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Literature summary for 1.1.1.205 extracted from

  • Shah, C.P.; Kharkar, P.S.
    Newer human inosine 5-monophosphate dehydrogenase 2 (hIMPDH2) inhibitors as potential anticancer agents (2018), J. Enzyme Inhib. Med. Chem., 33, 972-977 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.1.1.205

Inhibitors

Inhibitors Comment Organism Structure
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2R)-2-phenylpropyl]hex-4-enamide 73.94% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2S)-2-phenylpropyl]hex-4-enamide 59.15% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(2-methylphenyl)ethyl]hex-4-enamide 84% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(4-methylphenyl)ethyl]hex-4-enamide 73.42% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(pyridin-2-yl)ethyl]hex-4-enamide 59.38% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(pyridin-4-yl)ethyl]hex-4-enamide 57.38% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[3-(morpholin-4-yl)propyl]hex-4-enamide 36.05% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-(3-methoxyphenyl)-4-methylhex-4-enamide 30.82% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-(4-methoxyphenyl)-4-methylhex-4-enamide 54.84% inhibition at 0.01 mM Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-[2-(4-methoxyphenyl)ethyl]-4-methylhex-4-enamide 96.13% inhibition at 0.01 mM Homo sapiens
(4E)-N-[(4-butylphenyl)methyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide 93.62% inhibition at 0.01 mM Homo sapiens
(4E)-N-[2-(2-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide 72.04% inhibition at 0.01 mM Homo sapiens
(4E)-N-[2-(2H-1,3-benzodioxol-5-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide 87.09% inhibition at 0.01 mM Homo sapiens
(4E)-N-[2-(4-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide 81.36% inhibition at 0.01 mM Homo sapiens
(4E)-N-[2-(furan-2-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide 67.18% inhibition at 0.01 mM Homo sapiens
mizoribine competitive inhibitor Homo sapiens
mycophenolate mofetil
-
 Homo sapiens
Mycophenolic acid reversible, potent, uncompetitive inhibitor, 99.9% inhibition at 0.01 mM Homo sapiens
mycophenolic acid sodium
-
 Homo sapiens
ribavirin competitive inhibitor Homo sapiens
tiazofurin competitive inhibitor Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
IMP + NAD+ + H2O Homo sapiens
-
 XMP + NADH + H+
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P12268
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
 Homo sapiens
-
DU-145 cell
-
 Homo sapiens
-
glioblastoma cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-
prostate gland cancer cell
-
 Homo sapiens
-
U-87MG cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
IMP + NAD+ + H2O
-
 Homo sapiens XMP + NADH + H+
-
 ?

Synonyms

Synonyms Comment Organism
IMPDH2
-
 Homo sapiens
inosine 5-monophosphate dehydrogenase 2
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00033
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N-[2-(4-methoxyphenyl)ethyl]-4-methylhex-4-enamide
0.00048
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-N-[(4-butylphenyl)methyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.0005
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(2-methylphenyl)ethyl]hex-4-enamide
0.00051
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-N-[2-(2H-1,3-benzodioxol-5-yl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00057
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-N-[2-(4-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.0006
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[2-(4-methylphenyl)ethyl]hex-4-enamide
0.00073
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-N-[2-(2-chlorophenyl)ethyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
0.00082
-
 isoform IMPDH2, at pH 8.6 and 37°C Homo sapiens (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[(2R)-2-phenylpropyl]hex-4-enamide