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Literature summary extracted from

  • Heitman, L.H.; van Veldhoven, J.P.; Zweemer, A.M.; Ye, K.; Brussee, J.; IJzerman, A.P.
    False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase (2008), J. Med. Chem., 51, 4724-4729.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.13.12.7 1-phenyl-3-(5-phenylpyridin-2-yl)urea 10 microM, 20% inhibition Luciola mingrelica
1.13.12.7 2,4-dimethoxy-N-(5-methylpyridin-2-yl)benzamide
-
 Luciola mingrelica
1.13.12.7 3,4-dichloro-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 13% inhibition Luciola mingrelica
1.13.12.7 3,4-dimethoxy-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 26% inhibition Luciola mingrelica
1.13.12.7 3-chloro-N-(5-phenylpyridin-2-yl)benzamide
-
 Luciola mingrelica
1.13.12.7 4-(1-methylethoxy)-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 12% inhibition Luciola mingrelica
1.13.12.7 4-(dimethylamino)-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 35% inhibition Luciola mingrelica
1.13.12.7 4-amino-N-(5-phenylpyridin-2-yl)benzamide
-
 Luciola mingrelica
1.13.12.7 4-chloro-N-(5-phenylpyridin-2-yl)benzamide
-
 Luciola mingrelica
1.13.12.7 4-methoxy-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 28% inhibition Luciola mingrelica
1.13.12.7 4-methyl-N-(5-phenylpyridin-2-yl)benzamide 10 microM, 18% inhibition Luciola mingrelica
1.13.12.7 N-(5-methylpyridin-2-yl)benzamide
-
 Luciola mingrelica
1.13.12.7 N-(5-phenylpyridin-2-yl)benzamide 10 microM, 27% inhibition Luciola mingrelica
1.13.12.7 N-(5-phenylpyridin-2-yl)butanamide 10 mciroM, 22% inhibition Luciola mingrelica
1.13.12.7 N-(5-phenylpyridin-2-yl)cyclohexanecarboxamide
-
 Luciola mingrelica
1.13.12.7 N-(6-phenylpyridin-2-yl)benzamide 10 microM, 30% inhibition Luciola mingrelica
1.13.12.7 N-benzyl-5-phenylpyridin-2-amine 10 microM, 20% inhibition Luciola mingrelica
1.13.12.7 N-quinolin-2-ylbenzamide
-
 Luciola mingrelica
1.13.12.7 N-[5-(3,4-dichlorophenyl)pyridin-2-yl]benzamide 10 microM, 4% inhibition Luciola mingrelica
1.13.12.7 N-[5-(3-chlorophenyl)pyridin-2-yl]benzamide 10 microM, 38% inhibition Luciola mingrelica
1.13.12.7 N-[5-(4-chlorophenyl)pyridin-2-yl]benzamide
-
 Luciola mingrelica
1.13.12.7 N-[5-(4-methoxyphenyl)pyridin-2-yl]benzamide
-
 Luciola mingrelica
1.13.12.7 N-[5-(4-methylphenyl)pyridin-2-yl]benzamide 10 microM, 51% inhibition Luciola mingrelica
1.13.12.7 N-[5-(4-tert-butylphenyl)pyridin-2-yl]benzamide 10 microM, 49% inhibition Luciola mingrelica
1.13.12.7 N-[5-[4-(1-methylethoxy)phenyl]pyridin-2-yl]benzamide 10 microM, 38% inhibition Luciola mingrelica
1.13.12.7 N-[5-[4-(dimethylamino)phenyl]pyridin-2-yl]benzamide 10 microM, 14% inhibition Luciola mingrelica
1.13.12.7 N-[5-[4-(trifluoromethyl)phenyl]pyridin-2-yl]benzamide 10 microM, 39% inhibition Luciola mingrelica
1.13.12.7 phenyl (5-phenylpyridin-2-yl)carbamate
-
 Luciola mingrelica

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.13.12.7 0.003
-
 ATP 150 microM luciferin, two-site binding model Luciola mingrelica
1.13.12.7 0.0038
-
 ATP 150 microM luciferin, presence of 1 microM of N-quinolin-2-ylbenzamide, two-site binding model Luciola mingrelica
1.13.12.7 0.012
-
 Luciferin 90 microM ATP Luciola mingrelica
1.13.12.7 0.016
-
 Luciferin 90 microM ATP, presence of 0.1 microM of N-quinolin-2-ylbenzamide Luciola mingrelica
1.13.12.7 0.053
-
 Luciferin 90 microM ATP, presence of 1 microM of N-quinolin-2-ylbenzamide Luciola mingrelica
1.13.12.7 0.094
-
 ATP 150 microM luciferin, presence of 1 microM of N-quinolin-2-ylbenzamide, two-site binding model Luciola mingrelica
1.13.12.7 0.138
-
 ATP 150 microM luciferin, two-site binding model Luciola mingrelica

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.13.12.7 Mg2+ required Luciola mingrelica

Organism

EC Number Organism UniProt Comment Textmining
1.13.12.7 Luciola mingrelica
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.13.12.7 D-luciferin + ATP + O2 assay at pH 7.8 Luciola mingrelica luciferyl-AMP + diphosphate
-
 r
1.13.12.7 luciferyl-AMP + O2
-
 Luciola mingrelica oxyluciferin + hv + CO2 + AMP + diphosphate
-
 r

Synonyms

EC Number Synonyms Comment Organism
1.13.12.7 firefly luciferase
-
 Luciola mingrelica

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.13.12.7 0.000069
-
-
 Luciola mingrelica N-(5-phenylpyridin-2-yl)benzamide
1.13.12.7 0.00016
-
-
 Luciola mingrelica 3-chloro-N-(5-phenylpyridin-2-yl)benzamide
1.13.12.7 0.00031
-
-
 Luciola mingrelica N-[5-(4-methoxyphenyl)pyridin-2-yl]benzamide
1.13.12.7 0.00056
-
-
 Luciola mingrelica N-[5-(4-chlorophenyl)pyridin-2-yl]benzamide
1.13.12.7 0.0012
-
-
 Luciola mingrelica 4-amino-N-(5-phenylpyridin-2-yl)benzamide
1.13.12.7 0.0024
-
-
 Luciola mingrelica N-(5-phenylpyridin-2-yl)cyclohexanecarboxamide
1.13.12.7 0.0064
-
-
 Luciola mingrelica N-(5-methylpyridin-2-yl)benzamide
1.13.12.7 0.007
-
-
 Luciola mingrelica N-quinolin-2-ylbenzamide