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Literature summary 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

EC Number Inhibitors Comment Organism Structure
2.1.1.56 (2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)acetic acid
-
 Homo sapiens
2.1.1.56 (2R,6S)-2,6-dimethyl-4-[2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl]morpholine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1,8-dihydroxyanthracen-9(10H)-one
-
 Homo sapiens
2.1.1.56 1,8-dihydroxyanthracen-9(10H)-one
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
-
 Homo sapiens
2.1.1.56 1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1-(diphenylmethyl)-4-methylpiperazine hydrochloride (1:1)
-
 Homo sapiens
2.1.1.56 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
-
 Homo sapiens
2.1.1.56 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1-[(4-chlorophenyl)(phenyl)methyl]-4-methylpiperazine
-
 Homo sapiens
2.1.1.56 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
-
 Homo sapiens
2.1.1.56 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
-
 Homo sapiens
2.1.1.56 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
-
 Homo sapiens
2.1.1.56 1-[bis(4-fluorophenyl)methyl]-4-[(2Z)-3-phenylprop-2-en-1-yl]piperazine
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 2,3,7,8-tetrahydroxy[1]benzopyrano[5,4,3-cde][1]benzopyran-5,10-dione
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 2-(2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)ethan-1-ol
-
 Homo sapiens
2.1.1.56 3,3',4',5,5',7-hexahaxdroxyflavone
-
 Homo sapiens
2.1.1.56 3,3',4',5,5',7-hexahaxdroxyflavone
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 3,3',4',5,7-pentahydroxyflavone
-
 Homo sapiens
2.1.1.56 3,3',4',5,7-pentahydroxyflavone
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 3,4',5,7-tetrahydroxyflavone
-
 Homo sapiens
2.1.1.56 3,4',5,7-tetrahydroxyflavone
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
-
 Homo sapiens
2.1.1.56 3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 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
2.1.1.56 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
2.1.1.56 N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
-
 Homo sapiens
2.1.1.56 N-(2-[[(4-methoxyphenyl)methyl](pyrimidin-2-yl)amino]ethyl)-N,N-dimethylhexadecan-1-aminium
-
 Severe acute respiratory syndrome-related coronavirus
2.1.1.56 sinefungin 98.2% inhibition at 0.05 mM Homo sapiens
2.1.1.56 sinefungin 98.2% inhibition at 0.05 mM Severe acute respiratory syndrome-related coronavirus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.1.1.56 S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA] Homo sapiens
-
 S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
 ?
2.1.1.56 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

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

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.1.1.56 additional information no activity with 7mGpppA Homo sapiens ?
-
-
2.1.1.56 additional information no activity with 7mGpppA Severe acute respiratory syndrome-related coronavirus ?
-
-
2.1.1.56 S-adenosyl-L-methionine + a 5'-(5'-triphosphoguanosine)-[mRNA]
-
 Homo sapiens S-adenosyl-L-homocysteine + a 5'-(N7-methyl 5'-triphosphoguanosine)-[mRNA]
-
 ?
2.1.1.56 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]
-
 ?
2.1.1.56 S-adenosyl-L-methionine + GpppAC4
-
 Homo sapiens S-adenosyl-L-homocysteine + 7mGpppAC4
-
 ?
2.1.1.56 S-adenosyl-L-methionine + GpppAC4
-
 Severe acute respiratory syndrome-related coronavirus S-adenosyl-L-homocysteine + 7mGpppAC4
-
 ?

Subunits

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

Synonyms

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.1.1.56 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
2.1.1.56 0.00005
-
 at pH 8.0 and 30°C Homo sapiens 1,8-dihydroxyanthracen-9(10H)-one
2.1.1.56 0.000112
-
 at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus sinefungin
2.1.1.56 0.00032
-
 at pH 8.0 and 30°C Homo sapiens 3,3',4',5,5',7-hexahaxdroxyflavone
2.1.1.56 0.0004
-
 at pH 8.0 and 30°C Homo sapiens 3,3',4',5,7-pentahydroxyflavone
2.1.1.56 0.00074
-
 at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,3',4',5,5',7-hexahaxdroxyflavone
2.1.1.56 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
2.1.1.56 0.00128
-
 at pH 8.0 and 30°C Homo sapiens 1-(4-tert-butylphenyl)-N-methyl-N-[(naphthalen-1-yl)methyl]methanamine
2.1.1.56 0.0013
-
 at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,3',4',5,7-pentahydroxyflavone
2.1.1.56 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
2.1.1.56 0.002
-
 at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 1,8-dihydroxyanthracen-9(10H)-one
2.1.1.56 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
2.1.1.56 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
2.1.1.56 0.0055
-
 at pH 8.0 and 30°C Homo sapiens 3,8-diamino-5-[3-[diethyl(methyl)azaniumyl]propyl]-6-phenylphenanthridin-5-ium
2.1.1.56 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
2.1.1.56 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
2.1.1.56 0.0088
-
 at pH 8.0 and 30°C Homo sapiens 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
2.1.1.56 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
2.1.1.56 0.01
-
 at pH 8.0 and 30°C Homo sapiens 3,4',5,7-tetrahydroxyflavone
2.1.1.56 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
2.1.1.56 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
2.1.1.56 0.0137
-
 at pH 8.0 and 30°C Homo sapiens 1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
2.1.1.56 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
2.1.1.56 0.0168
-
 at pH 8.0 and 30°C Homo sapiens 1-(diphenylmethyl)-4-[(2E)-3-phenylprop-2-en-1-yl]piperazine
2.1.1.56 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
2.1.1.56 0.0237
-
 at pH 8.0 and 30°C Severe acute respiratory syndrome-related coronavirus 3,4',5,7-tetrahydroxyflavone
2.1.1.56 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
2.1.1.56 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
2.1.1.56 0.1022
-
 at pH 8.0 and 30°C Homo sapiens (2-[4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl]ethoxy)acetic acid
2.1.1.56 0.159
-
 at pH 8.0 and 30°C Homo sapiens 1-(diphenylmethyl)-4-methylpiperazine hydrochloride (1:1)
2.1.1.56 0.2268
-
 at pH 8.0 and 30°C Homo sapiens 1-[(4-chlorophenyl)(phenyl)methyl]-4-methylpiperazine