Target Validation Information
Target ID T83011
Target Name Amine oxidase [flavin-containing] B
Target Type
Successful
Drug Potency against Target 2-(2-cyclohexylidenehydrazinyl)-4-p-tolylthiazole Drug Info IC50 = 3689 nM
N-(2-Methyl-1H-indol-5-yl)cyclohexanecarboxamide Drug Info Ki = 3000 nM [531067]
3,4-Dichloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 30 nM [531067]
2-(4,5-dihydro-1H-imidazol-2-yl)quinoline Drug Info IC50 = 13300 nM [529853]
(+/-)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 160 nM [530614]
7-methoxy-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 7610 nM [530614]
7-fluoro-2-(4-fluorophenyl)-4H-chromene-4-thione Drug Info IC50 = 6890 nM [530614]
(R)-Indan-1-yl-methyl-prop-2-ynyl-amine Drug Info Ki = 600 nM [527719]
(E)-5-(3-Chlorostyryl)isatin Drug Info Ki = 1400 nM [530056]
(S)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 170 nM [530614]
7-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1290 nM [526993]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholine Drug Info Ki = 3850 nM [530683]
(S)(+)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 590 nM [530614]
8-Benzyloxycaffeine Drug Info Ki = 430 nM [530647]
8-[(3-Trifluoromethyl)benzyloxy]caffeine Drug Info Ki = 1300 nM [530647]
8-(3-Methoxybenzyloxy)caffeine Drug Info Ki = 1100 nM [530647]
6-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 480 nM [526994]
N-(2-Methyl-1H-indol-5-yl)benzamide Drug Info Ki = 1650 nM [531067]
N-Benzyl,N-methyl-1H-indole-2-carboxamide Drug Info Ki = 1600 nM [529768]
LAZEBEMIDE Drug Info Ki = 84 nM [527719]
1H-Indole-2,3-dione Drug Info Ki = 3000 nM [527719]
7-(3-chlorobenzyloxy)-4-carboxaldehyde-coumarin Drug Info Ki = 400 nM [529080]
(+/-)-2-(4-fluorophenyl)-7-methylchroman-4-one Drug Info IC50 = 130 nM [530614]
2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 6690 nM [530614]
(S)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 160 nM [530614]
(+/-)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 170 nM [530614]
1-(4-(benzyloxy)phenyl)propan-2-amine Drug Info Ki = 710 nM [529986]
(+/-)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 670 nM [530614]
(+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 7180 nM [530614]
5-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 300 nM [526993]
NSC-50393 Drug Info IC50 = 2870 nM [530614]
(+/-)-7-methoxy-2-p-tolylchroman-4-one Drug Info IC50 = 550 nM [530614]
(S)(+)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 150 nM [530614]
8-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 3.6 nM [526993]
C-(1H-Indol-3-yl)-methylamine Drug Info Ki = 3440 nM [526993]
7-fluoro-2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 4330 nM [530614]
(6-Benzyloxy-2-naphthyl)-2-aminopropane Drug Info Ki = 2560 nM [529986]
Trans-2-(4-chlorophenyl)-2-fluorocyclopropanamine Drug Info IC50 = 3700 nM [529607]
2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 2380 nM [530614]
N2-{4-[(3-chlorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 340 nM [529025]
Cis-2-fluoro-2-phenylcyclopropanamine Drug Info IC50 = 19000 nM [529607]
2-(4-methoxyphenyl)-4H-chromene-4-thione Drug Info IC50 = 480 nM [530614]
7-fluoro-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 1610 nM [530614]
(+/-)-7-fluoro-2-(4-methoxyphenyl)chroman-4-one Drug Info IC50 = 170 nM [530614]
2-(4-fluorophenyl)-7-methoxy-4H-chromen-4-one Drug Info IC50 = 5140 nM [530614]
Pargyline Drug Info Ki = 1800 nM [527719]
(S)-N2-[4-(benzyloxy)benzyl]serinamide Drug Info IC50 = 410 nM [529025]
CGS-19281A Drug Info Ki = 18 nM [526994]
(+/-)-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 4410 nM [530614]
NSC-50187 Drug Info IC50 = 2200 nM [530614]
2-Furan-2-yl-4,5-dihydro-1H-imidazole Drug Info Ki = 2340 nM [526918]
(+/-)-2-Phenylthiomorpholin-5-one Drug Info Ki = 9580 nM [530683]
Cis-2-(para-fluorophenyl)cyclopropylamine Drug Info IC50 = 10000 nM [529607]
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholin-5-one Drug Info Ki = 74 nM [530683]
(R)(+)-7-fluoro-2-p-tolylchroman-4-one Drug Info IC50 = 150 nM [530614]
(R)(+)-2-(4-fluorophenyl)-7-methoxychroman-4-one Drug Info IC50 = 200 nM [530614]
2-phenyl-9H-indeno[2,1-d]pyrimidine Drug Info IC50 = 13000 nM [529077]
5-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 84 nM [526993]
N-(3-Phenylpropyl)-1H-indole-2-carboxamide Drug Info Ki = 800 nM [529768]
2-(2,4-dichlorophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 3980 nM [529853]
N-Methyl,N-phenyl-1H-indole-2-carboxamide Drug Info Ki = 94 nM [529768]
2-Bromo-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 320 nM [530675]
N-Methyl-N-phenyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 8890 nM [530001]
2-Chloro-N-(2-morpholinoethyl)nicotinamide Drug Info IC50 = 1800 nM [530675]
2-BFi Drug Info IC50 = 9100 nM [529853]
(+/-)-2-(4'-Benzyloxyphenyl)thiomorpholine Drug Info Ki = 130 nM [530683]
(S)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 140 nM [529025]
(R/R)BEFLOXATONE Drug Info Ki = 220 nM [526287]
2-p-tolyl-4,5-dihydro-1H-imidazole Drug Info Ki = 13090 nM [529853]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholine Drug Info Ki = 270 nM [530683]
(R)(+)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 650 nM [530614]
Heptyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 2000 nM [526820]
4-methyl-7-(2-oxocyclopentyloxy)-2H-chromen-2-one Drug Info IC50 = 5570 nM [529735]
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 1100 nM [529025]
(S)(+)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 110 nM [530614]
5-Aminomethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 4400 nM [526287]
N-(4-Phenylbutyl)-1H-indole-2-carboxamide Drug Info Ki = 10000 nM [529768]
6-amino-9-methoxy-7H-furo[3,2-g]chromen-7-one Drug Info IC50 = 16530 nM [529735]
7-Methoxy-9H-beta-carboline Drug Info Ki = 87 nM [526993]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info IC50 = 1470 nM [530614]
(+/-)-2-p-tolylchroman-4-one Drug Info IC50 = 2070 nM [530614]
NSC-93405 Drug Info IC50 = 12940 nM [530614]
7-methyl-2-p-tolyl-4H-chromene-4-thione Drug Info IC50 = 6720 nM [530614]
N-benzyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 1960 nM [530001]
(R)(+)-7-fluoro-2-(4-fluorophenyl)chroman-4-one Drug Info IC50 = 150 nM [530614]
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 110 nM [529025]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholin-5-one Drug Info Ki = 3400 nM [530683]
(R)(+)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 140 nM [530614]
Trans-2-fluoro-2-phenylcyclopropylamin Drug Info IC50 = 6400 nM [529607]
(R)(+)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 530 nM [530614]
7-methoxy-2-p-tolyl-4H-chromen-4-one Drug Info IC50 = 11340 nM [530614]
(+/-)-2-(4-methoxyphenyl)-7-methylchroman-4-one Drug Info IC50 = 3350 nM [530614]
(7-Benzyloxy-2-oxo-2H-chromen-4-yl)acetonitrile Drug Info IC50 = 230 nM [530434]
N2-[4-(benzyloxy)benzyl]glycinamide Drug Info IC50 = 3150 nM [529025]
(+/-)-7-methyl-2-phenylchroman-4-one Drug Info IC50 = 3620 nM [530614]
(+/-)-7-methyl-2-p-tolylchroman-4-one Drug Info IC50 = 500 nM [530614]
N2-{4-[(4-nitrobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 9100 nM [529025]
(S)-N2-{4-[(4-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 2200 nM [529025]
N2-{4-[(3-fluorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 2240 nM [529025]
N-cyclohexyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 500 nM [530001]
3,4-Benzo-7-acetonyloxy-8-methoxycoumarin Drug Info IC50 = 9360 nM [529735]
(S)-N2-{4-[(4-nitrobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 7010 nM [529025]
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}serinamide Drug Info IC50 = 43 nM [529025]
3-(3-methoxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 0.8026 nM [530273]
3-(4-hydroxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 155.59 nM [530273]
3-(4-methoxyphenyl)-6-methyl-2H-chromen-2-one Drug Info IC50 = 13.05 nM [530273]
(+/-)-2-(4'-Methoxyphenyl)thiomorpholin-5-one Drug Info Ki = 13600 nM [530683]
Isopropyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 19000 nM [526820]
Methyl-pentyl-prop-2-ynyl-amine oxalic acid Drug Info IC50 = 370 nM [526820]
Butyl-methyl-prop-2-ynyl-amine hydrochloride Drug Info IC50 = 1400 nM [526820]
(S)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 33 nM [529025]
2-(2-cyclopentylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 296 nM
(S)-N2-[4-(benzyloxy)benzyl]alaninamide Drug Info IC50 = 260 nM [529025]
2-oxo-N-phenyl-2H-chromene-3-carboxamide Drug Info IC50 = 760 nM [530001]
N-(4-Ethylphenyl)-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 890 nM [530001]
N-isobutyl-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 3270 nM [530001]
7-fluoro-2-(4-methoxyphenyl)-4H-chromen-4-one Drug Info IC50 = 1340 nM [530614]
3-(2-Bromophenyl)-6-methylcoumarin Drug Info IC50 = 4300 nM [531055]
8-(3-Fluorobenzyloxy)caffeine Drug Info Ki = 370 nM [530647]
1,4-diphenyl-(1E,3E)-1,3-butadiene Drug Info Ki = 600 nM [527719]
CHALCONE Drug Info IC50 = 1410 nM [530087]
N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 620 nM [528641]
N-(1H-Indol-2-ylmethyl)-N-methyl-N-phenylamine Drug Info Ki = 1000 nM [529768]
2-Hydrazino-3-methyl-4(3H)-quinazolinone Drug Info Ki = 18580 nM [529873]
Methyl-(1,2,3,4-tetrahydro-naphthalen-1-yl)-amine Drug Info Ki = 1400 nM [533451]
8-Bromo-6-methyl-3-(4'-methoxyphenyl)coumarin Drug Info IC50 = 3230 nM [531055]
AS-605240 Drug Info IC50 = 13000 nM [531046]
4-(Aminomethyl)-7-(benzyloxy)-2H-chromen-2-one Drug Info IC50 = 21 nM [530434]
(E)-8-(3-chlorostyryl)-caffeine Drug Info Ki = 100 nM [530425]
(S)-2-amino-1-(4-butylthiophenyl)-propane Drug Info Ki = 8925 nM [528855]
(S)-2-amino-1-(4-propylthiophenyl)-propane Drug Info Ki = 14030 nM [528855]
TOLOXATONE Drug Info Ki = 15000 nM [526287]
5-Hydroxymethyl-3-pyrrol-1-yl-oxazolidin-2-one Drug Info Ki = 2000 nM [526287]
3-phenyl-9H-indeno[1,2-e][1,2,4]triazin-9-one Drug Info IC50 = 6310 nM [529077]
8-(3-Bromobenzyloxy)caffeine Drug Info Ki = 330 nM [530647]
2-(4-chlorophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 5350 nM [529853]
2-(3-nitrophenyl)-4,5-dihydro-1H-imidazole Drug Info Ki = 19270 nM [529853]
2-[7-(Benzyloxy)-2-oxo-2H-chromen-4-yl]acetamide Drug Info IC50 = 200 nM [530434]
2-Phenoxymethyl-4,5-dihydro-1H-imidazole Drug Info Ki = 5 nM [526918]
2-(2-cyclohexylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 116 nM
(E)-5-Styrylisatin Drug Info Ki = 310 nM [530056]
Tranylcypromine Drug Info Ki = 16 uM
(R)-3-Prop-2-ynylamino-indan-5-ol Drug Info Ki = 17000 nM [527719]
3-(phenoxymethyl)-5H-indeno[1,2-c]pyridazin-5-one Drug Info IC50 = 2510 nM [529077]
Rasagiline Drug Info Ki = 700 nM [527719]
TRACIZOLINE Drug Info Ki = 2 nM [526918]
TRYPTOLINE Drug Info Ki = 9.4 nM [526918]
6-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 1640 nM [526994]
8-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 270 nM [526993]
9-Methyl-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [526993]
2-Bromo-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 1900 nM [530675]
2-Phenyl-cyclopropylamine hydrochloride Drug Info IC50 = 19000 nM [527283]
(+/-)-2-(4'-Ethoxyphenyl)thiomorpholine Drug Info Ki = 2170 nM [530683]
Trans-2-fluoro-2-p-tolylcyclopropanamine Drug Info IC50 = 13000 nM [529607]
(E)-6-Styrylisatin Drug Info Ki = 560 nM [530056]
8-(3-Chlorobenzyloxy)caffeine Drug Info Ki = 230 nM [530647]
8-(3-Methylbenzyloxy)caffeine Drug Info Ki = 140 nM [530647]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info Ki = 6.5 nM [526994]
PNU-22394 Drug Info Ki = 1030 nM [526993]
(6-Methoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 16300 nM [529986]
N-Benzyl-N-(1H-indol-2-ylmethyl)-N-methylamine Drug Info Ki = 700 nM [529768]
N-Benzyl-1H-indole-2-carboxamide Drug Info Ki = 120 nM [529768]
(+/-)-2-(4'-Propoxyphenyl)thiomorpholin-5-one Drug Info Ki = 1490 nM [530683]
N2-{4-[(4-chlorobenzyl)oxy]benzyl}glycinamide Drug Info IC50 = 7100 nM [529025]
2-methyl-9H-indeno[2,1-d]pyrimidin-9-one Drug Info IC50 = 9400 nM [529077]
N-methyl,N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 20 nM [528641]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 12 nM [526918]
(6-Ethoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 13600 nM [529986]
8-Methoxy-4,9-dihydro-3H-beta-carboline Drug Info Ki = 160 nM [526993]
8-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 17 nM [526993]
5-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 5.4 nM [526993]
Cis-2-(4-chlorophenyl)-2-fluorocyclopropanamine Drug Info IC50 = 4800 nM [529607]
(+/-)-2-(4'-Butoxyphenyl)thiomorpholin-5-one Drug Info Ki = 160 nM [530683]
5-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 86 nM [526993]
4,9-Dihydro-3H-beta-carboline Drug Info Ki = 7.3 nM [526994]
2-oxo-N-p-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 710 nM [530001]
(+/-)-2-(4'-Propoxyphenyl)thiomorpholine Drug Info Ki = 980 nM [530683]
Phenyl 4-(4,5-dihydro-1H-imidazol-2-yl)benzoate Drug Info Ki = 1380 nM [529853]
6-Bromo-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info Ki = 2785 nM [526993]
N-(2-aminoethyl)-2-oxo-2H-chromene-3-carboxamide Drug Info IC50 = 7680 nM [530001]
3,4-Benzo-7-(beta-bromoallyloxy)-8-methylcoumarin Drug Info IC50 = 1.49 nM [529735]
N-Phenyl-1H-indole-2-carboxamide Drug Info Ki = 230 nM [529768]
N-(2-phenylethyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 700 nM [528641]
2-Chloro-N-(3-morpholinopropyl)nicotinamide Drug Info IC50 = 6500 nM [530675]
IPRONIAZIDE Drug Info IC50 = 7500 nM [530675]
(+/-)-2-Phenylthiomorpholine Drug Info Ki = 2230 nM [530683]
N-(2-Phenylethyl)-1H-indole-2-carboxamide Drug Info Ki = 190 nM [529768]
7-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 400 nM [526993]
2-(naphthalen-2-yl)-4,5-dihydro-1H-imidazole Drug Info Ki = 1490 nM [529853]
TRYPTAMINE Drug Info Ki = 5400 nM [526993]
(R)-N2-{4-[(3-chlorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 800 nM [529025]
7-Acetonyloxy-3,4-cyclopentene-8-methylcoumarin Drug Info IC50 = 165 nM [529735]
N-(1H-Indol-2-ylmethyl)-N-phenylamine Drug Info Ki = 320 nM [529768]
6-Bromo-4,9-dihydro-3H-beta-carboline Drug Info Ki = 790 nM [526993]
7-Acetonyloxy-3,4-cyclohexene-8-methylcoumarin Drug Info IC50 = 17300 nM [529735]
(6-Propoxy-2-naphthyl)-2-aminopropane Drug Info Ki = 13500 nM [529986]
N-(benzyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 7200 nM [528641]
2-oxo-N-m-tolyl-2H-chromene-3-carboxamide Drug Info IC50 = 600 nM [530001]
3-Chloro-N-(2-methyl-1H-indol-5-yl)benzamide Drug Info Ki = 330 nM [531067]
4-(2-oxo-2H-chromene-3-carboxamido)benzoic acid Drug Info IC50 = 1140 nM [530001]
Cis-2-Fluoro-2-(4-methoxyphenyl)cyclopropylamine Drug Info IC50 = 18000 nM [529607]
Cis-2-phenylcyclopropylamine Drug Info IC50 = 19000 nM [529607]
2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indole Drug Info Ki = 4.7 nM [526993]
(+/-)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 3770 nM [530614]
PIPERINE Drug Info Ki = 3190 nM [530562]
1,2,3,4-Tetrahydro-naphthalen-1-ylamine Drug Info Ki = 720 nM [533451]
(R)-N2-{4-[(3-fluorobenzyl)oxy]benzyl}alaninamide Drug Info IC50 = 450 nM [529025]
Trans-2-fluoro-2-(4-fluorophenyl)cyclopropanamine Drug Info IC50 = 4900 nM [529607]
4,8-Dimethyl-7-(2'-oxocyclohexyloxy)coumarin Drug Info IC50 = 3870 nM [529735]
2-(2-cycloheptylidenehydrazinyl)-4-phenylthiazole Drug Info IC50 = 27 nM
4-oxo-4H-chromene-3-carboxylic acid Drug Info IC50 = 48 nM [530841]
CORDOIN Drug Info IC50 = 18760 nM [530087]
L-136662 Drug Info IC50 = 195 nM [531046]
MOFEGILINE Drug Info IC50 = 3.6 nM [529842]
2-Phenethyl-4,5-dihydro-1H-imidazole Drug Info Ki = 5 nM [526918]
HYDRAZINECARBOXAMIDE Drug Info IC50 = 6700 nM [527283]
(S)(+)-7-fluoro-2-phenylchroman-4-one Drug Info IC50 = 620 nM [530614]
8-Bromo-6-methyl-3-phenylcoumarin Drug Info IC50 = 11050 nM [531055]
N-methyl,N-(propargyl),N-(pyrrol-2-ylmethyl)amine Drug Info Ki = 20 nM [528641]
Methyl piperate Drug Info Ki = 1600 nM [530562]
(E)-5-(3-Fluorostyryl)isatin Drug Info Ki = 600 nM [530056]
Benzyl-methyl-[1-(1H-pyrrol-2-yl)-vinyl]-amine Drug Info Ki = 20 nM [526566]
Action against Disease Model Tranylcypromine 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 [553102] Drug Info
Phenelzine 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. [552649] Drug Info
Rasagiline 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. [553059] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations MAO A and B knock-out mice exhibit distinct differences in neurotransmitter metabolism and behavior. MAO A knock-out mice have elevated brain levels of serotonin, norephinephrine, and dopamine and manifest aggressive behavior similar to h uMan males with a deletion of MAO A. In contrast, MAO B knock-out mice do not exhibit aggression and only levels of phenylethylamine are increased. Mice lacking MAO B are resistant to the Parkinsongenic neurotoxin, 1-methyl-4-phenyl-1,2,3,6-tetra-hydropyridine. Both MAO A and B knock-out mice show increased reactivity to stress. These knock-out mice are valuable models for investigating the role of monoamines in psychoses and neurodegenerative and stress-related disorders.
References
Ref 531067Eur J Med Chem. 2010 Oct;45(10):4458-66. Epub 2010 Jul 31.Inhibition of monoamine oxidase by indole and benzofuran derivatives.
Ref 531067Eur J Med Chem. 2010 Oct;45(10):4458-66. Epub 2010 Jul 31.Inhibition of monoamine oxidase by indole and benzofuran derivatives.
Ref 553102Inhibition of LSD1 sensitizes glioblastoma cells to histone deacetylase inhibitors. Neuro Oncol. 2011 Aug;13(8):894-903. doi: 10.1093/neuonc/nor049. Epub 2011 Jun 8.
Ref 529853Bioorg Med Chem Lett. 2009 Jan 15;19(2):546-9. Epub 2008 Mar 6.Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
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Ref 529025J Med Chem. 2007 Oct 4;50(20):4909-16. Epub 2007 Sep 7.Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase.
Ref 530683Bioorg Med Chem. 2010 Feb 15;18(4):1388-95. Epub 2010 Jan 15.2-Arylthiomorpholine derivatives as potent and selective monoamine oxidase B inhibitors.
Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
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Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
Ref 530614Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
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Ref 530683Bioorg Med Chem. 2010 Feb 15;18(4):1388-95. Epub 2010 Jan 15.2-Arylthiomorpholine derivatives as potent and selective monoamine oxidase B inhibitors.
Ref 526820J Med Chem. 1992 Oct 2;35(20):3705-13.Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors.
Ref 526820J Med Chem. 1992 Oct 2;35(20):3705-13.Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors.
Ref 526820J Med Chem. 1992 Oct 2;35(20):3705-13.Aliphatic propargylamines: potent, selective, irreversible monoamine oxidase B inhibitors.
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Ref 530001J Med Chem. 2009 Apr 9;52(7):1935-42.Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins.
Ref 530001J Med Chem. 2009 Apr 9;52(7):1935-42.Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins.
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Ref 526287J Med Chem. 2002 Mar 14;45(6):1180-3.3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.
Ref 529077J Med Chem. 2007 Nov 1;50(22):5364-71. Epub 2007 Oct 2.Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives.
Ref 530647Bioorg Med Chem. 2010 Feb;18(3):1018-28. Epub 2010 Jan 6.Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues.
Ref 529853Bioorg Med Chem Lett. 2009 Jan 15;19(2):546-9. Epub 2008 Mar 6.Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
Ref 529853Bioorg Med Chem Lett. 2009 Jan 15;19(2):546-9. Epub 2008 Mar 6.Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
Ref 530434J Med Chem. 2009 Nov 12;52(21):6685-706.Discovery of a novel class of potent coumarin monoamine oxidase B inhibitors: development and biopharmacological profiling of 7-[(3-chlorobenzyl)oxy]-4-[(methylamino)methyl]-2H-chromen-2-one methanesulfonate (NW-1772) as a highly potent, selective, reversible, and orally active monoamine oxidase B inhibitor.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 530056Bioorg Med Chem Lett. 2009 May 1;19(9):2509-13. Epub 2009 Mar 14.Inhibition of monoamine oxidase by (E)-styrylisatin analogues.
Ref 527719Bioorg Med Chem Lett. 2005 Oct 15;15(20):4438-46.Docking studies on monoamine oxidase-B inhibitors: estimation of inhibition constants (K(i)) of a series of experimentally tested compounds.
Ref 529077J Med Chem. 2007 Nov 1;50(22):5364-71. Epub 2007 Oct 2.Synthesis and monoamine oxidase inhibitory activity of new pyridazine-, pyrimidine- and 1,2,4-triazine-containing tricyclic derivatives.
Ref 527719Bioorg Med Chem Lett. 2005 Oct 15;15(20):4438-46.Docking studies on monoamine oxidase-B inhibitors: estimation of inhibition constants (K(i)) of a series of experimentally tested compounds.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 526994Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
Ref 526993Bioorg Med Chem Lett. 2004 Feb 23;14(4):999-1002.Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Ref 526993Bioorg Med Chem Lett. 2004 Feb 23;14(4):999-1002.Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Ref 530675Bioorg Med Chem. 2010 Feb 15;18(4):1659-64. Epub 2010 Jan 4.Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors.
Ref 527283J Med Chem. 2004 Nov 18;47(24):5860-71.Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase.
Ref 530683Bioorg Med Chem. 2010 Feb 15;18(4):1388-95. Epub 2010 Jan 15.2-Arylthiomorpholine derivatives as potent and selective monoamine oxidase B inhibitors.
Ref 529607Bioorg Med Chem. 2008 Aug 1;16(15):7148-66. Epub 2008 Jun 28.Fluorinated phenylcyclopropylamines. Part 5: Effects of electron-withdrawing or -donating aryl substituents on the inhibition of monoamine oxidases A and B by 2-aryl-2-fluoro-cyclopropylamines.
Ref 530056Bioorg Med Chem Lett. 2009 May 1;19(9):2509-13. Epub 2009 Mar 14.Inhibition of monoamine oxidase by (E)-styrylisatin analogues.
Ref 530647Bioorg Med Chem. 2010 Feb;18(3):1018-28. Epub 2010 Jan 6.Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues.
Ref 530647Bioorg Med Chem. 2010 Feb;18(3):1018-28. Epub 2010 Jan 6.Inhibition of monoamine oxidase by 8-benzyloxycaffeine analogues.
Ref 526994Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
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