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Literature summary for 1.1.1.205 extracted from

  • Lee, S.; Ku, A.F.; Vippila, M.R.; Wang, Y.; Zhang, M.; Wang, X.; Hedstrom, L.; Cuny, G.D.
    Mycophenolic anilides as broad specificity inosine-5-monophosphate dehydrogenase (IMPDH) inhibitors (2020), Bioorg. Med. Chem. Lett., 30, 127543 .
    View publication on PubMed
Search for more literature for 1.1.1.205

Inhibitors

Inhibitors Comment Organism Structure
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
-
 Cryptosporidium parvum
(2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide
-
 Homo sapiens
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
-
 Cryptosporidium parvum
(4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide
-
 Homo sapiens
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide
-
 Homo sapiens
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Cryptosporidium parvum
(4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide
-
 Homo sapiens
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
-
 Cryptosporidium parvum
3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate
-
 Homo sapiens
Mycophenolic acid
-
 Cryptosporidium parvum
Mycophenolic acid
-
 Homo sapiens
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
 Cryptosporidium parvum
N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide
-
 Homo sapiens
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
-
 Cryptosporidium parvum
N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide
-
 Homo sapiens
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
 Cryptosporidium parvum
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
 Homo sapiens
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
 Cryptosporidium parvum
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide
-
 Homo sapiens
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
-
 Cryptosporidium parvum
N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Cryptosporidium parvum
-
-
-
Homo sapiens P12268
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
IMPDH
-
 Cryptosporidium parvum
IMPDH2 isoform Homo sapiens
inosine-5-monophosphate dehydrogenase
-
 Cryptosporidium parvum
inosine-5-monophosphate dehydrogenase
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NAD+
-
 Cryptosporidium parvum
NAD+
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000007
-
 Mycophenolic acid isoform IMPDH2, at pH 8.0 and 25°C Homo sapiens
0.000016
-
 (4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.000041
-
 (4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.000042
-
 (4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.000046
-
 (4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00006
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhexanamide at pH 8.0 and 25°C Cryptosporidium parvum
0.000066
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00011
-
 (4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00013
-
 (4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.000151
-
 (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00018
-
 (4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00023
-
 (4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.00027
-
 (4E)-N-(4-fluorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.00029
-
 N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide at pH 8.0 and 25°C Homo sapiens
0.00034
-
 (4E)-N-(3,4-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.00035
-
 (4E)-N-(4-chloro-3-methoxyphenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.00035
-
 (4E)-N-(4-cyanophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.0004
-
 (4E)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methyl-N-[4-(trifluoromethyl)phenyl]hex-4-enamide at pH 8.0 and 25°C Homo sapiens
0.000405
-
 3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate at pH 8.0 and 25°C Cryptosporidium parvum
0.00045
-
 N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)butanamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00046
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1R,2S)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide at pH 8.0 and 25°C Homo sapiens
0.00048
-
 (2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00055
-
 (2E)-N-(4-chlorophenyl)-4-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)but-2-enamide at pH 8.0 and 25°C Homo sapiens
0.00057
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide at pH 8.0 and 25°C Cryptosporidium parvum
0.000681
-
 (4E)-N-(2,3-dichlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.0008
-
 N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide at pH 8.0 and 25°C Homo sapiens
0.00087
-
 (4E)-N-(4-chlorophenyl)-6-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-N,4-dimethylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.00087
-
 3-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)propyl (4-chlorophenyl)carbamate at pH 8.0 and 25°C Homo sapiens
0.0014
-
 N-[4-chloro-3-(trifluoromethyl)phenyl]-3-[(1S,2R)-2-[(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)methyl]-1-methylcyclopropyl]propanamide at pH 8.0 and 25°C Homo sapiens
0.0017
-
 (4E)-N-[4-chloro-3-(trifluoromethyl)phenyl]-6-(4,6-dimethoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)-4-methylhex-4-enamide at pH 8.0 and 25°C Cryptosporidium parvum
0.0028
-
 N-(4-chlorophenyl)-2-(4-hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydro-2-benzofuran-5-yl)acetamide at pH 8.0 and 25°C Cryptosporidium parvum
0.0093
-
 Mycophenolic acid at pH 8.0 and 25°C Cryptosporidium parvum