Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
 

 

Target Validation Information
TTD IDTTDS00140
Target NameAcetylcholinesterase    
Type of TargetSuccessful target    
Drug Potency against TargetAmbenoniumIC50 = 0.698 nM[1]
PhysostigmineIC50 = 12 nM[2]
TacrineIC50 = 200 nM[2]
MalathionIC50 = 2500 nM[3]
RivastigmineIC50 = 2615 nM[4]
PyridostigmineIC50 = 330 nM[2]
NeostigmineIC50 = 36 nM[5]
GalantamineIC50 = 365 nM[6]
DonepezilIC50 = 5 nM[7]
EdrophoniumIC50 = 5220 nM[7]
TacrineIC50 = 590 nM[8]
IsoflurophateIC50 = 640 nM[9]
DonepezilKi = 9000 nM[10]
LIPOCRINEIC50 = 0.253 nM[11]
Huprine-Tacrine HeterodimerIC50 = 0.29 nM[12]
Huprine-Tacrine HeterodimerIC50 = 0.32 nM[12]
Huprine-Tacrine HeterodimerIC50 = 0.33 nM[12]
Huprine-Tacrine HeterodimerIC50 = 0.33 nM[12]
Icopezil maleateIC50 = 0.33 nM[13]
Huprine-Tacrine HeterodimerIC50 = 0.34 nM[12]
Huprine-Tacrine HeterodimerIC50 = 0.4 nM[12]
4ALPHA-(HYDROXYMETHYL)-4ALPHA-DEMETHYLTERRITREM BIC50 = 0.423 nM[14]
Huprine-Tacrine HeterodimerIC50 = 0.45 nM[12]
Huprine-Tacrine HeterodimerIC50 = 0.5 nM[12]
(+/-)-huprineY hydrochlorideIC50 = 0.78 nM[15]
Huprine-Tacrine HeterodimerIC50 = 0.82 nM[12]
THIOCTIC ACIDIC50 = 1 nM[16]
Dimethyl-pent-4-enyl-ammonium; bromideIC50 = 1.13 nM[17]
(2-Ethoxy-ethyl)-trimethyl-ammonium; iodideIC50 = 1.16 nM[17]
MEMOQUINIC50 = 1.5 nM[11]
Bis-7-tacrineIC50 = 1.8 nM[18]
Huprine YIC50 = 1.84 nM[19]
(3-Hydroxy-2-methyl-phenyl)-trimethyl-ammoniumIC50 = 1.92 nM[17]
ETHYLPHENSERINEIC50 = 10 nM[20]
(-)-TolserineIC50 = 10.3 nM[21]
N-n-hexyl-7-methoxytacrine hydrochlorideIC50 = 100 nM[22]
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-iumIC50 = 1000 nM[23]
N-n-dodecyl-7-methoxytacrine hydrochlorideIC50 = 1000 nM[22]
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEPIC50 = 1000 nM[24]
BIS(8)-HUPERZINE BIC50 = 1020 nM[25]
3-[8-(benzylmethylamino)octyloxy]xanthen-9-oneIC50 = 10300 nM[26]
MESUAGENIN AIC50 = 1060 nM[27]
9-Amino-1,2,3,4-tetrahydro-acridine-1,7-diolIC50 = 10600 nM[28]
N-benzylnorlitebamineIC50 = 10670 nM[29]
PHENSERINEIC50 = 11.9 nM[30]
3-(2-N-Piperidyl-acetamino)-rutaecarpineIC50 = 111.4 nM[31]
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indoleIC50 = 11800 nM[23]
3-[2-(1-Benzyl-piperidin-4-yl)-ethyl]-1H-indazoleIC50 = 120 nM[13]
Ethyl octylfluorophosphonateIC50 = 120 nM[32]
3-hydroxy-N,N,N-trimethylbenzenaminium iodideIC50 = 12000 nM[33]
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amineIC50 = 12000 nM[18]
N,N'-(1',6-hexylene)-bis-(-)-nor-MEPIC50 = 1220 nM[24]
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromideIC50 = 123 nM[34]
10-Hydroxy-infractopicrinIC50 = 12700 nM[35]
PARAOXONIC50 = 13 nM[32]
6-methoxy-2,9-dimethyl-9H-beta-carbolin-2-iumIC50 = 1300 nM[23]
VELNACRINEIC50 = 1300 nM[28]
9-hydrazino-1,2,3,4-tetrahydroacridineIC50 = 13000 nM[36]
3-(2-N-Pyrrolyl-acetamino)-rutaecarpineIC50 = 131.2 nM[31]
4-[4-(benzhydryloxy)piperidino]butyl benzoateIC50 = 1310 nM[37]
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imineIC50 = 13200 nM[38]
9-O-[3-(Phenylamino)propyl]-berberine bromideIC50 = 138 nM[39]
(3R)-9-amino-3-methyl-1,2,3,4-tetrahydroacridineIC50 = 1384 nM[40]
QUILOSTIGMINEIC50 = 148 nM[20]
3-(4-Benzoylpiperazine-1-carbonyl)coumarinIC50 = 15000 nM[41]
7-methoxytacrineIC50 = 15000 nM[22]
N-allylnorlitebamineIC50 = 15800 nM[29]
N-(14-methylallyl)norgalanthamineIC50 = 160 nM[42]
N-n-nonyl-7-methoxytacrine hydrochlorideIC50 = 1600 nM[22]
LYSICAMINEIC50 = 16100 nM[43]
CAPROCTAMINEIC50 = 170 nM[44]
Caproctamine HClIC50 = 170 nM[45]
Isosorbide-2-(methylcarbamate)-5-mononitrateIC50 = 17200 nM[46]
GENESERINEIC50 = 1740 nM[47]
1,4-Di(berberine-9-O-yl)ethane dibromideIC50 = 176 nM[39]
AP-2243IC50 = 18 nM[48]
BIS(16)-HUPERZINE BIC50 = 18.5 nM[25]
N-ALLYLNORGALANTHAMINEIC50 = 180 nM[42]
6-hydroxy-2,9-dimethyl-9H-beta-carbolin-2-iumIC50 = 1800 nM[23]
pseudopalmatine trifluoroacetateIC50 = 1800 nM[43]
CRYPTADINE BIC50 = 18500 nM[49]
TURBINATINEIC50 = 1860 nM[50]
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-iumIC50 = 1900 nM[23]
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-olIC50 = 19200 nM[51]
(-)-HUPERZINE BIC50 = 19300 nM[25]
(2-Butyryloxy-ethyl)-trimethyl-ammonium; iodideIC50 = 2.29 nM[17]
(2-Chloro-ethyl)-trimethyl-ammonium; chlorideIC50 = 2.39 nM[17]
Allyl-trimethyl-ammonium; bromideIC50 = 2.92 nM[17]
XANTHOSTIGMINEIC50 = 20 nM[52]
1,9-bis(pyridinium)-nonane dibromideIC50 = 2000 nM[53]
3-(2-N-Piperidyl-propionamino)-rutaecarpineIC50 = 21.4 nM[31]
HEPTYPHYSOSTIGMINEIC50 = 22 nM[20]
6-methoxy-2-methyl-9H-beta-carbolin-2-iumIC50 = 2200 nM[23]
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromideIC50 = 224 nM[34]
1,3-Di(berberine-9-O-yl)ethane dibromideIC50 = 226 nM[39]
Alkylene Linked Bis-Galanthamine derivativeIC50 = 230 nM[54]
(-)-PhenserineIC50 = 24 nM[21]
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEPIC50 = 24 nM[24]
BIS(20)-HUPERZINE BIC50 = 25.2 nM[25]
3-(dimethylamino)phenyl phenylcarbamateIC50 = 2500 nM[21]
iso-OMPAIC50 = 2500 nM[46]
9-Ethyl-2-methyl-beta-carboline-2-ium iodideIC50 = 2567 nM[55]
3-[3-(benzylmethylamino)propoxy]xanthen-9-oneIC50 = 2680 nM[26]
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEPIC50 = 270 nM[24]
N-n-heptyl-7-methoxytacrine hydrochlorideIC50 = 270 nM[22]
N-isopropylnorlitebamineN-methoiodideIC50 = 2790 nM[29]
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-oneIC50 = 2820 nM[26]
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-oneIC50 = 2890 nM[26]
3-(2-N-Pyrrolyl-propionamino)-rutaecarpineIC50 = 29.24 nM[31]
CHOLINE IODIDEIC50 = 3.01 nM[17]
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEPIC50 = 3.9 nM[24]
1,2-Di(berberine-9-O-yl)ethane dibromideIC50 = 320 nM[39]
3-(2,5-Dioxo-pyrrolidin-1-yl)-benzoic acidIC50 = 33.4 nM[56]
N-benzyl-2-thiomorpholinopyrimidin-4-amineIC50 = 330 nM[18]
TASPINEIC50 = 330 nM[57]
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromideIC50 = 340 nM[39]
Bis(14)-Huperzine BIC50 = 35.9 nM[25]
5-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamineIC50 = 36 nM[58]
1-(3-Bromomethyl-phenyl)-2,2,2-trifluoro-ethanoneIC50 = 360 nM[59]
N-n-octyl-7-methoxytacrine hydrochlorideIC50 = 360 nM[22]
3-(2-Diethylamino-acetamino)-rutaecarpineIC50 = 372.3 nM[31]
1-benzene sulfonyl-cis-2,6-dimethyl piperidineIC50 = 388 nM[60]
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromideIC50 = 398 nM[34]
galanthamine derivativeIC50 = 4 nM[61]
(2-Mercapto-ethyl)-trimethyl-ammonium; iodideIC50 = 4.4 nM[17]
8-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamineIC50 = 4.43 nM[58]
(4-Iodo-butyl)-trimethyl-ammonium; iodideIC50 = 4.71 nM[17]
BIS(18)-HUPERZINE BIC50 = 4.93 nM[25]
7-Chloro-1,2,3,4-tetrahydro-acridin-9-ylamineIC50 = 40 nM[58]
TOLSERINEIC50 = 40 nM[20]
1,10-bis(pyridinium)-decane dibromideIC50 = 400 nM[53]
palmatine trifluoroacetateIC50 = 400 nM[43]
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEPIC50 = 42 nM[24]
6-hydroxy-2-methyl-9H-beta-carbolin-2-iumIC50 = 4200 nM[23]
AP-2238IC50 = 44 nM[62]
VOACANGINEIC50 = 4400 nM[63]
Alkylene Linked Bis-Galanthamine derivativeIC50 = 450 nM[54]
6-Methyl-4-(4-phenylpiperazin-1-yl)coumarinIC50 = 4500 nM[41]
BIS(9)-HUPERZINE BIC50 = 471 nM[25]
2-morpholino-N-phenethylpyrimidin-4-amineIC50 = 4800 nM[18]
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromideIC50 = 490 nM[39]
(5-Bromo-pentyl)-trimethyl-ammonium; bromideIC50 = 5.34 nM[17]
6-chlorotacrine hydrochlorideIC50 = 5.73 nM[64]
(4-Bromo-butyl)-trimethyl-ammonium; bromideIC50 = 5.97 nM[17]
Bis(14)-Huperzine BIC50 = 50.8 nM[25]
N-benzyl-2-morpholinopyrimidin-4-amineIC50 = 500 nM[18]
pseudocolumbamine trifluoroacetateIC50 = 5000 nM[43]
CHF-2819IC50 = 5120 nM[47]
GANSTIGMINEIC50 = 5120 nM[61]
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromideIC50 = 520 nM[34]
EDROPHONIUM BROMIDEIC50 = 5360 nM[61]
Isosorbide-di-(4-nitrophenyl carbamate)IC50 = 5400 nM[65]
Alkylene Linked Bis-Galanthamine derivativeIC50 = 560 nM[54]
1,3-Bis-(3-imidazolidin-2-yl-phenyl)-ureaIC50 = 590 nM[66]
Trimethyl-(3-nitro-phenyl)-ammonium; iodideIC50 = 6.28 nM[17]
3-[4-(benzylmethylamino)butoxy]xanthen-9-oneIC50 = 6250 nM[26]
BW-28C51IC50 = 63 nM[46]
Chlorphrifos oxonIC50 = 63 nM[32]
Isopropyl dodecylfluorophosphonateIC50 = 6300 nM[32]
Isosorbide-di-(ethylcarbamate)IC50 = 6500 nM[65]
N-isobutylnorlitebamineIC50 = 6510 nM[29]
GALANTAMINE HYDROBROMIDEIC50 = 670 nM[67]
N-n-pentyl-7-methoxytacrine hydrochlorideIC50 = 6700 nM[22]
3-(4-o-Tolylpiperazine-1-carbonyl)coumarinIC50 = 6700 nM[41]
N-isopropylnorlitebamineIC50 = 6800 nM[29]
MESUAGENIN BIC50 = 700 nM[27]
carinatumins B (2)IC50 = 7000 nM[68]
N-propylnorlitebamineIC50 = 7210 nM[29]
6-Methyl-4-(4-benzoylpiperazin-1-yl)coumarinIC50 = 7400 nM[41]
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromideIC50 = 743 nM[39]
BIS(12)-HUPERZINE BIC50 = 76.2 nM[25]
(-)-CymserineIC50 = 760 nM[21]
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-oneIC50 = 7780 nM[26]
N-butylnorlitebamineIC50 = 7790 nM[29]
N,N'-(1',8'-octylene)-bis-(-)-nor-MEPIC50 = 79 nM[24]
6-Methyl-4-(4-o-tolylpiperazin-1-yl)coumarinIC50 = 7900 nM[41]
BW-28C51IC50 = 8 nM[33]
Hexyl-trimethyl-ammonium; iodideIC50 = 8.16 nM[17]
But-3-enyl-trimethyl-ammonium; bromideIC50 = 8.48 nM[17]
Trimethyl-(4-oxo-pentyl)-ammonium; iodideIC50 = 8.48 nM[17]
(3-Bromo-propyl)-trimethyl-ammonium; bromideIC50 = 8.79 nM[17]
(RS)-tacrine(10)-hupyridoneIC50 = 8.8 nM[61]
3-(2-Diethylamino-propionamino)-rutaecarpineIC50 = 80.2 nM[31]
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-iumIC50 = 800 nM[23]
4-ISOPROPYLPHENSERINEIC50 = 8400 nM[69]
2-Propyl-beta-carboline-2-ium iodideIC50 = 845 nM[55]
CORONARIDINEIC50 = 8600 nM[63]
Mesuagenin DIC50 = 8730 nM[27]
CLEBOPRIDEIC50 = 890 nM[66]
N,N'-(1',10'-decylene)-bis-(-)-nor-MEPIC50 = 9.5 nM[24]
cis-2,6-dimethyl-1-methyl sulfonyl piperidineIC50 = 90 nM[60]
PetrosamineIC50 = 91 nM[70]
3-(3-Carboxy-propionylamino)-benzoic acidIC50 = 92.5 nM[56]
N-n-propyl-7-methoxytacrine hydrochlorideIC50 = 9200 nM[22]
3-(4-Phenylpiperazin-1-carbonyl)coumarinIC50 = 9300 nM[41]
INFRACTOPICRINIC50 = 9720 nM[35]
N-benzyl-2-(pyrrolidin-1-yl)pyrimidin-4-amineIC50 = 9800 nM[18]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-oneKi < 1000 nM[71]
huprine XKi = 0.13 nM[61]
(S,S)-(-)-bis(10)-hupyridoneKi = 0.8 nM[61]
6,8-Dichloro-1,2,3,4-tetrahydro-acridin-9-ylamineKi = 1 nM[72]
haloxysterol CKi = 1100 nM[51]
24-ethyl-cholest-7-ene-3,5,6-triolKi = 12600 nM[51]
2-Hex-5-enyl-5-non-8-enyl-3,4-dihydro-2H-pyrroleKi = 13000 nM[73]
7-Oxo-7H-dibenzo[de,g]quinolineKi = 14580 nM[74]
2-Hex-5-enyl-5-nonyl-pyrrolidineKi = 1500 nM[73]
GALLAMINEKi = 15000 nM[61]
LAWSARITOLKi = 16100 nM[51]
CHLORANILKi = 163 nM[75]
3,4,5,6-Tetrachloro-[1,2]benzoquinoneKi = 1670 nM[75]
haloxysterol DKi = 17000 nM[51]
(S,S)-(-)-bis(12)-hupyridoneKi = 19.6 nM[61]
DECIDIUMKi = 21.3 nM[61]
2-Hex-5-enyl-5-non-8-enyl-pyrrolidineKi = 2500 nM[73]
1,11-bis(pyridinium)-undecane dibromideKi = 30 nM[53]
1,2-NAPHTHOQUINONEKi = 320 nM[76]
(-)-huperzine BKi = 334 nM[61]
9-amino-7H-dibenzo[de,h]quinolin-7-oneKi = 3860 nM[74]
24-ethylcholest-6-ene-3,5-diolKi = 4000 nM[51]
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromideKi = 45 nM[34]
5-Hex-5-enyl-2-nonyl-3,4-dihydro-2H-pyrroleKi = 5000 nM[73]
4-formylphenyl-O-beta-D-ribopyranosideKi = 510 nM[77]
4-formylphenyl-O-beta-DglucopyranosideKi = 730 nM[77]
HALOXYSTEROL AKi = 7600 nM[51]
HALOXYSTEROL BKi = 850 nM[51]
NSC-23180Ki = 850 nM[76]
5,6-dinitroacenaphthoquinoneKi = 903 nM[76]
N-Methyl-1'H-phenothiazine-1'-carboxamideKi = 9360 nM[78]
BENZOQUINONEKi = 955 nM[75]
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National University of Singapore, Singapore


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