Target Validation Information
TTD ID T83875
Target Name Monoamine oxidase type A (MAO-A)
Type of Target
Successful
Drug Potency against Target Moclobemide Drug Info IC50 = 361380 nM [31]
Tranylcypromine Drug Info IC50 = 20000 nM [7]
Drug Info Ki = 2200 nM [25]
Drug Info Ki = 400 nM [5]
Drug Info Ki = 70 nM [19]
Drug Info IC50 = 100 nM [29]
Drug Info Ki = 392 nM [13]
Drug Info Ki = 1800 nM [11]
Drug Info IC50 = 11000 nM [17]
Drug Info IC50 = 7.6 nM [8]
Drug Info IC50 = 18000 nM [15]
Drug Info IC50 = 2560 nM [18]
Drug Info IC50 = 2510 nM [9]
Drug Info Ki = 1530 nM [23]
Drug Info Ki = 220 nM [23]
Drug Info Ki = 700 nM [12]
Drug Info Ki = 84 nM [5]
Drug Info Ki = 170 nM [19]
Drug Info Ki = 160 nM [5]
Drug Info Ki = 8680 nM [30]
Drug Info Ki = 30 nM [19]
Drug Info Ki = 1600 nM [19]
Drug Info Ki = 5 nM [4]
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine Drug Info Ki = 19000 nM [30]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one Drug Info Ki = 10000 nM [30]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholine Drug Info Ki = 14100 nM [30]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one Drug Info Ki = 12300 nM [30]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholine Drug Info Ki = 2170 nM [30]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one Drug Info Ki = 9280 nM [30]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholine Drug Info Ki = 6390 nM [30]
(+/-)-2-(4'-Propoxyphenyl)thiomorpholine Drug Info Ki = 3690 nM [30]
(+/-)-2-Phenylthiomorpholin-5-one Drug Info Ki = 9190 nM [30]
(+/-)-2-Phenylthiomorpholine Drug Info Ki = 10600 nM [30]
(6-Benzyloxy-2-naphthyl)-2-aminopropane Drug Info Ki = 3780 nM [23]
(6-Ethoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 450 nM [23]
(6-Methoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 180 nM [23]
(6-methylthio-2-naphthyl)isopropylamine Drug Info Ki = 500 nM [23]
(6-Propoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 680 nM [23]
(7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile Drug Info IC50 = 200 nM [26]
(E)-5-(3-Chlorostyryl)isatin Drug Info Ki = 5600 nM [25]
(E)-5-Styrylisatin Drug Info Ki = 780 nM [25]
(R)-Indan-1-yl-methyl-prop-2-ynyl-amine Drug Info IC50 = 70 nM [3]
(R,S)-N-(R-phenylethyl)-1H-pyrrole-2-carboxamide Drug Info Ki = 1220 nM [12]
(R/R)BEFLOXATONE Drug Info Ki = 2.5 nM [2]
(S)-2-amino-1-(4-ethylthiophenyl)-propane Drug Info Ki = 54 nM [13]
(S)-2-amino-1-(4-methylthiophenyl)-propane Drug Info Ki = 245 nM [13]
(S)-2-amino-1-(4-propylthiophenyl)-propane Drug Info Ki = 115 nM [13]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 6.5 nM [6]
1-(1-Naphthyl)-2-aminopropane Drug Info Ki = 5630 nM [23]
1-(2-Naphthyl)-2-aminopropane Drug Info Ki = 420 nM [23]
1-(3-(4-chlorobenzyl)quinoxalin-2-yl)hydrazine Drug Info IC50 = 2.1 nM [8]
1-(3-benzylquinoxalin-2-yl)hydrazine Drug Info IC50 = 8.8 nM [8]
1-(4-(benzyloxy)phenyl)propan-2-amine Drug Info Ki = 3420 nM [23]
1-(4-butoxyphenyl)propan-2-amine Drug Info Ki = 320 nM [23]
1-(4-propoxyphenyl)propan-2-amine Drug Info Ki = 130 nM [23]
2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole Drug Info Ki = 4.7 nM [5]
2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 14851 nM
2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 7883 nM
2-(3,4-dimethoxyphenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 13570 nM [21]
2-(3-benzylquinoxalin-2-ylamino)ethanol Drug Info IC50 = 3.7 nM [8]
2-(4,5-dihydro-1H-imidazol-2-yl)quinoline Drug Info IC50 = 12700 nM [21]
2-(4-methoxyphenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 15750 nM [21]
2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole Drug Info Ki = 13890 nM [21]
2-Amino-1-(4-methylthiophenyl)propane Drug Info Ki = 250 nM [23]
2-BFi Drug Info Ki = 1.7 nM [1]
2-Bromo-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 8500 nM [29]
2-Chloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 2600 nM [29]
2-Chloro-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 9400 nM [29]
2-Furan-2-yl-4,5-dihydro-1H-imidazole Drug Info Ki = 2340 nM [4]
2-oxo-N-m-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 14500 nM [24]
2-oxo-N-p-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 19450 nM [24]
2-oxo-N-phenyl-2H-chromene-3-carboxamide Drug Info IC50 = 13120 nM [24]
2-Phenoxymethyl-4,5-dihydro-1H-imidazole Drug Info Ki = 5 nM [4]
2-phenyl-9H-indeno[2,1-d]pyrimidine Drug Info IC50 = 16700 nM [15]
2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide Drug Info IC50 = 8000 nM [26]
3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin Drug Info IC50 = 2380 nM [18]
3,4-Benzo-7-acetonyloxy-8-methoxycoumarin Drug Info IC50 = 11930 nM [18]
3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 2580 nM [32]
3-aminoacetamido-4'-methylfuro[3,2-g]coumarin Drug Info IC50 = 12350 nM [9]
3-benzyl-N-(2-morpholinoethyl)quinoxalin-2-amine Drug Info IC50 = 1.3 nM [8]
3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 8180 nM [32]
3-methyl-2(1H)-thioxo-4(3H)-quinazolinone Drug Info IC50 = 3420 nM [22]
4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin Drug Info IC50 = 400 nM [18]
4,9-Dihydro-3H-beta-carboline Drug Info Ki = 7.3 nM [6]
4-(2-oxo-2H-chromene-3-carboxamido)benzoic acid Drug Info IC50 = 9970 nM [24]
4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one Drug Info IC50 = 4400 nM [26]
4-Chloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 750 nM [29]
4-Chloro-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 7500 nM [29]
4-methyl-2H-benzofuro[3,2-g]chromen-2-one Drug Info IC50 = 7240 nM [9]
4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one Drug Info IC50 = 40.5 nM [18]
5,6-Dichloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 84 nM [29]
5-Azidomethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 200 nM [2]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [5]
5-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 86 nM [5]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 300 nM [5]
5-Methoxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 4.9 nM [2]
6,11-dihydro-5H-benzo[a]carbazole Drug Info IC50 = 12000 nM [15]
6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one Drug Info IC50 = 12200 nM [18]
6-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 2785 nM [5]
6-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 790 nM [5]
6-Chloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 180 nM [29]
6-Chloro-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 380 nM [29]
6-Fluoro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 15000 nM [29]
6-Hydroxy-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 430 nM [29]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1640 nM [6]
6-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 480 nM [6]
7-(3-chlorobenzyloxy)-4-carboxaldehyde-coumarin Drug Info Ki = 11000 nM [16]
7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin Drug Info IC50 = 3.78 nM [18]
7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin Drug Info IC50 = 235 nM [18]
7-acetonyloxy-3-acetylamino-8-methoxycoumarin Drug Info IC50 = 6430 nM [9]
7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1290 nM [5]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 12 nM [4]
7-Methoxy-9H-beta-carboline Drug Info Ki = 87 nM [5]
8-(3-Bromobenzyloxy)caffeine Drug Info Ki = 23 nM [28]
8-(3-Chlorobenzyloxy)caffeine Drug Info Ki = 36 nM [28]
8-(3-Fluorobenzyloxy)caffeine Drug Info Ki = 180 nM [28]
8-(3-Methoxybenzyloxy)caffeine Drug Info Ki = 340 nM [28]
8-(3-Methylbenzyloxy)caffeine Drug Info Ki = 180 nM [28]
8-Benzyloxycaffeine Drug Info Ki = 590 nM [28]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 3.6 nM [5]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 17 nM [5]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 270 nM [5]
8-[(3-Trifluoromethyl)benzyloxy]caffeine Drug Info Ki = 51 nM [28]
9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [5]
Beta-methoxyamphetamine Drug Info Ki = 250 nM [23]
C-(1H-Indol-3-yl)-methylamine Drug Info Ki = 3440 nM [5]
CGS-19281A Drug Info Ki = 18 nM [6]
Cis-(+/-)-2-Fluoro-1,2-diphenylcyclopropylamine Drug Info IC50 = 18000 nM [17]
Ethyl 4-(2-oxo-2H-chromene-3-carboxamido)benzoate Drug Info IC50 = 15980 nM [24]
Harmine Drug Info Ki = 5 nM [27]
HYDRAZINECARBOXAMIDE Drug Info IC50 = 6700 nM [7]
IPRONIAZIDE Drug Info IC50 = 5000 nM [29]
MOFEGILINE Drug Info Ki = 1100 nM [20]
N'-(2-phenylallyl)hydrazine hydrochloride Drug Info IC50 = 1300 nM [10]
N-((1H-indol-2-yl)methyl)(phenyl)methanamine Drug Info Ki = 2100 nM [19]
N-(1-Methyl-1H-indol-2-ylmethyl)-N-phenylamine Drug Info Ki = 10 nM [19]
N-(1H-Indol-2-ylmethyl)-N-(4-phenylbutyl)amine Drug Info Ki = 10000 nM [19]
N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine Drug Info Ki = 10 nM [19]
N-(1H-Indol-2-ylmethyl)-N-phenylamine Drug Info Ki = 10000 nM [19]
N-(2-benzyl),N-(1-methylpyrrol-2-ylmethyl)amine Drug Info Ki = 24 nM [12]
N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide Drug Info Ki = 18290 nM [32]
N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 20 nM [12]
N-(3-Phenylpropyl)-1H-indole-2-carboxamide Drug Info Ki = 5 nM [19]
N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 15670 nM [24]
N-(4-Phenylbutyl)-1H-indole-2-carboxamide Drug Info Ki = 2200 nM [19]
N-(4-phenylbutyl)-1H-pyrrole-2-carboxamide Drug Info Ki = 55 nM [12]
N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 350 nM [12]
N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 300 nM [12]
N-2-phenylethyl-1H-pyrrole-2-carboxamide Drug Info Ki = 420 nM [12]
N-benzyl,N-methyl-1H-pyrrole-2-carboxamide Drug Info Ki = 600 nM [12]
N-Benzyl-(6-butoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 14500 nM [23]
N-Benzyl-(6-methoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 6930 nM [23]
N-benzyl-1H-pyrrole-2-carboxamide Drug Info Ki = 250 nM [12]
N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine Drug Info Ki = 60 nM [19]
N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 3500 nM [12]
N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 5.4 nM [12]
N-Methyl,N-phenyl-1H-indole-2-carboxamide Drug Info Ki = 3.5 nM [19]
N-methyl-N-(prop-2-ynyl)-1H-pyrrole-2-carboxamide Drug Info Ki = 75 nM [12]
N-Phenyl-1-methyl-1H-indole-2-carboxamide Drug Info Ki = 10000 nM [19]
N-Phenyl-1H-indole-2-carboxamide Drug Info Ki = 130 nM [19]
N-phenyl-1H-pyrrole-2-carboxamide Drug Info Ki = 400 nM [12]
N-propargyl-1H-pyrrole-2-carboxamide Drug Info Ki = 230 nM [12]
N2-[4-(benzyloxy)benzyl]glycinamide Drug Info IC50 = 8500 nM [14]
N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 13600 nM [14]
N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 12400 nM [14]
Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate Drug Info Ki = 12840 nM [21]
PIPERINE Drug Info Ki = 19000 nM [27]
PNU-22394 Drug Info Ki = 1030 nM [5]
TRACIZOLINE Drug Info Ki = 2 nM [4]
Trans-(+/-)-2-Fluoro-1,2-diphenylcyclopropylamine Drug Info IC50 = 10000 nM [17]
Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine Drug Info IC50 = 1600 nM [17]
Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine Drug Info IC50 = 3600 nM [17]
Trans-2-fluoro-2-p-tolylcyclopropanamine Drug Info IC50 = 13000 nM [17]
Trans-2-fluoro-2-phenylcyclopropylamin Drug Info IC50 = 12000 nM [17]
TRYPTAMINE Drug Info Ki = 5400 nM [5]
TRYPTOLINE Drug Info Ki = 9.4 nM [4]
References
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REF 18 Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors. J Med Chem. 2008 Nov 13;51(21):6740-51.
REF 19 Synthesis, structure-activity relationships and molecular modeling studies of new indole inhibitors of monoamine oxidases A and B. Bioorg Med Chem. 2008 Nov 15;16(22):9729-40.
REF 20 Structural and mechanistic studies of mofegiline inhibition of recombinant human monoamine oxidase B. J Med Chem. 2008 Dec 25;51(24):8019-26.
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REF 22 New pyrazoline bearing 4(3H)-quinazolinone inhibitors of monoamine oxidase: synthesis, biological evaluation, and structural determinants of MAO-A ... Bioorg Med Chem. 2009 Jan 15;17(2):675-89.
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