3.1.26.13: retroviral ribonuclease H
This is an abbreviated version!
For detailed information about retroviral ribonuclease H, go to the full flat file.
Word Map on EC 3.1.26.13
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3.1.26.13
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integrase
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hiv-rt
-
rna-dna
-
template-primer
-
moloney
-
polypurine
-
transcriptases
-
minus-strand
-
3'-azido-3'-deoxythymidine
-
nnrti
-
primer-template
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nonnucleoside
-
drug development
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medicine
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analysis
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pharmacology
- 3.1.26.13
-
integrase
- hiv-rt
- rna-dna
-
template-primer
-
moloney
-
polypurine
- transcriptases
-
minus-strand
- 3'-azido-3'-deoxythymidine
-
nnrti
-
primer-template
-
nonnucleoside
- drug development
- medicine
- analysis
- pharmacology
Reaction
Endohydrolysis of RNA in RNA/DNA hybrids. Three different cleavage modes: 1. sequence-specific internal cleavage of RNA. Human immunodeficiency virus type 1 and Moloney murine leukemia virus enzymes prefer to cleave the RNA strand one nucleotide away from the RNA-DNA junction. 2. RNA 5'-end directed cleavage 13-19 nucleotides from the RNA end. 3. DNA 3'-end directed cleavage 15-20 nucleotides away from the primer terminus. =
Synonyms
HIV reverse transcriptase ribonuclease H, HIV reverse transcriptase-associated RNase H, HIV RNase H, HIV RT RNaseH, HIV RT-associated RNase H, HIV-1 reverse transcriptase, HIV-1 reverse transcriptase ribonuclease H, HIV-1 reverse transcriptase RNase H, HIV-1 RH, HIV-1 ribonuclease H, HIV-1 ribonuclease H domain, HIV-1 RNase H, HIV-1 RT-associated RNase H, human immunodeficiency virus reverse transcriptase, human immunodeficiency virus reverse transcriptase-associated ribonuclease H, human immunodeficiency virus reverse transcriptase-associated RNase H, human immunodeficiency virus RT-associated RNase H, M-MuLV RT RNase H, reverse transcriptase, reverse transcriptase-associated ribonuclease H, reverse transcriptase-associated RNase H, reverse-transcriptase-associated ribonuclease H, ribonuclease H, ribonuclease H domain in HIV-1 reverse transcriptase, RNase H, RNase H activity of HIV-1 reverse transcriptase, RNase H domain of HIV-1 reverse transcriptase, RNase H of HIV-1 subtype C, RNaseH, RNH, RNHHIV, RT RNase H, RT-RNase H
ECTree
3.1.26.13 retroviral ribonuclease HAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.1.26.13 - retroviral ribonuclease H
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
(2S)-5,7-dihydroxy-2-(2-hydroxy-1-(phenylsulfonyl)propan-2-yl)-9-methyl-3,4-dihydro-1H-benzo[7]annulen-6(2H)-one
-
-
(2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoic acid
-
-
(4-N,N-dimethylaminobenzoyl)-2-hydroxy-1-naphthyl hydrazone
-
specific
(5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
-
(5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoic acid
-
-
(6,6,12,12,18,18,18-heptaoxido-5,7,11,13,17-pentaoxa-6l5,12l5,18l5-triphosphaoctadec-1-yl)phosphonate
-
-
1,2-bis[(3-oxobutan-2-yl)oxy]anthracene-9,10-dione
-
20% inhibition
1,2-dihydroxyanthracene-9,10-dione
-
i.e. alizarine, 8% inhibition
1,6-bis[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1,6-dibenzyl-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-(3-[[(4-benzyl-5-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]methyl]-4-methoxyphenyl)ethanone
-
-
1-(ethoxymethyl)-3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
1-(ethoxymethyl)-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-benzyl-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
1-hydroxy-4-((4-(morpholinomethyl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-((4-(pyridin-4-yl)phenyl)amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[3-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[3-(4-morpholinylmethyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[4-(4-morpholinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-([[4-(4-pyridinyl)phenyl]methyl]amino)pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[4-(quinolin-3-yl)anilino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[[4-(4-morpholinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
-
1-hydroxy-4-[[4-(quinolin-3-yl)phenyl]amino]pyrido[2,3-d]pyrimidin-2(1H)-one
-
GSK5724, exceptional RNase H inhibitory potency
1-[([1,1'-biphenyl]-4-yl)methyl]-5-hydroxy-4-oxo-1,4-dihydropyridine-3-carboxylic acid
-
-
1-[[(4-fluorophenyl)methoxy]methyl]-6-[(4-fluorophenyl)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
10,12,15,16-tetrahydroxy-8-methoxy-11-methyl-2-phenyl-6,7-dihydrotetraceno[1,2-g]phthalazine-1,9,14(2H)-trione
-
-
2',3'-dideoxy-3'-triaz-2-en-2-ium-3-id-1-yl-3,4-dihydrothymidine
-
-
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-guanosine
-
40% inhibition of RNase H at 0.05 microM
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-[2-(4-nitrophenyl)ethyl]guanosine
-
69% inhibition of RNase H at 0.05 microM
2'-deoxy-P-thioguanylyl-(3'->5')-guanosine
-
65% inhibition of RNase H at 0.05 microM
-
2,3,7-trihydroxy-6-(3-nitrobenzyl)cyclohepta-2,4,6-trien-1-one
-
-
2,6-dimethoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2,7-dihydroxy-4-isopropyl-cyclohepta-2,4,6-triene
-
i.e. beta-thujaplicinol
2,7-dihydroxy-4-methyl-5-(2-methylbutanoyl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(4-nitrophenyl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(naphthalen-1-yl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-(naphthalen-2-yl)cyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-phenylcyclohepta-2,4,6-trien-1-one
-
2,7-dihydroxy-4-methyl-5-[4-(trifluoromethyl)phenyl]cyclohepta-2,4,6-trien-1-one
-
2-(1,2-dihydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(1-benzylamino-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2,3-dihydro-1H-inden-1-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-(2,3-dihydro-1H-inden-2-ylamino)-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-(2,4-dichlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-(2-fluorophenyl)acetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-benzylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-bromobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chloro-4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-cyclohexylacetamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-diethylamino-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-ethanesulfonyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-ethylsulfanyl-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylic acid
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-methylbenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(2-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3,5-dimethylphenyl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)acetonitrile
-
-
2-(3-bromo-4-methoxybenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
inhibition of enzymatic activity, but no antiviral effect
2-(3-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(3-phenylpropanamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-aminobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-chlorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-fluorobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-(4-nitrobenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-([1,1'-biphenyl]-4-yl)-2-(3-(ethoxymethyl)-1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydro pyrimidin-4-yl)acetonitrile
-
-
2-acetamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-amino-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
-
-
2-amino-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-benzamido-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-hydroxy-(4H)-isoquinoline-1,3-dione
-
inhibits RNase H in vitro with submicromolar potency
2-hydroxy-4-(2-phenyl)ethylisoquinoline-1,3(2H,4H)-dione
-
enol-form
2-hydroxy-4-(3-phenyl)propylisoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-(4-methylbenzyl)isoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-(4-trifluoromethylbenzyl)isoquinoline-1,3(2H-4H)-dione
-
keto-form
2-hydroxy-4-butylisoquinoline-1,3(2H,4H)-dione
-
mixture of th mixed ketoenol forms or keto-form
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H, 4H)-dione
-
inhibits RNase H in vitro with nanomolar potency
2-hydroxy-4-methoxycarbonylisoquinoline-1,3(2H,4H)-dione
-
shows antiviral activity
2-hydroxy-6-methoxy-N-(3-(pyridin-2-ylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)nicotinamide
Human immunodeficiency virus type 1 group M subtype B
-
2-oxo-2-(1,2,3,4-tetrahydronaphthalen-1-ylamino)ethyl 5-nitrofuran-2-carboxylate
-
-
2-oxo-2-(tetrahydrofuran-2-ylamino)ethyl 5-nitrofuran-2-carboxylate
-
-
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl benzyl(phenyl)carbamodithioate
-
-
2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl dibenzylcarbamodithioate
-
-
2-oxo-2-[(2-phenylpropan-2-yl)amino]ethyl 5-nitrofuran-2-carboxylate
-
-
2-[(2,3,4-trichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[(2,4-dichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
-
2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[(2-bromo-5-chloro-1-benzothiophen-3-yl)methyl]-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-[(2-methoxy-5-methylphenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
-
-
2-[(2-methyl-1-phenylpropan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(2-methylbutan-2-yl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(3,4-dichlorophenyl)methyl]-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-[(3-cyanophenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate
-
-
2-[(3-cyanophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate
-
-
2-[(4-hydroxybenzyl)(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[(cyclohexanecarbonyl)amino]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[2-(2-fluoro-benzylamino)-1-hydroxy-1-methyl-ethyl]-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
2-[2-(4-bromophenyl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
-
-
2-[2-(biphenyl-4-yl)-2-oxoethoxy]-9,10-dioxo-9,10-dihydroanthracen-1-yl acetate
-
-
2-[3-(4-chlorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[3-(4-fluorophenyl)propanamido]-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine
-
inhibitor indentified by FRET-based high-throughput screening assay
2-[4-benzyl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridine
-
-
2-[benzyl(tetrahydrofuran-2-ylmethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[bis(4-methoxyphenyl)(phenyl)methoxy]ethyl 2-cyanoethyl dipropan-2-ylphosphoramidoite
-
-
2-[tert-butyl(2-phenylethyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-oxo-3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(3-phenylpropyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-fluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-methoxybenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(4-nitrobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(pentafluorobenzyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl(phenyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[2-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[3-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[tert-butyl[4-(trifluoromethyl)benzyl]amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[2-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[4-(acetyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
2-[[4-(benzyloxy)benzyl](tert-butyl)amino]-2-oxoethyl 5-nitrofuran-2-carboxylate
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
-
-
3'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
-
-
3'-[(E)-[2-(3,4,5-trihydroxybenzoyl)hydrazinylidene]methyl]biphenyl-4-carboxylic acid
-
-
3,4-dihydroxy-N'-[(E)-(2-methoxynaphthalen-1-yl)methylidene]benzohydrazide
-
-
3,9,11,14,15-pentahydroxy-7-methoxy-10-methyl-5,6-dihydrobenzo[9,10]tetrapheno[2,3-c]furan-1,8,13(3H)-trione
-
-
3-(benzyloxy)-6-((2'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-(furan-2-yl)-4-(4-methoxybenzyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
-
3-(furan-2-yl)-4-phenyl-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole
-
-
3-cyclopentyl-1,4-dihydroxy-1,8-naphthyridin-2(1H)-one
-
3-hydroxy-1,5,6,7-tetrahydro-2H-cyclopenta[4,5]thieno[2,3-d]pyrimidine-2,4(3H)-dione
-
-
3-hydroxy-1-methyl-6-((3-(pyrimidin-5-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((3-(tetrahydrofuran-3-yl)phenyl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-oxy)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-1-methyl-6-(4-(pyridin-4-yl)phenoxy)pyrimidine-2,4-(1H,3H)-dione
-
-
3-hydroxy-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrobromide
-
-
3-hydroxy-5,6-dimethylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5-methyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidine-6-carboxylic acid
-
-
3-hydroxy-5-methylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-5-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((2-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((3-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-2-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-hydroxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-2-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)amino)-pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-3-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)amino)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)oxy)-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methoxy-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4'-methyl-[1,1'-biphenyl]-4-yl)amino)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-(trifluoromethyl)phenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-hydroxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-methoxyphenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((4-nitrophenyl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-((40-methyl-[1,1'-biphenyl]-4-yl)thio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4'-(trifluoromethyl)-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4'-methoxy-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(4-(trifluoromethyl)benzoyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(40-methyl-[1,10-biphenyl]-4-carbonyl)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-(naphthalen-1-ylthio)pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-phenylthieno [3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-hydroxy-6-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
3-[2-(4-bromophenyl)-2-oxoethoxy]-1,8-dihydroxy-6-methylanthracene-9,10-dione
-
-
3-[4-(2-methyl-imidazo[4,5-c]pyridin-1-yl)-benzyl]-3H-benzothiazol-2-one
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-3-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)amino)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-3-carbonitrile
-
-
4'-((1-hydroxy-3-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)oxy)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-((3-(ethoxymethyl)-1-hydroxy-5-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)methyl)-[1,1'-biphenyl]-4-carbonitrile
-
-
4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,1'-biphenyl]-4-carbonitrile
-
-
4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
4-((cyclopropylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(([1,1'-biphenyl]-4-ylmethyl)amino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(3-bromophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(4,4-difluoropiperidin-1-yl)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-(4-bromophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(4-chlorophenyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(cyclohexanecarbonyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-(cyclohexylacetyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-carbonyl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-yl)-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxy-1,8-naphthyridin-2(1H)-one
Human immunodeficiency virus type 1 group M subtype B
-
4-([1,1'-biphenyl]-4-ylamino)-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-([[4-benzyl-5-(furan-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
-
4-acetyl-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-benzoyl-2,7-dihydroxy-5-methylcyclohepta-2,4,6-trien-1-one
-
4-benzyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
keto-form; mixture of th mixed ketoenol forms
4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-(furan-2-yl)-5-[(4-methoxybenzyl)sulfanyl]-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(furan-2-yl)-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole
-
inhibitor indentified by FRET-based high-throughput screening assay
4-hexyl-2-hydroxy-isoquinoline-1,3(2H,4H)-dione
-
keto-form; mixture of th mixed ketoenol forms
4-tert-butyl-N'-[(E)-(2-hydroxynaphthalen-1-yl)methylidene]benzohydrazide
-
-
4-[1-4-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)-piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
35% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
72% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(dimethylamino)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
26% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(morpholin-4-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
0.7% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
22% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-acetylpiperazin-1-yl)-4-(1h)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
30% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
34% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-ethylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
63% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
44% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(N-methylpiperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
41% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
44% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(piperazin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid ethyl ester
-
18% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-(thiomorpholin-1-yl)-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
74% inhibition at 0.01 mM
4-[1-[(4-fluorophenyl)methyl]-7-[N-(3-chloroprop-1-yl)piperazin-1-yl]-4-(1H)-quinolinon-3-yl]-2-hydroxy-4-oxo-2-butenoic acid
-
78% inhibition at 0.01 mM
4-[[(4-fluorophenyl)methyl]amino]-1-hydroxypyrido[2,3-d]pyrimidin-2(1H)-one
-
-
4-[[4'-(aminomethyl)biphenyl-4-yl]methyl]-1-hydroxy-1,8-naphthyridin-2(1H)-one
-
-
4-[[4'-(aminomethyl)[1,1'-biphenyl]-4-yl]methyl]-1-hydroxy-1,8-naphthyridin-2(1H)-one
-
-
4-[[4-([4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl]amino)pyrimidin-2-yl]amino]benzonitrile
-
i.e. TMC278 or rilpivirine, enzyme-bound structure, overview
5,6-dimethyl-2-(4-nitrophenyl)thieno[2,3-d]pyrimidin-4(3H)-one
Human immunodeficiency virus type 1 group M subtype B
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylaminoethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-phenylsulfanylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-piperidin-1-ylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-2-imadazol-1-yl-1-methyl ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-(1-hydroxy-ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
-
5,7-dihydroxy-2-isopropenyl-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
i.e. manicol, the alpha-hydroxytroplone potently and specifically inhibits HIV RT ribonuclease H, enzyme-bound structure, overview
5-(1,1-dioxido-1,2-thiazinan-2-yl)-N-(4-fluorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
-
5-(4-chlorophenyl)-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
5-benzyl-6-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-bromo-6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-ethyl-1-(((4-fluorobenzyl)oxy)methyl)-6-(4-fluorophenyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
6-( (3'- fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-bis(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dichloro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-difluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2',4'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2',6'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((2-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((2-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',4'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',4'-dimethoxy-[1,10-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-3-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((3',5'-dimethoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-5'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-[1,1'-biphenyl ] - 4 -yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-4'-methoxy-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((3-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-3'-fluoro-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl ]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-2-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)oxy)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-chloro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-3-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)methyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-3'-methyl-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-2-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)amino)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-3-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4'-fluoro-[1,1'-biphenyl]-4-yl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-(3,5-dimethylisoxazol-4-yl)phenyl)amino)-3-hydroxy-1-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-((4-bromophenyl)thio)-3-hydroxy-5-iodopyrimidine-2,4(1H,3H)-dione
-
-
6-((4-bromophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-chlorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-ethylphenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-((4-fluorophenyl)thio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3',4'-dimethoxy-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3',5'-dimethyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(3,5-dimethylbenzoyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-chloro-3'-fluoro-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-fluoro-3'-methyl-[1,10-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4'-fluoro-[1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-(4-chlorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-(4-fluorophenyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-2-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-3-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-carbonyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-carbonyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-yl)-1-(ethoxymethyl)-3-hydroxy-5-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylamino)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylmethyl)-1-(ethoxymethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylmethyl)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-yloxy)-3-hydroxy-1-methylpyrimidine-2,4-(1H,3H)-dione
-
-
6-([1,1'-biphenyl]-4-ylthio)-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methoxypyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(((4-fluorobenzyl)oxy)methyl)-5-isopropyl-3-methylpyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-(ethoxymethyl)-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[(benzyloxy)methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[2-(4-fluorophenyl)ethyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[3-(4-fluorophenyl)propyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[4-(4-fluorophenyl)butyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(2,4-difluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(3-chloro-2-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[(4-fluorophenyl)methoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[3-(4-fluorophenyl)propoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-1-[[4-(4-fluorophenyl)butoxy]methyl]-3-hydroxy-5-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione
-
-
6-benzyl-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
-
6-[(4'-chloro[1,1'-biphenyl]-3-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)amino]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)methyl]-2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)methyl]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)oxy]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[([1,1'-biphenyl]-4-yl)sulfanyl]-3-hydroxypyrimidine-2,4(1H,3H)-dione
-
-
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl)]-2,4-dioxo-5-hexenoic acid ethyl ester
-
i.e. RDS1643, RNase H inhibitor
6-[1-(4-fluorophenyl)methyl-1H-pyrrol-2-yl]-2,4-dioxo-5-hexenoic acid ethyl ester
-
i.e. RDS-1643, shows relatively weak but selective inhibitory activity against RNase H
6-[4-(diethylamino)phenoxy]-3-[ethoxy(hydroxy)methyl]-1,4-dihydroxy-1,8-naphthyridin-2(1H)-one
-
7-benzyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
7-benzyl-3-hydroxyhexahydropyrido[3,4-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
7-ethyl-3-hydroxy-5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione hydrochloride
-
-
9,10-dioxo-2-(2-oxo-2-phenylethoxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-(2-oxopropoxy)-9,10-dihydroanthracen-1-yl acetate
-
10% inhibition
9,10-dioxo-2-(prop-2-en-1-yloxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-(prop-2-yn-1-yloxy)-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-2-[(2-oxopentan-3-yl)oxy]-9,10-dihydroanthracen-1-yl acetate
-
inhibits the RNase H function and is inactive on the DNA polymerase function
9,10-dioxo-2-[(3-oxobutan-2-yl)oxy]-9,10-dihydroanthracen-1-yl acetate
-
-
9,10-dioxo-9,10-dihydroanthracene-1,2-diyl diacetate
-
12% inhibition
actinomycin D
-
limits the enzyme to the first strand synthesis
delaviridine
-
a nonnucleoside reverse transcriptase inhibitor
Dextran sulfate
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 0.1 nM
-
dimethyl 3-(chloromethyl)-5,7-dihydroxy-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
dimethyl 5,7-dihydroxy-3-(methoxymethyl)-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
dimethyl 5,7-dihydroxy-3-methyl-6-oxocyclohepta-2,4,7-triene-1,2-dicarboxylate
-
ethyl (2Z)-4-[1-(4-fluorobenzyl)-4-oxo-7-(pyrrolidin-1-yl)-1,4-dihydroquinolin-3-yl]-2-hydroxy-4-oxobut-2-enoate
-
-
ethyl (5E)-6-[1-(2,4-dimethylbenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(2-chlorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
selectively inhibits RNase H activity in the low micromolar range
ethyl (5E)-6-[1-(3-methoxybenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-2-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
-
ethyl (5E)-6-[1-(4-fluorobenzyl)-4-phenyl-1H-pyrrol-3-yl]-2,4-dioxohex-5-enoate
-
-
ethyl 2-(2-fluorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 2-(4-chlorobenzamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
ethyl 4,6-dihydroxy-2,7-dimethyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
ethyl 4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
F3284-8495
-
specific inhibitor with low micromolar potency in vitro
guanylyl-(3'->5')-guanosine
-
89% inhibition of RNase H at 0.05 microM
manicol
source of manicol is the root bark of a rare Guyanan tree, Dulacia guianeinsis
methyl 2-hydroxy-1,3-dioxo-1,2,3,4-tetrahydroisoquinoline-4-carboxylate
-
-
methyl 4'-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)-[1,10-biphenyl]-4-carboxylate
-
-
methyl 4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
methyl 4-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 4-(1-hydroxy-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carbonyl)benzoate
-
-
methyl 4-amino-1-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
Human immunodeficiency virus type 1 group M subtype B
-
methyl 7-bromo-4,6-dihydroxy-2-methyl-5-oxocyclohepta-1,3,6-triene-1-carboxylate
-
N-(3-((2-fluorophenyl)carbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-yl)picolinamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(4-chlorobenzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamide
-
-
N-(pyridin-2-yl)-2-(thiophene-2-carboxamido)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
N-(pyridin-2-yl)-2-[2-(quinolin-6-yl)acetamido]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide
Human immunodeficiency virus type 1 group M subtype B
-
NaCl
-
inhibits substrate binding by the enzyme, in the samples that are pretreated with DTT, the addition of salt strongly inhibits the reaction and completely eliminates off-register cleavage
P-thioguanylyl-(3'->5')-guanosine
-
50% inhibition of RNase H at 0.05 microM
-
tenofovir disoproxil
-
a nucleoside reverse transcriptase inhibitor
xylan polysulfate
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 8 nM
-
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
-
61% inhibition of RNase H at 0.05 microM
2'-deoxy-2'-fluoro-P-thioadenylyl-(3'->5')-N-naphthalen-1-ylguanosine
-
11% inhibition of RNase H at 0.05 microM
2,7-dihydroxy-4-(propan-2-yl)cyclohepta-2,4,6-trien-1-one
-
inhibition of enzymatic activity, but no antiviral effect
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
inhibition of enzymatic activity, but no antiviral effect
2-(3,4-dichlorobenzyl)-5,6-dihydroxypyrimidine-4-carboxylic acid
-
-
2-hydroxyisoquinoline-1,3(2H,4H)-dione
-
inhibition of enzymatic activity, but no antiviral effect
2-hydroxyisoquinoline-1,3(2H,4H)-dione
an active site directed inhibitor, stabilizes RH domain helix E
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
inhibitor indentified by FRET-based high-throughput screening assay
4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine
-
-
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
-
inhibitor has little effect on bacterial RNase H activity in vitro
5-nitrofuran-2-carboxylic acid adamantan-1-carbamoyl methyl ester
-
-
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
-
additionally inhibits HIV-1 replication effectively. Inhibitor has little effect on bacterial RNase H activity in vitro
5-nitrofuran-2-carboxylic acid [[4-(4-bromophenyl)-thiazol-2-yl]-(tetrahydrofuran-2-ylmethyl)-carbamoyl]-methyl ester
-
-
beta-thujaplicinol
slow-binding RNase H inhibitor with noncompetitive kinetics that forms a tropylium ion that interacts favorably with reverse transcriptase and the RNA:DNA substrate
beta-thujaplicinol
-
shows submicromolar inhibitory activity against RNase H
beta-thujaplicinol
a non-competitive inhibitor of RNase H
efavirenz
-
second generation non-nucleoside reverse transcriptase inhibitor, shows the effect of simultaneously reorienting domain motions and obstructing the p66 thumb fluctuations
efavirenz
-
stronger effect of mutation N348I on RNase H susceptibility to nevirapine as compared with efavirenz
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
interactions between MK1 and two Mn2+ ions, which are coordinated by the RNase H active site residues D443, E478, D498, and D549, binding structure, overview. In addition, G444, S499, A538, H539, V552, and S553 contribute to the binding site
ethyl 1,4-dihydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxylate
-
-
heparin
-
more potent inhibitor of RNase H than of reverse transcriptase. 50% infective dose corresponds to 0.5-1.5 nM
heparin
-
inhibits substrate binding by the enzyme, in the samples that are pretreated with DTT, the addition of heparin strongly inhibits the reaction and completely eliminates off-register cleavage
nevirapine
-
non-nucleoside RT inhibitors such as nevirapine interfere directly with the global hinge-bending mechanism that controls the cooperative motions of the p66 fingers and thumb subdomains. The net effect of nevirapine binding is to change the direction of domain movements rather than suppress their mobilities
nevirapine
-
a non-nucleoside RT inhibitor, NNRTI, stronger effect of mutation N348I on RNase H susceptibility to nevirapine as compared with efavirenz
nevirapine
a nonnucleoside reverse transcriptase inhibitor, NNRTI
NSC727447
-
mutation T473C increases sensitivity of the enzyme for NSC727447 by 50fold
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
-
additionally inhibits DNA strand transfer and DNA polymerase activity of the retroviral reverse transcriptase
[2-(4-chlorophenyl)hydrazinylidene]propanedioic acid
-
inhibits RNase H activity, does not significantly affect DNA polymerase activity of reverse transcriptase. In the absence of DNA synthesis, [2-(4-chlorophenyl)hydrazinylidene]propanedioic acid interferes with the translocation, or repositioning, of the enzyme on the RNA-DNA template duplex. Inhibitor is highly specific for human immunodeficiency virus. The dicarboxylic acid moiety is essential for activity, and Mg2+ chelates directly with a Kd value of 2.4 mM
additional information
-
synthesis of 2-hydroxyisoquinoline-1,3(2H,4H)-dione derivatives as inhibitors of the RNase H activity of the reverse transcriptase of HIV-1, docking, study, overview. No inhibition by keto-5i and 5l
-
additional information
-
antiretroviral drugs inhibit the reverse-transcriptase (RT) of HIV. The differences between HIV-1 and HIV-2 RTs explain why some of the anti-HIV-1 drugs are not effective against HIV-2. One major difference between the two HIV RTs is the low ribonuclease H (RNase H) activity of HIV-2 RT relative to HIV-1 RT
-
additional information
-
identification and evaluation of thiocarbamate and triazole inhibitors targeting RNase H activity of HIV reverse transcriptase, overview
-
additional information
-
design, synthesis, and screening of derivatives of 5-nitro-furan-2-carboxylic acid as inhibitors of the RNAse H activity of HIV-1 reverse transcriptase, overview. Modulation of the 5-nitro-furan-2-carboxylic moiety results in a drastic decrease in inhibitory potency. Binding mode of active derivatives, in which three oxygen atoms aligned in a straight form at the nitro-furan moiety are coordinated to two divalent metal ions located at RNase H reaction site. The nitro-furan-carboxylic moiety is one of the critical scaffolds for RNase H inhibition. Cytotoxicity of the synthesized compounds, overview
-
additional information
-
non-nucleoside RT inhibitors, NNRTIs, bind to an allosteric site that is 10 A from the polymerase active site and 60 A from the RNase H active site
-
additional information
-
no inhibition by 5,7-dihydroxy-2-(1-hydroxy-1-methyl-2-piperidin-1-ylethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, 5,7-dihydroxy-2-(1-hydroxy-2-imadazol-1-yl-1-methyl ethyl)-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, 2-(2-diethylamino-1-hydroxy-1-methyl-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one, and 2-(1-benzylamino-ethyl)-5,7-dihydroxy-9-methyl-1,2,3,4-tetrahydrobenzocyclohepten-6-one
-
additional information
structures of naphthyridinone-containing inhibitors bound to the RNase H active site, overview. This class of compounds binds to the active site via two metal ions that are coordinated by catalytic site residues, D443, E478, D498, and D549. The directionality of the naphthyridinone pharmacophore is restricted by the ordering of D549 and H539 in the RNase H domain
-
additional information
-
C-terminal domain mutations reduce RNase H activity either directly by affecting the RNase H cleavage activity of the enzyme, or indirectly by affecting the overall positioning of the template/primer strand, which in turn affects RNase H activity, template switching, polymerization and/or nucleotide excision. Effects of enzyme mutations on treatment with nucleoside reverse transcriptase inhibitors and nonnucleoside reverse transcriptase inhibitors, detailed overview. Nucleoside reverse transcriptase inhibitors are nucleoside analogues that lack the 3' OH on the sugar ring and competitively block reverse transcription by causing chain termination during DNA polymerization. Nucleoside reverse transcriptase inhibitors are prodrugs that require intracellular phosphorylation to the 5'-triphosphate formed by host cell kinases in order to become active. Nonnucleoside reverse transcriptase inhibitors in general are non-competitive inhibitors of RT that bind to a hydrophobic pocket near the polymerase active site, inducing conformational changes that inhibit RT enzymatic activity. Inhibition mechanisms of the two inhibitor classes, overview
-
additional information
-
mechanisms of catalysis and drug inhibition of polymerase and RNase H functions of RT by nucleos(t)ide reverse transcriptase inhibitor and non-nucleoside reverse transcriptase inhibitor drugs, and molecular mechanisms of drug resistance, detailed overview
-
additional information
-
discovery and development of bona fide RNase H inhibitors, overview
-
additional information
-
design, synthesis and biological evaluations of N-hydroxy thienopyrimidine-2,4-diones as inhibitors of HIV reverse transcriptase-associated RNase H, antiviral activity, overview. The compounds potently and selectively inhibit RNase H with considerable potency against HIV-1 in cell culture. They also show inhibition of integrase strand transfer (INST) activity. Structure-activity-relationship analysis. Molecular modeling of analogues 3-hydroxy-6-phenylthieno[2,3-d]pyrimidine-2,4(1H,3H)-dione and 5-(4-chlorophenyl)-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione at the RNase H active site. Analysis of the enzyme's crystal structure in complex with inhibitor 6-benzyl-3-hydroxythieno[2,3-d]pyrimidine-2,4(1H,3H)-dione
-
additional information
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major chemotypes reported as HIV RNase H active site inhibitors, overview. Design, synthesis, biochemical and antiviral evaluations of a 6-arylthio subtype of the 3-hydroxypyrimidine-2,4-dione (HPD) chemotype as inhibitors of the enzyme. The analogues inhibit RT RNase H in single-digit nanomolar range without inhibiting RT polymerase (pol) at concentrations up to 0.01 mM showing high inhibitory selectivity. Many of the analogues also inhibit integrase strand transfer (INST) activity in low to sub micromolar range. Most analogues inhibit HIV progression in low micromolar range without cytotoxicity. Molecular docking and modelling
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6-biphenylmethyl-3-hydroxypyrimidine-2,4-diones potently and selectively inhibit HIV reverse transcriptase-associated RNase H, overview. Design, synthesis, biochemical and antiviral evaluations of a 6-biphenylmethyl subtype of the 3-hydroxypyrimidine-2,4-dione (HPD) chemotype. The subtype potently inhibits RT RNase H in low nanomolar range without inhibiting RT polymerase (pol) or integrase strand transfer (INST) at the highest concentrations tested. A few analogues inhibit HIV in low micromolar range without cytotoxicity at concentrations up to 0.1 mM in cell-based assays. EC50 values and antiviral activity of the compounds, overview
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pharmacophore-based design and sythesis of 3-hydroxypyrimidine-2,4-dione subtypes as inhibitors of HIV reverse transcriptase-associated RNase H, enzyme inhibition shows tolerance of a nonflexible linker, overview. 3-Hydroxypyrimidine-2,4-dione (HPD) subtypes with a nonflexible C-6 carbonyl linkage exhibit potent and selective biochemical inhibitory profiles with strong RNase H inhibition at low nM, weak to moderate integrase strand transfer (INST) inhibition at low micromolecular range, and no to marginal RT polymerase (pol) inhibition up to 0.010 mM. A few analogues also demonstrate significant antiviral activity without cytotoxicity. EC50 values of the compounds, overview
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3-hydroxypyrimidine-2,4-diones act as selective active site inhibitors of HIV reverse transcriptase-associated RNase H, design, synthesis, and biochemical evaluations, overview. No inhibition by 9z. The activity and selectivity profiles of subtype 11 are manifested with a few selected analogues demonstrating exceptional potency in inhibiting RNase H. Although they also inhibit RT pol, the micromolar activity reflects a sizable selectivity (14-49 fold) strongly favoring RNase H inhibition. The compounds also show inhibition of integrase strand transfer (INST) activity. Molecular modelling
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library screening of alpha-hydroxytropolones synthesized through a convenient oxidopyrylium cycloaddition/ring-opening sequence, synthetic alpha-hydroxytropolones act as inhibitors of HIV reverse transcriptase ribonuclease H activity, structure-function analysis, overview. Homology model of substrate- and inhibitor-bound HIV-1 RNase H, molecular docking. beta-Thujaplicinol and manicol share a rare alpha-hydroxytropolone moiety that crystal-structure analysis reveals to be a key for the potent inhibition of the enzyme. Unfortunately, both of these natural products display cytotoxicity in cell-based antiviral assays that precludes cellular antiviral activity. The slight steric change from a methyl to chloromethylene to methoxymethylene decreases the inhibitory potency by close to a full order of magnitude. Enzyme residue Tyr501, which is predicted computationally to be involved in interactions with the side chain, is blocked by the substrate. HIV-1 cytopathicity assays are performed, cytotoxicity of synthetic alpha-hydroxytropolones and beta-thujaplicinol against CEM-SS cells
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additional information
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library screening of alpha-hydroxytropolones synthesized through a convenient oxidopyrylium cycloaddition/ring-opening sequence, synthetic alpha-hydroxytropolones act as inhibitors of HIV reverse transcriptase ribonuclease H activity, structure-function analysis, overview. Homology model of substrate- and inhibitor-bound HIV-1 RNase H, molecular docking. beta-Thujaplicinol and manicol share a rare alpha-hydroxytropolone moiety that crystal-structure analysis reveals to be a key for the potent inhibition of the enzyme. Unfortunately, both of these natural products display cytotoxicity in cell-based antiviral assays that precludes cellular antiviral activity. The slight steric change from a methyl to chloromethylene to methoxymethylene decreases the inhibitory potency by close to a full order of magnitude. Enzyme residue Tyr501, which is predicted computationally to be involved in interactions with the side chain, is blocked by the substrate. HIV-1 cytopathicity assays are performed, cytotoxicity of synthetic alpha-hydroxytropolones and beta-thujaplicinol against CEM-SS cells
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extracts of Uvaria angolensis from tropical zone of Cameroon (Mount Kalla in Yaounde City) are a promising source of inhibitors of HIV-1 reverse transcriptase-associated RNA-dependent DNA polymerase (RDDP) and HIV-1 RNase H functions. Usage of stem bark methanol extract that inhibits both HIV-1 RNase H function and RDDP activity with IC50 values of 0.001 mg/ml and 0.00062 mg/ml, respectively, and, after been fractionated with different solvents, its solid residue shows an IC50 of 0.00010 mg/ml and of 0.00023 mg/ml against RNase H and RDDP, respectively. Methanol and water extracts from leaves and twigs, are also effective but much less than stem bark extracts. Determination of cytotoxicity
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binding mode and resistance profile for a dual-target pyrrolyl diketo acid scaffold against HIV-1 integrase and reverse-transcriptase-associated ribonuclease H (RNase H), using wild-type and mutant enzymes, and detail energy components contribution of calculated binding free energies of studied inhibitors binding to HIV-1 IN and RNase H wild-types and mutants, overview
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Human immunodeficiency virus type 1 group M subtype B
inhibitor library screening, identification and synthesis of cycloheptathiophene-3-carboxamide derivatives as allosteric HIV-1 ribonuclease H inhibitors, binding mode of compounds 2-(3,4-dihydroxyphenyl)-3,5,6,7,8,9-hexahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one, 2-(3,4-dimethoxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, and 2-(3,4-dihydroxybenzamido)-N-(pyridin-2-yl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide, overview
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additional information
Human immunodeficiency virus type 1 group M subtype B
development and evaluation of inhibitors against the RNase H active site of HIV-1 reverse transcriptase. The RNase H active site of HIV-1 RT is sufficiently different from the active sites of the two cellular human enzymes, RNase H1 and RNase H2, that compounds can be developed as selective inhibitors of viral RH. Antiviral activities of compounds XZ456, XZ460, XZ462, and MK463 against wild-type enzyme and against HIV-1 vectors that carry well-known INSTI, NNRTI, and NRTI resistance mutations, overview. XZ456 and XZ460 both inhibit these NRTI mutants with efficacies similar to their antiviral activities against wild-type HIV-1. Conversely, the NRTI-resistant mutants cause a 3 to 4fold reduction in susceptibility to XZ462 and MK463. Compounds are tested in viral replication and cytotoxicity assays. For enzyme-inhibitor structural modelling, coordinates of the following retroviral RT-RT inhibitor structures are used: HIV RT-MK1 (PDB ID 3LP0) and HIV RT-MK2 (PDB ID 3LP1). The compounds target the catalytic magnesium ions in the HIV-1 RNase H
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inhibitory potency and binding of dumbbell oligonucleotides to MoMuL virus RNase H, overview. The best dumbbell oligonucleotide, inhibitor contained phosphorothioate residues in both the loops
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magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain, overview. 2-Hydroxyisoquinoline-1,3(2H,4H)-dione forms a 1:1 complex with Mg2+, but a 1:2 complex with Mn2+,
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