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Literature summary for 2.7.7.49 extracted from

  • Rajotte, D.; Tremblay, S.; Pelletier, A.; Salois, P.; Bourgon, L.; Coulombe, R.; Mason, S.; Lamorte, L.; Sturino, C.F.; Bethell, R.
    Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor series (2013), Antimicrob. Agents Chemother., 57, 2712-2718.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
4-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-(3-methoxypropyl)-8-(1-methyl-1H-pyrazol-4-yl)-2,5-dihydro-1H-indeno[1,2-d]pyrimidine inhibits HIV-1 reverse transcriptase in a primer extension assay but has no measurable activity against human DNA polymerase gamma at 0.01 mM. It potently inhibits HIV-1 replication in vitro with 1.5 nM 50% effective concentration. The antiviral potency is unaffected by the presence of nonnucleotide RT inhibitor mutations L100I, K103N/Y181C, V106A, or Y188L. Viruses encoding K65R are hypersusceptible to inhibition by the compound, and it retains full activity against viruses encoding M184V. A recombinant virus encoding the RT W153L is highly resistant Human immunodeficiency virus 1

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus 1
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000026
-
pH 7.8, 37°C Human immunodeficiency virus 1 4-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-(3-methoxypropyl)-8-(1-methyl-1H-pyrazol-4-yl)-2,5-dihydro-1H-indeno[1,2-d]pyrimidine