Application | Comment | Organism |
---|---|---|
drug development | mitochondrial malate dehydrogenase is a biological target for antiproliferative activity | Sus scrofa |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
11-chloro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 65.3% inhibition at 0.010 mM | Sus scrofa | |
2,3-dimethoxy-6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carbonitrile | 89.2% inhibition at 0.010 mM | Sus scrofa | |
2,3-dimethoxy-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 97.7% inhibition at 0.010 mM | Sus scrofa | |
3-methoxy-9-trifluormethyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 83.9% inhibition at 0.010 mM | Sus scrofa | |
4-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 87.6% inhibition at 0.010 mM | Sus scrofa | |
5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-(4-methylbenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-benzyl-9-bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 8.6% inhibition at 0.010 mM | Sus scrofa | |
5-benzyl-9-chloro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-benzyl-9-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-benzyl-9-methyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-benzyl-9-tert-butyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
5-benzyl-9-trifluoromethyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carbonitrile | 91.3% inhibition at 0.010 mM | Sus scrofa | |
6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylic acid | 98.7% inhibition at 0.010 mM | Sus scrofa | |
7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 78.7% inhibition at 0.010 mM | Sus scrofa | |
8,10-dichloro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 28.7% inhibition at 0.010 mM | Sus scrofa | |
9-(methylsulfinyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 96.2% inhibition at 0.010 mM | Sus scrofa | |
9-(methylthio)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 76.6% inhibition at 0.010 mM | Sus scrofa | |
9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 88.3% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-12-(prop-2-en-1-yl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 74.1% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-12-methyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 98.0% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-2,3-dimethoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 56.3% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-2-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 58.7% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-3-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 15.0% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-4-hydroxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 25.9% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-4-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 82.0% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
9-bromo-5-(4-methoxybenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
9-bromo-5-(4-methylbenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
9-bromo-5-methyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 81.9% inhibition at 0.010 mM | Sus scrofa | |
9-bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 74.5% inhibition at 0.010 mM | Sus scrofa | |
9-chloro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 73.4% inhibition at 0.010 mM | Sus scrofa | |
9-fluoro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 46.2% inhibition at 0.010 mM | Sus scrofa | |
9-methyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 87.8% inhibition at 0.010 mM | Sus scrofa | |
9-nitro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | 54.2% inhibition at 0.010 mM | Sus scrofa | |
9-tert-butyl-5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | - |
Sus scrofa | |
butyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa | |
ethyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa | |
hexyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa | |
methyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | 60.9% inhibition at 0.010 mM | Sus scrofa | |
additional information | development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mMDH, overview | Sus scrofa | |
octyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa | |
pentyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa | |
propyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | - |
Sus scrofa |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
mitochondrion | isozyme mMDH | Sus scrofa | 5739 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
(S)-malate + NAD+ | Sus scrofa | - |
oxaloacetate + NADH + H+ | - |
r |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Sus scrofa | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
commercial preparation | - |
Sus scrofa | - |
heart | - |
Sus scrofa | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
(S)-malate + NAD+ | - |
Sus scrofa | oxaloacetate + NADH + H+ | - |
r |
Synonyms | Comment | Organism |
---|---|---|
mitochondrial malate dehydrogenase | - |
Sus scrofa |
mMDH | - |
Sus scrofa |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Sus scrofa |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
8.5 | - |
assay at | Sus scrofa |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | - |
Sus scrofa | |
NADH | - |
Sus scrofa |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00077 | - |
pH 8.5, 25°C | Sus scrofa | 9-tert-butyl-5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0011 | - |
pH 8.5, 25°C | Sus scrofa | 9-bromo-5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0016 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-tert-butyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0016 | - |
pH 8.5, 25°C | Sus scrofa | 9-bromo-5-(4-methylbenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0018 | - |
pH 8.5, 25°C | Sus scrofa | 9-bromo-5-(4-methoxybenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0024 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-bromo-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0027 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-chloro-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0027 | - |
pH 8.5, 25°C | Sus scrofa | octyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.0042 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-trifluoromethyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0043 | - |
pH 8.5, 25°C | Sus scrofa | hexyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.0044 | - |
pH 8.5, 25°C | Sus scrofa | pentyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.0062 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-methyl-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0062 | - |
pH 8.5, 25°C | Sus scrofa | propyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.0079 | - |
pH 8.5, 25°C | Sus scrofa | 5-(3,4-dichlorobenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0099 | - |
pH 8.5, 25°C | Sus scrofa | butyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.0105 | - |
pH 8.5, 25°C | Sus scrofa | 5-(4-methylbenzyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0119 | - |
pH 8.5, 25°C | Sus scrofa | 5-benzyl-9-methoxy-7,12-dihydroindolo[3,2-d][1]benzazepin-6(5H)-one | |
0.0135 | - |
pH 8.5, 25°C | Sus scrofa | methyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate | |
0.02 | - |
pH 8.5, 25°C | Sus scrofa | ethyl 6-oxo-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepine-9-carboxylate |
General Information | Comment | Organism |
---|---|---|
additional information | mMDH inhibition is of minor relevance for the growth inhibition caused by paullones | Sus scrofa |