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Literature summary for 1.1.1.205 extracted from

  • Gollapalli, D.R.; Macpherson, I.S.; Liechti, G.; Gorla, S.K.; Goldberg, J.B.; Hedstrom, L.
    Structural determinants of inhibitor selectivity in prokaryotic IMP dehydrogenases (2010), Chem. Biol., 17, 1084-1091.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.1.1.205

Protein Variants

Protein Variants Comment Organism
S250A/L444Y mutation of residues corresponding to structural motif A250/Y358 of Cryptosporidium parvum. Mutation renders the enzyme susceptible to inhibitors Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
 Borreliella burgdorferi
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate not inhibitory to wild-type Escherichia coli
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
 Helicobacter pylori
1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
-
 Streptococcus pyogenes
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
 Borreliella burgdorferi
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide not inhibitory to wild-type Escherichia coli
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
 Helicobacter pylori
2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
-
 Streptococcus pyogenes
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
 Borreliella burgdorferi
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate not inhibitory to wild-type Escherichia coli
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
 Helicobacter pylori
3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
-
 Streptococcus pyogenes
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
 Borreliella burgdorferi
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate not inhibitory to wild-type Escherichia coli
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
 Helicobacter pylori
methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
-
 Streptococcus pyogenes
additional information compounds are not inhibitory to Escherichia coli, Tritrichomonas foetus, and Leishmania donovani IMPDH. Susceptible enzymes are defined by structural motif A165/Y358, Cryptosporidium parvum numbering Helicobacter pylori
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
 Borreliella burgdorferi
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide not inhibitory to wild-type Escherichia coli
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
 Helicobacter pylori
N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
-
 Streptococcus pyogenes
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
 Borreliella burgdorferi
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide not inhibitory to wild-type Escherichia coli
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
 Helicobacter pylori
N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
-
 Streptococcus pyogenes
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
 Borreliella burgdorferi
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide not inhibitory to wild-type Escherichia coli
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
 Helicobacter pylori
N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
-
 Streptococcus pyogenes

Organism

Organism UniProt Comment Textmining
Borreliella burgdorferi
-
-
-
Escherichia coli
-
-
-
Helicobacter pylori
-
-
-
Streptococcus pyogenes
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000011
-
 pH 8.0, 25°C Helicobacter pylori N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
0.0000019
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
0.0000054
-
 pH 8.0, 25°C Streptococcus pyogenes N-(naphthalen-2-yl)-2-[2-(pyridin-2-yl)-5,6-dihydro-1H-benzimidazol-1-yl]acetamide
0.00022
-
 pH 8.0, 25°C Borreliella burgdorferi 1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
0.0003
-
 pH 8.0, 25°C Helicobacter pylori 1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
0.0004
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli 1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
0.00055
-
 pH 8.0, 25°C Streptococcus pyogenes 1H-naphtho[2,3-d]imidazol-2-ylmethyl 4-aminobenzoate
0.0006
-
 pH 8.0, 25°C Helicobacter pylori N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
0.0006
-
 pH 8.0, 25°C Borreliella burgdorferi N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
0.0006
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide
0.0008
-
 pH 8.0, 25°C Borreliella burgdorferi 2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
0.00086
-
 pH 8.0, 25°C Streptococcus pyogenes 3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
0.0009
-
 pH 8.0, 25°C Borreliella burgdorferi methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
0.0009
-
 pH 8.0, 25°C Borreliella burgdorferi 3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
0.001
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli 3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
0.0011
-
 pH 8.0, 25°C Helicobacter pylori 2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
0.0011
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli 2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
0.0012
-
 pH 8.0, 25°C Helicobacter pylori 3-(1H-naphtho[2,3-d]imidazol-2-yl)propyl 4-aminobenzoate
0.0015
-
 pH 8.0, 25°C Helicobacter pylori methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
0.0017
-
 pH 8.0, 25°C Borreliella burgdorferi N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
0.0018
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
0.0023
-
 mutant S250A/L444Y, pH 8.0, 25°C Escherichia coli N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
0.003
-
 pH 8.0, 25°C Helicobacter pylori N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
0.013
-
 pH 8.0, 25°C Streptococcus pyogenes 2-[(3-ethyl-4-oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)sulfanyl]-N-(4-methoxyphenyl)acetamide
0.015
-
 pH 8.0, 25°C Streptococcus pyogenes methyl 3-methyl-2-oxo-1,2-dihydroquinoline-4-carboxylate
0.049
-
 pH 8.0, 25°C Streptococcus pyogenes N-(4-methoxyphenyl)-2-(3-methyl-4-oxo-3,4-dihydrophthalazin-1-yl)acetamide
0.07
-
 pH 8.0, 25°C Streptococcus pyogenes N-(4-methoxyphenyl)-2-[2-(1,3-thiazol-4-yl)-1H-benzimidazol-1-yl]acetamide