etravirine profile

ID Source	ID
PubMed CID	193962
CHEMBL ID	308954
CHEBI ID	63589
SCHEMBL ID	52691
MeSH ID	M0420447

Synonym
HY-90005
r165335-tmc125
tmc 125
benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-
intelence(tm)
diaminopyrimidine deriv
r165335 ,
etravirine ,
tmc125
tmc-125
dapy deriv
tmc-125/r-165335
4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethyl-benzonitrile
intelence
r-165335
intelence (tn)
etravirine (jan/usan/inn)
D04112
269055-15-4
4-({6-amino-5-bromo-2-[(4-cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-dimethylbenzonitrile
65b ,
chebi:63589 ,
CHEMBL308954 ,
4-(6-amino-5-bromo-2-(4-cyanophenylamino)pyrimidin-4-ylamino)-3,5-dimethylbenzonitrile
bdbm50103642
4-(6-amino-5-bromo-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile
4-[6-amino-5-bromo-2-(4-cyano-phenylamino)-pyrimidin-4-yloxy]-3,5-dimethyl-benzonitrile
FT-0658058
4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethylbenzonitrile
4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-benzonitrile
benzonitrile, 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-
tmc125 cpd
4-[6-azanyl-5-bromanyl-2-[(4-cyanophenyl)amino]pyrimidin-4-yl]oxy-3,5-dimethyl-benzenecarbonitrile
4-[[6-amino-5-bromo-2-(4-cyanoanilino)-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile
A818671
BCP9000006
0c50hw4fo1 ,
etravirine [usan:inn:ban:jan]
4-(6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile
unii-0c50hw4fo1
r 165335
BCP0726000193
PB32778
cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-
4-({6-amino-5-bromo-2-[(4-
etravirine [vandf]
4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile
etravirine [orange book]
etravirine [who-dd]
etravirine [mi]
etravirine [mart.]
etravirine [jan]
etravirine [ema epar]
etravirine [usan]
etravirine [inn]
CS-0435
AKOS015896355
AM20080899
S3080
DB06414
4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile
SCHEMBL52691
3M8P
HE-0088
mfcd09837879
PYGWGZALEOIKDF-UHFFFAOYSA-N
4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]-amino]benzonitrile
4-[[4-amino 5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile
4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile
4-((6-amino-5-bromo-2-((4-cyanophenyl) amino) pyrimidin-4-yl) oxy)-3, 5-dimethylbenzonitrile
4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)pyrimidin-4-yl)oxy)-3,5-dimethylbenzonitrile
etravirine (tmc125)
AB01566873_01
DTXSID30181412 ,
J-513179
AC-8503
sr-01000944895
SR-01000944895-1
HMS3651P20
SW219570-1
etravine; etravirine
FT-0668442
BCP03562
Q414762
gtpl12675
FT-0668443
benzonitrile,4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-
CCG-269074
NCGC00345885-04
A26965
EX-A4282
4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl -benzonitrile
NCGC00345885-02
etravirine- bio-x
BA164437
etravirinum
etravirine (mart.)
dtxcid40103903
etravirina
j05ag04
EN300-23542752
SY097013

Excerpt	Reference	Relevance
"Etravirine (ETR) is a second-generation nonnucleoside reverse transcriptase (RT) inhibitor (NNRTI) active against common human immunodeficiency virus type 1 (HIV-1) drug-resistant strains. "	( Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. Bar-Magen, T; Brenner, BG; Oliveira, M; Quan, Y; Schader, SM; Wainberg, MA; Xu, H, 2009)	1.99
"Etravirine (ETV) is a second-generation nonnucleoside reverse transcriptase (RT) inhibitor (NNRTI) introduced recently for salvage antiretroviral treatment after the emergence of NNRTI-resistant human immunodeficiency virus type 1 (HIV-1). "	( Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. Gatanaga, H; Hachiya, A; Hayashida, T; Ode, H; Oka, S; Sato, H, 2010)	2
"Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections. "	( Interaction potential of etravirine with drug transporters assessed in vitro. Haefeli, WE; Weiss, J; Zembruski, NC, 2011)	2.12
"Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of human immunodeficiency virus type 1 infection. "	( Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review. Fletcher, CV; Havens, JP; Podany, AT; Scarsi, KK, 2020)	2.25
"Etravirine is a substrate and inducer of cytochrome P450 (CYP) 3A and a substrate and inhibitor of CYP2C9 and CYPC2C19. "	( Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial. DeMasi, R; Kakuda, TN; Mohammed, P; van Delft, Y, 2013)	2.11
"Etravirine (TMC125) is an orally administered second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved in treatment-experienced patients as addition to an optimized background therapy (OBT)."	( Etravirine for the treatment of HIV/AIDS. Schrijvers, R, 2013)	3.28
"Etravirine is a well-tolerated NNRTI with a good safety profile and a higher genetic barrier for resistance compared to first-generation NNRTIs. "	( Etravirine for the treatment of HIV/AIDS. Schrijvers, R, 2013)	3.28
"Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with reduced cross-resistance to first-generation NNRTIs. "	( Prevalence and risk factors associated with resistance-associated mutations to etravirine in a cohort of perinatally HIV-infected children. Bell, CS; Contreras, GA; Del Bianco, GP; Heresi, GP; Kleinosky, MT; Murphy, JR; Pérez, N, 2013)	2.06
"Etravirine is an NNRTI option for treatment-experienced paediatric patients."	( Etravirine in treatment-experienced, HIV-1-infected children and adolescents: 48-week safety, efficacy and resistance analysis of the phase II PIANO study. Cahn, P; Chokephaibulkit, K; Dincq, S; Fourie, J; Kakuda, TN; Karatzios, C; Nijs, S; Opsomer, M; Tambuyzer, L; Tomaka, FL; Tudor-Williams, G, 2014)	2.57
"Etravirine is a non-nucleoside reverse transcriptase inhibitor used in combination with other antiretrovirals for the treatment of HIV infection. "	( Etravirine plasma exposure is associated with virological efficacy in treatment-experienced HIV-positive patients. Aldieri, C; Bonora, S; Calcagno, A; Carbone, A; Castagna, A; D'Avolio, A; Di Perri, G; Ghisetti, V; Marinaro, L; Nozza, S; Trentalange, A, 2014)	3.29
"Etravirine (TMC125) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is being developed for the treatment of HIV-1 infections. "	( Etravirine for the treatment of HIV infection. Castagna, A; Lazzarin, A; Seminari, E, 2008)	3.23
"Etravirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that demonstrates potent in vitro activity against wild-type strains of HIV type 1 (HIV-1), as well as against numerous strains resistant to available NNRTIs. "	( Etravirine. Deeks, ED; Keating, GM, 2008)	3.23
"Etravirine is an NNRTI that is able to adapt its binding orientation and overcome common NNRTI resistance associated mutations (RAMs) such as K103N. "	( Etravirine: a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) active against NNRTI-resistant strains of HIV. Schiller, DS; Youssef-Bessler, M, 2009)	3.24
"Etravirine is an NNRTI that was reported to be effective when used as part of an optimized, highly active antiretroviral therapy regimen in NNRTI treatment-experienced adult patients with HIV."	( Etravirine: a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) active against NNRTI-resistant strains of HIV. Schiller, DS; Youssef-Bessler, M, 2009)	3.24
"Etravirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) developed for the treatment of HIV-1 infection. "	( Clinical pharmacokinetics and pharmacodynamics of etravirine. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Raoof, A; Schöller-Gyüre, M, 2009)	2.05
"Etravirine (ETV) is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) with reduced cross-resistance to first-generation NNRTIs, which has been primarily studied in randomized clinical trials and not in routine clinical settings."	( Prevalence of etravirine mutations and impact on response to treatment in routine clinical care: the Swiss HIV Cohort Study (SHCS). Böni, J; Bucher, HC; Bürgisser, P; Günthard, HF; Hasse, B; Klimkait, T; Ledergerber, B; Scherrer, AU; von Wyl, V; Yerly, S, 2009)	2.16
"Etravirine (ETR) is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed for treatment-experienced patients infected with HIV-1. "	( Etravirine for HIV-I: addressing the limitations of the nonnucleoside reverse transcriptase inhibitor class. Grennan, T; Walmsley, S, )	3.02
"Etravirine is a novel NNRTI, active against HIV-1 strains harboring multiple NNRTI mutations."	( Validation of an electrospray ionization LC-MS/MS method for quantitative analysis of raltegravir, etravirine, and 9 other antiretroviral agents in human plasma samples. Giocanti, M; Lacarelle, B; Paccou, A; Quaranta, S; Solas, C; Woloch, C, 2009)	1.29
"Etravirine (ETR) is a diarylpyrimidine derivative with a polycyclic molecule composed of 3 aromatic rings with single bonds between the rings (C(20)H(15)BrN(60)). "	( [Chemical characteristics, mechanism of action and antiviral activity of etravirine]. Estévez, MA; García, FG; Suay, VG, 2009)	2.03
"Etravirine (ETR) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with a potent and broad in vitro spectrum of activity against HIV-1 and viruses with NNRTI resistances, allowing sequential use of drugs of this family. "	( [Etravirine in first-line therapy]. Garcés, PA; Tena, EV, 2009)	2.71
"Etravirine (ETR) is a new antiretroviral drug of the non-nucleoside reverse transcriptase inhibitor (NNRTI) family that has recently been approved by the regulatory agencies for the treatment of patients with prior experience with antiretrovirals, evidence of active viral replication, and who harbor multidrug resistant HIV-1 strains. "	( [Role of etravirine in combination antiretroviral therapy]. Domingo, P, 2009)	2.21
"Etravirine is a recently approved nonnucleoside reverse transcriptase inhibitor. "	( Etravirine limits the emergence of darunavir and other protease inhibitor resistance-associated mutations in the DUET trials. Azijn, H; De Meyer, S; Hill, A; Peeters, M; Picchio, G; Tambuyzer, L; Vingerhoets, J, 2010)	3.25
"Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against both wild-type HIV and viruses harboring NNRTI resistance. "	( Effects of hepatic impairment on the steady-state pharmacokinetics of etravirine 200 mg BID: an open-label, multiple-dose, controlled Phase I study in adults. Berckmans, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2010)	2.04
"Etravirine is an effective and well-tolerated recently approved non-nucleoside reverse transcriptase inhibitor (NNRTI) for HIV type-1-infected patients with previous antiretroviral treatment experience. "	( Clinical perspective on antiretroviral drug-drug interactions with the non-nucleoside reverse transcriptase inhibitor etravirine. Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M, 2010)	2.01
"Etravirine is an enzyme inducer and could lower the concentration of combined drugs. "	( Pharmacokinetics of etravirine, raltegravir and darunavir/ritonavir in treatment experienced patients. Barrail-Tran, A; Bollens, D; Chêne, G; Colin, C; Descamps, D; Fagard, C; Goldwirt, L; Katlama, C; Molina, JM; Piketty, C; Taburet, AM; Yazdanpanah, Y, 2010)	2.13
"Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that is active against NNRT-resistant HIV-1. "	( LC-MS/MS determination of etravirine in rat plasma and its application in pharmacokinetic studies. Abobo, CV; Bates, TR; John, J; Joseph, MK; Liang, D; Wu, L, 2010)	2.1
"Etravirine (ETR) is a second-generation non-nucleoside reverse transcriptase inhibitor prescribed for the treatment of HIV-1. "	( Biotransformation of the antiretroviral drug etravirine: metabolite identification, reaction phenotyping, and characterization of autoinduction of cytochrome P450-dependent metabolism. Bumpus, NN; Yanakakis, LJ, 2012)	2.08
"Etravirine (ETR) is a non-nucleoside analogue reverse transcriptase inhibitor (NNRTI) with a high genetic barrier to the development of resistance and with potential activity against Human immunodeficiency virus type 1 (HIV-1) strains resistant to first-generation NNRTIs. "	( Prevalence of etravirine resistance associated mutations in HIV-1 strains isolated from infected individuals failing efavirenz: comparison between subtype B and non-B genetic variants. Duque, V; Meliço-Silvestre, A; Morais, C; Mota, V; Pereira, B; Pereira-Vaz, J; Saraiva-da-Cunha, J, 2012)	2.18
"Etravirine (Intelence®) is an orally administered next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). "	( Etravirine: a review of its use in the management of treatment-experienced patients with HIV-1 infection. Croxtall, JD, 2012)	3.26
"Etravirine (ETR) is an expanded-spectrum nonnucleoside reverse transcriptase inhibitor (NNRTI) approved for use as an antiretroviral agent in treatment-experienced patients. "	( Molecular mechanism of antagonism between the Y181C and E138K mutations in HIV-1 reverse transcriptase. Asahchop, EL; Han, Y; McCallum, M; Oliveira, M; Quan, Y; Quashie, PK; Wainberg, MA; Xu, HT, 2012)	1.82
"Etravirine [TMC 125] is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is being developed by Tibotec (Tibotec-Virco Group; now Johnson & Johnson) for the treatment of HIV-1 infections. "	( Etravirine: R165335, TMC 125, TMC-125, TMC125. , 2006)	3.22
"Etravirine is a next generation nonnucleoside reverse transcriptase inhibitor with activity against nonnucleoside reverse transcriptase inhibitor resistant HIV-1 virus. "	( Is there a role for etravirine in patients with Nonnucleoside reverse transcriptase inhibitor resistance? Grover, D; Nelson, M; Scott, C, 2008)	2.11
"Etravirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against wild-type and NNRTI-resistant HIV. "	( A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in HIV-negative volunteers. Bouche, MP; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Vanaken, H; Woodfall, B, 2008)	2.09

Excerpt	Reference	Relevance
"Etravirine has a satisfactory safety profile and, in this case, was a durable alternative therapy for HIV meningoencephalitis."	( Efficacy of etravirine for treatment of acute HIV meningoencephalitis. Couzigou, C; Escaut, L; Morand-Joubert, L; Roque-Afonso, AM; Seang, S; Vittecoq, D, 2009)	1.45
"Etravirine (ETR) has demonstrated good tolerability in clinical trials and may be an option for patients who switch therapy due to adverse events."	( Switching to an etravirine-containing regimen due to drug intolerance in clinical practice. Martín-Carbonero, L; Moreno, V; Ramírez-Olivenza, G; Valencia, E, )	1.2
"Etravirine and darunavir have been used in HAART since 2010 in South Korea. "	( Drug susceptibility to etravirine and darunavir among Human Immunodeficiency Virus Type 1-derived pseudoviruses in treatment-experienced patients with HIV/AIDS in South Korea. Choi, JY; Kee, MK; Kim, SS; Kwon, OK; Oh, HR; Park, M; Rhee, JE, 2015)	2.17
"Etravirine has unique activity against most HIV isolates that are resistant to other NNRTIs. "	( Etravirine: the renaissance of non-nucleoside reverse transcriptase inhibitors. Castro, J; Espinoza, L; Jayaweera, DT, 2008)	3.23
"Etravirine has a satisfactory safety profile and, in this case, was a durable alternative therapy for HIV meningoencephalitis."	( Efficacy of etravirine for treatment of acute HIV meningoencephalitis. Couzigou, C; Escaut, L; Morand-Joubert, L; Roque-Afonso, AM; Seang, S; Vittecoq, D, 2009)	1.45
"Etravirine has the potential for interactions by inducing CYP3A and inhibiting CYP2C9 and 2C19; it is a mild inhibitor of P-glycoprotein but not a substrate."	( Clinical pharmacokinetics and pharmacodynamics of etravirine. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Raoof, A; Schöller-Gyüre, M, 2009)	1.33
"Etravirine (ETR) has demonstrated efficacy in patients with multiple prior treatments with prior virological failure and resistance mutations to various families of antiretroviral drugs. "	( [Etravirine in highly treatment-experienced patients]. Corbera, EF; Palter, DP; Tiraboschi, JM, 2009)	2.71
"Etravirine has compromised activity in approximately half of the patients failing nevirapine-based first-line treatment in this cohort, which supports guidelines that caution against using it with NRTIs alone in such patients."	( Suboptimal etravirine activity is common during failure of nevirapine-based combination antiretroviral therapy in a cohort infected with non-B subtype HIV-1. Adewole, I; Akanmu, S; Chaplin, B; Gashau, W; Idoko, J; Kanki, P; Meloni, S; Murphy, R; Penugonda, S; Taiwo, B, 2010)	2.19
"Etravirine (ETR) has previously shown potent in vitro activity against different primary HIV-1 isolates and demonstrated durable efficacy in treatment-experienced, HIV-1-infected patients in the Phase III DUET studies. "	( Short communication: activity of etravirine on different HIV type 1 subtypes: in vitro susceptibility in treatment-naive patients and week 48 pooled DUET study data. Azijn, H; de Béthune, MP; De Meyer, S; De Smedt, G; Dierynck, I; Nijs, S; Picchio, G; Rimsky, L; Tambuyzer, L; Vingerhoets, J, 2010)	2.08
"Etravirine has demonstrated a favorable safety and tolerability profile; the incidence of treatment-emergent adverse events was comparable with placebo in the DUET trials, with the exception of rash."	( Etravirine in the treatment of HIV-1: a clinical overview for healthcare professionals. De Smedt, G; Kakuda, TN; Mills, A; Peeters, M; Vingerhoets, J; Woodfall, B; Yeni, P, 2010)	2.52
"Etravirine has been approved in several countries for use as part of highly active antiretroviral therapy in treatment-experienced patients."	( Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M, 2011)	1.36
"Etravirine has high affinity for plasma drug-binding proteins, such as albumin and α1-acid glycoprotein, which limits the amount of unbound etravirine available to enter the CNS. "	( Etravirine in CSF is highly protein bound. Best, BM; Capparelli, E; Clifford, D; Collier, AC; Croteau, D; Ellis, RJ; Gelman, B; Grant, I; Letendre, S; Marra, C; McArthur, J; McCutchan, JA; Morgello, S; Nguyen, A; Rossi, S; Simpson, D, 2013)	3.28
"Etravirine (ETR) has shown a good lipid profile in previous studies. "	( Lipid-lowering effect and efficacy after switching to etravirine in HIV-infected patients with intolerance to suppressive HAART. Casado, JL; de Los Santos, I; Del Palacio, M; García-Fraile, L; Moreno, S; Pérez-Elías, MJ; Sanz, J, )	1.82
"Etravirine has superseded dapivirine as Tibotec's lead NNRTI in clinical development worldwide."	( Etravirine: R165335, TMC 125, TMC-125, TMC125. , 2006)	2.5

Excerpt	Reference	Relevance
"Etravirine did not inhibit P-gp/ABCB1 and was not transported by the tested ABC transporters but was a potent inhibitor of BCRP/ABCG2."	( Interaction potential of etravirine with drug transporters assessed in vitro. Haefeli, WE; Weiss, J; Zembruski, NC, 2011)	1.39

Excerpt	Reference	Relevance
" There were few hepatic adverse events, and rashes were predominantly early onset and mild to moderate in severity."	( Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: primary 24-week analysis. Berger, DS; Blick, G; Cimoch, PJ; Cohen, CJ; Greenberg, RN; Hicks, CB; Hoetelmans, RM; Iveson, KJ; Jayaweera, DS; Mills, AM; Nadler, JP; Peeters, MP; Ruane, PJ; Schrader, SR; Shalit, P; Smith, SM; Steinhart, CR; Thompson, M; Vingerhoets, JH; Voorspoels, E; Ward, D; Woodfall, B, 2007)	0.65
" Most adverse events were mild or moderate in severity."	( Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Cahn, P; de Smedt, G; Grinsztejn, B; Haubrich, R; Lalezari, J; Leopold, L; Madruga, JV; Mills, A; Peeters, M; Pialoux, G; Trefiglio, R; Vingerhoets, J; Wilkin, T; Woodfall, B, 2007)	0.63
" The type and frequency of adverse events were much the same in the two groups."	( Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Baeten, B; Beets, G; Campbell, T; Clotet, B; de Smedt, G; Johnson, M; Katlama, C; Lazzarin, A; Moll, A; Peeters, M; Sinha, R; Towner, W; Trottier, B; Vingerhoets, J; Woodfall, B, 2007)	0.63
"Neuropsychiatric adverse events (AEs) of interest occurred in 46."	( Safety, tolerability, and preliminary efficacy of 48 weeks of etravirine therapy in a phase IIb dose-ranging study involving treatment-experienced patients with HIV-1 infection. Clumeck, NN; Fätkenheuer, G; Gatell, J; Hay, P; Montaner, J; Peeters, MP; Schöller-Gyüre, M; Seminari, E; Simonts, M; Woodfall, B; Yeni, P, 2008)	0.59
"ETR was generally safe and well tolerated during long-term administration in treatment-experienced, HIV-1-infected patients, and it had a safety profile comparable to that of placebo."	( Safety, tolerability, and preliminary efficacy of 48 weeks of etravirine therapy in a phase IIb dose-ranging study involving treatment-experienced patients with HIV-1 infection. Clumeck, NN; Fätkenheuer, G; Gatell, J; Hay, P; Montaner, J; Peeters, MP; Schöller-Gyüre, M; Seminari, E; Simonts, M; Woodfall, B; Yeni, P, 2008)	0.59
" There is a complex, combined effect of HIV infection plus antiretroviral treatment on the incidence of gastrointestinal symptoms, and, for some trials, the majority of gastrointestinal adverse events may not be related to antiretroviral treatment."	( Risk factors for gastrointestinal adverse events in HIV treated and untreated patients. Balkin, A; Hill, A, )	0.13
" Rash was the only adverse event to occur at a significantly higher incidence in the etravirine group (19 vs."	( Efficacy and safety of etravirine in treatment-experienced, HIV-1 patients: pooled 48 week analysis of two randomized, controlled trials. De Smedt, G; Haubrich, R; Katlama, C; Lalezari, J; Lazzarin, A; Madruga, JV; Molina, JM; Peeters, M; Picchio, G; Schechter, M; Vingerhoets, J; Woodfall, B, 2009)	0.89
" The most frequent adverse effect is rash (affecting 19% of patients), which is usually mild (grades 1 or 2) and does not lead to drug withdrawal."	( [Safety and tolerability of etravirine]. Portilla, J, 2009)	0.65
" Furthermore, etravirine was shown to be safe and well-tolerated over this period."	( Etravirine in combination with darunavir/ritonavir and optimized background regimen results in suppression of HIV replication in treatment-experienced patients. Evaluation of Katlama C, Haubrich R, Lalezari J, et al. Efficacy and safety of etravirine in t Hull, MW; Montaner, JS, 2010)	2.16
" The nature and magnitude of adverse events observed during treatment suggest that etravirine may offer improved tolerability over existing antiretrovirals, including NNRTIs."	( A review of the safety and tolerability profile of the next-generation NNRTI etravirine. De Smedt, G; Di Perri, G; Grinsztejn, B; Peeters, M; Towner, W; Woodfall, B, 2010)	0.81
" Adverse events (AEs) and laboratory parameters were analysed."	( Safety of etravirine in HIV-1/hepatitis B and/or C virus co-infected patients: pooled 96 week results from the Phase III DUET trials. Clotet, B; Clumeck, N; Katlama, C; Nijs, S; Witek, J, 2010)	0.76
"A randomized, double-blind trial in patients with viral suppression but ongoing CNS adverse events after more than 12 weeks EFV."	( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine. Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011)	0.56
" Baseline CNS adverse events were similar."	( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine. Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011)	0.56
"Switching EFV to ETR led to a significant reduction in overall G2-4 CNS adverse events, including insomnia, abnormal dreams and nervousness as individual adverse event."	( A phase IV, double-blind, multicentre, randomized, placebo-controlled, pilot study to assess the feasibility of switching individuals receiving efavirenz with continuing central nervous system adverse events to etravirine. Fisher, M; Garvey, L; Hadley, W; Higgs, C; Mandalia, S; Nelson, M; Nicola, M; Perry, N; Waters, L; Winston, A, 2011)	0.56
"Although efavirenz is a universally recommended treatment for naive HIV-infected individuals, neuropsychiatric adverse events are common."	( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population. Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011)	0.59
" The primary end point was the percentage of patients with grade 1-4 drug-related treatment-emergent neuropsychiatric adverse events up to week 12."	( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population. Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011)	0.59
"After 12 weeks, first-line treatment with etravirine 400 mg once daily with two NRTIs was associated with significantly fewer neuropsychiatric adverse events when compared with efavirenz with two NRTIs."	( A comparison of neuropsychiatric adverse events during 12 weeks of treatment with etravirine and efavirenz in a treatment-naive, HIV-1-infected population. Banhegyi, D; Gazzard, B; Hill, A; Marks, S; Nelson, M; Podzamczer, D; Stark, T; Stellbrink, HJ; van Delft, Y; Vingerhoets, J, 2011)	0.86
"0%) men discontinued ETR due to adverse events."	( Efficacy and safety outcomes among treatment-experienced women and men treated with etravirine in gender, race and clinical experience. Hodder, S; Jayaweera, D; Mrus, J; Ryan, R; Witek, J, 2012)	0.6
"The aim of the study was to investigate the frequency and severity of adverse events (AEs) and laboratory abnormalities of interest over 96 weeks of treatment with etravirine or placebo in the pooled TMC125 DUET (Demonstrate Undetectable viral load in patients Experienced with ARV Therapy) trials."	( Pooled week 96 results of the phase III DUET-1 and DUET-2 trials of etravirine: further analysis of adverse events and laboratory abnormalities of special interest. Campbell, TB; Girard, PM; Grinsztejn, B; Hartikainen, J; Nijs, S; Rachline, A; Witek, J, 2012)	0.81
" All treatments and combinations were well tolerated, with no grade 3 or 4 adverse events observed during treatment."	( Pharmacokinetics and short-term safety of etravirine in combination with fluconazole or voriconazole in HIV-negative volunteers. Aharchi, F; Hoetelmans, RM; Kakuda, TN; Nijs, S; Smedt, GD; Van Solingen-Ristea, R; Vyncke, V; Witek, J, 2013)	0.65
" However, data on the long-term exposure to these therapeutic options are needed, and a handful of case reports are emerging, reporting rare but potentially life-threatening adverse hepatic events in patients with hepatitis co-infection or taking other hepatotoxic drugs."	( Hepatoxicity of new antiretrovirals: a systematic review. Lacombe, K; Surgers, L, 2013)	0.39
" The pathogenic mechanisms involved are related to hypersensitivity, as described with nevirapine, impaired metabolism and therefore increased drug levels, and direct toxic effects with production of toxic metabolites."	( Liver toxicity in HIV-infected patients receiving novel second-generation nonnucleoside reverse transcriptase inhibitors etravirine and rilpivirine. Casado, JL, )	0.34
" At week 48, the most common treatment-related grade ≥ 2 adverse event (AE) was rash (13%); 12% experienced grade 3 AEs."	( Etravirine in treatment-experienced, HIV-1-infected children and adolescents: 48-week safety, efficacy and resistance analysis of the phase II PIANO study. Cahn, P; Chokephaibulkit, K; Dincq, S; Fourie, J; Kakuda, TN; Karatzios, C; Nijs, S; Opsomer, M; Tambuyzer, L; Tomaka, FL; Tudor-Williams, G, 2014)	1.85
" Lersivirine and etravirine were generally safe and well-tolerated."	( Efficacy and safety of lersivirine versus etravirine for the treatment of HIV-1 infection in patients with prior non-nucleoside reverse transcriptase inhibitor (NNRTI) use and evidence of NNRTI resistance: a randomized phase 2B trial. Craig, C; DeJesus, E; Fätkenheuer, G; Heera, J; Jones, J; Orrell, C; Tawadrous, M; Wang, C, )	0.74
"3%) adverse events (AEs) were of mild or moderate severity with few grade 3/4 events, discontinuations, or temporary discontinuations/dose reductions due to AEs or serious AEs."	( The maraviroc expanded access program - safety and efficacy data from an open-label study. Craig, C; Heera, J; Lazzarin, A; Molina, JM; Mukwaya, G; Reynes, J; Sierra-Madero, JG; Valluri, S; van der Ryst, E, )	0.13
"Our data suggest that etravirine is a safe option for HIV/HCV-coinfected patients, including those with significant liver fibrosis."	( Liver toxicity and risk of discontinuation in HIV/hepatitis C virus-coinfected patients receiving an etravirine-containing antiretroviral regimen: influence of liver fibrosis. Bañón, S; Casado, JL; Castro, A; Mena, A; Moreno, A; Moreno, S; Pedreira, J; Quereda, C, 2016)	0.96
"8% of patients for adverse events in 23."	( Long-term efficacy and safety of etravirine-containing regimens in a real-life cohort of treatment-experienced HIV-1-infected patients. Allavena, C; Cabie, A; Cheret, A; Cotte, L; Delobel, P; Duvivier, C; Hoen, B; Katlama, C; Lahoulou, R; Poizot-Martin, I; Pugliese, P; Raffi, F; Roger, PM, 2016)	0.72

Excerpt	Reference	Relevance
"To assess the pharmacokinetic profile, safety and virological response of two novel investigational antiretroviral agents when used in combination in HIV-1-infected subjects with multidrug-resistant virus."	( Pharmacokinetics and antiretroviral response to darunavir/ritonavir and etravirine combination in patients with high-level viral resistance. Boffito, M; Fletcher, C; Gazzard, B; Hoetelmans, R; Jackson, A; Miralles, D; Moyle, G; Nelson, M; Pozniak, A; Tolowinska, I; Winston, A, 2007)	0.57
" Detailed pharmacokinetic assessments of darunavir and etravirine were determined on days 7 and 28."	( Pharmacokinetics and antiretroviral response to darunavir/ritonavir and etravirine combination in patients with high-level viral resistance. Boffito, M; Fletcher, C; Gazzard, B; Hoetelmans, R; Jackson, A; Miralles, D; Moyle, G; Nelson, M; Pozniak, A; Tolowinska, I; Winston, A, 2007)	0.82
"This first study to assess the use of etravirine and darunavir in HIV-1-infected subjects with no treatment options showed highly effective virological and immunological responses over 24 weeks of therapy with no new safety concerns or unexpected pharmacokinetic interactions."	( Pharmacokinetics and antiretroviral response to darunavir/ritonavir and etravirine combination in patients with high-level viral resistance. Boffito, M; Fletcher, C; Gazzard, B; Hoetelmans, R; Jackson, A; Miralles, D; Moyle, G; Nelson, M; Pozniak, A; Tolowinska, I; Winston, A, 2007)	0.84
" For TMC125 200 mg twice daily coadministered with DRV/r, AUC12h, Cmax and Cmin of TMC125 were 80%, 81% and 67% greater, respectively, versus TMC125 100 mg twice daily alone."	( Pharmacokinetics of darunavir/ritonavir and TMC125 alone and coadministered in HIV-negative volunteers. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Lefebvre, E; Peeters, M; Schöller-Gyüre, M; Sekar, V; Woodfall, B, 2007)	0.34
" Plasma concentrations and pharmacokinetic parameters of R- and S-methadone isomers were determined on days -1, 7, and 14 and of TMC125 on days 7 and 14."	( Pharmacokinetic and pharmacodynamic study of the concomitant administration of methadone and TMC125 in HIV-negative volunteers. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Stevens, T; van den Brink, W; Vanaken, H; Vandermeulen, K; Woodfall, B, 2008)	0.35
" Lack of pharmacokinetic alteration bounds for 90% confidence intervals (CI) about the geometric mean ratio (GMR; coadministration versus alone) were 70-143% for elvitegravir and ritonavir pharmacokinetics (maximum concentration [C(max)], concentration at the end of the dosing interval [C(tau)] and area under the plasma concentration-time curve [AUC(tau); 0-24 h] and 80-125% for etravirine pharmacokinetics (AUC(tau) 0-12 h)."	( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine. Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008)	0.79
" Elvitegravir pharmacokinetic GMR was 6-7% higher following elvitegravir/r plus etravirine dosing versus elvitegravir/r."	( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine. Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008)	0.85
"Two open-label, randomized, cross-over trials in healthy volunteers were conducted to investigate the pharmacokinetic interaction between etravirine and tenofovir disoproxil fumarate."	( Assessment of the steady-state pharmacokinetic interaction between etravirine administered as two different formulations and tenofovir disoproxil fumarate in healthy volunteers. Aharchi, F; Beets, G; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, MP; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, BJ, 2009)	0.79
"Etravirine was administered as either 800 mg twice a day (bid) (phase II formulation in Study 1) or 200 mg bid (phase III formulation in Study 2) for 8 days followed by a 12 h pharmacokinetic evaluation."	( Assessment of the steady-state pharmacokinetic interaction between etravirine administered as two different formulations and tenofovir disoproxil fumarate in healthy volunteers. Aharchi, F; Beets, G; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, MP; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, BJ, 2009)	2.03
" Etravirine 200 mg bid was coadministered on Day 1 to Day 15 of Cycle 3, with pharmacokinetic assessments of ethinylestradiol, norethindrone and etravirine on Day 15."	( Effect of steady-state etravirine on the pharmacokinetics and pharmacodynamics of ethinylestradiol and norethindrone. Aharchi, F; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, B, 2009)	1.57
" Pharmacokinetic parameters were compared (before and after efavirenz 14-day intake) by determining geometric mean ratios and 90% confidence intervals."	( Pharmacokinetics and safety of etravirine administered once or twice daily after 2 weeks treatment with efavirenz in healthy volunteers. Asboe, D; Back, D; Boffito, M; Gazzard, B; Jackson, A; Lamorde, M; Pozniak, A; Taylor, J; Waters, L; Watson, V, 2009)	0.64
"9%) to albumin and alpha(1)-acid glycoprotein and shows a relatively long elimination half-life of 30-40 hours."	( Clinical pharmacokinetics and pharmacodynamics of etravirine. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Raoof, A; Schöller-Gyüre, M, 2009)	0.61
"In this Phase I pharmacokinetic study, no clinically relevant differences were observed between patients with mild or moderate hepatic impairment and healthy matched subjects with regard to the pharmacokinetics of etravirine."	( Effects of hepatic impairment on the steady-state pharmacokinetics of etravirine 200 mg BID: an open-label, multiple-dose, controlled Phase I study in adults. Berckmans, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2010)	0.78
" Drug concentrations were measured using a validated LC-MS/MS assay and pharmacokinetic analysis was performed using non-linear mixed effect modelling."	( Intracellular and plasma steady-state pharmacokinetics of raltegravir, darunavir, etravirine and ritonavir in heavily pre-treated HIV-infected patients. Beijnen, JH; Huitema, AD; Mulder, JW; Ter Heine, R; van Gorp, EC; Wagenaar, JF, 2010)	0.59
"A pharmacokinetic trial was conducted to evaluate the potential for once-daily etravirine in antiretroviral regimens without and with darunavir/ritonavir."	( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults. DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010)	0.87
"Of 23 enrolled patients (male 87%, Caucasian 39%), pharmacokinetic profiles for etravirine were available for 21 and 20 patients on day 14 and 28, respectively."	( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults. DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010)	0.87
" Pharmacokinetic data were available in 577 patients randomized to receive etravirine."	( Pharmacokinetics and pharmacodynamics of the non-nucleoside reverse-transcriptase inhibitor etravirine in treatment-experienced HIV-1-infected patients. Corbett, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Leopold, L; Nijs, S; Peeters, MP; Schöller-Gyüre, M; Snoeck, E; Vingerhoets, J; Vis, P; Wade, JR; Woodfall, BJ, 2010)	0.81
" All pharmacokinetic parameters appeared to be highly variable regardless to the addition of etravirine."	( Pharmacokinetics of etravirine, raltegravir and darunavir/ritonavir in treatment experienced patients. Barrail-Tran, A; Bollens, D; Chêne, G; Colin, C; Descamps, D; Fagard, C; Goldwirt, L; Katlama, C; Molina, JM; Piketty, C; Taburet, AM; Yazdanpanah, Y, 2010)	0.9
" The assay has been successfully used for pharmacokinetic evaluation of etravirine using the rat as an animal model."	( LC-MS/MS determination of etravirine in rat plasma and its application in pharmacokinetic studies. Abobo, CV; Bates, TR; John, J; Joseph, MK; Liang, D; Wu, L, 2010)	0.89
" An extensive drug-drug interaction programme in HIV-negative subjects has been carried out to assess the potential for pharmacokinetic interactions between etravirine and a variety of non-antiretroviral drugs."	( Pharmacokinetic interactions between etravirine and non-antiretroviral drugs. Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M, 2011)	0.84
" Thus, a once-daily dosing regimen is supported not only by plasma etravirine pharmacokinetic profiles but also by intracellular levels."	( Intracellular and plasma pharmacokinetics of 400 mg of etravirine once daily versus 200 mg of etravirine twice daily in HIV-infected patients. Castillo-Ferrando, JR; Gutiérrez-Valencia, A; López-Cortés, LF; Martin-Peña, R; Ruiz-Valderas, R; Torres-Cornejo, A, 2012)	0.86
"A pharmacokinetic (PK) study was performed in 12 HIV-negative men receiving 600 mg of darunavir, 100 mg of ritonavir, and 200 mg of etravirine orally, twice daily for 8 days."	( Single- and multiple-dose pharmacokinetics of darunavir plus ritonavir and etravirine in semen and rectal tissue of HIV-negative men. Asher Prince, HM; Brown, KC; Cohen, MS; Jennings, SH; Kashuba, AD; Malone, SA; Patterson, KB; Shaheen, NJ; Spacek, M, 2012)	0.81
" To identify the potential impact of genetic and non-genetic factors involved in ETV metabolism, we carried out a two-step pharmacogenetics-based population pharmacokinetic study in HIV-1 infected individuals."	( Pharmacogenetics-based population pharmacokinetic analysis of etravirine in HIV-1 infected individuals. Arab-Alameddine, M; Bernasconi, E; Buclin, T; Calmy, A; Cavassini, M; Csajka, C; Decosterd, LA; di Iulio, J; Fayet-Mello, A; Furrer, H; Guidi, M; Günthard, HF; Lubomirov, R; Martinez, R; Marzolini, C; Rotger, M; Telenti, A, 2013)	0.63
" A first step population pharmacokinetic model included non-genetic and known genetic factors (seven SNPs in CYP2C, one SNP in CYP3A5) as covariates."	( Pharmacogenetics-based population pharmacokinetic analysis of etravirine in HIV-1 infected individuals. Arab-Alameddine, M; Bernasconi, E; Buclin, T; Calmy, A; Cavassini, M; Csajka, C; Decosterd, LA; di Iulio, J; Fayet-Mello, A; Furrer, H; Guidi, M; Günthard, HF; Lubomirov, R; Martinez, R; Marzolini, C; Rotger, M; Telenti, A, 2013)	0.63
" This single-center, open-label, two-period, single-sequence crossover study evaluated the effects of ETR coadministration on the pharmacokinetic profile of S/GSK1265744, an investigational integrase inhibitor in phase 2 studies."	( Effects of etravirine on the pharmacokinetics of the integrase inhibitor S/GSK1265744. Chen, S; Dumont, E; Ford, SL; Gould, E; Lou, Y; Piscitelli, S; Spreen, W, 2013)	0.78
" Pharmacokinetic parameters were analysed using non-compartmental methods."	( Effects of etravirine on the pharmacokinetics and pharmacodynamics of warfarin in rats. Abobo, CV; Hsiao, C; John, J; John, M; Liang, D; Wu, L, 2013)	0.78
" Pharmacokinetic interactions and safety of etravirine 200 mg twice daily coadministered with fluconazole 200 mg daily or voriconazole 200 mg twice daily, both inhibitors of CYP3A4, CYP2C9, and CYP2C19, were evaluated in an open-label, randomized, 3-period crossover trial in 18 HIV-negative volunteers."	( Pharmacokinetics and short-term safety of etravirine in combination with fluconazole or voriconazole in HIV-negative volunteers. Aharchi, F; Hoetelmans, RM; Kakuda, TN; Nijs, S; Smedt, GD; Van Solingen-Ristea, R; Vyncke, V; Witek, J, 2013)	0.92
" The current study evaluated the pharmacokinetic interaction between etravirine and the lopinavir/ritonavir melt extrusion formulation."	( Steady-state pharmacokinetics of etravirine and lopinavir/ritonavir melt extrusion formulation, alone and in combination, in healthy HIV-negative volunteers. Akuma, SH; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M; Spittaels, K; Vyncke, V; Witek, J, 2013)	0.91
" Steady-state pharmacokinetics were assessed for all antiretrovirals alone and coadministered; pharmacokinetic parameters were obtained by noncompartmental analysis."	( Steady-state pharmacokinetics of etravirine and lopinavir/ritonavir melt extrusion formulation, alone and in combination, in healthy HIV-negative volunteers. Akuma, SH; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M; Spittaels, K; Vyncke, V; Witek, J, 2013)	0.67
" The objective was to investigate pharmacokinetic interactions between darunavir/ritonavir or etravirine and arthemether/lumefrantrine."	( Pharmacokinetic interaction between etravirine or darunavir/ritonavir and artemether/lumefantrine in healthy volunteers: a two-panel, two-way, two-period, randomized trial. DeMasi, R; Kakuda, TN; Mohammed, P; van Delft, Y, 2013)	0.88
" The long terminal elimination half-life of etravirine should support once-daily dosing."	( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients. Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y, )	0.66
" Area under the curve over the dosing interval (AUC24h) and trough concentration (C0h) were estimated using a population pharmacokinetic model and compared with previous results using the 200-mg twice-daily dosage."	( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients. Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y, )	0.4
" Pharmacokinetic parameters were determined using non-compartmental analysis and least square means (LSM) ratios and 90% confidence intervals (CI) were calculated."	( Single-dose pharmacokinetics of pediatric and adult formulations of etravirine and swallowability of the 200-mg tablet: results from three Phase 1 studies. Berckmans, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Leemans, R; Leopold, L; Nijs, S; Peeters, M; van Solingen-Ristea, R; Vyncke, V, 2013)	0.63
" Full pharmacokinetic profiles of each drug and safety/tolerability were assessed."	( Pharmacokinetic evaluation of the interaction between etravirine and rifabutin or clarithromycin in HIV-negative, healthy volunteers: results from two Phase 1 studies. Aharchi, F; De Marez, T; Hoetelmans, RM; Kakuda, TN; Peeters, M; Vandermeulen, K; Woodfall, B, 2014)	0.65
" Pharmacokinetic assessments were conducted for each drug at steady-state when given alone and when coadministered; statistical analyses were least-square means with 90% confidence intervals."	( Pharmacokinetic interaction between etravirine or rilpivirine and telaprevir in healthy volunteers: A randomized, two-way crossover trial. Bertelsen, KM; Crauwels, HM; Hoetelmans, RM; Kakuda, TN; Leopold, L; Nijs, S; Stevens, M; Tomaka, F; van Delft, Y; Vandevoorde, A; Witek, J, 2014)	0.68
"Population pharmacokinetic (PopPK) analyses often rely on steady state and full adherence to prescribed dosage regimen assumptions from data gathered during therapeutic drug monitoring (TDM)."	( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study. Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016)	0.63
" At each time point, plasma concentrations were measured over 12 hours (12-hour time point was obtained before the second daily dose of etravirine); pharmacokinetic parameters were derived using noncompartmental analysis and were compared between pregnancy and postpartum using general linear models."	( Pharmacokinetics of Total and Unbound Etravirine in HIV-1-Infected Pregnant Women. Baugh, B; Brown, K; Crauwels, HM; Hillewaert, V; Osiyemi, O; Ramgopal, M; Ryan, R; Zorrilla, C, 2016)	0.91
"Etravirine pharmacokinetic profiles were available for 13 of 15 enrolled women."	( Pharmacokinetics of Total and Unbound Etravirine in HIV-1-Infected Pregnant Women. Baugh, B; Brown, K; Crauwels, HM; Hillewaert, V; Osiyemi, O; Ramgopal, M; Ryan, R; Zorrilla, C, 2016)	2.15
" Full pharmacokinetic profiles were obtained on days 0 and 14 in the DRV cohort, and on days 0 and 7 in the ETR cohort."	( Pharmacokinetics of darunavir/cobicistat and etravirine alone and co-administered in HIV-infected patients. Challenger, E; Clotet, B; Curran, A; Khoo, S; Miranda, C; Moltó, J; Ribera, E; Santos, JR; Valle, M, 2018)	0.74
"Etravirine co-administration decreased cobicistat AUC0-24, Cmax and C24 by 30%, 14% and 66%, respectively."	( Pharmacokinetics of darunavir/cobicistat and etravirine alone and co-administered in HIV-infected patients. Challenger, E; Clotet, B; Curran, A; Khoo, S; Miranda, C; Moltó, J; Ribera, E; Santos, JR; Valle, M, 2018)	2.18
" The pharmacokinetic profile of etravirine and clinical data support twice-daily dosing, although once-daily dosing has been investigated in treatment-naïve and treatment-experienced persons."	( Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review. Fletcher, CV; Havens, JP; Podany, AT; Scarsi, KK, 2020)	1.09

Excerpt	Reference	Relevance
" Proton pump inhibitors and H(2)-antagonists are frequently used in the HIV-negative-infected population, and drug-drug interactions have been described with other antiretrovirals."	( A pharmacokinetic study of etravirine (TMC125) co-administered with ranitidine and omeprazole in HIV-negative volunteers. Bouche, MP; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Schöller-Gyüre, M; Vanaken, H; Woodfall, B, 2008)	0.64
" However, N348I significantly decreases tenofovir susceptibility when combined with thymidine analogue mutations and etravirine susceptibility when combined with Y181C."	( N348I in HIV-1 reverse transcriptase decreases susceptibility to tenofovir and etravirine in combination with other resistance mutations. Moore, K; Radzio, J; Sluis-Cremer, N; Sonza, S; Tachedjian, G, 2010)	0.8
" Interaction with fosamprenavir/ritonavir is not clinically significant, although their plasma levels vary slightly when used in combination with ETR."	( [Etravirine drug interactions]. Pérez, VE; Sánchez-Parra, C; Serrano Villar, S, 2009)	1.26
" Considering the importance of combining antiretrovirals for their optimal use in treating HIV, a number of drug-drug interactions with etravirine and other antiretrovirals have been evaluated."	( Clinical perspective on antiretroviral drug-drug interactions with the non-nucleoside reverse transcriptase inhibitor etravirine. Hoetelmans, RM; Kakuda, TN; Schöller-Gyüre, M, 2010)	0.77
"The aim of this open-label, fixed-sequence study was to investigate the potential of the botanical supplement Echinacea purpurea to interact with etravirine, a nonnucleoside reverse transcriptase inhibitor of HIV."	( Herb-drug interaction between Echinacea purpurea and etravirine in HIV-infected patients. Cedeño, S; Clotet, B; Miranda, C; Moltó, J; Negredo, E; Valle, M, 2012)	0.83
"We report the cases of two treatment-experienced HIV-infected patients with complex antiretroviral regimens that showed significant drug-drug interactions with etravirine."	( Optimizing concentrations of concomitant antiretrovirals by reducing etravirine doses: two case reports of complex drug-drug interactions. Cabot, JF; Denault, JS; Langlois, H; Marcotte, S; Sheehan, NL, 2019)	0.95

Excerpt	Reference	Relevance
" The Phase III formulation of etravirine significantly improves the bioavailability of etravirine over the Phase II formulation with reduced interpatient variability in etravirine pharmacokinetics."	( Single- and multiple-dose pharmacokinetics of etravirine administered as two different formulations in HIV-1-infected patients. Arasteh, K; Beets, G; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Peeters, M; Pozniak, AL; Schöller-Gyüre, M; Vandermeulen, K; Woodfall, BJ; Workman, C, 2008)	0.89
" Relative bioavailability of ritonavir was low, when compared with other ritonavir regimens."	( Intracellular and plasma steady-state pharmacokinetics of raltegravir, darunavir, etravirine and ritonavir in heavily pre-treated HIV-infected patients. Beijnen, JH; Huitema, AD; Mulder, JW; Ter Heine, R; van Gorp, EC; Wagenaar, JF, 2010)	0.59
" While providing for a potentially increased oral bioavailability secondary to an increased drug dissolution rate, amorphous dispersions can be limited by their physical stability."	( Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: etravirine. Brewster, ME; Craig, DQ; Davies, MC; De Cort, S; Leemans, R; Qi, S; Reading, M; Roberts, CJ; Segmuller, B; Stokbroekx, S; Turner, YT; Van Dycke, F; Voorspoels, J; Weuts, I; Xu, D, 2011)	0.57
" We hypothesized that the presence of multiple drugs would reduce crystallization tendency, thereby providing stable, supersaturating formulations for bioavailability enhancement."	( Multidrug, Anti-HIV Amorphous Solid Dispersions: Nature and Mechanisms of Impacts of Drugs on Each Other's Solution Concentrations. Arca, HÇ; Dahal, D; Edgar, KJ; Mosquera-Giraldo, LI; Taylor, LS, 2017)	0.46
"The aim of this study was to develop a fast, effective, and material sparing screening method to design amorphous solid dispersions (ASDs) of etravirine to drive more effectively the development process, leading to improved bioavailability (BA) and stability."	( Five-Stage Approach for a Systematic Screening and Development of Etravirine Amorphous Solid Dispersions by Hot-Melt Extrusion. Cadonau, S; Cardoso, S; Pereira, A; Pinto, RMA; Simões, MF; Simões, S; Werner, K, 2020)	1
" The antiviral drugs Raltegravir, Indinavir, Tipranavir, Dolutegravir, and Etravirine also exhibited good bioavailability and drug-likeness properties."	( Raltegravir, Indinavir, Tipranavir, Dolutegravir, and Etravirine against main protease and RNA-dependent RNA polymerase of SARS-CoV-2: A molecular docking and drug repurposing approach. Al-Dhabi, NA; Arunagirinathan, N; Ignacimuthu, S; Indu, P; Rameshkumar, MR; Valan Arasu, M, 2020)	1.04
"The inadequate bioavailability and toxicity potential of antiretroviral therapy limit their effectiveness in the complete eradication of HIV from viral reservoirs."	( Multi-organ targeting of HIV-1 viral reservoirs with etravirine loaded nanostructured lipid carrier: An in-vivo proof of concept. Fotooh Abadi, L; Kulkarni, S; Mahajan, K; Pai, R; Rojekar, S; Vavia, PR, 2021)	0.87
"Many lead compounds fail to reach clinical trials despite being potent because of low bioavailability attributed to their insufficient solubility making solubility a primary and crucial factor in early phase drug discovery."	( Structural modification aimed for improving solubility of lead compounds in early phase drug discovery. Baidya, ATK; Das, B; Kumar, R; Mathew, AT; Yadav, AK, 2022)	0.72

Excerpt	Relevance	Reference
"Dietary dosing of the non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC125, under development for treatment of HIV-1, resulted in a syndrome in male mice in a previous experiment that was termed hemorrhagic cardiomyopathy."	( Hemorrhagic cardiomyopathy in male mice treated with an NNRTI: the role of vitamin K. Bouche, MP; Coussement, W; De Jonghe, S; Lachau-Durand, S; Lammens, L; Starckx, S; Verbeeck, J; Vinken, P; Willems, B, 2008)	0.35
"To evaluate the effect of 2 etravirine dosing regimens on QT/corrected QT interval (QTc) in HIV-negative volunteers and assess pharmacokinetic and additional safety parameters."	( Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers. De Smedt, G; Hoetelmans, RM; Janssen, K; Kakuda, TN; Lachaert, R; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2008)	2.08
" Short-term dosing of etravirine in HIV-negative volunteers was generally safe and well tolerated."	( Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers. De Smedt, G; Hoetelmans, RM; Janssen, K; Kakuda, TN; Lachaert, R; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2008)	2.1
"Administration of etravirine in a fasted state resulted in 51% lower mean exposure compared with dosing after a standard breakfast."	( Effects of different meal compositions and fasted state on the oral bioavailability of etravirine. Boffito, M; Hoetelmans, RM; Kakuda, TN; Leemans, R; Peeters, M; Pozniak, AL; Schöller-Gyüre, M; Vandermeulen, K; Vyncke, V; Woodfall, B, 2008)	0.9
" Group 1 (n = 20) followed a sequence of 10-day dosing of elvitegravir/r (150/100 mg once daily) and elvitegravir/r plus etravirine (200 mg twice daily) or the reverse (n = 10 per sequence)."	( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine. Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008)	0.83
" Elvitegravir pharmacokinetic GMR was 6-7% higher following elvitegravir/r plus etravirine dosing versus elvitegravir/r."	( Pharmacokinetics of elvitegravir and etravirine following coadministration of ritonavir-boosted elvitegravir and etravirine. Kakuda, TN; Kearney, BP; Mack, R; Ramanathan, S; West, S, 2008)	0.85
" The pharmacokinetics of etravirine in HIV-infected patients at the recommended dosage of 200 mg twice daily demonstrates moderate intersubject variability and no time dependency."	( Clinical pharmacokinetics and pharmacodynamics of etravirine. De Smedt, G; Hoetelmans, RM; Kakuda, TN; Raoof, A; Schöller-Gyüre, M, 2009)	0.91
" Several drug interactions are expected with etravirine use, and some may require dosage adjustment or substitution of concurrent drugs."	( Etravirine: A novel nonnucleoside reverse transcriptase inhibitor for managing human immunodeficiency virus infection. Caldwell, DJ; Elsayed, RK, 2010)	2.06
" During a 12 h dosing interval plasma and peripheral blood mononuclear cells were collected."	( Intracellular and plasma steady-state pharmacokinetics of raltegravir, darunavir, etravirine and ritonavir in heavily pre-treated HIV-infected patients. Beijnen, JH; Huitema, AD; Mulder, JW; Ter Heine, R; van Gorp, EC; Wagenaar, JF, 2010)	0.59
" The ability to assess formulation risk in this regard early in development programs can not only help in guiding development strategies but can also point to critical design elements in the configuration of the dosage form."	( Physicochemical properties of the amorphous drug, cast films, and spray dried powders to predict formulation probability of success for solid dispersions: etravirine. Brewster, ME; Craig, DQ; Davies, MC; De Cort, S; Leemans, R; Qi, S; Reading, M; Roberts, CJ; Segmuller, B; Stokbroekx, S; Turner, YT; Van Dycke, F; Voorspoels, J; Weuts, I; Xu, D, 2011)	0.57
"Addition of darunavir/ritonavir to etravirine, all dosed once daily, did not have a clinically significant effect on the pharmacokinetics of etravirine."	( Pharmacokinetics of once-daily etravirine without and with once-daily darunavir/ritonavir in antiretroviral-naive HIV type-1-infected adults. DeJesus, E; Kakuda, TN; Lalezari, JP; Osiyemi, OO; Ruane, PJ; Ryan, R; Witek, J, 2010)	0.92
" However, ENF treatment is associated with injection site reactions and dosing fatigue."	( A 48-week pilot study switching suppressed patients to darunavir/ritonavir and etravirine from enfuvirtide, protease inhibitor(s), and non-nucleoside reverse transcriptase inhibitor(s). Alas, B; Perniciaro, A; Ruane, P; Ryan, R; Witek, J, 2010)	0.59
"The need to adjust the dosage of raltegravir in HIV-infected patients who are also receiving etravirine is unclear."	( Raltegravir dosage adjustment in HIV-infected patients receiving etravirine. Do, VT; Fulco, PP; Higginson, RT, 2011)	0.83
"74) were similar with both dosing schedules at the intracellular level."	( Intracellular and plasma pharmacokinetics of 400 mg of etravirine once daily versus 200 mg of etravirine twice daily in HIV-infected patients. Castillo-Ferrando, JR; Gutiérrez-Valencia, A; López-Cortés, LF; Martin-Peña, R; Ruiz-Valderas, R; Torres-Cornejo, A, 2012)	0.63
"Our results show that intracellular etravirine levels were similar with both dosing regimens in patients with PI-sparing regimens, while etravirine plasma AUC(0-τ) and C(max) were 30% and 76% higher with the once-daily regimen, respectively."	( Intracellular and plasma pharmacokinetics of 400 mg of etravirine once daily versus 200 mg of etravirine twice daily in HIV-infected patients. Castillo-Ferrando, JR; Gutiérrez-Valencia, A; López-Cortés, LF; Martin-Peña, R; Ruiz-Valderas, R; Torres-Cornejo, A, 2012)	0.9
" The use of SF and PK-PD disease models can be a valuable tool to predict dose-response of NMEs and support rational dose selection for monotherapy trials."	( From in vitro EC₅₀ to in vivo dose-response for antiretrovirals using an HIV disease model. Part I: a framework. Fang, J; Jadhav, PR, 2012)	0.38
"44) for the concentration at the end of the dosing interval."	( Herb-drug interaction between Echinacea purpurea and etravirine in HIV-infected patients. Cedeño, S; Clotet, B; Miranda, C; Moltó, J; Negredo, E; Valle, M, 2012)	0.63
"2 mg/kg twice daily (maximum dosage 200 mg twice daily) plus an optimized background therapy regimen achieved complete viral response (defined as HIV-1 RNA <50 copies/mL) in approximately half of treatment-experienced children and adolescents with HIV-1 infection and evidence of viral replication, and had an acceptable tolerability profile."	( Etravirine: a guide to its use in treatment-experienced pediatric patients with HIV-1 infection in the US. Lyseng-Williamson, KA, 2012)	1.82
" Etravirine had no effects on S/GSK1265744 geometric mean ratios of the area under the curve from time zero until the end of the dosing interval (1."	( Effects of etravirine on the pharmacokinetics of the integrase inhibitor S/GSK1265744. Chen, S; Dumont, E; Ford, SL; Gould, E; Lou, Y; Piscitelli, S; Spreen, W, 2013)	1.69
"Etravirine (ETR) is recommended as twice-daily dosing in pretreated patients."	( Switch from etravirine twice daily to once daily in non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-infected patients with suppressed viremia: the Monetra study. Agher, R; Assoumou, L; Blanc, C; Caby, F; Calvez, V; Courbon, E; Fourati, S; Katlama, C; Ktorza, N; Marcelin, AG; Peytavin, G; Schneider, L; Tindel, M, )	1.95
" Once-daily dosing options are essential to treatment simplification strategies, which have been shown to enhance regimen compliance and durabiltiy."	( New therapeutic landscape of NNRTIs for treatment of HIV: a look at recent data. Dilanchian, P; Jayaweera, D, 2012)	0.38
" Despite having a 30- to 40-h elimination half-life, etravirine was never considered for once-daily dosing during development due to an unacceptably high pill burden in phase II trials."	( Does once-daily etravirine have a role in the management of HIV-1 infection? McNicholl, IR, 2013)	0.99
" Area under the curve over the dosing interval (AUC24h) and trough concentration (C0h) were estimated using a population pharmacokinetic model and compared with previous results using the 200-mg twice-daily dosage."	( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients. Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y, )	0.4
"In the SENSE trial, etravirine 400 mg once daily achieved similar exposures to historical reference data on etravirine when dosed at 200 mg twice daily."	( Pharmacokinetics and pharmacodynamics of etravirine 400 mg once daily in treatment-naïve patients. Bickel, M; Di Perri, G; Faetkenheuer, G; Green, B; Hill, A; Kakuda, T; Kurowski, M; Morrish, G; van Delft, Y, )	0.72
"Two randomized studies in healthy adults investigated the single-dose pharmacokinetics of etravirine in various dosage strengths and the effects of dispersion in water and film-coating."	( Single-dose pharmacokinetics of pediatric and adult formulations of etravirine and swallowability of the 200-mg tablet: results from three Phase 1 studies. Berckmans, C; De Smedt, G; Hoetelmans, RM; Kakuda, TN; Leemans, R; Leopold, L; Nijs, S; Peeters, M; van Solingen-Ristea, R; Vyncke, V, 2013)	0.85
" The complexity index was based on a score which takes into account the number of pills per day, the dosing schedule, the dosage form and any specific instructions linked to use of the drug."	( Influence of adding etravirine on complexity index and patients' perceived complexity. Almeida-González, CV; Calvo-Cidoncha, E; González-Bueno, J; Morillo-Verdugo, R, 2014)	0.73
" The once-a-day ETV treatment was as effective as the twice daily dosing regimen."	( Clinical and virological efficacy of etravirine plus two active Nucleos(t)ide analogs in an heterogeneous HIV-infected population. de la Torre-Lima, J; Delgado-Fernández, M; Garcia-Lázaro, M; Girón-González, JA; López-Cortés, LF; López-Ruz, MA; Lozano, F; Márquez-Solero, M; Martinez-Perez, MA; Mohamed-Balghata, MO; Romero-Palacios, A; Téllez-Pérez, F; Viciana, P, 2014)	0.68
"Etravirine (ETR), a non-nucleoside reverse transcriptase inhibitor approved for 200 mg twice-daily dosing in conjunction with other antiretrovirals (ARVs), has pharmacokinetic properties which support once-daily dosing."	( Antiretroviral activity and safety of once-daily etravirine in treatment-naive HIV-infected adults: 48-week results. Eron, JJ; Floris-Moore, MA; Francis, O; Johnson, MA; Kashuba, AD; Kronk, C; Mollan, K; Patterson, KB; Wilkin, AM; Wohl, DA, 2016)	2.13
"Population pharmacokinetic (PopPK) analyses often rely on steady state and full adherence to prescribed dosage regimen assumptions from data gathered during therapeutic drug monitoring (TDM)."	( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study. Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016)	0.63
"Published PopPK models for lopinavir, atazanavir, efavirenz, and etravirine were applied to estimate PK parameters and individual concentrations in 140 HIV patients taking part in a medication adherence program using 2 dosing data sets."	( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study. Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016)	0.87
"Clearance estimates and likewise predicted concentrations did not markedly differ between the 2 dosing histories."	( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study. Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016)	0.63
"PopPK analysis assuming steady state with full adherence produced similar results to those based on detailed electronic dosing history reconciled with patients' allegations."	( Comparison of Population Pharmacokinetics Based on Steady-State Assumption Versus Electronically Monitored Adherence to Lopinavir, Atazanavir, Efavirenz, and Etravirine: A Retrospective Study. Buclin, T; Bugnon, O; Cavassini, M; Csajka, C; Fuchs, A; Rotzinger, A; Schneider, MP, 2016)	0.63
" The CCR5-antagonist maraviroc (MVC), the non-nucleoside reverse transcriptase inhibitors (NNRTIs) etravirine (ETV) and rilpivirine (RPV), as well as the integrase strand transfer inhibitor (INSTI) raltegravir (RAL), have all been evaluated using both oral and non-oral dosing regimens, demonstrating a need for dynamic and sensitive bioanalytical tools for drug quantification in plasma and tissue."	( Development and validation of a liquid chromatographic-tandem mass spectrometric method for the multiplexed quantification of etravirine, maraviroc, raltegravir, and rilpivirine in human plasma and tissue. Marzinke, MA; Parsons, TL, 2016)	0.86
" It is desirable for multidrug combinations to be coformulated into single dosage forms where possible, to promote patient convenience and adherence to dosage regimens, for which amorphous solid dispersion (ASD) is particularly well-suited."	( Multidrug, Anti-HIV Amorphous Solid Dispersions: Nature and Mechanisms of Impacts of Drugs on Each Other's Solution Concentrations. Arca, HÇ; Dahal, D; Edgar, KJ; Mosquera-Giraldo, LI; Taylor, LS, 2017)	0.46
" The pharmacokinetic profile of etravirine and clinical data support twice-daily dosing, although once-daily dosing has been investigated in treatment-naïve and treatment-experienced persons."	( Clinical Pharmacokinetics and Pharmacodynamics of Etravirine: An Updated Review. Fletcher, CV; Havens, JP; Podany, AT; Scarsi, KK, 2020)	1.09
"Solid dosage forms of amorphous solid dispersions (ASDs) have rarely been assessed for their crushability, although it might possibly be a more frequent practice than thought to facilitate oral administration in several clinical conditions (e."	( The influence of crushing amorphous solid dispersion dosage forms on the in-vitro dissolution kinetics. Appeltans, B; Pas, T; Van den Mooter, G; Verbert, S, 2020)	0.56

Role	Description
HIV-1 reverse transcriptase inhibitor	An entity which inhibits the activity of HIV-1 reverse transcriptase.
antiviral agent	A substance that destroys or inhibits replication of viruses.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
dinitrile	A dinitrile is a compound containing two nitrile groups.
organobromine compound	A compound containing at least one carbon-bromine bond.
aminopyrimidine	A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	35.4813	0.0096	10.5250	35.4813	AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Reverse transcriptase/ribonuclease H	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0021	0.0021	0.0021	0.0021	AID977608
Chain B, p51 RT	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0021	0.0021	0.0021	0.0021	AID977608
Chain A, Reverse transcriptase/ribonuclease H	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0021	0.0021	0.0021	0.0021	AID977608
Chain B, p51 RT	HIV-1 M:B_HXB2R	IC50 (µMol)	0.0021	0.0021	0.0021	0.0021	AID977608
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50 (µMol)	5.1000	0.6315	4.4531	9.3000	AID586881
Cytochrome P450 1A2	Homo sapiens (human)	IC50 (µMol)	0.0250	0.0001	1.7740	10.0000	AID1561725
ATP-dependent translocase ABCB1	Homo sapiens (human)	IC50 (µMol)	7.6000	0.0002	2.3185	10.0000	AID586877
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	0.0190	0.0001	1.7536	10.0000	AID1561730
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	0.0320	0.0000	2.0151	10.0000	AID1561728
Cytochrome P450 2C9	Homo sapiens (human)	IC50 (µMol)	0.0170	0.0000	2.8005	10.0000	AID1561726
Gag-Pol polyprotein	Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)	IC50 (µMol)	0.3700	0.0002	0.1042	1.7000	AID1801807
Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)	IC50 (µMol)	1,258.9301	0.1200	4.0480	10.0000	AID1207370
Cruzipain	Trypanosoma cruzi	IC50 (µMol)	102.0000	0.0002	2.0450	8.0000	AID484274; AID484275
Multidrug resistance-associated protein 1	Homo sapiens (human)	IC50 (µMol)	8.5000	0.0015	3.7110	9.6600	AID586879
Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.6003	10.0000	AID1141979
Kappa-type opioid receptor	Cavia porcellus (domestic guinea pig)	IC50 (µMol)	0.0970	0.0003	0.7123	7.0700	AID573468
Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)	IC50 (µMol)	1,258.9301	0.1200	4.0480	10.0000	AID1207370
Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.6306	10.0000	AID1141979
Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0006	1.5257	10.0000	AID1141979
Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.7472	10.0000	AID1141979
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	193.9050	0.0009	1.9014	10.0000	AID1207464; AID1207495; AID1207524
Sodium channel protein type 5 subunit alpha	Homo sapiens (human)	IC50 (µMol)	2,241.1285	0.0003	3.6484	9.2000	AID1207310; AID1207341
Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.7411	10.0000	AID1141979
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	IC50 (µMol)	0.2711	0.0001	1.0768	10.0000	AID1060625; AID1072797; AID1077216; AID1124998; AID1126511; AID1141975; AID1141976; AID1141978; AID1141979; AID1171593; AID1171594; AID1171595; AID1171596; AID1171597; AID1171598; AID1197835; AID1200848; AID1231487; AID1248227; AID1275539; AID1292014; AID1298247; AID1298248; AID1298249; AID1298250; AID1298251; AID1298253; AID1304407; AID1316359; AID1320869; AID1357809; AID1379964; AID1391088; AID1410405; AID1418468; AID1421298; AID1421299; AID1421300; AID1421301; AID1421302; AID1421310; AID1421311; AID1457063; AID1457064; AID1457065; AID1504705; AID1520066; AID1558858; AID1561723; AID1561724; AID1561725; AID1561726; AID1561727; AID1561728; AID1561729; AID1561730; AID1572075; AID1572530; AID1609110; AID1637387; AID1705194; AID1705195; AID1729163; AID1750722; AID1754648; AID1761021; AID1763907; AID1773463; AID1773843; AID1775803; AID1811038; AID1822283; AID1880369; AID1888706; AID517489; AID517490; AID517491; AID518734; AID518735; AID518737; AID518738; AID557019; AID557043; AID557044; AID573464; AID573465; AID573466; AID573468; AID573469; AID573470; AID648425; AID665276; AID698144; AID698145; AID698146; AID738336; AID779524
Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.7411	10.0000	AID1141979
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50 (µMol)	7.8000	2.4100	6.3433	10.0000	AID586880
Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0100	0.0007	1.7411	10.0000	AID1141979
Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)	IC50 (µMol)	3,162.2800	1.4000	5.3500	9.3000	AID1207430
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	6.0000	0.0040	1.9666	10.0000	AID586878
Reverse transcriptase	Human immunodeficiency virus 1	IC50 (µMol)	0.0186	0.0100	0.5356	7.1300	AID1815391; AID1815397; AID1815398; AID1815399; AID1815400; AID1815401; AID1815402
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	EC50 (µMol)	0.0140	0.0004	0.6153	9.7000	AID1326646; AID1326647; AID1410481; AID1410482; AID1410487; AID1421325; AID1456307; AID1456308; AID1483271; AID1483272; AID1483273; AID1483274; AID1483275; AID1483276; AID1483277; AID1750717; AID1750718; AID1750719; AID757627
Reverse transcriptase	Human immunodeficiency virus 1	EC50 (µMol)	0.0121	0.0002	1.1683	9.0740	AID1731746; AID1731747; AID1731749; AID1731750; AID1731751; AID1741393; AID1741394; AID1741395; AID1741396; AID1741397
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Reverse transcriptase/RNaseH	Human immunodeficiency virus 1	ID50	0.0455	0.0060	2.1898	9.0000	AID1574384; AID1574385
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
xenobiotic metabolic process	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
bile acid and bile salt transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
leukotriene transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monoatomic anion transmembrane transport	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
transport across blood-brain barrier	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
porphyrin-containing compound metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
toxin biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
post-embryonic development	Cytochrome P450 1A2	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
regulation of gene expression	Cytochrome P450 1A2	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
dibenzo-p-dioxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
lung development	Cytochrome P450 1A2	Homo sapiens (human)
methylation	Cytochrome P450 1A2	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 1A2	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
cellular respiration	Cytochrome P450 1A2	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 1A2	Homo sapiens (human)
hydrogen peroxide biosynthetic process	Cytochrome P450 1A2	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 1A2	Homo sapiens (human)
cellular response to cadmium ion	Cytochrome P450 1A2	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 1A2	Homo sapiens (human)
G2/M transition of mitotic cell cycle	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic metabolic process	ATP-dependent translocase ABCB1	Homo sapiens (human)
response to xenobiotic stimulus	ATP-dependent translocase ABCB1	Homo sapiens (human)
phospholipid translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
terpenoid transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of response to osmotic stress	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
transepithelial transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
stem cell proliferation	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide translocation	ATP-dependent translocase ABCB1	Homo sapiens (human)
export across plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
positive regulation of anion channel activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	ATP-dependent translocase ABCB1	Homo sapiens (human)
regulation of chloride transport	ATP-dependent translocase ABCB1	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
epoxygenase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
urea metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
monocarboxylic acid metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2C9	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
amide metabolic process	Cytochrome P450 2C9	Homo sapiens (human)
icosanoid biosynthetic process	Cytochrome P450 2C9	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2C9	Homo sapiens (human)
omega-hydroxylase P450 pathway	Cytochrome P450 2C9	Homo sapiens (human)
epithelial cell maturation	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
sensory perception of sound	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
male gonad development	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
vestibular nucleus development	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
secretory granule organization	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cellular response to cAMP	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cellular response to acidic pH	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cellular response to light stimulus	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cardiac muscle cell contraction	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
negative regulation of protein targeting to membrane	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
regulation of delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
negative regulation of delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
leukotriene metabolic process	Multidrug resistance-associated protein 1	Homo sapiens (human)
xenobiotic metabolic process	Multidrug resistance-associated protein 1	Homo sapiens (human)
response to xenobiotic stimulus	Multidrug resistance-associated protein 1	Homo sapiens (human)
cobalamin transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
sphingolipid biosynthetic process	Multidrug resistance-associated protein 1	Homo sapiens (human)
cellular response to oxidative stress	Multidrug resistance-associated protein 1	Homo sapiens (human)
heme catabolic process	Multidrug resistance-associated protein 1	Homo sapiens (human)
xenobiotic transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
phospholipid translocation	Multidrug resistance-associated protein 1	Homo sapiens (human)
positive regulation of inflammatory response	Multidrug resistance-associated protein 1	Homo sapiens (human)
transmembrane transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
cell chemotaxis	Multidrug resistance-associated protein 1	Homo sapiens (human)
transepithelial transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
cyclic nucleotide transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
leukotriene transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
sphingolipid translocation	Multidrug resistance-associated protein 1	Homo sapiens (human)
export across plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
transport across blood-brain barrier	Multidrug resistance-associated protein 1	Homo sapiens (human)
cellular response to amyloid-beta	Multidrug resistance-associated protein 1	Homo sapiens (human)
carboxylic acid transmembrane transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Multidrug resistance-associated protein 1	Homo sapiens (human)
glutathione transmembrane transport	Multidrug resistance-associated protein 1	Homo sapiens (human)
gastrin-induced gastric acid secretion	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
glucose metabolic process	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
heart development	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
sensory perception of sound	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
rhythmic behavior	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of heart contraction	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of blood pressure	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
positive regulation of heart rate	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
iodide transport	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
erythrocyte differentiation	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
intracellular chloride ion homeostasis	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
response to insulin	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
social behavior	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
corticosterone secretion	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
inner ear morphogenesis	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
inner ear development	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
intestinal absorption	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of sound	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
auditory receptor cell development	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
positive regulation of cardiac muscle contraction	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of gastric acid secretion	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
stomach development	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
renal absorption	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
renal sodium ion absorption	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cellular response to cAMP	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cellular response to epinephrine stimulus	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
adrenergic receptor signaling pathway	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cardiac muscle cell contraction	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
atrial cardiac muscle cell action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cochlea development	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane repolarization during atrial cardiac muscle cell action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
non-motile cilium assembly	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
action potential	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac conduction system development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac ventricle development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
brainstem development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sodium ion transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of sodium ion transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
response to denervation involved in regulation of muscle adaptation	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
telencephalon development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cerebellum development	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sodium ion transmembrane transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
odontogenesis of dentin-containing tooth	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
positive regulation of epithelial cell proliferation	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac muscle contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarization	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cellular response to calcium ion	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cardiac muscle cell action potential involved in contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of cardiac muscle cell contraction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
atrial cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
AV node cell to bundle of His cell communication	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
regulation of sodium ion transmembrane transport	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
xenobiotic metabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
negative regulation of gene expression	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bile acid and bile salt transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
heme catabolic process	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic export from cell	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transepithelial transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
leukotriene transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
monoatomic anion transmembrane transport	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
potassium ion transport	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
protein homooligomerization	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
action potential	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
lipid transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid biosynthetic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate metabolic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transmembrane transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transepithelial transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
renal urate salt excretion	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
export across plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
cellular detoxification	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
ATP binding	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
glucuronoside transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type bile acid transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATP hydrolysis activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
icosanoid transmembrane transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
ABC-type transporter activity	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 1A2	Homo sapiens (human)
iron ion binding	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	Cytochrome P450 1A2	Homo sapiens (human)
electron transfer activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 1A2	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 1A2	Homo sapiens (human)
enzyme binding	Cytochrome P450 1A2	Homo sapiens (human)
heme binding	Cytochrome P450 1A2	Homo sapiens (human)
demethylase activity	Cytochrome P450 1A2	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 1A2	Homo sapiens (human)
aromatase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 1A2	Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activity	Cytochrome P450 1A2	Homo sapiens (human)
protein binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
efflux transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATP hydrolysis activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ubiquitin protein ligase binding	ATP-dependent translocase ABCB1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
carboxylic acid transmembrane transporter activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylcholine floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
phosphatidylethanolamine flippase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
ceramide floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
floppase activity	ATP-dependent translocase ABCB1	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
iron ion binding	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
(S)-limonene 7-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 2C9	Homo sapiens (human)
(R)-limonene 6-monooxygenase activity	Cytochrome P450 2C9	Homo sapiens (human)
aromatase activity	Cytochrome P450 2C9	Homo sapiens (human)
heme binding	Cytochrome P450 2C9	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2C9	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
potassium channel regulator activity	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
telethonin binding	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
protein-containing complex binding	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
transmembrane transporter binding	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
ATP binding	Multidrug resistance-associated protein 1	Homo sapiens (human)
ABC-type vitamin B12 transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
efflux transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ATP hydrolysis activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ATPase-coupled lipid transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
glutathione transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
sphingolipid transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
carboxylic acid transmembrane transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ABC-type transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Multidrug resistance-associated protein 1	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
calmodulin binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
protein phosphatase 1 binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
outward rectifier potassium channel activity	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
protein kinase A catalytic subunit binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
protein kinase A regulatory subunit binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
transmembrane transporter binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
voltage-gated potassium channel activity involved in atrial cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated sodium channel activity	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
calmodulin binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
fibroblast growth factor binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
enzyme binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein kinase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein domain specific binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ankyrin binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
ubiquitin protein ligase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
transmembrane transporter binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nitric-oxide synthase binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potential	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
scaffold protein binding	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
protein binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP binding	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
organic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
bilirubin transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATP hydrolysis activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
ABC-type transporter activity	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
A-type (transient outward) potassium channel activity	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
transmembrane transporter binding	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
metal ion binding	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
efflux transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP hydrolysis activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
identical protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein homodimerization activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basal plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
basolateral plasma membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
membrane	ATP-binding cassette sub-family C member 3	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 1A2	Homo sapiens (human)
cytoplasm	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cell surface	ATP-dependent translocase ABCB1	Homo sapiens (human)
membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
extracellular exosome	ATP-dependent translocase ABCB1	Homo sapiens (human)
external side of apical plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
plasma membrane	ATP-dependent translocase ABCB1	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2C9	Homo sapiens (human)
plasma membrane	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
cytoplasm	Cytochrome P450 2C9	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2C9	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
lysosome	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
apical plasma membrane	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
Z disc	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
membrane raft	Potassium voltage-gated channel subfamily E member 1	Homo sapiens (human)
plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
basal plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
apical plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
lateral plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
extracellular exosome	Multidrug resistance-associated protein 1	Homo sapiens (human)
basolateral plasma membrane	Multidrug resistance-associated protein 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 1	Rattus norvegicus (Norway rat)
early endosome	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
endoplasmic reticulum	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cytoplasm	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
lysosome	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
early endosome	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
late endosome	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
endoplasmic reticulum	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
basolateral plasma membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
apical plasma membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
transport vesicle	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
cytoplasmic vesicle membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
neuron projection	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
neuronal cell body	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane raft	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
ciliary base	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
lumenal side of membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
basolateral part of cell	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
monoatomic ion channel complex	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
membrane	Potassium voltage-gated channel subfamily KQT member 1	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2A	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2B	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2C	Rattus norvegicus (Norway rat)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
caveola	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nucleoplasm	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
nucleolus	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
endoplasmic reticulum	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
plasma membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
caveola	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
cell surface	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
intercalated disc	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
lateral plasma membrane	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
Z disc	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
T-tubule	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
sarcolemma	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
perinuclear region of cytoplasm	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
voltage-gated sodium channel complex	Sodium channel protein type 5 subunit alpha	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 2D	Rattus norvegicus (Norway rat)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3B	Rattus norvegicus (Norway rat)
plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
cell surface	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
intercellular canaliculus	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
apical plasma membrane	Canalicular multispecific organic anion transporter 1	Homo sapiens (human)
endoplasmic reticulum membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
plasma membrane	Glutamate receptor ionotropic, NMDA 3A	Rattus norvegicus (Norway rat)
plasma membrane	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
sarcolemma	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
GABA-ergic synapse	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
postsynaptic specialization membrane	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
dendritic spine	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
neuronal cell body	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
postsynaptic membrane	Potassium voltage-gated channel subfamily D member 3	Homo sapiens (human)
nucleoplasm	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
brush border membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
mitochondrial membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
membrane raft	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
external side of apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1343)

Assay ID	Title	Year	Journal	Article
AID977608	Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1775803	Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1435517	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase F227L/V106A double mutant
AID541252	Antiviral activity against multidrug resistant HIV1 A17 containing reverse transcripatseK103N and Y181C mutation infected in human MT2 cells assessed as reduction in p24 antigen level after 4 days by ELISA	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID347633	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 32 with reverse transcriptase V106, V179, Y181, G190 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1693808	Antiviral activity against HIV-3B harboring reverse transcriptase Y181C mutant infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID508828	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1729153	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID347630	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 21 with reverse transcriptase K103, V179, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1565099	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID573474	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1572107	Sub-acute toxicity in Kunming mouse assessed as alveolar hemorrhage at 50 mg/kg/day, po administered for 2 weeks by hematoxylin and eosin staining-based assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1572554	Solubility in water at pH 7
AID1418464	Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22	Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID1357784	Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508646	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1483274	Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1583019	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1165076	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1705185	Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1572072	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1583026	Antiviral activity against HIV1 containing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID517495	Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1357794	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508636	Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID557044	Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1483272	Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1866020	Thermodynamic aqueous solubility of the compound	2022	Bioorganic & medicinal chemistry, 02-15, Volume: 56	Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
AID1754646	Antiviral activity against HIV1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1750718	Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1446820	Antiviral activity against HIV1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1815402	Inhibition of HIV1 reverse transcriptase F227L/V106A double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID584084	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-3	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1637399	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring L100I mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1773449	Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1421311	Inhibition of HIV1 reverse transcriptase K103N/Y188C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1483269	Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1165078	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1446826	Inhibition of wild-type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID508831	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1761015	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID726438	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID1487262	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
AID557042	Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1862564	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT4 cells
AID1298252	Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID449196	Antimalarial activity against Plasmodium falciparum W2mef assessed as DNA positive erythrocytes by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID1561712	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID1811039	Anti-viral activity against HIV1 harboring RT L100I mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID508782	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID517489	Inhibition of HIV1 recombinant wild type reverse transcriptase by SPA heteropolymeric assay	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID517493	Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 40% human serum	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID573464	Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID83554	Potency evaluated against wild type HIV-1 strain IIIB	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID449193	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1561738	Solubility of the compound in pH 7.0 buffer by HPLC analysis
AID1811046	Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID518737	Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID347622	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 1 with reverse transcriptase G190, Y188 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID533680	Tmax in healthy human plasma at 200 mg, po twice a day for 8 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID586904	Activity at BCRP	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1197836	Lipophilicity, log P of the compound at pH 7.0 by HPLC method	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1811038	Inhibition of recombinant wild-type HIV1 p66/p51 reverse transcriptase assessed as inhibition of [3H]dGTP incorporation using poly (rA) as templates incubated for 40 mins by spectrofluorometer	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1572075	Inhibition of recombinant HIV1 reverse transcriptase using (DIG)-dUTP and biotin-labeled dNTPs as substrate after 1 hr by ELISA	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID584237	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1352320	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1773443	Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells
AID1884229	Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1773456	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells
AID1249717	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1705189	Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1743631	Antiviral activity against HIV1 harboring RT F227L/V106Amutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID541244	Antiviral activity against HIV1 NL4-3 infected in human TZM-bl cells after 4 days by luciferase reporter gene assay	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID465424	Oral bioavailability in Beagle dog at 4 mg/kg	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1862568	Antiviral activity against HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1072808	Antiviral activity against HIV1 harboring wild type reverse transcriptase infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID476469	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus replication by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1565095	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1743630	Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID619638	Antiviral activity against HIV-1 3B harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1207370	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform
AID1882476	Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1884489	Antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID517496	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID508658	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508642	Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1457063	Inhibition of HIV1 NL4-3 reverse transcriptase His-tagged p66/p51 associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation c	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1731749	Inhibition of reverse transcriptase Y188L mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID557035	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1705186	Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1435513	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase K103N mutant
AID1561727	Inhibition of HIV1 RT Y188L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1206937	Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1743629	Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1316343	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID508775	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1815384	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID508785	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773836	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID508633	Cytotoxicity against human MT4 cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1157583	Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID726439	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID586876	Antiproliferative activity against MDCK2 cells assessed as growth inhibition	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1572527	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1691439	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1763897	Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1171591	Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase L100I mutant to EC50 for wild type HIV1 NL4-3	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID83553	Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID1231488	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID449198	Antimalarial activity against Plasmodium falciparum W2mef ring form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID522374	Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A mutant clone to EC50 for wild type HIV1	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1457058	Antiviral activity against HIV1 harboring reverse transcriptase K103N /Y1881C double mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1292014	Inhibition of wild type HIV1 Reverse transcriptase assessed as reduction of biotin deoxyuridine triphosphate incorporation into the wild type HIV1 reverse transcriptase after 1 hr by ELISA	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1558854	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID517491	Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant by SPA heteropolymeric assay	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1483283	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y188L mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1457062	Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y1881C double mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID417447	Inhibition of HIV1 reverse transcriptase Y181C mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1773840	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID508769	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1775796	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability for 5 days by MTT assay to EC50 for antiviral activity against NNRTI-resistant HIV-1 RES056 harboring RT K103N/Y181C mutant infected in human MT4 cells a	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1880374	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1163255	Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID779524	Inhibition of recombinant wild type HIV-1 reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 (1:1.2) as template/primer after 40 mins by spectrofluorometric analysis	2013	Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21	Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies.
AID1231489	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID508780	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID347623	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 2 with reverse transcriptase A98, K101, Y181, G190 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID648424	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1761019	Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID508653	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1171587	Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1320866	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1561704	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID1572523	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1561707	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1446816	Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1636147	Antiviral activity against NNRTI resistant HIV1 harboring reverse transcriptase V106I/Y181C/G190A/H221Y mutant assessed as inhibition of viral infection in human TZM-bl cells after 48 hrs by luciferase reporter gene assay	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID738336	Inhibition of HIV 1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly rA.dT by ELISA	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1558848	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1565092	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1773460	Resistance factor, ratio of EC50 for HIV1 harboring Y188L mutant mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1572106	Sub-acute toxicity in Kunming mouse assessed as alveolar interstitial thickening at 50 mg/kg/day, po administered for 2 weeks by hematoxylin and eosin staining-based assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID632799	Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID508656	Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1207495	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform
AID1561709	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1888693	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID508628	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1316344	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1410397	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID541249	Selectivity index, ratio of CC50 for human MT2 cells to EC50 for HIV1 3B	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1072806	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID1572054	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID490362	Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 10 % fetal bovine serum	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID508657	Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID541248	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for HIV1 NL4-3	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1483285	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase F227L/V106A double mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1157592	Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID557062	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C and K103N mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1815380	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1275544	Antiviral activity against HIV1 3B expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1069123	Antiviral activity against HIV harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1457060	Ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1558856	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID508640	Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1298253	Inhibition of HIV1 3B reverse transcriptase p66/p51 K103N/Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID573465	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1596753	Antiviral activity against HIV-1 3B harboring reverse transcriptase RES056 mutant infected in MT4 cells measured after 5 days by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID1773464	Solubility in phosphate buffer at pH7
AID1171585	Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID614142	Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay	2011	Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17	Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID1275539	Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-dUTP/biotin-dUTP/dTTP nucleotides incubated for 1 hr by ELISA	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1357809	Inhibition of wild-type HIV1 reverse transcriptase assessed as decrease in digoxigenin and biotin-dUTP incorporation in to DNA using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1504704	Antiviral activity against HIV1 3B harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1248222	Antiviral activity against wild type HIV 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1443668	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1773839	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1357791	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1743620	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1421300	Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1731756	Solubility in water at pH 7.4 at 0.1 to 10 mg
AID1750727	Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase E138K mutant	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID508626	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1583021	Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1171412	Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1410406	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID1483292	Fold resistance, ratio of EC50 for reverse transcriptase Y188L mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1304408	Antiviral activity against HIV-1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	2016	Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13	Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1572074	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1248226	Antiviral activity against wild type HIV 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1456311	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1561729	Inhibition of HIV1 RT V106A/F227L mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID508764	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1126507	Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1421302	Inhibition of HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID260238	Cytotoxicity against human MT2 cells by MTT assay	2006	Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3	Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508792	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1320863	Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1572060	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1565091	Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1504701	Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID496628	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36A, T39D, V60I, I135V, T139I, K173A, Q174K, T200E, Q207A, R211K, F214L mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1298246	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1316346	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID508624	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773463	Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA
AID1197831	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1773462	Resistance factor, ratio of EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1637401	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y181C mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID586895	Induction of SLCO2B1 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID368563	Binding affinity to HIV1 reverse transcriptase treated for 3 mins by surface plasmon resonance	2009	Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3	Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants.
AID1862565	Antiviral activity against HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1572065	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1069125	Inhibition of HIV wild-type reverse transcriptase by electrochemiluminescence assay	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1572058	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID557040	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1163253	Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1743619	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1435512	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase L100I mutant
AID518736	Selectivity ratio of IC50 for RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID476468	Cytotoxicity against human MT2 cells by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID557061	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase L100I and K103N mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1583027	Antiviral activity against HIV1 containing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID738335	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1352317	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1775801	Antiviral activity against HIV-1 harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID496620	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/K30E, I31P, V35Q, T39S, E44G, E53G, A62G, N81H, Q91H,I135V,S162A, K173S, Q174R, D177E, V179I, T200I, Q207N, R211K, F214L mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1572108	Sub-acute toxicity in Kunming mouse assessed as proximal convoluted tubule edema in kidney at 50 mg/kg/day, po administered for 2 weeks by hematoxylin and eosin staining-based assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1206935	Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID496631	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,Y181C/V35T, T39M, P119S, D123E, S162A, E169D, K173T, Q174K, D177E, T200A, Q207E, K219N, V245Q, E248D mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1773455	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells
AID1561720	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenes
AID465423	Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1292012	Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1815400	Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1822281	Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1729150	Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1435506	Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1761014	Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1165075	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1729152	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1822278	Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID465421	Binding affinity to human serum albumin	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1561718	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu
AID508637	Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1535519	Solubility of the compound	2019	Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3	Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
AID709859	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/V179F double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1391084	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID517494	Selectivity ratio of IC50 for wild type HIV1 in presence of 40% human serum to IC50 for wild type HIV1 in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1235377	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity incubated for 4 days by MTT method	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1884490	Antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID508627	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1741391	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID517490	Inhibition of HIV1 recombinant reverse transcriptase K103N/Y181C double mutant by SPA heteropolymeric assay	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1206934	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathicity after 4 days by MTT assay	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1561719	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v
AID1705184	Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1583022	Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1687681	Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID484276	Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 1% DMSO	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID1888707	Solubility in water at pH 7.4
AID1316342	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1446813	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1443662	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1561723	Inhibition of HIV1 RT in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID491829	Resistant fold, ratio of EC50 for HIV1 with reverse transcriptase A17 (K103N, Y181C) mutant to EC50 for wild type HIV1 3B	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1572518	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1443661	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID583852	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.005 multiplicities of infection after 6 days	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1884227	Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID648422	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508777	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID347625	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 12 with reverse transcriptase L100, K103 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1731745	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID698144	Inhibition of HIV1 reverse transcriptase L100I mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate	2012	Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14	New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1474166	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1763899	Antiviral activity against HIV-1 IIIB harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1596754	Cytotoxicity against human MT4 cells measured after 5 days by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID1171592	Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant to EC50 for wild type HIV1 NL4-3	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1200848	Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA using poly(A) x oligo(dT)15 as template/primer after 1 hr by ELISA	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID106057	Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1357790	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1352319	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID533679	Cmax in healthy human plasma at 200 mg, po twice a day for 4 days coadministered with 400 mg of raltegravir, po twice a day for 4 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1574385	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1583023	Selectivity index, ratio of CC50 for cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay to EC50 for antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptas	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID490371	Antiviral activity against HIV1 expressing reverse transcriptase G190A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1235380	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1819211	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1200843	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID508788	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1357803	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID586909	Induction of MRP3 activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1763900	Antiviral activity against HIV-1 IIIB harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID767493	Aqueous solubility of the compound	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID491828	Antiviral activity against HIV1 with reverse transcriptase A17 (K103N, Y181C) mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1207558	Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform
AID383497	Inhibition of HIV reverse transcriptase	2008	European journal of medicinal chemistry, Mar, Volume: 43, Issue:3	SAR and QSAR studies: modelling of new DAPY derivatives.
AID665276	Inhibition of HIV1 wildtype reverse transcriptase using poly(rA)/oligo(dT)15 as template by colometric streptavidin alkaline phosphate reporter assay	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID508830	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1750720	Inhibition of HIV-1 p66/p51 reverse transcriptase Y188L mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1574377	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1326643	Inhibition of wild type HIV-1 3B reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID1888699	Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1326645	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B reverse transcriptase infected in human MT4 cells	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID767501	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1754637	Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1763901	Antiviral activity against HIV-1 IIIB harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1443663	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1572530	Inhibition of HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by pico-green based spectrofluorometric analysis
AID1750726	Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y188L mutant	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1572064	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1561708	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID1421299	Inhibition of HIV1 reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID508763	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1880378	Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y181C mutant infected in human MT4 cells by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1207310	Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID1561724	Inhibition of HIV1 RT L100I mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID496633	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, K43R, V60I, K101R, K122E, D123S, I135V, S162A, K173T, Q174K, D177E, V179I, G196E, T200A, Q207E mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1483271	Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID246283	Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1743636	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1379962	Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay	2017	European journal of medicinal chemistry, Nov-10, Volume: 140	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID465420	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1815387	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1435508	Antiviral activity against HIV1 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID541247	Cytotoxicity in human MT2 cells after 4 day by XTT assay	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID347624	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 6 with reverse transcriptase L100, K103 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID106069	Inhibitory activity against 188L strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID476472	Antiviral activity against HIV1 reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1418467	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells	2018	Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22	Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID1884540	Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1390712	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1888696	Antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1882473	Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1316329	Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID106065	Inhibitory activity against 181C strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1729163	Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1435514	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y181C mutant
AID1561725	Inhibition of HIV1 RT K103N mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1157580	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID584238	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N, V108V/I mutant derived from 10 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1298251	Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1687686	Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1819234	Aqueous solubility of the compound at pH 2.0 by HPLC analysis
AID1743634	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1275543	Antiviral activity against HIV1 RES056 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1069124	Antiviral activity against HIV harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1819217	Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1754641	Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1596755	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in MT4 cells	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID586882	Cmax in human plasma at 200 mg bid after 8 days	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID347636	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 43 with reverse transcriptase K103, Y181, P225 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1561695	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1357788	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1750723	Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase L100I mutant	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1165077	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID573466	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1687683	Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1884491	Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1357783	Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID533678	Cmax in healthy human plasma at 200 mg, po twice a day for 8 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID586878	Inhibition of BCRP expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1157582	Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1249719	Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1520059	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID508796	Ratio of EC50 for HIV1 in presence of 1 mg/ml alpha-1 acid-glycoprotein to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID584240	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V108V/I, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to w	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID573471	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID586911	Induction of SLCO1B1 activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1357801	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID557039	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID584241	Ratio of EC50 for wild type HIV1 NL4-3 to EC50 for HIV1 NL4-3 harboring reverse transcriptase V179V/D mutant	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID508791	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1574375	Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1815383	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1060625	Inhibition of wild-type HIV1 reverse transcriptase assessed as incorporation of biotin-labeled dUTP	2014	Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1	Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.
AID1637387	Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-duTP incorporation using biotin-labeled dUTP and hybrid poly(A)-oligo (dT)15 template primer after 2 hrs by ELISA	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1435505	Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1888703	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID484390	Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering-based beads autocorrelation assay in presence of 1% DMSO	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID1819219	Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1775791	Antiviral activity against HIV-1 strain IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1775798	Antiviral activity against HIV-1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1761018	Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID586890	Induction of SLCO1B1 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1761016	Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID347637	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 47 with reverse transcriptase A98, V108, G190, F227 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID508786	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508776	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1761008	Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1884541	Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID522376	Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V179D mutant clone to EC50 for wild type HIV1	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1775797	Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1207430	Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform
AID1298245	Cytotoxicity against human MT4 cells after 5 days MTT assay	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1352312	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1636150	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase L100I/K103N/H221Y mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID665552	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant	2012	Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12	Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID1583028	Antiviral activity against HIV1 containing reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1483273	Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1572520	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
AID1316332	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1483278	Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1275546	Antiviral activity against HIV1 3B expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID614141	Antiviral activity against wild type Human immunodeficiency virus 1 3B bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay	2011	Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17	Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID557043	Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1888706	Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation
AID635346	Cytotoxicity against human MT4 cells measured by MTT assay	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1275545	Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID449276	Cytotoxicity against human erythrocytes assessed as change in internal complexity by flow cytometry	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID693584	Antiviral activity against HIV1 RES056 harbouring RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID1520058	Antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID276232	Cytotoxicity against MT2 cells	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1775794	Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1882475	Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1152374	Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B	2014	Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12	Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1446817	Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1884223	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wildtype HIV-1 3B infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1687685	Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1483284	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID586906	Inhibition of BCRP activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1558847	Antiviral activity against HIV1 3B infected in human MT4 cells incubated assessed as reduction in virus-induced cytopathic effect for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1731748	Inhibition of reverse transcriptase Y183C mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID518735	Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID573468	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID586891	Induction of PXR mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID584083	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase K103N mutant infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type HIV1 NL4-3	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID522371	Antiviral activity against recombinant HIV1 harboring reverse transcriptase V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID508629	Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID464765	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1231485	Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1773461	Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1457059	Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1304407	Inhibition of HIV-1 BH10 recombinant reverse transcriptase K103N mutant expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer	2016	Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13	Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID491834	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA	2010	Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13	Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID709863	Selectivity ratio of EC50 for NNRTI-resistant HIV1 harboring reverse transcriptase Y181V mutant to EC50 for HIV1 expressing wild type reverse transcriptase	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID586889	Induction of SLCO1B3 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID619636	Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1822275	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1171594	Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1761020	Antiviral activity against HIV-1 harboring reverse transcriptase RES056 mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1884492	Antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1077216	Inhibition of wild type HIV-1 reverse transcriptase using poly (rC)/oligo (dG) as template/primer assessed as inhibition of biotin-dUTP incorporation after 1 hr by microtiter plate ELISA reader analysis	2014	European journal of medicinal chemistry, Apr-09, Volume: 76	Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID665553	Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B	2012	Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12	Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
AID1731750	Inhibition of reverse transcriptase E138K mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1884221	Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1561721	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC
AID1561702	Antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1884542	Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID517498	Clearance in human liver microsomes	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1200844	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1235382	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity at 0.19 uM added 3 to 5 hrs post infection and measured 31 hrs post infection by p24 enzyme-linked immunosorbent assay	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508756	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1157595	Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID508765	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M236L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1882468	Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1754648	Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into cDNA measured after 1 hr by ELISA	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1357789	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1171411	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1572062	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1561714	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID1248227	Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1773453	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells
AID490370	Antiviral activity against HIV1 expressing reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1126511	Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1446814	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID106061	Inhibitory activity against 103N strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID665275	Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1391079	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1815392	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1884220	Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1352314	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID541246	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as reduction in p24 antigen level after 4 days by ELISA	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID417448	Inhibition of HIV1 reverse transcriptase Y188L mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1565097	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1558861	Aqueous solubility of compound at 2 mg measured for 24 hrs by HPLC analysis	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1446829	Solubility of the compound in water at pH 7.4	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1691435	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1410483	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1574382	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1773448	Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1705197	Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N/Y181C mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillati	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1761006	Antiviral activity against wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in viral infection measured after 1 day by luciferase reporter gene assay based luminiscence assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID508650	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID496629	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36D, T39N, V60I, D123N, I135V, S162A, K173T, Q174K, D177E, T200A, Q207E, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID508774	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1171414	Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID508638	Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1207524	Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay
AID1207281	Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform
AID1443666	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1754642	Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1124998	Inhibition of recombinant HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation in to poly [A] x oligo[dT]15 by ELISA	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID1687687	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopa	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID738334	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1743640	Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template preincubated for 1 hr followed by template/primer and dNTP addition and measured after 1 hr by ELISA	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID417449	Hydrophobic index, Log P of the compound	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1773458	Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID533674	Trough drug concentration at 12 hrs in healthy human plasma at 200 mg, po twice a day for 8 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1456307	Inhibition of HIV-1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1574383	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1731751	Inhibition of reverse transcriptase F227L/V106A double mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID465422	Half life in Beagle dog at 0.5 mg/kg, iv or. 5 mg/kg, po	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID449194	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID496742	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/V35T, K122E, I135V, T139A, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1171581	Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496626	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K22N, V35T, T39A, K122E, I135V, T139A, S162A, K173T, Q174A, D177E, T200A, Q207E, R211K, F214L mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1141977	Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting	2014	European journal of medicinal chemistry, Jun-10, Volume: 80	New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435518	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase mutant
AID1298250	Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1357786	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1435511	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase
AID1326644	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by cell titer glo based luciferase reporter gene assay	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID522370	Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1572519	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1504699	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1811050	Oral bioavailability in rat	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID586884	Induction of CYP2B6 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1141975	Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting	2014	European journal of medicinal chemistry, Jun-10, Volume: 80	New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1249723	Antiviral activity against HIV1 expressing reverse transcriptase F227L + V106A mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1729161	Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID573480	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID508623	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1596752	Antiviral activity against HIV-1 3B harboring reverse transcriptase E138K mutant infected in MT4 cells measured after 5 days by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID757627	Inhibition of HIV RT K103N/Y181C mutant by cell based assay	2013	European journal of medicinal chemistry, Jul, Volume: 65	Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1316341	Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1741398	Inhibition of reverse transcriptase F227L and V106A mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1637397	Antiviral activity against human HIV-1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1157585	Antiviral activity against zidovudine-resistant HIV1 harboring RT 67N, 70R, 215F, 219Q mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1390715	Resistance index, ratio of EC50 for HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1357785	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1231487	Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1390711	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID508790	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508829	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773450	Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1483282	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase Y181C mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1141979	Inhibition of HIV1 wild-type reverse transcriptase V106A mutant using [3H]dTTP by scintillation counting	2014	European journal of medicinal chemistry, Jun-10, Volume: 80	New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1352315	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1072805	Antiviral activity against HIV1 harboring reverse transcriptase K101N/Y181C double mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID1773827	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1884228	Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1773829	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1390714	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1574373	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1773837	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID347628	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 17 with reverse transcriptase A98, K103, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1152370	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay	2014	Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12	Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435525	Inhibition of recombinant wild type HIV1 reverse transcriptase using poly (A).oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA
AID1743628	Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1191400	Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3	Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1819215	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1171595	Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496617	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, T39K, I50V, V60I, S68G, I135V, S162A, K173V, Q174K,D177E, T200A, E203Q, Q207D, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID522368	Antiviral activity against wild type HIV1 infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID648425	Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT)	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1320869	Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1636927	Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID1572066	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1446819	Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1637390	Cytotoxicity against mock-infected human MT4 cells assessed as reduction of cell viability after 5 days by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1822282	Antiviral activity against HIV-1 harboring RES056 mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID508652	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID347635	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 36 with reverse transcriptase K103, V106, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID246301	Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1862562	Antiviral activity against HIV-1 ROD infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1822277	Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1421325	Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured 5 days post infection by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID557030	Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1815390	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT4	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID541245	Cytotoxicity in human TZM-bl cells after 4 day by XTT assay	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1811034	Anti-viral activity against HIV1 harboring RT E138K mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1763906	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1565096	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1435502	Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1750715	Cytotoxicity against in human MT-4 cells after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1124993	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID1316359	Inhibition of recombinant HIV1 reverse transcriptase K103N/Y181C double mutant using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1357795	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1443669	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1574380	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1275554	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID508772	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1750717	Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID83549	Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID1391077	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID522372	Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1435515	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y188L mutant
AID1390710	Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID1773835	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1815393	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1304406	Inhibition of wild type HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer	2016	Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13	Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1352318	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1754639	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Antiviral activity against HIV-1 IIIB infected in human MT4 cells	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1561701	Antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID541253	Resistance index, ratio of EC50 for multidrug resistant HIV1 A17 to EC50 for wild type HIV1 3B	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1583020	Antiviral activity against NNRTI-resistant HIV1 RES056 containing reverse transcriptase K103N+Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID496615	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, K64R, K102Q, D123E, S162A, K173T, Q174K, D177E, G196E,T200A, Q207E, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1761011	Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID508631	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID518742	Selectivity ratio of EC50 for antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant to EC50 for antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1316330	Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1862570	Antiviral activity against HIV-1 F227L-V106A mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1561706	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID1410405	Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides after 1 hr by ELISA	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID586897	Induction of CYP3A4 mRNA expression in human LS180 cells at 1 umol/liter after 4 days by RT-PCR analysis relative to beta-glucuronidase gene expression	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID508654	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID496624	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/A33E, V35T, T39A, D123E, S162A, Q174G, T200E, I202V, Q207E mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID508794	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID693586	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID1743618	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1157581	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1819214	Antiviral activity against HIV1 L1001 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID508832	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1819209	Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay
AID1561728	Inhibition of HIV1 RT E138K mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1822274	Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1316334	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID347629	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 20 with reverse transcriptase K103, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1761021	Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into cDNA incubated for 1 hr with DIG-dUTP, biotin-dUTP and dTTP followed by transferring onto streptavidin-coated plate and measured after 1 hr by ELISA	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1572071	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1457055	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1435507	Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID496634	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,A98G/V35T, E36D, T39K, S48A, I50V, V60I, S68G, I135V, S162A, K173T, Q174K, D177E, G196E, T200A, E203G, Q207D, R211K, Q222P mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID632800	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1418468	Inhibition of recombinant wild-type HIV1 GST-fused reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40	2018	Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22	Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID1304409	Antiviral activity against HIV-1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay	2016	Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13	Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1888709	Solubility in water at pH 2
AID1443670	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1124992	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID586899	Induction of ABCG2 protein expression in human LS180 cells at 1 umol/liter after 7 days by RT-PCR analysis relative to control	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1456310	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1171593	Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1561717	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag
AID1822273	Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1483286	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1561705	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1574381	Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV-1 NL4-3	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1773459	Resistance factor, ratio of EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1235379	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days MTT method	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1637396	Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1126510	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1191399	Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3	Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID496616	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39M, K46Q, V60I, S68G, D123E, I135V, S162A, K173A, Q174K,D177E, T200A, Q207E, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1126509	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1357792	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID508768	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1191403	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells	2015	Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3	Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1705183	Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells assessed as virus induced cytopathic effect by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1750725	Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y181C mutant	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID508630	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1316328	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1888697	Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1754640	Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID508648	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, T386A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508643	Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1572069	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1483291	Fold resistance, ratio of EC50 for reverse transcriptase Y181C mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID533677	AUC (0 to 12 hrs) in healthy human plasma at 200 mg, po twice a day for 4 days coadministered with 400 mg of raltegravir, po twice a day for 4 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1248225	Antiviral activity against HIV 1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1391083	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1819232	Aqueous solubility of the compound at pH 7.4 by HPLC analysis
AID1572526	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1520066	Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 as template/primer incubated for 40 mins by pico-green based spectrofluorometric analysis	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1763907	Inhibition of wild type HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in presence of template-primer incubated for 60 mins followed by transferring to streptavidin-coated plate and further incubation for 60 mins by ELISA	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1483302	Inhibition of recombinant wild type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as decrease in biotin-dUTP incorporation after 1 hr	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID417450	Inhibition of HIV1 wild type reverse transcriptase	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1410487	Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID586900	Activity at ABCB1	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID586903	Activity at MRP3	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID464771	Volume of distribution at steady state in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1483277	Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1520060	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1637394	Antiviral activity against human HIV-1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID586885	Induction of ABCC1 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1320867	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID522378	Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone to EC50 for wild type HIV1	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID619639	Antiviral activity against HIV-1 3B harboring RT F227L and V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID246299	Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1235376	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity incubated for 4 days by MTT method	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1316345	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID648420	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496622	Antiviral activity against HIV-1 subtype CRF06_cpx ontaining reverse transcriptase V106I/V21I, V35T, V60I, K122T, D123R, I135V, S162A, K173T, Q174K, D177E, I178L, T200A, Q207D, R211K, V245Q, E248D mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1811049	Aqueous solubility of compound in PBS at pH 7.4 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1316339	Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID518741	Antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1572051	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1443660	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1773441	Antiviral activity against wild type HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1862569	Antiviral activity against HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID709860	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID260237	Antiviral activity against HIV1 3B in MT2 cells by MTT assay	2006	Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3	Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508758	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1743626	Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID586908	Induction of MRP1 activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID508825	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID517497	Antiviral activity against HIV1 harboring reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID586893	Induction of ABCC3 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1811048	Aqueous solubility of compound in PBS at pH 7 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID508754	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1141976	Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting	2014	European journal of medicinal chemistry, Jun-10, Volume: 80	New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1741397	Inhibition of reverse transcriptase E138K mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID533676	AUC (0 to 12 hrs) in healthy human plasma at 200 mg, po twice a day for 8 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1775802	Antiviral activity against HIV-1 harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID738331	Cytotoxicity against mock-infected human MT4 cells assessed as cell viability after 5 days by MTT assay	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1750719	Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1446830	Solubility of the compound in 0.1 N HCl at pH 2	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1435504	Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1884487	Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1249718	Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID302621	Cytotoxicity against human MT2 cells by MTT assay	2007	Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22	From docking false-positive to active anti-HIV agent.
AID583854	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.5 multiplicities of infection after 6 days	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1163233	Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1326646	Inhibition of HIV-1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID464766	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1561715	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1888695	Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID246300	Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1197830	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1565094	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV RES056
AID1379961	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay	2017	European journal of medicinal chemistry, Nov-10, Volume: 140	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1572067	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1483290	Fold resistance, ratio of EC50 for reverse transcriptase K103N/Y181C double mutant in human MT4 cells infected HIV1 RES056 to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1637389	Antiviral activity against human HIV-1 3B harboring RES056 mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID533681	Tmax in healthy human plasma at 200 mg, po twice a day for 4 days coadministered with 400 mg of raltegravir, po twice a day for 4 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1880377	Antiviral activity against HIV-1 IIIB harboring reverse transcriptase K103N mutant infected in human MT4 cells by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID586905	Inhibition of ABCB1 activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1609110	Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1572077	Aqueous solubility of the compound at pH at 2 by HPLC analysis	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID508751	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1705190	Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1815385	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1275550	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1446812	Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1815404	Water solubility of compound at pH 7 at 0.1 to 10 mg by HPLC-UV analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1862566	Antiviral activity against HIV-1 K103N mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1298248	Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID767499	Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1207401	Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform
AID1773457	Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID586881	Inhibition of MRP3 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1636149	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase K103N/V179F/Y181C mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1069122	Antiviral activity against HIV harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1884224	Antiviral activity against HIV-1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID586910	Induction of BCRP activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1609106	Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1884493	Antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1815399	Inhibition of HIV1 reverse transcriptase Y181C mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1163232	Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1572056	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1750724	Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase K103N mutant	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1561722	Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam
AID614139	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 IIIB infected in human MT4 cells	2011	Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17	Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID709868	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1504697	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID236429	Area under the concentration time curve in human after 100 mg/kg oral dosage	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
AID1421310	Inhibition of HIV1 reverse transcriptase L100I/K103N double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1636929	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID1815395	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1561730	Inhibition of HIV1 RT K103N/Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1410488	Inhibition of HIV1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1572047	Aqueous solubility of the compound at pH at 7.4 by HPLC analysis	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID508753	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1421301	Inhibition of HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1357796	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1888704	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1248224	Selectivity index, ratio of CC50 for uninfected human MT4 cells to EC50 for wild type HIV 1 3B infected in human MT4 cells	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID106053	Inhibitory activity against 100I strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1565113	Sub-acute toxicity in Kunming mouse assessed as increase in alveolar interstitial thickening administered for 14 days measured on day 14 by HE-staining based assay
AID1705187	Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1754645	Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1750722	Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1391086	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1292009	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1197837	Solubility in water at pH 7.0 after 2 hrs by HPLC-UV method	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1888701	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1466764	Inhibition of wild-type HIV-1 3B reverse transcriptase infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 06-15, Volume: 27, Issue:12	Drug-like property-driven optimization of 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against rilpivirine-resistant mutant virus.
AID619641	Ratio of EC50 for HIV-1 3B harboring RT K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID586901	Activity at MRP1	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1561737	Solubility of the compound in pH 7.4 buffer by HPLC analysis
AID508651	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID701097	Antiviral activity against HIV1 harboring reverse transcriptase L100I/K103N mutant	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1862571	Antiviral activity against HIV-1 K103N-Y181C mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1565115	Sub-acute toxicity in Kunming mouse assessed as increase in proximal convoluted tubule edema administered for 14 days measured on day 14 by HE-staining based assay
AID518738	Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1775799	Antiviral activity against HIV-1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1884488	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1880369	Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1483280	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1483276	Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1815377	Anti-HIV activity against HIV-1 IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1157594	Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1815382	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1815398	Inhibition of HIV1 reverse transcriptase K103N mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1456306	Inhibition of HIV-1 3B wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1357804	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1126506	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1316337	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1561700	Antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1561716	Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in absence of test compound assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1457053	Antiviral activity against HIV1 NL4-3 infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1435516	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase E138K mutant
AID1126508	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8	Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1884225	Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1171413	Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay	2014	ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11	Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID698145	Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate	2012	Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14	New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID541250	Antiviral activity against multidrug resistant HIV1 RTMDR containing reverse transcriptase L74V, M41L, V106A and T215Y mutant infected in human TZM-bl cells after 4 days by luciferase reporter gene assay	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246298	Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID701096	Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1637398	Antiviral activity against human HIV-1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID83550	Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID1316333	Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1687682	Antiviral activity against HIV-1 Y181C mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1819213	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB harboring K103N/Y181C double mutant infected in human MT4 cells
AID1446818	Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1520057	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1775793	Antiviral activity against HIV-1 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1609104	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1561693	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1811071	Oral bioavailability in Sprague-Dawley rat at 5 mg/kg by LCMS analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1410408	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID517492	Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1410482	Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1811044	Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1275548	Antiviral activity against HIV1 3B expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID508757	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1435509	Antiviral activity against HIV1 RES056 expressing reverse transcriptase mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1357798	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID476470	Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1435503	Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay
AID1761017	Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1504702	Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1815405	Water solubility of compound at pH 7.4 at 0.1 to 10 mg by HPLC-UV analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1729160	Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1884226	Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1822280	Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1636928	Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID557066	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K101P mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1687684	Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID665272	Antiviral activity against HIV1 RES056 harboring K103N/Y181C RT mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID508635	Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1741393	Inhibition of reverse transcriptase L100I mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID508759	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1888705	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1197833	Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID508833	Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1743637	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID557036	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1572059	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1884539	Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1304403	Cytotoxicity against mock-infected human MT4 cells	2016	Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13	Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy.
AID1574386	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1773444	Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells
AID1637393	Antiviral activity against human HIV-1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1561739	Solubility of the compound in pH 2.0 buffer by HPLC analysis
AID1152372	Antiviral activity against HIV1 RES056 harboring RT K103N,Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay	2014	Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12	Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID586879	Inhibition of MRP1 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID83547	Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID508639	Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1171578	Cytotoxic activity against human MT4 cells by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1235378	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity incubated for 4 days by MTT method	2015	Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15	Hybrid chemistry. Part 4: Discovery of etravirine-VRX-480773 hybrids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1822276	Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1558849	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1157587	Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID496619	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase A98G/V35T, V60I, I135L, S162A, K173A, Q174K, D177E, I178M, T200A,Q207E, R211K, V245Q, D250E mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID632795	Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID508781	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID522373	Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1880380	Antiviral activity against HIV-1 IIIB harboring reverse transcriptase E138K mutant infected in human MT4 cells by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1888694	Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1773830	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 infected in human MT4 cells	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1352322	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID508634	Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1811037	Anti-viral activity against HIV1 harboring RT K103N mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1157584	Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1391085	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1320865	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1637403	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring E138K mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID484395	Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 200 uM by dynamic light scattering assay in presence of 1% DMSO	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID465419	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1316336	Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1326647	Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by cell titer glo based luciferase reporter gene assay	2016	European journal of medicinal chemistry, Oct-21, Volume: 122	Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1.
AID1171583	Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1819233	Aqueous solubility of the compound at pH 7.0 by HPLC analysis
AID1561698	Antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID484275	Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID1815381	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID557019	Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID586887	Induction of ABCC4 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1609105	Selectivity index, ratio of CC50 for human MT4 cells to EC50 of antiviral activity against HIV-1 IIIB infected in human MT4 cells	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1729157	Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1637400	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring K103N mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID508767	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1572522	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells
AID508762	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1457061	Ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1888690	Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID738333	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1750721	Inhibition of HIV-1 p66/p51 reverse transcriptase E138K mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID557067	Plasma protein binding in HIV1 infected patient	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1884222	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 to 7 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1561726	Inhibition of HIV1 RT Y181C mutant in presence of reconstituted template and viral nucleotides [digoxigenin (DIG)-dUTP, biotin-dUTP and dTTP] incubated for 1 hr by ELISA method
AID1693799	Antiviral activity against HIV-3B infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID1741399	Inhibition of reverse transcriptase RES056 mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1705188	Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1731755	Solubility in water at pH 7 at 0.1 to 10 mg
AID586883	fCmax in human plasma at 200 mg bid after 8 days	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID632801	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1761009	Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID465418	Antiviral activity against wild type HIV1 infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1457056	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1691438	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID490368	Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID586886	Induction of ABCC2 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1558855	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1705192	Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1609109	Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1197835	Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA after 1 hr using poly(A) x oligo(dT)15 template/primer hybrid, digoxigenin and biotin-labeled nucleotides	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1457066	Inhibition of HIV1 reverse transcriptase p66 K103N/Y1881C double mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintilla	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID259755	Cytotoxicity against MT2 cells	2006	Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3	Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1483293	Fold resistance, ratio of EC50 for reverse transcriptase F227L/V106A double mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID476473	Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase K103N/Y181C mutation by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1583024	Antiviral activity against HIV1 containing reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID586898	Induction of ABCB1 protein expression in human LS180 cells at 1 umol/liter after 7 days by RT-PCR analysis relative to control	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID508797	Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1435510	Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay
AID1504705	Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1731747	Inhibition of reverse transcriptase K103N mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID464772	Oral bioavailability in Beagle dog at 4 mg/kg, po	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1705196	Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase Y188L mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1072807	Antiviral activity against HIV1 harboring reverse transcriptase K101N mutant infected in human MT4 cells	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID1152371	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay	2014	Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12	Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1773826	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID508771	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1197834	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID508778	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID586892	Induction of ABCB1 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1561736	Aqueous solubility of the compound in pH 7 buffer
AID1572052	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1446831	Lipophilicity, log P of the compound	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1815403	Water solubility of compound at pH 2 at 0.1 to 10 mg by HPLC-UV analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID476471	Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase Y181C mutation by MTT assay	2010	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8	Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives.
AID1292011	Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1379959	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay	2017	European journal of medicinal chemistry, Nov-10, Volume: 140	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID522369	Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1609107	Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1888708	Solubility in water at pH 7
AID1171584	Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1637402	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y188L mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID522577	Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I mutant clone to EC50 for wild type HIV1	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1391080	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID583853	Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as inhibition of virus-induced cell death at 0.05 multiplicities of infection after 6 days	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1124991	Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID1888700	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1163254	Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1572524	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1815401	Inhibition of HIV1 reverse transcriptase E138K mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1207464	Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform
AID635302	Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1754647	Antiviral activity against HIV1 harboring RT RES056 mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1763898	Antiviral activity against HIV-1 IIIB harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1249720	Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1773454	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells
AID1565114	Sub-acute toxicity in Kunming mouse assessed as increase in alveolar hemorrhage administered for 14 days measured on day 14 by HE-staining based assay
AID1320868	Solubility of the compound	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1275552	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1298243	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID106074	Inhibitory activity against LAI strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID698956	Antiviral activity against HIV-1 NL4-3 infected in human TZM-bl cells assessed as inhibition of viral replication after 2 days by luciferase reporter gene based luminescence assay	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.
AID1729158	Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID698146	Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate	2012	Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14	New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508621	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1141978	Inhibition of HIV1 wild-type reverse transcriptase L1001 mutant using [3H]dTTP by scintillation counting	2014	European journal of medicinal chemistry, Jun-10, Volume: 80	New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1316340	Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID1410481	Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID484383	Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 10 uM by dynamic light scattering assay in presence of 1% DMSO	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID709836	Ratio of EC50 for HIV1 expressing wild type reverse transcriptase in presence of human serum albumin and human alpha-1 acid glycoprotein to EC50 for HIV1 expressing wild type reverse transcriptase	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1574374	Antiviral activity against HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID508641	Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID557038	Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1574372	Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID541251	Resistance index, ratio of EC50 for multidrug resistant HIV1 RTMDR to EC50 for wild type HIV1 NL4-3	2010	Journal of medicinal chemistry, Dec-09, Volume: 53, Issue:23	Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID449195	Antimalarial activity against Plasmodium falciparum W2mef at 10 uM after 48 hrs by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID1815389	Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1882474	Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1743639	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L/V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1763904	Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1457052	Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1811035	Anti-viral activity against HIV1 harboring RT Y188L mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID347627	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 16 with reverse transcriptase K103, P225 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID586894	Induction of CYP3A5 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1231486	Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13	Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID1773440	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID619642	Ratio of EC50 for HIV-1 3B harboring RT E138K mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1357793	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1298247	Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID1773828	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID1249714	Antiviral activity against HIV1 3B expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1775792	Antiviral activity against NNRTI-resistant HIV-1 RES056 harboring RT K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID236424	Area under the concentration time curve in rat after 40 mg/kg oral dosage	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
AID1609108	Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID709867	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1561711	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1691436	Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1483288	Fold resistance, ratio of EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1637395	Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID619634	Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID557063	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase Y181I mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1636930	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method	2016	Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20	Computer-aided discovery of anti-HIV agents.
AID522377	Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone to EC50 for wild type HIV1	2010	Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4	Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine.
AID1565098	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1754638	Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID246343	Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1691437	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1292010	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1191402	Cytotoxicity against human MT4 cells after 5 days MTT assay	2015	Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3	Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID347626	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 14 with reverse transcriptase A98, K103, V108, M230 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1815386	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1206938	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	European journal of medicinal chemistry, Jun-05, Volume: 97	Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID709869	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1729156	Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID518734	Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1572521	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells
AID1165074	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2014	European journal of medicinal chemistry, Nov-24, Volume: 87	Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1743621	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1456308	Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8	Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID573476	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1298249	Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry	2016	Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11	1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus.
AID709870	Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508795	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508647	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1171596	Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID383498	Partition coefficient, log P of the compound	2008	European journal of medicinal chemistry, Mar, Volume: 43, Issue:3	SAR and QSAR studies: modelling of new DAPY derivatives.
AID1249721	Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1249715	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID508632	Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1888702	Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells
AID1750714	Antiviral activity against HIV-1 infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID693583	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID464770	Half life in Beagle dog at 0.5 mg/kg, iv or 0.5 mg/kg, po	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID573481	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1249722	Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1775795	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability for 5 days by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-ind	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID573469	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1888689	Antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID449273	Antimalarial activity against Plasmodium falciparum W2mef trophozoite form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID508827	Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID417446	Inhibition of HIV1 reverse transcriptase L100I mutant	2009	European journal of medicinal chemistry, Feb, Volume: 44, Issue:2	QSAR studies for diarylpyrimidines against HIV-1 reverse transcriptase wild-type and mutant strains.
AID1572070	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID557068	Plasma protein binding in healthy human at 200 mg/kg	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1171582	Antiviral activity against HIV2 ROD infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1862561	Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1207341	Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID1691434	Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in to cDNA chain at 0.267 uM in presence of DIG-dUTP, biotin-dUTP and dTTP measured after 1 hr by ELISA relative to control	2020	European journal of medicinal chemistry, May-01, Volume: 193	In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID557037	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID635301	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID586907	Induction of ABCB1 activity	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1773442	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
AID1357800	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1352321	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103 N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID508784	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1819212	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells
AID693587	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID1693800	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 01-15, Volume: 30	Novel indolylarylsulfone derivatives as covalent HIV-1 reverse transcriptase inhibitors specifically targeting the drug-resistant mutant Y181C.
AID490372	Antiviral activity against HIV1 expressing reverse transcriptase V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1124989	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID619643	Ratio of EC50 for HIV-1 3B harboring RT L100I mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID347631	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 29 with reverse transcriptase K103, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID693585	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Dec, Volume: 58	Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID1815394	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID246344	Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	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.
AID1811036	Anti-viral activity against HIV1 harboring RT Y181C mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1882471	Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID508644	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1773447	Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID767498	Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1687680	Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay	2020	European journal of medicinal chemistry, Jan-15, Volume: 186	Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1731746	Inhibition of reverse transcriptase L100I mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID518739	Selectivity ratio of IC50 for DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1171589	Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1880372	Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID508793	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID635345	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID259754	Antiviral activity against wild-type HIV1 in MT2 cells by MTT assay	2006	Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3	Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508625	Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID619635	Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1729159	Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1483279	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1316335	Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID632804	Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID573479	Antiviral activity of Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID586880	Inhibition of MRP2 expressed in MDCK2 cells assessed as cell growth inhibition by calcein and pheophorbide A efflux assays	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1888691	Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay
AID1731744	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1483287	Fold resistance, ratio of EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID726437	Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID1171580	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1815388	Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1574387	Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1200845	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1811045	Cytotoxicity against mock infected human MT4 cells by MTT assay	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1609103	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay	2019	European journal of medicinal chemistry, Nov-15, Volume: 182	Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1761007	Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 1 day by CytoTox-Glo assay	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID632796	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID1520061	Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1421298	Inhibition of HIV1 LAI reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay	2018	European journal of medicinal chemistry, Oct-05, Volume: 158	Advances in diarylpyrimidines and related analogues as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1561697	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells
AID1572525	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1574371	Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in human MT4 cells	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1763902	Antiviral activity against HIV-1 IIIB harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1773439	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1882469	Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID632797	Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection	2011	Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24	Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents.
AID665273	Antiviral activity against HIV2 ROD mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID557064	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase F227C mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1487263	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
AID586877	Inhibition of MDR1 expressed in MDCK2 cells assessed as inhibition of cell proliferation by calcein and pheophorbide A efflux assays	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1487261	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
AID508622	Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1483289	Fold resistance, ratio of EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1558857	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1561694	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1811047	Aqueous solubility of compound in PBS at pH 2 by HPLC-UV analysis	2021	Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14	Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs.
AID1391076	Inhibition of wild type HIV1 reverse transcriptase using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1731754	Solubility in water at pH 2 at 0.1 to 10 mg
AID635347	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B	2011	Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23	Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1457054	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1357805	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1773838	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID726436	Cytotoxicity in human MT2 cells assessed as inhibition of cell growth	2013	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4	Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency.
AID1880373	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1320864	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Oct-04, Volume: 121	Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1773445	Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1379963	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2017	European journal of medicinal chemistry, Nov-10, Volume: 140	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1572531	Solubility of the compound in deionized water at pH 7
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1822283	Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID573482	Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID83551	Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID1124990	Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay	2014	Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7	Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.
AID1591876	Solubility of the compound in water at pH 7	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase.
AID573477	Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1583029	Antiviral activity against HIV1 containing reverse transcriptase F227L+V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1457065	Inhibition of HIV1 reverse transcriptase p66 Y181I mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1558853	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1862563	Cytotoxicity against human MT4 cells assessed as reduction on cell growth by MTT assay
AID584239	Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase Y181C, V179V/D mutant derived from 17 days viral passages with lersivirine infected in human SupT1 cells assessed as inhibition of viral replication after 21 days relative to wild type	2010	Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10	Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1637404	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring F227L/V106A double mutant infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID1572068	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID106049	Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cells	2001	Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17	Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID573473	Antiviral activity of wild-type Human immunodeficiency virus 1 harboring Y181C mutation in reverse transcriptase infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1191401	Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3	Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1880379	Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y188L mutant infected in human MT4 cells by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID449275	Cytotoxicity against human erythrocytes assessed as intact cells by propidium iodide stain based flow cytometry	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID508649	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1200846	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID533675	Trough drug concentration at 12 hrs in healthy human plasma at 200 mg, po twice a day for 4 days coadministered with 400 mg of raltegravir, po twice a day for 4 days by reverse-phase HPLC-MS method	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects.
AID1754643	Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1572063	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1637388	Antiviral activity against human HIV-1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID464767	Binding affinity to human serum albumin	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID508752	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1410485	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1561703	Antiviral activity against HIV1 expressing RT F227L + V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID701102	Antiviral activity against wild type HIV1	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID1743627	Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID586888	Induction of ABCC5 mRNA expression in human LS180 cells at 0.1 to 1 umol/liter after 4 days by RT-PCR analysis	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID586902	Activity at MRP2	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1357802	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1163234	Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1410411	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site.
AID1637391	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B infected in human MT4 cells	2016	Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18	Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
AID496632	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39L, K122E, D123N, S162A, E169T, K173E, Q174E, D177E,T200A, I202V, Q207E mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID738332	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID484274	Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100	2010	Journal of medicinal chemistry, May-27, Volume: 53, Issue:10	Colloid formation by drugs in simulated intestinal fluid.
AID1565090	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1741394	Inhibition of reverse transcriptase K103N mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1446815	Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1249713	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID496621	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/V35T, E36D, K49R, V60I, K122P, I135R, S162A, E169R, K173T, Q174E,D177E, V189I, T200A, I202V, Q207E, R211K, V245Q mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1882470	Antiviral activity against HIV-1 harboring K103N/Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay	2022	Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5	Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID1822279	Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID1572061	Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID496627	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K32R, V35E, T39S, S48T, V60I, D121Y, K122E, I135T, S162A, K173A, Q174K, D177E, V179I, T200E, Q207D, R211K mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1572057	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1391081	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1157593	Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID83552	Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu	2004	Journal of medicinal chemistry, May-06, Volume: 47, Issue:10	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
AID1594856	Half life in human serum at 200 mg, bid	2019	Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10	The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID1773452	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells
AID464768	Half life in human microsomes	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1418466	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22	Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID1171588	Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1880376	Antiviral activity against HIV-1 IIIB harboring reverse transcriptase L1001 mutant infected in human MT4 cells by MTT assay	2022	Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12	Structure-Based Discovery of Novel NH
AID1504696	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID557029	Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1750716	Selectivity index, ratio of CC50 for human MT-4 cells to EC50 for HIV-1 infected in MT-4 cells	2021	Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8	Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from
AID1171579	Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1197832	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1819210	Antiviral activity against HIV-1 IIIB harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay
AID508773	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181V mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1884486	Antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID490369	Antiviral activity against wild type HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect in presence of 40 % human serum	2010	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14	Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
AID1152373	Cytotoxicity against human MT4 cells by MTT assay	2014	Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12	Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1565100	Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1743638	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1069126	Antiviral activity against wild-type HIV infected in human MT4 cells assessed as inhibition of viral infection in presence of 50% normal human serum	2014	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 24, Issue:3	Discovery of MK-1439, an orally bioavailable non-nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses.
AID1352316	Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay	2018	European journal of medicinal chemistry, Feb-10, Volume: 145	Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1819218	Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1741400	Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based fluorescence assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1249716	Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay	2015	European journal of medicinal chemistry, Sep-18, Volume: 102	Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1483275	Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1561710	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect
AID508789	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1729149	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1636146	Antiviral activity against wild type HIV1 NL4-3	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1862567	Antiviral activity against HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in viral replication by MTT assay
AID1741395	Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1741392	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID709858	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181I/V179F double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID518740	Antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay	2010	Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6	The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
AID1357797	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID1574376	Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID1743622	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 RES056 infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID508755	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID709865	Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C/F227C double mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay	2012	Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23	Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1275547	Antiviral activity against HIV1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay	2016	European journal of medicinal chemistry, Feb-15, Volume: 109	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1504694	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID573467	Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1457064	Inhibition of HIV1 reverse transcriptase p66 K103N mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID1443667	Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID508798	Ratio of EC50 for HIV1 in presence of 50% human serum to EC50 for HIV1 in absence of serum proteins by GFP assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1443664	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID508787	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1561696	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID236595	pKa value was determined	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Concentration and pH dependent aggregation of hydrophobic drug molecules and relevance to oral bioavailability.
AID1572078	Aqueous solubility of the compound in FASSIF by HPLC analysis	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1596751	Antiviral activity against wild type HIV-1 3B infected in MT4 cells measured after 5 days by MTT assay	2019	European journal of medicinal chemistry, Aug-15, Volume: 176	Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID1888692	Selectivity index, ratio of CC50 for toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induc
AID496630	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase Y181C/V35T, V60I, I135V, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K, H221Y mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID517499	Antiviral activity against HIV1 harboring reverse transcriptase K103N/L100I double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect by replication assay in presence of 10% FBS	2010	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20	Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
AID1884538	Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells	2022	European journal of medicinal chemistry, Aug-05, Volume: 238	Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1729151	Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp
AID1171590	Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID767497	Cytotoxicity against human MT2 cells assessed as growth inhibition	2013	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18	Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID508760	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V108I mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1705191	Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1574384	Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysis	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID573478	Antiviral activity of Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1773446	Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1761012	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells	2021	European journal of medicinal chemistry, Feb-05, Volume: 211	Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1316338	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay	2016	Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17	Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
AID557028	Ratio of EC95 for HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant in presence of 50% human serum to EC95 for HIV1 isolate R8 harboring wild type reverse transcriptase in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1815391	Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1583025	Antiviral activity against HIV1 containing reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3	Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.
AID1815397	Inhibition of HIV1 reverse transcriptase L100I mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1775800	Antiviral activity against HIV-1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay	2021	Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7	2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies.
AID1391088	Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1741390	Inhibition of reverse transcriptase in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID573472	Antiviral activity of wild-type Human immunodeficiency virus 1 infected in human TZM-bl cells human assessed as inhibition of viral replication by luciferase reporter gene assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID619640	Antiviral activity against HIV-1 3B harboring RT K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID1558858	Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis	2019	Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24	Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID508766	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508770	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID614140	Cytotoxicity against human MT4 cells after 4 days by MTT assay	2011	Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17	Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
AID1504700	Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1773451	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells
AID1197829	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	2015	European journal of medicinal chemistry, Mar-06, Volume: 92	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches.
AID1773843	Inhibition of wild type HIV1 p66/p51 reverse transcriptase using poly(rA) as template, oligo(dT)16 as primer and RNA/DNA as substrate measured after 40 mins by PICOGreen-dye based spectrofluorimetry analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18	Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.
AID665274	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1379964	Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 assessed as reduction in biotin-dUTP incorporation incubated for 40 mins using poly(rA) template and oligo(dT)16 primer by picogreen dye based spectrofluorometry	2017	European journal of medicinal chemistry, Nov-10, Volume: 140	Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1763903	Antiviral activity against HIV-1 IIIB harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 06-15, Volume: 40	Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1819216	Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID665271	Antiviral activity against HIV1 3B harboring wild type RT infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2012	European journal of medicinal chemistry, Jul, Volume: 53	Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1565093	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID276231	Antiviral activity against HIV1 3B in MT2 cells	2006	Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21	Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1504703	Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID1487264	Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation at 50 uM using poly(A)/oligo(dT)15 as template/primer by ELISA relative to control	2017	Bioorganic & medicinal chemistry, 08-15, Volume: 25, Issue:16	Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.
AID1636148	Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase A98G/K101E/Y181C/G190A mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells	2016	Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15	Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors.
AID1457057	Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay	2017	Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15	Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents.
AID648421	Cytotoxicity against human MT4 cells after 5 days by MTT assay	2012	European journal of medicinal chemistry, May, Volume: 51	Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID586896	Induction of ABCG2 mRNA expression in human LS180 cells at 1 umol/liter after 4 days by RT-PCR analysis relative to beta-glucuronidase gene expression	2011	Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3	Interaction potential of etravirine with drug transporters assessed in vitro.
AID1292013	Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells	2016	European journal of medicinal chemistry, Jun-10, Volume: 115	Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1504698	Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2017	ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11	Discovery of Thiophene[3,2-
AID347632	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 31 with reverse transcriptase A98, V179, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1705195	Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1410484	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells	2018	ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4	Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery.
AID1163230	Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1248223	Cytotoxicity against uninfected human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay	2015	Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20	A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1754649	Water solubility of compound at pH 2	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID619637	Antiviral activity against HIV-1 3B harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	2011	European journal of medicinal chemistry, Oct, Volume: 46, Issue:10	Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors.
AID508779	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID464764	Antiviral activity against wild type HIV1 infected in human MT2 cells	2010	Bioorganic & medicinal chemistry letters, Mar-01, Volume: 20, Issue:5	N1-Heterocyclic pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1072797	Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA	2014	Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6	Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
AID1572055	Selectivity ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1157586	Antiviral activity against MDR-resistant HIV1 harboring 41L, 74V, 106A, 215Y mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay	2014	Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12	Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1171598	Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID557041	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID449277	Cytotoxicity against human erythrocytes assessed as change in cell shape by flow cytometry	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID1561699	Antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1572073	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild type HIV1	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID347634	Antiviral activity against NNRTI-resistant HIV HXB2 isolate 34 with reverse transcriptase K101, V106, Y181 mutation in human MT4 cells assessed as protection against virus-induced cell death after 5 days by MTT assay	2008	Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23	Design of annulated pyrazoles as inhibitors of HIV-1 reverse transcriptase.
AID1163231	Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs	2014	Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19	From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1171586	Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1743635	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells	2020	European journal of medicinal chemistry, Nov-15, Volume: 206	Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1446811	Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay	2017	European journal of medicinal chemistry, Apr-21, Volume: 130	Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID508761	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, F227L mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID508645	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1572076	Aqueous solubility of the compound at pH at 7 by HPLC analysis	2019	Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3	Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
AID1483281	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B	2017	Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10	Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
AID1822303	Oral bioavailability in Sprague-Dawley rat at 5 mg/kg administered via gavage measured up to 24 hrs by LCMS analysis	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK.
AID449274	Antimalarial activity against Plasmodium falciparum W2mef schizont form by hoechst 33342-thiazole orange stain based flow cytometry assay	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
AID1741396	Inhibition of reverse transcriptase Y188L mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1200847	Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant	2015	European journal of medicinal chemistry, Mar-26, Volume: 93	Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1705193	Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1390713	Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells	2018	Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8	First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain.
AID557065	Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase M230L mutant relative to drug-sensitive HIV1 CNDO	2009	Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6	Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1391082	Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1705194	Inhibition of RNA-dependent DNA polymerase activity of wild type recombinant HIV-1 His-tagged p66/p51 reverse transcriptase assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintilla	2020	European journal of medicinal chemistry, Dec-15, Volume: 208	New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1171597	Inhibition of wild type HIV1 reverse transcriptase V106A mutant assessed as reduction in enzyme activity	2014	Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23	Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1888698	Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1561713	Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells
AID1391087	Antiviral activity against HIV1 harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay	2018	Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8	The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
AID1357799	Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B	2018	European journal of medicinal chemistry, May-10, Volume: 151	Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus.
AID701095	Half life in plasma	2012	Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8	Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
AID508783	Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID1572528	Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID1889295	Aqueous solubility of the compound	2022	Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3	Dose Number as a Tool to Guide Lead Optimization for Orally Bioavailable Compounds in Drug Discovery.
AID573475	Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1754644	Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1731743	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID496618	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, V60I, K122E, D123S, I135V, E138D, S162A, K173T,Q174S, D177E, I178M, V189I, T200A, I202V, Q207E, F214L, V245Q mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1574378	Antiviral activity against HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	2019	Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2	Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones.
AID508826	Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1.
AID573470	Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay	2009	Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11	Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
AID1731752	Inhibition of reverse transcriptase RES056 mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay
AID1418463	Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay	2018	Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22	Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine.
AID496623	Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/G18V, Q23P, V35T, E40D, V60I, S68G, D123E, I135V, S162A, K173T, Q174N, T200A, Q207E, R211K, F214L mutant relative to control	2010	Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2	Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes.
AID1801807	HIV-1 RT Inhibition Assay from Article 10.1111/cbdd.12751: \\Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.\\	2016	Chemical biology & drug design, 08, Volume: 88, Issue:2	Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.
AID1801345	In vitro Anti-HIV RT Assay from Article 10.1111/cbdd.12497: \\Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents.\\	2015	Chemical biology & drug design, Sep, Volume: 86, Issue:3	Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents.
AID1745855	NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854	NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS	2023	Disease models & mechanisms, 03-01, Volume: 16, Issue:3	In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	144 (26.52)	29.6817
2010's	342 (62.98)	24.3611
2020's	57 (10.50)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	90 (15.73%)	5.53%
Reviews	63 (11.01%)	6.00%
Case Studies	27 (4.72%)	4.05%
Observational	10 (1.75%)	0.25%
Other	382 (66.78%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (60)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
An Open-Label Trial With TMC125 in HIV-1 Infected Subjects, Who Were Randomized to a TMC125 Treatment Arm in a Sponsor-Selected TMC125 Trial and Were Treated for at Least 48 Weeks [NCT00128830]	Phase 2	211 participants (Actual)	Interventional	2005-06-30	Completed
An Open-label Trial With TMC125 as Part of an ART Including TMC114/Rtv and an Investigator-selected OBR in HIV-1 Infected Subjects Who Participated in a DUET Phase III Trial (TMC125-C206 or TMC125-C216). [NCT00359021]	Phase 3	503 participants (Actual)	Interventional	2006-06-30	Completed
A Randomised, Open Label, Prospective Study to Assess Two Different Therapeutic Strategies Following First Treatment Failure in HIV-1 Infected Subjects [NCT01118871]	Phase 4	3 participants (Actual)	Interventional	2010-05-31	Terminated
Open-Label, Single-Sequence Study to Evaluate the Pharmacokinetic Interaction of BMS-663068 With Darunavir/Ritonavir and/or Etravirine in Healthy Subjects [NCT02063360]	Phase 1	42 participants (Actual)	Interventional	2014-02-01	Completed
A Phase III Randomized, Double-blinded, Placebo-controlled Trial to Investigate the Efficacy, Tolerability and Safety of TMC125 as Part of an ART Regimen, Including TMC114/RTV and an Investigator-selected OBR, in HIV-1 Infected Patients With Limited Treat [NCT00255099]	Phase 3	593 participants (Actual)	Interventional	2005-12-31	Completed
Continued Access to Etravirine (ETR) in Treatment Experienced HIV-1 Infected Subjects [NCT00980538]	Phase 3	180 participants (Actual)	Interventional	2009-12-09	Active, not recruiting
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]		1,578 participants (Actual)	Observational	2003-06-09	Completed
Plasma and Intracellular Concentrations of Raltegravir and Etravirine Administered Once Daily (800 mg and 400 mg, Respectively) Compared With Standard Dosing (400 mg and 200 mg/12 h) in Patients With HIV Infection [NCT01121809]	Phase 4	16 participants (Actual)	Interventional	2010-04-30	Completed
A Phase I, Open-label Trial to Investigate the Pharmacokinetic Effect of Multiple-dose TMC125 on Buprenorphine and Norbuprenorphine Administered in HIV-negative Subjects on Stable Buprenorphine/Naloxone Maintenance Therapy. [NCT00828815]	Phase 1	22 participants (Actual)	Interventional	2009-03-31	Completed
A Phase 1, Open-label, Fixed-sequence, 2-Panel Study to Assess the Effects of Itraconazole and Etravirine on the Single-dose Pharmacokinetics of JNJ-64417184 in Healthy Adult Subjects [NCT04208373]	Phase 1	32 participants (Actual)	Interventional	2019-12-20	Completed
A Phase I, Open-label Trial to Investigate the Pharmacokinetic Interaction Between TMC125 and Two Antifungal Agents (Fluconazole and Voriconazole), All at Steady-state in Healthy Subjects. [NCT00740389]	Phase 1	18 participants (Actual)	Interventional	2008-09-30	Completed
Antiretroviral Activity and Tolerability of Once Daily Etravirine in Treatment-Naïve Adults With HIV-1 Infection [NCT00959894]	Phase 2	80 participants (Actual)	Interventional	2009-09-30	Completed
A Phase I, Open Label Crossover Study to Evaluate the Effect of Etravirine on GSK1265744 Pharmacokinetics in Healthy Adult Subjects [NCT00920296]	Phase 1	12 participants (Actual)	Interventional	2009-07-31	Completed
Evaluation of the Capacity of a Weekly Strategy of 4 Consecutive Days on Treatment Followed by 3 Days Off Treatment, in HIV-1 Infected Patients With Undetectable Viral Load for at Least 12 Months, to Maintain a Virological Success With This Intermittent M [NCT02157311]	Phase 3	100 participants (Actual)	Interventional	2014-07-31	Completed
IMPAACT P1058A: Intensive Pharmacokinetic Studies of New Classes of Antiretroviral Drug Combinations in Children, Adolescents and Young Adults [NCT00977756]		168 participants (Actual)	Observational	2002-08-31	Completed
A Phase I, Open-label, Randomized Cross-over, 2-period, 2-way Interaction Trial to Investigate the Pharmacokinetic Interaction Between Lopinavir/Ritonavir and TMC125 Both at Steady-state in Healthy Subjects. [NCT00767117]	Phase 1	16 participants (Actual)	Interventional	2008-09-30	Completed
A Prospective Longitudinal Pilot Study to Measure the Effect of Intensification With Raltegravir +/- a Protease Inhibitor (PI) or Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) on HIV-1 Levels in the Gut [NCT00884793]		8 participants (Actual)	Interventional	2008-09-30	Completed
TMC125-TiDP2-C238: A Randomized, Exploratory, Open-label 48-week Trial to Investigate the Pharmacokinetics, Safety, Tolerability and Antiviral Activity of Etravirine (ETR) in Combination With Ritonavir-boosted Atazanavir (ATV/Rtv) and 1 NRTI in Treatment- [NCT00896051]	Phase 2	50 participants (Actual)	Interventional	2009-08-31	Completed
Open Label Phase 3b, 48 wk Pilot Study of the Antiviral Efficacy and Tolerability of Combination of PREZISTA/r and TMC125 When Substituted for Enfuvirtide, Current Protease Inhibitor(s) and NNRTI(s) in Antiretroviral Resistant Patients With Viral Suppress [NCT00460746]	Phase 3	10 participants (Actual)	Interventional	2007-05-31	Completed
A Phase 2b Multicenter, Randomized, Comparative Trial Of Uk-453,061 Versus Etravirine In Combination With Darunavir/Ritonavir And A Nucleotide/Nucleoside Reverse Transcriptase Inhibitor For The Treatment Of Antiretroviral Experienced Hiv-1 Infected Subjec [NCT00823979]	Phase 2	105 participants (Actual)	Interventional	2009-03-25	Terminated(stopped due to See termination reason in detailed description.)
A Single Arm, Open Label Study to Assess the Pharmacokinetics of Darunavir and Ritonavir, Darunavir and Cobicistat, Etravirine, and Rilpivirine in HIV-1 Infected Pregnant Women [NCT00855335]	Phase 3	77 participants (Actual)	Interventional	2009-04-09	Completed
A Multicenter, Single Arm, Open-Label Study of the Once Daily Combination of Etravirine and Darunavir/Ritonavir As Dual Therapy in Early Treatment-Experienced Patients [NCT01199939]	Phase 2	54 participants (Actual)	Interventional	2010-05-31	Completed
A Multicenter, Randomized, Open, Comparative Trial Of Maraviroc Versus Etravirine Each In Combination With Darunavir/Ritonavir And Raltegravir For The Treatment Of Antiretroviral-Experienced HIV-1 Subjects Co-Infected With Hepatitis C And/Or Hepatitis B [NCT00782301]	Phase 4	0 participants (Actual)	Interventional	2009-03-31	Withdrawn
A Phase II, Open-label Trial, to Evaluate the Safety, Tolerability and Antiviral Activity of TMC125 in Antiretroviral Experienced HIV-1 Infected Children and Adolescents [NCT00665847]	Phase 2	103 participants (Actual)	Interventional	2008-11-30	Completed
CID 0708 - Sex, Aging and Antiretroviral Pharmacokinetics [NCT00666055]		11 participants (Actual)	Observational	2008-03-31	Completed
Pilot Study to Assess the Efficacy and Safety of Switching Protease Inhibitor to Etravirine in HIV-1-infected Subjects With Viremia Suppression [NCT01034917]	Phase 3	43 participants (Actual)	Interventional	2009-12-31	Completed
Clinical Trial to Evaluate Drug-drug Interactions Between Darunavir/Cobicistat and Etravirine in Hiv- Infected Patients [NCT02818348]	Phase 1	30 participants (Actual)	Interventional	2016-06-30	Completed
A Phase IV 48 Week, Open Label, Pilot Study of Kaletra and Intelence Tablets in Naive Subjects [NCT01045369]	Phase 4	30 participants (Anticipated)	Interventional	2010-01-31	Completed
A Phase I, Open Label, Randomized, Three Period, One-way, Two Cohort, Adaptive Crossover Study to Evaluate the Effect of Darunavir/Ritonavir Plus Etravirine and Lopinavir/Ritonavir Plus Etravirine on GSK1349572 Pharmacokinetics in Healthy Adult Subjects ( [NCT00867152]	Phase 1	17 participants (Actual)	Interventional	2009-04-30	Completed
Effects of Etravirine (INTELENCETM) on Endothelial Function in HIV-uninfected Adults: A Pilot Study [NCT00871234]	Phase 1	28 participants (Actual)	Interventional	2009-04-30	Completed
A Phase III, Double Blind, Mulit-centre, Randomised Placebo Controlled, Pilot Study to Assess the Feasibility of Switching Individuals Receiving Efavirez With Continuing Central Nervous System (CNS) Toxicity to TMC125. [NCT00792324]	Phase 3	24 participants (Actual)	Interventional	2008-06-30	Completed
The Optimized Treatment That Includes or Omits NRTIs Trial: A Randomized Strategy Study for HIV-1-Infected Treatment-Experienced Subjects Using the cPSS to Select an Effective Regimen [NCT00537394]	Phase 3	517 participants (Actual)	Interventional	2008-01-31	Completed
A Multicenter Study to Evaluate the Pharmacokinetic Profile and Safety of TMC125 Plus Tenofovir DF/Emtricitabine All Dosed Once Daily With and Without Darunavir (PREZISTA™)/ Ritonavir Once Daily in Antiretroviral naïve HIV-1 Infected Subjects [NCT00534352]	Phase 2	23 participants (Actual)	Interventional	2008-01-31	Completed
Patient Preference, Sleep Quality, and Anxiety/Depression: A Randomized Comparison of Etravirine and Efavirenz [NCT00792584]		50 participants (Anticipated)	Interventional	2008-11-30	Completed
A Phase 2 Clinical Trial to Test the Safety and Efficacy of Etravirine in Friedreich Ataxia Patients [NCT04273165]	Phase 2	30 participants (Actual)	Interventional	2020-09-17	Completed
A Study to Survey the Swallowability of Uncoated 200-mg Tablets of Etravirine in HIV-1 Infected Subjects [NCT01090648]	Phase 1	49 participants (Actual)	Interventional	2010-03-31	Completed
A Phase I, Partially Randomized, Open Label, Two-way, Two Period Cross-over Study to Investigate the Pharmacokinetic Interaction Between Etravirine or Darunavir/Rtv and Artemether/Lumefantrine at Steady-state in Healthy HIV-negative Subjects [NCT01876966]	Phase 1	33 participants (Actual)	Interventional	2011-03-31	Completed
A Randomized, Placebo-controlled Phase II Trial in HIV-1-infected, NRTI-, PI and NNRTI-experienced Subjects to Evaluate the Safety, Tolerability and Efficacy of Different Doses of TMC125 b.i.d. on Top of an Individually Optimized Antiretroviral Therapy by [NCT00412646]	Phase 2	260 participants (Actual)	Interventional	2002-06-30	Completed
A Phase 2b Study to Select a Once Daily Oral Dose of GSK2248761 in HIV-1 Infected Antiretroviral Therapy Experienced Adults With Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI) Resistance [NCT01199731]	Phase 2	30 participants (Actual)	Interventional	2010-10-05	Terminated(stopped due to The study was stopped due to safety concerns)
A Phase IV, Open Label Study in Healthy Male Subjects to Investigate the Extent of Darunavir/Ritonavir and Etravirine Exposure in Blood, Seminal Fluid, and Rectal Mucosal Tissue Following Single and Multiple Dosing of Darunavir/Ritonavir and Etravirine [NCT00855088]	Phase 1	13 participants (Actual)	Interventional	2009-07-31	Completed
A Phase IIb, Multi-centre, Randomised, Double-blind, Active-controlled Trial Comparing the Neuropsychiatric Adverse Event Profile of Etravirine 400mg qd Versus Efavirenz 600mg qd in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors [NCT00903682]	Phase 2	157 participants (Actual)	Interventional	2009-06-30	Completed
A Long Term Open-Label Extension Study Of Lersivirine For The Treatment Of HIV-1 Infection [NCT01254656]	Phase 2	108 participants (Actual)	Interventional	2011-02-28	Terminated(stopped due to See termination reason in detailed description.)
An Open-Label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Etravirine (ETR) in Combination With Other Antiretrovirals (ARVs) in Antiretroviral Treatment-Experienced HIV-1 Infected Subjects [NCT01422330]	Phase 4	211 participants (Actual)	Interventional	2011-09-30	Completed
Evaluation of the Pharmacokinetics and Safety of TMC125 Administered Once and Twice-Daily and Following a 2-Week-Treatment Period With Efavirenz in Male and Female Healthy Volunteers. [NCT00531323]	Phase 1	24 participants (Anticipated)	Interventional	2007-09-30	Completed
Open-Label, Single-Sequence Study to Evaluate the Effects of Darunavir/Ritonavir and/or Etravirine on the Pharmacokinetics of GSK3640254 and the Effects of GSK3640254 on the Pharmacokinetics of Darunavir/Ritonavir and/or Etravirine in Heathy Adults [NCT04630002]	Phase 1	54 participants (Actual)	Interventional	2020-10-28	Completed
Antiretroviral Drug Concentrations and HIV Viral Load in Breast Milk and Plasma in HIV+ Women Receiving HAART (Highly Active Antiretroviral Therapy) Therapy: Etravirine (ETR) Pharmacokinetics (PK) in Breast Milk and Plasma [NCT01625169]		9 participants (Actual)	Interventional	2010-04-30	Completed
A Phase II, Randomized, Active Controlled, Open Label Trial to Investigate the Efficacy and Tolerability of TMC125 in HIV-1 Infected Subjects, Who Are PI-na�ve and With Documented Genotypic Evidence of NNRTI Resistance From Previous NNRTI Use. [NCT00225303]	Phase 2	116 participants (Actual)	Interventional	2005-03-31	Completed
A Phase III Randomized, Double-blinded, Placebo-controlled Trial to Investigate the Efficacy, Tolerability and Safety of TMC125 as Part of an ART Regimen, Including TMC114/RTV and an Investigator-selected OBR, in HIV-1 Infected Patients With Limited Treat [NCT00254046]	Phase 3	616 participants (Actual)	Interventional	2005-11-30	Completed
Prospective Clinical Trial to Assess Safety and Efficacy of DRV/r(TMC 114/r), ETV(TMC 125) and MK-0518 in Addition to OBT in HIV-1 Infected Patients With Limited to No Treatment Options ANRS 139 TRIO [NCT00460382]	Phase 2	103 participants (Actual)	Interventional	2007-05-31	Completed
HIV-1 Infected Subjects Who Were Randomized in Any Sponsor-selected TMC125 Trial to an Active Control Arm and Either Virologically Failed or Completed the Entire Treatment Period, or to Placebo Arm and Were Treated for at Least 48 Weeks. [NCT00111280]	Phase 2	48 participants (Actual)	Interventional	2004-09-30	Completed
A Randomized, Controlled, Partially Blinded Phase IIb Dose-Finding Trial of TMC125 in HIV-1 Infected Subjects With Documented Genotypic Evidence of Resistance to Currently Available NNRTIs and With at Least Three Primary PI Mutations [NCT00081978]	Phase 2	211 participants (Actual)	Interventional	2004-03-31	Completed
Early Access of TMC125 in Combination With Other Antiretrovirals in Treatment-experienced HIV-1 Infected Subjects With Limited Treatment Options [NCT00354627]	Phase 3	5,178 participants (Actual)	Interventional	2006-01-31	Completed
CID 0821 - Pilot Study to Evaluate HIV Viremia and Persistence in Acutely HIV-Infected Antiretroviral Naïve Patients Treated With Darunavir/Ritonavir and Etravirine [NCT00855413]	Phase 4	15 participants (Actual)	Interventional	2009-03-31	Terminated(stopped due to Study halted by sponsor due to slow enrollment.)
A Bioequivalence Study to Evaluate the Potential for Drug-drug Interactions Between Boceprevir 800mg Thrice Daily and the HIV Non-nucleoside Reverse Transcriptase Inhibitor Etravirine 200mg Twice Daily in HIV/(Hepatitis C Virus) (HCV) Negative Volunteers [NCT01427504]		26 participants (Actual)	Interventional	2011-08-31	Completed
A Phase I/II, Open-Label Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Antiviral Activity of Etravirine (ETR) in Antiretroviral (ARV) Treatment-Experienced HIV-1 Infected Infants and Children, Aged ≥ 2 Months to < 6 Years [NCT01504841]	Phase 1/Phase 2	26 participants (Actual)	Interventional	2013-03-14	Completed
PREZISTA or INTELENCE Switch Evaluation in Virologically Suppressed Patients Naïve to Darunavir or Etravirine and Who Are Intolerant of Their Current or Prior Combination Antiretroviral Therapy Regimen: A Phase IV, Open-label, Multicentre Observational Tr [NCT01615601]		77 participants (Actual)	Observational	2011-10-31	Completed
Management Using the Latest Technologies in Resource-limited Settings to Optimize Combination Therapy After Viral Failure (MULTI-OCTAVE) [NCT01641367]	Phase 4	545 participants (Actual)	Interventional	2013-02-22	Completed
HIV Neurocognitive Disorders: A Randomized Clinical Trial of CNS-Targeted HAART [NCT00624195]	Phase 2/Phase 3	59 participants (Actual)	Interventional	2007-03-31	Completed
Randomized Clinical Trial to Evaluate the Interest of a Down-scaled Treatment Strategy Using Dual Therapy (Nucleoside Analogs) in HIV Infected Patients Already Being Treated Using Triple Therapy, Who Present With a Successful Virological Control and for W [NCT02302547]	Phase 3	224 participants (Actual)	Interventional	2014-12-31	Completed
Dual Therapy Combining Raltegravir With Etravirine Maintains a High Level of Viral Suppression Over 96 Weeks in Long-term Experienced HIV-infected Individuals Over 45 Years on a PI-based Regimen: Results From the Phase II ANRS 163 ETRAL Study [NCT02212379]	Phase 2	170 participants (Actual)	Interventional	2015-01-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]	Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]	Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]	Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]	Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]	Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]	PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00128830 (10) [back to overview]	Median Change From TMC125-C229 Basline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 48
NCT00128830 (10) [back to overview]	Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 192
NCT00128830 (10) [back to overview]	Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 96
NCT00128830 (10) [back to overview]	Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 48
NCT00128830 (10) [back to overview]	Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 96
NCT00128830 (10) [back to overview]	Number of Participants With Adverse Events
NCT00128830 (10) [back to overview]	Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Viral Load Less Than 400 Copies/mL; and Greater Than or Equal to 1 log10 Decrease From Baseline) at Week 192
NCT00128830 (10) [back to overview]	Number of Participants With Emerging Mutation (Reverse Transcriptase Mutation)
NCT00128830 (10) [back to overview]	Median Change From TMC125-C229 Baseline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 96
NCT00128830 (10) [back to overview]	Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Less Than 400 Copies/mL; and Greater Than or Equal to 1 Log 10 Decrease From Baseline) at Week 96
NCT00359021 (3) [back to overview]	Change in Plasma Viral Load Versus Baseline (ie, Mean Change in log10 Plasma Viral Load From Baseline Over Time)
NCT00359021 (3) [back to overview]	The Number of Participants Experiencing Adverse Events
NCT00359021 (3) [back to overview]	The Percentage of Participants With Virologic Outcomes Over Time
NCT00460746 (10) [back to overview]	Median Change From Baseline in Total Cholesterol at Week 48.
NCT00460746 (10) [back to overview]	Median Change From Baseline in Triglycerides at Week 48.
NCT00460746 (10) [back to overview]	Proportion of Patients Who Have Viral Load Measurements <50 Copies/ml at 2, 4, 8, 12, 16, 24, 36 and 48 Weeks After Switching to DRV/r and ETR, Missing Equals Failure.
NCT00460746 (10) [back to overview]	Proportion of Patients Who Maintain Plasma HIV Viral Load Measurements < 400 Copies/ml at 2, 4, 8, 12, 16, 24, 36 and 48 Weeks After Switching to DRV/r and ETR, Missing Equals Failure.
NCT00460746 (10) [back to overview]	CD4+ Cell Count (x 10^6 Cell/L): Baseline and Mean Changes From Baseline at 4, 8, 12, 16, 24,36 and 48 Weeks.
NCT00460746 (10) [back to overview]	CD4+ Cell Count (x 10^6 Cell/L): Baseline and Median Changes From Baseline at 4, 8, 12, 16, 24, 36 and 48 Weeks.
NCT00460746 (10) [back to overview]	Median Change From Baseline in Glucose at Week 48.
NCT00460746 (10) [back to overview]	Median Change From Baseline in HDL Cholesterol.
NCT00460746 (10) [back to overview]	Median Change From Baseline in LDL Cholesterol at Week 48.
NCT00460746 (10) [back to overview]	Median Change From Baseline in Total Cholesterol (TC) / High Denisty Lipoprotein (HDL) Ratio at Week 48.
NCT00534352 (12) [back to overview]	Virologic Response < 50 HIV-1 RNA Copies/mL (ITT-Observed Case)
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Non-Graded Laboratory Abnormalities(Worst Abnormality): Lipids- High-density Lipoprotein (HDL)
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Non-Graded Laboratory Abnormalities(Worst Abnormality): Glucose- Insulin
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Graded Laboratory Abnormalities(Worst Grade): Lipids- Triglycerides
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Graded Laboratory Abnormalities(Worst Grade): Lipids- Low-density Lipoprotein (LDL) Direct
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Graded Laboratory Abnormalities (Worst Grade): Lipids- Total Cholesteral
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Graded Laboratory Abnormalities (Worst Grade): Glucose-Hyperglycemia
NCT00534352 (12) [back to overview]	Number of Participants With Treatment-Emergent Graded Laboratory Abnormalities (Worst Grade): Glucose- Hypoglycemia
NCT00534352 (12) [back to overview]	Log10 Viral Load (HIV-1 RNA Copies/mL): Mean Changes From Baseline(ITT-Observed Case)
NCT00534352 (12) [back to overview]	CD4+ Cell Count (x 10^6 Cell/L): Baseline and Median Changes From Baseline (ITT-Observed Case)
NCT00534352 (12) [back to overview]	CD4+ Cell Count (Percent): Baseline and Median Changes From Baseline (ITT-Observed Case)
NCT00534352 (12) [back to overview]	Number of Participants Contributing to the Pharmacokinetic (PK) Evaluations: Cmin, Cmax, AUC24 & Css,av
NCT00537394 (15) [back to overview]	Change in Cardiovascular Risk Score From Baseline
NCT00537394 (15) [back to overview]	Change in CD4 Count From Baseline
NCT00537394 (15) [back to overview]	Change in Fasting Non-HDL Cholesterol From Baseline
NCT00537394 (15) [back to overview]	Change in Summarized Quality of Life Score
NCT00537394 (15) [back to overview]	Number of Participants Self-reporting Non-adherence to Assigned Study ARVS (Excluding NRTIs, if Applicable)
NCT00537394 (15) [back to overview]	Number of Participants With Plasma HIV-1 Viral Load < 50 Copies/ml
NCT00537394 (15) [back to overview]	Time From Randomization to Confirmed Virological Failure
NCT00537394 (15) [back to overview]	Time From Randomization to Discontinuation of Randomized NRTI Component of Study Treatment
NCT00537394 (15) [back to overview]	Time From Treatment Dispensation to First Grade 3 or Higher (and at Least One Grade Higher Than Baseline) Signs/Symptom or Laboratory Abnormality
NCT00537394 (15) [back to overview]	Time From Treatment Dispensation to First Study ARV Modification (Excluding NRTIs, if Applicable)
NCT00537394 (15) [back to overview]	Time From Treatment Dispensation to Serious Non-AIDS-defining Events
NCT00537394 (15) [back to overview]	Change in Plasma HIV-1 Viral Load From Baseline to Week 1
NCT00537394 (15) [back to overview]	Number of Participants With Change in Virus Co-receptor Tropism Among Those With R5-only Tropic Virus at Study Entry
NCT00537394 (15) [back to overview]	Participants With Newly Acquired HIV Drug Resistance Between Study Entry and Confirmed Virologic Failure
NCT00537394 (15) [back to overview]	Percent of Participants With Regimen Failure, Defined as a Confirmed Virologic Failure or Discontinuation of Randomized NRTI Component of Study Treatment
NCT00624195 (1) [back to overview]	Neuropsychological Performance Change
NCT00665847 (9) [back to overview]	The Change From Baseline in CD4 Cell Counts Over Time
NCT00665847 (9) [back to overview]	Population Pharmacokinetic (PK) Estimates of Etravirine/TMC125 (ETR): Trough Plasma Concentration (C0h)
NCT00665847 (9) [back to overview]	The Percentage of Patients With Treatment-emergent Adverse Events (TEAEs)
NCT00665847 (9) [back to overview]	The Emergence of Non-nucleoside Reverse Transcriptase Inhibitor Resistance-associated Mutations (NNRTI RAMs) in Patients Classified as Virologic Failures
NCT00665847 (9) [back to overview]	The Number of Patients With Treatment-emergent Adverse Events (TEAEs)
NCT00665847 (9) [back to overview]	Change From Baseline in Human Immunodeficiency Virus - Type 1 (HIV-1) Ribonucleic Acid (RNA) in Plasma Over Time
NCT00665847 (9) [back to overview]	Percentage of Patients With Virologic Response at Week 24
NCT00665847 (9) [back to overview]	Population Pharmacokinetic (PK) Estimates of Etravirine/TMC125 (ETR): Area Under the Plasma Concentration-time Curve Over 12 Hours at Steady-state (AUC12h)
NCT00665847 (9) [back to overview]	Population Pharmacokinetic (PK) Estimates of Etravirine/TMC125 (ETR): Maximum Plasma Concentration (Cmax)
NCT00823979 (10) [back to overview]	Percentage of Participants With HIV-1 RNA Levels <50 Copies/mL at Week 48 and 96
NCT00823979 (10) [back to overview]	Percentage of Participants With Human Immunodeficiency Virus Type 1 Ribonucleic Acid (HIV-1 RNA) Levels Less Than (<) 50 Copies/Milliliter (mL) at Week 24
NCT00823979 (10) [back to overview]	Percentage of Participants With Response as Determined by the Time to Loss of Virologic Response (TLOVR50) Algorithm at Week 24, 48 and 96
NCT00823979 (10) [back to overview]	Time-Averaged Difference (TAD) in log10 Transformed HIV-1 RNA Levels at Week 24, 48 and 96
NCT00823979 (10) [back to overview]	Percentage of Participants With HIV-1 RNA Levels <400 Copies/mL at Week 24, 48 and 96
NCT00823979 (10) [back to overview]	Change From Baseline in Cluster of Differentiation 4 (CD4+) Absolute Lymphocyte Counts at Week 24, 48 and 96
NCT00823979 (10) [back to overview]	Change From Baseline in Cluster of Differentiation 4 (CD4+) Percentage Lymphocyte Counts at Week 24, 48, 96
NCT00823979 (10) [back to overview]	Change From Baseline in log10 Transformed HIV-1 RNA Levels at Week 24, 48 and 96
NCT00823979 (10) [back to overview]	Number of Participants With Laboratory Test Abnormalities
NCT00823979 (10) [back to overview]	Number of Participants With Non-nucleoside Reverse Transcriptase Inhibitors (NNRTI) Resistance-Associated Mutations (RAMs) and/or Phenotypic Susceptibility at Time of Treatment Failure Through Week 48
NCT00855335 (15) [back to overview]	Area Under the Plasma Concentration-Time Curve From Time of Administration to 12 Hours Post-dose (AUC0-12h)
NCT00855335 (15) [back to overview]	Area Under the Plasma Concentration-Time Curve From Time of Administration to 24 Hours Post-dose (AUC0-24h)
NCT00855335 (15) [back to overview]	Maximum Plasma Concentration (Cmax)
NCT00855335 (15) [back to overview]	Mean Change From Baseline in CD4+ Cell Count
NCT00855335 (15) [back to overview]	Number of Participants With Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Plasma Viral Load (<) 50 Copies/Milliliter (mL)
NCT00855335 (15) [back to overview]	Mean Change From Baseline in Log10 Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Viral Load Value
NCT00855335 (15) [back to overview]	Number of Participants With Resistance at Virological Failure
NCT00855335 (15) [back to overview]	Minimum Plasma Concentration (Cmin)
NCT00855335 (15) [back to overview]	Plasma Concentration of Drug in the Cord Plasma and Maternal Plasma Samples Collected at the Time of Delivery
NCT00855335 (15) [back to overview]	Mean Change From Baseline in Log10 Human Immunodeficiency Virus (HIV)-1 Ribonucleic Acid (RNA) Viral Load Value
NCT00855335 (15) [back to overview]	Predose (Trough) Plasma Concentration (C0h)
NCT00855335 (15) [back to overview]	Time to Reach the Maximum Plasma Concentration (Tmax)
NCT00855335 (15) [back to overview]	Number of Infants With Human Immunodeficiency Virus (HIV) Positive Test Result
NCT00855335 (15) [back to overview]	Mean Change From Baseline in CD4+ Cell Count
NCT00855335 (15) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00855413 (38) [back to overview]	Minimum Etravirine Exposure in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Minimum Darunavir Exposure in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Minimum Etravirine Exposure in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00855413 (38) [back to overview]	Minimum Etravirine Exposure Range in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Minimum Ritonavir Exposure Range in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Minimum Ritonavir Exposure Range in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Number of Participants Who Stopped Study Treatment Due to Adverse Event or Intolerance
NCT00855413 (38) [back to overview]	Number of Participants With HIV RNA Measurement Above the Limits of Detection in Cerebrospinal Fluid
NCT00855413 (38) [back to overview]	Number of Participants With Neurocognitive Impairment at Baseline
NCT00855413 (38) [back to overview]	Number of Participants With Neurocognitive Impairment at Week 24
NCT00855413 (38) [back to overview]	Number of Participants With Neurocognitive Impairment at Week 48
NCT00855413 (38) [back to overview]	Number of Participants With Virologic Response
NCT00855413 (38) [back to overview]	Number of Participants With Virologic Response
NCT00855413 (38) [back to overview]	Overall Neurocognitive Impairment at Week 24
NCT00855413 (38) [back to overview]	Overall Neurocognitive Impairment at Week 48
NCT00855413 (38) [back to overview]	Overall Neurocognitive Impairment Score at Week 2 or 4
NCT00855413 (38) [back to overview]	Minimum Ritonavir Exposure in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00855413 (38) [back to overview]	Adverse Events Possibly or Definitely Related to Study Treatment Through Week 48
NCT00855413 (38) [back to overview]	Change in Overall Neurocognitive Impairment From Baseline to Week 24 or 48
NCT00855413 (38) [back to overview]	Correlation of HIV RNA Levels in CSF and Drug Levels With Neurocognitive Functioning
NCT00855413 (38) [back to overview]	Correlation of Time to HIV RNA Levels <200 Copies/mL With Improvement in Neurocognitive Functioning From Baseline to Week 24 and 48
NCT00855413 (38) [back to overview]	HIV RNA Detection in Ileal Biopsy Specimens
NCT00855413 (38) [back to overview]	HIV RNA Detection in Semen
NCT00855413 (38) [back to overview]	HIV RNA Levels Immediately Prior to Initiating Study Treatment.
NCT00855413 (38) [back to overview]	Maximum Darunavir Exposure in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Maximum Darunavir Exposure in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00855413 (38) [back to overview]	Maximum Darunavir Exposure Range in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Maximum Etravirine Exposure in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Maximum Etravirine Exposure in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Maximum Etravirine Exposure in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00855413 (38) [back to overview]	Maximum Ritonavir Exposure in Cerebrospinal Fluid Among Participants Who Consented to an Optional Lumbar Puncture
NCT00855413 (38) [back to overview]	Maximum Ritonavir Exposure in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00855413 (38) [back to overview]	Maximum Ritonavir Exposure Range in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Median Change in CD4 Cell Count From Week 0 to Week 24.
NCT00855413 (38) [back to overview]	Median Change in CD4 Cell Count From Week 0 to Week 48.
NCT00855413 (38) [back to overview]	Median Time to HIV RNA Suppression to <200 Copies/mL
NCT00855413 (38) [back to overview]	Minimum Darunavir Exposure Range in Ileal Tissue Among Participants Who Consented to an Optional Gut Biopsy Procedure
NCT00855413 (38) [back to overview]	Minimum Darunavir Exposure Range in Semen Among Participants Who Consented to an Optional Collection of Semen
NCT00871234 (1) [back to overview]	Flow-mediated Dilation (FMD) of the Brachial Artery
NCT00884793 (4) [back to overview]	"Average Change in Activated (CD38+HLADR+) CD8+ T Cells in the Ileum"
NCT00884793 (4) [back to overview]	Number of Subjects Who Experienced an Increase in CD4% in the Ileum.
NCT00884793 (4) [back to overview]	Number of Subjects Who Experienced an Increase in CD4+ T Cells (as a % of All Cells) in the Ileum.
NCT00884793 (4) [back to overview]	Number of Subjects Who Had a Decrease in HIV RNA Per Million CD4+ T Cells in the Ileum
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Atazanavir (ATV): Treatment A: ATV/Low-Dose Ritonavir (Rtv) 300/100 mg (Results for C0h, Cmin, and Cmax)
NCT00896051 (18) [back to overview]	Percentage of Participants With Undetectable Plasma Viral Load (VL) Values (<50 Copies/mL) at Week 48
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Atazanavir (ATV): Treatment A: ATV/Low-Dose Ritonavir (Rtv) 300/100 mg (Results for AUC24hr)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Atazanavir (ATV): Treatment B: ATV/Low-Dose Ritonavir (Rtv) 400/100 mg (Results for AUC24hr)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Etravirine (ETR) (Results for AUC12hr)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment A: Atazanavir (ATV)/Rtv 300/100 mg (Results for AUC24hr)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment B: Atazanavir (ATV)/Rtv 400/100 mg (Results for AUC24hr)
NCT00896051 (18) [back to overview]	Change From Pre-Baseline in Log10 Viral Load Over Time
NCT00896051 (18) [back to overview]	Change From Prebaseline in CD4+ Cell Count Over Time
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Etravirine (ETR) (Results for C0h, Cmin, and Cmax)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Atazanavir (ATV): Treatment B: ATV/Low-Dose Ritonavir (Rtv) 400/100 mg (Results for C0h, Cmin, and Cmax)
NCT00896051 (18) [back to overview]	Time to Virologic Failure
NCT00896051 (18) [back to overview]	Time to Confirmed Virologic Response
NCT00896051 (18) [back to overview]	The Percentage of Participants With a Virologic Response Using the Time to Loss of Virologic Response (TLOVR) Imputation Method
NCT00896051 (18) [back to overview]	The Percentage of Participants With a Virologic Response Using the Non-Completing = Failure (NC=F) Imputation Method
NCT00896051 (18) [back to overview]	The Percentage of Participants With a Virologic Response (Plasma Viral Load < 50 Copies/mL) at Week 48 Using the Snapshot Analysis Method
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment B: Atazanavir (ATV)/Rtv 400/100 mg (Results for C0h, Cmin, and Cmax)
NCT00896051 (18) [back to overview]	Pharmacokinetic Results of Low-Dose Ritonavir (Rtv): Treatment A: Atazanavir (ATV)/Rtv 300/100 mg (Results for C0h, Cmin, and Cmax)
NCT00903682 (7) [back to overview]	Antiviral Activity of ETR vs. EFV
NCT00903682 (7) [back to overview]	Neuropsychiatric Adverse Events by Week 48
NCT00903682 (7) [back to overview]	Proportion of Patients With at Least 1 Treatment-emergent Grade 1-4 Central Nervous System or Psychiatric Adverse Event
NCT00903682 (7) [back to overview]	Mean Change From Baseline in CD4+ Cell Count
NCT00903682 (7) [back to overview]	Mean Change From Baseline in Neuropsychiatric and Total Tolerabililty Score
NCT00903682 (7) [back to overview]	Resistance Determinations
NCT00903682 (7) [back to overview]	Antiviral Activity of ETR vs. EFV
NCT00959894 (25) [back to overview]	Probability of Remaining Free of a Safety/Tolerability Event at 96 Weeks
NCT00959894 (25) [back to overview]	Change in Limb and Trunk Fat Distribution as Measured by DEXA Scan, in the Same Subgroup of up to 40 Participants (as in Aim 8), From Baseline to Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in CD4+ Cell Count From Baseline to Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in CD4+ Cell Count From Baseline to Week 48 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in CD4+ Cell Count From Baseline to Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Fat Mass Ratio as Measured by DEXA Scan, in the Same Subgroup of up to 40 Participants (as in Aim 8), From Baseline to Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Fat Mass Ratio as Measured by DEXA Scan, in the Same Subgroup of up to 40 Participants (as in Aim 8), From Baseline to Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Glucose Metabolism (Insulin Resistance), in a Subgroup of up to 40 Participants, From Baseline to Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Glucose Metabolism (Insulin Resistance), in a Subgroup of up to 40 Participants, From Baseline to Week 48 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Glucose Metabolism (Insulin Resistance), in a Subgroup of up to 40 Participants, From Baseline to Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Pharmacokinetics of Etravirine in Genital Secretions of up to 10 Men and up to 10 Women at Week 4 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Population Pharmacokinetics of Etravirine 400 mg Once Daily, in Combination With Fixed-dose Emtricitabine-tenofovir Among Treatment-naïve HIV-1 Infected Adults: Etravirine AUC-24 Hours at Steady State
NCT00959894 (25) [back to overview]	The Antiretroviral Activity of Etravirine 400 mg Given Once Daily, With Fixed-dose Truvada Once Daily, Among Treatment-naïve HIV-1 Infected Adults as Measured by the Percentage of Participants With HIV RNA < 50 Copies/mL at Week 24
NCT00959894 (25) [back to overview]	The Proportion of Participants With HIV RNA <200 Copies/mL at Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	The Proportion of Participants With HIV RNA <200 Copies/mL at Week 48 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	The Proportion of Participants With HIV RNA <200 Copies/mL at Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	The Proportion of Participants With HIV RNA <50 Copies/mL at Week 48 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	The Proportion of Participants With HIV RNA <50 Copies/mL at Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in Limb and Trunk Fat Distribution as Measured by DEXA Scan, in the Same Subgroup of up to 40 Participants (as in Aim 8), From Baseline to Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in the Lipid Profile and Glucose Metabolism, in a Subgroup of up to 40 Participants, From Baseline to Week 24 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in the Lipid Profile and Glucose Metabolism, in a Subgroup of up to 40 Participants, From Baseline to Week 48 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Change in the Lipid Profile and Glucose Metabolism, in a Subgroup of up to 40 Participants, From Baseline to Week 96 of Treatment With Etravirine and Fixed-dose Tenofovir/Emtricitabine
NCT00959894 (25) [back to overview]	Population Pharmacokinetics of Etravirine 400 mg Once Daily, in Combination With Fixed-dose Emtricitabine-tenofovir Among Treatment-naïve HIV-1 Infected Adults
NCT00959894 (25) [back to overview]	Resistance Mutations in the Subset of Patients With Confirmed Virologic Failure Who Have HIV RNA >500 Copies/mL and Genotype Resistance Results
NCT00959894 (25) [back to overview]	Tolerability of Etravirine in HIV-1 Infected Adults Initiating Antiretroviral Therapy
NCT00980538 (1) [back to overview]	Number of Participants With At-least One Adverse Event as a Measure of Safety Until Etravirine (ETR)-Based Treatment Regimen is Commercially Available
NCT01199731 (16) [back to overview]	Percentage of Participants With Human Immunodeficiency Virus Type 1 (HIV-1) Ribonucleic Acid (RNA) <50 Copies Per Milliliter (/mL) at Week 16
NCT01199731 (16) [back to overview]	Absolute Values of CD4+ Cell Counts After Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in CD4+ Cell Counts After Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in CD4+ Cell Counts After Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in CD4+ Cell Counts Prior to Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in CD4+ Cell Counts Prior to Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in Plasma HIV-1 RNA After Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in Plasma HIV-1 RNA Prior to Switch of GSK2248761
NCT01199731 (16) [back to overview]	Change From Baseline in Plasma HIV-1 RNA Prior to Switch of GSK2248761
NCT01199731 (16) [back to overview]	Number of Participants Who Experienced Disease Progression (HIV-associated Conditions, AIDS and Death)
NCT01199731 (16) [back to overview]	Number of Participants With Electrocardiograph (ECG) With Values of Potential Critical Concern (PCI)
NCT01199731 (16) [back to overview]	Number of Participants With Abnormal Clinical Chemistry Laboratory Data With Grade 3 or 4 Treatment-Emergent (TE) Toxicities
NCT01199731 (16) [back to overview]	Number of Participants With Abnormal Hematology Laboratory Data With Grade 3 or 4 TE Toxicities
NCT01199731 (16) [back to overview]	Number of Participants With Treatment-emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01199731 (16) [back to overview]	Number of Participants Who Discontinued Treatment Due to AEs
NCT01199731 (16) [back to overview]	Absolute Values of CD4+ Cell Counts After Switch of GSK2248761
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 48
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 8
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 24
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 20
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 16
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 12
NCT01199939 (14) [back to overview]	Change From Baseline in Cluster of Differentiation 4 (CD4+) and Cluster of Differentiation 8 (CD8+) Cell Counts at Week 48
NCT01199939 (14) [back to overview]	Time to Reach First Confirmed Virologic Response
NCT01199939 (14) [back to overview]	Number of Participants With Virologic Failure
NCT01199939 (14) [back to overview]	Number of Participants With Confirmed Virologic Response (CVR) at Week 48
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 36
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 4
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 42
NCT01199939 (14) [back to overview]	Change From Baseline in Log10 Plasma Human Immunodeficiency Virus - Type 1 (HIV-1) Viral Load at Week 30
NCT01254656 (7) [back to overview]	Number of Participants With Plasma HIV-1 RNA Level <50 Copies/mL up to Week 208
NCT01254656 (7) [back to overview]	Number of Participants With Plasma Human Immunodeficiency Virus - 1 (HIV-1) Ribonucleic Acid (RNA) Level <50 Copies/mL at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]	Virology Analysis Participant Accountability From Week 96 Through Study Termination
NCT01254656 (7) [back to overview]	Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]	Change From Baseline in CD4+ Lymphocyte Counts (Absolute) at 192 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]	Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 144 Weeks From Day 1 of the Parent Protocol
NCT01254656 (7) [back to overview]	Change From Baseline in CD4+ Lymphocyte Counts (Percentage) at 192 Weeks From Day 1 of the Parent Protocol
NCT01427504 (12) [back to overview]	Etravirine Cmin Pharmacokinetics Coadministered With Boceprevir
NCT01427504 (12) [back to overview]	Boceprevir AUC Pharmacokinetics
NCT01427504 (12) [back to overview]	Boceprevir AUC Pharmacokinetics Coadministered With Etravirine
NCT01427504 (12) [back to overview]	Boceprevir C8 Pharmacokinetics
NCT01427504 (12) [back to overview]	Boceprevir C8 Pharmacokinetics Coadministered With Etravirine
NCT01427504 (12) [back to overview]	Boceprevir Cmax Pharmacokinetics
NCT01427504 (12) [back to overview]	Boceprevir Cmax Pharmacokinetics Coadministered With Etravirine
NCT01427504 (12) [back to overview]	Etravirine AUC Pharmacokinetics
NCT01427504 (12) [back to overview]	Etravirine AUC Pharmacokinetics Coadministered With Boceprevir
NCT01427504 (12) [back to overview]	Etravirine Cmax Pharmacokinetics
NCT01427504 (12) [back to overview]	Etravirine Cmax Pharmacokinetics Coadministered With Boceprevir
NCT01427504 (12) [back to overview]	Etravirine Cmin Pharmacokinetics
NCT01504841 (3) [back to overview]	Area Under the Plasma Concentration-Time Curve Over 12 Hours of ETR
NCT01504841 (3) [back to overview]	Decline in Absolute CD4 Percent of Greater Than 5 Percent Any Time After 12 Weeks of Therapy
NCT01504841 (3) [back to overview]	HIV-1 RNA Virologic Failure Status at Weeks 24 and 48
NCT01625169 (10) [back to overview]	Peak Concentration of Etravirine in Breast Milk
NCT01625169 (10) [back to overview]	HIV Viral Load in Breast Milk and Plasma
NCT01625169 (10) [back to overview]	Peak Plasma Concentration of Etravirine in Plasma
NCT01625169 (10) [back to overview]	Peak Plasma Concentration of Etravirine in Plasma
NCT01625169 (10) [back to overview]	HIV Viral Load in Breast Milk and Plasma
NCT01625169 (10) [back to overview]	Area Under the Curve (AUC) 0-12 for Breast Milk
NCT01625169 (10) [back to overview]	Area Under the Curve (AUC) 0-12 for Breast Milk
NCT01625169 (10) [back to overview]	Area Under the Curve (AUC) 0-12 for Plasma
NCT01625169 (10) [back to overview]	Area Under the Curve (AUC) 0-12 for Plasma
NCT01625169 (10) [back to overview]	Peak Concentration of Etravirine in Breast Milk
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Triglycerides [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Triglycerides
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Total Cholesterol [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Total Cholesterol
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of High-density Lipoprotein Cholesterol [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of High-density Lipoprotein Cholesterol
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Glucose [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Glucose
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Calculated Low-density Lipoprotein Cholesterol [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in Fasting Values of Calculated Low-density Lipoprotein Cholesterol
NCT01641367 (60) [back to overview]	Change From Baseline in CD4+ T-cell Count [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Change From Baseline in CD4+ T-cell Count
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 72 Weeks [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 72 Weeks
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 48 Weeks [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 48 Weeks
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 24 Weeks [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the First of Death or Hospitalization [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With Treatment Modification or Discontinuation Due to Toxicity by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants With Treatment Modification or Discontinuation by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With Treatment Modification or Discontinuation by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants With Death or Hospitalization by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With Death or Hospitalization by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing, by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing, by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants With Confirmed Virologic Failure by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With Confirmed Virologic Failure by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants With a Dose Modification Due to Grade 3 or 4 Toxicity by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants With a Dose Modification Due to Grade 3 or 4 Toxicity by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants That Developed Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants That Developed Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants Experiencing Death, AIDS-defining Event or a Non-AIDS-defining Event by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants Experiencing Death, AIDS-defining Event or a Non-AIDS-defining Event by Week 48
NCT01641367 (60) [back to overview]	Percent of Participants Experiencing Death by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Percent of Participants Experiencing Death by Week 48
NCT01641367 (60) [back to overview]	Number of Weeks of Follow-up [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Number of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Number of Weeks of Follow-up
NCT01641367 (60) [back to overview]	Time to Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time to Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Treatment Modification or Discontinuation.
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Treatment Modification or Discontinuation Due to Toxicity [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Treatment Modification or Discontinuation Due to Toxicity
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Treatment Modification or Discontinuation [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the First of Death, an AIDS-defining Event or a Non-AIDS-defining Event [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the First of Death, an AIDS-defining Event or a Non-AIDS-defining Event
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the First of Death or Hospitalization.
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the Development of Immune Reconstitution Inflammatory Syndrome (IRIS) [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to the Development of Immune Reconstitution Inflammatory Syndrome (IRIS)
NCT01641367 (60) [back to overview]	Proportion of Participants With Plasma HIV-1 RNA ≤200 Copies/mL at 24 Weeks
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Death [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time From Study Entry/Randomization to Death
NCT01641367 (60) [back to overview]	Percent of Participants With Treatment Modification or Discontinuation Due to Toxicity by Week 48 [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Number of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study
NCT01641367 (60) [back to overview]	Number of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Number of Participants With Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing
NCT01641367 (60) [back to overview]	Time to Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing
NCT01641367 (60) [back to overview]	Time to Confirmed Virologic Failure, Defined as First HIV-1 RNA ≥1000 Copies/mL at or After 24 Weeks on Study, With a New Resistance-associated Mutation Detected in Population-based Sequencing [CPI+SOC v SOC]
NCT01641367 (60) [back to overview]	Time to First Dose Modification Due to Grade 3 or 4 Toxicity
NCT01641367 (60) [back to overview]	Time to First Dose Modification Due to Grade 3 or 4 Toxicity [CPI+SOC v SOC]
NCT02212379 (24) [back to overview]	Percentage of Participants With Detectable Seminal HIV-RNA Viral Load at Week 48
NCT02212379 (24) [back to overview]	Median Time of Virological Failure
NCT02212379 (24) [back to overview]	Number of Patients With RAL and/or ETR Resistance Mutations Among Those With Virological Failure
NCT02212379 (24) [back to overview]	Percent Change of Renal Function
NCT02212379 (24) [back to overview]	Evolution of Body Fat Distribution From Day 0 to W96 (DXA Scan Sub-study, 80 Patients)
NCT02212379 (24) [back to overview]	Evolution of CD4+, CD8+ T Cells Counts and CD4/CD8 Ratio
NCT02212379 (24) [back to overview]	Evolution of Metabolic Parameters (Fasting Triglycerides, Total Cholesterol, HDL-cholesterol, LDL-cholesterol and Fasting Glycemia)
NCT02212379 (24) [back to overview]	Evolution of the Calibrated 5-year Framingham Risk Score
NCT02212379 (24) [back to overview]	Evolution of the Level of MCP1 From D0 to W48 on Frozen Samples
NCT02212379 (24) [back to overview]	Evolution of the Ovarian Reserve From D0 to W48 Measured by AMH on Frozen Aliquots
NCT02212379 (24) [back to overview]	Evolution of Total Cell-associated HIV-DNA
NCT02212379 (24) [back to overview]	Factors Associated With the Occurrence of Plasma HIV-RNA Viral Load > 50 Copies/mL
NCT02212379 (24) [back to overview]	Inflammatory Parameters
NCT02212379 (24) [back to overview]	Number of Participants Experiencing Adverse Events and Effects
NCT02212379 (24) [back to overview]	Percentage of Participants Compliant With Treatment Program.
NCT02212379 (24) [back to overview]	Percentage of Participants Reporting a Very Good or an Excellent Quality of Life at Day 0, Weeks 48 and 96
NCT02212379 (24) [back to overview]	Percentage of Participants With Successful Virological Suppression at Weeks 48 and 96
NCT02212379 (24) [back to overview]	Percentage of Patients With High Grade of Virological Failure Defined as HIV RNA > 200 Copies/mL
NCT02212379 (24) [back to overview]	Percentage of Patients With Therapeutic Success at Week 48 and Week 96
NCT02212379 (24) [back to overview]	Percentage of Patients With Trial Treatment Interruption at Week 48 and Week 96
NCT02212379 (24) [back to overview]	Percentage of Patients With With Grade Virological Failure (HIV-RNA Plasma VL Between 51 and 200 Copies/mL)
NCT02212379 (24) [back to overview]	Sub-study in Women : Comparison of the Evolution Fat Distribution Measured by DXA Scan and Body Weight According to AMH Status
NCT02212379 (24) [back to overview]	Sub-study in Women : Comparison of the Metabolic/Inflammatory Profile in Women According to Their Ovarian Reserve and Menopausal Status at D0 and Its Evolution up to Week 96
NCT02212379 (24) [back to overview]	Sub-study: Bone Mineral Density
NCT04630002 (54) [back to overview]	Cohort 1: Tmax of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 1: Time of Maximum Observed Concentration (Tmax) of DRV
NCT04630002 (54) [back to overview]	Cohort 1: Plasma Concentration at the End of the Dosing Interval (Ctau) of DRV
NCT04630002 (54) [back to overview]	Cohort 1: Maximum Observed Concentration (Cmax) of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 1: Ctau of RTV
NCT04630002 (54) [back to overview]	Cohort 1: Ctau of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 1: Cmax of RTV
NCT04630002 (54) [back to overview]	Cohort 1: Cmax of DRV
NCT04630002 (54) [back to overview]	Cohort 1: AUC(0-tau) of RTV
NCT04630002 (54) [back to overview]	Cohort 1: AUC(0-tau) of DRV
NCT04630002 (54) [back to overview]	Cohort 1: Area Under the Plasma Concentration-time Curve From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Vital Sign Values of PCI Criteria
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With SAEs and Non-SAEs
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Urinalysis Parameters
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Hematology Parameters
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Glucose, Triglycerides, Lipase, Urate and Cholesterol
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Calcium, Creatine Kinase, Creatinine, Phosphate, Potassium and Sodium
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Alanine Aminotransferase, Albumin, Alkaline Phosphatase, Amylase, Aspartate Aminotransferase, Bilirubin and Direct Bilirubin
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Clinically Significant Abnormal ECG Findings
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With Clinically Significant Abnormal ECG Findings
NCT04630002 (54) [back to overview]	Cohort 3: Number of Participants With AEs Leading to Discontinuations and Deaths
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Vital Sign Values of PCI Criteria
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With SAEs and Non-SAEs
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Urinalysis Parameters
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Hematology Parameters
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Alanine Aminotransferase, Albumin, Alkaline Phosphatase, Amylase, Aspartate Aminotransferase, Bilirubin and Direct Bilirubin
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Clinically Significant Abnormal ECG Findings
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Clinically Significant Abnormal ECG Findings
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With AEs Leading to Discontinuations and Deaths
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Calcium, Creatine Kinase, Creatinine, Phosphate, Potassium and Sodium
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Vital Sign Values of Potential Clinical Importance (PCI) Criteria
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Serious Adverse Events (SAEs) and Non-serious Adverse Events (Non-SAEs)
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Urinalysis Parameters
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Glucose, Triglycerides, Lipase, Urate and Cholesterol
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Hematology Parameters
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Glucose, Triglycerides, Lipase, Urate and Cholesterol
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Calcium, Creatine Kinase, Creatinine, Phosphate, Potassium and Sodium
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Grade Increase Post-Baseline Relative to Baseline in Clinical Chemistry Parameters: Alanine Aminotransferase, Albumin, Alkaline Phosphatase, Amylase, Aspartate Aminotransferase, Bilirubin and Direct Bilirubin
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Clinically Significant Abnormal Electrocardiogram (ECG) Findings
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Clinically Significant Abnormal Electrocardiogram (ECG) Findings
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With Clinically Significant Abnormal Electrocardiogram (ECG) Findings
NCT04630002 (54) [back to overview]	Cohort 1: Number of Participants With AEs Leading to Discontinuations and Deaths
NCT04630002 (54) [back to overview]	Cohort 3: Cmax of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 3: AUC(0-tau) of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 2: Tmax of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 2: Tmax of ETR
NCT04630002 (54) [back to overview]	Cohort 2: Number of Participants With Clinically Significant Abnormal ECG Findings
NCT04630002 (54) [back to overview]	Cohort 2: Ctau of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 2: Ctau of ETR
NCT04630002 (54) [back to overview]	Cohort 2: Cmax of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 2: Cmax of ETR
NCT04630002 (54) [back to overview]	Cohort 2: AUC(0-tau) of GSK3640254
NCT04630002 (54) [back to overview]	Cohort 2: AUC(0-tau) of ETR
NCT04630002 (54) [back to overview]	Cohort 1: Tmax of RTV

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Intervention	mg/L (Median)
	3rd Trimester	Postpartum
EFV 600mg q.d.	5.44	5.10

Intervention	mg*hour/L (Median)
	2nd Trimester	3rd Trimester	Postpartum
ATV/COBI 300/150 mg q.d.	25.33	18.85	36.20
ATV/RTV Arm 1: 300/100mg q.d.	88.2	41.9	57.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.	30.6	45.7	48.8
DRV/COBI 800/150 mg q.d.	50.00	42.05	95.55
DRV/RTV 800/100mg q.d.	64.6	63.5	103.9
DTG 50mg q.d.	47.6	49.2	65.0
EFV 600 mg q.d. (Outside THA)	47.30	60.02	62.70
EVG/COBI 150/150mg q.d.	15.3	14.0	21.0
TAF 10mg q.d. w/COBI	0.197	0.206	0.216
TAF 25mg q.d.	0.171	0.212	0.271
TAF 25mg q.d. w/COBI or RTV Boosting	0.181	0.257	0.283
TFV 300mg q.d.	1.9	2.4	3.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.	14.5	28.8	39.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.	26.2	37.7	58.7

Intervention	hour (Median)
DTG 50mg q.d.	32.8
EVG/COBI 150/150mg q.d.	7.6
DRV/COBI 800/150 mg q.d.	NA
EFV 600 mg q.d. (Outside THA)	65.6

Intervention	unitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.	0.15
DTG 50mg q.d.	1.25
EVG/COBI 150/150mg q.d.	0.91
DRV/COBI 800/150 mg q.d.	0.07
ATV/COBI 300/150 mg q.d.	0.07
TFV 300mg q.d.	0.88

Intervention	unitless (Median)
TAF 10mg q.d. w/COBI	0.97
EFV 600 mg q.d. (Outside THA)	0.67
EFV 600mg q.d.	0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.	0.2
RAL 400mg b.i.d.	1.5
ETR 200mg b.i.d.	0.52
MVC 150 or 300mg b.i.d.	0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.	0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.	0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.	0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)	0.12
RPV 25mg q.d.	0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.	0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.	0.18

Intervention	pg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG	604
LPV/RTV 400/100 b.i.d. With ENG	428
EFV 600mg q.d. With ENG	125

Intervention	mcg*hr/mL (Median)
	Before contraceptive initiation	After contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG	115.97	100.20

Intervention	mcg/mL (Median)
	2-10 hours after birth	18-28 hours after birth	36-72 hours after birth	5-9 days after birth
DRV/COBI 800/150 mg q.d.	0.35	1.43	1.87	1.72
DTG 50mg q.d.	1.73	1.53	1.00	0.06
EFV 600 mg q.d. (Outside THA)	1.1	1.0	0.9	0.4
EVG/COBI 150/150mg q.d.	0.132	0.032	0.005	0.005

Intervention	Participants (Number)
Viral Load More Than or Equal to 50 Copies/mL	22
Viral Load Less Than 50 Copies/mL	80

Intervention	Participants (Number)
	Viral load (VL) less than 50 copies/mL	VL less than 400 copies/mL	VL greater than or equal to 1log10
Etravirine	69	81	83

Intervention	Participants (Number)
	Viral load (VL) less than 50 copies/mL	Viral load less than 400 copies/mL	Viral load more than or equal to 1log10
Etravirine	105	124	132

Intervention	log10 copies/mL (Mean)
	Week 24	Week 48	Week 96
DUET PLACEBO	-0.8	-0.7	-0.5
DUET TMC125	0	-0.1	-0.2

Intervention	Participants (Number)
	Serious Adverse Events (SAEs)	Other Adverse Events (AEs)
All Participants	88	297
DUET PLACEBO	46	160
DUET TMC125	42	137

Intervention	Percentage of Participants (Number)
	Week 24 - Virologic Response (<50 cop/mL)	Week 24 - Virologic Failure	Week 24 - No VL Data available	Week 48 - Virologic Response (<50 cop/mL)	Week 48 - Virologic Failure	Week 48 - No VL Data available	Week 96 -Virologic Response (<50 cop/mL)	Week 96 - Virologic Failure	Week 96 - No VL Data available
DUET PLACEBO	43.0	46.9	10.2	35.2	50.4	14.5	7.4	48.0	44.5
DUET TMC125	62.3	31.6	6.1	44.5	31.2	24.3	4.5	27.5	68.0

Intervention	mg/dL (Median)
	Baseline (Day 1)	Week 48 Change from Baseline
Darunavir(TMC114)/Eravirine(TMC125)	189.0	-27.5

Intervention	percentage of participants (Number)
	Baseline (Day 1)	Week 2	Week 4	Week 8	Week 12	Week 16	Week 24	Week 36	Week 48	Post-Treatment Follow Up
Darunavir(TMC114)/Eravirine(TMC125)	100	90	90	90	80	90	90	90	80	90

Intervention	cells/mm^3 (Mean)
	Baseline (Day 1)	Week 4 Change from Baseline	Week 8 Change from Baseline	Week 12 Change from Baseline	Week 16 Change from Baseline	Week 24 Change from Baseline	Week 36 Change from Baseline	Week 48 Change from Baseline
Darunavir(TMC114)/Eravirine(TMC125)	338.3	2.3	-25.0	-18.9	0.5	24.5	22.7	47.3

Intervention	participants (Number)
	Day 8 (n=19)	Day 14 (n=21)	Day 22 (n=19)	Day 28 (n=20)	Day 42 (n=20)	Week 48 (n=13)
TDF/FTC +/- TMC125 +/- DRV/Rtv	0	3	4	6	7	10

Intervention	participants (Number)
	Below 40 mG/dL (1.03 mmol/L)	Above 59 mG/dL (1.53 mmol/L)
Optional Extension	2	1
Treatment A	4	0
Treatment B	8	0
Treatment C	6	0

Intervention	participant (Number)
	Below 3.0 ulU/mL	Above 27.0 ulU/mL
Optional Extension	1	3
Treatment A	1	1
Treatment B	2	3
Treatment C	1	2

Intervention	participants (Number)
	Grade 1	Grade 2
Optional Extension	0	0
Treatment A	0	0
Treatment B	0	0
Treatment C	0	0

etravirine

Cross-References

Synonyms (102)

Research Excerpts

Overview

Effects

Actions

Toxicity

Pharmacokinetics

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Bioavailability

Dosage Studied

Roles (2)

Drug Classes (4)

Protein Targets (31)

Potency Measurements

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Biological Processes (183)

Molecular Functions (95)

Ceullar Components (45)

Bioassays (1343)

Research

Studies (543)

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Research Demand Index: 48.12

Study Types

Clinical Trials (60)

Trial Overview

Trial Outcomes

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Plasma Concentration for Contraceptives

Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Median Change From TMC125-C229 Basline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 48

Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 192

Median Change in Cluster of Differentiation 4 (CD4+) Cell Count From Baseline in TMC125-C229 Feeder Study at Week 96

Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 48

Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL) at Week 96

Number of Participants With Adverse Events

Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Viral Load Less Than 400 Copies/mL; and Greater Than or Equal to 1 log10 Decrease From Baseline) at Week 192

Number of Participants With Emerging Mutation (Reverse Transcriptase Mutation)

Median Change From TMC125-C229 Baseline in Cluster of Differentiation 4 (CD4+) Cell Count at Week 96

Number of Participants Who Achieved Virologic Response (ie, Viral Load Less Than 50 Copies/mL; Less Than 400 Copies/mL; and Greater Than or Equal to 1 Log 10 Decrease From Baseline) at Week 96

Change in Plasma Viral Load Versus Baseline (ie, Mean Change in log10 Plasma Viral Load From Baseline Over Time)

The Number of Participants Experiencing Adverse Events

The Percentage of Participants With Virologic Outcomes Over Time

Median Change From Baseline in Total Cholesterol at Week 48.

Median Change From Baseline in Triglycerides at Week 48.

Proportion of Patients Who Have Viral Load Measurements <50 Copies/ml at 2, 4, 8, 12, 16, 24, 36 and 48 Weeks After Switching to DRV/r and ETR, Missing Equals Failure.

Proportion of Patients Who Maintain Plasma HIV Viral Load Measurements < 400 Copies/ml at 2, 4, 8, 12, 16, 24, 36 and 48 Weeks After Switching to DRV/r and ETR, Missing Equals Failure.

CD4+ Cell Count (x 10^6 Cell/L): Baseline and Mean Changes From Baseline at 4, 8, 12, 16, 24,36 and 48 Weeks.

CD4+ Cell Count (x 10^6 Cell/L): Baseline and Median Changes From Baseline at 4, 8, 12, 16, 24, 36 and 48 Weeks.

Median Change From Baseline in Glucose at Week 48.

Median Change From Baseline in HDL Cholesterol.

Median Change From Baseline in LDL Cholesterol at Week 48.

Median Change From Baseline in Total Cholesterol (TC) / High Denisty Lipoprotein (HDL) Ratio at Week 48.

Intervention	copies/mL (Mean)
	Baseline (n=23)	Day 8 (n=19)	Day 14 (n=21)	Day 22 (n=19)	Day 28 (n=20)	Day 42 (n=20)	Week 48 (n=13)
TDF/FTC +/- TMC125 +/- DRV/Rtv	4.19	-1.41	-1.71	-1.77	-1.86	-2.04	-2.30

Intervention	x 10^6 cell/L (Median)
	Baseline (n=23)	Day 8 (n=20)	Day 14 (n=20)	Day 22 (n=20)	Day 28 (n=21)	Day 42 (n=19)	Week 48 (n=14)
TDF/FTC +/- TMC125 +/- DRV/Rtv	403.0	45.5	94.0	59.0	62.0	56.0	160.0

Intervention	participants (Number)
Treatment A: TMC125 + TDF/FTC	23
Treatment B: TMC125 + TDF/FTC + DRV/Rtv	21

Intervention	units on a scale (Mean)
	Week 24 (N= 150; N=147)	Week 48 (N=143; N=144)	Week 96 (N=129; N=132)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	-0.7	0.1	0.5
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	0.3	0.8	1.1

Intervention	cells/mm^3 (Median)
	Change from entry to week 48 (N=166; N=163)	Change from entry to week 96 (N= 154; N=157)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	105.5	140.8
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	89.5	115.5

Intervention	mg/dL (Mean)
	Change from baseline to week 24 (N=131; N=121)	Change from baseline to week 48 (N=125 ; N=117)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	4.1	7.6
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	20.8	19.8

Intervention	units on a scale (Median)
	Change from baseline to week 24 (N=165; N=165)	Change from baseline to week 48 (N=161; N=158)	Change from baseline to week 96 (N=155; N=154)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	0	0	0
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	5	0	0.5

Intervention	participants (Number)
	Week 24 (N=170; N=172)	Week 48 (N=167; N=163)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	25	30
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	26	26

Intervention	participants (Number)
	Week 24: Number with RNA < 50 c/mL (N=170; N=171)	Week 48: Number with RNA < 50 c/mL (N=169; N=165)	Week 96: Number with RNA < 50 c/mL (N=158; N=158)
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	122	112	107
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	117	106	109

Intervention	weeks (Number)
	5th percentile	10th percentile	25th percentile
Add NRTIs (Randomized) to Individualized Regimen (cPSS > 2.0)	12	12	48
Omit NRTIs (Randomized) From Individualized Regimen(cPSS > 2)	12	12	48