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Literature summary for 2.1.1.6 extracted from

  • Harrison, S.T.; Poslusney, M.S.; Mulhearn, J.J.; Zhao, Z.; Kett, N.R.; Schubert, J.W.; Melamed, J.Y.; Allison, T.J.; Patel, S.B.; Sanders, J.M.; Sharma, S.; Smith, R.F.; Hall, D.L.; Robinson, R.G.; Sachs, N.A.; Hutson, P.H.; Wolkenberg, S.E.; Barrow, J.C.
    Synthesis and evaluation of heterocyclic catechol mimics as inhibitors of catechol-O-methyltransferase (COMT) (2015), ACS Med. Chem. Lett., 6, 318-323 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.1.6

Crystallization (Commentary)

Crystallization (Comment) Organism
struktures of soluble isoforms in complex with inhibitors, S-adenosyl-L-methionine and Mg2+ Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4-butylphenyl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-3-hydroxypyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxy-2-methylpropyl)pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxybutyl)pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxyethyl)pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-methylpyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-phenylpyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-[hydroxy(phenyl)methyl]pyridin-4(1H)-one
-
 Homo sapiens
1-([1,1'-biphenyl]-4-yl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
-
 Homo sapiens
5-hydroxy-2-(thiophen-2-yl)pyrimidin-4(1H)-one
-
 Homo sapiens
9-hydroxypyrido[2,1-c][1,4]benzothiazin-8(6H)-one
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P21964
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000047
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-3-hydroxypyridin-4(1H)-one
0.000053
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-methylpyridin-4(1H)-one
0.000088
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-[hydroxy(phenyl)methyl]pyridin-4(1H)-one
0.000099
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxyethyl)pyridin-4(1H)-one
0.00014
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
0.00014
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-4-yl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
0.00016
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(4-butylphenyl)-5-hydroxy-2-(hydroxymethyl)pyridin-4(1H)-one
0.00018
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxy-2-methylpropyl)pyridin-4(1H)-one
0.0004
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 9-hydroxypyrido[2,1-c][1,4]benzothiazin-8(6H)-one
0.00057
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxybutyl)pyridin-4(1H)-one
0.00086
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-hydroxy-2-(thiophen-2-yl)pyrimidin-4(1H)-one
0.00087
-
 membrane-bound isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-phenylpyridin-4(1H)-one
0.001
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxybutyl)pyridin-4(1H)-one
0.0011
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-3-hydroxypyridin-4(1H)-one
0.0013
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-[hydroxy(phenyl)methyl]pyridin-4(1H)-one
0.0014
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxyethyl)pyridin-4(1H)-one
0.0019
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-(1-hydroxy-2-methylpropyl)pyridin-4(1H)-one
0.0021
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-methylpyridin-4(1H)-one
0.0025
-
 soluble isoform, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-([1,1'-biphenyl]-3-yl)-5-hydroxy-2-phenylpyridin-4(1H)-one