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Literature summary for 2.4.1.1 extracted from

  • Birch, A.M.; Kenny, P.W.; Oikonomakos, N.G.; Otterbein, L.; Schofield, P.; Whittamore, P.R.; Whalley, D.P.
    Development of potent, orally active 1-substituted-3,4-dihydro-2-quinolone glycogen phosphorylase inhibitors (2007), Bioorg. Med. Chem. Lett., 17, 394-399.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in comlex with inhibitor N-[1-(2-amino-2-oxoethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-2-methyl-6H-thieno[2,3-b]pyrrole-5-carboxamide, localization of two inhibitor molecules at the enzyme dimer interface Oryctolagus cuniculus

Inhibitors

Inhibitors Comment Organism Structure
2,3-dichloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.002 microM Homo sapiens
2,3-dichloro-N-(1-[3-hydroxy-2-(hydroxymethyl)propyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.038 microM Homo sapiens
2,3-dichloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.007 microM Homo sapiens
2-chloro-N-((3R)-1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.040 microM Homo sapiens
2-chloro-N-((3R)-1-[(2S)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.021 microM Homo sapiens
2-chloro-N-((3S)-1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.027 microM Homo sapiens
2-chloro-N-((3S)-1-[(2S)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.012 microM Homo sapiens
2-chloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.029 microM Homo sapiens
2-chloro-N-(1-[2-(methylsulfinyl)ethyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.048 microM Homo sapiens
2-chloro-N-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.041 microM Homo sapiens
2-chloro-N-[1-(2-hydroxybutyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.044 microM Homo sapiens
2-chloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.026 microM Homo sapiens
2-chloro-N-[1-(2-methoxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.05 microM Homo sapiens
2-chloro-N-[1-(3-hydroxypropyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.021 microM Homo sapiens
2-chloro-N-[1-(cyanomethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.028 microM Homo sapiens
5-chloro-N-(1-[(2R)-2,3-dihydroxypropyl]-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-1H-indole-2-carboxamide 50% inhibition at 0.044 microM Homo sapiens
5-chloro-N-[1-(2-hydroxyethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-1H-indole-2-carboxamide 50% inhibition at 0.017 microM Homo sapiens
methyl [3-([(2-chloro-6H-thieno[2,3-b]pyrrol-5-yl)carbonyl]amino)-2-oxo-3,4-dihydroquinolin-1(2H)-yl]acetate 50% inhibition at 0.084 microM Homo sapiens
N-[1-(2-amino-2-oxoethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-2-methyl-6H-thieno[2,3-b]pyrrole-5-carboxamide 50% inhibition at 0.135 microM Homo sapiens
N-[1-(2-amino-2-oxoethyl)-2-oxo-1,2,3,4-tetrahydroquinolin-3-yl]-2-methyl-6H-thieno[2,3-b]pyrrole-5-carboxamide
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Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
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recombinant enzyme
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Oryctolagus cuniculus
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Source Tissue

Source Tissue Comment Organism Textmining
muscle
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Oryctolagus cuniculus
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