Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T83011 | ||||
Target Name | Monoamine oxidase type B (MAO-B) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Pargyline | Drug Info | Ki = 1800 nM | [8] | |
Rasagiline | Drug Info | Ki = 700 nM | [8] | ||
Tranylcypromine | Drug Info | Ki = 16 uM | |||
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholin-5-one | Drug Info | Ki = 74 nM | [31] | ||
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine | Drug Info | Ki = 130 nM | [31] | ||
(+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one | Drug Info | Ki = 160 nM | [31] | ||
(+/-)-2-(4'-Butoxyphenyl)thiomorpholine | Drug Info | Ki = 270 nM | [31] | ||
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one | Drug Info | Ki = 3400 nM | [31] | ||
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholine | Drug Info | Ki = 2170 nM | [31] | ||
(+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one | Drug Info | Ki = 13600 nM | [31] | ||
(+/-)-2-(4'-Methoxyphenyl)thiomorpholine | Drug Info | Ki = 3850 nM | [31] | ||
(+/-)-2-(4'-Propoxyphenyl)thiomorpholin-5-one | Drug Info | Ki = 1490 nM | [31] | ||
(+/-)-2-(4'-Propoxyphenyl)thiomorpholine | Drug Info | Ki = 980 nM | [31] | ||
(+/-)-2-(4-fluorophenyl)-7-methoxychroman-4-one | Drug Info | IC50 = 170 nM | [28] | ||
(+/-)-2-(4-fluorophenyl)-7-methylchroman-4-one | Drug Info | IC50 = 130 nM | [28] | ||
(+/-)-2-(4-fluorophenyl)chroman-4-one | Drug Info | IC50 = 4410 nM | [28] | ||
(+/-)-2-(4-methoxyphenyl)-7-methylchroman-4-one | Drug Info | IC50 = 3350 nM | [28] | ||
(+/-)-2-p-tolylchroman-4-one | Drug Info | IC50 = 2070 nM | [28] | ||
(+/-)-2-Phenylthiomorpholin-5-one | Drug Info | Ki = 9580 nM | [31] | ||
(+/-)-2-Phenylthiomorpholine | Drug Info | Ki = 2230 nM | [31] | ||
(+/-)-7-fluoro-2-(4-fluorophenyl)chroman-4-one | Drug Info | IC50 = 670 nM | [28] | ||
(+/-)-7-fluoro-2-(4-methoxyphenyl)chroman-4-one | Drug Info | IC50 = 170 nM | [28] | ||
(+/-)-7-fluoro-2-p-tolylchroman-4-one | Drug Info | IC50 = 160 nM | [28] | ||
(+/-)-7-fluoro-2-phenylchroman-4-one | Drug Info | IC50 = 3770 nM | [28] | ||
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one | Drug Info | IC50 = 7180 nM | [28] | ||
(+/-)-7-methoxy-2-p-tolylchroman-4-one | Drug Info | IC50 = 550 nM | [28] | ||
(+/-)-7-methoxy-2-phenylchroman-4-one | Drug Info | IC50 = 1470 nM | [28] | ||
(+/-)-7-methyl-2-p-tolylchroman-4-one | Drug Info | IC50 = 500 nM | [28] | ||
(+/-)-7-methyl-2-phenylchroman-4-one | Drug Info | IC50 = 3620 nM | [28] | ||
(6-Benzyloxy-2-naphthyl)-2-aminopropane | Drug Info | Ki = 2560 nM | [20] | ||
(6-Ethoxy-2-naphthyl)-2-aminopropane | Drug Info | Ki = 13600 nM | [20] | ||
(6-Methoxy-2-naphthyl)-2-aminopropane | Drug Info | Ki = 16300 nM | [20] | ||
(6-Propoxy-2-naphthyl)-2-aminopropane | Drug Info | Ki = 13500 nM | [20] | ||
(7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile | Drug Info | IC50 = 230 nM | [26] | ||
(E)-5-(3-Chlorostyryl)isatin | Drug Info | Ki = 1400 nM | [22] | ||
(E)-5-(3-Fluorostyryl)isatin | Drug Info | Ki = 600 nM | [22] | ||
(E)-5-Styrylisatin | Drug Info | Ki = 310 nM | [22] | ||
(E)-6-Styrylisatin | Drug Info | Ki = 560 nM | [22] | ||
(E)-8-(3-chlorostyryl)-caffeine | Drug Info | Ki = 100 nM | [25] | ||
(R)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one | Drug Info | IC50 = 200 nM | [28] | ||
(R)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one | Drug Info | IC50 = 150 nM | [28] | ||
(R)(+)-7-fluoro-2-p-tolylchroman-4-one | Drug Info | IC50 = 150 nM | [28] | ||
(R)(+)-7-fluoro-2-phenylchroman-4-one | Drug Info | IC50 = 650 nM | [28] | ||
(R)(+)-7-methyl-2-p-tolylchroman-4-one | Drug Info | IC50 = 530 nM | [28] | ||
(R)(+)-7-methyl-2-phenylchroman-4-one | Drug Info | IC50 = 140 nM | [28] | ||
(R)-3-Prop-2-ynylamino-indan-5-ol | Drug Info | Ki = 17000 nM | [8] | ||
(R)-Indan-1-yl-methyl-prop-2-ynyl-amine | Drug Info | Ki = 600 nM | [8] | ||
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide | Drug Info | IC50 = 800 nM | [11] | ||
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide | Drug Info | IC50 = 110 nM | [11] | ||
(R)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}alaninamide | Drug Info | IC50 = 450 nM | [11] | ||
(R/R)BEFLOXATONE | Drug Info | Ki = 220 nM | [1] | ||
(S)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one | Drug Info | IC50 = 160 nM | [28] | ||
(S)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one | Drug Info | IC50 = 170 nM | [28] | ||
(S)(+)-7-fluoro-2-p-tolylchroman-4-one | Drug Info | IC50 = 150 nM | [28] | ||
(S)(+)-7-fluoro-2-phenylchroman-4-one | Drug Info | IC50 = 620 nM | [28] | ||
(S)(+)-7-methyl-2-p-tolylchroman-4-one | Drug Info | IC50 = 590 nM | [28] | ||
(S)(+)-7-methyl-2-phenylchroman-4-one | Drug Info | IC50 = 110 nM | [28] | ||
(S)-2-amino-1-(4-butylthiophenyl)-propane | Drug Info | Ki = 8925 nM | [10] | ||
(S)-2-amino-1-(4-propylthiophenyl)-propane | Drug Info | Ki = 14030 nM | [10] | ||
(S)-N2-[4-(benzyloxy)benzyl]alaninamide | Drug Info | IC50 = 260 nM | [11] | ||
(S)-N2-[4-(benzyloxy)benzyl]serinamide | Drug Info | IC50 = 410 nM | [11] | ||
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide | Drug Info | IC50 = 33 nM | [11] | ||
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide | Drug Info | IC50 = 43 nM | [11] | ||
(S)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}serinamide | Drug Info | IC50 = 140 nM | [11] | ||
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}alaninamide | Drug Info | IC50 = 2200 nM | [11] | ||
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}serinamide | Drug Info | IC50 = 1100 nM | [11] | ||
(S)-N2-{4-[(4-nitrobenzyl)oxy]benzyl}serinamide | Drug Info | IC50 = 7010 nM | [11] | ||
1,2,3,4-Tetrahydro-naphthalen-1-ylamine | Drug Info | Ki = 720 nM | [36] | ||
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole | Drug Info | Ki = 6.5 nM | [6] | ||
1,4-diphenyl-(1E,3E)-1,3-butadiene | Drug Info | Ki = 600 nM | [8] | ||
1-(4-(benzyloxy)phenyl)propan-2-amine | Drug Info | Ki = 710 nM | [20] | ||
1H-Indole-2,3-dione | Drug Info | Ki = 3000 nM | [8] | ||
2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole | Drug Info | Ki = 4.7 nM | [5] | ||
2-(2,4-dichlorophenyl)-4,5-dihydro-1H-imidazole | Drug Info | Ki = 3980 nM | [18] | ||
2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole | Drug Info | IC50 = 27 nM | |||
2-(2-cyclohexylidenehydrazinyl)-4-p-tolylthiazole | Drug Info | IC50 = 3689 nM | |||
2-(2-cyclohexylidenehydrazinyl)-4-phenylthiazole | Drug Info | IC50 = 116 nM | |||
2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole | Drug Info | IC50 = 296 nM | |||
2-(3-nitrophenyl)-4,5-dihydro-1H-imidazole | Drug Info | Ki = 19270 nM | [18] | ||
2-(4,5-dihydro-1H-imidazol-2-yl)quinoline | Drug Info | IC50 = 13300 nM | [18] | ||
2-(4-chlorophenyl)-4,5-dihydro-1H-imidazole | Drug Info | Ki = 5350 nM | [18] | ||
2-(4-fluorophenyl)-7-methoxy-4H-chromen-4-one | Drug Info | IC50 = 5140 nM | [28] | ||
2-(4-methoxyphenyl)-4H-chromene-4-thione | Drug Info | IC50 = 480 nM | [28] | ||
2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole | Drug Info | Ki = 1490 nM | [18] | ||
2-BFi | Drug Info | IC50 = 9100 nM | [18] | ||
2-Bromo-N-(2-morpholinoethyl)nicotinamide | Drug Info | IC50 = 320 nM | [30] | ||
2-Bromo-N-(3-morpholinopropyl)nicotinamide | Drug Info | IC50 = 1900 nM | [30] | ||
2-Chloro-N-(2-morpholinoethyl)nicotinamide | Drug Info | IC50 = 1800 nM | [30] | ||
2-Chloro-N-(3-morpholinopropyl)nicotinamide | Drug Info | IC50 = 6500 nM | [30] | ||
2-Furan-2-yl-4,5-dihydro-1H-imidazole | Drug Info | Ki = 2340 nM | [4] | ||
2-Hydrazino-3-methyl-4(3H)-quinazolinone | Drug Info | Ki = 18580 nM | [19] | ||
2-methyl-9H-indeno[2,1-d]pyrimidin-9-one | Drug Info | IC50 = 9400 nM | [12] | ||
2-oxo-N-m-tolyl-2H-chromene-3-carboxamide | Drug Info | IC50 = 600 nM | [21] | ||
2-oxo-N-p-tolyl-2H-chromene-3-carboxamide | Drug Info | IC50 = 710 nM | [21] | ||
2-oxo-N-phenyl-2H-chromene-3-carboxamide | Drug Info | IC50 = 760 nM | [21] | ||
2-p-tolyl-4,5-dihydro-1H-imidazole | Drug Info | Ki = 13090 nM | [18] | ||
2-p-tolyl-4H-chromen-4-one | Drug Info | IC50 = 2380 nM | [28] | ||
2-p-tolyl-4H-chromene-4-thione | Drug Info | IC50 = 6690 nM | [28] | ||
2-Phenethyl-4,5-dihydro-1H-imidazole | Drug Info | Ki = 5 nM | [4] | ||
2-Phenoxymethyl-4,5-dihydro-1H-imidazole | Drug Info | Ki = 5 nM | [4] | ||
2-phenyl-9H-indeno[2,1-d]pyrimidine | Drug Info | IC50 = 13000 nM | [12] | ||
2-Phenyl-cyclopropylamine hydrochloride | Drug Info | IC50 = 19000 nM | [7] | ||
2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide | Drug Info | IC50 = 200 nM | [26] | ||
3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin | Drug Info | IC50 = 1.49 nM | [15] | ||
3,4-Benzo-7-acetonyloxy-8-methoxycoumarin | Drug Info | IC50 = 9360 nM | [15] | ||
3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide | Drug Info | Ki = 30 nM | [35] | ||
3-(2-Bromophenyl)-6-methylcoumarin | Drug Info | IC50 = 4300 nM | [34] | ||
3-(3-methoxyphenyl)-6-methyl-2H-chromen-2-one | Drug Info | IC50 = 0.8026 nM | [24] | ||
3-(4-hydroxyphenyl)-6-methyl-2H-chromen-2-one | Drug Info | IC50 = 155.59 nM | [24] | ||
3-(4-methoxyphenyl)-6-methyl-2H-chromen-2-one | Drug Info | IC50 = 13.05 nM | [24] | ||
3-(phenoxymethyl)-5H-indeno[1,2-c]pyridazin-5-one | Drug Info | IC50 = 2510 nM | [12] | ||
3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide | Drug Info | Ki = 330 nM | [35] | ||
3-phenyl-9H-indeno[1,2-e][1,2,4]triazin-9-one | Drug Info | IC50 = 6310 nM | [12] | ||
4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin | Drug Info | IC50 = 3870 nM | [15] | ||
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 = 1140 nM | [21] | ||
4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one | Drug Info | IC50 = 21 nM | [26] | ||
4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one | Drug Info | IC50 = 5570 nM | [15] | ||
4-oxo-4H-chromene-3-carboxylic acid | Drug Info | IC50 = 48 nM | [32] | ||
5-Aminomethyl-3-pyrrol-1-yl-oxazolidin-2-one | Drug Info | Ki = 4400 nM | [1] | ||
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-Hydroxymethyl-3-pyrrol-1-yl-oxazolidin-2-one | Drug Info | Ki = 2000 nM | [1] | ||
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | Ki = 300 nM | [5] | ||
5-Methoxy-4,9-dihydro-3H-beta-carboline | Drug Info | Ki = 84 nM | [5] | ||
5-QUINOXALIN-6-YLMETHYLENE-THIAZOLIDINE-2,4-DIONE | Drug Info | IC50 = 13000 nM | [33] | ||
6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one | Drug Info | IC50 = 16530 nM | [15] | ||
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-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 = 400 nM | [13] | ||
7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin | Drug Info | IC50 = 17300 nM | [15] | ||
7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin | Drug Info | IC50 = 165 nM | [15] | ||
7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | Ki = 1290 nM | [5] | ||
7-Bromo-4,9-dihydro-3H-beta-carboline | Drug Info | Ki = 400 nM | [5] | ||
7-fluoro-2-(4-fluorophenyl)-4H-chromene-4-thione | Drug Info | IC50 = 6890 nM | [28] | ||
7-fluoro-2-(4-methoxyphenyl)-4H-chromen-4-one | Drug Info | IC50 = 1340 nM | [28] | ||
7-fluoro-2-p-tolyl-4H-chromen-4-one | Drug Info | IC50 = 4330 nM | [28] | ||
7-fluoro-2-p-tolyl-4H-chromene-4-thione | Drug Info | IC50 = 1610 nM | [28] | ||
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | Ki = 12 nM | [4] | ||
7-methoxy-2-p-tolyl-4H-chromen-4-one | Drug Info | IC50 = 11340 nM | [28] | ||
7-methoxy-2-p-tolyl-4H-chromene-4-thione | Drug Info | IC50 = 7610 nM | [28] | ||
7-Methoxy-9H-beta-carboline | Drug Info | Ki = 87 nM | [5] | ||
7-methyl-2-p-tolyl-4H-chromene-4-thione | Drug Info | IC50 = 6720 nM | [28] | ||
8-(3-Bromobenzyloxy)caffeine | Drug Info | Ki = 330 nM | [29] | ||
8-(3-Chlorobenzyloxy)caffeine | Drug Info | Ki = 230 nM | [29] | ||
8-(3-Fluorobenzyloxy)caffeine | Drug Info | Ki = 370 nM | [29] | ||
8-(3-Methoxybenzyloxy)caffeine | Drug Info | Ki = 1100 nM | [29] | ||
8-(3-Methylbenzyloxy)caffeine | Drug Info | Ki = 140 nM | [29] | ||
8-Benzyloxycaffeine | Drug Info | Ki = 430 nM | [29] | ||
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-Bromo-6-methyl-3-(4'-methoxyphenyl)coumarin | Drug Info | IC50 = 3230 nM | [34] | ||
8-Bromo-6-methyl-3-phenylcoumarin | Drug Info | IC50 = 11050 nM | [34] | ||
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | Ki = 270 nM | [5] | ||
8-Methoxy-4,9-dihydro-3H-beta-carboline | Drug Info | Ki = 160 nM | [5] | ||
8-[(3-Trifluoromethyl)benzyloxy]caffeine | Drug Info | Ki = 1300 nM | [29] | ||
9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline | Drug Info | Ki = 5.4 nM | [5] | ||
Benzyl-methyl-[1-(1H-pyrrol-2-yl)-vinyl]-amine | Drug Info | Ki = 20 nM | [2] | ||
Butyl-methyl-prop-2-ynyl-amine hydrochloride | Drug Info | IC50 = 1400 nM | [3] | ||
C-(1H-Indol-3-yl)-methylamine | Drug Info | Ki = 3440 nM | [5] | ||
CGS-19281A | Drug Info | Ki = 18 nM | [6] | ||
CHALCONE | Drug Info | IC50 = 1410 nM | [23] | ||
Cis-2-(4-chlorophenyl)-2-fluorocyclopropanamine | Drug Info | IC50 = 4800 nM | [14] | ||
Cis-2-(para-fluorophenyl)cyclopropylamine | Drug Info | IC50 = 10000 nM | [14] | ||
Cis-2-Fluoro-2-(4-methoxyphenyl)cyclopropylamine | Drug Info | IC50 = 18000 nM | [14] | ||
Cis-2-fluoro-2-phenylcyclopropanamine | Drug Info | IC50 = 19000 nM | [14] | ||
Cis-2-phenylcyclopropylamine | Drug Info | IC50 = 19000 nM | [14] | ||
CORDOIN | Drug Info | IC50 = 18760 nM | [23] | ||
Flavanone | Drug Info | IC50 = 2870 nM | [28] | ||
Heptyl-methyl-prop-2-ynyl-amine hydrochloride | Drug Info | IC50 = 2000 nM | [3] | ||
HYDRAZINECARBOXAMIDE | Drug Info | IC50 = 6700 nM | [7] | ||
IPRONIAZIDE | Drug Info | IC50 = 7500 nM | [30] | ||
Isopropyl-methyl-prop-2-ynyl-amine hydrochloride | Drug Info | IC50 = 19000 nM | [3] | ||
L-136662 | Drug Info | IC50 = 195 nM | [33] | ||
Lazabemide | Drug Info | Ki = 84 nM | [8] | ||
Methyl piperate | Drug Info | Ki = 1600 nM | [27] | ||
Methyl-(1,2,3,4-tetrahydro-naphthalen-1-yl)-amine | Drug Info | Ki = 1400 nM | [36] | ||
Methyl-pentyl-prop-2-ynyl-amine oxalic acid | Drug Info | IC50 = 370 nM | [3] | ||
MOFEGILINE | Drug Info | IC50 = 3.6 nM | [17] | ||
N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine | Drug Info | Ki = 1000 nM | [16] | ||
N-(1H-Indol-2-ylmethyl)-N-phenylamine | Drug Info | Ki = 320 nM | [16] | ||
N-(2-aminoethyl)-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 7680 nM | [21] | ||
N-(2-Methyl-1H-indol-5-yl)benzamide | Drug Info | Ki = 1650 nM | [35] | ||
N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide | Drug Info | Ki = 3000 nM | [35] | ||
N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine | Drug Info | Ki = 700 nM | [9] | ||
N-(2-Phenylethyl)-1H-indole-2-carboxamide | Drug Info | Ki = 190 nM | [16] | ||
N-(3-Phenylpropyl)-1H-indole-2-carboxamide | Drug Info | Ki = 800 nM | [16] | ||
N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 890 nM | [21] | ||
N-(4-Phenylbutyl)-1H-indole-2-carboxamide | Drug Info | Ki = 10000 nM | [16] | ||
N-(benzyl),N-(pyrrol-2-ylmethyl)amine | Drug Info | Ki = 7200 nM | [9] | ||
N-(propargyl),N-(pyrrol-2-ylmethyl)amine | Drug Info | Ki = 620 nM | [9] | ||
N-Benzyl,N-methyl-1H-indole-2-carboxamide | Drug Info | Ki = 1600 nM | [16] | ||
N-Benzyl-1H-indole-2-carboxamide | Drug Info | Ki = 120 nM | [16] | ||
N-benzyl-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 1960 nM | [21] | ||
N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine | Drug Info | Ki = 700 nM | [16] | ||
N-cyclohexyl-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 500 nM | [21] | ||
N-isobutyl-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 3270 nM | [21] | ||
N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine | Drug Info | Ki = 20 nM | [9] | ||
N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine | Drug Info | Ki = 20 nM | [9] | ||
N-Methyl,N-phenyl-1H-indole-2-carboxamide | Drug Info | Ki = 94 nM | [16] | ||
N-Methyl-N-phenyl-2-oxo-2H-chromene-3-carboxamide | Drug Info | IC50 = 8890 nM | [21] | ||
N-Phenyl-1H-indole-2-carboxamide | Drug Info | Ki = 230 nM | [16] | ||
N2-[4-(benzyloxy)benzyl]glycinamide | Drug Info | IC50 = 3150 nM | [11] | ||
N2-{4-[(3-chlorobenzyl)oxy]benzyl}glycinamide | Drug Info | IC50 = 340 nM | [11] | ||
N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide | Drug Info | IC50 = 2240 nM | [11] | ||
N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide | Drug Info | IC50 = 7100 nM | [11] | ||
N2-{4-[(4-nitrobenzyl)oxy]benzyl}glycinamide | Drug Info | IC50 = 9100 nM | [11] | ||
NSC-50187 | Drug Info | IC50 = 2200 nM | [28] | ||
NSC-93405 | Drug Info | IC50 = 12940 nM | [28] | ||
Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate | Drug Info | Ki = 1380 nM | [18] | ||
PIPERINE | Drug Info | Ki = 3190 nM | [27] | ||
PNU-22394 | Drug Info | Ki = 1030 nM | [5] | ||
TOLOXATONE | Drug Info | Ki = 15000 nM | [1] | ||
TRACIZOLINE | Drug Info | Ki = 2 nM | [4] | ||
Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine | Drug Info | IC50 = 3700 nM | [14] | ||
Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine | Drug Info | IC50 = 4900 nM | [14] | ||
Trans-2-fluoro-2-p-tolylcyclopropanamine | Drug Info | IC50 = 13000 nM | [14] | ||
Trans-2-fluoro-2-phenylcyclopropylamin | Drug Info | IC50 = 6400 nM | [14] | ||
TRYPTAMINE | Drug Info | Ki = 5400 nM | [5] | ||
TRYPTOLINE | Drug Info | Ki = 9.4 nM | [4] | ||
Action against Disease Model | Phenelzine | Drug Info | In ongoing studies of the neuroprotective properties of monoamine oxidase inhibitors, we found that phenelzine provided robust neuroprotection in the gerbil model of transient forebrain ischemia, with drug administration delayed up to 3 h post reperfusion. Since ischemia-reperfusion brain injury is associated with large increases in the concentrations of reactive aldehydes in the pen uMbra area, we investigated if the hydrazine function of phenelzine was capable of sequestering reactive aldehydes. Both aminoaldehydes and acrolein are generated from the metabolism of polyamines to putrescine by polyamine oxidase. These toxic aldehydes in turn compromise mitochondrial and lysosomal integrity and initiate apoptosis and necrosis. Previous studies have demonstrated that pharmacological neutralization of reactive aldehydes via the formation of thioacetal derivatives results in significant neuroprotection in ischemia-reperfusion injury, in both focal and global ischemiamodels. In our studies of acrolein and 3-aminopropanal toxicity, using an immortalized retinal cell line, we found that aldehyde sequestration with phenelzine was neuroprotective. The neuroprotectionobserved with phenelzine is in agreement with previous studies of aldehyde sequestering agents in the treatment of ischemia-reperfusion brain injury and supports the concept that "aldehyde load" is amajor factor in the delayed cell losses of the ischemic pen uMbra. | [37] | |
Rasagiline | Drug Info | It has demonstrated neuroprotective properties in laboratory studies. Current concepts of PD aetiopathogenesis include the role of alpha-synuclein, protein aggregation, free radical metabolism and mitochondrial dysfunction in contributing to cell death. We have used a combination of alpha-synuclein and free radical mediated toxicity in a dopaminergic cell line to provide a model of nigral toxicity in order to investigate the potential molecular mechanisms that mediate rasagiline protection. We demonstrate that rasagiline protects against cell death induced by the combination of free radicals generated by paraquat and either wild-type or A53T mutant alpha-synuclein over-expression. This protection was associated with a reduction in caspase 3 activation, a reduction insuperoxide generation and a trend to ameliorate the fall in mitochondrial membrane potential. Rasagiline induced an increase in cellular glutathione levels. The results support a role for rasagiline in protecting dopaminergic cells against free radical mediated damage and apoptosis in the presence of alpha-synuclein over-expression. The data are of relevance to the interpretation of the potentialmechanisms of action of rasagiline in explaining the results of disease modification trials in PD. | [38] | ||
Tranylcypromine | Drug Info | Glioblastoma multiforme (GBM) is a particularly aggressive brain t uMor and remains a clinically devastating disease. Pharmacologically inhibiting the lysine specific demethylase 1 with the monoamine oxidase inhibitor tranylcypromine, in combination with HDAC inhibitors, led to synergistic apoptotic cell death in GBM cells | [39] | ||
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