Page last updated: 2024-09-05

dapivirine and efavirenz

dapivirine has been researched along with efavirenz in 19 studies

Compound Research Comparison

Studies
(dapivirine)
Trials
(dapivirine)
Recent Studies (post-2010)
(dapivirine)
Studies
(efavirenz)
Trials
(efavirenz)
Recent Studies (post-2010) (efavirenz)
196641603,1106311,611

Protein Interaction Comparison

ProteinTaxonomydapivirine (IC50)efavirenz (IC50)
Chain A, POL POLYPROTEINHuman immunodeficiency virus 10.2612
Chain A, POL POLYPROTEINHuman immunodeficiency virus 10.2612
Chain B, POL POLYPROTEINHuman immunodeficiency virus 10.2612
Chain A, POL POLYPROTEINHuman immunodeficiency virus 10.2612
Chain B, POL POLYPROTEINHuman immunodeficiency virus 10.2612
Chain A, Pol PolyproteinHuman immunodeficiency virus 10.2612
Chain B, Pol PolyproteinHuman immunodeficiency virus 10.2612
Prothrombin Bos taurus (cattle)0.022
Gag-Pol polyproteinHIV-1 M:B_HXB2R0.1852
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)0.02
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)0.018
Microsomal triglyceride transfer protein large subunitHomo sapiens (human)0.054
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)0.004
Envelope glycoprotein gp160 [Cleaved into: Surface protein gp120 Human immunodeficiency virus 10.0035
Reverse transcriptase/RNaseH Human immunodeficiency virus 10.1627
Reverse transcriptase Human immunodeficiency virus 10.0643

Research

Studies (19)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's6 (31.58)29.6817
2010's12 (63.16)24.3611
2020's1 (5.26)2.80

Authors

AuthorsStudies
Andries, K; Arnold, E; Azijn, H; Daeyaert, FF; Das, K; de Béthune, MP; De Corte, BL; de Jonge, MR; Heeres, J; Ho, CY; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Van Aken, KJ; Ye, H1
Andries, K; Arnold, E; Boyer, PL; Clark, AD; Clark, P; Daeyaert, F; Das, K; De Béthune, MP; De Corte, B; De Jonge, MR; Heeres, J; Ho, CY; Hughes, SH; Janssen, PA; Kavash, RW; Koymans, LM; Kukla, MJ; Lewi, PJ; Lichtenstein, MA; Ludovici, DW; Pauwels, R; Vinkers, HM; Ye, H1
De Corte, BL1
Andries, K; Arnold, E; Bohets, H; Clark, AD; Daeyaert, F; Das, K; de Béthune, MP; De Clerck, F; de Jonge, M; De Knaep, F; Frenkel, YV; Guillemont, J; Heeres, J; Hughes, SH; Janssen, PA; Koymans, L; Kukla, M; Lampo, A; Lewi, PJ; Ludovici, D; Medaer, B; Pasquier, E; Pauwels, R; Stoffels, P; Vinkers, M; Williams, P1
Armanasco, N; Azijn, H; de Bethune, MP; Fletcher, P; Harman, S; Manlow, P; Nuttall, J; Perumal, D; Romano, J; Shattock, R1
Bar-Magen, T; Brenner, BG; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, H1
Bar-Magen, T; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, HT1
Artico, M; Clotet, B; Esté, JA; Gonzalez-Ortega, E; Maga, G; Mai, A; Nawrozkij, MB; Rotili, D; Samuele, A; Tarantino, D1
Ariën, KK; Augustyns, K; Dirié, B; Heeres, J; Joossens, J; Lewi, PJ; Michiels, J; Van der Veken, P; Van Goethem, S; Vande Velde, CM; Vanham, G; Venkatraj, M1
Artico, M; Ballante, F; Botta, G; Cirilli, R; Clotet, B; Esté, JA; Gonzalez, E; Maga, G; Mai, A; Morera, L; Musmuca, I; Nawrozkij, MB; Pierini, M; Ragno, R; Rotili, D; Samuele, A; Tarantino, D1
Anderson, KS; Arnold, E; Bauman, JD; Bollini, M; Cisneros, JA; Das, K; Frey, KM; Jorgensen, WL; Spasov, KA1
Anderson, KS; Bollini, M; Cisneros, JA; Jorgensen, WL; Spasov, KA1
Collu, G; Giliberti, G; La Colla, P; Loddo, R; Loksha, YM; Pedersen, EB; Sanna, G1
Ariën, KK; Augustyns, K; Cos, P; Dirié, B; Heeres, J; Joossens, J; Lewi, PJ; Lyssens, S; Maes, L; Michiels, J; Van der Veken, P; Vanham, G; Venkatraj, M1
Jorgensen, WL1
Gu, SX; Ju, XL; Liu, GY; Lu, HH; Zhu, YY1
Armijos Rivera, JI; Badia, R; Cirilli, R; Crespan, E; Esté, JA; Forgione, M; Hailu, GS; Kirillov, IA; Lucidi, A; Maga, G; Mai, A; Nawrozkij, MB; Panella, C; Patsilinakos, A; Ragno, R; Riveira-Muñoz, E; Rotili, D; Tomaselli, D; Yablokov, AS1
Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M1
Colby-Germinario, SP; Han, Y; Huang, W; Oliveira, M; Petropoulos, CJ; Quan, Y; Wainberg, MA; Xu, HT1

Reviews

3 review(s) available for dapivirine and efavirenz

ArticleYear
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
    Journal of medicinal chemistry, 2005, Mar-24, Volume: 48, Issue:6

    Topics: Anti-HIV Agents; Benzodiazepines; Drug Design; Drug Resistance, Viral; HIV Reverse Transcriptase; Imidazoles; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors

2005
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
    Journal of medicinal chemistry, 2005, Mar-24, Volume: 48, Issue:6

    Topics: Administration, Oral; Anti-HIV Agents; Biological Availability; Crystallography, X-Ray; Drug Design; Drug Evaluation, Preclinical; Genome, Viral; HIV; HIV Infections; Humans; Interdisciplinary Communication; Models, Molecular; Molecular Structure; Mutation; Nitriles; Pyrimidines; Rilpivirine

2005
Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
    European journal of medicinal chemistry, 2018, Oct-05, Volume: 158

    Topics: Anti-HIV Agents; HIV Infections; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2018

Other Studies

16 other study(ies) available for dapivirine and efavirenz

ArticleYear
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
    Bioorganic & medicinal chemistry letters, 2001, Sep-03, Volume: 11, Issue:17

    Topics: Anti-HIV Agents; Drug Evaluation, Preclinical; HIV Reverse Transcriptase; HIV-1; Inhibitory Concentration 50; Mutation; Nitriles; Pyrimidines; Reverse Transcriptase Inhibitors; Structure-Activity Relationship

2001
Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian
    Journal of medicinal chemistry, 2004, May-06, Volume: 47, Issue:10

    Topics: Anti-HIV Agents; Crystallography, X-Ray; Drug Resistance, Viral; HIV Reverse Transcriptase; Models, Molecular; Mutation; Nitriles; Protein Conformation; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors

2004
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:2

    Topics: Anti-HIV Agents; Cells, Cultured; Cervix Uteri; Dose-Response Relationship, Drug; Female; HIV Infections; HIV-1; Humans; Luciferases; Macrophages; Organ Culture Techniques; Pyrimidines; Reverse Transcriptase Inhibitors; T-Lymphocytes

2009
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
    Antimicrobial agents and chemotherapy, 2009, Volume: 53, Issue:11

    Topics: Anti-HIV Agents; Drug Resistance, Viral; HIV Reverse Transcriptase; Microbial Sensitivity Tests; Mutation; Nitriles; Pyridazines; Pyrimidines; Recombinant Proteins; Reverse Transcriptase Inhibitors

2009
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
    Antimicrobial agents and chemotherapy, 2010, Volume: 54, Issue:6

    Topics: Anti-HIV Agents; Base Sequence; Cell Line; DNA, Viral; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Recombinant Proteins; Reverse Transcriptase Inhibitors; Virus Replication

2010
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
    Journal of medicinal chemistry, 2011, Apr-28, Volume: 54, Issue:8

    Topics: Anti-HIV Agents; HIV-1; Pyrimidines

2011
Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
    Bioorganic & medicinal chemistry, 2011, Oct-15, Volume: 19, Issue:20

    Topics: Anti-HIV Agents; HIV Reverse Transcriptase; Humans; Models, Molecular; Phthalazines; Pyridazines; Pyridones; Reverse Transcriptase Inhibitors

2011
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
    Journal of medicinal chemistry, 2012, Apr-12, Volume: 55, Issue:7

    Topics: Anti-HIV Agents; Benzene Derivatives; Cell Line; Enzyme Assays; HIV Reverse Transcriptase; HIV-1; Humans; Kinetics; Models, Molecular; Mutation; Pyrimidinones; Stereoisomerism; Structure-Activity Relationship

2012
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
    Bioorganic & medicinal chemistry letters, 2013, Sep-15, Volume: 23, Issue:18

    Topics: Anti-HIV Agents; Crystallography, X-Ray; Dose-Response Relationship, Drug; Enzyme Inhibitors; HIV Reverse Transcriptase; HIV-1; Models, Molecular; Molecular Structure; Pyrimidines; Solubility; Structure-Activity Relationship

2013
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
    Bioorganic & medicinal chemistry letters, 2013, Sep-15, Volume: 23, Issue:18

    Topics: Anti-HIV Agents; Cell Line, Transformed; Cell Proliferation; Dose-Response Relationship, Drug; HIV-1; Humans; Hydrazines; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Solubility; Structure-Activity Relationship

2013
Synthesis of novel fluoro analogues of MKC442 as microbicides.
    Journal of medicinal chemistry, 2014, Jun-26, Volume: 57, Issue:12

    Topics: Anti-HIV Agents; Cell Line; Drug Resistance, Viral; HIV Protease Inhibitors; HIV Reverse Transcriptase; HIV-1; Humans; Mutation; Pyrimidinones; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Uracil

2014
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
    Bioorganic & medicinal chemistry, 2014, Oct-01, Volume: 22, Issue:19

    Topics: Anti-HIV Agents; Cell Line; Cell Survival; Dose-Response Relationship, Drug; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Molecular Structure; Parasitic Sensitivity Tests; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; Trypanocidal Agents; Trypanosoma brucei brucei; Trypanosoma brucei rhodesiense

2014
Computer-aided discovery of anti-HIV agents.
    Bioorganic & medicinal chemistry, 2016, 10-15, Volume: 24, Issue:20

    Topics: Anti-HIV Agents; Computer-Aided Design; Dose-Response Relationship, Drug; Drug Design; HIV Reverse Transcriptase; HIV-1; Humans; Microbial Sensitivity Tests; Models, Molecular; Molecular Structure; Reverse Transcriptase Inhibitors; Structure-Activity Relationship; T-Lymphocytes

2016
Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
    Journal of medicinal chemistry, 2019, 01-24, Volume: 62, Issue:2

    Topics: Anti-HIV Agents; Binding Sites; Cell Line; Drug Resistance, Viral; HIV Reverse Transcriptase; HIV-1; Humans; Molecular Docking Simulation; Mutation; Protein Structure, Tertiary; Pyrimidinones; Stereoisomerism; Structure-Activity Relationship

2019
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
    Disease models & mechanisms, 2023, 03-01, Volume: 16, Issue:3

    Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries

2023
Role of the K101E substitution in HIV-1 reverse transcriptase in resistance to rilpivirine and other nonnucleoside reverse transcriptase inhibitors.
    Antimicrobial agents and chemotherapy, 2013, Volume: 57, Issue:11

    Topics: Alkynes; Amino Acid Substitution; Benzoxazines; Cyclopropanes; Delavirdine; Deoxycytidine; Drug Resistance, Viral; Emtricitabine; HEK293 Cells; HIV Reverse Transcriptase; HIV-1; Humans; Leukocytes, Mononuclear; Microbial Sensitivity Tests; Mutagenesis, Site-Directed; Nevirapine; Nitriles; Pyridazines; Pyrimidines; Reverse Transcriptase Inhibitors; Rilpivirine; Virus Replication

2013