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Literature summary for 1.13.12.7 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

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

KM Value [mM]

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Luciola mingrelica

Organism

Organism UniProt Comment Textmining
Luciola mingrelica
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
firefly luciferase
-
Luciola mingrelica

IC50 Value

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