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Literature summary for 2.7.7.49 extracted from

  • Himmel, D.M.; Myshakina, N.S.; Ilina, T.; Van Ry, A.; Ho, W.C.; Parniak, M.A.; Arnold, E.
    Structure of a dihydroxycoumarin active-site inhibitor in complex with the RNase H domain of HIV-1 reverse transcriptase and structure-activity analysis of inhibitor analogs (2014), J. Mol. Biol., 426, 2617-2631.
    View publication on PubMedView publication on EuropePMC
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Cloned(Commentary)

Cloned (Comment) Organism
-
 Human immunodeficiency virus type 1 BH10

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structure of inhibitor 6-([4-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile bound to the active site of an isolated RNase H domain of HIV-1 reverse transcriptase at a resolution limit of 1.71 A Human immunodeficiency virus type 1 BH10

Inhibitors

Inhibitors Comment Organism Structure
4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-7,8-dihydroxy-2H-chromen-2-one
-
 Human immunodeficiency virus type 1 BH10
6-([4-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile i.e. F3284-8495, a specific inhibitor of reverse transcriptase RNase H, with low micromolar potency in vitro Human immunodeficiency virus type 1 BH10

Organism

Organism UniProt Comment Textmining
Human immunodeficiency virus type 1 BH10 P03366
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0004
-
 RNase H activity, presence of 10 mM Mg2+, pH 8.0, temperature not specified in the publication Human immunodeficiency virus type 1 BH10 4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-7,8-dihydroxy-2H-chromen-2-one
0.0008
-
 RNase H activity, presence of 1 mM Mg2+, pH 7.4, temperature not specified in the publication Human immunodeficiency virus type 1 BH10 4-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-7,8-dihydroxy-2H-chromen-2-one
0.0011
-
 RNase H activity, presence of 10 mM Mg2+, pH 8.0, temperature not specified in the publication Human immunodeficiency virus type 1 BH10 6-([4-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile
0.0048
-
 RNase H activity, presence of 1 mM Mg2+, pH 7.4, temperature not specified in the publication Human immunodeficiency virus type 1 BH10 6-([4-[(4-cyanophenyl)amino]-1,3,5-triazin-2-yl]amino)-5,7-dimethylnaphthalene-2-carbonitrile