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Literature summary for 2.1.1.56 extracted from

  • Aouadi, W.; Eydoux, C.; Coutard, B.; Martin, B.; Debart, F.; Vasseur, J.J.; Contreras, J.M.; Morice, C.; Querat, G.; Jung, M.L.; Canard, B.; Guillemot, J.C.; Decroly, E.
    Toward the identification of viral cap-methyltransferase inhibitors by fluorescence screening assay (2017), Antiviral Res., 144, 330-339 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)acetic acid
-
Homo sapiens
(2R,6S)-2,6-dimethyl-4-[2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine
-
Severe acute respiratory syndrome-related coronavirus
1,8-dihydroxyanthracen-9(10H)-one
-
Homo sapiens
1,8-dihydroxyanthracen-9(10H)-one
-
Severe acute respiratory syndrome-related coronavirus
1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
-
Homo sapiens
1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
-
Severe acute respiratory syndrome-related coronavirus
1-(diphenylmethyl)-4-methylpiperazine hydrochloride (1:1)
-
Homo sapiens
1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
-
Homo sapiens
1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
-
Severe acute respiratory syndrome-related coronavirus
1-[(4-chlorophenyl)(phenyl)methyl]-4-methylpiperazine
-
Homo sapiens
1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
-
Homo sapiens
1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
-
Severe acute respiratory syndrome-related coronavirus
1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
-
Homo sapiens
1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
-
Severe acute respiratory syndrome-related coronavirus
1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
-
Homo sapiens
1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
-
Severe acute respiratory syndrome-related coronavirus
2,3,7,8-tetrahydroxy[1]benzopyrano[5,4,3-cde][1]benzopyran-5,10-dione
-
Severe acute respiratory syndrome-related coronavirus
2-(2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)ethan-1-ol
-
Homo sapiens
3,3',4',5,5',7-hexahaxdroxyflavone
-
Homo sapiens
3,3',4',5,5',7-hexahaxdroxyflavone
-
Severe acute respiratory syndrome-related coronavirus
3,3',4',5,7-pentahydroxyflavone
-
Homo sapiens
3,3',4',5,7-pentahydroxyflavone
-
Severe acute respiratory syndrome-related coronavirus
3,4',5,7-tetrahydroxyflavone
-
Homo sapiens
3,4',5,7-tetrahydroxyflavone
-
Severe acute respiratory syndrome-related coronavirus
3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
-
Homo sapiens
3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
-
Severe acute respiratory syndrome-related coronavirus
bis[6-(dimethylamino)-2-[(E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methylquinolin-1-ium] 4-[(3-carboxy-2-oxidonaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylate
-
Homo sapiens
bis[6-(dimethylamino)-2-[(E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methylquinolin-1-ium] 4-[(3-carboxy-2-oxidonaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylate
-
Severe acute respiratory syndrome-related coronavirus
N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
-
Homo sapiens
N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
-
Severe acute respiratory syndrome-related coronavirus
sinefungin 98.2% inhibition at 0.05 mM Homo sapiens
sinefungin 98.2% inhibition at 0.05 mM Severe acute respiratory syndrome-related coronavirus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA] Homo sapiens
-
S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
?
S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA] Severe acute respiratory syndrome-related coronavirus
-
S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Severe acute respiratory syndrome-related coronavirus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information no activity with 7mGpppA Homo sapiens ?
-
-
additional information no activity with 7mGpppA Severe acute respiratory syndrome-related coronavirus ?
-
-
S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA]
-
Homo sapiens S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
?
S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA]
-
Severe acute respiratory syndrome-related coronavirus S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
?
S-adenosyl-L-methionine + GpppAC4
-
Homo sapiens S-adenosyl-L-homocysteine + 7mGpppAC4
-
?
S-adenosyl-L-methionine + GpppAC4
-
Severe acute respiratory syndrome-related coronavirus S-adenosyl-L-homocysteine + 7mGpppAC4
-
?

Subunits

Subunits Comment Organism
? x * 60000, SDS-PAGE Homo sapiens
? x * 60000, SDS-PAGE Severe acute respiratory syndrome-related coronavirus

Synonyms

Synonyms Comment Organism
cap N7-MTase
-
Homo sapiens
cap N7-MTase
-
Severe acute respiratory syndrome-related coronavirus
cap-methyltransferase
-
Homo sapiens
cap-methyltransferase
-
Severe acute respiratory syndrome-related coronavirus
nsp14
-
Severe acute respiratory syndrome-related coronavirus
RNA N7-MTase
-
Homo sapiens
RNA N7-MTase
-
Severe acute respiratory syndrome-related coronavirus
RNMT
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000019
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 2,3,7,8-tetrahydroxy[1]benzopyrano[5,4,3-cde][1]benzopyran-5,10-dione
0.00005
-
at pH 8.0 and 30°C Homo sapiens 1,8-dihydroxyanthracen-9(10H)-one
0.000112
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus sinefungin
0.00032
-
at pH 8.0 and 30°C Homo sapiens 3,3',4',5,5',7-hexahaxdroxyflavone
0.0004
-
at pH 8.0 and 30°C Homo sapiens 3,3',4',5,7-pentahydroxyflavone
0.00074
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,3',4',5,5',7-hexahaxdroxyflavone
0.001
-
at pH 8.0 and 30°C Homo sapiens N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
0.00128
-
at pH 8.0 and 30°C Homo sapiens 1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
0.0013
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,3',4',5,7-pentahydroxyflavone
0.0015
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
0.002
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1,8-dihydroxyanthracen-9(10H)-one
0.0045
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus bis[6-(dimethylamino)-2-[(E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methylquinolin-1-ium] 4-[(3-carboxy-2-oxidonaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylate
0.0051
-
at pH 8.0 and 30°C Homo sapiens bis[6-(dimethylamino)-2-[(E)-2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methylquinolin-1-ium] 4-[(3-carboxy-2-oxidonaphthalen-1-yl)methyl]-3-hydroxynaphthalene-2-carboxylate
0.0055
-
at pH 8.0 and 30°C Homo sapiens 3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
0.0062
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
0.0073
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
0.0088
-
at pH 8.0 and 30°C Homo sapiens 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
0.0091
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
0.01
-
at pH 8.0 and 30°C Homo sapiens 3,4',5,7-tetrahydroxyflavone
0.011
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
0.0135
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
0.0137
-
at pH 8.0 and 30°C Homo sapiens 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
0.0143
-
at pH 8.0 and 30°C Homo sapiens 1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
0.0168
-
at pH 8.0 and 30°C Homo sapiens 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
0.0184
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus (2R,6S)-2,6-dimethyl-4-[2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine
0.0237
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,4',5,7-tetrahydroxyflavone
0.031
-
at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
0.03652
-
at pH 8.0 and 30°C Homo sapiens 2-(2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)ethan-1-ol
0.1022
-
at pH 8.0 and 30°C Homo sapiens (2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)acetic acid
0.159
-
at pH 8.0 and 30°C Homo sapiens 1-(diphenylmethyl)-4-methylpiperazine hydrochloride (1:1)
0.2268
-
at pH 8.0 and 30°C Homo sapiens 1-[(4-chlorophenyl)(phenyl)methyl]-4-methylpiperazine