3 | QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. |
| AID1409657 | Hepatotoxicity in ICR mouse assessed as serum ALT activity at 30 mg/kg, administered intragastrically measured 8 hrs post dose (Rvb = 35 +/- 8.4 U/L) | |||
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7 | Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID1879286 | Inhibition of BuchE (unknown origin) | 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. |
| 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. |
| AID1174273 | Inhibition of equine serum BuChE using butylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method | 2015 | European journal of medicinal chemistry, Jan-07, Volume: 89 | New tetracyclic tacrine analogs containing pyrano[2,3-c]pyrazole: efficient synthesis, biological assessment and docking simulation study. |
| AID1271505 | Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2016 | Journal of medicinal chemistry, Jan-14, Volume: 59, Issue:1 | Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography. |
| AID1330753 | Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured up to 3 mins by Ellman's method | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease. |
| AID1351113 | Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition measured every minute by Ellman's method | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Development of tacrine-bifendate conjugates with improved cholinesterase inhibitory and pro-cognitive efficacy and reduced hepatotoxicity. |
| AID1186583 | Inhibition of human recombinant AChE pre-incubated for 5 mins before acetylthiocholine substrate addition by Ellman's method | 2014 | Journal of medicinal chemistry, Aug-28, Volume: 57, Issue:16 | Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors. |
| AID1761236 | Permeability of compound at pH 7.4 measured after 6 hrs by PAMPA assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | 2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease. |
| AID32109 | Inhibitory dose for anticholinesterase activity by ex vivo determination in rat forebrain after intraperitoneal administration | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
| AID1379229 | Inhibition of electric eel AChE at 200 nM using acetylthiocholine as substrate preincubated for 20 mins followed by substrate addition measured every 2 mins for 20 mins by Ellman's method relative to control | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation. |
| AID1330798 | Inhibition of soybean 15-LOX type 1B assessed as reduction in conversion of linoleic acid to 13-hydroperoxylinoleic acid incubated for 5 mins followed by substrate addition measured for 1 min by spectrophotometric analysis | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX. |
| AID1515532 | Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition and measured every 30 secs for 1 hr by Ellman's assay | 2019 | Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2 | Leucoflavonine, a new bioactive racemic flavoalkaloid from the leaves of Leucosceptrum canum. |
| AID1409650 | Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability after 48 hrs by MTT assay | |||
| AID315742 | Hepatotoxicity in Wistar rat serum assessed as albumin level at 5.93 umol, ip after 36 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1071357 | Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition by Ellman's method | 2014 | European journal of medicinal chemistry, Feb-12, Volume: 73 | 1,2,3,4-Tetrahydrobenzo[h][1,6]naphthyridines as a new family of potent peripheral-to-midgorge-site inhibitors of acetylcholinesterase: synthesis, pharmacological evaluation and mechanistic studies. |
| AID1576568 | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2019 | MedChemComm, Dec-01, Volume: 10, Issue:12 | Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling. |
| AID594255 | Inhibition of equine serum BChE by Ellman's method | 2011 | European journal of medicinal chemistry, May, Volume: 46, Issue:5 | Syntheses and characterization of novel oxoisoaporphine derivatives as dual inhibitors for cholinesterases and amyloid beta aggregation. |
| AID1198137 | Hepatotoxicity in Sprague-Dawley rat assessed as large area of necrosis at 6 umol/100g body weight, ip measured after 24 hrs by histomorphological study | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties. |
| AID681116 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells | 2002 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3 | Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. |
| AID659699 | Inhibition of amyloid beta (1 to 42) self aggregation after 48 hrs by thioflavin T fluorescence assay | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids. |
| AID1810904 | Binding affinity to human serum BChE assessed as half life | |||
| AID1845457 | Inhibition of AchE (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1 | Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery? |
| AID714528 | Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging activity incubated for 15 mins prior to AAPH induction measured every 1 min for 80 mins by ORAC-FL assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease. |
| AID716446 | Toxicity in ip dosed Wistar rat assessed per 100 g body weight | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Tacrine-silibinin codrug shows neuro- and hepatoprotective effects in vitro and pro-cognitive and hepatoprotective effects in vivo. |
| AID274651 | Inhibition of human serum BuChE | 2006 | Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26 | Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease. |
| 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. |
| AID170028 | Peripheral cholinergic effects in male wistar rats when administered orally at a dose of 30 mg/Kg. | 1994 | Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15 | Central cholinergic agents. 6. Synthesis and evaluation of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-benzazepi n-8-yl)-1-propanones and their analogs as central selective acetylcholinesterase inhibitors. |
| AID315744 | Hepatotoxicity in Wistar rat serum assessed as lactate dehydrogenase level at 5.93 umol, ip after 20 hrs relative to control | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4 | Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates. |
| AID1361155 | Inhibition of recombinant human AChE expressed in HEK293 cells using acetylthiocholine as substrate pretreated for 20 mins followed by substrate addition by Ellman's method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Tacripyrimidines, the first tacrine-dihydropyrimidine hybrids, as multi-target-directed ligands for Alzheimer's disease. |
| AID707697 | Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP at 10 uM after 30 mins by scintillation counting | 2012 | Journal of medicinal chemistry, Nov-08, Volume: 55, Issue:21 | Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B. |
| 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. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID31169 | In vitro inhibition of Acetylcholinesterase from human erythrocytes | 1995 | Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15 | 5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety. |
| AID196038 | Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation | 1996 | Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2 | Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease. |
| AID1379236 | Hepatotoxicity against human HepG2 cells assessed as reduction in cell viability at 100 to 300 uM after 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Novel tacrine derivatives exhibiting improved acetylcholinesterase inhibition: Design, synthesis and biological evaluation. |
| AID349871 | Inhibition of electric eel AChE by Rappaport method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID604026 | Unbound CSF to plasma concentration ratio in human | 2009 | Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20 | Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. |
| AID1768735 | Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE | 2021 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 49 | Design, synthesis and biological evaluation of naringenin carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease. |
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| AID1382561 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1.25 uM after 24 hrs by MTT assay relative to control | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
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| AID196789 | Ratio of the concentrations of the test compound and dequalinium that cause 50% inhibition, as determined in the same experiment was reported. (number of neurons tested, n=3). Insufficient activity at this concentration | 1995 | Journal of medicinal chemistry, Feb-17, Volume: 38, Issue:4 | Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle. |
| AID1728621 | Induction of apoptosis in human SH-SY5Y cells assessed as necrotic cells at 5 uM incubated for 24 hrs by annexin V FITC/propidium iodide staining based flow cytometry (Rvb = 0.8 %) | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | ROS-responsive and multifunctional anti-Alzheimer prodrugs: Tacrine-ibuprofen hybrids via a phenyl boronate linker. |
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| AID44288 | Inhibition of butyrylcholinesterase from human serum | 2001 | Journal of medicinal chemistry, Aug-16, Volume: 44, Issue:17 | Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. |
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| AID111983 | Reversal of scopolamine-induced memory impairment in mice at 0.31 mg/Kg administered subcutaneously. | 1989 | Journal of medicinal chemistry, Aug, Volume: 32, Issue:8 | 9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics. |
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| AID594820 | Inhibition of AChE-induced amyloid beta aggregation | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9 | (+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase. |
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| AID114807 | Compound was evaluated for the cholinergic activity in vivo in mice, by administering the compound intraperitoneally and observation of the salivation was made after 30 min. | 1994 | Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5 | Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity. |
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| AID548344 | Inhibition of equine serum BuChE by Ellman's method | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Old phenothiazine and dibenzothiadiazepine derivatives for tomorrow's neuroprotective therapies against neurodegenerative diseases. |
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| AID404430 | Ratio of Ki for human recombinant AChE to Ki for human recombinant 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. |
| AID663254 | Hepatotoxicity in Sprague-Dawley rat assessed increase in aminotransferase level in serum at 6 umol/100g of body weight, ip after 36 hrs | 2012 | Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7 | Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases. |
| AID1663425 | Antialzheimer activity in scopolamine-induced impairment in ICR mouse assessed as total distance to platform at 15 mg/kg, ip administered once a day for 10 days pretreated with scopolamine for 30 mins and measured at 5th day of training session by Morris | 2020 | Bioorganic & medicinal chemistry, 06-15, Volume: 28, Issue:12 | Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity. |
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| AID1382541 | Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by DTNB addition for 5 mins and subsequent addition of substrate measured after 3 mins by Ellman's method | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Synthesis and activity towards Alzheimer's disease in vitro: Tacrine, phenolic acid and ligustrazine hybrids. |
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| AID1667715 | Cytotoxicity against human SH-SY5Y cells at 100 uM by MTT assay relative to control | 2020 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9 | Discovery of 9-phenylacridinediones as highly selective butyrylcholinesterase inhibitors through structure-based virtual screening. |
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| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
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| AID1801052 | Cholinesterase Inhibition Assay from Article 10.1016/j.bioorg.2015.05.005: \\Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis.\\ | 2015 | Bioorganic chemistry, Aug, Volume: 61 | Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis. |
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| AID1796459 | Enzyme Inhibition Assay from Article 10.1074/jbc.271.39.23646: \\Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease.\\ | 1996 | The Journal of biological chemistry, Sep-27, Volume: 271, Issue:39 | Highly potent, selective, and low cost bis-tetrahydroaminacrine inhibitors of acetylcholinesterase. Steps toward novel drugs for treating Alzheimer's disease. |
| AID1799778 | Radiochemical Assay from Article 10.1074/jbc.M111.290619: \\Thermodynamic evaluation of ligand binding in the plant-like phosphoethanolamine methyltransferases of the parasitic nematode Haemonchus contortus.\\ | 2011 | The Journal of biological chemistry, Nov-04, Volume: 286, Issue:44 | Thermodynamic evaluation of ligand binding in the plant-like phosphoethanolamine methyltransferases of the parasitic nematode Haemonchus contortus. |
| AID1799711 | Enzyme Assay from Article 10.1016/j.bioorg.2011.05.001: \\Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors.\\ | 2011 | Bioorganic chemistry, Aug, Volume: 39, Issue:4 | Synthesis and biological activity of derivatives of tetrahydroacridine as acetylcholinesterase inhibitors. |
| AID1798999 | Measurement of hAChE Activity from Article 10.1021/jm801292b: \\Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.\\ | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease. |
| AID1802939 | Acetylcholinesterase Inhibition Assay from Article 10.3109/14756360903213481: \\Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesovu00E1 27/97.\\ | 2010 | Journal of enzyme inhibition and medicinal chemistry, Jun, Volume: 25, Issue:3 | Nostotrebin 6, a bis(cyclopentenedione) with cholinesterase inhibitory activity isolated from Nostoc sp. str. Lukesová 27/97. |
| AID1800423 | Assay of Substrate Hydrolysis from Article 10.1021/bi401043w: \\The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity.\\ | 2013 | Biochemistry, Oct-22, Volume: 52, Issue:42 | The natural product dihydrotanshinone I provides a prototype for uncharged inhibitors that bind specifically to the acetylcholinesterase peripheral site with nanomolar affinity. |
| AID1796284 | Cholinesterase Inhibition Assay from Article 10.1016/s0968-0896(99)00306-5: \\Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivativ | 2000 | Bioorganic & medicinal chemistry, Mar, Volume: 8, Issue:3 | Acetylcholinesterase inhibitors for potential use in Alzheimer's disease: molecular modeling, synthesis and kinetic evaluation of 11H-indeno-[1,2-b]-quinolin-10-ylamine derivatives. |
| AID1796451 | Enzyme Inhibition Assay from Article 10.1016/s0968-0896(98)00133-3: \\Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series.\\ | 1998 | Bioorganic & medicinal chemistry, Oct, Volume: 6, Issue:10 | Potent acetylcholinesterase inhibitors: design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series. |
| 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. |
| 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. |
| AID1801604 | AChE Inhibition Assay from Article 10.1016/j.bioorg.2015.12.002: \\Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives.\\ | 2016 | Bioorganic chemistry, Apr, Volume: 65 | Synthesis and anti-acetylcholinesterase activity of scopoletin derivatives. |
| AID1796462 | Enzyme Inhibition Assay from Article 10.1021/jm010826r: \\A structure-based design approach to the development of novel, reversible AChE inhibitors.\\ | 2001 | Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20 | A structure-based design approach to the development of novel, reversible AChE inhibitors. |
| AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
| AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
| AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2005 | Journal of molecular biology, Oct-21, Volume: 353, Issue:2 | Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2005 | Journal of molecular biology, Oct-21, Volume: 353, Issue:2 | Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2001 | Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20 | A structure-based design approach to the development of novel, reversible AChE inhibitors. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1345358 | Mouse M2 receptor (Acetylcholine receptors (muscarinic)) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1345946 | Human acetylcholinesterase (Cartwright blood group) (Hydrolases) | 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. |
| AID1345244 | Mouse M1 receptor (Acetylcholine receptors (muscarinic)) | 1992 | Journal of medicinal chemistry, Mar-20, Volume: 35, Issue:6 | Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine. |
| AID1345972 | Human butyrylcholinesterase (Hydrolases) | 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. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2003 | Chemistry & biology, Apr, Volume: 10, Issue:4 | Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2003 | Chemistry & biology, Apr, Volume: 10, Issue:4 | Crystal structure of human carboxylesterase 1 complexed with the Alzheimer's drug tacrine: from binding promiscuity to selective inhibition. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 168 (8.19) | 18.7374 |
| 1990's | 739 (36.03) | 18.2507 |
| 2000's | 440 (21.45) | 29.6817 |
| 2010's | 540 (26.33) | 24.3611 |
| 2020's | 164 (8.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (56.58) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 161 (7.52%) | 5.53% |
| Reviews | 231 (10.79%) | 6.00% |
| Case Studies | 29 (1.35%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,720 (80.34%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Prospective Randomized Controlled 4-arm Study for the Evaluation of 4 Surgical Techniques in Primary Total Hip Arthroplasty [NCT01031732] | 120 participants (Anticipated) | Interventional | 2009-11-30 | Recruiting | |||
| Is Ceramic-on-Ceramic THA Superior to Ceramic-on-Highly Cross-Linked Polyethylene THA in Patients Less Than 55 Years Old? [NCT03639532] | Phase 4 | 148 participants (Actual) | Interventional | 2000-01-01 | Completed | ||
| In Vivo Determination of Total Hip Arthroplasty (THA) Kinematics and Sound for Subjects for Normal, Diseased and Implanted Hips [NCT02682602] | 21 participants (Actual) | Observational | 2016-04-30 | Completed | |||
| Fixation of OsseoTi™ Porous Structure Versus PPS (Porous Plasma Spray) Coating on the G7™ Acetabular Component for Primary Total Hip Arthroplasty: A Single-Blinded Randomized Controlled Trial Evaluating Implant Migration, Acetabular Liner Wear, and Patien [NCT02316704] | 98 participants (Anticipated) | Interventional | 2014-12-31 | Active, not recruiting | |||
| Ceramic-on-Ceramic Total Hip Arthroplasty and Squeaking: A Prospective, Blinded, Randomized Clinical Trial of Influence of Component Design [NCT01420900] | 204 participants (Actual) | Interventional | 2011-09-30 | Completed | |||
| Etude de Cohorte Observationnelle Rétrospective SYMBOL CUP 2 [NCT04209426] | 20 participants (Actual) | Observational | 2015-03-18 | Completed | |||
| Effectiveness of Fast-track Clinical Pathway on Minimally-invasive Total Hip Arthroplasty Surgery in NTUH [NCT04145921] | 75 participants (Actual) | Interventional | 2014-01-07 | Completed | |||
| Tacrine Effects on Cocaine Self-Administration and Pharmacokinetics [NCT01406522] | Phase 2 | 0 participants (Actual) | Interventional | 2012-10-31 | Withdrawn(stopped due to One of the study medications, tacrine, is no longer clinically available) | ||
| Dynamic Range of Motion (ROM) Assessment Using Gait Analysis and Three-dimensional Fluoroscopy in Patients Treated by Total Hip Arthroplasty (THA) With Different Head Diameters [NCT02047292] | 30 participants (Actual) | Interventional | 2014-01-31 | Completed | |||
| Evaluation of Functional Rehabilitation Therapy in Patients Undergoing Physiotherapy After Total Hip Arthroplasty [NCT01491048] | 104 participants (Actual) | Interventional | 2009-07-31 | Completed | |||
| Minimal Invasive Surgery in Total Hip Arthroplasty Patients; Short- and Long Term Results [NCT01506024] | 60 participants (Actual) | Interventional | 2011-09-30 | Completed | |||
| Pre-Op Total Hip Arthroplasty Modelling: Individualized Care, Improved Outcomes [NCT05221554] | 80 participants (Anticipated) | Interventional | 2022-08-01 | Recruiting | |||
| A Prospective Randomised Controlled Trial Comparing Computerised Tomography Based Planning of Conventional Total Hip Arthroplasty Versus Mako Robotic-arm Assisted Total Hip Arthroplasty [NCT04095845] | 60 participants (Actual) | Interventional | 2018-11-09 | Active, not recruiting | |||
| Age-based Cut-off Point as Methodological Approach in Search for Differences in Mortality and Revision for Fixation Type: Cemented Versus Uncemented Total Hip Arthroplasty [NCT05108155] | 43,789 participants (Actual) | Observational [Patient Registry] | 2007-01-31 | Completed | |||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||