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Literature summary for 1.13.12.5 extracted from

  • Auld, D.S.; Southall, N.T.; Jadhav, A.; Johnson, R.L.; Diller, D.J.; Simeonov, A.; Austin, C.P.; Inglese, J.
    Characterization of chemical libraries for luciferase inhibitory activity (2008), J. Med. Chem., 51, 2372-2386.
    View publication on PubMed

Application

Application Comment Organism
analysis analysis of luciferase inhibitors by quantitative high-throughput screening and comparison of and structure-activity relationship using various luciferase-based detection reagents Renilla reniformis

Inhibitors

Inhibitors Comment Organism Structure
(2Z)-3-[(2-bromophenyl)amino]-1-pyridin-2-ylprop-2-en-1-one
-
Renilla reniformis
(2Z)-3-[[4-(dimethylamino)cyclohexa-1,5-dien-1-yl]amino]-1-phenylprop-2-en-1-one
-
Renilla reniformis
(3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1,3-dihydro-2H-indol-2-one common name SU4312 Renilla reniformis
2-(4-ethoxyphenyl)-4-[(4-methylpiperazin-1-yl)carbonyl]quinoline
-
Renilla reniformis
2-(4-ethoxyphenyl)-4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]quinoline
-
Renilla reniformis
2-(4-methylphenyl)-4-[(4-pyrimidin-2-ylpiperazin-1-yl)carbonyl]quinoline
-
Renilla reniformis
2-(5-naphthalen-2-yl-1,2,4-oxadiazol-3-yl)pyridine
-
Renilla reniformis
2-hydroxy-N'-[(1E)-(2-hydroxyphenyl)methylidene]benzohydrazide common name SCS Renilla reniformis
2-[5-(3-chlorophenyl)-1,2,4-oxadiazol-3-yl]pyridine
-
Renilla reniformis
4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)-2-(4-ethoxyphenyl)quinoline
-
Renilla reniformis
4-amino-6-[(E)-[4'-[(Z)-(8-amino-1-hydroxy-5,7-disulfonato-6,7-dihydronaphthalen-2-yl)diazenyl]-3-methylbiphenyl-4-yl]diazenyl]-5-hydroxy-2,3-dihydronaphthalene-1,3-disulfonate common name Evans Blue Renilla reniformis
4-[1-(1,3-benzothiazol-2-yl)-2-(4-methylpiperazin-1-yl)-2-oxoethyl]phenol
-
Renilla reniformis
6-methyl-2-[(Z)-phenyldiazenyl]pyridin-3-ol common name SIB1757 Renilla reniformis
ethyl 4-[[2-(4-ethoxyphenyl)quinolin-4-yl]carbonyl]piperazine-1-carboxylate
-
Renilla reniformis
additional information structure-activity relationship of luciferase inhibitors determined by quantitative high-throughput screening. Comparison of effect on various luciferase-based detection reagents Renilla reniformis
N'-(3-chlorophenyl)-N-[(1Z)-(3-chlorophenyl)methylidene]imidoformamide common name DCB Renilla reniformis

Organism

Organism UniProt Comment Textmining
Renilla reniformis
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-luciferin + O2 + ATP
-
Renilla reniformis oxidized D-luciferin + CO2 + H2O + AMP + diphosphate + hv
-
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Synonyms

Synonyms Comment Organism
firefly luciferase
-
Renilla reniformis
Luc
-
Renilla reniformis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.01
-
-
Renilla reniformis 4-amino-6-[(E)-[4'-[(Z)-(8-amino-1-hydroxy-5,7-disulfonato-6,7-dihydronaphthalen-2-yl)diazenyl]-3-methylbiphenyl-4-yl]diazenyl]-5-hydroxy-2,3-dihydronaphthalene-1,3-disulfonate
0.011
-
-
Renilla reniformis (2Z)-3-[[4-(dimethylamino)cyclohexa-1,5-dien-1-yl]amino]-1-phenylprop-2-en-1-one
0.011
-
-
Renilla reniformis 2-(4-ethoxyphenyl)-4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]quinoline
0.011
-
-
Renilla reniformis 4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)-2-(4-ethoxyphenyl)quinoline
0.011
-
pH 7.2, 22°C Renilla reniformis (2Z)-3-[[4-(dimethylamino)cyclohexa-1,5-dien-1-yl]amino]-1-phenylprop-2-en-1-one
0.011
-
pH 7.2, 22°C Renilla reniformis 2-(4-ethoxyphenyl)-4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]quinoline
0.011
-
pH 7.2, 22°C Renilla reniformis 4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)-2-(4-ethoxyphenyl)quinoline
0.019
-
-
Renilla reniformis (3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1,3-dihydro-2H-indol-2-one
0.019
-
pH 7.2, 22°C Renilla reniformis (3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1,3-dihydro-2H-indol-2-one
0.02
-
-
Renilla reniformis 2-hydroxy-N'-[(1E)-(2-hydroxyphenyl)methylidene]benzohydrazide
0.02
-
-
Renilla reniformis ethyl 4-[[2-(4-ethoxyphenyl)quinolin-4-yl]carbonyl]piperazine-1-carboxylate
0.02
-
pH 7.2, 22°C Renilla reniformis 2-hydroxy-N'-[(1E)-(2-hydroxyphenyl)methylidene]benzohydrazide
0.02
-
pH 7.2, 22°C Renilla reniformis ethyl 4-[[2-(4-ethoxyphenyl)quinolin-4-yl]carbonyl]piperazine-1-carboxylate
0.0225
-
-
Renilla reniformis 4-[1-(1,3-benzothiazol-2-yl)-2-(4-methylpiperazin-1-yl)-2-oxoethyl]phenol
0.0225
-
pH 7.2, 22°C Renilla reniformis 4-[1-(1,3-benzothiazol-2-yl)-2-(4-methylpiperazin-1-yl)-2-oxoethyl]phenol
0.025
-
-
Renilla reniformis 2-(5-naphthalen-2-yl-1,2,4-oxadiazol-3-yl)pyridine
0.025
-
IC50 above 0.025 mM Renilla reniformis 2-(4-ethoxyphenyl)-4-[(4-methylpiperazin-1-yl)carbonyl]quinoline
0.025
-
IC50 above 0.025 mM Renilla reniformis 2-(4-methylphenyl)-4-[(4-pyrimidin-2-ylpiperazin-1-yl)carbonyl]quinoline
0.025
-
pH 7.2, 22°C Renilla reniformis 2-(5-naphthalen-2-yl-1,2,4-oxadiazol-3-yl)pyridine
0.036
-
-
Renilla reniformis 6-methyl-2-[(Z)-phenyldiazenyl]pyridin-3-ol
0.05
-
IC50 above 0.05 mM Renilla reniformis (2Z)-3-[(2-bromophenyl)amino]-1-pyridin-2-ylprop-2-en-1-one
0.05
-
IC50 above 0.05 mM Renilla reniformis 2-[5-(3-chlorophenyl)-1,2,4-oxadiazol-3-yl]pyridine
0.05
-
IC50 above 0.05 mM Renilla reniformis N'-(3-chlorophenyl)-N-[(1Z)-(3-chlorophenyl)methylidene]imidoformamide