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Literature summary for 1.1.1.205 extracted from

  • Watterson,S.H.; Carlsen, M.; Dhar, T.G.M.; Shen, Z.; Pitts, W.J.; Guo, J.; Gu, H.H.; Norris, D.; Chorba, J.; Chen, P.; Cheney, D.; Witmer, M.; Fleener, C.A.; Rouleau, K.; Townsend, R.; Hollenbaugh D.L.; Iwanowicz, E.J.
    Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series (2003), Bioorg. Med. Chem. Lett., 13, 543-546.
    View publication on PubMed
Search for more literature for 1.1.1.205

Inhibitors

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
 type I and type II isozymes
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
IMPDH
-
 Homo sapiens
inosine monophosphate dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+ dependent on Homo sapiens

Ki Value [mM]

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 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