Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00143
Target NameCholinesterase    
Type of TargetSuccessful target    
Drug Potency against TargetIsosorbide-2-benzylcarbamate-5-(o-toluate)IC50 = 1.2 nM[1]
N,N'-(1',9'-nonylene)-bis-(-)-nor-MEPIC50 = 10 nM[2]
Bis-7-tacrineIC50 = 10.5 nM[3]
3-[10-(benzylmethylamino)decyloxy]xanthen-9-oneIC50 = 100 nM[4]
3-[9-(benzylmethylamino)nonyloxy]xanthen-9-oneIC50 = 100 nM[4]
N,N'-(1',12'-dodecydene)-bis-(-)-nor-MEPIC50 = 100 nM[2]
N-n-hexyl-7-methoxytacrine hydrochlorideIC50 = 1000 nM[5]
VAGANINE DIC50 = 10000 nM[6]
N,N'-(1',7'-heptylene)-bis-(-)-nor-MEPIC50 = 102 nM[2]
PHENSERINEIC50 = 103.7 nM[7]
N,N'-(1',4'-butylene)-bis-(-)-nor-MEPIC50 = 104 nM[2]
Isosorbide-di-(propylcarbamate)IC50 = 10400 nM[8]
LIPOCRINEIC50 = 11 nM[9]
1,2-Di(berberine-9-O-yl)ethane dibromideIC50 = 1110 nM[10]
CAPROCTAMINEIC50 = 11600 nM[11]
Caproctamine HClIC50 = 11600 nM[12]
N,N'-(1',6-hexylene)-bis-(-)-nor-MEPIC50 = 119 nM[2]
3-[11-(benzylmethylamino)undecyloxy]xanthen-9-oneIC50 = 120 nM[4]
N-n-octyl-7-methoxytacrine hydrochlorideIC50 = 120 nM[5]
6-methoxy-1,2-dimethyl-9H-beta-carbolin-2-iumIC50 = 1200 nM[13]
Isosorbide-di-(butylcarbamate)IC50 = 1220 nM[8]
N,N'-(1',2'-ethylene)-bis-(-)-nor-MEPIC50 = 125 nM[2]
N,N'-(1',3'-propylene)-bis-(-)-nor-MEPIC50 = 132 nM[2]
NOSTOCARBOLINEIC50 = 13200 nM[14]
4-[4-(benzyloxy)piperidino]butyl-3-chlorobenzoateIC50 = 1350 nM[15]
(-)-DEBROMOFLUSTRAMINE BIC50 = 1370 nM[16]
N-phenethyl-2-(pyrrolidin-1-yl)pyrimidin-4-amineIC50 = 13800 nM[3]
Huprine-Tacrine HeterodimerIC50 = 14 nM[17]
bis-cyclosal-d4TMPIC50 = 14000 nM[18]
3-[6-(benzylmethylamino)hexyloxy]xanthen-9-oneIC50 = 1430 nM[4]
MEMOQUINIC50 = 1440 nM[9]
3-[12-(benzylmethylamino)dodecyloxy]xanthen-9-oneIC50 = 150 nM[4]
MEPTAZINOLIC50 = 15000 nM[2]
GALANTAMINE HYDROBROMIDEIC50 = 1520 nM[19]
(-)-PhenserineIC50 = 1560 nM[20]
4-[4-(benzyloxy)piperidino]butyl-3-fluorobenzoateIC50 = 1580 nM[15]
Huprine-Tacrine HeterodimerIC50 = 16.4 nM[17]
6-hydroxy-1,2-dimethyl-9H-beta-carbolin-2-iumIC50 = 1600 nM[13]
N-n-pentyl-7-methoxytacrine hydrochlorideIC50 = 16000 nM[5]
N,N'-(1',10'-decylene)-bis-(-)-nor-MEPIC50 = 17 nM[2]
CHF-2819IC50 = 1700 nM[21]
6-methoxy-1,9-dimethyl-9H-pyrido[3,4-b]indoleIC50 = 17400 nM[13]
6-methoxy-2-methyl-9H-beta-carbolin-2-iumIC50 = 17500 nM[13]
9-O-[3-(Phenylamino)propyl]-berberine bromideIC50 = 1760 nM[10]
3-(2-Diethylamino-acetamino)-rutaecarpineIC50 = 17620 nM[22]
3-(dimethylamino)phenyl phenylcarbamateIC50 = 18000 nM[20]
4-[4-(benzyloxy)piperidino]butyl benzoateIC50 = 1890 nM[15]
N,N'-(1',5'-pentylene)-bis-(-)-nor-MEPIC50 = 192 nM[2]
(-)-TolserineIC50 = 1950 nM[20]
TOLSERINEIC50 = 1950 nM[23]
9-Ethyl-2-methyl-beta-carboline-2-ium iodideIC50 = 2019 nM[24]
9-O-[3-(4-Nitro-phenoxyl)butyl]-berberine bromideIC50 = 2050 nM[10]
3-(2-N-Piperidyl-propionamino)-rutaecarpineIC50 = 2112 nM[22]
9-O-[3-(Phenylol-1-yloxy)propyl]berberine bromideIC50 = 2220 nM[25]
3-sal-cyclosal-d4TMPIC50 = 2300 nM[18]
N-benzyl-2-thiomorpholinopyrimidin-4-amineIC50 = 2300 nM[3]
2-Propyl-beta-carboline-2-ium iodideIC50 = 2305 nM[24]
1,4-Di(berberine-9-O-yl)ethane dibromideIC50 = 231 nM[10]
(+/-)-huprineY hydrochlorideIC50 = 236 nM[26]
4-ISOPROPYLPHENSERINEIC50 = 240 nM[27]
3-[5-(benzylmethylamino)pentyloxy]xanthen-9-oneIC50 = 2490 nM[4]
Isosorbide-2-(cyclohexylcarbamate)-5-mononitrateIC50 = 2500 nM[28]
(+/-)-DEBROMOFLUSTRAMINE BIC50 = 2590 nM[16]
DEMETHYLDEBROMOFLUSTRAMINE BIC50 = 260 nM[16]
3-[4-(benzylmethylamino)butoxy]xanthen-9-oneIC50 = 2650 nM[4]
9-O-[5-(Phenylol-1-yloxy)pentyl]berberine bromideIC50 = 2690 nM[25]
6-hydroxy-1,2,9-trimethyl-9H-beta-carbolin-2-iumIC50 = 2700 nM[13]
3-(2-Diethylamino-propionamino)-rutaecarpineIC50 = 2848 nM[22]
Isosorbide-2-(benzylcarbamate)-5-mononitrateIC50 = 3.6 nM[28]
9-O-[2-(Phenylol-1-yloxy)ethyl]berberine bromideIC50 = 3000 nM[25]
Huprine-Tacrine HeterodimerIC50 = 31.1 nM[17]
Isosorbide-2-benzylcarbamate-5-cyclopropanoateIC50 = 334 nM[28]
AS-1397IC50 = 3370 nM[29]
3-phenyl-cyclosal-d4TMPIC50 = 350 nM[18]
4-[4-(benzyloxy)piperidino]butyl-4-chlorobenzoateIC50 = 3520 nM[15]
Isosorbide-2-benzylcarbamate-5-triflateIC50 = 359 nM[28]
N-n-nonyl-7-methoxytacrine hydrochlorideIC50 = 360 nM[5]
isosorbide-2-benzyl carbamateIC50 = 3700 nM[1]
Isosorbide-2-(ethylcarbamate)-5-mononitrateIC50 = 3900 nM[28]
Isosorbide-2-(benzylcarbamate)-5-benzoateIC50 = 4.3 nM[28]
Huprine-Tacrine HeterodimerIC50 = 4.74 nM[17]
N-n-heptyl-7-methoxytacrine hydrochlorideIC50 = 40 nM[5]
Isosorbide-di-(benzylcarbamate)IC50 = 400 nM[8]
7-Oxo-7H-dibenzo[de,g]quinolineIC50 = 4010 nM[30]
Isosorbide-2-benzylcarbamate-5-acetateIC50 = 4100 nM[28]
9-O-[3-(2-Pyridinoxyl)butyl]-berberine bromideIC50 = 4160 nM[10]
9-O-[2-(Phenylol-1-yloxy)hexyl]berberine bromideIC50 = 4180 nM[25]
5-methyl-cyclosal-d4TMPIC50 = 4600 nM[18]
3-isopr-sal-cyclosal-d4TMPIC50 = 4700 nM[18]
XANTHOSTIGMINEIC50 = 48 nM[31]
HEPTYPHYSOSTIGMINEIC50 = 5 nM[23]
Huprine-Tacrine HeterodimerIC50 = 5.55 nM[17]
1,10-bis(pyridinium)-decane dibromideIC50 = 5000 nM[32]
(-)-CymserineIC50 = 51 nM[20]
Isosorbide-2-(methylcarbamate)-5-mononitrateIC50 = 5100 nM[28]
4-[4-(benzyloxy)piperidino]butyl-4-nitrobenzoateIC50 = 5230 nM[15]
1,3-Di(berberine-9-O-yl)ethane dibromideIC50 = 531 nM[10]
2-Methyl-beta-carboline-2-ium iodideIC50 = 540 nM[24]
9-O-[3-(4-Bromo-phenoxyl)butyl]-berberine bromideIC50 = 5440 nM[10]
1-methyl-3-(phenylcarbamoyloxy)pyridinium bromideIC50 = 550 nM[20]
4-[4-(benzyloxy)piperidino]butyl-4-fluorobenzoateIC50 = 560 nM[15]
Isosorbide-2-benzylcarbamate-5-nicotinateIC50 = 57 nM[28]
(-)-PhenethylcymserineIC50 = 6 nM[20]
Isosorbide-2-benzylcarbamate-5-cyclopentanoateIC50 = 6 nM[28]
Huprine-Tacrine HeterodimerIC50 = 6.7 nM[17]
1,9-bis(pyridinium)-nonane dibromideIC50 = 6000 nM[32]
N,N'-(1',8'-octylene)-bis-(-)-nor-MEPIC50 = 63 nM[2]
Isosorbide-2-(propylcarbamate)-5-mononitrateIC50 = 639 nM[28]
Isosorbide-2-(methylcarbamate)-5-benzoateIC50 = 669 nM[28]
3-(2-N-Pyrrolyl-acetamino)-rutaecarpineIC50 = 696.1 nM[22]
Huprine-Tacrine HeterodimerIC50 = 7.38 nM[17]
Huprine-Tacrine HeterodimerIC50 = 7.69 nM[17]
Huprine-Tacrine HeterodimerIC50 = 7.8 nM[17]
Isosorbide-2-benzylcarbamate-5-pentanoateIC50 = 700 nM[28]
1,11-bis(pyridinium)-undecane dibromideIC50 = 7000 nM[32]
Isosorbide-2-(butylcarbamate)-5-benzoateIC50 = 72 nM[28]
2,3-dihydropyrrolo[2,1-b]quinazolin-9(1H)-imineIC50 = 7200 nM[33]
iso-OMPAIC50 = 733 nM[28]
N,N'-(1',11'-undecydene)-bis-(-)-nor-MEPIC50 = 74 nM[2]
cyclosal-d4TMPIC50 = 770 nM[18]
3-[8-(benzylmethylamino)octyloxy]xanthen-9-oneIC50 = 80 nM[4]
3-[7-(benzylmethylamino)-heptyloxy]xanthen-9-oneIC50 = 800 nM[4]
(RS)-tacrine(10)-hupyridoneIC50 = 81.5 nM[34]
3-[3-(benzylmethylamino)propoxy]xanthen-9-oneIC50 = 8330 nM[4]
3-(2-N-Pyrrolyl-propionamino)-rutaecarpineIC50 = 844.5 nM[22]
6-hydroxy-2-methyl-9H-beta-carbolin-2-iumIC50 = 8700 nM[13]
Isosorbide-2-benzylcarbamate-5-isonicotinateIC50 = 88 nM[28]
Isosorbide-2-(butylcarbamate)-5-mononitrateIC50 = 894 nM[28]
6-chlorotacrine hydrochlorideIC50 = 916 nM[35]
Isosorbide-2-benzylcarbamate-5-propionateIC50 = 980 nM[28]
N-Cyclobutyl-1'H-phenothiazine-1'-carboxamideKi = 10000 nM[36]
9-O-[4-(Phenylol-1-yloxy)butyl]berberine bromideKi = 1020 nM[25]
methyl 10H-phenothiazine-10-carboxylateKi = 10200 nM[37]
N,N-Diethyl-1'H-phenothiazine-1'-carboxamideKi = 1050 nM[36]
4-chlorophenyl 10H-phenothiazine-10-carboxylateKi = 10500 nM[37]
N-tert-Butyl-1'H-phenothiazine-1'-carboxamideKi = 10600 nM[36]
huprine XKi = 120 nM[38]
naphthalen-2-yl 10H-phenothiazine-10-carboxylateKi = 120 nM[37]
N-p-Tolyl-1'H-phenothiazine-1'-carboxamideKi = 12100 nM[36]
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dioneKi = 12600 nM[39]
1,2-bis(2,3-fluorophenyl)ethane-1,2-dioneKi = 1270 nM[40]
(4-bromophenyl)(10H-phenothiazin-10-yl)methanoneKi = 1300 nM[41]
butyl 10H-phenothiazine-10-carboxylateKi = 13400 nM[37]
(1'H-Phenothiazin-1'-yl)(piperidin-1-yl)methanoneKi = 1560 nM[36]
NSC-23180Ki = 1670 nM[42]
m-tolyl 10H-phenothiazine-10-carboxylateKi = 1690 nM[37]
1-(10H-phenothiazin-10-yl)-3-phenylbutan-1-oneKi = 1700 nM[41]
2-biphenyl-4-yl-1-phenothiazin-10-yl-ethanoneKi = 1700 nM[41]
N,N-Diisopropyl-1'H-phenothiazine-1'-carboxamideKi = 180 nM[36]
haloxysterol CKi = 18000 nM[43]
isopropyl 10H-phenothiazine-10-carboxylateKi = 18100 nM[37]
N-Methyl-1'H-phenothiazine-1'-carboxamideKi = 18300 nM[36]
phenanthrene-9,10-dioneKi = 190 nM[42]
(10H-phenothiazin-10-yl)(m-tolyl)methanoneKi = 1900 nM[41]
BENZOQUINONEKi = 2050 nM[44]
1,2-di(10H-phenothiazin-10-yl)ethane-1,2-dioneKi = 220 nM[41]
1-(10H-phenothiazin-10-yl)-4-phenylbutan-1-oneKi = 220 nM[41]
haloxysterol DKi = 2200 nM[43]
4-methoxyphenyl 10H-phenothiazine-10-carboxylateKi = 2260 nM[37]
1,2-NAPHTHOQUINONEKi = 2290 nM[42]
(10H-phenothiazin-10-yl)(p-tolyl)methanoneKi = 2500 nM[41]
24-ethyl-cholest-7-ene-3,5,6-triolKi = 2500 nM[43]
HALOXYSTEROL BKi = 2500 nM[43]
1,2-indanedioneKi = 2630 nM[42]
N-Neopentyl-1'H-phenothiazine-1'-carboxamideKi = 2660 nM[36]
CHLORANILKi = 268 nM[44]
N-Cyclohexyl-1'H-phenothiazine-1'-carboxamideKi = 2810 nM[36]
p-tolyl 10H-phenothiazine-10-carboxylateKi = 2850 nM[37]
ACENAPHTHOQUINONEKi = 2970 nM[42]
N-Cyclopentyl-1'H-phenothiazine-1'-carboxamideKi = 2990 nM[36]
anthracen-10-yl(10H-phenothiazin-10-yl)methanoneKi = 3.5 nM[41]
N-Phenyl-1'H-phenothiazine-1'-carboxamideKi = 310 nM[36]
5,6-dinitroacenaphthoquinoneKi = 3100 nM[42]
(10H-phenothiazin-10-yl)(o-tolyl)methanoneKi = 3100 nM[41]
cyclopentyl 10H-phenothiazine-10-carboxylateKi = 3190 nM[37]
3,4,5,6-Tetrachloro-[1,2]benzoquinoneKi = 3200 nM[44]
2-methoxyphenyl 10H-phenothiazine-10-carboxylateKi = 340 nM[37]
N-Isopropyl-1'H-phenothiazine-1'-carboxamideKi = 3410 nM[36]
N-(Adamant-1-yl)-1'H-phenothiazine-1'-carboxamideKi = 350 nM[36]
naphthalen-1-yl 10H-phenothiazine-10-carboxylateKi = 36 nM[37]
LAWSARITOLKi = 3700 nM[43]
o-tolyl 10H-phenothiazine-10-carboxylateKi = 390 nM[37]
1-(10H-phenothiazin-10-yl)-2-phenylbutan-1-oneKi = 400 nM[41]
24-ethylcholest-6-ene-3,5-diolKi = 4200 nM[43]
N,N-Dipropyl-1'H-phenothiazine-1'-carboxamideKi = 430 nM[36]
tert-butyl 10H-phenothiazine-10-carboxylateKi = 4300 nM[37]
N-Benzyl-1'H-phenothiazine-1'-carboxamideKi = 4450 nM[36]
HALOXYSTEROL AKi = 4500 nM[43]
(24S)-ethylcholesta-7,9(11),22(E)-triene-3b-olKi = 4600 nM[43]
naphthalen-2-yl(10H-phenothiazin-10-yl)methanoneKi = 470 nM[41]
1-(10H-phenothiazin-10-yl)-2-phenylpropan-1-oneKi = 560 nM[41]
3-chlorophenyl 10H-phenothiazine-10-carboxylateKi = 570 nM[37]
phenyl 10H-phenothiazine-10-carboxylateKi = 570 nM[37]
(10H-phenothiazin-10-yl)(phenyl)methanoneKi = 5800 nM[41]
(3-bromophenyl)(10H-phenothiazin-10-yl)methanoneKi = 600 nM[41]
1-(10H-phenothiazin-10-yl)-2-phenylethanoneKi = 610 nM[41]
1-(10H-phenothiazin-10-yl)-3-phenylpropan-1-oneKi = 6200 nM[41]
3-methoxyphenyl 10H-phenothiazine-10-carboxylateKi = 710 nM[37]
N-o-Tolyl-1'H-phenothiazine-1'-carboxamideKi = 710 nM[36]
Morpholino(1'H-phenothiazin-1'-yl)methanoneKi = 7100 nM[36]
(4-nitrophenyl)(10H-phenothiazin-10-yl)methanoneKi = 820 nM[41]
naphthalen-1-yl(10H-phenothiazin-10-yl)methanoneKi = 88 nM[41]
N,N-Dimethyl-1'H-phenothiazine-1'-carboxamideKi = 9200 nM[36]
Ref 1J Med Chem. 2010 Feb 11;53(3):1190-9.Isosorbide-2-benzyl carbamate-5-salicylate, a peripheral anionic site binding subnanomolar selective butyrylcholinesterase inhibitor. To Reference
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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