Page last updated: 2024-08-07 20:37:08
Gag-Pol polyprotein
A lentivirus-type gag-pol polyprotein that is encoded in the genome of human immunodeficiency virus type 1 group M subtype B (isolate HXB2). [PRO:DAN]
Synonyms
Pr160Gag-Pol
Research
Bioassay Publications (59)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 23 (38.98) | 18.2507 |
| 2000's | 26 (44.07) | 29.6817 |
| 2010's | 10 (16.95) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (50)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bevirimat | HIV-1 M:B_HXB2R | EC50 | 0.4369 | 5 | 5 |
[no title available]Biochemistry, , Jan-10, Volume: 56, Issue:1, 2017
Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic chemistry, , Volume: 70, 2017
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.Journal of enzyme inhibition and medicinal chemistry, , Volume: 28, Issue:1, 2013
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.Bioorganic & medicinal chemistry, , Dec-01, Volume: 12, Issue:23, 2004
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.Journal of medicinal chemistry, , May-04, Volume: 43, Issue:9, 2000
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors.Bioorganic & medicinal chemistry, , Volume: 4, Issue:6, 1996
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.Journal of medicinal chemistry, , Jan-19, Volume: 39, Issue:2, 1996
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.Bioorganic & medicinal chemistry letters, , Feb-07, Volume: 10, Issue:3, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Synthesis and study of anti-HIV-1 RT activity of 5-benzoyl-4-methyl-1,3,4,5-tetrahydro-2H-1,5-benzodiazepin-2-one derivatives.Bioorganic chemistry, , Volume: 72, 2017
Natural Product Kuwanon-L Inhibits HIV-1 Replication through Multiple Target Binding.Chembiochem : a European journal of chemical biology, , 02-16, Volume: 18, Issue:4, 2017
Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives.Bioorganic chemistry, , Volume: 67, 2016
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Studies of non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: synthesis and structure-activity relationships of 2-cyano and 2-hydroxy thiazolidenebenzenesulfonamide derivatives.Bioorganic & medicinal chemistry, , Feb-15, Volume: 13, Issue:4, 2005
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.Bioorganic & medicinal chemistry, , Dec-01, Volume: 12, Issue:23, 2004
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-04, Volume: 11, Issue:11, 2001
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Jul-23, Volume: 11, Issue:14, 2001
Synthesis and evaluation of quinoxalinones as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 9, Issue:22, 1999
Synthesis and evaluation of analogs of Efavirenz (SUSTIVA) as HIV-1 reverse transcriptase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 1999
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.Biochemistry, , Sep-28, Volume: 43, Issue:38, 2004
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.Biochemistry, , Jan-28, Volume: 42, Issue:3, 2003
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.Journal of medicinal chemistry, , Jun-07, Volume: 44, Issue:12, 2001
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variaJournal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1 specific reverse transcriptase inhibitors. 1. Phthalimidoalkyl and -alkylamino analogues.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 39, Issue:19, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piJournal of medicinal chemistry, , May-14, Volume: 36, Issue:10, 1993
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.Journal of medicinal chemistry, , Aug-20, Volume: 36, Issue:17, 1993
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C variaJournal of medicinal chemistry, , Feb-12, Volume: 47, Issue:4, 2004
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.Journal of medicinal chemistry, , Feb-25, Volume: 42, Issue:4, 1999
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.Journal of medicinal chemistry, , Oct-16, Volume: 35, Issue:21, 1992
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:9, 1991
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.Biochemistry, , Sep-28, Volume: 43, Issue:38, 2004
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.Biochemistry, , Jan-28, Volume: 42, Issue:3, 2003
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-identical aromatic rings.Bioorganic & medicinal chemistry, , Volume: 10, Issue:2, 2002
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.Journal of medicinal chemistry, , Jun-05, Volume: 46, Issue:12, 2003
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Modeling, analysis, and validation of a novel HIV integrase structure provide insights into the binding modes of potent integrase inhibitors.Journal of molecular biology, , Jul-11, Volume: 380, Issue:3, 2008
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.Journal of medicinal chemistry, , Dec-08, Volume: 38, Issue:25, 1995
Comparing the accumulation of active- and nonactive-site mutations in the HIV-1 protease.Biochemistry, , Sep-28, Volume: 43, Issue:38, 2004
A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance.Biochemistry, , Jan-28, Volume: 42, Issue:3, 2003
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.Proceedings of the National Academy of Sciences of the United States of America, , Apr-26, Volume: 91, Issue:9, 1994