Inhibitors | Comment | Organism | Structure |
---|---|---|---|
2-(dimethylamino)-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 200 nM | Homo sapiens | |
2-amino-oxazole-cyanoindoles | - |
Homo sapiens | |
2-benzyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 180 nM | Homo sapiens | |
2-furan-3-yl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 32 nM | Homo sapiens | |
2-tert-butyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 0.01 mM | Homo sapiens | |
3-phenyl quinolone derivatives | several, isozyme IMPDH II IC50: 5-160 nM, overview | Homo sapiens | |
7-methoxy-2-(methylamino)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 220 nM | Homo sapiens | |
7-methoxy-2-methyl-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 110 nM | Homo sapiens | |
7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one | isozyme IMPDH II IC50: 65 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-(1,3-thiazol-4-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 34 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one | isozyme IMPDH II IC50: 8 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-2-ylquinolin-4(1H)-one | isozyme IMPDH II IC50: 43 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-3-ylquinolin-4(1H)-one | isozyme IMPDH II IC50: 70 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-4-ylquinolin-4(1H)-one | isozyme IMPDH II IC50: 46 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-2-ylquinolin-4(1H)-one | isozyme IMPDH II IC50: 63 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-3-ylquinolin-4(1H)-one | isozyme IMPDH II IC50: 9 nM | Homo sapiens | |
7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | isozyme IMPDH II IC50: 300 nM | Homo sapiens | |
BMS-337197 | i.e. BMS-337197 | Homo sapiens | |
additional information | development and synthesis of inhibitors, determination and analysis of structure-activity relationships of the different inhibitor molecules with isozyme IMPDH II, overview | Homo sapiens | |
Mycophenolic acid | potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil, isozyme IMPDH II IC50: 14 nM | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
inosine 5'-phosphate + NAD+ + H2O | Homo sapiens | rate-limiting step of the de novo guanine nucleotide biosynthesis | xanthosine 5'-phosphate + NADH | - |
ir |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
type I and type II isozymes | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
inosine 5'-phosphate + NAD+ + H2O | - |
Homo sapiens | xanthosine 5'-phosphate + NADH | - |
ir | |
inosine 5'-phosphate + NAD+ + H2O | rate-limiting step of the de novo guanine nucleotide biosynthesis | Homo sapiens | xanthosine 5'-phosphate + NADH | - |
ir |
Synonyms | Comment | Organism |
---|---|---|
IMPDH | - |
Homo sapiens |
inosine monophosphate dehydrogenase | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
NAD+ | dependent on | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000007 | - |
7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000005 | 0.00016 | several, isozyme IMPDH II IC50: 5-160 nM, overview | Homo sapiens | 3-phenyl quinolone derivatives | |
0.000008 | - |
isozyme IMPDH II IC50: 8 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one | |
0.000009 | - |
isozyme IMPDH II IC50: 9 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-3-ylquinolin-4(1H)-one | |
0.000014 | - |
potent, uncompetitive, reversible, inhibits both isozymes, prodrug is mycophenolate mofetil, isozyme IMPDH II IC50: 14 nM | Homo sapiens | Mycophenolic acid | |
0.000032 | - |
isozyme IMPDH II IC50: 32 nM | Homo sapiens | 2-furan-3-yl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.000034 | - |
isozyme IMPDH II IC50: 34 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-(1,3-thiazol-4-yl)quinolin-4(1H)-one | |
0.000043 | - |
isozyme IMPDH II IC50: 43 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-2-ylquinolin-4(1H)-one | |
0.000046 | - |
isozyme IMPDH II IC50: 46 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-4-ylquinolin-4(1H)-one | |
0.000063 | - |
isozyme IMPDH II IC50: 63 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-thiophen-2-ylquinolin-4(1H)-one | |
0.000065 | - |
isozyme IMPDH II IC50: 65 nM | Homo sapiens | 7-methoxy-3-methyl-6-(1,3-oxazol-5-yl)-2-phenylquinolin-4(1H)-one | |
0.00007 | - |
isozyme IMPDH II IC50: 70 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)-2-pyridin-3-ylquinolin-4(1H)-one | |
0.00011 | - |
isozyme IMPDH II IC50: 110 nM | Homo sapiens | 7-methoxy-2-methyl-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.00018 | - |
isozyme IMPDH II IC50: 180 nM | Homo sapiens | 2-benzyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.0002 | - |
isozyme IMPDH II IC50: 200 nM | Homo sapiens | 2-(dimethylamino)-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.00022 | - |
isozyme IMPDH II IC50: 220 nM | Homo sapiens | 7-methoxy-2-(methylamino)-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.0003 | - |
isozyme IMPDH II IC50: 300 nM | Homo sapiens | 7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one | |
0.01 | - |
isozyme IMPDH II IC50: 0.01 mM | Homo sapiens | 2-tert-butyl-7-methoxy-6-(1,3-oxazol-5-yl)quinolin-4(1H)-one |