rivastigmine profile

rivastigmine tartrate : A tartrate salt obtained by reaction of rivastigmine with one equivalent of (R,R)-tartaric acid. A reversible cholinesterase inhibitor. [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	77990
CHEMBL ID	3187096
SCHEMBL ID	2763
MeSH ID	M0196402
PubMed CID	77991
CHEMBL ID	636
CHEBI ID	8874
SCHEMBL ID	2764
MeSH ID	M0196402

Synonym
rivastigmine tartrate
dtxcid4027818
cas-129101-54-8
dtxsid8047840 ,
tox21_112528
SCHEMBL2763
tox21_112528_1
NCGC00167531-02
AKOS025149495
CHEMBL3187096
BIDD:GT0316
AB01275472-01
pki06m3iw0 ,
rivastigmine transdermal system
exelon patch
rivastigmine [usan:inn:ban:jan]
nimvastid
unii-pki06m3iw0
ono-2540
sdz-212-713
prometax
ena-713d
3-[(1s)-1-(dimethylamino)ethyl]phenyl ethyl(methyl)carbamate
prometax (tn)
D03822
rivastigmine (jan/usp/inn)
sdz ena 713
123441-03-2
rivastigmine ,
rivastigmine.tartrate
bdbm10620
ethyl-methyl-carbamic acid 3-((r)-1-dimethylamino-ethyl)-phenyl ester
ethyl-methyl-carbamic acid 3-((s)-1-dimethylamino-ethyl)-phenyl ester
3-((1s)-1-(dimethylamino)ethyl)phenyl n-ethyl n-methyl carbamate
2,3-dihydroxybutanedioic acid; 3-[(1s)-1-(dimethylamino)ethyl]phenyl n-ethyl-n-methylcarbamate
3-[(1s)-1-(dimethylamino)ethyl]phenyl n-ethyl-n-methylcarbamate
ethyl-methyl-carbamic acid 3-(1-dimethylamino-ethyl)-phenyl ester
bdbm11682
(s)-3-(1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
DB00989
m-((s)-1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
(s)-3-(1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate
chembl636 ,
carbamic acid, ethylmethyl-, 3-(1-(dimethylamino)ethyl)phenyl ester, (s)-
ena 713 free base
sdz 212-713
carbamic acid, ethylmethyl-, 3-((1s)-1-(dimethylamino)ethyl)phenyl ester
3-((1s)-1-(dimethylamino)ethyl)phenyl ethylmethylcarbamate
(s)-n-ethyl-3-((1-dimethyl-amino)ethyl)-n-methylphenylcarbamate
HMS2089H18
rivastigmine hexal
sdz-212713
rivastigmine sandoz
chebi:8874 ,
rivastigmine teva
[3-[(1s)-1-(dimethylamino)ethyl]phenyl] n-ethyl-n-methylcarbamate
HY-17368
MLS003876822
smr002203623
NCGC00167531-03
CS-0946
AKOS015896334
gtpl6602
[3-[(1s)-1-dimethylaminoethyl]phenyl] n-ethyl-n-methylcarbamate
rivastigmine [orange book]
rivastigmine 1 a pharma
rivastigmine [usp monograph]
rivastigmine [vandf]
rivastigmine [inn]
rivastigmine [ema epar]
rivastigmine [jan]
rivastigmine [mart.]
rivastigmine [usp-rs]
rivastigmine [mi]
rivastigmine 3m health care ltd
rivastigmine [ep monograph]
rivastigmine [who-dd]
rivastigmine [usan]
CCG-221197
SCHEMBL2764
XSVMFMHYUFZWBK-NSHDSACASA-N
W-200966
(s)-rivastigmine
AB01275472_02
AB01275472_03
DTXSID7023564 ,
s-rivastigmine
3-((1s)-1-(dimethylamino)ethyl)phenyl n-ethyl-n-methylcarbamate
AC-8250
sr-05000001475
SR-05000001475-1
SR-05000001475-2
AS-73448
ethylmethylcarbamic acid 3-[(1s)-1-(dimethylamino)ethyl]phenyl ester
HMS3715P15
Q411887
S4687
carbamic acid, n-ethyl-n-methyl-, 3-[(1s)-1-(dimethylamino)ethyl]phenyl ester
NCGC00167531-17
HMS3885B18
AMY3808
(s)-3-[1-(dimethylamino)ethyl]phenyl n-ethyl-n-methylcarbamate
D82061
rivastigmine impurity d
rivastigmine (usp-rs)
rivastigmine (usp monograph)
rivastigmina
rivastigmine (ep monograph)
3-((1s)-1-(dimethylamino)ethyl)phenyl ethyl(methyl)carbamate
dtxcid703564
n06da03
rivastigminum
rivastigmine (mart.)
R0250
EN300-7403044

Excerpt	Reference	Relevance
" Most adverse events were mild to moderate in severity and of limited duration, most commonly headache, nausea, dizziness, and diarrhea."	( Safety/tolerability trial of SDZ ENA 713 in patients with probable Alzheimer's disease. Anand, R; Cutler, NR; Hartman, RD; Irwin, P; Sramek, JJ; Wardle, TS, 1996)	0.29
" Adverse events were predominantly gastrointestinal, of mild to moderate severity, transient, and occurred mainly during escalation of the dose."	( Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. Agid, Y; Anand, R; Cicin-Sain, A; Dal-Bianco, P; Gauthier, S; Gharabawi, M; Hartman, R; Rösler, M; Stähelin, HB, 1999)	0.3
" Safety was monitored by physical examinations, vital signs, laboratory tests, ECG recording and by the assessment of adverse events."	( An open-label study to evaluate the safety, tolerability and efficacy of rivastigmine in patients with mild to moderate probable Alzheimer's disease in the community setting. Barcikowska, M; Bilikiewicz, A; Bilińska, M; Gabryelewicz, T; Ochudło, S; Opala, G; Paradowski, B; Parnowski, T; Pfeffer, A; Podemski, R; Puzyński, S; Sołtys, K; Łapin, J, 2002)	0.31
" Exelon was generally well tolerated with 11% of patients withdrawing due to adverse events."	( An open-label study to evaluate the safety, tolerability and efficacy of rivastigmine in patients with mild to moderate probable Alzheimer's disease in the community setting. Barcikowska, M; Bilikiewicz, A; Bilińska, M; Gabryelewicz, T; Ochudło, S; Opala, G; Paradowski, B; Parnowski, T; Pfeffer, A; Podemski, R; Puzyński, S; Sołtys, K; Łapin, J, 2002)	0.31
" Adverse events caused by co-administration were assessed."	( A pilot, randomized, open-label trial assessing safety and pharmakokinetic parameters of co-administration of rivastigmine with risperidone in dementia patients with behavioral disturbances. Anand, R; Cicin-Sain, A; Hartman, R; Korczyn, AD; Rotmensch, HH; Weiser, M, 2002)	0.31
"No clinically relevant adverse interactions were observed."	( A pilot, randomized, open-label trial assessing safety and pharmakokinetic parameters of co-administration of rivastigmine with risperidone in dementia patients with behavioral disturbances. Anand, R; Cicin-Sain, A; Hartman, R; Korczyn, AD; Rotmensch, HH; Weiser, M, 2002)	0.31
" Rivastigmine was generally well tolerated, the most common adverse events being nausea and vomiting, consistent with reports from previous clinical studies."	( Efficacy and safety of rivastigmine in patients with Alzheimer's disease who failed to benefit from treatment with donepezil. Auriacombe, S; Loria-Kanza, Y; Pere, JJ; Vellas, B, 2002)	0.31
"The correlates of dropout, efficacy, and adverse events in the treatment of Alzheimer's disease (AD) with acetylcholinesterase inhibitors (ChEI) are unclear."	( Correlates of dropout, efficacy, and adverse events in treatment with acetylcholinesterase inhibitors in Korean patients with Alzheimer's disease. Kim, JM; Shin, IS; Yoon, JS, 2002)	0.31
"We conducted a comparative retrospective study of the tolerance and the adverse events (AE) of two AChEI in a group of patients with very slight and mild probable AD over a 6 month period."	( [Tolerance and adverse events of treatment with acetylcholinesterase inhibitors in a clinical sample of patients with very slight and mild Alzheimer s disease over a six-month period]. Fajardo-Tibau, C; Garre-Olmo, J; Gelada-Batlle, E; Hernández-Ferràndiz, M; López-Pousa, S; Lozano-Gallego, M; Morante-Muñoz, V; Turon-Estrada, A; Vilalta-Franch, J, )	0.13
"6 %)treatment was withdrawn because of mostly gastrointestinal adverse events."	( Effectiveness and safety of cholinesterase inhibitors in elderly subjects with Alzheimer's disease: a "real world" study. Bardelli, F; Bencini, F; Biagini, CA; Caleri, V; Cantini, C; Cavallini, MC; Marini, M; Masotti, G; Mecacci, R; Mossello, E; Razzi, E; Sarcone, E; Tilli, S; Tonon, E, 2004)	0.32
" In this open label extension, high-dose rivastigmine therapy was safe and well tolerated over a 5-year period."	( Rivastigmine: an open-label, observational study of safety and effectiveness in treating patients with Alzheimer's disease for up to 5 years. Farlow, MR; Lilly, ML, 2005)	0.33
"Long-term cholinesterase inhibition therapy with rivastigmine was well tolerated, with no dropouts due to adverse effects past the initial titration period."	( Rivastigmine: an open-label, observational study of safety and effectiveness in treating patients with Alzheimer's disease for up to 5 years. Farlow, MR; Lilly, ML, 2005)	0.33
"To provide a systematic review of the best quality evidence of the effects of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in people with mild to moderately-severe AD."	( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease. Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006)	0.33
" Adverse events were generally related to the gastrointestinal system, with a tendency for these to be more common in the treatment arms."	( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease. Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006)	0.33
" The most common adverse effects occurring in >10% of patients were nausea, vomiting, dizziness and diarrhoea."	( A pilot study evaluating the efficacy and safety of rivastigmine in patients with mixed dementia. Alva, G; Chen, M; Gunay, I; Koumaras, B; Mirski, D; Potkin, SG, 2006)	0.33
" Four subjects experienced no adverse events (AEs)."	( Safety and efficacy of rivastigmine in adolescents with Down syndrome: a preliminary 20-week, open-label study. Crissman, BG; Doraiswamy, PM; Eells, RL; Heller, JH; Kishnani, PS; Krishnan, KR; Li, JS; Spiridigliozzi, GA; Sullivan, JA, 2006)	0.33
" Trial methods, clinical characteristics, outcomes, and adverse events were extracted and checked."	( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials. Kavirajan, H; Schneider, LS, 2007)	0.34
" Compared with placebo, more dropouts and adverse events (anorexia, nausea, vomiting, diarrhoea, and insomnia) occurred with the cholinesterase inhibitors, but not with memantine."	( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials. Kavirajan, H; Schneider, LS, 2007)	0.34
" Adverse events were recorded."	( Efficacy, safety and tolerability of rivastigmine capsules in patients with probable vascular dementia: the VantagE study. Ballard, C; Barkhof, F; He, Y; Hsu, C; Lane, R; Sauter, M; Scheltens, P; van der Flier, WM; van Straaten, EC; Wu, S, 2008)	0.35
" Predominant adverse events were nausea and vomiting."	( Efficacy, safety and tolerability of rivastigmine capsules in patients with probable vascular dementia: the VantagE study. Ballard, C; Barkhof, F; He, Y; Hsu, C; Lane, R; Sauter, M; Scheltens, P; van der Flier, WM; van Straaten, EC; Wu, S, 2008)	0.35
" Across trials, the incidence of adverse events was generally lowest for donepezil and highest for rivastigmine."	( Efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer's disease: a systematic review and meta-analysis. Gartlehner, G; Hansen, RA; Jonas, DE; Moore, CG; Morgan, LC; Webb, AP, 2008)	0.35
"Rivastigmine is safe in stroke patients with delirium even after rapid titration."	( A pilot study of rivastigmine in the treatment of delirium after stroke: a safe alternative. de Kort, PL; Jansen, BP; Kappelle, LJ; Oldenbeuving, AW; Roks, G, 2008)	0.35
" Primary measures included safety and tolerability assessments, including adverse events and serious adverse events."	( Safety and tolerability of the rivastigmine patch: results of a 28-week open-label extension. Frölich, L; Fröstl, H; Grossberg, G; Nagel, J; Orgogozo, JM; Ros, J; Sadowsky, C; Tekin, S; Zechner, S, )	0.13
" The most common adverse events were nausea, vomiting, and dizziness."	( Safety and tolerability of rivastigmine capsule with memantine in patients with probable Alzheimer's disease: a 26-week, open-label, prospective trial (Study ENA713B US32). Bhatnagar, V; Brannan, S; Koumaras, B; Meng, X; Olin, JT; Reyes, P, 2010)	0.36
"Results from this study suggest the combination of rivastigmine capsule and memantine in patients with moderate AD is safe and tolerable."	( Safety and tolerability of rivastigmine capsule with memantine in patients with probable Alzheimer's disease: a 26-week, open-label, prospective trial (Study ENA713B US32). Bhatnagar, V; Brannan, S; Koumaras, B; Meng, X; Olin, JT; Reyes, P, 2010)	0.36
"Galantamine, a centrally acting cholinesterase (ChE) inhibitor and a nicotinic allosteric potentiating ligand used to treat Alzheimer's disease, is an effective and safe antidote against poisoning with nerve agents, including soman."	( Effectiveness of donepezil, rivastigmine, and (+/-)huperzine A in counteracting the acute toxicity of organophosphorus nerve agents: comparison with galantamine. Adler, M; Akkerman, M; Albuquerque, EX; Aracava, Y; Pereira, EF, 2009)	0.35
" Although pretreatment with atropine minimizes the adverse effect of pralidoxime reported in these models, concerns over the risks of pralidoxime in humans with carbamate poisoning continue."	( Use of pralidoxime without atropine in rivastigmine (carbamate) toxicity. Felberbaum, M; Hoffman, RS; Manini, AF; Mercurio-Zappala, M; Russell-Haders, AL, 2009)	0.35
" However, dose-limiting adverse effects restrict its tolerability and clinical outcomes."	( Peripheral cholinoceptor antagonist anisodamine counteracts cholinergic adverse effects and facilitates cognitive amelioration of rivastigmine. Chen, HZ; Cui, YY; Li, J; Shao, BY; Song, MK; Wang, H; Xia, Z; Xu, ZP; Zhang, WW, 2009)	0.35
" The primary outcome measure for this trial was the incidence of emerging adverse events."	( Safety/Tolerability and efficacy of rivastigmine in taiwanese patients with Alzheimer's disease: a prospective post-marketing surveillance study. Chiu, PY; Dai, DE; Hsu, HP; Huang, YC; Kuo, HC; Lee, C; Lin, JJ; Liu, YC; Tsai, CP, 2009)	0.35
"3%) reported at least one adverse event."	( Safety/Tolerability and efficacy of rivastigmine in taiwanese patients with Alzheimer's disease: a prospective post-marketing surveillance study. Chiu, PY; Dai, DE; Hsu, HP; Huang, YC; Kuo, HC; Lee, C; Lin, JJ; Liu, YC; Tsai, CP, 2009)	0.35
" Although the rate of adverse events was high, the majority of these symptoms were mild in severity and short in duration."	( Safety/Tolerability and efficacy of rivastigmine in taiwanese patients with Alzheimer's disease: a prospective post-marketing surveillance study. Chiu, PY; Dai, DE; Hsu, HP; Huang, YC; Kuo, HC; Lee, C; Lin, JJ; Liu, YC; Tsai, CP, 2009)	0.35
" Fewer donepezil-treated subjects withdrew due to adverse events (AEs) compared with rivastigmine and galantamine-treated subjects."	( Safety and tolerability of donepezil, rivastigmine and galantamine for patients with Alzheimer's disease: systematic review of the 'real-world' evidence. Kelly, S; Lockhart, IA; Mitchell, SA, 2009)	0.35
"The main adverse events reported with rivastigmine therapy are gastrointestinal in nature."	( Safety and tolerability of transdermal and oral rivastigmine in Alzheimer's disease and Parkinson's disease dementia. Darreh-Shori, T; Jelic, V, 2010)	0.36
" Safety outcomes included adverse events (AEs), discontinuations caused by AEs and serious AEs (SAEs)."	( Safety and tolerability of rivastigmine transdermal patch compared with rivastigmine capsules in patients switched from donepezil: data from three clinical trials. Farlow, MR; Meng, X; Olin, JT; Sadowsky, CH, 2010)	0.36
" Rivastigmine was safe in the acute phase of stroke patients even after the rapid titration."	( [Efficacy and safety of rivastigmine (exelon) in the confusion syndrome in the acute phase of ischemic stroke]. Fedorov, BB; Khlystov, IuV; Litvineneko, IV; Odinak, MM; Perstnev, SV, 2010)	0.36
" Rivastigmine, a cholinesterase inhibitor, is commonly used as a treatment for dementia due to its ability to moderate cholinergic neurotransmission; however, treatment with oral rivastigmine can lead to gastrointestinal adverse effects such as nausea and vomiting."	( Transdermal rivastigmine: management of cutaneous adverse events and review of the literature. Adam, DN; Greenspoon, J; Herrmann, N, 2011)	0.37
" Their known adverse effects include bradycardia."	( Bradycardia due to cholinesterase inhibitors: identify adverse effects and take them into account. , 2011)	0.37
"Safety and tolerability assessment included the monitoring and recording of adverse events and withdrawals at any time during the study."	( Safety and tolerability of rivastigmine transdermal patch formulation in newly diagnosed patients with Alzheimer's dementia in naturalistic conditions. Pregelj, P, 2012)	0.38
"54%) suffered serious adverse events."	( Safety and tolerability of rivastigmine transdermal patch formulation in newly diagnosed patients with Alzheimer's dementia in naturalistic conditions. Pregelj, P, 2012)	0.38
"The results of this study suggest that the rivastigmine transdermal patch is safe and tolerable for Alzheimer's dementia patients in naturalistic conditions."	( Safety and tolerability of rivastigmine transdermal patch formulation in newly diagnosed patients with Alzheimer's dementia in naturalistic conditions. Pregelj, P, 2012)	0.38
" Primary outcomes included incidence of, and discontinuation due to, predefined adverse events (AEs) potentially arising from worsening of Parkinson disease motor symptoms with capsules."	( Long-term safety of rivastigmine in parkinson disease dementia: an open-label, randomized study. Barone, P; Burn, D; Callegari, F; De Deyn, PP; Durif, F; Emre, M; Kulisevsky, J; Micheli, F; Pahwa, R; Poewe, W; Pourcher, E; Storch, A; Strohmaier, C; Tenenbaum, N; van Laar, T, )	0.13
" Compared with placebo, more dropouts and adverse events occurred with the cholinesterase inhibitors, but not with memantine."	( Efficacy and safety of donepezil, galantamine, rivastigmine, and memantine for the treatment of Alzheimer's disease: a systematic review and meta-analysis. Jiang, T; Meng, XF; Tan, CC; Tan, L; Tan, MS; Wang, C; Wang, HF; Yu, JT; Zhu, XC, 2014)	0.4
" The incidence of adverse events (AEs), serious AEs and discontinuations due to AEs was similar in patients who continued on, and patients who uptitrated to, 13."	( A 24-Week, Open-Label Extension Study to Investigate the Long-term Safety, Tolerability, and Efficacy of 13.3 mg/24 h Rivastigmine Patch in Patients With Severe Alzheimer Disease. Farlow, MR; Grossberg, GT; Meng, X; Sadowsky, CH; Velting, DM, )	0.13
"This survey analyzes two national pharmacovigilance databases in order to determine the major adverse reactions observed with the use of cholinesterase inhibitors in dementia."	( Adverse Effects of Cholinesterase Inhibitors in Dementia, According to the Pharmacovigilance Databases of the United-States and Canada. Abagyan, R; Ali, TB; Chen, WY; Reilly, BM; Schleret, TR, 2015)	0.42
" Withdrawals due to adverse events and number of patients experiencing nausea, vomiting, diarrhoea and dizziness were examined as safety profiles."	( The comparative efficacy and safety of cholinesterase inhibitors in patients with mild-to-moderate Alzheimer's disease: a Bayesian network meta-analysis. Kobayashi, H; Nakagawa, R; Ohnishi, T; Yoshizawa, K, 2016)	0.43
" Safety measures included reports of adverse events, laboratory parameters, and electrocardiograms."	( Safety and efficacy of rivastigmine in children with Down syndrome: A double blind placebo controlled trial. Baker, JA; Capone, GT; Hart, SJ; Heller, JH; Kishnani, PS; Schneider, HE; Spiridigliozzi, GA; Weadon, C, 2016)	0.43
" Acetylcholinesterase inhibitors (AChEIs) aim to provide symptomatic benefit for cognitive decline, however these drugs are not without adverse events (AEs)."	( Acetylcholinesterase inhibitors for treating dementia symptoms - a safety evaluation. Bradley, J; Chan, P; Herrmann, N; Lanctôt, K; Mohammad, D, 2017)	0.46
" The adverse drug effects and discontinuation rates were investigated with self-reported complaint after starting or increasing anti-dementia drugs."	( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia. Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018)	0.48
" The adverse drug effects were observed in 26 (33."	( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia. Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018)	0.48
"The use of anti-dementia agents in the oldest old dementia patients may be safe and effective as the younger old dementia patients."	( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia. Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018)	0.48
"1%) experienced adverse effects (AEs) during the study; common AEs included nausea (20."	( Sixteen-Week Interventional Study to Evaluate the Clinical Effects and Safety of Rivastigmine Capsules in Chinese Patients with Alzheimer's Disease. Fan, D; Feng, T; Ji, Y; Jia, J; Kuang, W; Li, Y; Liang, Z; Ning, Y; Peng, D; Wei, W; Xiao, S; Ye, Q, 2019)	0.51
"The purpose of this study was to perform a comparative analysis of the number of reported pneumonia cases in individuals prescribed rivastigmine relative to the number of reported cases by patients using other therapeutics including over-the-counter drugs and other AD therapeutics, as reported to the FDA Adverse Event Reporting System (FAERS) database."	( The Association Between Use of Rivastigmine and Pneumonia: Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Morris, R; Umeukeje, G, 2021)	0.62
"Patients prescribed rivastigmine were more likely to report pneumonia as an adverse event than many drugs except galantamine."	( The Association Between Use of Rivastigmine and Pneumonia: Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Morris, R; Umeukeje, G, 2021)	0.62
"We aimed to perform an updated umbrella review to identify an efficacious and safe treatment for AD patients."	( The Efficacy and Safety of Alzheimer's Disease Therapies: An Updated Umbrella Review. Ai, Y; Cheng, Y; Fan, F; Liu, H; Liu, Q; Shi, X, 2022)	0.72
" We examined the cognitive functions, behavioral symptoms, global clinical assessment, and Activities of Daily Living as efficacy endpoints, and the incidence of adverse events as safety profiles."	( The Efficacy and Safety of Alzheimer's Disease Therapies: An Updated Umbrella Review. Ai, Y; Cheng, Y; Fan, F; Liu, H; Liu, Q; Shi, X, 2022)	0.72
"We included trials assessing cognition with the Mini-Mental State Examination (MMSE), and adverse events."	( Comparative safety and efficacy of cognitive enhancers for Alzheimer's dementia: a systematic review with individual patient data network meta-analysis. Ashoor, HM; Clarke, M; Hemmelgarn, BR; Holroyd-Leduc, J; Mavridis, D; Rios, P; Seitidis, G; Stewart, L; Straus, SE; Tricco, AC; Tudur-Smith, C; Veroniki, AA, 2022)	0.72
" This study evaluated the risk of serious adverse events (SAEs) associated with individual ChEIs in older adults with dementia and also examined sex-based and dose-based effects on this risk."	( Risk of Serious Adverse Events Associated With Individual Cholinesterase Inhibitors Use in Older Adults With Dementia: A Population-Based Cohort Study. Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML; Masurkar, PP; Sherer, JT, 2022)	0.72
"Dysphagia has been reported as an adverse event for patients receiving rivastigmine for Alzheimer's disease (AD) treatment."	( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022)	0.72
"The purpose of this study was to determine the association between dysphagia and the usage of rivastigmine by using the pharmacovigilance data from the FDA Adverse Event Reporting System (FAERS)."	( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022)	0.72
"When compared to patients prescribed donepezil, galantamine, or memantine, individuals prescribed rivastigmine were almost twice as likely to report dysphagia as an adverse event."	( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022)	0.72
"Patients prescribed rivastigmine were at greater risk of reporting dysphagia as an adverse event than patients prescribed many other medicines."	( Dysphagia Risk in Patients Prescribed Rivastigmine: A Systematic Analysis of FDA Adverse Event Reporting System. Bu, K; Cheng, F; Han, W; Morris, R; Patel, D; Umeukeje, G; Zhu, T, 2022)	0.72
"While these drugs are known to induce classic cholinergic adverse events such as diarrhea, their potential to cause psychiatric adverse events has yet to be thoroughly examined."	( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis. Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023)	0.91
"We sought to determine the risk of psychiatric adverse events associated with the use of AChEIs through a systematic review and meta-analysis of double-blind randomized controlled trials involving patients with Alzheimer's dementia and Parkinson's dementia."	( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis. Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023)	0.91
" Anorexia was the most commonly reported psychiatric adverse event, followed by agitation, insomnia, and depression."	( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis. Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023)	0.91
" Lowering the dose may resolve some psychiatric adverse events, as may switching to galantamine in the case of insomnia."	( Psychiatric Adverse Events of Acetylcholinesterase Inhibitors in Alzheimer's Disease and Parkinson's Dementia: Systematic Review and Meta-Analysis. Algharably, EEA; Bermpohl, F; Bittner, N; Brandl, EJ; Funk, CSM; Kreutz, R; Riemer, TG; Schmidt, A, 2023)	0.91

Excerpt	Reference	Relevance
" 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
" A pharmacodynamic analysis of rivastigmine administered concomitantly with other medications (22 different therapeutic classes) did not reveal any significant pattern of increase in adverse events that would indicate a drug interaction."	( Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medications. Anand, R; Grossberg, GT; Messina, JC; Stahelin, HB; Veach, J, 2000)	0.31
" Specifically, certain metabolic parameters (ie, half-life and route of metabolism/elimination) can affect a drug's tolerability and become important when a switch from one agent to another is contemplated."	( Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine. Farlow, MR, 2001)	0.31
" Nonlinear mixed-effects modeling of pharmacokinetic and pharmacodynamic data was conducted using NONMEM."	( Pharmacokinetic-pharmacodynamic modeling of rivastigmine, a cholinesterase inhibitor, in patients with Alzheimer's disease. Cutler, NR; Gobburu, JV; Jhee, SS; Lesko, L; Sramek, JJ; Tammara, V; Yuan, R, 2001)	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
" The current objective was to evaluate the pharmacokinetic profile and patch adhesiveness following application at the upper back, chest, abdomen, thigh, and upper arm."	( Pharmacokinetics of a rivastigmine transdermal patch formulation in healthy volunteers: relative effects of body site application. Fordham, P; Huang, HL; Kiese, B; Lefèvre, G; Rosenberg, M; Saltzman, M; Sedek, G, 2007)	0.34
" The patch showed lower Cmax (ca."	( Pharmacokinetics and pharmacodynamics of the novel daily rivastigmine transdermal patch compared with twice-daily capsules in Alzheimer's disease patients. Appel-Dingemanse, S; Enz, A; Ereshefsky, L; Huang, HL; Jhee, SS; Lefèvre, G; Leibowitz, MT; Maton, S; Pommier, F; Schmidli, H; Sedek, G, 2008)	0.35
" Pharmacokinetic studies have shown that transdermal administration of rivastigmine prolongs t(max), lowers C(max), and reduces fluctuations in plasma concentration."	( Pharmacokinetic rationale for the rivastigmine patch. Appel-Dingemanse, S; Cummings, J; Lefèvre, G; Small, G, 2007)	0.34
" 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
" The patients spent the baseline period and day 35 at the study centre, where plasma samples for pharmacokinetic evaluation were taken at specified time intervals over a 10-hour time period."	( Steady-state pharmacokinetics of rivastigmine in patients with mild to moderate Alzheimer's disease not affected by co-administration of memantine: an open-label, crossover, single-centre study. Athalye, S; Lefèvre, G; Picard, F; Pommier, F; Sedek, G; Shua-Haim, J; Smith, J, 2008)	0.35
" At each dose level of rivastigmine, the area under the concentration-time curve (AUC) values of rivastigmine and its metabolite as well as the metabolite-to-parent AUC ratios were unaffected by co-administration of memantine, confirming the absence of a meaningful pharmacokinetic drug-drug interaction."	( Steady-state pharmacokinetics of rivastigmine in patients with mild to moderate Alzheimer's disease not affected by co-administration of memantine: an open-label, crossover, single-centre study. Athalye, S; Lefèvre, G; Picard, F; Pommier, F; Sedek, G; Shua-Haim, J; Smith, J, 2008)	0.35
" The method has been successfully applied in a pharmacokinetic study of rivastigmine in rats."	( Fluorimetric determination of rivastigmine in rat plasma by a reverse phase--high performance liquid chromatographic method. Application to a pharmacokinetic study. Kamat, SB; Karthik, A; Ranjithkumar, A; Subramanian, GS; Surulivelrajan, M, 2008)	0.35
"To review the available pharmacokinetic data that supported the rationale behind the development of the rivastigmine transdermal patch and its clinical effects in dementia therapy."	( Pharmacokinetics of a novel transdermal rivastigmine patch for the treatment of Alzheimer's disease: a review. Farlow, M; Kurz, A; Lefèvre, G, 2009)	0.35
" The pharmacodynamic performances of the nanoparticles (NPs) were evaluated for brain targeting and memory improvement in scopolamine-induced amnesic mice using Morris Water Maze Test."	( Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies. Chavhan, SS; Joshi, SA; Sawant, KK, 2010)	0.36
" Its pharmacokinetic profile in rats was evaluated after intranasal administration."	( [Preparation of rivastigmine liposome and its pharmacokinetics in rats after intranasal administration]. Qi, XR; Wang, ZZ; Wu, K; Yang, ZZ, 2011)	0.37
" In vivo pharmacokinetic studies were carried out in rabbits, and attempts were made to establish in vitro/ in vivo correlations (IVIVC)."	( Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation. Beg, S; Dhawan, S; Kapil, R; Singh, B, 2013)	0.39
" Pharmacokinetic studies indicated extension of plasma drug levels and level A of IVIVC was successfully established."	( Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation. Beg, S; Dhawan, S; Kapil, R; Singh, B, 2013)	0.39
" Donepezil, galantamine and rivastigmine are acetylcholinesterase inhibitors with different pharmacodynamic and pharmacokinetic profiles."	( Pharmacodynamic, pharmacokinetic and pharmacogenetic aspects of drugs used in the treatment of Alzheimer's disease. Eap, CB; Noetzli, M, 2013)	0.39
" A dermal absorption pharmacokinetic (PK) model was developed to simulate the plasma concentration-time profile of rivastigmine to answer questions relative to the efficacy and safety risks after misuse of the patch (e."	( Pharmacokinetic Modeling to Simulate the Concentration-Time Profiles After Dermal Application of Rivastigmine Patch. Lefèvre, G; Nozaki, S; Yamaguchi, M, 2016)	0.43
" On completing the in vivo pharmacokinetic studies of 36 rabbits showed 424."	( Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo, bio-distribution and in vivo pharmacokinetic studies. Abd Elbary, A; El-Nabarawi, MA; Kassem, MA; Nageeb El-Helaly, S, 2017)	0.46
"Gamma scintigraphy and in vivo pharmacokinetic study suggested enhanced RHT concentration, upon intranasal administration of RHT:CH-ME, compare with other groups administered formulations intranasally."	( Formulation and In-vivo Pharmacokinetic Consideration of Intranasal Microemulsion and Mucoadhesive Microemulsion of Rivastigmine for Brain Targeting. Khunt, D; Misra, M; Padh, H; Shah, B, 2018)	0.48
" Therefore, the present study attempts to evaluate the pharmacokinetic and pharmacodynamic properties of nasal liposomal and PLGA nanoparticle formulations of rivastigmine in acute scopolamine-induced amnesia and chronic colchicine induced cognitive dysfunction animal models, and validate the best formulation by employing pharmacokinetic and pharmacodynamic (PK-PD) modeling."	( Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer's disease. Arumugam, K; Bojja, SL; Kumar, N; Rao, CM; Rompicherla, SKL, 2021)	0.62
" A significant difference between male and female Cmax (maximum plasma concentration) (P = 0."	( Validated LC/MS/MS Method for the Determination of Rivastigmine in Human Plasma: Application to a Pharmacokinetic Study in Egyptian Volunteers to Determine the Effect of Gender and Body Mass Index. ElKady, EF; Mostafa, EA, 2023)	0.91

Excerpt	Reference	Relevance
" Therefore, its combination with acetylcholinesterase inhibitors (AChEIs) is anticipated."	( Tolerability of memantine in combination with cholinesterase inhibitors in dementia therapy. Hartmann, S; Möbius, HJ, 2003)	0.32
"Oestro-progestagen treatment did not provide further improvement when combined with rivastigmine during mild to moderately severe Alzheimer's disease."	( [Oestro-progestagen treatment combined with rivastigmine in menopausal women suffering from Alzheimer's disease. The results of a 28-weeks controlled study]. André, G; Loria-Kanza, Y; Pere, JJ; Rigaud, AS; Touchon, J; Vellas, B, 2003)	0.32
"To study the efficacy of cognitive rehabilitation combined with acetylcholinesterase inhibitor (AChE-I) treatment in patients with mild Alzheimer's disease and their relatives."	( Cognitive rehabilitation combined with drug treatment in Alzheimer's disease patients: a pilot study. Alvarez, AM; Andrade, FC; Avila, R; Bottino, CM; Bustamante, SE; Câmargo, CH; Carvalho, IA; Hototian, SR; Saffi, F; Zukauskas, PR, 2005)	0.33
"Cholinesterase inhibitors (ChEIs) could be involved in several drug-drug interactions (DDIs) because of their complex pharmacodynamic and/or pharmacokinetic properties."	( Drug interactions with cholinesterase inhibitors: an analysis of the French pharmacovigilance database and a comparison of two national drug formularies (Vidal, British National Formulary). Bagheri, H; Lapeyre-Mestre, M; Montrastruc, JL; Sommet, A; Tavassoli, N, 2007)	0.34
" We conducted this study in order to determine the safety (adverse events, mood changes, cardiovascular effects) and preliminary efficacy (subjective effects) of the AChE inhibitor rivastigmine (Riv) when tested in combination with Meth."	( Evaluation of the cardiovascular and subjective effects of rivastigmine in combination with methamphetamine in methamphetamine-dependent human volunteers. De La Garza, R; Newton, TF; Shoptaw, S, 2008)	0.35

Excerpt	Reference	Relevance
"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
" In animals and human subjects this compound showed superior chemical stability, oral bioavailability and a longer duration of action than physostigmine."	( Pharmacological evaluation of phenyl-carbamates as CNS-selective acetylcholinesterase inhibitors. Chorev, M; Enz, A; Razin, M; Weinstock, M, 1994)	0.29
" Extensive, saturable first-pass metabolism, however, leads to bioavailability of approximately 35% of the administered dose and nonlinear pharmacokinetics."	( Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Polinsky, RJ, )	0.13
" 93%) absorbed, although the bioavailability of the parent drug was low, ca."	( Absorption, metabolism, and disposition of [14C]SDZ ENA 713, an acetylcholinesterase inhibitor, in minipigs following oral, intravenous, and dermal administration. Laplanche, R; Tse, FL, 1998)	0.3
"Dermal administration in minipigs provided a markedly greater bioavailability of SDZ ENA 713 than the oral route."	( Absorption, metabolism, and disposition of [14C]SDZ ENA 713, an acetylcholinesterase inhibitor, in minipigs following oral, intravenous, and dermal administration. Laplanche, R; Tse, FL, 1998)	0.3
" This may be explained by better bioavailability and/or by reduced stability of the circadian rhythmicity in elderly individuals."	( The effect of rivastigmine on sleep in elderly healthy subjects. Berger, M; Braus, D; Gattaz, WF; Heuser, I; Riemann, D; Schredl, M; Weber, B, 2000)	0.31
" The relative bioavailability at the 6 mg dose was about 140%."	( Pharmacokinetic-pharmacodynamic modeling of rivastigmine, a cholinesterase inhibitor, in patients with Alzheimer's disease. Cutler, NR; Gobburu, JV; Jhee, SS; Lesko, L; Sramek, JJ; Tammara, V; Yuan, R, 2001)	0.31
"To investigate the bioavailability of rivastigmine, an approved therapy for patients with mild to moderate dementia of the Alzheimer's type, at the highest approved single dose of 6 mg."	( Estimation of the absolute bioavailability of rivastigmine in patients with mild to moderate dementia of the Alzheimer's type. Cutler, NR; Hossain, M; Jhee, SS; McDonald, C; Pommier, F; Sedek, G; Shiovitz, T, 2002)	0.31
" By a noncompartmental approach, the absolute bioavailability of the 6 mg oral dose of rivastigmine was 71."	( Estimation of the absolute bioavailability of rivastigmine in patients with mild to moderate dementia of the Alzheimer's type. Cutler, NR; Hossain, M; Jhee, SS; McDonald, C; Pommier, F; Sedek, G; Shiovitz, T, 2002)	0.31
"2% respectively, for the absolute bioavailability of a single 6 mg oral dose of rivastigmine."	( Estimation of the absolute bioavailability of rivastigmine in patients with mild to moderate dementia of the Alzheimer's type. Cutler, NR; Hossain, M; Jhee, SS; McDonald, C; Pommier, F; Sedek, G; Shiovitz, T, 2002)	0.31
" The relative bioavailability of rivastigmine from all three regions of the GI tract was comparable to that following oral administration."	( Absorption of rivastigmine from different regions of the gastrointestinal tract in humans. Hossain, M; Lee, L; Sedek, G; Wang, Y, 2004)	0.32
" Augmentation of drug bioavailability by the avoidance of first-pass effect through the buccal route and reduction in GI side effects would be other key advantages of this system."	( Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation. Beg, S; Dhawan, S; Kapil, R; Singh, B, 2013)	0.39
"Besides unraveling the polymer synergism, the study helped in developing an optimal once-a-day buccoadhesive drug delivery system exhibiting excellent trans-buccal permeation and buccoadhesive characteristics with improved bioavailability potential."	( Buccoadhesive films for once-a-day administration of rivastigmine: systematic formulation development and pharmacokinetic evaluation. Beg, S; Dhawan, S; Kapil, R; Singh, B, 2013)	0.39
"The rivastigmine (RHT) loaded chitosan nanoparticles (CS-RHT NPs) were prepared by ionic gelation method to improve the bioavailability and enhance the uptake of RHT to the brain via intranasal (i."	( Development and evaluation of rivastigmine loaded chitosan nanoparticles for brain targeting. Ali, J; Baboota, S; Fazil, M; Haque, S; Kumar, M; Md, S; Sahni, JK, 2012)	0.38
" Rivastigmine, a reversible cholinesterase inhibitor used for the treatment of AD, undergoes extensive first-pass metabolism, thus limiting its absolute bioavailability to only 36% after 3-mg dose."	( Nose to brain microemulsion-based drug delivery system of rivastigmine: formulation and ex-vivo characterization. Misra, M; Padh, H; Shah, BM; Shishoo, CJ, 2015)	0.42
" The intestinal absorption rate for each drug was acquired by deconvolution, using historical intravenous data as reference, and used with the intestinal surface area and the dose remaining in the lumen to estimate the Peff."	( Human in vivo regional intestinal permeability: quantitation using site-specific drug absorption data. Dahlgren, D; Lennernäs, H; Roos, C; Sjögren, E, 2015)	0.42
" Deconvolution of bioavailability data using the Wagner-Nelson method enabled the fraction of RV absorbed to be determined and a point-to-point IVIVC to be established."	( Comparative evaluation of rivastigmine permeation from a transdermal system in the Franz cell using synthetic membranes and pig ear skin with in vivo-in vitro correlation. Amaro, MI; Cabral, LM; de Sousa, VP; Healy, AM; Simon, A, 2016)	0.43
"A single dose, crossover absolute bioavailability and safety study was conducted with rivastigmine intravenous solution (1 mg) and nasal spray (3."	( Absolute bioavailability and safety of a novel rivastigmine nasal spray in healthy elderly individuals. Morgan, TM; Soh, B, 2017)	0.46
"The rivastigmine nasal spray had superior absolute bioavailability compared to historical values for oral capsule and transdermal patch determined by other researchers."	( Absolute bioavailability and safety of a novel rivastigmine nasal spray in healthy elderly individuals. Morgan, TM; Soh, B, 2017)	0.46
"The results revealed that enhanced bioavailability of rivastigmine might be caused by the combination of their effects due to CYP3A and esterase inhibition, Therefore, concomitant administration of NQC influences the bioavailability of rivastigmine and also has synergetic effect in the treatment of Alzheimer's disease."	( Enhancement of oral bioavailability of rivastigmine with quercetin nanoparticles by inhibiting CYP3A4 and esterases. Neerati, P; Palle, S, 2017)	0.46
"2% relative bioavailability of the mean plasma levels of the formula ESS compared to that of RHT intranasal solution and 486% relative bioavailability of the mean brain levels."	( Electrosteric stealth Rivastigmine loaded liposomes for brain targeting: preparation, characterization, ex vivo, bio-distribution and in vivo pharmacokinetic studies. Abd Elbary, A; El-Nabarawi, MA; Kassem, MA; Nageeb El-Helaly, S, 2017)	0.46
" In present work, we have selected Rivastigmine hydrogen tartrate (RHT), a reversible cholinesterase inhibitor, which exhibits extensive first-pass metabolism, resulting in limited absolute bioavailability (36%)."	( Formulation and In-vivo Pharmacokinetic Consideration of Intranasal Microemulsion and Mucoadhesive Microemulsion of Rivastigmine for Brain Targeting. Khunt, D; Misra, M; Padh, H; Shah, B, 2018)	0.48
"The present study aimed to develop nanolipid carrier (NLC) loaded transdermal system of rivastigmine for bioavailability enhancement."	( Optimization and characterization of rivastigmine nanolipid carrier loaded transdermal patches for the treatment of dementia. Chauhan, MK; Sharma, PK, 2019)	0.51
"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
"71), enhanced systemic bioavailability (F = 118."	( Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer's disease. Arumugam, K; Bojja, SL; Kumar, N; Rao, CM; Rompicherla, SKL, 2021)	0.62
"Acetylcholinesterase inhibitors are the most used drugs to manage Alzheimer's disease, although they show low bioavailability in the brain."	( Thermosensitive in situ hydrogels of rivastigmine-loaded lipid-based nanosystems for nose-to-brain delivery: characterisation, biocompatibility, and drug deposition studies. Bellahnid, Y; Cunha, S; Forbes, B; Silva, AC; Sousa Lobo, JM; Swedrowska, M; Xu, Z, 2022)	0.72
" This study was designed to evaluate the bioavailability and to assess the bioequivalence of two rivastigmine transdermal patches at steady state (RIV-TDS Test Product versus Exelon Marketed Reference Product), with a release rate of 13."	( Bioavailability Study of a Transdermal Patch Formulation of Rivastigmine Compared with Exelon in Healthy Subjects. De la Torre, R; Iniesta, M; Koch, C; Morte, A; Schug, B; Schurad, B; Vaqué, A, 2022)	0.72
" RIV-HT intranasal delivery can avoid these side effects, but its low brain bioavailability remains challenging."	( Rivastigmine-DHA ion-pair complex improved loading in hybrid nanoparticles for better amyloid inhibition and nose-to-brain targeting in Alzheimer's. Kathuria, H; Monohar Pandey, M; Subhash Hinge, N, 2023)	0.91

Excerpt	Relevance	Reference
"2 hours after oral dosing in both healthy volunteers and patients with AD."	( Clinical pharmacology of rivastigmine: a new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Polinsky, RJ, )	0.13
" The lower dosage range of 1 to 4 mg/day was not as effective as 6 to 12 mg/day, as measured using these criteria and other efficacy parameters."	( Rivastigmine. A review of its use in Alzheimer's disease. Noble, S; Spencer, CM, 1998)	0.3
" Safety evaluations were performed 23 hours after drug dosing and at the end of the study."	( Preferential cerebrospinal fluid acetylcholinesterase inhibition by rivastigmine in humans. Ebert, MH; Enz, A; Johnson, B; Kennedy, JS; Laplanche, R; Loosen, P; Mancione, LC; Parris, WC; Polinsky, RJ; Schmidt, D, 1999)	0.3
" They occurred mostly during the dosage titration phase and decreased during the maintenance phase."	( Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease. Jann, MW, 2000)	0.31
" Further resarch is desirable on dosage (frequency and quanitity) in a search for ways to minimize adverse effects."	( Rivastigmine for Alzheimer's disease. Birks, J; Iakovidou, V; Tsolaki, M, 2000)	0.31
" 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)	0.31
" 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
" They are usually mild-to-moderate, of short duration and responsive to dosage reduction."	( Review of rivastigmine and its clinical applications in Alzheimer's disease and related disorders. Desai, A; Grossberg, G, 2001)	0.31
" The PK-PD model presented in this study can provide valuable information to optimize the drug development of rivastigmine and other related compounds and also in rationalizing dosing recommendations."	( Pharmacokinetic-pharmacodynamic modeling of rivastigmine, a cholinesterase inhibitor, in patients with Alzheimer's disease. Cutler, NR; Gobburu, JV; Jhee, SS; Lesko, L; Sramek, JJ; Tammara, V; Yuan, R, 2001)	0.31
" Testing was conducted prior to dosing and then again at weeks 12, 20 and 23."	( Effects of rivastigmine on cognitive function in dementia with lewy bodies: a randomised placebo-controlled international study using the cognitive drug research computerised assessment system. Anand, R; Cicin-Sain, A; Del Ser, T; Emre, M; Ferrara, R; McKeith, IG; Spano, PF; Spiegel, R; Wesnes, KA, 2002)	0.31
" Rivastigmine shows a clear dose-response relationship, and physicians should aim to maintain patients on doses of 6 mg/day or higher, to a maximum of 12 mg/day."	( The clinical benefits of rivastigmine may reflect its dual inhibitory mode of action: an hypothesis. Bullock, R, 2002)	0.31
"Cholinesterase inhibitors (ChEIs) are dosed in two phases for the treatment of dementia, an initial dose-escalation phase to achieve a therapeutic dose and a maintenance phase where the therapeutic dose is given for long-term therapy."	( The tolerability and safety of cholinesterase inhibitors in the treatment of dementia. Inglis, F, 2002)	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
" Both medications were administered open label according to recommended dosing regimens from the respective product labelling available during the conduct of the study."	( A multinational, randomised, 12-week, comparative study of donepezil and rivastigmine in patients with mild to moderate Alzheimer's disease. Bahra, RS; Bullock, R; Engelbrecht, I; Hock, C; Hopker, SW; Ieni, JR; Maud, CM; Passmore, AP; Potocnik, FC; Smith, R; Wilkinson, DG, )	0.13
"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
"Effective therapy requires up-titration from initial dosage of 3 mg/d to 6 mg/d with additional increases to 9 mg or 12 mg/d giving additional benefits in some patients."	( Update on rivastigmine. Farlow, MR, 2003)	0.32
"The authors estimated the effects of each of the three commonly used drugs for Alzheimer disease (donepezil, galantamine, and rivastigmine) in terms of predefined clinical outcomes and trial completion rates, by dosing level, and described differences among them."	( Metaanalysis of randomized trials of the efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer disease. Ames, D; Clayton, T; Lai, R; Ritchie, CW, )	0.13
" Three head-to-head trials of ChEIs in the treatment of AD have been published to date, but are limited due to their open-label design, rates of titration, and the drug dosage levels utilised."	( The benefits and risks associated with cholinesterase inhibitor therapy in Alzheimer's disease. Herrmann, N; Lanctôt, KL; Thompson, S, 2004)	0.32
" Higher dosages often did not exert beneficial effects in accordance with inverted U-shaped dose-response curves described for cholinomimetics."	( Symptomatic effect of donepezil, rivastigmine, galantamine and memantine on cognitive deficits in the APP23 model. Abramowski, D; De Deyn, PP; Staufenbiel, M; Van Dam, D, 2005)	0.33
"An isocratic, reversed-phase liquid chromatographic (RPLC) method was developed for the quantitative determination of Rivastigmine hydrogen tartrate, a cholinesterase inhibitor in bulk drugs and in pharmaceutical dosage forms."	( A stability indicating LC method for rivastigmine hydrogen tartrate. Bhradwaj, N; Kumar, KP; Kumar, PR; Mohakhud, PK; Rao, BM; Ravi, R; Reddy, GO; Srinivasu, MK, 2005)	0.33
" The author provides information on recommended dosing for all three medications, noting that cholinesterase inhibitors must be titrated carefully."	( Cholinesterase inhibitors in the treatment of dementia. Ellis, JM, 2005)	0.33
" Therapeutic dosing is 6-12 mg/day given twice daily, with higher doses having the potential for greater benefits."	( Rivastigmine for Alzheimer's disease. Desai, AK; Grossberg, GT, 2005)	0.33
"In a 24-week, randomized, double-blind, placebo-controlled, multicenter study of rivastigmine, 487 patients with dementia associated with Parkinson disease underwent assessment of attention on the Cognitive Drug Research computerized cognitive assessment system before dosing and 16 and 24 weeks later."	( Benefits of rivastigmine on attention in dementia associated with Parkinson disease. Edgar, C; Emre, M; Lane, R; McKeith, I; Wesnes, KA, 2005)	0.33
" For this purpose, neuronal activity was measured in rats with rivastigmine-induced elevated ACh levels after a 95% 5-HT depletion obtained by dosing p-chlorophenylalanine followed by D,L-fenfluramine."	( Serotonin depletion results in a decrease of the neuronal activation caused by rivastigmine in the rat hippocampus. Aznar, S; Knudsen, GM; Kornum, BR; Moller, A; Ronn, LC; Weikop, P, 2006)	0.33
" To reduce bias, the Alzheimer's Disease Assessment Scale-Cognitive (ADAS-Cog) raters were blinded to all efficacy measures and to patient dosage information."	( A pilot study evaluating the efficacy and safety of rivastigmine in patients with mixed dementia. Alva, G; Chen, M; Gunay, I; Koumaras, B; Mirski, D; Potkin, SG, 2006)	0.33
"This study compared dosing and utilization patterns of the cholinesterase inhibitors (ChEIs) donepezil, rivastigmine, and galantamine in the nursing home setting."	( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006)	0.33
" The mean daily dosage of donepezil was above the effective dose throughout the study period, whereas the mean daily dosage was below the effective dose for the first 3 months with rivastigmine and did not approach the effective dose for galantamine until month 12."	( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006)	0.33
"The results of this study suggest that early effective dosing occurred more often with donepezil than with rivastigmine or galantamine in these nursing home residents."	( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis. Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006)	0.33
"Twenty-four consecutive patients with mild or moderate Alzheimer's disease were enrolled in the study and were treated with rivastigmine at a target dosage of 12 mg/day for 4 months."	( Changes in metabolite ratios after treatment with rivastigmine in Alzheimer's disease: a nonrandomised controlled trial with magnetic resonance spectroscopy. Díaz, M; Fayed, N; Modrego, PJ; Pina, MA, 2006)	0.33
" Dosage was a function of tolerability, beginning at 3 mg/day and progressively increasing to 9 mg/day."	( Rivastigmine treatment as an add-on to antipsychotics in patients with schizophrenia and cognitive deficits. Chouinard, S; Cohen, H; Godbout, R; Guillem, F; Melun, JP; Poulin, J; Stip, E, 2007)	0.34
" We attempt to throw light on the dosage regimens, degree of effectiveness and safety profile of rivastigmine solution by means of a retrospective, descriptive, cross-sectional study known as the RIVASOL study."	( [Rivastigmine solution prescribing habits in patients with Alzheimer-type dementia in Spain (RIVASOL study)]. Gobartt, AL; González-Gutiérrez, JL, )	0.13
" These untoward effects make it difficult to increase rivastigmine dosage above 6 mg daily in most patients."	( Domperidone is effective in the prevention of rivastigmine-related gastrointestinal disturbances. Costanza, A; Scarzella, L; Vastola, K, )	0.13
" Rivastigmine 3 mg/d was given for the first 4 wk of treatment; the dosage was then increased to 6 mg/d."	( Effect of rivastigmine on regional cerebral blood flow in Alzheimer's disease. Arslan, S; Cerci, SS; Kaya, H; Tamam, Y; Yildiz, M, )	0.13
"To provide a simplified dosing schedule and potentially reduce side effects associated to peak plasma concentrations, an in situ-forming oleogel implant was studied for the sustained-release of rivastigmine."	( In situ-forming oleogel implant for rivastigmine delivery. Bastiat, G; Lafleur, M; Leroux, JC; Vintiloiu, A, 2008)	0.35
" We determine the effects of sub-chronic dosing of ChEIs on alpha7 and non-alpha7 nAChRs and determine if differences can be observed between them."	( Effects of cholinesterase inhibitors on rat nicotinic receptor levels in vivo and in vitro. Reid, RT; Sabbagh, MN, 2008)	0.35
" Patients were treated with rivastigmine (exelon) in dosage 3-12 mg daily during 3 months."	( [The treatment of Alzheimer's disease in patients with comorbid somatic pathology]. Fedorova, IaB; Gavrilova, SI; Kalyn, IaB; Kolykhalov, IV; Selezneva, ND, 2008)	0.35
"Cholinesterase inhibitors such as rivastigmine and donepezil exhibit a dose-response relationship, with higher doses of the drugs demonstrating greater efficacy."	( Use of rivastigmine transdermal patch in the treatment of Alzheimer's disease. Machado, JC; Winblad, B, 2008)	0.35
" After equimolar dosage compared to the reference drug rivastigmine (CAS 123441-03-2), two of the new substances slightly improved cognition in rats, but only to a significantly lower degree compared to the irreversible inhibitor rivastigmine."	( A new way of data interpretation for cognition tests in rats used to characterise six choline esterase inhibitors with heterocyclic nitrogen bridgehead structure. Application in Alzheimer therapy. Appenroth, D; Decker, M; Fleck, C; Lehmann, J, 2008)	0.35
" A dose-response effect was observed for donepezil, with the highest-dose group at greatest risk (HR=2."	( Cholinesterase inhibitors and incidence of bradycardia in patients with dementia in the veterans affairs new England healthcare system. Cantor, MD; Farwell, W; Hernandez, RK; Lawler, EV, 2009)	0.35
" The proposed methods have been successfully applied to the analysis of RIV in pharmaceutical dosage forms without interference from other dosage form additives and the results were statistically compared with reference method."	( Spectrophotometric and spectrodensitometric methods for the determination of rivastigmine hydrogen tartrate in presence of its degradation product. Abd El-Rahman, MK; El-Bardicy, MG; El-Kosasy, AM; Salem, MY, 2010)	0.36
" The dosage of ChEI treatment could possibly lead to a different functional outcome."	( Long-term outcome and prediction models of activities of daily living in Alzheimer disease with cholinesterase inhibitor treatment. Londos, E; Minthon, L; Wallin, ÅK; Wattmo, C, )	0.13
" Demographic variables, quantity and rate of prescriptions, dosage forms and strengths were analyzed."	( [Drugs used for cognitive impairment. Analysis of 1.5 million prescriptions in Argentina]. Arizaga, RL; Demey, I; Rojas, G, 2013)	0.39
"5 mg/24 h patch on ADL, including autonomy and HLF factors, supports this additional dosing option to prolong patients' independence."	( Efficacy of higher dose 13.3 mg/24 h rivastigmine patch on instrumental activities of daily living in patients with mild-to-moderate Alzheimer's disease. Bellelli, G; Cummings, J; Frölich, L; Grossberg, G; Krahnke, T; Molinuevo, JL; Strohmaier, C, 2013)	0.39
" To compare the transdermal with oral dosage forms, physicians were asked to enrol patients who recently switched from oral to transdermal medication."	( The transdermal formulation of rivastigmine improves caregiver burden and treatment adherence of patients with Alzheimer's disease under daily practice conditions. Adler, G; Articus, K; Mueller, B, 2014)	0.4
" The ability to achieve adjustable, individual, twice-daily dosing during waking hours has good potential to minimise undesirable cholinergic burden and sleep disturbances whilst delivering an effective dose for the treatment of dementia associated with Alzheimer's and Parkinson's disease."	( Absolute bioavailability and safety of a novel rivastigmine nasal spray in healthy elderly individuals. Morgan, TM; Soh, B, 2017)	0.46
" Hence, we analyzed the therapeutic responses of rivastigmine, measured by neuropsychological assessments, among 63 clinically diagnosed AD patients taking a daily dosage of 6-9 mg in relation to their plasma concentration of rivastigmine and NAP 226-90, apolipoprotein E (APOE) genotype and demographic characteristics."	( Factors affecting therapeutic response to Rivastigmine in Alzheimer's disease patients in Taiwan. Chen, TH; Chou, MC; Hsu, CL; Lai, CL; Wu, SJ; Yang, YH, 2017)	0.46
" However, current treatments require frequent dosing either orally or via transdermal patch that lead to compliance issues and administration errors risking serious adverse effects."	( In Vitro and in Vivo Optimization of Phase Sensitive Smart Polymer for Controlled Delivery of Rivastigmine for Treatment of Alzheimer's Disease. Banerjee, A; Lipp, L; Sharma, D; Singh, J, 2020)	0.56
" The optimized formulation significantly increases the dosing interval, and can potentially improve patient compliance as well as quality of life of patients living with Alzheimer's disease."	( In Vitro and in Vivo Optimization of Phase Sensitive Smart Polymer for Controlled Delivery of Rivastigmine for Treatment of Alzheimer's Disease. Banerjee, A; Lipp, L; Sharma, D; Singh, J, 2020)	0.56
" Besides, transdermal drug delivery systems seem to provide hope for the management of various diseases, due to the advantages that they offer in comparison with oral dosage forms."	( Transdermal Drug Delivery Systems and their Potential in Alzheimer's Disease Management. Bülbül, EÖ; Karantas, ID; Mutlu, G; Okur, ME; Okur, NÜ; Siafaka, PI, 2020)	0.56
"0 mg/kg), donepezil tended to promote depression-like behavior, suggesting a u-shaped dose-response curve for FST immobility."	( Multiple cholinesterase inhibitors have antidepressant-like properties in the mouse forced swim test. Fitzgerald, PJ; Ghimire, A; Hale, PJ; Watson, BO, 2021)	0.62
" Patch adhesion favored RID-TDS despite the longer dosing interval."	( Comparative Bioavailability Study of a Novel Multi-Day Patch Formulation of Rivastigmine (Twice Weekly) with Exelon® Transdermal Patch (Daily)- A Randomized Clinical Trial. De la Torre, R; Iniesta, M; Koch, C; Morte, A; Schug, B; Schurad, B; Vaqué, A, 2022)	0.72
" This can be delivered orally or via nasogastric tube with dosing each hour until resolution of symptoms."	( Oral and Transdermal Rivastigmine for the Treatment of Anticholinergic Delirium: A Case Report. Fratta, KA; Ginder, M; Haggerty, DA, 2023)	0.91

Role	Description
EC 3.1.1.8 (cholinesterase) inhibitor	An EC 3.1.1.* (carboxylic ester hydrolase) inhibitor that interferes with the action of cholinesterase (EC 3.1.1.8).
neuroprotective agent	Any compound that can be used for the treatment of neurodegenerative disorders.
cholinergic drug	Any drug used for its actions on cholinergic systems. Included here are agonists and antagonists, drugs that affect the life cycle of acetylcholine, and drugs that affect the survival of cholinergic neurons.
[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
carbamate ester	Any ester of carbamic acid or its N-substituted derivatives.
tertiary amino compound	A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[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]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
acetylcholinesterase	Homo sapiens (human)	Potency	14.6283	0.0025	41.7960	15,848.9004	AID1347395; AID1347397; AID1347398; AID1347399
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	29.8493	0.0002	29.3054	16,493.5996	AID743080
cytochrome P450 2D6	Homo sapiens (human)	Potency	21.8761	0.0010	8.3798	61.1304	AID1645840
histone deacetylase 9 isoform 3	Homo sapiens (human)	Potency	18.8336	0.0376	17.0823	61.1927	AID1259364
[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)
Acetylcholinesterase	Electrophorus electricus (electric eel)	IC50 (µMol)	45.8867	0.0000	0.9453	9.9400	AID1057267; AID1197878; AID1240922; AID1267380; AID1272534; AID1272947; AID1282037; AID1286907; AID1290886; AID1317852; AID1336711; AID1339189; AID1459902; AID1498899; AID1545333; AID1568788; AID1585836; AID1609064; AID1631830; AID1653673; AID1666831; AID1666849; AID1691674; AID1703015; AID1709253; AID1773262; AID1800998; AID1801428; AID1801911; AID1802572; AID1802597; AID1803029; AID1877961; AID1896375; AID548338; AID730448
Acetylcholinesterase	Tetronarce californica (Pacific electric ray)	IC50 (µMol)	187.2000	0.0057	0.4285	5.1200	AID1796782
Cholinesterase	Homo sapiens (human)	IC50 (µMol)	2.7549	0.0000	1.5599	10.0000	AID1068374; AID1164690; AID1166455; AID1313249; AID1330299; AID1406252; AID1428332; AID1472431; AID1503621; AID1526845; AID1545272; AID1601893; AID1631821; AID1633165; AID1673635; AID1691670; AID1698412; AID1702420; AID1729631; AID1739254; AID1763912; AID1767557; AID1773256; AID1796482; AID1796571; AID1796572; AID1856400; AID1865085; AID1889340; AID1901713; AID241439; AID276346; AID298279; AID407881; AID444043; AID594821; AID625547; AID669791; AID724167
Acyl-CoA desaturase 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	1.7100	0.0004	0.1594	1.7100	AID1057266
Acetylcholine receptor subunit epsilon	Rattus norvegicus (Norway rat)	IC50 (µMol)	9.0000	9.0000	9.0000	9.0000	AID1597538
Amine oxidase [flavin-containing] B	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.8750	0.0004	0.7649	12.5000	AID1796508
Amine oxidase [flavin-containing] A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.8750	0.0007	1.9798	12.5000	AID1796508
Acetylcholinesterase	Mus musculus (house mouse)	IC50 (µMol)	5.7375	0.0007	1.1181	8.4000	AID1525514; AID1801050; AID318846; AID696204
Acetylcholinesterase	Mus musculus (house mouse)	Ki	5.6800	0.0000	1.4282	9.3000	AID1327299
Acetylcholinesterase	Homo sapiens (human)	IC50 (µMol)	4.7159	0.0000	0.9332	10.0000	AID1068377; AID1164699; AID1166454; AID1254737; AID1313248; AID1330297; AID1406251; AID1428331; AID1472433; AID1525504; AID1526844; AID1545271; AID1601892; AID1631822; AID1633164; AID1673636; AID1691671; AID1698411; AID1702419; AID1709254; AID1729630; AID1739253; AID1763911; AID1767556; AID1796482; AID1796508; AID1796571; AID1796572; AID1856401; AID1865084; AID1889339; AID1901714; AID241408; AID241692; AID262754; AID276345; AID298278; AID31163; AID31195; AID314091; AID407880; AID511766; AID594820; AID599248; AID600978; AID600980; AID625546; AID669790; AID724168
Acetylcholinesterase	Bos taurus (cattle)	IC50 (µMol)	0.6200	0.0000	0.6106	8.7000	AID710238
Sodium-dependent serotonin transporter	Homo sapiens (human)	IC50 (µMol)	1.0000	0.0001	0.8645	8.7096	AID314096
Sodium-dependent serotonin transporter	Rattus norvegicus (Norway rat)	IC50 (µMol)	1.0000	0.0003	0.8197	8.4900	AID1525515
Delta-type opioid receptor	Mus musculus (house mouse)	IC50 (µMol)	54.0000	0.0001	0.7298	10.0000	AID276346
Cholinesterase	Canis lupus familiaris (dog)	IC50 (µMol)	6.2700	6.2700	6.2700	6.2700	AID1666848
Acetylcholinesterase	Rattus norvegicus (Norway rat)	IC50 (µMol)	9.8042	0.0002	0.5259	7.2000	AID1163504; AID1186312; AID1192720; AID1225690; AID1585834; AID1702416; AID1801409; AID1889336; AID242428; AID395657; AID454342
Tyrosine-protein kinase SYK	Homo sapiens (human)	IC50 (µMol)	0.1600	0.0001	0.8260	10.0000	AID710237
Beta-secretase 1	Homo sapiens (human)	IC50 (µMol)	9.3950	0.0006	1.6194	10.0000	AID1801911
Cholinesterase	Equus caballus (horse)	IC50 (µMol)	4.7835	0.0000	2.2214	9.4000	AID1057266; AID1240923; AID1267381; AID1272535; AID1272948; AID1282036; AID1317853; AID1339190; AID1459903; AID1545334; AID1568789; AID1609066; AID1631819; AID1653674; AID1666832; AID1691672; AID1703002; AID1773260; AID1784743; AID1803029; AID1896376; AID548340; AID730447
Cholinesterase	Mus musculus (house mouse)	IC50 (µMol)	0.8290	0.0091	0.5602	1.9920	AID1633232; AID318847
Carboxylic ester hydrolase	Rattus norvegicus (Norway rat)	IC50 (µMol)	7.3825	0.0004	1.4811	9.8700	AID1585835; AID1702417; AID1709255; AID1889337
Carboxylic ester hydrolase	Equus caballus (horse)	IC50 (µMol)	0.4950	0.0051	2.6984	8.5000	AID44100; AID710237
[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)
Cholinesterase	Equus caballus (horse)	Kd	1.1500	1.1500	1.1500	1.1500	AID1773277
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	Cholinesterase	Homo sapiens (human)
learning	Cholinesterase	Homo sapiens (human)
negative regulation of cell population proliferation	Cholinesterase	Homo sapiens (human)
neuroblast differentiation	Cholinesterase	Homo sapiens (human)
peptide hormone processing	Cholinesterase	Homo sapiens (human)
response to alkaloid	Cholinesterase	Homo sapiens (human)
cocaine metabolic process	Cholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission	Cholinesterase	Homo sapiens (human)
response to glucocorticoid	Cholinesterase	Homo sapiens (human)
response to folic acid	Cholinesterase	Homo sapiens (human)
choline metabolic process	Cholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Cholinesterase	Homo sapiens (human)
acetylcholine catabolic process in synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
regulation of receptor recycling	Acetylcholinesterase	Homo sapiens (human)
osteoblast development	Acetylcholinesterase	Homo sapiens (human)
acetylcholine catabolic process	Acetylcholinesterase	Homo sapiens (human)
cell adhesion	Acetylcholinesterase	Homo sapiens (human)
nervous system development	Acetylcholinesterase	Homo sapiens (human)
synapse assembly	Acetylcholinesterase	Homo sapiens (human)
receptor internalization	Acetylcholinesterase	Homo sapiens (human)
negative regulation of synaptic transmission, cholinergic	Acetylcholinesterase	Homo sapiens (human)
amyloid precursor protein metabolic process	Acetylcholinesterase	Homo sapiens (human)
positive regulation of protein secretion	Acetylcholinesterase	Homo sapiens (human)
retina development in camera-type eye	Acetylcholinesterase	Homo sapiens (human)
acetylcholine receptor signaling pathway	Acetylcholinesterase	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Acetylcholinesterase	Homo sapiens (human)
monoamine transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to hypoxia	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to nutrient	Sodium-dependent serotonin transporter	Homo sapiens (human)
memory	Sodium-dependent serotonin transporter	Homo sapiens (human)
circadian rhythm	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to xenobiotic stimulus	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to toxic substance	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of gene expression	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of serotonin secretion	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Sodium-dependent serotonin transporter	Homo sapiens (human)
response to estradiol	Sodium-dependent serotonin transporter	Homo sapiens (human)
social behavior	Sodium-dependent serotonin transporter	Homo sapiens (human)
vasoconstriction	Sodium-dependent serotonin transporter	Homo sapiens (human)
sperm ejaculation	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of neuron differentiation	Sodium-dependent serotonin transporter	Homo sapiens (human)
positive regulation of cell cycle	Sodium-dependent serotonin transporter	Homo sapiens (human)
negative regulation of organ growth	Sodium-dependent serotonin transporter	Homo sapiens (human)
behavioral response to cocaine	Sodium-dependent serotonin transporter	Homo sapiens (human)
enteric nervous system development	Sodium-dependent serotonin transporter	Homo sapiens (human)
brain morphogenesis	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin uptake	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane depolarization	Sodium-dependent serotonin transporter	Homo sapiens (human)
platelet aggregation	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to retinoic acid	Sodium-dependent serotonin transporter	Homo sapiens (human)
cellular response to cGMP	Sodium-dependent serotonin transporter	Homo sapiens (human)
regulation of thalamus size	Sodium-dependent serotonin transporter	Homo sapiens (human)
conditioned place preference	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion transmembrane transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
amino acid transport	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein import into nucleus	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of DNA-binding transcription factor activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
angiogenesis	Tyrosine-protein kinase SYK	Homo sapiens (human)
cell activation	Tyrosine-protein kinase SYK	Homo sapiens (human)
lymph vessel development	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of receptor internalization	Tyrosine-protein kinase SYK	Homo sapiens (human)
stimulatory C-type lectin receptor signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
adaptive immune response	Tyrosine-protein kinase SYK	Homo sapiens (human)
macrophage activation involved in immune response	Tyrosine-protein kinase SYK	Homo sapiens (human)
neutrophil activation involved in immune response	Tyrosine-protein kinase SYK	Homo sapiens (human)
leukocyte activation involved in immune response	Tyrosine-protein kinase SYK	Homo sapiens (human)
serotonin secretion by platelet	Tyrosine-protein kinase SYK	Homo sapiens (human)
negative regulation of inflammatory response to antigenic stimulus	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein phosphorylation	Tyrosine-protein kinase SYK	Homo sapiens (human)
leukocyte cell-cell adhesion	Tyrosine-protein kinase SYK	Homo sapiens (human)
integrin-mediated signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
animal organ morphogenesis	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of platelet activation	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of tumor necrosis factor-mediated signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Tyrosine-protein kinase SYK	Homo sapiens (human)
leukotriene biosynthetic process	Tyrosine-protein kinase SYK	Homo sapiens (human)
calcium-mediated signaling	Tyrosine-protein kinase SYK	Homo sapiens (human)
platelet activation	Tyrosine-protein kinase SYK	Homo sapiens (human)
B cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
neutrophil chemotaxis	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of protein-containing complex assembly	Tyrosine-protein kinase SYK	Homo sapiens (human)
receptor internalization	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of type I interferon production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of granulocyte macrophage colony-stimulating factor production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-10 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-12 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-3 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-4 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-6 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of interleukin-8 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of tumor necrosis factor production	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of mast cell cytokine production	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of superoxide anion generation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of superoxide anion generation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of cell adhesion mediated by integrin	Tyrosine-protein kinase SYK	Homo sapiens (human)
intracellular signal transduction	Tyrosine-protein kinase SYK	Homo sapiens (human)
collagen-activated tyrosine kinase receptor signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
Fc-epsilon receptor signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
Fc-gamma receptor signaling pathway involved in phagocytosis	Tyrosine-protein kinase SYK	Homo sapiens (human)
interleukin-3-mediated signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
gamma-delta T cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
defense response to bacterium	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic process	Tyrosine-protein kinase SYK	Homo sapiens (human)
mast cell degranulation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of mast cell degranulation	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of neutrophil degranulation	Tyrosine-protein kinase SYK	Homo sapiens (human)
beta selection	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of MAPK cascade	Tyrosine-protein kinase SYK	Homo sapiens (human)
innate immune response	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of B cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of gamma-delta T cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of bone resorption	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of alpha-beta T cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of alpha-beta T cell proliferation	Tyrosine-protein kinase SYK	Homo sapiens (human)
blood vessel morphogenesis	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of phagocytosis	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Tyrosine-protein kinase SYK	Homo sapiens (human)
B cell receptor signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of killing of cells of another organism	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of ERK1 and ERK2 cascade	Tyrosine-protein kinase SYK	Homo sapiens (human)
cellular response to molecule of fungal origin	Tyrosine-protein kinase SYK	Homo sapiens (human)
cellular response to lipid	Tyrosine-protein kinase SYK	Homo sapiens (human)
cellular response to low-density lipoprotein particle stimulus	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of monocyte chemotactic protein-1 production	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of arachidonic acid secretion	Tyrosine-protein kinase SYK	Homo sapiens (human)
regulation of platelet aggregation	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Tyrosine-protein kinase SYK	Homo sapiens (human)
positive regulation of TORC1 signaling	Tyrosine-protein kinase SYK	Homo sapiens (human)
cellular response to lectin	Tyrosine-protein kinase SYK	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Tyrosine-protein kinase SYK	Homo sapiens (human)
cell differentiation	Tyrosine-protein kinase SYK	Homo sapiens (human)
proteolysis	Beta-secretase 1	Homo sapiens (human)
membrane protein ectodomain proteolysis	Beta-secretase 1	Homo sapiens (human)
response to lead ion	Beta-secretase 1	Homo sapiens (human)
protein processing	Beta-secretase 1	Homo sapiens (human)
amyloid-beta formation	Beta-secretase 1	Homo sapiens (human)
amyloid precursor protein catabolic process	Beta-secretase 1	Homo sapiens (human)
positive regulation of neuron apoptotic process	Beta-secretase 1	Homo sapiens (human)
amyloid-beta metabolic process	Beta-secretase 1	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain	Beta-secretase 1	Homo sapiens (human)
prepulse inhibition	Beta-secretase 1	Homo sapiens (human)
cellular response to copper ion	Beta-secretase 1	Homo sapiens (human)
cellular response to manganese ion	Beta-secretase 1	Homo sapiens (human)
presynaptic modulation of chemical synaptic transmission	Beta-secretase 1	Homo sapiens (human)
signaling receptor ligand precursor processing	Beta-secretase 1	Homo sapiens (human)
cellular response to amyloid-beta	Beta-secretase 1	Homo sapiens (human)
amyloid fibril formation	Beta-secretase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
amyloid-beta binding	Cholinesterase	Homo sapiens (human)
catalytic activity	Cholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Cholinesterase	Homo sapiens (human)
cholinesterase activity	Cholinesterase	Homo sapiens (human)
protein binding	Cholinesterase	Homo sapiens (human)
hydrolase activity, acting on ester bonds	Cholinesterase	Homo sapiens (human)
enzyme binding	Cholinesterase	Homo sapiens (human)
choline binding	Cholinesterase	Homo sapiens (human)
identical protein binding	Cholinesterase	Homo sapiens (human)
amyloid-beta binding	Acetylcholinesterase	Homo sapiens (human)
acetylcholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
cholinesterase activity	Acetylcholinesterase	Homo sapiens (human)
protein binding	Acetylcholinesterase	Homo sapiens (human)
collagen binding	Acetylcholinesterase	Homo sapiens (human)
hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
serine hydrolase activity	Acetylcholinesterase	Homo sapiens (human)
acetylcholine binding	Acetylcholinesterase	Homo sapiens (human)
protein homodimerization activity	Acetylcholinesterase	Homo sapiens (human)
laminin binding	Acetylcholinesterase	Homo sapiens (human)
amyloid-beta binding	Acetylcholinesterase	Bos taurus (cattle)
protein binding	Acetylcholinesterase	Bos taurus (cattle)
integrin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoatomic cation channel activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin:sodium:chloride symporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
monoamine transmembrane transporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
antiporter activity	Sodium-dependent serotonin transporter	Homo sapiens (human)
syntaxin-1 binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
cocaine binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
sodium ion binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
identical protein binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
nitric-oxide synthase binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
actin filament binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonin binding	Sodium-dependent serotonin transporter	Homo sapiens (human)
acetylcholinesterase activity	Cholinesterase	Canis lupus familiaris (dog)
cholinesterase activity	Cholinesterase	Canis lupus familiaris (dog)
phosphotyrosine residue binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein kinase activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein serine/threonine kinase activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein tyrosine kinase activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
non-membrane spanning protein tyrosine kinase activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
signaling receptor binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
integrin binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
ATP binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
interleukin-15 receptor binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
kinase activity	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein kinase binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
phosphatase binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
Toll-like receptor binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
SH2 domain binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
phospholipase binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
scaffold protein binding	Tyrosine-protein kinase SYK	Homo sapiens (human)
amyloid-beta binding	Beta-secretase 1	Homo sapiens (human)
endopeptidase activity	Beta-secretase 1	Homo sapiens (human)
aspartic-type endopeptidase activity	Beta-secretase 1	Homo sapiens (human)
protein binding	Beta-secretase 1	Homo sapiens (human)
peptidase activity	Beta-secretase 1	Homo sapiens (human)
beta-aspartyl-peptidase activity	Beta-secretase 1	Homo sapiens (human)
enzyme binding	Beta-secretase 1	Homo sapiens (human)
protein serine/threonine kinase binding	Beta-secretase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
extracellular region	Cholinesterase	Homo sapiens (human)
nuclear envelope lumen	Cholinesterase	Homo sapiens (human)
endoplasmic reticulum lumen	Cholinesterase	Homo sapiens (human)
blood microparticle	Cholinesterase	Homo sapiens (human)
plasma membrane	Cholinesterase	Homo sapiens (human)
extracellular space	Cholinesterase	Homo sapiens (human)
extracellular region	Acetylcholinesterase	Homo sapiens (human)
basement membrane	Acetylcholinesterase	Homo sapiens (human)
extracellular space	Acetylcholinesterase	Homo sapiens (human)
nucleus	Acetylcholinesterase	Homo sapiens (human)
Golgi apparatus	Acetylcholinesterase	Homo sapiens (human)
plasma membrane	Acetylcholinesterase	Homo sapiens (human)
cell surface	Acetylcholinesterase	Homo sapiens (human)
membrane	Acetylcholinesterase	Homo sapiens (human)
neuromuscular junction	Acetylcholinesterase	Homo sapiens (human)
synaptic cleft	Acetylcholinesterase	Homo sapiens (human)
synapse	Acetylcholinesterase	Homo sapiens (human)
perinuclear region of cytoplasm	Acetylcholinesterase	Homo sapiens (human)
side of membrane	Acetylcholinesterase	Homo sapiens (human)
synapse	Acetylcholinesterase	Bos taurus (cattle)
side of membrane	Acetylcholinesterase	Bos taurus (cattle)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
focal adhesion	Sodium-dependent serotonin transporter	Homo sapiens (human)
endosome membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
endomembrane system	Sodium-dependent serotonin transporter	Homo sapiens (human)
presynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
membrane raft	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
postsynaptic membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
serotonergic synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
synapse	Sodium-dependent serotonin transporter	Homo sapiens (human)
plasma membrane	Sodium-dependent serotonin transporter	Homo sapiens (human)
neuron projection	Sodium-dependent serotonin transporter	Homo sapiens (human)
extracellular region	Cholinesterase	Canis lupus familiaris (dog)
cytoplasm	Tyrosine-protein kinase SYK	Homo sapiens (human)
nucleus	Tyrosine-protein kinase SYK	Homo sapiens (human)
cytoplasm	Tyrosine-protein kinase SYK	Homo sapiens (human)
cytosol	Tyrosine-protein kinase SYK	Homo sapiens (human)
plasma membrane	Tyrosine-protein kinase SYK	Homo sapiens (human)
early phagosome	Tyrosine-protein kinase SYK	Homo sapiens (human)
B cell receptor complex	Tyrosine-protein kinase SYK	Homo sapiens (human)
protein-containing complex	Tyrosine-protein kinase SYK	Homo sapiens (human)
T cell receptor complex	Tyrosine-protein kinase SYK	Homo sapiens (human)
plasma membrane	Tyrosine-protein kinase SYK	Homo sapiens (human)
lysosome	Beta-secretase 1	Homo sapiens (human)
endosome	Beta-secretase 1	Homo sapiens (human)
early endosome	Beta-secretase 1	Homo sapiens (human)
late endosome	Beta-secretase 1	Homo sapiens (human)
multivesicular body	Beta-secretase 1	Homo sapiens (human)
endoplasmic reticulum lumen	Beta-secretase 1	Homo sapiens (human)
Golgi apparatus	Beta-secretase 1	Homo sapiens (human)
trans-Golgi network	Beta-secretase 1	Homo sapiens (human)
plasma membrane	Beta-secretase 1	Homo sapiens (human)
synaptic vesicle	Beta-secretase 1	Homo sapiens (human)
cell surface	Beta-secretase 1	Homo sapiens (human)
endosome membrane	Beta-secretase 1	Homo sapiens (human)
membrane	Beta-secretase 1	Homo sapiens (human)
axon	Beta-secretase 1	Homo sapiens (human)
dendrite	Beta-secretase 1	Homo sapiens (human)
neuronal cell body	Beta-secretase 1	Homo sapiens (human)
membrane raft	Beta-secretase 1	Homo sapiens (human)
recycling endosome	Beta-secretase 1	Homo sapiens (human)
Golgi-associated vesicle lumen	Beta-secretase 1	Homo sapiens (human)
hippocampal mossy fiber to CA3 synapse	Beta-secretase 1	Homo sapiens (human)
endosome	Beta-secretase 1	Homo sapiens (human)
plasma membrane	Beta-secretase 1	Homo sapiens (human)
trans-Golgi network	Beta-secretase 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (517)

Assay ID	Title	Year	Journal	Article
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1347425	Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
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.
AID1347424	RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)	2019	The Journal of biological chemistry, 11-15, Volume: 294, Issue:46	Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1796782	Cholinesterase Inhibition Assay from Article 10.1021/jm060293s: \\Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).\\	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
AID1609066	Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method	2019	European journal of medicinal chemistry, Nov-01, Volume: 181	Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies.
AID1773279	Pseudo-irreversible inhibition of equine serum BuChE assessed as overall carbamolyation-rate using butyrylthiocholine iodide as substrate preincubated with enzyme for 60 mins prior to substrate addition	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1282034	n-Octanol-water partition coefficient, log P of the compound after 15 mins by shake flask method	2016	Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7	Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.
AID1704774	Effect on total exploration time in Sprague-Dawley rat at 0.2 mg/kg, po measured after 1 hr by novel object recognition test
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.
AID1666843	Inhibition of human erythrocyte AChE assessed as decarbamylation rate constant using S-acetylthiocholine iodide as substrate preincubated for 15 to 60 mins followed by substrate addition by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID1068377	Inhibition of human AChE using acetylthiocholine as substrate by Ellman's method	2014	European journal of medicinal chemistry, Feb-12, Volume: 73	Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.
AID1601893	Inhibition of human serum BChE using butyrylthiocholine as substrate by Ellman's assay	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Indazolylketones as new multitarget cannabinoid drugs.
AID1889339	Inhibition of human erythrocyte AChE using acetylthiocholine as substrate incubated for 15 mins by DTNB reagent based Ellman's method	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1186316	Inhibition of Amyloid beta (1 to 40) (unknown origin) assessed as self-mediated fibril formation at 50 uM incubated for 48 hrs by transmission electron microscopy	2014	Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17	Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.
AID1272949	Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.
AID1576365	Solubility of the compound in water	2019	MedChemComm, Nov-01, Volume: 10, Issue:11	Druggability profile of stilbene-derived PPAR agonists: determination of physicochemical properties and PAMPA study.
AID1336711	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2017	Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3	Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1272534	Inhibition of electric eel AChE using ATC as substrate preincubated for 15 mins followed by substrate addition measured at 1 min intervals by Ellman method	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.
AID1633232	Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate measured after 30 mins by Ellman's method relative to control	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID1896377	Selectivity index, ratio of IC50 for inhibition of electric eel AChE to IC50 for inhibition of equine serum BuChE 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.
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.
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.
AID395658	Inhibition of BChE in rat serum after 15 mins by modified Ellman method	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
AID1763911	Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured by Ellman's method	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.
AID436566	Inhibition of BChE in human serum assessed as hydrolysis of butyrylthiocholine by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
AID1773277	Pseudo-irreversible inhibition of equine serum BuChE assessed as binding affinity in an equilibrium state using butyrylthiocholine iodide as substrate preincubated with enzyme for 60 mins prior to substrate addition	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1763912	Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured by Ellman's method	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.
AID1076771	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 2	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
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.
AID1773280	Pseudo-irreversible inhibition of equine serum BuChE assessed as decarbamolyation-rate using butyrylthiocholine iodide as substrate preincubated with enzyme for 60 mins prior to substrate addition	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1327290	Neuroprotective activity against scopolamine-induced oxidative damage in albino mouse assessed as glutathione reductase level in brain measured per mg of protein at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge by Ellamns assay (Rvb = 0.008	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1702425	Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at IC50 using diluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
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.
AID511766	Inhibition of human AChE by Ellmans 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.
AID1739254	Inhibition of BuChE (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.
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.
AID1186312	Inhibition of AChE in rat cortex homogenates using acetylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method	2014	Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17	Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.
AID1327302	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as basal latency to reach shock free zone at 0.5 mg/kg, ip administered 5 mins post scopolamine-challengen and 35 mins prior to training by passive avoidance test (Rvb =	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
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.
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).
AID1076768	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1865084	Inhibition of human recombinant AChe using acetylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method
AID396863	Inhibition of BuChE in Wistar rat brain homogenates at 1 uM by Ellman's method	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Site-activated multifunctional chelator with acetylcholinesterase and neuroprotective-neurorestorative moieties for Alzheimer's therapy.
AID1286907	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate by Ellman's method	2016	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6	In silico to in vitro screening of hydroxypyridinones as acetylcholinesterase inhibitors.
AID314096	Inhibition of SERT	2008	Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3	Multi-target-directed ligands to combat neurodegenerative diseases.
AID1076769	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1428330	Inhibition of carboxylesterase (unknown origin) using 4-nitrophenyl acetate as substrate by UV-Vis spectrophotometer
AID1225690	Inhibition of AChE in rat cortex using acetylthiocholine iodide as substrate after 15 mins by Ellman's method	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
AID1702421	Selectivity index, ratio of IC50 for human serum BChe to IC50 for human erythrocytes AChE	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1568795	Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity preincubated for 15 mins followed by AAPH addition and measured every minute for 90 mins by ORAC-FL assay	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1076772	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 10 nM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1702431	Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at 0.1 times IC50 measured immediately using diluted compound	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1327299	Competitive inhibition of albino mouse brain AChE using acetylthiocholine iodide as substrate measured up to 2 mins by Ellmans method	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1666844	Inhibition of human plasma BChE assessed as decarbamylation rate constant using S-butyrylthiocholine iodide as substrate preincubated for 15 to 60 mins followed by substrate addition by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID1702419	Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1633203	Inhibition of mouse plasma BuChE using S-butyrylacetylthiocholine iodide as substrate at 10 uM measured after 30 mins by Ellman's method relative to control	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1568791	Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1 times IC50 using butyrylthiocholine iodide as substrate by Ellman's method relative to control	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1290889	Antioxidant activity assessed as AAPH scavenging activity assessed as trolox equivalent after 15 mins measured every min for 90 mins by ORAC-FL method relative to control trolox	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease.
AID1653673	Inhibition of electric eel AChE using acetylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	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.
AID1709503	In vivo inhibition of AChE in ICR mouse assessed as reduction in enzyme activity in cerebral cortex at 2 mg/kg, ig via gavage measured after 30 mins using acetylthiocholine iodide as substrate by DTNB reagent based assay	2021	Bioorganic & medicinal chemistry, 05-01, Volume: 37	Twin drug design, synthesis and evaluation of diosgenin derivatives as multitargeted agents for the treatment of vascular dementia.
AID1568816	Effect on total arm entries in Kunming mouse model of scopolamine-induced cognitive impairment in at 6 mg/kg, ig pretreated for 30 min followed by scopolamine challenge and measured after 30 mins by Y-maze test	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1192720	Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman method	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID454342	Inhibition of AChE in rat cortex after 15 mins by modified Ellman's method	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.
AID1666849	Inhibition of Electric eel AChE using acetylcholine iodide as substrate by spectrophotometry based Ellman's method	2020	Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6	Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
AID1313249	Inhibition of human serum BuChE using acetylthiocholine iodide as substrate preincubated for 20 to 60 mins followed by substrate addition by Ellman's method	2016	Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13	Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
AID1666841	Inhibition of human erythrocyte AChE assessed as second order carbamylation rate constant using S-acetylthiocholine iodide as substrate preincubated for 15 to 60 mins followed by substrate addition by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
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).
AID230720	Ratio of the IC50 value against AChE of human erythrocytes to that of BuChE of horse serum	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1525504	Inhibition of AChE in human erythrocytes preincubated for 60 mins followed by substrate addition by Ellman's method	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID1631821	Inhibition of human BuChE using ACTI as substrate incubated for 40 mins 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.
AID1327291	Neuroprotective activity against scopolamine-induced oxidative damage in albino mouse assessed as superoxide dismutase level in brain at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge measured at every 30 to 60 secs interval for 2 mins by NB	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1691673	Selectivity index, ratio of IC50 for Electrophorus electricus AChE to IC50 for equine serum BuChE	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
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).
AID1163504	Inhibition of Sprague-Dawley rat brain AChE using acetylthiocholin iodide as substrate preincubated for 25 mins by Ellman's/UV-vis spectroscopy analysis	2014	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 24, Issue:19	Synthesis and acetylcholinesterase inhibitory activity of Mannich base derivatives flavokawain B.
AID1698412	Inhibition of human BChE by Ellman's method	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.
AID1691672	Inhibition of equine serum BuChE using BTC as substrate after 15 mins by Ellman's method	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1076764	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1585837	Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity at 5 uM preincubated for 15 mins followed by AAPH addition measured every minute for 90 mins by ORAC fluorescein assay	2018	Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24	Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1568793	Reversible inhibition of equine serum BuChE assessed as enzyme activity at IC50 using butyrylthiocholine iodide as substrate by Ellman's method relative to control	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1327306	Neuroprotective activity against scopolamine-induced oxidative damage in albino mouse assessed as catalase activity by measuring H2O2 decomposition per mg of protein at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge (Rvb = 1.37 +/- 0.25 micr	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID454343	Inhibition of BChE in rat serum after 15 mins by modified Ellman's method	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	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).
AID1668220	Inhibition of rat bone marrow myeloperoxidase using H2O2 as substrate at 10 uM after 20 mins by TMB based method (Rvb = - 1.4 +/- 12.7%)	2020	Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10	Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation.
AID1503621	Inhibition of BuChE (unknown origin) pre-incubated for 20 mins before S-Butyrylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
AID1282036	Inhibition of equine serum BChE by spectrophotometric-based Ellman's method	2016	Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7	Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.
AID407784	Inhibition of human AChE assessed as carbamylation	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.
AID1633165	Inhibition of human serum butyrylcholinesterase using BTCI as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method	2019	European journal of medicinal chemistry, Apr-01, Volume: 167	Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
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.
AID1631824	Selectivity ratio of IC50 for human AChE to IC50 for human BuChE	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.
AID1666831	Inhibition of electric eel AChE using S-acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition and measured for 5 mins by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID599248	Inhibition of human recombinant AChE preincubated for 30 mins before DTNB substrate addition by spectrophotometric assay based Ellman's method	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID318846	Inhibition of mouse brain AChE	2008	Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7	Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID1220559	Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID1666848	Inhibition of dog serum BChE using butrylthiocholine iodide as substrate by spectrophotometry based Ellman's method	2020	Bioorganic & medicinal chemistry letters, 03-15, Volume: 30, Issue:6	Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
AID1445561	Toxicity in ip dosed CD1 mouse assessed as mortality administered as qd after 48 hrs	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.
AID1729631	Inhibition of human BuChE using S-butyrylthiocholine as substrate preincubated for 30 mins followed by substrate addition and measured after 25 mins by DTNB-reagent based spectrophotometric method	2021	European journal of medicinal chemistry, Jan-15, Volume: 210	Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
AID1272947	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by Ellman's method	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.
AID318848	Selectivity for mouse brain AChE over mouse serum BChE	2008	Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7	Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID1254737	Inhibition of AChE (unknown origin)	2015	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21	A computational view on the significance of E-ring in binding of (+)-arisugacin A to acetylcholinesterase.
AID444042	Inhibition of BuChE in human liver microsomes assessed as dissociation constant for Michaelis complex formation by enzyme kinetic study	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
AID1327289	Neuroprotective activity against scopolamine-induced oxidative damage in albino mouse assessed as nitrite level in plasma at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge by Greiss assay (Rvb = 483.5 +/- 27.1 ug/ml)	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1691667	Inhibition of human serum BuChE assessed as residual activity at IC50 using acetylcholine iodide as substrate measured after dilution by Ellman's method relative to control	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID436568	Inhibition of BChE in human serum assessed as hydrolysis of butyrylthiocholine at 10 ug/mL by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
AID1282042	Pseudo-irreversible inhibition of Torpedo californica AChE using acetylthiocholine as substrate by cornish bowden plot analysis	2016	Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7	Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.
AID1313248	Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate preincubated for 20 to 60 mins followed by substrate addition by Ellman's method	2016	Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13	Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
AID1225691	Inhibition of BuChE in rat serum using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
AID1517880	Inhibition of LPS-induced nitric oxide in mouse BV2 cells assessed as reduction in intracellular nitric oxide level at 1 uM preincubated with compound for 1 hr followed by LPS addition and measured after 24 hrs by cell analyser based assay (Rvb = 145.7 +/	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Design and synthesis of H
AID599264	Toxicity in rat assessed as induction of seizures incidence at 5 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID395657	Inhibition of AChE in rat cortex after 15 mins by modified Ellman method	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
AID1773262	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1526845	Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 20 to 60 mins followed by substrate addition by Ellman's method	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer's Disease Mouse Model.
AID1568817	Reversal of scopolamine-induced memory cognitive memory impairment in Kunming mouse assessed as change in spontaneous alteration behavior at 6 mg/kg, ig pretreated for 30 mins followed by scopolamine challenge and after 30 mins by Y-maze test (Rvb = 45.6%	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID395659	Selectivity ratio of IC50 for BChE in rat serum to IC50 for AChE in rat cortex	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
AID1736966	Reversible inhibition of human BChE assessed as residual activity at IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1767554	Inhibition of human amyloid beta (25 to 35) self-induced aggregation at 100 uM after 48 hrs by thioflavin-T fluorescence relative to control	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID1901713	Inhibition of C-terminal 6His-tagged human recombinant BuChE (29 to 602 residues) using butyrylthiocholine iodide 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.
AID1220557	Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
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).
AID1668218	Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM after 30 mins (Rvb = 1.9 +/- 1.2%)	2020	Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10	Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation.
AID1702520	Reversal of scopolamine-induced Kunming mouse model of memory impairment assessed as spontaneous alteration at 6 mg/kg by Y-maze test (Rvb = 41.6 %)	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1877962	Inhibition of rat serum BuChE by Ellman's method	2022	European journal of medicinal chemistry, Feb-15, Volume: 230	Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1503624	Permeability at 100 ug/ml incubated for 10 hrs by PAMPA method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1076767	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 100 nM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rel	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID781326	pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X	2014	Pharmaceutical research, Apr, Volume: 31, Issue:4	Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1597573	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Dyskinesia recovery rate at 250 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1702427	Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at IC50 using undiluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
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.
AID1197878	Inhibition of electric eel acetylcholinesterase using acetylthiocholine iodide as substrate after 15 mins by Ellman's method	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Potent acetylcholinesterase inhibitors: design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives.
AID599251	Toxicity in po dosed rat assessed as maximum tolerated dose at which reversible and non-life threatening cholinergic effect observed	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID599263	Toxicity in rat assessed as induction of diarrhea incidence at 5 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1338166	Inhibition of AChE (unknown origin) at 1 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents 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.
AID1691792	Effect on spontaneous alteration behavior in mouse assessed as change in total arm entry at 6 mg/kg by Y-maze test	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1166454	Inhibition of AChE (unknown origin) using acetylthiocholine iodide as substrate incubated for 25 mins by Ellman's method	2014	Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21	Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
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.
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.
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
AID1889337	Inhibition of rat serum Butyrylcholine esterase using butyrylthiocholine as substrate incubated for 15 mins by DTNB reagent based Ellman's method	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1428331	Inhibition of acetylcholinesterase (unknown origin) using acetylthiocholine iodide as substrate after 25 mins by Ellmann method
AID1729630	Inhibition of human AChE using acetylthiocholine as substrate preincubated for 30 mins followed by substrate addition and measured after 25 mins by DTNB-reagent based spectrophotometric method	2021	European journal of medicinal chemistry, Jan-15, Volume: 210	Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
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.
AID1076770	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 24	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1597572	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Dyskinesia recovery rate at 50 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID599267	Inhibition of human recombinant AChE pre-inhibited with exposure to compound followed by incubation in phosphate buffer at 37 degC assessed as reconstituted enzyme-mediated decarbamylation half life by spectrophotometric assay based Ellman's method	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1784746	Inhibition of HFIP-pretreated human recombinant amyloid beta (1 to 42) self aggregation at 10 uM incubated up to 48 hrs under shaking condition and measured every 3 min by Thioflavin T based fluorescence assay relative to control	2021	European journal of medicinal chemistry, Dec-05, Volume: 225	Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT
AID407880	Inhibition of human recombinant AchE after 20 mins by Ellman's method	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
AID1192742	Neuroprotective effect in scopolamine-treated Kunming mouse hippocampus assessed as increase in vitality of ChAT at 6 mg/kg by Ellman method	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1525515	Inhibition of rat synaptosome SERT	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID1736969	Inhibition of human BChE assessed as residual activity at IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID407782	Inhibition of Torpedo californica AChE assessed as carbamylation	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.
AID44100	In vitro inhibitory concentration against Butyrylcholinesterase of horse serum; value ranges from 0.81-0.86	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID444043	Inhibition of BuChE	2010	Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3	Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor.
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.
AID1545333	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by Ellman's method	2019	Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6	Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1889336	Inhibition of rat cortex AChE using acetylthiocholine as substrate incubated for 15 mins by DTNB reagent based Ellman's method	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1691794	Improvement in cognitive impairment in scopolamine-induced mouse model of amnesia assessed as change in spontaneous alteration at 6 mg/kg by Y-maze test (Rvb = 40.8%)	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
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.
AID1220558	Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID1631831	Selectivity ratio of IC50 for human plasma BuChE to IC50 for human erythrocyte AChE	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.
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.
AID1889348	Reversible inhibition of human AChE assessed as increase in enzyme activity at 0.1 times of IC50 concentration by dilution method relative to control	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1327304	Inhibition of albino mouse brain AChE using acetylthiocholine iodide as substrate measured for 2 mins by Ellmans method	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1653674	Inhibition of equine serum BuChE using butyrylthiocholine chloride as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	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.
AID242428	In vitro inhibitory concentration against rat cortex acetylcholinesterase	2005	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17	Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
AID1517868	Induction of H2S generation in mouse BV2 cells at 100 uM after 45 mins by WSP-1 fluorescence dye based spectrofluorimetric analysis	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Design and synthesis of H
AID1186313	Inhibition of BChE in rat serum using butyrylthiocholine iodide substrate incubated for 15 mins by UV spectroscopy based Ellman's method	2014	Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17	Design, synthesis and evaluation of rivastigmine and curcumin hybrids as site-activated multitarget-directed ligands for Alzheimer's disease therapy.
AID1736967	Reversible inhibition of human BChE assessed as residual activity at 0.1 times of IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1673633	Selectivity index, ratio of IC50 for human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method to IC50 for human erythrocytes AChE using acetylthiocholine iodide as substrate p	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.
AID1773255	Inhibition of human AChE using acetylthiocholine iodide as substrate at 20 uM preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
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.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	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).
AID1702423	Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at 0.1 times IC50 using diluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1597578	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Response efficiency at 50 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1597577	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Response efficiency at 10 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1767555	Inhibition of human AchE-induced amyloid beta (25 to 35)aggregation at 100 uM after 48 hrs by ThT fluorescence assay relative to control	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID1702416	Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1736964	Reversible inhibition of human AChE assessed as residual activity at IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID600980	Inhibition of human erythrocytes 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.
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.
AID1076775	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of amyloid beta 1 to 42-induced toxicity by measuring cell viability at 100 uM pretreated for 24 hrs followed by amyloid beta 1 to 42 challenge measured after 2	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1290886	Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholine iodide substrate after 15 mins by spectrophotometric method	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease.
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.
AID669791	Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated for 90 mins before substrate addition by Ellman's method	2012	ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3	The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?
AID1666832	Inhibition of equine serum BChE using S-butyrylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition and measured for 5 mins by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID1877961	Inhibition of electric eel AChE by Ellman's method	2022	European journal of medicinal chemistry, Feb-15, Volume: 230	Development of novel 2-aminoalkyl-6-(2-hydroxyphenyl)pyridazin-3(2H)-one derivatives as balanced multifunctional agents against Alzheimer's disease.
AID1327305	Inhibition of albino mouse brain AChE assessed as Km for substrate using acetylthiocholine iodide as substrate measured for 2 mins by Ellmans method	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1767556	Inhibition of recombinant human AChE using acetylthiocholine iodide as substrate measured after 7 mins by Ellman's method	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID1282035	Selectivity ratio of IC50 for electric eel AChE to IC50 for equine serum BChE	2016	Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7	Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.
AID1338167	Inhibition of AChE (unknown origin) at 5 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease.
AID669790	Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 90 mins before substrate addition by Ellman's method	2012	ACS medicinal chemistry letters, Mar-08, Volume: 3, Issue:3	The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?
AID1503620	Inhibition of AChE (unknown origin) at 500 nM pre-incubated for 20 mins before acetylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
AID276345	Inhibition of AChE	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID1633169	Selectivity index, ratio of IC50 for inhibition of human serum butyrylcholinesterase to IC50 for inhibition of human erythrocyte acetylcholinesterase	2019	European journal of medicinal chemistry, Apr-01, Volume: 167	Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
AID1773260	Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1691671	Inhibition of human erythrocytes AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID599266	Inhibition of human recombinant AChE pre-inhibited with exposure to compound followed by incubation in phosphate buffer at 37 degC assessed as reconstituted enzyme-mediated decarbamylation rates by spectrophotometric assay based Ellman's method	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
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.
AID1569986	Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1xIC50 using butyrylthiocholine iodide as substrate measured at 240 mins after dilution by Ellman's method relative to control	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
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).
AID1709254	Inhibition of human AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2021	Bioorganic & medicinal chemistry, 04-01, Volume: 35	Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1220554	Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID1773256	Inhibition of human serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 5 mins by Ellman's method	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
AID1290888	Selectivity index, ratio of IC50 for rat serum butyrylcholinesterase to IC50 for Electrophorus electricus acetylcholinesterase	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease.
AID1889345	Reversible inhibition of human AChE assessed as enzyme recovery activity at IC50 concentration by dilution method relative to control	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1901716	Selectivity ratio of IC50 for inhibition of C-terminal 6His-tagged human recombinant BuChE (29 to 602 residues) using butyrylthiocholine iodide as substrate to IC50 for inhibition of C-terminal 6His-tagged human recombinant AChE (32 to 614 residues) expre	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.
AID1568788	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1702422	Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at IC50 using diluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1472433	Inhibition of recombinant human AChE using acetylthiocholine as substrate after 1 min by Ellman's method	2018	Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1	The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
AID436569	Inhibition of BChE in human serum assessed as hydrolysis of butyrylthiocholine at 1 ug/mL by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
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AID1889350	Pseudo-irreversible inhibition of human AChE assessed as restoration of enzyme activity at 0.1 time of IC50 concentration incubated for 120 mins by dilution method relative to control	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1633205	Inhibition of mouse brain AChE at 10 uM using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID31195	In vitro inhibitory concentration against purified Acetylcholinesterase of human erythrocytes; value ranges from 0.74-1.2	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for 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.
AID1503619	Inhibition of BuChE (unknown origin) at 500 nM pre-incubated for 20 mins before S-Butyrylthiocholine iodide substrate addition by Ellman reagent based spectrophotometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Nature-based molecules combined with rivastigmine: A symbiotic approach for the synthesis of new agents against Alzheimer's disease.
AID1773259	Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 2 hrs by microplate reader method	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
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.
AID1585835	Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman's method	2018	Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24	Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID298280	Inhibition of human AChE-induced amyloid beta (1-40) aggregation at 100 uM	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.
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.
AID1865085	Inhibition of human recombinant BuChe using butyrylthiocholine iodide as substrate incubated for 10 mins by DTNB reagent based Ellman's method
AID1569985	Reversible inhibition of equine serum BuChE assessed as enzyme activity at 1xIC50 using butyrylthiocholine iodide as substrate measured after dilution by Ellman's method relative to control	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1569984	Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1xIC50 using butyrylthiocholine iodide as substrate measured after dilution by Ellman's method relative to control	2019	European journal of medicinal chemistry, Oct-15, Volume: 180	Design, synthesis, in-silico and biological evaluation of novel chalcone derivatives as multi-function agents for the treatment of Alzheimer's disease.
AID1889338	Selectivity index, ratio of IC50 for inhibition of rat serum butyrylcholine esterase to IC50 for inhibition of rat cortex AChE	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1526844	Inhibition of human serum AChE using acetylthiocholine iodide as substrate preincubated for 20 to 60 mins followed by substrate addition by Ellman's method	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Highly Selective Butyrylcholinesterase Inhibitors with Tunable Duration of Action by Chemical Modification of Transferable Carbamate Units Exhibit Pronounced Neuroprotective Effect in an Alzheimer's Disease Mouse Model.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
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.
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.
AID318847	Inhibition of mouse serum BChE	2008	Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7	Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
AID1691670	Inhibition of human serum BuChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1327296	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as escape latency time at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 4 by Morris water maze test (Rvb = 8	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
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).
AID26924	Pseudo-first order rate constant for carbamoylation of ACHE at 10 (uM) concentration	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1330304	Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 25 uM after 48 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1267381	Inhibition of horse serum butyrylcholinesterase using butyrylthiocholine 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.
AID599252	Inhibition of total plasma cholinesterase in rat at 5 mg/kg, po measured 30 to 180 mins post dose	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1633164	Inhibition of human erythrocyte acetylcholinesterase using acetylthiocholine iodide as substrate pre-incubated for 10 mins followed by substrate addition and measured for 6 mins by Ellman's method	2019	European journal of medicinal chemistry, Apr-01, Volume: 167	Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
AID710236	Selectivity ratio of IC50 for equine BuChE to IC50 for bovine AChE	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Carbamate derivatives of indolines as cholinesterase inhibitors and antioxidants for the treatment of Alzheimer's disease.
AID1192722	Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex AChE	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
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.
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.
AID1428332	Inhibition of butyrylcholinesterase (unknown origin) using butyrylthiocholine iodide as substrate after 25 mins by Ellmann method
AID1330297	Inhibition of human recombinant AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1068374	Inhibition of human BuChE using butyrylthiocholine as substrate by Ellman's method	2014	European journal of medicinal chemistry, Feb-12, Volume: 73	Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.
AID703067	Ratio of drug level from brain to plasma in rat administered via intranasal route	2012	Journal of medicinal chemistry, Oct-11, Volume: 55, Issue:19	Design, synthesis, and structure-activity relationship of N-arylnaphthylamine derivatives as amyloid aggregation inhibitors.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID567091	Drug absorption in human assessed as human intestinal absorption rate	2011	European journal of medicinal chemistry, Jan, Volume: 46, Issue:1	Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID1330303	Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 12.5 uM after 48 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID436578	Cytotoxicity against human A549 cells assessed as cell viability at 100 ug/mL after 24 hrs by MTT assay relative to control	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
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).
AID1709253	Inhibition of Electrophorus electricus AChE using acetylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2021	Bioorganic & medicinal chemistry, 04-01, Volume: 35	Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID730446	Lipophilicity, log P of the compound by HPLC analysis	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
AID1886773	Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in amyloid beta (1 to 42) peptide level in brain at 1 mg/kg, icv measured on day 14 by ELISA
AID276346	Inhibition of BChE	2006	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22	6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
AID1901714	Inhibition of C-terminal 6His-tagged human recombinant AChE (32 to 614 residues) expressed in HEK293 cells using acetylthiocholine iodide 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.
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).
AID1597579	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Response efficiency at 250 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID710237	Inhibition of equine BuChE after 120 mins by Ellman's method	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Carbamate derivatives of indolines as cholinesterase inhibitors and antioxidants for the treatment of Alzheimer's disease.
AID1889347	Reversible inhibition of human AChE assessed as enzyme recovery activity at undiluted IC50 concentration relative to control	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of 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.
AID1736965	Reversible inhibition of human AChE assessed as residual activity at 0.1 times of IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
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.
AID1290887	Inhibition of rat serum butyrylcholinesterase using butyrylthiocholine iodide substrate after 15 mins by spectrophotometric method	2016	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8	Pterostilbene-O-acetamidoalkylbenzylamines derivatives as novel dual inhibitors of cholinesterase with anti-β-amyloid aggregation and antioxidant properties for the treatment of Alzheimer's disease.
AID1856401	Pseudo-irreversible inhibition of human AChE using acetylthiocholineiodide as substrate preincubated for 20 to 60 mins followed by substrate addition and measured for 5 mins by DTNB reagent based Ellman's 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.
AID26927	Pseudo-first order rate constant for carbamoylation of ACHE at 20 (uM) concentration	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1702424	Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at IC50 using undiluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
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.
AID1724106	Memory enhancement effect in rat assessed as increase in total exploratory time for novel objects at 0.1 to 0.3 mg/kg, po administered 1 hr prior to acquisition trial and measured after 24 hrs by novel object recognition test	2020	Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20	Synthesis and pharmacological evaluation of piperidine (piperazine)-amide substituted derivatives as multi-target antipsychotics.
AID407881	Inhibition of human serum BuchE after 20 mins by Ellman's method	2008	Journal of medicinal chemistry, May-22, Volume: 51, Issue:10	Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
AID1666842	Inhibition of human plasma BChE assessed as second order carbamylation rate constant using S-butyrylthiocholine iodide as substrate preincubated for 15 to 60 mins followed by substrate addition by Ellman's method	2020	Bioorganic & medicinal chemistry, 03-01, Volume: 28, Issue:5	Design, synthesis and biological evaluation of novel carbamates as potential inhibitors of acetylcholinesterase and butyrylcholinesterase.
AID625546	Inhibition of human serum recombinant AChE after 20 mins using acetylthiocholine iodide as a substrate by Ellman's assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID1889341	Selectivity index, ratio of IC50 for inhibition of human serum BuChE to IC50 for inhibition of human erythrocyte AChE	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1585834	Inhibition of rat cortex AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method	2018	Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24	Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1702426	Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at 0.1 times IC50 using diluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1729632	Selectivity index, ratio of IC50 for human BuCHE using S-butyrylthiocholine as substrate to IC50 human AChE using acetylthiocholine as substrate	2021	European journal of medicinal chemistry, Jan-15, Volume: 210	Pleiotropic prodrugs: Design of a dual butyrylcholinesterase inhibitor and 5-HT
AID1327292	Neuroprotective activity against scopolamine-induced oxidative damage in albino mouse assessed as lipid peroxidation in brain by measuring MDA level per mg protein at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge by TBARS assay (Rvb = 2.73	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1585836	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate after 15 mins by Ellman's method	2018	Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24	Discovery of novel 2,5-dihydroxyterephthalamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1597538	Inhibition of rat brain cortex AChE using acetylthiocholine iodide as substrate incubated for 15 mins by spectrophotometry	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1568789	Inhibition of equine serum BuChE using S-butyrylthiocholine iodide as susbtrate preincubated for 6 mins followed by substrate addition measured up to 3 mins by Ellman's method	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
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.
AID1336714	Antioxidant activity assessed as trolox equivalents of AAPH radical scavenging activity at 5 uM preincubated for 15 mins followed by AAPH addition measured every 60 sec for 90 mins by ORAC-FL assay	2017	Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3	Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease.
AID1327300	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as escape latency time at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 1 by Morris water maze test (Rvb = 8	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1767558	Selectivity index, ratio of IC50 for human BuChE to IC50 for human AChE	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID1330306	Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 100 uM after 48 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1698414	Selectivity index, ratio of IC50 for human BChE to IC50 for human AChE by Ellman's method	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.
AID1500949	Passive permeability of the compound at 100 uM after 6 hrs by PAMPA	2017	European journal of medicinal chemistry, Oct-20, Volume: 139	Hydroxy-substituted trans-cinnamoyl derivatives as multifunctional tools in the context of Alzheimer's disease.
AID1428334	Octanol-water partition coefficient, log P of the compound at pH 7.4 by shake flask method
AID1192721	Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate after 15 mins by Ellman method	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1327297	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as escape latency time at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 3 by Morris water maze test (Rvb = 8	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1330298	Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 6.25 uM after 48 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1889340	Inhibition of human serum BuChE using butyrylthiocholine as substrate incubated for 15 mins by DTNB reagent based Ellman's method	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1240925	Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BChE	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.
AID1596338	Inhibition of equine serum BChE at 50 nM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured for 5 mins by Ellman's method	2019	European journal of medicinal chemistry, Jul-15, Volume: 174	Multi-targeted ChEI-copper chelating molecules as neuroprotective agents.
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.
AID395660	Cognitive enhancing effect against scopolamine-induced acquisition memory deficit in mouse assessed as times of step-down at 2 mg/kg, intragastric gavage after 24 hrs by step-down passive avoidance test	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
AID1339189	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	2017	Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4	Synthesis, anticholinesterase activity and molecular modeling study of novel carbamate-substituted thymol/carvacrol derivatives.
AID1762102	Cognitive enhancement effect in rat assessed as effect on total exploration time at 0.05 to 0.3 mg/kg, po administered 1 hr prior to acquisition trial and by novel object recognition test	2021	Bioorganic & medicinal chemistry letters, 05-15, Volume: 40	Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1472431	Inhibition of human BuChE using butyrylthiocholine as substrate after 1 min by Ellman's method	2018	Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1	The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity.
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.
AID1633202	Inhibition of mouse brain AChE using acetylthiocholine iodide as substrate measured after 30 mins by Ellman's method	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
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).
AID1762069	Cognitive enhancement effect in rat assessed as increase in time spent in exploring novel object at 0.3 mg/kg, po administered 1 hr prior to acquisition trial by novel object recognition test	2021	Bioorganic & medicinal chemistry letters, 05-15, Volume: 40	Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
AID1192729	Neuroprotective effect against H2O2-induced rat PC12 cell injury assessed as cell viability at 10 uM incubated for 2 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay (Rvb = 57.6%)	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1633201	Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
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.
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.
AID599249	Inhibition of purified human plasma BuChE preincubated for 30 mins before DTNB substrate addition by spectrophotometric assay based Ellman's method	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1703015	Inhibition of recombinant electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by addition of substrate and measured after 20 mins by DTNB reagent based Ellman's method	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	The structure-based optimization of δ-sultone-fused pyrazoles as selective BuChE inhibitors.
AID1327294	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as time spent in target quadrant at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 5 by Morris water maze tes	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1192739	Neuroprotective effect in Kunming mouse hippocampus assessed as reduction of scopolamine-induced vitality of AChE at 6 mg/kg by Ellman method	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
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).
AID395663	Cognitive enhancing effect against scopolamine-induced acquisition memory deficit in mouse assessed as escape latency at 2 mg/kg, intragastric gavage after 24 hrs by step-down passive avoidance test	2009	European journal of medicinal chemistry, Jan, Volume: 44, Issue:1	Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
AID540209	Volume of distribution at steady state 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.
AID1704775	Cognitive enhancement effect in Sprague-Dawley rat assessed as increase in time spent in exploring novel object at 0.2 mg/kg, po administered 1 hr prior to acquisition trial and measured after 24 hrs by novel object recognition test
AID1889346	Reversible inhibition of human AChE assessed as enzyme recovery activity at 0.1 times of IC50 concentration by dilution method relative to control	2022	Bioorganic & medicinal chemistry letters, 03-15, Volume: 60	Development of naringenin-O-carbamate derivatives as multi-target-directed liagnds for the treatment of 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.
AID625547	Inhibition of human serum recombinant BChE after 20 mins using butyrylthiocholine iodide as a substrate by Ellman's assay	2011	European journal of medicinal chemistry, Nov, Volume: 46, Issue:11	Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
AID396862	Inhibition of AChE in Wistar rat brain homogenates at 1 uM by Ellman's method	2009	Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14	Site-activated multifunctional chelator with acetylcholinesterase and neuroprotective-neurorestorative moieties for Alzheimer's therapy.
AID1272948	Inhibition of equine serum BChE using acetylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by Ellman's method	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's.
AID1691674	Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
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.
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.
AID1192736	Cognitive enhancing effect in Kunming mouse assessed as inhibition of scopolamine-induced decreased spontaneous alternation behavior at 6 mg/kg after 30 mins by T-maze test	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1517872	Antioxidant activity in mouse BV2 cells assessed as effect on LPS-induced ROS release at 1 uM preincubated with compound for 1 hr followed by LPS addition and measured after 24 hrs by cell analyser based assay (Rvb = 154 +/- 3.8%)	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Design and synthesis of H
AID407783	Reactivation 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.
AID26926	Pseudo-first order rate constant for carbamoylation of ACHE at 2.5(uM) concentration	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1691666	Inhibition of human serum BuChE assessed as residual activity at 0.1 times IC50 using acetylcholine iodide as substrate measured after dilution by Ellman's method relative to control	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1702420	Inhibition of human serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1339190	Inhibition of horse serum BuChE using butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	2017	Bioorganic & medicinal chemistry, 02-15, Volume: 25, Issue:4	Synthesis, anticholinesterase activity and molecular modeling study of novel carbamate-substituted thymol/carvacrol derivatives.
AID1702417	Inhibition of rat serum BChE using acetylthiocholine iodide as substrate measured after 15 mins by Ellman's method	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1736968	Inhibition of human AChE assessed as residual activity at IC50 concentration relative to control	2020	European journal of medicinal chemistry, Apr-15, Volume: 192	The development of advanced structural framework as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1076765	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 10 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay rela	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
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.
AID1166455	Inhibition of BuChE (unknown origin) using butyrylthiocholine iodide as substrate incubated for 25 mins by Ellman's method	2014	Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21	Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
AID730447	Inhibition of equine BChE using after 10 mins by Ellman's method	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
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.
AID407785	Reactivation of human 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.
AID1057265	Selectivity index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE	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.
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).
AID1330299	Inhibition of human serum BChE using S-Butyrylthiocholine iodide as substrate preincubated for 15 mins followed by substrate addition by Ellman's method	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1597571	Cognition enhancement in aluminium chloride-induced Alzheimer's disease zebra fish model assessed as Dyskinesia recovery rate at 10 uM treated from 3 dpf to 5 dpf relative to control	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1709255	Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2021	Bioorganic & medicinal chemistry, 04-01, Volume: 35	Novel 3-benzylidene/benzylphthalide Mannich base derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1886770	Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in latency at 1 mg/kg, icv measured on day 14 by Morris Water maze method
AID1272535	Inhibition of equine serum BChE using BTC as substrate preincubated for 15 mins followed by substrate addition measured at 1 min intervals by Ellman method	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.
AID1597592	Cognition enhancement in aluminium trichloride-induced amnesia mouse model assessed as error times at 2 mg/kg administered via gastric gavage for 30 days by SMG-2 programmable water maze test	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1409478	Cognitive enhancing effect in Sprague-Dawley rat assessed as effect on total exploration time for familiar objects in acquisition trial at 0.3 mg/kg, po administered 1 hr measured for 3 mins by novel object recognition test	2018	Journal of medicinal chemistry, 11-21, Volume: 61, Issue:22	Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
AID1673635	Inhibition of human serum BChE using butyrylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.
AID27158	Bimolecular rate constant for carbamoylation of ACHE	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1702418	Selectivity index, ratio of IC50 for rat serum butyrylcholinesterase to IC50 for rat cortex acetylcholinesterase	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1330305	Cytotoxicity against human SH-SY5Y cells assessed as cell viability at 50 uM after 48 hrs by MTT assay relative to control	2017	Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1	Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
AID1702429	Pseudo-irreversible inhibition of human erythrocytes AChE assessed as enzyme recovery activity at 0.1 times IC50 measured at 120 mins using diluted compound relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID241408	Inhibitory concentration against human serum acetylcholinesterase activity	2004	Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24	Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
AID1703002	Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by addition of substrate and measured after 20 mins by DTNB reagent based Ellman's method	2020	European journal of medicinal chemistry, Sep-01, Volume: 201	The structure-based optimization of δ-sultone-fused pyrazoles as selective BuChE inhibitors.
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
AID241439	Inhibitory concentration against human serum butyrylcholinesterase activity	2004	Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24	Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
AID1596337	Inhibition of electric eel AChE at 50 nM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured for 5 mins by Ellman's method	2019	European journal of medicinal chemistry, Jul-15, Volume: 174	Multi-targeted ChEI-copper chelating molecules as neuroprotective agents.
AID1656473	In-vivo inhibition of BuChE in human brain at 0.6 mg/kg, ip relative to control	2020	Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3	Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
AID241886	In vitro inhibitory concentration against butyrylcholinesterase was determined using rat serum homogenate	2005	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 15, Issue:17	Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
AID1856400	Pseudo-irreversible inhibition of human BChE using butyrylthiocholineiodide as substrate preincubated for 20 to 60 mins followed by substrate addition and measured for 5 mins by DTNB reagent based Ellman's 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.
AID314091	Inhibition of human AchE	2008	Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3	Multi-target-directed ligands to combat neurodegenerative diseases.
AID1568792	Reversible inhibition of equine serum BuChE assessed as enzyme activity at 0.1 times IC50 using butyrylthiocholine iodide as substrate measured at 120 mins by Ellman's method relative to control	2019	European journal of medicinal chemistry, Sep-15, Volume: 178	Design, synthesis, in-silico and biological evaluation of novel chalcone-O-carbamate derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID1525514	Inhibition of mouse brain AChE	2019	Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20	Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.
AID1698411	Inhibition of human AChE by Ellman's method	2020	Bioorganic & medicinal chemistry, 11-15, Volume: 28, Issue:22	Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.
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).
AID1656472	In-vivo inhibition of AChE in human brain at 0.6 mg/kg, ip relative to control	2020	Bioorganic & medicinal chemistry letters, 02-01, Volume: 30, Issue:3	Propargylamine-derived multi-target directed ligands for Alzheimer's disease therapy.
AID1327293	Inhibition of scopolamine-induced increase in AchE level in albino mouse assessed as AChE level in brain at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge using acetlythiocholine iodidie as substrate by Ellman's method (Rvb = 0.011 +/- 0.002	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1517870	Cytoprotection against LPS-induced cell damage in mouse BV2 cells assessed as cell viability at 1 uM preincubated with compound for 1 hr followed by LPS addition and measured after 24 hrs by cell analyser based assay (Rvb = 80.6 +/- 1.2%)	2019	European journal of medicinal chemistry, Dec-15, Volume: 184	Design and synthesis of H
AID7783	Unbound fraction (plasma)	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.
AID436572	Inhibition of AChE in bovine erythrocytes assessed as hydrolysis of acetylthiocholine by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
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.
AID1076766	Neuroprotective activity in Sprague-Dawley rat primary cortical neurons assessed as inhibition of glutamate-induced toxicity by measuring cell viability at 1 uM pretreated for 24 hrs followed by glutamate challenge measured after 24 hrs by MTT assay relat	2014	Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6	Evaluation of nicotine and cotinine analogs as potential neuroprotective agents for Alzheimer's disease.
AID1192728	Antioxidant activity assessed as trolox equivalent of APPH-induced radical scavenging activity by ORAC-FL method	2015	Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4	Multifunctional scutellarin-rivastigmine hybrids with cholinergic, antioxidant, biometal chelating and neuroprotective properties for the treatment of Alzheimer's disease.
AID1327301	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as latency to reach shock free zone at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training by passive avoidance test (Rvb = 53.25	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID599257	Inhibition of total brain cholinesterase activity in rat at 5 mg/kg, po measured 30 to 180 mins post dose	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1773278	Pseudo-irreversible inhibition of equine serum BuChE assessed as carbamolyation-rate using butyrylthiocholine iodide as substrate preincubated with enzyme for 60 mins prior to substrate addition	2021	European journal of medicinal chemistry, Nov-05, Volume: 223	Novel cannabidiol-carbamate hybrids as selective BuChE inhibitors: Docking-based fragment reassembly for the development of potential therapeutic agents against Alzheimer's disease.
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.
AID1739255	Selectivity index, ratio of IC50 for BuChE (unknown origin) to IC50 for AChE (unknown origin)	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.
AID1723544	Inhibition of human blood BChE at 1 to 25 uM using butyrylthiocholine iodide as substrate measured after 20 mins by fluorescence assay	2020	Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17	MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis.
AID1166456	Selectivity ratio of IC50 for BChE (unknown origin) to IC50 for AChE (unknown origin)	2014	Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21	Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
AID1631822	Inhibition of human AChE using ACTI as substrate incubated for 40 mins 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.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	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).
AID1220555	Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID671038	Selectivity ratio of Torpedo californica AChE to human AChE	2012	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14	Re-engineering aryl methylcarbamates to confer high selectivity for inhibition of Anopheles gambiae versus human acetylcholinesterase.
AID1633204	Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells at 10 uM incubated for 30 mins by beta-lactamase complementation technology relative to control	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID1327295	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as escape latency time at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 5 by Morris water maze test (Rvb = 8	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
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.
AID31163	Ex vivo inhibition of human erythrocyte Acetylcholinesterase.	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.
AID1220556	Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
AID540211	Fraction unbound 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.
AID1896376	Inhibition of equine serum BuChE 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.
AID1886771	Cognitive enhancing effect in amyloid beta (1 to 42)-induced ICR mouse model assessed as reduction in latency at 2.5 mg/kg, icv measured on day 14 by Morris Water maze method
AID436567	Inhibition of BChE in human serum assessed as hydrolysis of butyrylthiocholine at 100 ug/mL by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
AID1597593	Cognition enhancement in aluminium trichloride-induced amnesia mouse model assessed as total swimming time at 2 mg/kg administered via gastric gavage for 30 days by SMG-2 programmable water maze test	2019	European journal of medicinal chemistry, Sep-01, Volume: 177	Development of the "hidden" multifunctional agents for Alzheimer's disease.
AID1702517	Cognitive enhancing effect in scopolamine-induced Kunming mouse model of memory impairment assessed as effect on total arm entries at 6 mg/kg by Y-maze test	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
AID1609064	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method	2019	European journal of medicinal chemistry, Nov-01, Volume: 181	Discovery of δ-sultone-fused pyrazoles for treating Alzheimer's disease: Design, synthesis, biological evaluation and SAR studies.
AID436570	Inhibition of BChE in human serum assessed as hydrolysis of butyrylthiocholine at 0.1 ug/mL by Ellman's method	2009	Bioorganic & medicinal chemistry, Jul-15, Volume: 17, Issue:14	Synthesis of novel purine nucleosides towards a selective inhibition of human butyrylcholinesterase.
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.
AID1327307	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as number of mistakes at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training by passive avoidance test (Rvb = 12.25 +/- 0.47 No_un	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID730448	Inhibition of Electrophorus electricus AChE using acetylthiocholine as substrate after 10 mins by Ellman's method	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and in vitro evaluation of new derivatives of 2-substituted-6-fluorobenzo[d]thiazoles as cholinesterase inhibitors.
AID1197879	Inhibition of equine serum butylcholinesterase using acetylthiocholine iodide as substrate after 15 mins by Ellman's method	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Potent acetylcholinesterase inhibitors: design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives.
AID1336712	Inhibition of rat serum BuChE using butyrylthiocholine iodide as substrate incubated for 15 mins by Ellman's method	2017	Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3	Design, synthesis and biological evaluation of 4'-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of 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.
AID1691669	Selectivity index, ratio of IC50 for human erythrocytes Ache to IC50 for human serum BuChe	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1691802	Improvement in brain cholinergic activity in scopolamine-induced mouse model of amnesia assessed as change in ChAT vitality at 6 mg/kg (Rvb = 28.8 U/g)	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1653675	Selectivity index, ratio of IC50 for electric eel AChE to IC50 for equine serum BuChE	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.
AID1691665	Inhibition of human serum BuChE assessed as residual activity at IC50 using acetylcholine iodide as substrate measured by Ellman's method relative to control	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1317854	Selectivity ratio, ratio of IC50 for equine serum BuChE to electric eel AChE	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.
AID1601892	Inhibition of human erythrocyte AChE using acetylthiocholine as substrate by Ellman's assay	2019	European journal of medicinal chemistry, Mar-15, Volume: 166	Indazolylketones as new multitarget cannabinoid drugs.
AID1338168	Inhibition of BuChE (unknown origin) at 1 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease.
AID1428333	Selectivity index, ratio of IC50 for butyrylcholinesterase (unknown origin) to IC50 for acetylcholinesterase (unknown origin)
AID599265	Toxicity in rat assessed as induction of severe fasciculation, salivation and lacrimation incidence at 5 mg/kg, po	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
AID1633211	Selectivity index, ratio of CC50 for human SH-SY5Y cells IC50 for mouse plasma BuChE	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID1225693	Selectivity index, ratio of IC50 for rat serum BuChE to IC50 for rat cortex AChE	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
AID1327298	Antiamnesic activity against scopolamine-induced memory loss in albino mouse assessed as escape latency time at 0.5 mg/kg, ip administered 5 mins post scopolamine-challenge and 35 mins prior to training measured on day 2 by Morris water maze test (Rvb = 8	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Ameliorative effects of amide derivatives of 1,3,4-thiadiazoles on scopolamine induced cognitive dysfunction.
AID1406252	Inhibition of BChE (unknown origin)	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.
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).
AID135326	BBB penetration classification	2000	Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11	Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID1762070	Cognitive enhancement effect in rat assessed as increase in novelty discrimination index at 0.3 mg/kg, po administered 1 hr prior to acquisition trial by novel object recognition test	2021	Bioorganic & medicinal chemistry letters, 05-15, Volume: 40	Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
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.
AID710238	Inhibition of bovine AChE after 120 mins by Ellman's method	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Carbamate derivatives of indolines as cholinesterase inhibitors and antioxidants for the treatment of Alzheimer's disease.
AID1545334	Inhibition of equine serum BuChE preincubated for 15 mins followed by substrate addition and measured after 15 mins by Ellman's method	2019	Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6	Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1673636	Inhibition of human erythrocytes AChE using acetylthiocholine iodide as substrate preincubated for 10 mins followed by substrate addition by Ellman's method	2019	European journal of medicinal chemistry, Dec-01, Volume: 183	Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.
AID1338169	Inhibition of BuChE (unknown origin) at 5 uM using acetylthiocholine iodide as substrate preincubated for 60 mins followed by substrate addition measured after 5 mins by Ellman's method relative to control	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Discovery of novel rivastigmine-hydroxycinnamic acid hybrids as multi-targeted agents for Alzheimer's disease.
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.
AID454344	Selectivity ratio of IC50 for BChE in rat serum to IC50 for AChE in rat cortex	2009	Bioorganic & medicinal chemistry, Sep-15, Volume: 17, Issue:18	Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors.
AID1459902	Inhibition of electric eel AChE using acetylthiocholine 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.
AID1406251	Inhibition of AChE (unknown origin)	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.
AID1702432	Pseudo-irreversible inhibition of human serum BChE assessed as enzyme recovery activity at 0.1 times IC50 measured at 240 mins using diluted compound relative to basal level	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease.
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.
AID1633207	Cytotoxicity in human SH-SY5Y cells assessed as reduction in cell viability after 72 hrs incubation by MTT assay	2019	European journal of medicinal chemistry, Apr-15, Volume: 168	Design, synthesis, and evaluation of isoflavone analogs as multifunctional agents for the treatment of Alzheimer's disease.
AID1691663	Pseudo-irreversible inhibition of human serum BuChE assessed as residual activity at 0.1 times IC50 using acetylcholine iodide as substrate measured 240 mins post dilution by Ellman's method relative to control	2020	European journal of medicinal chemistry, May-15, Volume: 194	Design, synthesis and biological evaluation of novel O-carbamoyl ferulamide derivatives as multi-target-directed ligands for the treatment of Alzheimer's disease.
AID1282037	Inhibition of electric eel AChE by spectrophotometric-based Ellman's method	2016	Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7	Synthesis, structural characterization, docking, lipophilicity and cytotoxicity of 1-[(1R)-1-(6-fluoro-1,3-benzothiazol-2-yl)ethyl]-3-alkyl carbamates, novel acetylcholinesterase and butyrylcholinesterase pseudo-irreversible inhibitors.
AID1767557	Inhibition of recombinant human BuChe using S-butyrylthiocholine iodide as substrate measured after 7 mins by Ellman's method	2021	European journal of medicinal chemistry, Oct-15, Volume: 222	Synthesis, biological evaluation and molecular modeling of benzofuran piperidine derivatives as Aβ antiaggregant.
AID1668222	Inhibition of Electrophorus electricus AChE at 100 uM using acetylthiocholine iodide as substrate preincubated for 30 mins followed by substrate addition and measured after 10 mins by Ellman's method (Rvb = 7 +/- 7.1%)	2020	Bioorganic & medicinal chemistry, 05-15, Volume: 28, Issue:10	Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation.
AID1272536	Selectivtiy index, ratio of IC50 for equine serum BChE to IC50 for electric eel AChE	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.
AID1220560	Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method	2011	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7	Species independence in brain tissue binding using brain homogenates.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1796571	Enzyme Inhibition Assay from Article 10.1021/jm049782n: \\Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.\\	2004	Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24	Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
AID1802572	AChE and BChE Inhibition Assay from Article 10.1016/j.bioorg.2016.11.011: \\Synthesis of novel chromenones linked to 1,2,3-triazole ring system: Investigation of biological activities against Alzheimer's disease.\\	2017	Bioorganic chemistry, 02, Volume: 70	Synthesis of novel chromenones linked to 1,2,3-triazole ring system: Investigation of biological activities against Alzheimer's disease.
AID1802597	Cholinesterase Inhibition Assay from Article 10.1016/j.bioorg.2017.02.010: \\Synthesis of readily available fluorophenylalanine derivatives and investigation of their biological activity.\\	2017	Bioorganic chemistry, 04, Volume: 71	Synthesis of readily available fluorophenylalanine derivatives and investigation of their biological activity.
AID1803029	Enzyme Inhibition Assay from Article 10.3109/14756366.2010.548329: \\Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands.\\	2011	Journal of enzyme inhibition and medicinal chemistry, Oct, Volume: 26, Issue:5	Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands.
AID1801409	Modified Ellman Assay from Article 10.1111/cbdd.12580: \\Design, synthesis, and biological evaluation of scutellarein carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.\\	2015	Chemical biology & drug design, Nov, Volume: 86, Issue:5	Design, synthesis, and biological evaluation of scutellarein carbamate derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
AID1801428	AChE and BChE Inhibition Assay from Article 10.1111/cbdd.12609: \\Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.\\	2015	Chemical biology & drug design, Dec, Volume: 86, Issue:6	Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.
AID1796508	Cholinesterase Inhibition Assay from Article 10.1021/jm020120c: \\Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.\\	2002	Journal of medicinal chemistry, Nov-21, Volume: 45, Issue:24	Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
AID1796482	Cholinesterase Inhibition Assay from Article 10.1021/jm050578p: \\Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.\\	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.
AID1796572	Cholinesterase Inhibition Assay from Article 10.1021/jm010491d: \\Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.\\	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.
AID1801911	AChE and BChE Inhibition Assay from Article 10.1016/j.bioorg.2016.06.001: \\Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.\\	2016	Bioorganic chemistry, 08, Volume: 67	Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.
AID1801050	In Vitro AChE Inhibition Assay from Article 10.1016/j.bioorg.2015.04.004: \\Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.\\	2015	Bioorganic chemistry, Jun, Volume: 60	Design and synthesis of newer potential 4-(N-acetylamino)phenol derived piperazine derivatives as potential cognition enhancers.
AID1800998	Ellman's Method from Article 10.1016/j.bioorg.2014.11.005: \\Salicylanilide diethyl phosphates as cholinesterases inhibitors.\\	2015	Bioorganic chemistry, Feb, Volume: 58	Salicylanilide diethyl phosphates as cholinesterases inhibitors.
AID1345972	Human butyrylcholinesterase (Hydrolases)	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.
AID1345946	Human acetylcholinesterase (Cartwright blood group) (Hydrolases)	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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	45 (3.44)	18.2507
2000's	554 (42.35)	29.6817
2010's	531 (40.60)	24.3611
2020's	178 (13.61)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Trials	266 (19.04%)	5.53%
Reviews	0 (0.00%)	6.00%
Reviews	279 (19.97%)	6.00%
Case Studies	0 (0.00%)	4.05%
Case Studies	97 (6.94%)	4.05%
Observational	0 (0.00%)	0.25%
Observational	22 (1.57%)	0.25%
Other	9 (100.00%)	84.16%
Other	733 (52.47%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (84)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
Noradrenaline, Acetylcholine and Dynamic Learning in Healthy Humans [NCT03957174]		107 participants (Actual)	Interventional	2019-06-01	Completed
Exploratory Controlled Prospective Randomized Trial to Compare the Efficacy and Safety of Two Different Pharmacology Strategies on Neurocognitive Impairment in HIV Infection. The TRIANT-TE Study [NCT01348282]	Phase 4	33 participants (Actual)	Interventional	2011-05-31	Completed
Effects of Exercise and Rivastigmine on Quality of Life of Alzheimer's Disease Patients [NCT01183806]	Phase 3	40 participants (Actual)	Interventional	2010-07-31	Completed
Determination of Serum Rivastigmine Levels After Using Rivastigmine Transdermal Delivery Systems With and Without Standardized Heat Application in Healthy Human Volunteers [NCT03915626]	Early Phase 1	7 participants (Actual)	Interventional	2019-10-04	Completed
A Six-month, Open Labeled, Multi-centered, Observational Study for the Tolerability of Exelon Patch (Rivastigmine) for Patients With Alzheimer's Disease [NCT01312363]		300 participants (Actual)	Observational	2009-06-30	Completed
Changes of Cognitive Function in Patients With Mild to Moderate Alzheimer's Disease Associated With or Without White Matter Changes After Rivastigmine Patch Therapy - Multi-center, Prospective, Open-label Clinical Trial [NCT01380288]		300 participants (Actual)	Interventional	2011-06-30	Completed
Multiple Dose Crossover Comparative Bioavailability Study of a Transdermal Patch Formulation of Rivastigmine Compared With Exelon® Transdermal Patch With a Release Rate of 13.3 mg/24 Hours in Healthy Male Subjects With Preceding Adaptation Phase and Post- [NCT03573050]	Phase 1	36 participants (Actual)	Interventional	2018-05-16	Completed
A Discontinuation of Cholinesterase Inhibitors for the Treatment of Severe Alzheimer's Disease in Long Term Care Setting [NCT02035982]	Phase 3	40 participants (Actual)	Interventional	2010-07-31	Completed
A Multi-center, Randomised, Open-label Study to Evaluate Convenience and Safety of Change in the Mode of Administration of Rivastigmine (From Capsules to a Transdermal Patch) in Patients With Alzheimer's Disease [NCT00549601]	Phase 4	142 participants (Actual)	Interventional	2007-09-30	Completed
Open, Randomized, 2-period, 2-sequence, Cross-over Relative Bioavailability Study to Investigate the Pharmacokinetics and to Assess the Bioequivalence of a Rivastigmine Test Patch Formulation 9.5 mg/24 h (Twice Weekly Patch) Compared to the Reference Exel [NCT03659435]	Phase 1	58 participants (Actual)	Interventional	2018-08-22	Completed
A 76-week Prospective, Open-label, Multicenter Study to Evaluate the Long-term Effect of Rivastigmine Capsule and Transdermal Patch on Worsening of the Underlying Motor Symptoms of PD in Patients With Mild to Moderately Severe Dementia Associated With Par [NCT00623103]	Phase 3	583 participants (Actual)	Interventional	2008-01-31	Completed
Open, Randomized, 2-period, 2-sequence, Cross-over Relative Bioavailability Study to Investigate the Pharmacokinetics and to Assess the Bioequivalence of a Rivastigmine Test Patch Formulation 13.3 mg/24 h (Twice-weekly Patch) Compared to the Reference Exe [NCT05853341]	Phase 1	48 participants (Actual)	Interventional	2023-05-02	Completed
Bioequivalence Study of Rivastigmine 1.5 mg Capsules (Test)of Dr.Reddy's Laboratories Limited Versus Exelon (Reference),Administered as 1 x 1.5 mg Capsule Under Fasting Conditions [NCT01146067]	Phase 1	44 participants (Actual)	Interventional	2004-01-31	Completed
A Prospective, 16 Week, Phase IV Study to Evaluate Safety, Tolerability and Effectiveness in Patients With Severe Dementia of the Alzheimer's Type Exposed to Rivastigmine (Exelon)15cm2 Transdermal Patch [NCT02989402]	Phase 4	102 participants (Actual)	Interventional	2018-12-31	Completed
Randomized, 2-Way Crossover, Bioequivalence Study of Rivastigmine 1.5 mg Capsules and Exelon Administered as 1 x 1.5 mg Capsule in Healthy Subjects Under Fed Conditions [NCT01146041]	Phase 1	44 participants (Actual)	Interventional	2004-02-29	Completed
A Double-Blind, Placebo-controlled Crossover Study to Assess the Pharmacokinetic Profile and the Physiological and Behavioral Effects of Repeat Rivastigmine (Exelon®) Administration in Young Healthy Male Volunteers [NCT00624663]		15 participants (Actual)	Interventional	2009-01-31	Completed
A 16-week, Multicenter, Double-blind, Randomized, Placebo-controlled, Parallel Group Study to Evaluate the Efficacy of Rivastigmine Patch (10 cm²) on Cognitive Deficits in Patients With Multiple Sclerosis, Followed by a 1-year Open-label Treatment Phase [NCT00881205]	Phase 4	86 participants (Actual)	Interventional	2009-04-30	Terminated(stopped due to Termination of study due to low enrollment)
Rivastigmine for Delirium in Intensive Care Patients, a Double-blind, Randomized Placebo-controlled add-on Trial [NCT00704301]	Phase 4	104 participants (Actual)	Interventional	2008-11-30	Terminated(stopped due to The study is prematurely terminated due to a safety issue)
Differences of Functional Changes in Brain by Rivastigmine According to Butyrylcholinesterase Alleles in Alzheimer's Disease Patients(Rivastigmine, Imaging, and BuChE in AD: RIBA) [NCT02063269]		70 participants (Anticipated)	Interventional	2014-02-28	Active, not recruiting
CHolinesterase Inhibitor to prEvent Falls in Parkinson's Disease: A Phase 3 Randomised, Double-blind Placebo-controlled Trial of Rivastigmine to Prevent Falls in Parkinson's Disease. [NCT04226248]	Phase 3	600 participants (Anticipated)	Interventional	2020-01-02	Active, not recruiting
Open Label Trial of Rivastigmine Patch in Subjects With Mild to Moderate Stage Alzheimer's Disease Having Coexisting Small Vessel Cerebrovascular Disease [NCT02444637]	Phase 4	100 participants (Actual)	Interventional	2015-04-30	Completed
A 48-Week, Multicenter, Randomized, Double-Blind, Parallel-Group Evaluation of the Comparative Efficacy, Safety, and Tolerability of Exelon® 10 and 15 cm^2 Patch in Patients With Mild to Moderate Alzheimer's Disease (AD) Showing Functional and Cognitive D [NCT00506415]	Phase 3	1,584 participants (Actual)	Interventional	2007-06-30	Completed
A 24-week, Multi-center, Open, Evaluation of the Clinical Effectiveness of the Once-daily 10 cm^2 Rivastigmine Patch Formulation in Patients With Probable Alzheimer's Disease (MMSE10-26) [NCT00561392]	Phase 4	208 participants (Actual)	Interventional	2007-11-30	Completed
Efficacy of Rivastigmine in Patients With Down Syndrome [NCT00748007]		14 participants (Actual)	Interventional	2008-01-31	Completed
Open, Randomized, 2-period, 2-sequence, Cross-over Relative Bioavailability Study to Investigate the Pharmacokinetics and to Assess the Bioequivalence of a Rivastigmine Test Patch Formulation 9.5 mg/24 h (Twice-weekly Patch) (Luye Pharma AG, Germany) Comp [NCT05883124]	Phase 1	38 participants (Anticipated)	Interventional	2023-04-17	Active, not recruiting
A Multicenter, Randomized, Open-label Study to Compare the Tolerability Between Rivastigmine Patch Monotherapy and Combination Therapy With Memantine in Patients With Alzheimer's Disease [NCT01025466]	Phase 4	206 participants (Actual)	Interventional	2008-12-31	Completed
A 12 Week, Multicenter, Open Label Evaluation of Caregiver Preference, Safety and Tolerability of Exelon® Patch (Rivastigmine Transdermal) in Patients With Alzheimer's Disease [NCT01047579]	Phase 4	51 participants (Actual)	Interventional	2010-04-30	Completed
Rivastigmine and Huperzine A as Treatments for Cocaine Dependence [NCT01030692]	Phase 1	72 participants (Actual)	Interventional	2009-01-31	Completed
Toward a Computationally-Informed, Personalized Treatment for Hallucinations [NCT04366518]	Early Phase 1	35 participants (Anticipated)	Interventional	2021-07-15	Recruiting
A Randomized, Double-blind, Placebo-controlled, Parallel-group, Multicentric Trial [NCT00767091]	Phase 3	40 participants (Actual)	Interventional	2009-03-31	Completed
A 24-week, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group, Dose-finding Evaluation of the Efficacy, Safety, and Tolerability of the Once-daily Rivastigmine Transdermal Patch in Patients With Probable Alzheimer's Disease (MMSE 10 [NCT00423085]	Phase 3	859 participants (Actual)	Interventional	2007-01-31	Completed
A 24 Week, Multicenter, Open, Evaluation of the Clinical Effectiveness of the Once-daily 10 cm2 Rivastigmine Patch Formulation in Patients With Probable Alzheimer's Disease (MMSE 10-26) [NCT00622713]	Phase 4	228 participants (Actual)	Interventional	2008-01-31	Completed
RIVA-PSP: Efficacy of Rivastigmine on Motor, Cognitive and Behavioural Impairment in Progressive Supranuclear Palsy: A Randomised Double Blind Placebo-controlled Clinical Trial [NCT02839642]	Phase 3	106 participants (Actual)	Interventional	2016-07-26	Completed
A Randomized, Double-Blind, Placebo-Controlled, Ascending-Dose Phase 1b Safety Study of Three Different Doses of an Alpha-7 Nicotinic Acetylcholine Receptor Agonist (EVP-6124) or Placebo in Patients With Mild to Moderate Probable Alzheimer's Disease [NCT00766363]	Phase 1	49 participants (Actual)	Interventional	2008-10-31	Completed
Effect of Rivastigmine on FMRI in Mild Alzheimer's Disease [NCT00627848]		20 participants (Actual)	Interventional	2007-03-31	Completed
Efficacy and Safety of Rivastigmine in Patients With Traumatic Brain Injury and Cognitive Impairment [NCT00171795]	Phase 3	67 participants (Actual)	Interventional	2002-11-30	Completed
Double-Blind Randomized Placebo Controlled Trial of Rivastigmine (Excelon) as a Potential Medication for Methamphetamine Abuse [NCT00158210]	Phase 1	18 participants (Actual)	Interventional	2006-05-31	Completed
Rivastigmine as a Treatment for Methamphetamine Dependence [NCT01073319]	Phase 1	17 participants (Actual)	Interventional	2009-07-31	Completed
Study of the Effects of Current Drug Treatments on Levels of Certain Brain Chemicals in Alzheimer's Disease [NCT00104442]	Phase 4	80 participants	Interventional	2003-10-31	Completed
Comparison of Therapeutic Strategies With Cholinesterase Inhibitors: Stop or Still (SOS) Trial [NCT03454646]	Phase 4	1,205 participants (Anticipated)	Interventional	2024-06-01	Not yet recruiting
A 20-Week Double-Blind Placebo Controlled Clinical Trial to Evaluate the Safety and Efficacy of Rivastigmine in Children (Ages 10-18) With Down Syndrome [NCT01084135]	Phase 1/Phase 2	42 participants (Actual)	Interventional	2009-11-30	Completed
Lewy Body Spectrum Disorders: Investigating Neuropsychiatric Benefit and Adverse Effects in Response to Cholinesterase Inhibitors Using Genetics and Brain SPECT [NCT01944436]		57 participants (Actual)	Observational	2006-09-30	Completed
A 26-Week Open-Label Extension to Protocol No. CENA713BUS11: A 12-Week, Prospective, Double-blind, Placebo-controlled, Multi-center Study Evaluating the Efficacy and Safety of Rivastigmine 3 to 6 mg/Day in Patients With Traumatic Brain Injury (TBI) With P [NCT00219245]	Phase 4	157 participants (Actual)	Interventional	2002-11-30	Completed
Cholinergic Neurotransmission - A Common Underlying Mechanism of Cognitive and Gait Impairment in Parkinson Disease [NCT03840837]	Phase 4	31 participants (Actual)	Interventional	2019-05-02	Completed
Evaluation and Treatment of Autonomic Failure. [NCT00223691]	Phase 1	389 participants (Actual)	Interventional	2002-03-31	Completed
A Prospective, 5-Week, Open-Label, Randomized, Multi-Center, Parallel-Group Study With a 20-Week, Open-Label Extension Evaluating the Tolerability and Safety of Switching From Donepezil to an Initial Dose of 5 cm2 Rivastigmine Patch Formulation in Patient [NCT00428389]	Phase 3	262 participants (Actual)	Interventional	2007-01-31	Completed
A 24-week, Multi-center, Open-label Evaluation of Compliance and Tolerability of the Once-daily 10 cm² Rivastigmine Patch Formulation in Patients With Probable Alzheimer's Disease. [NCT00731224]	Phase 4	380 participants (Actual)	Interventional	2008-07-31	Completed
A 24-week Prospective, Double Blind, Randomized, Placebo-controlled Pilot Study of 9 mg/Day Rivastigmine in Patients With Vascular Cognitive Impairment Not Dementia to Evaluate Efficacy, Safety and Tolerability in Asian Patients [NCT00669344]	Phase 4	50 participants (Actual)	Interventional	2006-02-28	Completed
Rivastigmine Patch (Exelon Patch) Compared to Melatonin Patch in Prevention of Postoperative Delirium in Elderly [NCT04189666]	Phase 1/Phase 2	180 participants (Actual)	Interventional	2019-11-18	Completed
A 24 Week, Prospective, Randomized, Parallel-group, Double-blind, Multi-center Study (ENA713DUS44) Comparing the Effects of Rivastigmine Patch 15 cm^2 vs. Rivastigmine Patch 5 cm^2 on ACTivities of Daily Living and CognitION in Patients With Severe Dement [NCT00948766]	Phase 4	716 participants (Actual)	Interventional	2009-07-31	Completed
Cholinesterase Inhibitors to Slow Progression of Visual Hallucinations in Parkinson's Disease:a Multi-center Placebo-controlled Trial. [NCT01856738]	Phase 4	91 participants (Actual)	Interventional	2013-11-30	Terminated(stopped due to enrollment to slow, insufficient funds)
24-week, Randomized, Double-blind, Placebo-controlled, Parallel Group Study of the Exelon® [Rivastigmine] Transdermal Patch in 120 APOE e4 Positive Amnestic MCI Patients [NCT01602198]		1 participants (Actual)	Interventional	2011-06-30	Terminated(stopped due to Study revised to use a different study medication and patient population.)
[NCT00000174]	Phase 3	0 participants	Interventional		Completed
Methylphenidate, Rivastigmine or Haloperidol in Hypoactive Delirium in Intensive Care Patients: a Randomized, Mono-blind Pilot Trial [NCT00599287]	Phase 3	80 participants (Anticipated)	Interventional	2008-02-29	Terminated(stopped due to Inclusion rate too low due to a lack of eligible patients and difficulties obtaining informed consent.)
Rivastigmine (Exelon®) for Treatment of Dementia in Patient With Progressive Supranuclear Paresis Open Label Phase 2 Study [NCT00522015]	Phase 2	20 participants (Anticipated)	Interventional	2008-02-29	Recruiting
The Effects of the Rivastigmine Patch on Attention and Behavior in Parkinson's Disease With Dementia (PDD) [NCT00988117]	Phase 4	15 participants (Actual)	Interventional	2010-04-30	Completed
Rivastigmine Patch in Veterans With Cognitive Impairment Following TBI [NCT01670526]	Phase 3	94 participants (Actual)	Interventional	2012-12-31	Completed
Prediction of ECT Treatment Response and Reduction of Cognitive Side-effects Using EEG and Rivastigmine [NCT05768126]	Phase 4	100 participants (Anticipated)	Interventional	2021-09-29	Recruiting
An Open-label Study to Evaluate the Efficacy and Safety of add-on Memantine [5-10 mg b.i.d (10-20 mg/Day)] to Rivastigmine [1.5-6 mg b.i.d. (3-12 mg/Day)] Treatment in Patients With Alzheimer's Disease Who Continued With Rivastigmine Treatment After a Pre [NCT00234637]	Phase 4	204 participants (Actual)	Interventional	2003-11-30	Completed
Efficacy and Safety of Rivastigmine Capsules in Patients With Probable Vascular Dementia [NCT00099216]	Phase 3	708 participants (Actual)	Interventional	2001-08-31	Completed
Efficacy and Safety of the Rivastigmine Transdermal Patch in Patients With Probable Alzheimer's Disease [NCT00099242]	Phase 3	1,040 participants	Interventional	2003-11-30	Completed
Improved Language Acquisition Through Neuromodulation, Project Stage Ia [NCT00102284]	Phase 4	100 participants	Interventional	2004-03-31	Terminated
Cognitive and Physical Impairment in Frail Older Adults [NCT04962841]		485 participants (Anticipated)	Observational	2020-04-01	Recruiting
A Randomized, Double-blind, Placebo-controlled Study of an Acetylcholinesterase Inhibitor in the Management of Delirium in Hospitalized Patients Aged 75 Years and Over [NCT01487317]	Phase 3	23 participants (Actual)	Interventional	2011-06-30	Completed
A 24-week, Open-label, Multicenter Study to Evaluate the Efficacy, Safety and Tolerability of Rivastigmine Patch in Patients With Mild to Moderate Alzheimer's Disease (MMSE 10-23) Switched From Cholinesterase Inhibitors (Donepezil, Galantamine) [NCT01529619]	Phase 4	52 participants (Actual)	Interventional	2012-03-31	Completed
Neuromodulation and Language Acquisition (KS-Neuromod_01, Stage Ib) [NCT00102856]	Phase 4	60 participants	Interventional	2005-01-31	Suspended
The Effect of Deep Brain Stimulation on Memory Network and Neurological Function of Alzheimer's Disease [NCT03959124]		30 participants (Anticipated)	Interventional	2020-04-06	Recruiting
An Open-label Extension to Evaluate the Efficacy and Safety of Rivastigmine Capsules in Patients With Probable Vascular Dementia [NCT00130338]	Phase 3	521 participants (Actual)	Interventional	2002-02-28	Completed
An Open-label Extension to Evaluate the Efficacy and Safety of the Rivastigmine Transdermal Patch in Patients With Probable Alzheimer's Disease [NCT00219232]	Phase 3	868 participants (Actual)	Interventional	2003-02-28	Completed
Efficacy and Safety of Rivastigmine in Patients With Mild Cognitive Impairment [NCT00134953]	Phase 3	24 participants	Interventional	2003-01-31	Terminated(stopped due to The Principal Investigator left the clinic and there was no one who could take over this study.)
Rivastigmine in the Treatment of Postoperative Delirium: a Pilot Clinical Trial [NCT00835159]	Phase 4	30 participants (Actual)	Interventional	2008-12-31	Completed
Rivastigmine for the Prevention of Postoperative Delirium After Cardiac Surgery [NCT00257868]	Phase 3	120 participants (Actual)	Interventional	2006-01-31	Completed
A Prospective, 26-Week, Open-Label, Multi-Center, Single-Arm Pilot Study to Evaluate the Safety and Tolerability of Rivastigmine Capsule With Add on Memantine HCl in Patients With Probable Alzheimer's Disease (MMSE 10-20) [NCT00305903]	Phase 4	150 participants (Anticipated)	Interventional	2006-03-31	Completed
A 24-week, Multicenter, Parallel-group, Randomized,Double-blind Study to Evaluate the Tolerability, Safety and Efficacy of 2 Different Titration Methods of Rivastigmine Patch (ENA713D/ONO-2540) in Patients With Mild to Moderate Alzheimer's Disease (MMSE 1 [NCT01614886]	Phase 3	216 participants (Actual)	Interventional	2012-07-31	Completed
Comparative Effectiveness Research Trial of Alzheimer's Disease Drugs [NCT01362686]		200 participants (Actual)	Interventional	2011-04-30	Terminated(stopped due to Low study accrual caused the study to be ended early.)
A 24-Week, Randomized, Double-blind, Double-dummy, Parallel-group, Active-controlled Study to Assess the Efficacy, Safety, and Tolerability of the Once-daily Rivastigmine Patch Formulation in Patients With Probable Alzheimer's Disease (Mini-Mental State E [NCT01399125]	Phase 3	501 participants (Actual)	Interventional	2011-07-31	Completed
Rivastigmine Patch Effect on the Post-operative Delirium Limited to Femur Neck Fracture Operation in Patients at Risk of Dementia. [NCT02413554]	Phase 4	62 participants (Actual)	Interventional	2013-04-30	Completed
A 24-week, Open-label, Multicenter Study to Evaluate the Efficacy, Safety and Tolerability of Rivastigmine Patch With 1-step Titration in Patients With Mild to Moderate Alzheimer's Disease (MMSE 10 - 23) Switched Directly From Holinesterase Inhibitors (Do [NCT02703636]	Phase 4	118 participants (Actual)	Interventional	2016-05-09	Completed
A Phase IV Randomized, Double-Blind, Placebo-Controlled, Crossover Single Site Study Of Exelon® Patch (Rivastigmine Transdermal System) For Mild Cognitive Impairment In Parkinson's Disease [NCT01519271]	Phase 4	28 participants (Actual)	Interventional	2011-12-31	Completed
Cognitive Dysfunction in PD: Pathophysiology and Potential Treatments, a Pilot Study [NCT01340885]	Phase 4	9 participants (Actual)	Interventional	2011-01-31	Completed
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]	Phase 3	407 participants (Actual)	Interventional	2015-01-31	Terminated
A Phase II, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Study to Investigate the Efficacy and Safety of RO4602522 Added to Background Alzheimer's Disease Therapy in Patients With Moderate Severity Alzheimer's Disease [NCT01677754]	Phase 2	542 participants (Actual)	Interventional	2012-10-24	Completed
A 52-week, Prospective, Multi-center, Open-label Study to Assess the Tolerability of Rivastigmine Before and After Switching From Oral Formulation to Transdermal Patch in Patients With Alzheimer's Dementia in a Controlled Titration Schedule [NCT01585272]	Phase 4	121 participants (Actual)	Interventional	2012-08-31	Completed
16 Weeks Interventional Study on Titration and Dose/Efficacy Assessment of Exelon (Rivastigmine) in Chinese Alzheimer's Disease Patients (INSTINCT) [NCT01948791]	Phase 4	222 participants (Actual)	Interventional	2014-08-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00423085 (9) [back to overview]	Overall Clinical Rating of Change From Baseline to Week 24 Measured by the Clinician's Interview-Based Impression of Change Plus - Japan (CIBIC Plus-J)
NCT00423085 (9) [back to overview]	Extension Phase: Change From Extension Phase Baseline to End of Extension in Modified Crichton Scale
NCT00423085 (9) [back to overview]	Change From Baseline in CIBIC Plus-J Score Behavioral Pathology in Alzheimer's Disease Rating Scale (Behave-AD)
NCT00423085 (9) [back to overview]	Extension Phase: Change From Extension Phase Baseline to End of Extension in Mini-Mental State Examination (MMSE)
NCT00423085 (9) [back to overview]	Extension Phase: Change From Extension Phase Baseline to End of Extension in CIBIC Plus-J Score Disability Assessment for Dementia (DAD)
NCT00423085 (9) [back to overview]	Change From Baseline in the Alzheimer's Disease Assessment Scale - Japan Cognitive Subscale (ADAS-J Cog)
NCT00423085 (9) [back to overview]	Change From Baseline in CIBIC Plus-J Score Mental Function Impairment Scale (MENFIS)
NCT00423085 (9) [back to overview]	Change From Baseline in CIBIC Plus-J Score Disability Assessment for Dementia (DAD)
NCT00423085 (9) [back to overview]	Change From Baseline in Mini-Mental State Examination (MMSE)
NCT00428389 (7) [back to overview]	Mean Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living (ADCS-ADL) Total Score at Week 25 and at the End of Study
NCT00428389 (7) [back to overview]	Mean Change From Baseline in Neuropsychiatric Inventory - 10 Item (NPI-10) Score at Week 25 and at the End of Study.
NCT00428389 (7) [back to overview]	Mean Change From Baseline in Mini Mental State Exam (MMSE) Score at Week 25 and at the End of Study
NCT00428389 (7) [back to overview]	Number of Participants Who Discontinued From the Study Due to Any Reason During the Core Phase of the Study
NCT00428389 (7) [back to overview]	Number of Participants Who Discontinued From Study Due to Any Reason During Extension Phase
NCT00428389 (7) [back to overview]	Mean Change From Baseline in the Clinical Global Impression of Change (CGIC) Score at Week 5 and Week 25
NCT00428389 (7) [back to overview]	Number of Participants Who Discontinued From the Study Due to Any Adverse Event (AE) During the Combined Core and Extension Phases of the Study
NCT00506415 (7) [back to overview]	Change From Baseline in Alzheimer's Disease Assessment Scale-Cognitive (ADAS-Cog) Subscale at Week 48 of Double Blind Period
NCT00506415 (7) [back to overview]	Change in Alzheimer's Disease Cooperative Study-Instrumental Activities of Daily Living (ADCS-IADL) Subscale Score From Baseline to Week 48 of Double Blind Period
NCT00506415 (7) [back to overview]	Change in Attention and Executive Function as Assessed by the Trail Making Test (Part A) at Week 48 of the Double Blind Period
NCT00506415 (7) [back to overview]	Change in Attention and Executive Function as Assessed by the Trail Making Test (Part B) at Week 48 of Double Blind Period
NCT00506415 (7) [back to overview]	Number of Patients With Adverse Events, Serious Adverse Events and Discontinuations Due to Adverse Events
NCT00506415 (7) [back to overview]	Change From Baseline in Neuropsychiatric Inventory (NPI)-10 Score at Week 48 of Double Blind Period
NCT00506415 (7) [back to overview]	Time to Functional Decline as Measured by Alzheimer's Disease Cooperative Study-Instrumental Activities of Daily Living (ADCS-IADL) Subscale During the Double Blind Period
NCT00549601 (6) [back to overview]	Overall Patient Satisfaction With Treatment
NCT00549601 (6) [back to overview]	Change in the Total Mini-Mental State Examination (MMSE) Score From Baseline to Month 1 and Month 3
NCT00549601 (6) [back to overview]	Percentage of Patients With at Least 1 AE of Any Kind Recorded During the Period of the Study.
NCT00549601 (6) [back to overview]	Percentage of Patients With an AE Involving the Skin (Local Tolerance) Recorded Over the Course of the Study Period (Patch Groups Only)
NCT00549601 (6) [back to overview]	Percentage of Patients Who Had a Gastrointestinal Adverse Event (AE) at Any Time During the Study
NCT00549601 (6) [back to overview]	Overall Caregiver Satisfaction With Treatment
NCT00561392 (9) [back to overview]	Mean Change From Baseline in the Mini-Mental State Examination (MMSE) Score at Week 24
NCT00561392 (9) [back to overview]	Mean Change From Baseline in the Alzheimer's Disease Cooperative Study- Clinical Global Impression of Change (ADCS-CGIC) at Week 24 Assessed by the Caregiver
NCT00561392 (9) [back to overview]	Change From Baseline in the Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change (ADCS-CGIC) at Week 24 Assessed by the Physician
NCT00561392 (9) [back to overview]	Mean Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living (ADCS-ADL) Score at Week 24
NCT00561392 (9) [back to overview]	Percentage of Participants Treated by Rivastigmine 10 cm^2 Patch for at Least 8 Weeks Who Completed the Study
NCT00561392 (9) [back to overview]	Percentage of Participants Treated by Rivastigmine 10 cm^2 Patch for at Least 8 Weeks Regardless Whether They Completed the Study
NCT00561392 (9) [back to overview]	Mean Change From Baseline in the Trail-making Test Part A Score at Week 24
NCT00561392 (9) [back to overview]	Mean Change From Baseline in the Mini-Zarit Inventory Score of Caregiver Burden at Week 24
NCT00561392 (9) [back to overview]	Percentage of Participants Who Were Compliant to the 10 cm^2 Patch
NCT00622713 (5) [back to overview]	Clinical Global Impression of Change (CGI-C) by Physician
NCT00622713 (5) [back to overview]	Mean Change From Baseline to Week 24 in the 4-item Instrumental Activities of Daily Living (4-IADL) Score
NCT00622713 (5) [back to overview]	Mean Change From Baseline to Week 24 in the Mini-Mental State Examination (MMSE) Score
NCT00622713 (5) [back to overview]	Mean Change From Baseline to Week 24 in the Mini-Zarit Inventory Score
NCT00622713 (5) [back to overview]	Percentage of Patients Who Achieved and Maintained the Maximum Dose of 10 cm^2 Rivastigmine Patch for at Least 8 Weeks During 24 Weeks Study
NCT00623103 (8) [back to overview]	Change in Unified Parkinson Disease Rating Scale (UPDRS) Part III Motor Examination Scores at Weeks 8, 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline
NCT00623103 (8) [back to overview]	Percentage of Participants With Adverse Events (AEs) Due, or Potentially Due, to Worsening of Parkinson Disease (PD) Motor Symptoms (Tremor, Muscle Rigidity, Bradykinesia, Fall)
NCT00623103 (8) [back to overview]	Percentage of Participants With Study Drug Discontinuations Due to Predefined AEs That Are Due, or Potentially Due, to Worsening of PD Motor Symptoms (Tremor, Muscle Rigidity, Bradykinesia, Fall)
NCT00623103 (8) [back to overview]	UPDRS Part V Stage (Modified Hoehn and Yahr Staging)at Baseline, Week 8,16,24,52 and 76 (or Early Discontinuation)
NCT00623103 (8) [back to overview]	Change in Alzheimer's Disease Cooperative Study-Activities Of Daily Living (ADCS-ADL) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline
NCT00623103 (8) [back to overview]	Change in Mattis Dementia Rating Scale (Mattis DRS-2) Scores at Weeks 16, 24, 52 and 76 Compared to Baseline
NCT00623103 (8) [back to overview]	Change in Neuropsychiatric Inventory-10 (NPI-10) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline
NCT00623103 (8) [back to overview]	Change in Ten Point Clock Test (TPCT) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline
NCT00766363 (10) [back to overview]	Rivastigmine PK Data Following the First Dose of EVP-6124 - Area Under the Curve (AUC[0-24 h])
NCT00766363 (10) [back to overview]	Rivastigmine PK Data Following the First Dose of EVP-6124 - Maximum Concentration (Cmax)
NCT00766363 (10) [back to overview]	Rivastigmine PK Data Following the First Dose of EVP-6124 - Time to Maximum Concentration (Tmax)
NCT00766363 (10) [back to overview]	Safety and Tolerability of Multiple Doses of EVP-6124 or Placebo in Subjects With Alzheimer's Disease
NCT00766363 (10) [back to overview]	Donepezil PK Data Following the First Dose of EVP-6124 - Area Under the Curve (AUC[0-24 h])
NCT00766363 (10) [back to overview]	Donepezil PK Data Following the First Dose of EVP-6124 - Maximum Concentration (Cmax)
NCT00766363 (10) [back to overview]	Donepezil PK Data Following the First Dose of EVP-6124 - Time to Maximum Concentration (Tmax)
NCT00766363 (10) [back to overview]	EVP-6124 PK Data Following the First Dose of EVP-6124 - Area Under the Curve (AUC[0-24 h])
NCT00766363 (10) [back to overview]	EVP-6124 PK Data Following the First Dose of EVP-6124 - Maximum Concentration (Cmax)
NCT00766363 (10) [back to overview]	EVP-6124 PK Data Following the First Dose of EVP-6124 - Time to Maximum Concentration (Tmax)
NCT00835159 (1) [back to overview]	Incidence of POD
NCT00948766 (7) [back to overview]	Core Study: Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living-Severe Impairment Version (ADCS-ADL-SIV) Score at Week 24
NCT00948766 (7) [back to overview]	Core Study: Change From Baseline in the Neuropsychiatric Inventory (NPI-12) Score at Week 24
NCT00948766 (7) [back to overview]	Core Study: Change From Baseline in the Severity Impairment Battery (SIB) Score at Week 24
NCT00948766 (7) [back to overview]	Extension Study: Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living-Severe Impairment Version (ADCS-ADL-SIV) Score at Week 24
NCT00948766 (7) [back to overview]	Extension Study: Change From Baseline in the Severity Impairment Battery (SIB) Score at Week 24
NCT00948766 (7) [back to overview]	Core Study: Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change (ADCS-CGIC) Score at Week 24
NCT00948766 (7) [back to overview]	Extension Study: Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change (ADCS-CGIC) Score at Week 24
NCT00988117 (3) [back to overview]	Pre-post Change in Continuous Performance Test of Attention (Median Reaction Time)
NCT00988117 (3) [back to overview]	Pre-post Change in Montreal Cognitive Assessment
NCT00988117 (3) [back to overview]	Resting State Functional Activity Change From Baseline to 12 Weeks
NCT01084135 (2) [back to overview]	Behavior Rating Inventory of Executive Function-Preschool (BRIEF-P)
NCT01084135 (2) [back to overview]	Vineland Adaptive Behavior Scales, Second Edition (Survey Interview Form)
NCT01362686 (3) [back to overview]	Discontinuation Rates
NCT01362686 (3) [back to overview]	Healthy Aging Brain Care (HABC)-Monitor
NCT01362686 (3) [back to overview]	Neuropsychiatric Inventory (NPI)
NCT01399125 (5) [back to overview]	Change From Baseline in Global Functioning, Assessed by the Alzheimer's Disease Assessment Scale Clinical Impression of Change (ADCS-CGIC)
NCT01399125 (5) [back to overview]	Change From Baseline in Alzheimer's Disease Cooperative Study - Activities of Daily Living (ADCS-ADL) Total Score
NCT01399125 (5) [back to overview]	Change From Baseline in Mini-Mental State Examination (MMSE) Total Score
NCT01399125 (5) [back to overview]	Change From Baseline on Cognition, Assessed by the Alzheimer's Disease Assessment Scale-Cognitive (ADAS-Cog)
NCT01399125 (5) [back to overview]	Change From Baseline in Neuropsychiatric Inventory (NPI) Total Score
NCT01519271 (2) [back to overview]	Montreal Cognitive Assessment (MoCA)
NCT01519271 (2) [back to overview]	Alzheimer's Disease Cooperative Study- Clinical Global Impression Change (ADCS-CGIC)
NCT01585272 (5) [back to overview]	Number of Patients With Adverse Events, Serious Adverse Events, and Death
NCT01585272 (5) [back to overview]	The Discontinuation Rate Due to the Treatment Switching From Oral Capsule to Rivastigmine Patch Treatment
NCT01585272 (5) [back to overview]	Percentage of Patients Successfully Titrated to Rivastigmine Patch 10 cm^2
NCT01585272 (5) [back to overview]	Change From Baseline in Alzheimer Disease Assessment Scale-Cognitive Subscale (ADAS-Cog)
NCT01585272 (5) [back to overview]	Change From Baseline in Mini-Mental Status Examination (MMSE)
NCT01614886 (5) [back to overview]	Percentage of Patients With Adverse Events Leading to Study Drug Discontinuation
NCT01614886 (5) [back to overview]	"Number of Participants With Improvement in Japanese Clinical Global Impression of Change (J-CGIC). Patients With Improvement: a Total of 1. Markedly Improved, 2. Improved, and 3. Slightly"
NCT01614886 (5) [back to overview]	The Percentage of Treatment Retention.
NCT01614886 (5) [back to overview]	Change From Baseline in the Alzheimer's Disease Assessment Scale - Japan Cognitive Subscale (ADAS-J Cog)
NCT01614886 (5) [back to overview]	Change From Baseline in Mini-Mental State Examination (MMSE)
NCT01670526 (4) [back to overview]	Twelve-week Change in Beck Depression Inventory-II (BDI-II)
NCT01670526 (4) [back to overview]	Twelve-week Change in The PTSD Symptom Checklist-Military Version (PCL-M)
NCT01670526 (4) [back to overview]	Twelve-week Change in University of California San Diego Performance-based Skills Assessment - Brief (UPSA-B)
NCT01670526 (4) [back to overview]	Number of Participants With Demonstrated Improvement From Baseline on the Hopkins Verbal Learning Test-Revised (HVLT-R) Total Recall
NCT01948791 (5) [back to overview]	Mean Change From Baseline in Neuropsychiatric Inventory (NPI) Score
NCT01948791 (5) [back to overview]	Change From Baseline in Caregiver Burden Inventory (CBI) Score
NCT01948791 (5) [back to overview]	Change From Baseline in Mini-Mental State Examination (MMSE)
NCT01948791 (5) [back to overview]	Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living (ADCS-ADL) Score
NCT01948791 (5) [back to overview]	Mean Change From Baseline in the Alzheimer's Disease Assessment Scale - Cognitive Subscale (ADAS-cog)
NCT02703636 (8) [back to overview]	Change in Neuropsychiatric Inventory - 10 Item (NPI-10) Score From Baseline to Week 8 and Week 24
NCT02703636 (8) [back to overview]	Change in QOL-AD Score From Baseline to Week 24
NCT02703636 (8) [back to overview]	MMSE Total Score: Change From Baseline to Week 8 and Week 24
NCT02703636 (8) [back to overview]	MMSE Total Score: Change From Baseline to Week 8 and Week 24 (Full Analysis Set)
NCT02703636 (8) [back to overview]	Change From Baseline to Week 8 in Mini-Mental State Examination (MMSE) Total Score
NCT02703636 (8) [back to overview]	Change in as Modified Crichton Scale Score From Baseline to Week 4, 8, 16 and 24
NCT02703636 (8) [back to overview]	Change in J-CGIC Score From Baseline and at Week 24
NCT02703636 (8) [back to overview]	Formulation Usability Questionnaire Form Score up to Week 24
NCT03915626 (1) [back to overview]	Total Area Under the Curve (AUC) 0-12 Hours

Overall Clinical Rating of Change From Baseline to Week 24 Measured by the Clinician's Interview-Based Impression of Change Plus - Japan (CIBIC Plus-J)

"The overall clinical rating of change from baseline to week 24 measured by the 7-point CIBIC plus-J scale. The Clinician's Interview-Based Impression of Change plus Caregiver Input consists of 3 subscales: Disability Assessment of Dementia Scale, Behavioral Pathology in Alzheimer's Disease Rating Scale and Mental Function Impairment Scale, as well as the Clinician's Global Impression of Change (CGIC). Participants are scored according to the following:~Markedly improved~Moderately improved~Minimally improved~Unchanged~Minimally worse~Moderately worse~Markedly worse" (NCT00423085)
Timeframe: Baseline and Week 24

Intervention	Participants (Number)
	Markedly improved	Moderately improved	Minimally improved	Unchanged	Minimally worse	Moderately worse	Markedly worse
Placebo	0	5	36	111	84	29	2
Rivastigmine 10 cm^2	0	6	53	109	78	22	2
Rivastigmine 5 cm^2	0	12	45	109	82	21	0

Intervention	units on a scale (Mean)
	Extension Baseline	End of Extension	Change from Baseline
Open-label Extension Arm	20.0	24.0	4.0

Intervention	units on a scale (Mean)
	Baseline Score	Week 24 Score	Change from Baseline
Placebo	4.8	4.8	-0.1
Rivastigmine 10 cm^2	5.4	5.1	-0.3
Rivastigmine 5 cm^2	4.7	4.6	-0.1

Intervention	Scores on a scale (Mean)
	At Week 25 (n= 95, 107)	At the End of Study (n= 113, 117)
Delayed Switch	-4.2	-4.2
Immediate Switch	-3.9	-3.1

Intervention	Scores on a scale (Mean)
	At week 25 (n= 95, 107)	At the End of Study (n= 114, 118)
Delayed Switch	0.4	0.5
Immediate Switch	-0.1	-0.8

Intervention	Scores on a scale (Mean)
	At Week 25 (n= 96, 106)	At the End of Study (n= 115, 118)
Delayed Switch	-0.4	-0.3
Immediate Switch	-0.7	-0.5

Intervention	Scores on a scale (Mean)
	At Week 5 (n= 116, 114)	At Week 25 (n= 105, 109)
Delayed Switch	4.0	4.3
Immediate Switch	3.9	4.1

Intervention	units on a scale (Mean)
Double Blind: Rivastigmine (10 cm^2)	4.9
Double Blind: Rivastigmine (15 cm^2)	4.1

Intervention	units on a scale (Mean)
Double Blind: Rivastigmine (10 cm^2)	-6.2
Double Blind: Rivastigmine (15 cm^2)	-4.4

Intervention	Time in seconds (Mean)
Double Blind: Rivastigmine (10 cm^2)	18.2
Double Blind: Rivastigmine (15 cm^2)	16.3

Intervention	Participants (Number)
Initial Open Label: Rivastigmine (5 cm^2 / 10 cm^2)	1135
Double Blind: Rivastigmine (10 cm^2)	193
Double Blind: Rivastigmine (15 cm^2)	210
Extended Open Label (10 cm^2)	263

Intervention	Participants (Number)
	Not Decided (ND)	Very good	Good	Average	Poor	Very Poor
Rivastigmine Capsules (6 mg to 12 mg/Day)	1	12	29	5	2	0
Rivastigmine Patch (4.6 mg/Day Switch to 9.5 mg/Day)	0	18	20	3	2	0
Rivastigmine Patch (9.5 mg/Day)	3	14	21	6	2	1

Intervention	Units on a scale (Mean)
	Month 1	Month 3
Rivastigmine Capsules (6 mg to 12 mg/Day)	1.00	-0.40
Rivastigmine Patch (4.6 mg/Day Switch to 9.5 mg/Day)	0.12	-0.59
Rivastigmine Patch (9.5 mg/Day)	0.59	0.12

Intervention	Percentage of participants (Number)
Rivastigmine Patch (4.6 mg/Day Switch to 9.5 mg/Day)	48.84
Rivastigmine Patch (9.5 mg/Day)	55.32
Rivastigmine Capsules (6 mg to 12 mg/Day)	53.06

Intervention	Percentage of participants (Number)
Rivastigmine 4.6 mg/9.5 mg Patch	11.63
Rivastigmine 9.5 mg Patch	17.02

Intervention	Percentage of participants (Number)
Rivastigmine Patch (4.6 mg/Day Switch to 9.5 mg/Day)	4.65
Rivastigmine Patch (9.5 mg/Day)	4.26
Rivastigmine Capsules (6 mg to 12 mg/Day)	6.12

Intervention	Participants (Number)
	No change	Minimal improvement	Moderate improvement	Marked improvement	Minimal decline	Moderate decline	Marked decline
Rivastigmine 5 and 10 cm^2 Patch	21	23	16	15	56	20	14

Intervention	Percentage of participants (Number)
	Very much improved	Much improved	Slightly improved	Unchanged	Slightly worsened	Much worsened	Very much worsened
Rivastigmine Transdermal Patch	4.3	13.0	23.1	32.2	19.2	5.8	2.4

Intervention	scores on a scale (Mean)
	Baseline (n= 198)	Week 24 (n= 181)	Change from Baseline to week 24 (n= 172)
Rivastigmine Transdermal Patch	3.2	3.2	0.1

Intervention	scores on a scale (Mean)
	Baseline (n = 216)	Week 24 (n = 203)	Change from baseline to week 24 (n = 203)
Rivastigmine Transdermal Patch	19.2	19.2	0.0

Intervention	Scores on a scale (Mean)
	Baseline (n= 211)	Week 24 (n= 199)	Change from baseline to week 24 (n= 197)
Rivastigmine Transdermal Patch	2.8	2.9	0.1

rivastigmine

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Dosage Studied

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Biological Processes (147)

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Studies (1,308)

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Clinical Trials (84)

Trial Overview

Trial Outcomes

Overall Clinical Rating of Change From Baseline to Week 24 Measured by the Clinician's Interview-Based Impression of Change Plus - Japan (CIBIC Plus-J)

Extension Phase: Change From Extension Phase Baseline to End of Extension in Modified Crichton Scale

Change From Baseline in CIBIC Plus-J Score Behavioral Pathology in Alzheimer's Disease Rating Scale (Behave-AD)

Extension Phase: Change From Extension Phase Baseline to End of Extension in Mini-Mental State Examination (MMSE)

Extension Phase: Change From Extension Phase Baseline to End of Extension in CIBIC Plus-J Score Disability Assessment for Dementia (DAD)

Change From Baseline in the Alzheimer's Disease Assessment Scale - Japan Cognitive Subscale (ADAS-J Cog)

Change From Baseline in CIBIC Plus-J Score Mental Function Impairment Scale (MENFIS)

Change From Baseline in CIBIC Plus-J Score Disability Assessment for Dementia (DAD)

Change From Baseline in Mini-Mental State Examination (MMSE)

Mean Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living (ADCS-ADL) Total Score at Week 25 and at the End of Study

Mean Change From Baseline in Neuropsychiatric Inventory - 10 Item (NPI-10) Score at Week 25 and at the End of Study.

Mean Change From Baseline in Mini Mental State Exam (MMSE) Score at Week 25 and at the End of Study

Number of Participants Who Discontinued From the Study Due to Any Reason During the Core Phase of the Study

Number of Participants Who Discontinued From Study Due to Any Reason During Extension Phase

Mean Change From Baseline in the Clinical Global Impression of Change (CGIC) Score at Week 5 and Week 25

Number of Participants Who Discontinued From the Study Due to Any Adverse Event (AE) During the Combined Core and Extension Phases of the Study

Change From Baseline in Alzheimer's Disease Assessment Scale-Cognitive (ADAS-Cog) Subscale at Week 48 of Double Blind Period

Change in Alzheimer's Disease Cooperative Study-Instrumental Activities of Daily Living (ADCS-IADL) Subscale Score From Baseline to Week 48 of Double Blind Period

Change in Attention and Executive Function as Assessed by the Trail Making Test (Part A) at Week 48 of the Double Blind Period

Change in Attention and Executive Function as Assessed by the Trail Making Test (Part B) at Week 48 of Double Blind Period

Number of Patients With Adverse Events, Serious Adverse Events and Discontinuations Due to Adverse Events

Change From Baseline in Neuropsychiatric Inventory (NPI)-10 Score at Week 48 of Double Blind Period

Time to Functional Decline as Measured by Alzheimer's Disease Cooperative Study-Instrumental Activities of Daily Living (ADCS-IADL) Subscale During the Double Blind Period

Overall Patient Satisfaction With Treatment

Change in the Total Mini-Mental State Examination (MMSE) Score From Baseline to Month 1 and Month 3

Percentage of Patients With at Least 1 AE of Any Kind Recorded During the Period of the Study.

Percentage of Patients With an AE Involving the Skin (Local Tolerance) Recorded Over the Course of the Study Period (Patch Groups Only)

Percentage of Patients Who Had a Gastrointestinal Adverse Event (AE) at Any Time During the Study

Overall Caregiver Satisfaction With Treatment

Mean Change From Baseline in the Mini-Mental State Examination (MMSE) Score at Week 24

Mean Change From Baseline in the Alzheimer's Disease Cooperative Study- Clinical Global Impression of Change (ADCS-CGIC) at Week 24 Assessed by the Caregiver

Change From Baseline in the Alzheimer's Disease Cooperative Study-Clinical Global Impression of Change (ADCS-CGIC) at Week 24 Assessed by the Physician

Mean Change From Baseline in the Alzheimer's Disease Cooperative Study-Activities of Daily Living (ADCS-ADL) Score at Week 24

Percentage of Participants Treated by Rivastigmine 10 cm^2 Patch for at Least 8 Weeks Who Completed the Study

Percentage of Participants Treated by Rivastigmine 10 cm^2 Patch for at Least 8 Weeks Regardless Whether They Completed the Study

Mean Change From Baseline in the Trail-making Test Part A Score at Week 24

Mean Change From Baseline in the Mini-Zarit Inventory Score of Caregiver Burden at Week 24

Percentage of Participants Who Were Compliant to the 10 cm^2 Patch

Clinical Global Impression of Change (CGI-C) by Physician

Mean Change From Baseline to Week 24 in the 4-item Instrumental Activities of Daily Living (4-IADL) Score

Mean Change From Baseline to Week 24 in the Mini-Mental State Examination (MMSE) Score

Mean Change From Baseline to Week 24 in the Mini-Zarit Inventory Score

Percentage of Patients Who Achieved and Maintained the Maximum Dose of 10 cm^2 Rivastigmine Patch for at Least 8 Weeks During 24 Weeks Study

Change in Unified Parkinson Disease Rating Scale (UPDRS) Part III Motor Examination Scores at Weeks 8, 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline

Percentage of Participants With Adverse Events (AEs) Due, or Potentially Due, to Worsening of Parkinson Disease (PD) Motor Symptoms (Tremor, Muscle Rigidity, Bradykinesia, Fall)

Percentage of Participants With Study Drug Discontinuations Due to Predefined AEs That Are Due, or Potentially Due, to Worsening of PD Motor Symptoms (Tremor, Muscle Rigidity, Bradykinesia, Fall)

UPDRS Part V Stage (Modified Hoehn and Yahr Staging)at Baseline, Week 8,16,24,52 and 76 (or Early Discontinuation)

Change in Alzheimer's Disease Cooperative Study-Activities Of Daily Living (ADCS-ADL) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline

Change in Mattis Dementia Rating Scale (Mattis DRS-2) Scores at Weeks 16, 24, 52 and 76 Compared to Baseline

Change in Neuropsychiatric Inventory-10 (NPI-10) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline

Change in Ten Point Clock Test (TPCT) Scores at Weeks 16, 24, 52 and 76 (or Early Discontinuation) Compared to Baseline

Rivastigmine PK Data Following the First Dose of EVP-6124 - Area Under the Curve (AUC[0-24 h])

Rivastigmine PK Data Following the First Dose of EVP-6124 - Maximum Concentration (Cmax)

Rivastigmine PK Data Following the First Dose of EVP-6124 - Time to Maximum Concentration (Tmax)

Intervention	Score on a scale (Mean)
	Week 8 (n=276,277)	Week 16 (n=254,252)	Week 24 (n=229,237)	Week 52 (n=203,206)	Week 76 (n=183,175)
Rivastigmine Capsule	-0.4	0.5	0.1	0.7	2.1
Rivastigmine Patch	-0.9	-1.7	-1.4	1.6	2.1

Intervention	Percentage of participants (Number)
	Tremor	Muscle Rigidity	Bradykinesia	Fall
Rivastigmine Capsule	24.5	4.1	5.1	17.0
Rivastigmine Patch	9.7	5.2	6.3	20.1

Intervention	Score (Mean)
	Baseline (n = 294,288)	Week 8 (n=17,18)	Week 16 (n=254,252)	Week 24 (229, 236)	Week 52 (n=202,208)	Week 76 (n=184, 175)
Rivastigmine Capsule	2.7	2.6	2.8	2.7	2.8	2.8
Rivastigmine Patch	2.7	2.7	2.7	2.7	2.8	2.8

Intervention	Score (Mean)
	Week 16 (n=273, 270)	Week 24 (n=273,270)	Week 52 (n=273,270)	Week 76 (n=273, 270)
Rivastigmine Capsule	-0.4	-0.6	-2.2	-4.4
Rivastigmine Patch	-1.3	-1.5	-5.4	-7.8

Intervention	Score on a scale (Mean)
	Week 16	Week 24	Week 52	Week 76
Rivastigmine Capsule	5.4	6.5	4.6	3.9
Rivastigmine Patch	3.4	4.4	1.3	-1.4

Intervention	Participants (Number)
	Serious Adverse Events	Non-Serious Adverse Events	No Adverse Events Reported
EVP-6124 (0.1 mg/Day)	0	2	10
EVP-6124 (0.3 mg/Day)	0	3	10
EVP-6124 (1.0 mg/Day)	0	4	7
Placebo	0	4	9

Intervention	ng/mL (Mean)
EVP-6124 (0.1 mg/Day)	29.5
EVP-6124 (0.3 mg/Day)	24.7
EVP-6124 (1.0 mg/Day)	39.2
Placebo	41.9

Intervention	hours (Mean)
EVP-6124 (0.1 mg/Day)	2.30
EVP-6124 (0.3 mg/Day)	1.85
EVP-6124 (1.0 mg/Day)	3.31
Placebo	3.56

Intervention	h*ng/mL (Mean)
EVP-6124 (0.1 mg/Day)	1.31
EVP-6124 (0.3 mg/Day)	3.89
EVP-6124 (1.0 mg/Day)	11.44

Intervention	ng/mL (Mean)
EVP-6124 (0.1 mg/Day)	0.0715
EVP-6124 (0.3 mg/Day)	0.1911
EVP-6124 (1.0 mg/Day)	0.6122