Page last updated: 2024-11-04

nevirapine

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Description

Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that is used to treat HIV infection. It was first synthesized in the 1980s and was approved by the FDA in 1996. Nevirapine works by blocking the activity of reverse transcriptase, an enzyme that HIV uses to copy its genetic material. This prevents the virus from replicating and spreading. Nevirapine is typically given in combination with other antiretroviral drugs. It is effective in reducing viral load and improving CD4+ cell count. Nevirapine is also used to prevent mother-to-child transmission of HIV. Nevirapine is studied because it is a valuable tool in the fight against HIV infection. It is effective in reducing viral load and improving CD4+ cell count. Nevirapine is also relatively inexpensive and is available in generic formulations. This makes it an important treatment option in resource-limited settings. Nevirapine is also being studied for its potential use in other diseases, such as cancer and autoimmune disorders.'

Nevirapine: A potent, non-nucleoside reverse transcriptase inhibitor used in combination with nucleoside analogues for treatment of HIV INFECTIONS and AIDS. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nevirapine : A dipyridodiazepine that is 5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepine which is substituted by methyl, oxo, and cyclopropyl groups at positions 4, 6, and 11, respectively. A non-nucleoside reverse transcriptase inhibitor with activity against HIV-1, it is used in combination with other antiretrovirals for the treatment of HIV infection. [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]

Cross-References

ID SourceID
PubMed CID4463
CHEMBL ID57
CHEBI ID63613
SCHEMBL ID3318
MeSH IDM0029429

Synonyms (148)

Synonym
BIDD:GT0326
AC-643
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido[3,2-b:2 ,3 -e][1,4]diazepin-6-one
bdbm1434
2-cyclopropyl-7-methyl-2,4,9,15-tetraazatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-10-one
chembl57 ,
HMS3393J09
AB00393001-15
birg-0587
viramune xr
viramune ir
hsdb 7164
nsc 641530
6h-dipyrido(3,2-b:2',3'-e)(1,4)diazepin-6-one, 11-cyclopropyl-5,11-dihydro-4-methyl-
nsc-641530
viramune
smr000048458
MLS000084585 ,
nevirapine & pro 140
11-cyclopropyl-4-methyl-5,11-dihydro-6h-dipyrido[2,3-e:3',2'-b][1,4]diazepin-6-one & pro 140 (anti-ccr5 monoclonal antibody)
bi-rg-587 & cd4-igg
nevirapine & cd4-igg
n11-cyclopropyl-4-methyl-5,11-dihydro-6h-dipyrido[3,2-b:2',3'-e]-[1,4]diazepin-6-one & cd4-immunoadhesin
bi-rg-587
nvp ,
birg 0587
birg 587
nsc641530
viramune(tm)
11-cyclopropyl-4-methyl-5,11-dihydro-6h-dipyrido[2,3-e:3',2'-b][1,4]diazepin-6-one
birg-587
11-cyclopropyl-4-methyl-5h-dipyrido[[?],[?]][1,4]diazepin-6-one
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one
NCGC00065890-02
MLS001055309
nevirapine
C07263
129618-40-2
nev ,
non-nucleoside rt inhibitor nevirapine
MLS000759409
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido(3,2-b:2',3'-e)(1,4)diazepin-6-one
DB00238
nevirapine, anhydrous
1VRT
2HNY
nevirapine anhydrous
D00435
nevirapine (jan/usp/inn)
viramune (tn)
11-cyclopropyl-4-methyl-5,11-dihydro-6h-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one
MLS001201730
birg587
HMS2051J09
chebi:63613 ,
nevirapine teva
nevirapinum anhydrous
NCGC00065890-03
NCGC00065890-04
HMS3264D21
nevirapine [usan:usp:inn:ban]
unii-99dk7fvk1h
99dk7fvk1h ,
NCGC00258324-01
tox21_200770
STK580320
BBL010768
nsc759902
pharmakon1600-01503842
nsc-759902
MLS001424058
dtxsid7031797 ,
dtxcid9010787
tox21_110982
cas-129618-40-2
bi-rg 587
N0922
HMS2231O23
CCG-100939
AKOS005504351
FT-0607215
NCGC00065890-07
AB07544
nevirapine [vandf]
nevirapinum anhydrous [who-ip latin]
nevirapine [usp impurity]
nevirapine [mi]
nevirapine [ema epar]
nevirapine [orange book]
nevirapine [ep monograph]
nevirapine [hsdb]
nevirapine [usan]
nevirapine [mart.]
nevirapine [who-dd]
nevirapine [jan]
nevirapine [inn]
nevirapine anhydrous [who-ip]
nevirapine [usp monograph]
nevirapine anhydrous [usp-rs]
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido[3,2-b:2', 3'-e][1,4]diazepin-6-one
HMS3371E03
AB00393001-13
HY-10570
MLS006011423
NC00189
SCHEMBL3318
NCGC00065890-05
tox21_110982_1
KS-5019
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido-[3,2-b:2',3'-e][1,4]diazepin-6-one
11-cyclopropyl-5,11-dihydro-4-methyl-6h-dipyrido[3,2-b :2',3'-e][1,4 ]diazepin-6-one
F2173-0607
tox21 110982
11-cyclopropyl-4-methyl-5h-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6(11h)-one
AB00393001_16
OPERA_ID_934
AB00393001_17
mfcd00866928
2-cyclopropyl-7-methyl-2,4,9,15-tetraazatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3,5,7,11,13-hexaen-10-one
2-cyclopropyl-7-methyl-2,4,9,15-tetrazatricyclo[9.4.0.03,8]pentadeca-1(11),3,5,7,12,14-hexaen-10-one
nevirapine anhydrous, united states pharmacopeia (usp) reference standard
HMS3655I08
nevirapine for peak identification, european pharmacopoeia (ep) reference standard
nevirapine (anhydrous), european pharmacopoeia (ep) reference standard
nevirapine, pharmaceutical secondary standard; certified reference material
HMS3715B10
11-cyclopropyl-4-methyl-5,11-dihydro-6h-dipyrido[3,2-b:2 inverted exclamation mark ,3 inverted exclamation mark -e][1,4]diazepin-6-one
SY009679
SW197569-2
bi-rg 587;nsc 641530;nvp
BCP05587
bi-rg-587; birg 0587; birg587; hsdb 7164; nsc 641530; nvp
Z1521553473
gtpl12676
nevirapine (viramune)
S1742
FT-0672686
nevirapine,(s)
Q263713
AC1280
EN300-119500
2-cyclopropyl-7-methyl-2,4,9,15-tetraazatricyclo[9.4.0.0,3,8]pentadeca-1(15),3(8),4,6,11,13-hexaen-10-one
NCGC00065890-14
nevirapine 100 microg/ml in acetonitrile
nevirapine for peak identification
nevirapine (anhydrous)
nevirapine)
6h-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one, 11-cyclopropyl-5,11-dihydro-4-methyl-

Research Excerpts

Overview

Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) widely used in the treatment of human immunodeficiency virus type 1 (HIV-1) and is the first-choice NNRTI during pregnancy. It is a key component of antiretroviral prophylaxis and treatment for neonates.

ExcerptReferenceRelevance
"Nevirapine (NVP) is an effective drug for the treatment of HIV infections, but its use is limited by a high incidence of severe skin rash and liver injury. "( Sulfation of 12-hydroxy-nevirapine by human SULTs and the effects of genetic polymorphisms of SULT1A1 and SULT2A1.
Cao, Y; Kurogi, K; Liu, MC; Sakakibara, Y; Segawa, K; Suiko, M; Uetrecht, J, 2022
)
2.47
"Nevirapine (NVP) is a key component of antiretroviral prophylaxis and treatment for neonates. "( Assessment of Nevirapine Prophylactic and Therapeutic Dosing Regimens for Neonates.
Aarons, L; Borkird, T; Capparelli, EV; Cressey, TR; Jittayanun, K; Jourdain, G; Lallemant, M; Le Coeur, S; Luvira, A; Phanomcheong, S; Puangsombat, A; Punyawudho, B; Saenjum, C; Sukrakanchana, PO; Urien, S, 2017
)
2.26
"Nevirapine (NVP), is an HIV-1 antiretroviral with treatment-limiting hypersensitivity reactions (HSRs) associated with multiple class I and II HLA alleles."( Shared peptide binding of HLA Class I and II alleles associate with cutaneous nevirapine hypersensitivity and identify novel risk alleles.
Bracey, A; Buus, S; Carrington, M; Chopra, A; Gaudieri, S; Haas, DW; Hunt, DF; Jing, Y; Kaever, T; Koelle, D; Malaker, SA; Mallal, S; McKinnon, EJ; Myers, P; Ostrov, DA; Pavlos, R; Peters, B; Phillips, EJ; Redwood, A; Restrepo, S; Rive, C; Schutte, R; Shabanowitz, J; Speers, E, 2017
)
1.4
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor frequently used in combination with other antiretroviral agents for highly active antiretroviral therapy (HAART) of patients infected with the human immunodeficiency virus type 1 (HIV-1). "( Nevirapine induced mitochondrial dysfunction in HepG2 cells.
Kittisenachai, S; Paemanee, A; Roytrakul, S; Sirinonthanawech, N; Smith, DR; Sornjai, W; Wongtrakul, J, 2017
)
3.34
"Nevirapine is a known inhibitor of cytochrome P450 3A4, which metabolizes artemether and lumefantrine."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
1.56
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) widely used in the treatment of human immunodeficiency virus type 1 (HIV-1) and is the first-choice NNRTI during pregnancy. "( Sex-dependent metabolism of nevirapine in rats: impact on plasma levels, pharmacokinetics and interaction with nortriptyline.
Compañ, P; Peris, JE; Usach, I, 2018
)
2.22
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 (HIV-1) widely used as a component of High Active Antiretroviral Therapy (HAART) since it is inexpensive, readily absorbed after oral administration and non-teratogenic. "( In vitro assessment of competitive and time-dependent inhibition of the nevirapine metabolism by nortriptyline in rats.
Ferrer, JM; Peris, JE; Usach, I, 2018
)
2.16
"Nevirapine is a BCS class II drug which shows dissolution rate limited absorption."( Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach.
Awasthi, R; Dua, K; Kamate, VJ; Madan, JR,
)
1.15
"Nevirapine (NVP) is a first-generation non-nucleoside reverse transcriptase inhibitor widely used for the treatment and prophylaxis of human immunodeficiency virus infection. "( Singularities of nevirapine metabolism: from sex-dependent differences to idiosyncratic toxicity.
Antunes, AMM; Caixas, U; Charneira, C; Gonçalves-Dias, C; Marinho, AT; Marques, MM; Miranda, JP; Monteiro, EC; Pereira, SA, 2019
)
2.3
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used against HIV-1. "( 2'-Deoxythymidine adducts from the anti-HIV drug nevirapine.
Antunes, AM; Beland, FA; Marques, MM; Oliveira, MC; Wolf, B, 2013
)
2.09
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV infections and has been reported to be toxic to the male reproductive system. "( Nevirapine induces testicular toxicity in Wistar rats: reversal effect of kolaviron (biflavonoid from Garcinia kola seeds).
Adaramoye, OA; Akanni, OO; Farombi, EO, 2013
)
3.28
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor, widely prescribed for type 1 human immunodeficiency virus infection. "( Association between CYP2B6 polymorphisms and Nevirapine-induced SJS/TEN: a pharmacogenetics study.
Borgiani, P; Ciccacci, C; Di Fusco, D; Erba, F; Liotta, G; Marazzi, MC; Novelli, G; Palombi, L; Zimba, I, 2013
)
2.09
"Nevirapine is an important component of highly active antiretroviral therapy used in the treatment of HIV infection. "( Measuring the overall genetic component of nevirapine pharmacokinetics and the role of selected polymorphisms: towards addressing the missing heritability in pharmacogenetic phenotypes?
Bangsberg, DR; Chinn, LW; Kroetz, DL; Martin, JN; Micheli, JE; Patel, A; Shugarts, SB, 2013
)
2.1
"Nevirapine is a non-nucleoside reverse transcriptase (RT) inhibitor used for the treatment of AIDS and the prevention of mother-to-child transmission of HIV-1. "( Differential responses of human hepatocytes to the non-nucleoside HIV-1 reverse transcriptase inhibitor nevirapine.
Beland, FA; Fang, JL, 2013
)
2.05
"Nevirapine is a much cheaper drug than its alternative efavirenz, and might be beneficial in resource constrained settings."( Nevirapine versus efavirenz-based antiretroviral therapy regimens in antiretroviral-naive patients with HIV and tuberculosis infections in India: a pilot study.
Ahmad, H; Chandrashekhar, R; Dhooria, S; Ekka, M; Khan, NH; Kumar, S; Pandey, RM; Raghunandan, P; Ranjan, S; Rewari, BB; Samantaray, JC; Sharma, SK; Sinha, S; Velpandian, T; Venkatesh, S, 2013
)
2.55
"Nevirapine (NVP) is an anti-retroviral drug used for the treatment of HIV infection, that may cause several severe adverse events, including Stevens Johnsons Syndrome/Toxic Epidermal Necrolysis (SJS/TEN). "( HCP5 genetic variant (RS3099844) contributes to Nevirapine-induced Stevens Johnsons Syndrome/Toxic Epidermal Necrolysis susceptibility in a population from Mozambique.
Borgiani, P; Ciccacci, C; Di Fusco, D; Erba, F; Mancinelli, S; Marazzi, MC; Novelli, G; Palombi, L, 2014
)
2.1
"Nevirapine is an inducer of hepatic metabolism. "( Switching from tenofovir/emtricitabine and nevirapine to a tenofovir/emtricitabine/rilpivirine single-tablet regimen in virologically suppressed, HIV-1-infected subjects.
Allavena, C; André-Garnier, E; Billaud, E; Bonnet, B; Bouchez, S; Bouquié, R; Boutoille, D; Dailly, E; Pineau, S; Raffi, F; Raveleau, A; Reliquet, V, 2014
)
2.11
"Nevirapine (NVP) is a frequently used anti-HIV drug. "( Human sulfotransferase 1A1-dependent mutagenicity of 12-hydroxy-nevirapine: the missing link?
Alves, M; Antunes, P; Kranendonk, M; Rueff, J, 2014
)
2.08
"Nevirapine is a hydrophobic non-nucleoside reverse transcriptase inhibitor, used in first line regimens of highly active antiretroviral therapy (HAART). "( Compatibility studies of nevirapine in physical mixtures with excipients for oral HAART.
de Oliveira, GG; Ferraz, HG; Severino, P; Souto, EB, 2013
)
2.14
"Nevirapine (NVP) is an effective nonnucleoside reverse transcriptase inhibitor (NNRTI) of particular interest as it is often used in resource limited countries. "( Proteomic analysis of serum and urine of HIV-monoinfected and HIV/HCV-coinfected patients undergoing long term treatment with nevirapine.
Janphen, K; Kumrapich, B; Praparattanapan, J; Roytrakul, S; Smith, DR; Supparatpinyo, K; Thongtan, T; Wongtrakul, J, 2014
)
2.05
"Nevirapine (NVP) is an orally taken anti-HIV drug associated with severe idiosyncratic reactions elicited by toxic metabolites, with women at increased risk."( Sex differences in hepatic and intestinal contributions to nevirapine biotransformation in rats.
Antunes, AM; Marinho, AT; Marques, MM; Miranda, JP; Pereira, SA; Pinheiro, PF, 2015
)
1.38
"Nevirapine is a very potent antiretroviral drug frequently used in the management of Human Immunodeficiency Virus (HIV). "( Evaluation of anti-ulcerogenic and ulcer-healing activities of nevirapine in rats.
Adeyemi, JA; Faborode, SO; Latinwo, GG; Mishra, V; Onasanwo, SA, 2015
)
2.1
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase-inhibitor, which is associated with severe idiosyncratic skin rash and hepatotoxicity. "( Different Reactive Metabolites of Nevirapine Require Distinct Glutathione S-Transferase Isoforms for Bioinactivation.
Commandeur, JN; Dekker, SJ; Vermeulen, NP; Vos, JC; Zhang, Y, 2016
)
2.16
"Nevirapine is a reverse-transcriptase inhibitor widely used in combination therapy to treat HIV infection. "( Exploring CYP2B6 activity by measuring the presence ofnevirapine hydroxy metabolites in plasma.
Ab Rahman, AK; Hassan, NB; Low, LL; Mustafa, S; Tan, SC; Wan Yusuf, WN, 2016
)
2.13
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used against the human immunodeficiency virus type 1 (HIV-1), mostly to prevent mother-to-child HIV transmission in developing countries. "( Synthesis and characterization of DNA adducts from the HIV reverse transcriptase inhibitor nevirapine.
Antunes, AM; Beland, FA; Duarte, MP; Gamboa da Costa, G; Heinze, TM; Marques, MM; Santos, PP, 2008
)
2.01
"Nevirapine (NVP) is a nonnucleoside reverse transcriptase inhibitor used in HIV patients and recently evaluated as a differentiating and antiproliferative agent in human malignancies. "( Nevirapine toxicity in non-HIV cancer patients.
Barone, C; Cignarelli, M; De Vis, K; Fabiano, A; Fersini, A; Landriscina, M; Lombardi, V; Piscazzi, A; Santodirocco, M, 2008
)
3.23
"Nevirapine is a nonnucleoside reverse transcriptase inhibitor used as part of combination therapy for human immunodeficiency virus (HIV) infection. "( Pharmacokinetic assessment of nevirapine and metabolites in human immunodeficiency virus type 1-infected patients with hepatic fibrosis.
Cammett, AM; Felizarta, F; MacGregor, TR; Mallolas, J; Miailhes, P; Piliero, PJ; Wruck, JM, 2009
)
2.08
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used against the human immunodeficiency virus type-1 (HIV-1), mostly to prevent mother-to-child transmission of the virus in developing countries. "( Amino acid adduct formation by the nevirapine metabolite, 12-hydroxynevirapine--a possible factor in nevirapine toxicity.
Antunes, AM; Beland, FA; Godinho, AL; Justino, GC; Marques, MM; Martins, IL, 2010
)
2.08
"Nevirapine is a first generation of non-nucleoside reverse transcriptase inhibitors (NNRTIs), which is usually used for the therapy of AIDS."( Study on the interaction between HIV reverse transcriptase and its non-nucleoside inhibitor nevirapine by capillary electrophoresis.
Chen, W; Li, W; Ling, X; Liu, J; Wang, X, 2010
)
1.3
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used against human immunodeficiency virus type-1 (HIV-1), mostly to prevent mother-to-child HIV-1 transmission in developing countries. "( Protein adducts as prospective biomarkers of nevirapine toxicity.
Antunes, AM; Beland, FA; Coelho, AV; Godinho, AL; Gomes, RA; Marques, MM; Martins, IL; Oliveira, MC, 2010
)
2.06
"Nevirapine-based ART is an option for HIV-infected patients who receive rifampin in resource-limited countries or those who cannot tolerate efavirenz."( Treatment outcomes of patients co-infected with HIV and tuberculosis who received a nevirapine-based antiretroviral regimen: a four-year prospective study.
Chimsuntorn, S; Eampokarap, B; Manosuthi, W; Nilkamhang, S; Sungkanuparph, S; Tantanathip, P; Thongyen, S, 2010
)
2.03
"Nevirapine is a poorly water-soluble antiretroviral drug. "( In vitro protein adsorption studies on nevirapine nanosuspensions for HIV/AIDS chemotherapy.
Jansch, M; Müller, RH; Shegokar, R; Singh, KK, 2011
)
2.08
"Nevirapine is an important component of paediatric combination HIV therapy. "( Factors influencing plasma nevirapine levels: a study in HIV-infected children on generic antiretroviral treatment in India.
Agibothu Kupparam, HK; Karunaianandham, R; Mahalingam, V; Navaneethapandian, PG; Perumal Kannabiran, B; Ramachandran, G; Shah, I; Sikhamani, R; Soundararajan, L; Swaminathan, S, 2011
)
2.11
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor of human immunodeficiency virus type-1. "( Bioavailability of nevirapine in rats after oral and subcutaneous administration, in vivo absorption from gastrointestinal segments and effect of bile on its absorption from duodenum.
Peris, JE; Usach, I, 2011
)
2.14
"Nevirapine (NVP) is a widely used non-nucleoside reverse transcriptase inhibitor. "( Bioavailability of extended-release nevirapine 400 and 300 mg in HIV-1: a multicenter, open-label study.
Arasteh, K; Battegay, M; Berger, F; Bogner, JR; Livrozet, JM; Macha, S; Mossdorf, E; Plettenberg, A; Quinson, AM; Robinson, P; Stern, J; Witt, MD; Yong, CL; Zhang, W, 2011
)
2.09
"Nevirapine is a substrate for ABCC10 and genetic variants influence its plasma concentrations. "( Association of ABCC10 polymorphisms with nevirapine plasma concentrations in the German Competence Network for HIV/AIDS.
Back, DJ; Brockmeyer, NH; Fätkenheuer, G; Hoffmann, C; Hopper-Borge, E; Khoo, SH; Knechten, H; Liptrott, NJ; Mauss, S; Owen, A; Pirmohamed, M; Pushpakom, S; Siccardi, M; Wyen, C, 2012
)
2.09
"Nevirapine (NVP) is an anti-HIV drug associated with severe hepatotoxicity and skin rashes, which raises concerns about its chronic administration. "( Oxidation of 2-hydroxynevirapine, a phenolic metabolite of the anti-HIV drug nevirapine: evidence for an unusual pyridine ring contraction.
Antunes, AM; Beland, FA; Ferreira da Silva, JL; Harjivan, SG; Marques, MM; Novais, DA; Santos, PP; Sidarus, M, 2012
)
2.14
"Nevirapine (NVP) is a nonnucleoside reverse transcriptase inhibitor (NNRTI) used worldwide as part of combination antiretroviral therapy in infants and children to treat HIV infection. "( Nevirapine exposure with WHO pediatric weight band dosing: enhanced therapeutic concentrations predicted based on extensive international pharmacokinetic experience.
Acosta, EP; Aweeka, FT; Burger, D; Capparelli, EV; Cressey, TR; Kabamba, D; Nikanjam, M; Spector, SA, 2012
)
3.26
"Nevirapine (NVP) is an antiretroviral medication that prevents human immunodeficiency virus (HIV) cells from multiplying in the blood. "( Chronic administration of the antiretroviral nevirapine increases body weight, food, and water intake in albino Wistar rats.
Obembe, AO; Osim, EE; Umoren, EB, 2012
)
2.08
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used for chronic human immunodeficiency virus infections in adults and children. "( Evaluation of nevirapine dosing recommendations in HIV-infected children.
Benaboud, S; Blanche, S; Bouazza, N; Dollfus, C; Faye, A; Foissac, F; Frange, P; Hirt, D; Lachassinne, E; Treluyer, JM; Urien, S, 2013
)
2.19
"Nevirapine (NVP) is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase. "( Nevirapine resistance after single dose prophylaxis.
Eshleman, SH; Jackson, JB,
)
3.02
"Nevirapine is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin."( Exposure of normal and transformed cells to nevirapine, a reverse transcriptase inhibitor, reduces cell growth and promotes differentiation.
Barone, C; Careddu, A; Landriscina, M; Lavia, P; Lorenzini, R; Mangiacasale, R; Mattei, E; Nervi, C; Pittoggi, C; Sciamanna, I; Spadafora, C; Travaglini, L, 2003
)
1.3
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that was first reported in the scientific literature in 1990. "( Efficacy and durability of nevirapine in antiretroviral drug näive patients.
Lange, JM, 2003
)
2.06
"Nevirapine is a nonnucleoside reverse transcriptase antiretroviral agent. "( Serious adverse cutaneous and hepatic toxicities associated with nevirapine use by non-HIV-infected individuals.
Belknap, SM; Bennett, C; Chan, J; Johnson, S; Patel, SM; Sha, BE, 2004
)
2
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor used in the treatment of human immunodeficiency virus (HIV)-infected patients and in post-exposure prophylaxis. "( Severe leukopenia associated with mild hepatotoxicity in an HIV carrier treated with nevirapine.
Krivoy, N; Pollack, S; Shahar, E; Weltfriend, S, 2004
)
1.99
"Nevirapine is an antiretroviral drug that is used for treatment as well as for the prevention of mother-to-child transmission of the human immunodeficiency virus (HIV). "( RAT CYP3A and CYP2B1/2 were not associated with nevirapine-induced hepatotoxicity.
Abraham, AM; Barr, S; Walubo, A, 2006
)
2.03
"Nevirapine is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase and is indicated for use in combination with other antiretroviral agents for the treatment of HIV-1 infection. "( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
2.04
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor commonly used in human immunodeficiency virus-1 multidrug regimens and associated with life-threatening cutaneous reactions. "( Nevirapine-induced Stevens-Johnson syndrome in a pediatric patient.
Cortes, GY; Mason, AR; Pollack, RB,
)
3.02
"Nevirapine (BI-RG-587) is a potent inhibitor of the polymerase activity of reverse transcriptase of human immunodeficiency virus type-1. "( High-performance liquid chromatography and photoaffinity crosslinking to explore the binding environment of nevirapine to reverse transcriptase of human immunodeficiency virus.
Cohen, KA; Grob, PM; Hopkins, JL; Ingraham, RH; Kapadia, SR; Palladino, DE; Stevenson, JM; Van Moffaert, GJ; Warren, TC, 1994
)
1.94
"Nevirapine is a highly potent and specific inhibitor of human immunodeficiency virus type 1 (HIV-1) polymerase, but is inactive against HIV-2 and other polymerase. "( Amino acid substitutions in HIV-1 reverse transcriptase with corresponding residues from HIV-2. Effect on kinetic constants and inhibition by non-nucleoside analogs.
Bacolla, A; Cousins, RC; Greenwood, DJ; Grygon, CA; Ingraham, RH; Piras, G; Richman, D; Rose, JM; Shih, CK; Warren, TC, 1993
)
1.73
"Nevirapine is a nonnucleoside inhibitor of reverse transcriptase (RT) which decreases the level of HIV-1 viral particles in the blood plasma of infected individuals."( Kinetic analysis of intravirion reverse transcription in the blood plasma of human immunodeficiency virus type 1-infected individuals: direct assessment of resistance to reverse transcriptase inhibitors in vivo.
Dornadula, G; Havlir, D; Pomerantz, RJ; Richman, DD; Wu, Y; Zhang, H, 1996
)
1.02
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor of HIV-1 which exhibits synergy in vitro with zidovudine (ZDV) and also is active against ZDV-resistant HIV. "( A controlled trial of nevirapine plus zidovudine versus zidovudine alone in p24 antigenaemic HIV-infected patients. The Dutch-Italian-Australian Nevirapine Study Group.
Boucher, CA; Carr, A; Cooper, DA; de Jong, MD; Imrie, A; Sorice, F; Vella, S, 1996
)
2.05
"Nevirapine is a potent antiretroviral agent whose use, especially as monotherapy, may be limited by rapid onset of resistance as well as by hypersensitivity reactions. "( Current clinical experience with nevirapine for HIV infection.
Carr, A; Cooper, DA, 1996
)
2.02
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1-infected patients. "( Rapid determination of nevirapine in human plasma by ion-pair reversed-phase high-performance liquid chromatography with ultraviolet detection.
Beijnen, JH; Hoetelmans, RM; Meenhorst, PL; Mulder, JW; van Heeswijk, RP, 1998
)
2.05
"Nevirapine (NVP) is a nonnucleoside reverse transcriptase inhibitor widely used in combination with other antiretroviral agents for the treatment of human immunodeficiency virus disease. "( Safety profile of nevirapine, a nonnucleoside reverse transcriptase inhibitor for the treatment of human immunodeficiency virus infection.
Dransfield, K; Pollard, RB; Robinson, P,
)
1.91
"Nevirapine (NVP) is a potent noncompetitive inhibitor of the reverse transcriptase enzyme, which is necessary for HIV replication. "( [Antiretroviral agent nevirapine: its pharmacological action and potential for clinical use].
Osugi, T; Takeuchi, S, 1999
)
2.06
"Nevirapine (VIRAMUNE) is a non-nucleoside reverse transcriptase inhibitor with activity against human immunodeficiency virus type 1 (HIV-1), currently marketed for the treatment of HIV-1 infected adults. "( HPLC-UV method for the quantitation of nevirapine in biological matrices following solid phase extraction.
Korpalski, DJ; Pav, JW; Rowland, LS, 1999
)
2.02
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used as part of combination antiretroviral therapy for the treatment of HIV infection."( Late onset hepatitis and prolonged deterioration in hepatic function associated with nevirapine therapy.
Clarke, S; Condon, C; Harrington, P; Kelleher, D; Mulcahy, F; Smith, OP, 2000
)
1.25
"(4) Nevirapine is a liver enzyme inducer, hence the possibility of drug interactions, especially with protease inhibitors of HIV; the clinical consequences are poorly known."( Nevirapine: new preparation. In second-line triple-drug anti-HIV regimens.
, 1998
)
2.22
"Nevirapine is a highly specific inhibitor of HIV-1 reverse transcriptase (RT), an important therapeutic target for the treatment of HIV infection. "( Nevirapine: a review of its use in the prevention and treatment of paediatric HIV infection.
Bardsley-Elliot, A; Perry, CM,
)
3.02
"Nevirapine is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase. "( Nevirapine: pharmacokinetic considerations in children and pregnant women.
Clarke, DF; Dorenbaum, A; Mirochnick, M, 2000
)
3.19
"Nevirapine is a nonnucleoside reverse transcriptase inhibitor (NNRTI) that has the most common treatment limiting side effect of rash. "( Sex differences in nevirapine rash.
Aberg, JA; Bersoff-Matcha, SJ; Hamrick, HJ; Miller, WC; Mundy, LM; Powderly, WG; van Der Horst, C, 2001
)
2.08
"Nevirapine is a non-nucleoside reverse transcriptase inhibitor widely used in combination with other antiretroviral agents for the treatment of HIV infection. "( Stevens-Johnson syndrome caused by the antiretroviral drug nevirapine.
Farmer, KL; Hebert, AA; Lahart, CJ; Metry, DW, 2001
)
2
"Nevirapine is an antiretroviral agent belonging to the class of non-nucleoside reverse transcriptase inhibitors. "( Simple and rapid determination of nevirapine in human serum by reversed-phase high-performance liquid chromatography.
Gomez, MR; Lopez, RM; Monterde, J; Pou, L; Ruiz, I, 2001
)
2.03
"Nevirapine is a non-nucleoside HIV reverse transcriptase inhibitor."( Nevirapine: ethical dilemmas and care for HIV-infected mothers.
Benson, M; Shannon, M, 1995
)
2.46
"Nevirapine is a nonnucleoside reverse transcription inhibitor that is used as part of highly active antiretroviral therapeutic combinations. "( Jaundice and hepatocellular damage associated with nevirapine therapy.
Bonacini, M; Poreddy, V; Prakash, M; Tiyyagura, L, 2001
)
2.01
"Nevirapine (BI-RG-587) is a potent and specific non-nucleoside inhibitor of human immunodeficiency virus type-1 reverse transcriptase. "( Characterization of the binding site for nevirapine (BI-RG-587), a nonnucleoside inhibitor of human immunodeficiency virus type-1 reverse transcriptase.
Adams, J; Cohen, KA; Hopkins, J; Ingraham, RH; Kinkade, P; Palladino, DE; Pargellis, C; Rogers, S; Warren, TC; Wu, JC, 1991
)
1.99

Effects

Nevirapine has an exceptional record for long-term tolerability with few side effects in human immunodeficiency virus (HIV) combined antiretroviral therapy. It has a short and limited inductive effect on rilpivirine metabolism, which is not clinically significant.

Nevirapine has a short and limited inductive effect on rilpivirine metabolism, which is not clinically significant. The drug has a half life for enantiomerisation at room temperature of the order of seconds, and cannot exist as separable enantiomers.

ExcerptReferenceRelevance
"Nevirapine has an exceptional record for long-term tolerability with few side effects in human immunodeficiency virus (HIV) combined antiretroviral therapy (cART). "( Nevirapine in HIV maintenance therapy - can "old drugs" survive in current HIV management?
Bregenzer, A; Kahlert, CR; Notter, J; Vernazza, P, 2019
)
3.4
"Nevirapine has a short and limited inductive effect on rilpivirine metabolism, which is not clinically significant. "( Switching from tenofovir/emtricitabine and nevirapine to a tenofovir/emtricitabine/rilpivirine single-tablet regimen in virologically suppressed, HIV-1-infected subjects.
Allavena, C; André-Garnier, E; Billaud, E; Bonnet, B; Bouchez, S; Bouquié, R; Boutoille, D; Dailly, E; Pineau, S; Raffi, F; Raveleau, A; Reliquet, V, 2014
)
2.11
"Nevirapine has a half life for enantiomerisation at room temperature of the order of seconds, is not atropisomeric, and cannot exist as separable enantiomers."( Is nevirapine atropisomeric? Experimental and computational evidence for rapid conformational inversion.
Burke, EW; Clayden, J; Hillier, IH; Morris, GA; Vincent, MA, 2012
)
1.72
"Nevirapine has a beneficial effect on the lipid profile in both treatment-naive and -experienced patients."( Nevirapine in the treatment of HIV.
Martínez, E; Milinkovic, A, 2004
)
2.49
"Nevirapine has a long half-life and achieves high steady-state plasma concentrations relative to the concentration required to inhibit 50% viral replication in vitro (IC(50)) in patients."( Once-daily nevirapine dosing: a pharmacokinetics, efficacy and safety review.
Cooper, CL; van Heeswijk, RP, 2007
)
1.45
"Nevirapine has been proved to suppress tumor growth and induce differentiation in several tumor cells, but has not previously been evaluated in metastasis of thyroid cancer."( Nevirapine inhibits migration and invasion in dedifferentiated thyroid cancer cells.
Dong, J; Liao, L; Shang, H; Wang, H; Wang, S; Yao, J; Zhao, J, 2019
)
2.68
"Nevirapine has been used as antiretroviral agent since early '90. "( Clinical and genetic factors associated with increased risk of severe liver toxicity in a monocentric cohort of HIV positive patients receiving nevirapine-based antiretroviral therapy.
Cattaneo, D; Cheli, S; Clementi, E; Di Cristo, V; Falvella, FS; Galli, M; Giacomelli, A; Lupo, A; Oreni, ML; Renisi, G; Ridolfo, AL; Riva, A; Rusconi, S, 2018
)
2.12
"Nevirapine has an exceptional record for long-term tolerability with few side effects in human immunodeficiency virus (HIV) combined antiretroviral therapy (cART). "( Nevirapine in HIV maintenance therapy - can "old drugs" survive in current HIV management?
Bregenzer, A; Kahlert, CR; Notter, J; Vernazza, P, 2019
)
3.4
"Nevirapine has a short and limited inductive effect on rilpivirine metabolism, which is not clinically significant. "( Switching from tenofovir/emtricitabine and nevirapine to a tenofovir/emtricitabine/rilpivirine single-tablet regimen in virologically suppressed, HIV-1-infected subjects.
Allavena, C; André-Garnier, E; Billaud, E; Bonnet, B; Bouchez, S; Bouquié, R; Boutoille, D; Dailly, E; Pineau, S; Raffi, F; Raveleau, A; Reliquet, V, 2014
)
2.11
"Nevirapine has low solubility, an acid medium being the most appropriate medium for assessing the release of the drug from dosage forms."( Compatibility studies of nevirapine in physical mixtures with excipients for oral HAART.
de Oliveira, GG; Ferraz, HG; Severino, P; Souto, EB, 2013
)
1.41
"Nevirapine has a half life for enantiomerisation at room temperature of the order of seconds, is not atropisomeric, and cannot exist as separable enantiomers."( Is nevirapine atropisomeric? Experimental and computational evidence for rapid conformational inversion.
Burke, EW; Clayden, J; Hillier, IH; Morris, GA; Vincent, MA, 2012
)
1.72
"Nevirapine has a beneficial effect on the lipid profile in both treatment-naive and -experienced patients."( Nevirapine in the treatment of HIV.
Martínez, E; Milinkovic, A, 2004
)
2.49
"Nevirapine has a long half-life and achieves high steady-state plasma concentrations relative to the concentration required to inhibit 50% viral replication in vitro (IC(50)) in patients."( Once-daily nevirapine dosing: a pharmacokinetics, efficacy and safety review.
Cooper, CL; van Heeswijk, RP, 2007
)
1.45
"Nevirapine has been widely used in pregnancy for its efficacy, low pill burden, bioavailability and rapid transplacental transfer. "( Safety of nevirapine in pregnancy.
Anderson, J; de Ruiter, A; Edwards, SG; Hay, P; McDonald, C; Natarajan, U; Pym, A; Taylor, GP; Velisetty, P; Welch, J, 2007
)
2.18
"Nevirapine resistance has been detected in a considerable proportion of women after single-dose nevirapine (SD-NVP) for the prevention of mother-to-child human immunodeficiency virus-1 transmission. "( Use of single-dose nevirapine for the prevention of mother-to-child transmission of HIV-1: does development of resistance matter?
Eshleman, SH; Kourtis, AP; McConnell, MS; Stringer, JS; Weidle, PJ, 2007
)
2.11
"Nevirapine has shown antiretroviral efficacy as part of combination therapy with zidovudine and either didanosine or lamivudine in small numbers of paediatric patients in phase I/II trials."( Nevirapine: a review of its use in the prevention and treatment of paediatric HIV infection.
Bardsley-Elliot, A; Perry, CM,
)
2.3
"Nevirapine has been associated with a skin rash in 32 to 48% of patients."( Jaundice and hepatocellular damage associated with nevirapine therapy.
Bonacini, M; Poreddy, V; Prakash, M; Tiyyagura, L, 2001
)
1.28

Actions

Nevirapine did not inhibit hydroxylation of tolbutamide (CYP2C9) or S-mephenytoin (Cyp2C19) These CYP isoforms were importantly inhibited by delavirdine and efavirenz.

ExcerptReferenceRelevance
"Nevirapine (NVP) can cause serious skin rashes and hepatotoxicity. "( Identification of danger signals in nevirapine-induced skin rash.
Sharma, AM; Uetrecht, J; Zhang, X, 2013
)
2.11
"Nevirapine treatment can cause a skin rash. "( A study of the specificity of lymphocytes in nevirapine-induced skin rash.
Chen, X; Gou, H; Mannargudi, B; Tharmanathan, T; Uetrecht, JP, 2009
)
2.06
"Nevirapine did not inhibit hydroxylation of tolbutamide (CYP2C9) or S-mephenytoin (CYP2C19), but these CYP isoforms were importantly inhibited by delavirdine and efavirenz."( Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors.
Daily, JP; Duan, SX; Giancarlo, GM; Granda, BW; Greenblatt, DJ; Harmatz, JS; Shader, RI; von Moltke, LL, 2001
)
1.03

Treatment

Nevirapine (NVP) treatment is associated with a significant incidence of skin rash in humans, and it also causes a similar immune-mediated skin rash. When treated with nevirapine, Brown Norway rats developed red ears on about day 7 and skin rash on aboutday 21.

ExcerptReferenceRelevance
"Nevirapine (NVP) treatment is associated with a significant incidence of skin rash in humans, and it also causes a similar immune-mediated skin rash in Brown Norway (BN) rats. "( 12-OH-nevirapine sulfate, formed in the skin, is responsible for nevirapine-induced skin rash.
Novalen, M; Sharma, AM; Tanino, T; Uetrecht, JP, 2013
)
2.31
"Nevirapine (0-250 µM) treatment caused a slight increase in the amount of lactate dehydrogenase released into the medium."( Differential responses of human hepatocytes to the non-nucleoside HIV-1 reverse transcriptase inhibitor nevirapine.
Beland, FA; Fang, JL, 2013
)
1.33
"Nevirapine treated cells strongly accumulated SA-b-Gal activity and also expressed increased levels of p53 and p21 when analyzed via RT-PCR."( Nevirapine induces growth arrest and premature senescence in human cervical carcinoma cells.
Anastasiadou, V; Antsaklis, A; Kiapekou, E; Loutradis, D; Nikas, V; Patris, G; Rodolakis, A; Stefanidis, K; Vassiliou, LV; Vlachos, G, 2008
)
2.51
"Nevirapine treatment can cause a skin rash. "( A study of the specificity of lymphocytes in nevirapine-induced skin rash.
Chen, X; Gou, H; Mannargudi, B; Tharmanathan, T; Uetrecht, JP, 2009
)
2.06
"Nevirapine treatment was stopped and was substituted with efavirenz: the patient continued on therapy with tenofovir and lamivudine."( Hyperhidrosis related to nevirapine therapy.
Belda, A; Borrás-Blasco, J; Casterá, E; Jiménez, I; López-Montes, L; Rosique-Robles, D, 2012
)
1.4
"Nevirapine (NVP) treatment is associated with a significant incidence of liver injury. "( Bioactivation of nevirapine to a reactive quinone methide: implications for liver injury.
Hayes, MA; Li, Y; Novalen, M; Sharma, AM; Uetrecht, J, 2012
)
2.16
"Nevirapine (NVP) treatment is associated with serious skin rashes that appear to be immune-mediated. "( Nevirapine bioactivation and covalent binding in the skin.
Klarskov, K; Sharma, AM; Uetrecht, J, 2013
)
3.28
"Nevirapine, used for the treatment of HIV infection, is associated with development of skin rash and liver toxicity. "( Study of the sequence of events involved in nevirapine-induced skin rash in Brown Norway rats.
Caswell, JL; Mannargudi, B; Popovic, M; Shenton, JM; Uetrecht, JP, 2006
)
2.04
"Nevirapine-treated babies were tested after 15 months of age, and two of 13 HIV-exposed infants had a positive rapid HIV antibody test (15.3% transmission rate with treatment)."( Birth attendants trained in "Prevention of Mother-To-Child HIV Transmission" provide care in rural Cameroon, Africa.
Diom, E; Meyer, DJ; Mitchell, P; Tih, PM; Wanyu, B,
)
0.85
"Mass treatment of nevirapine would increase access to antiretroviral drugs among pregnant women because they can access nevirapine without volunteer counseling and testing, which 31% of pregnant women in developing countries refused to accept due to the fear of stigmatization."( Mass treatment with nevirapine to prevent mother-to-child transmission of HIV/AIDS in sub-Saharan African countries.
Hashimoto, H; Kapiga, SH; Murata, Y, 2002
)
0.96
"When treated with nevirapine, Brown Norway rats developed red ears on about day 7 and skin rash on about day 21."( Study of the sequence of events involved in nevirapine-induced skin rash in Brown Norway rats.
Caswell, JL; Mannargudi, B; Popovic, M; Shenton, JM; Uetrecht, JP, 2006
)
0.92

Toxicity

There was a trend towards a lower rate of serious adverse reactions in Ugandan adults with low CD4 starting ARV regimens with abacavir. The ultimate goal is to develop diagnostic methods for predicting the onset of nevirapine-induced toxic reactions.

ExcerptReferenceRelevance
" Drug-related adverse events were similar in adults and children, with rash and nausea most frequently reported in adults and rash and granulocytopenia most frequently reported in children."( Safety profile of nevirapine, a nonnucleoside reverse transcriptase inhibitor for the treatment of human immunodeficiency virus infection.
Dransfield, K; Pollard, RB; Robinson, P,
)
0.47
"The number and type of adverse events; nevirapine concentrations in the plasma and breast milk; maternal plasma HIV-1 RNA copy number before and up to 6 weeks after delivery; and HIV-1 infection status of the infants were monitored."( A phase I/II study of the safety and pharmacokinetics of nevirapine in HIV-1-infected pregnant Ugandan women and their neonates (HIVNET 006).
Allen, M; Bagenda, D; Dransfield, K; Elliott, T; Fleming, T; Fowler, MG; Guay, LA; Hom, D; Horton, S; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, L; Murarka, A; Musoke, P; Nakabiito, C; Pav, JW, 1999
)
0.82
"Nevirapine was well tolerated by women and infants; no serious adverse events that were related to nevirapine were observed."( A phase I/II study of the safety and pharmacokinetics of nevirapine in HIV-1-infected pregnant Ugandan women and their neonates (HIVNET 006).
Allen, M; Bagenda, D; Dransfield, K; Elliott, T; Fleming, T; Fowler, MG; Guay, LA; Hom, D; Horton, S; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, L; Murarka, A; Musoke, P; Nakabiito, C; Pav, JW, 1999
)
1.99
"Eight patients who were infected with human immunodeficiency virus, and who had each sustained an adverse drug reaction while following a regimen including nevirapine, were switched to a regimen including efavirenz."( The tolerability of efavirenz after nevirapine-related adverse events.
Barry, M; Clarke, S; Harrington, P; Mulcahy, F, 2000
)
0.78
"(1) Introduce nevirapine at half the target dose, and monitor the skin, mucous membranes and liver to avoid fatal adverse effects."( Severe hepatic and cutaneous adverse effects with nevirapine.
, 2000
)
0.92
" To characterize NVP-associated PEP toxicity, CDC and the Food and Drug Administration (FDA) reviewed MedWatch reports of serious adverse events in persons taking NVP for PEP received by FDA (Figure 1)."( Serious adverse events attributed to nevirapine regimens for postexposure prophylaxis after HIV exposures--worldwide, 1997-2000.
, 2001
)
0.58
"Cutaneous and hepatic adverse reactions and clinical hepatitis were assessed."( Hepatotoxicity in HIV-1-infected patients receiving nevirapine-containing antiretroviral therapy.
Arnaiz, JA; Blanco, JL; Carné, X; Cruceta, A; García-Viejo, MA; Gatell, JM; Mallolas, J; Marcos, MA; Martínez, E; Milinkovic, A; Mocroft, A; Pérez-Cuevas, JB; Phillips, A, 2001
)
0.56
" Three patients discontinued therapy for drug-related adverse events."( Safety and antiviral activity at 48 weeks of lopinavir/ritonavir plus nevirapine and 2 nucleoside reverse-transcriptase inhibitors in human immunodeficiency virus type 1-infected protease inhibitor-experienced patients.
Benson, CA; Brun, SC; Deeks, SG; Eron, JJ; Feinberg, J; Gulick, RM; Hicks, C; Hsu, A; Japour, AJ; Kempf, D; Kessler, HA; King, M; Murphy, RL; Real, K; Riddler, S; Sax, PE; Stryker, R; Sun, E; Thompson, M; Wheeler, D, 2002
)
0.55
" All other patients have been taking nevirapine for more than 3 months without any adverse reaction."( Long-term safety and efficacy of nevirapine tolerance induction.
Bousquet, J; Demoly, P; Fabre, J; Messaad, D; Reynes, J, 2002
)
0.87
" No significant differences were detected between the treatment groups in virological or immunological response or cessation of study drugs due to adverse events, although it is possible that the study was underpowered to detect differences."( Randomized, open-label, comparative trial to evaluate the efficacy and safety of three antiretroviral drug combinations including two nucleoside analogues and nevirapine for previously untreated HIV-1 Infection: the OzCombo 2 study.
Amin, J; Carr, A; Cooper, D; Drummond, F; Emery, S; French, M; Law, M; Roth, N,
)
0.33
"Simplification is safe and effective, but it should be offered to patients with shorter treatment duration, and in good clinical and immunovirological conditions."( Simplification of protease inhibitor-containing regimens with efavirenz, nevirapine or abacavir: safety and efficacy outcomes.
Adorni, F; Bini, T; Bongiovanni, M; Capetti, A; Castelnuovo, B; Chiesa, E; Cicconi, P; d'Arminio Monforte, A; Faggion, I; Melzi, S; Mussini, C; Rizzardini, G; Rusconi, S; Sollima, S; Tordato, F, 2003
)
0.55
"Antiretroviral therapy is associated with serious adverse events."( Drug rash with eosinophilia and systemic symptoms syndrome and renal toxicity with a nevirapine-containing regimen in a pregnant patient with human immunodeficiency virus.
Boswell, H; Fan-Havard, P; Knudtson, E; Para, M, 2003
)
0.54
"The A/S/D regimen had a low efficacy and a high frequency of adverse events and cannot be recommended."( Low efficacy and high frequency of adverse events in a randomized trial of the triple nucleoside regimen abacavir, stavudine and didanosine.
Gerstoft, J; Katzenstein, TL; Kirk, O; Lundgren, JD; Mathiesen, L; Nielsen, H; Obel, N; Pedersen, C, 2003
)
0.32
" Using the recommended lead-in dosing schedule in conjunction with good health care management, this adverse event can be controlled in the vast majority of patients."( Defining the toxicity profile of nevirapine and other antiretroviral drugs.
Murphy, RL, 2003
)
0.6
" Our data indicate that NVP prophylaxis for 6 months was safe and well tolerated in infants."( Safety and trough concentrations of nevirapine prophylaxis given daily, twice weekly, or weekly in breast-feeding infants from birth to 6 months.
Abdool Karim, SS; Bassett, MT; Coovadia, HM; Emel, L; Eshleman, SH; Fleming, T; George, K; Jones, SA; Katzenstein, DA; Maldonado, Y; Maponga, CC; Mirochnick, MM; Mofenson, LM; Mwatha, A; Shetty, AK; Wells, J, 2003
)
0.59
" Assessment consisted of CD4+ cell count, plasma HIV-1 RNA load, and adverse effects of study medications."( Nevirapine plus efavirenz plus didanosine: a simple, safe, and effective once-daily regimen for patients with HIV infection.
Carroll, H; Conlon, V; Green, A; Green, DC; Green, R; Jefferson, R; Jordan, WC; Tolbert, L; Yemofio, F, 2003
)
1.76
"In HIV-infected women receiving prenatal care and ART, adverse events were uncommon."( Maternal toxicity and pregnancy complications in human immunodeficiency virus-infected women receiving antiretroviral therapy: PACTG 316.
Balasubramanian, R; Culnane, M; Cunningham, CK; Delfraissy, JF; Delke, I; Dorenbaum, A; Fiore, S; Gelber, RD; Maupin, RT; Mofenson, LM; Newell, ML; Watts, DH, 2004
)
0.32
" The one adverse event associated with nelfinavir occurred in a subject with a CD4 cell count less than 250 cells/microL."( Maternal toxicity with continuous nevirapine in pregnancy: results from PACTG 1022.
Baker, D; Foca, M; Frenkel, LM; Gandia, J; Gonzalez-Garcia, A; Hitti, J; Huang, S; McNamara, J; Nachman, SA; Paul, ME; Provisor, A; Stek, AM; Stevens, LM; Thorpe, EM; Watts, DH; Wei, LJ, 2004
)
0.6
"5), severe adverse effects 17."( Effectiveness and safety of a generic fixed-dose combination of nevirapine, stavudine, and lamivudine in HIV-1-infected adults in Cameroon: open-label multicentre trial.
Andrieux-Meyer, I; Bourgeois, A; Calmy, A; Delaporte, E; Kazatchkine, M; Kouanfack, C; Koulla-Shiro, S; Lactuock, B; Laurent, C; Liégeois, F; Mougnutou, R; Mpoudi-Ngolé, E; Nerrienet, E; Nkoué, N; Nzeusseu, V; Peeters, M; Peytavin, G; Tardy, M; Zekeng, L,
)
0.37
" Twelve subjects in the QD Group (14%) discontinued treatment due to adverse events, mainly nevirapine-related hepatitis (6%)."( Safety and efficacy of once-daily didanosine, tenofovir and nevirapine as a simplification antiretroviral approach.
Burger, D; Clotet, B; Galindos, MJ; Gel, S; Miralles, C; Moltó, J; Muñoz-Moreno, JA; Negredo, E; Pedrol, E; Puig, J; Ribera, E; Rodriguez Fumaz, C; Rodríguez, E; Ruiz, L; Viciana, P; Videla, S, 2004
)
0.79
"The switching of a PI to nevirapine is a safe and well-tolerated option for maintaining long-term virological suppression and immunological control."( Long-term efficacy and safety of protease inhibitor switching to nevirapine in HIV-infected patients with undetectable virus load.
Arranz, A; de Górgolas, M; Estrada, V; Fernández-Guerrero, M; García, R; Gil, P; Granizo, JJ; Rivas, P; Yera, C, 2004
)
0.86
" However, its use has recently been limited because of adverse cutaneous and hepatic effects."( Severe leukopenia associated with mild hepatotoxicity in an HIV carrier treated with nevirapine.
Krivoy, N; Pollack, S; Shahar, E; Weltfriend, S, 2004
)
0.55
" The incidence of rash in the NVP group was significantly higher in female patients with higher CD4 cell counts, while adverse events in the EFV group were not associated with CD4 cell count."( The effect of baseline CD4 cell count and HIV-1 viral load on the efficacy and safety of nevirapine or efavirenz-based first-line HAART.
Andrews, S; Grinsztejn, B; Lange, JM; Lazanas, MK; Montaner, J; van Leth, F; Wilkins, E, 2005
)
0.55
" These data have now provided a clear and clinically relevant understanding of the individual profiles of drugs within the nucleoside analogue reverse transcriptase inhibitor , HIV protease inhibitor and non-nucleoside analogue reverse transcriptase inhibitor drug classes, and have provided a rational basis for assessing and monitoring these adverse effects in clinical practice."( Adverse effects of antiretroviral therapy for HIV infection: a review of selected topics.
Mallal, S; Nolan, D; Reiss, P, 2005
)
0.33
" Based on current knowledge, the immense benefits of antiretroviral prophylaxis in reducing the risk of MTCT, far outweigh the potential for adverse effects."( The safety of antiretroviral drugs in pregnancy.
Newell, ML; Thorne, C, 2005
)
0.33
"In 15 centres specializing in HIV in The Netherlands, data on patient characteristics, HAART, adverse events, viral load response, mode of delivery and HIV status of the neonate were obtained from medical records of HIV-infected pregnant women who received HAART during pregnancy between January 1997 and June 2003."( Nelfinavir and nevirapine side effects during pregnancy.
Boer, K; de Wolf, F; Dieleman, J; Godfried, MH; Nellen, J; Schneider, ME; Sprenger, H; Tempelman, C; Timmermans, S; van der Ende, ME, 2005
)
0.68
" No major adverse events occurred."( Nelfinavir and nevirapine side effects during pregnancy.
Boer, K; de Wolf, F; Dieleman, J; Godfried, MH; Nellen, J; Schneider, ME; Sprenger, H; Tempelman, C; Timmermans, S; van der Ende, ME, 2005
)
0.68
"The relationships between adverse events (AEs) and plasma concentrations of nevirapine (NVP) and efavirenz (EFV) were investigated as part of the large, international, randomized 2NN study."( Are adverse events of nevirapine and efavirenz related to plasma concentrations?
Baraldi, E; Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Montella, F; Robinson, PA; Russell, DB; Thompson, MA; Uip, DE; van Leth, F, 2005
)
0.87
"To compare the adverse events after initiation of NVP-based ART among HIV-infected patients who did not receive fluconazole (group A), received fluconazole 400 mg/week (group B), and received fluconazole 200 mg/day (group C)."( Safety and tolerability of nevirapine-based antiretroviral therapy in HIV-infected patients receiving fluconazole for cryptococcal prophylaxis: a retrospective cohort study.
Chaovavanich, A; Chumpathat, N; Manosuthi, W; Sungkanuparph, S, 2005
)
0.63
"Initiation of NVP-based ART among Thais with advance HIV disease receiving fluconazole is safe and well-tolerated."( Safety and tolerability of nevirapine-based antiretroviral therapy in HIV-infected patients receiving fluconazole for cryptococcal prophylaxis: a retrospective cohort study.
Chaovavanich, A; Chumpathat, N; Manosuthi, W; Sungkanuparph, S, 2005
)
0.63
" Therapy was discontinued in 18 patients due to virological failure in 11, adverse events in seven, loss to follow-up or withdrawal of consent in four and death in one."( Efficacy and safety of once-daily combination therapy with didanosine, lamivudine and nevirapine in antiretroviral-naive HIV-infected patients.
Blanco, JL; Crespo, M; Deig, E; Falcó, V; González, A; Miró, JM; Ocaña, I; Pahissa, A; Pedrol, E; Ribera, E; Rodríguez-Pardo, D; Rubio, M; Soler, A, 2005
)
0.55
"A once-daily combination of ddI, 3TC and NVP seems to be an effective, safe and easy-to-take regimen in antiretroviral-naive patients, at least in those who do not have severe immunodepression at baseline."( Efficacy and safety of once-daily combination therapy with didanosine, lamivudine and nevirapine in antiretroviral-naive HIV-infected patients.
Blanco, JL; Crespo, M; Deig, E; Falcó, V; González, A; Miró, JM; Ocaña, I; Pahissa, A; Pedrol, E; Ribera, E; Rodríguez-Pardo, D; Rubio, M; Soler, A, 2005
)
0.55
" Clinical assessment included plasma HIV-1 RNA, blood chemistry, haematology, lymphocyte counts and adverse events reports."( A randomized controlled trial investigating the efficacy and safety of switching from a protease inhibitor to nevirapine in patients with undetectable viral load.
Arranz Caso, JA; Castilla, V; Estrada, V; Fernández Guerrero, M; Górgolas, M; López, JC; Molina, JP; Santos, I; Sanz, J, 2005
)
0.54
"Nevirapine-based therapy is associated with increased frequency of adverse events among women with CD4+ cell count of 250 cells/microL or greater."( Third-trimester maternal toxicity with nevirapine use in pregnancy.
Brady, MT; Fan-Havard, P; Hughes, L; Joy, S; Koletar, SL; Para, MF; Poi, M, 2005
)
2.04
" The incidence of adverse events was determined and analyzed by CD4+ cell count of either less than or greater than or equal to 250 cells/microL, and gestational age when nevirapine was initiated."( Third-trimester maternal toxicity with nevirapine use in pregnancy.
Brady, MT; Fan-Havard, P; Hughes, L; Joy, S; Koletar, SL; Para, MF; Poi, M, 2005
)
0.79
" All 3 cases of adverse events occurred in this group within 6 weeks of initiating therapy and with CD4+ cell count greater than 250 cells/microL."( Third-trimester maternal toxicity with nevirapine use in pregnancy.
Brady, MT; Fan-Havard, P; Hughes, L; Joy, S; Koletar, SL; Para, MF; Poi, M, 2005
)
0.6
"The incidence of adverse events with nevirapine may be lower than previously reported (13% versus 29%) and may be primarily noted with initiating the drug late in pregnancy."( Third-trimester maternal toxicity with nevirapine use in pregnancy.
Brady, MT; Fan-Havard, P; Hughes, L; Joy, S; Koletar, SL; Para, MF; Poi, M, 2005
)
0.87
" Several observational studies have described a higher frequency of antiretroviral-related adverse effects among women compared with men."( Sex differences in antiretroviral therapy-associated intolerance and adverse events.
Clark, R, 2005
)
0.33
" Multivariate logistic regression was used to test independent association of CD4 and hepatitis C virus (HCV) infection related to the outcome of toxic effects of NVP."( Nevirapine toxicity in a cohort of HIV-1-infected pregnant women.
Calvet, GA; Cruz, ML; D'Ippolito, MM; João, EC; Matos, HJ; Menezes, JA; Salgado, LA, 2006
)
1.78
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"7% of all adverse events reported during the investigation were attributable to NVP."( Long-term safety and efficacy of nevirapine-based approaches in HIV type 1-infected patients.
Bonjoch, A; Cervantes, M; Cinquegrana, D; Clotet, B; Cucurull, J; Dalmau, D; Domingo, P; Force, L; Llibre, JM; Masabeu, A; Mascaró, J; Paredes, R; Pedrol, E; Pérez-Alvarez, N; Puig, J; Ribera, E; Vilaró, J, 2006
)
0.62
" This is a retrospective analysis of virologic efficacy and changes in adverse neuropsychiatric effects and serum lipid levels after this switch."( Switch from efavirenz to nevirapine associated with resolution of efavirenz-related neuropsychiatric adverse events and improvement in lipid profiles.
Curtin, JM; Ward, DJ, 2006
)
0.64
"To assess the incidence and consequences of adverse reactions among African HIV-positive pregnant women treated with fixed-dose combinations of a nevirapine-containing antiretroviral (ARV) triple therapy."( Safety of nevirapine-containing antiretroviral triple therapy regimens to prevent vertical transmission in an African cohort of HIV-1-infected pregnant women.
da Cruz Gomes, A; Germano, P; Guidotti, G; Liotta, G; Loureiro, S; Mancinelli, S; Marazzi, MC; Narciso, P; Palombi, L; Perno, CF; Valls Blazquez, MC, 2006
)
0.94
" Multivariate analysis to assess the impact of several factors on the adverse reaction rate was performed."( Safety of nevirapine-containing antiretroviral triple therapy regimens to prevent vertical transmission in an African cohort of HIV-1-infected pregnant women.
da Cruz Gomes, A; Germano, P; Guidotti, G; Liotta, G; Loureiro, S; Mancinelli, S; Marazzi, MC; Narciso, P; Palombi, L; Perno, CF; Valls Blazquez, MC, 2006
)
0.74
"Nevirapine-containing regimens in pregnant woman, at all CD4 cell count levels, appear to be safe in African settings."( Safety of nevirapine-containing antiretroviral triple therapy regimens to prevent vertical transmission in an African cohort of HIV-1-infected pregnant women.
da Cruz Gomes, A; Germano, P; Guidotti, G; Liotta, G; Loureiro, S; Mancinelli, S; Marazzi, MC; Narciso, P; Palombi, L; Perno, CF; Valls Blazquez, MC, 2006
)
2.18
" Unfortunately, its adverse effects, mainly hypersensitivity skin reactions and hepatotoxicity, have hampered the use of nevirapine."( RAT CYP3A and CYP2B1/2 were not associated with nevirapine-induced hepatotoxicity.
Abraham, AM; Barr, S; Walubo, A, 2006
)
0.8
"Liver toxicity is one of the most relevant adverse effects of antiretroviral therapy."( Liver toxicity induced by non-nucleoside reverse transcriptase inhibitors.
Mira, JA; Pineda, JA; Rivero, A, 2007
)
0.34
" The objectives were to compare NVP levels, adverse events, and 36-week efficacy of NVP-based ART between patients who did not receive FLU (group A) and those who received FLU 200 mg/day or 400 mg/day (group B)."( Plasma nevirapine levels, adverse events and efficacy of antiretroviral therapy among HIV-infected patients concurrently receiving nevirapine-based antiretroviral therapy and fluconazole.
Athichathanabadi, C; Manosuthi, W; Phoorisri, T; Sungkanuparph, S; Uttayamakul, S, 2007
)
0.79
" Neutropenia (usually transient) was the most common severe adverse event."( Safety of HIV-1 Perinatal Transmission Prophylaxis With Zidovudine and Nevirapine in Rural South India.
Bethel, J; Dharmarajan, S; Jacob, SM; Junankar, V; Parameshwari, S; Read, JS; Samuel, NM; Stoszek, SK; Van Hook, HM; Xu, J, 2007
)
0.57
" All papers, abstracts, or presentations, regardless of study design, that made reference to the response of patients who were switched from one NNRTI to another as a result of an adverse drug reaction were included."( Is it safe to switch between efavirenz and nevirapine in the event of toxicity?
Maartens, G; Mehta, U, 2007
)
0.6
" Therefore, it is important to monitor adverse events from NVP, including liver function tests among HIV/AIDS patients with history of drug allergy, especially against sulfamethoxazole, and those concurrently treated with antituberculosis drugs."( Predisposing factors for nevirapine toxicity among AIDS patients with low baseline CD4 count.
Aung, SE; Kaewkungwal, J; Maek-a-nantawat, W; Phonrat, B; Pitisuttithum, P; Tansuphaswadikul, S,
)
0.43
"The aim of this article is to present the clinical characteristics and management of an oral adverse effect stemming from the use of the antiretroviral medication Nevirapine (NVP)."( Oral adverse effects due to the use of Nevirapine.
Fonseca, LM; Madureira, DF; Mesquita, RA; Moura, MD; Senna, MI, 2008
)
0.81
" From 1996 to 2002 several medications were changed due to their adverse effects: indinavir (renal colic and fever), nelfinavir (cutaneous rash), and efavirenz (nausea and temporary memory loss)."( Oral adverse effects due to the use of Nevirapine.
Fonseca, LM; Madureira, DF; Mesquita, RA; Moura, MD; Senna, MI, 2008
)
0.62
"Unfortunately, the clinical features of the oral adverse effect from NVP are not well known."( Oral adverse effects due to the use of Nevirapine.
Fonseca, LM; Madureira, DF; Mesquita, RA; Moura, MD; Senna, MI, 2008
)
0.62
"Transmission prophylaxis in offspring of HIV-positive mothers may give rise to adverse effects."( [Side effects of antiretroviral treatment for transmission prophylaxis in preterm and near-term infants].
Bauer, K; Dunsch, D; Haberl, A; Linde, R; Reitter, A; Schlösser, R, 2007
)
0.34
"HIV-infected women on selected ARV regimens or no ARV were administered DMPA 150 mg intramuscularly and evaluated for 12 weeks for adverse events, changes in CD4+ count and HIV RNA levels, and ovulation."( Safety and tolerability of depot medroxyprogesterone acetate among HIV-infected women on antiretroviral therapy: ACTG A5093.
Clax, PA; Cohn, SE; Hitti, J; Lertora, JJ; Muderspach, L; Park, JG; Stek, A; Watts, DH; Yu, S, 2008
)
0.35
" Nine Grade 3 or 4 adverse events occurred in seven subjects; none were judged related to DMPA."( Safety and tolerability of depot medroxyprogesterone acetate among HIV-infected women on antiretroviral therapy: ACTG A5093.
Clax, PA; Cohn, SE; Hitti, J; Lertora, JJ; Muderspach, L; Park, JG; Stek, A; Watts, DH; Yu, S, 2008
)
0.35
" The primary endpoint was any serious adverse event (SAE) definitely/probably or uncertain whether related to blinded nevirapine/abacavir."( Twenty-four-week safety and tolerability of nevirapine vs. abacavir in combination with zidovudine/lamivudine as first-line antiretroviral therapy: a randomized double-blind trial (NORA).
, 2008
)
0.82
"There was a trend towards a lower rate of serious adverse reactions in Ugandan adults with low CD4 starting ARV regimens with abacavir than with nevirapine."( Twenty-four-week safety and tolerability of nevirapine vs. abacavir in combination with zidovudine/lamivudine as first-line antiretroviral therapy: a randomized double-blind trial (NORA).
, 2008
)
0.81
"Nevirapine-based therapy is associated with increased frequency of adverse events among HIV-infected pregnant women."( Nevirapine-induced side effects in pregnant women: experience of a Brazilian university hospital.
Carraro, EA; Cornelsen, TC; Dias, JM; Kondo, W; Macedo, RL; Perini, J; Prandel, E; Sasaki, Md; Sbalquiero, R, 2007
)
3.23
" Symptoms disappeared after discontinuation of antiretroviral therapy and we suggest that syncope may be a side effect to one of the three antiretroviral drugs that has not been described previously."( Syncope as a probable side effect to combination antiretroviral therapy initiated during primary HIV-1 infection.
Larsen, CS; Lybaek, D, 2008
)
0.35
"To determine the incidence of clinically significant adverse events after long-term, fixed-dose, generic highly active antiretroviral therapy (HAART) use among HIV-infected individuals in South India, we examined the experiences of 3154 HIV-infected individuals who received a minimum of 3 months of generic HAART between February 1996 and December 2006 at a tertiary HIV care referral center in South India."( Spectrum of adverse events after generic HAART in southern Indian HIV-infected patients.
Balakrishnan, P; Cecelia, AJ; Devaleenal, B; Flanigan, TP; Kumarasamy, N; Lai, AR; Mayer, KH; Poongulali, S; Saghayam, S; Solomon, S; Venkatesh, KK; Yepthomi, T, 2008
)
0.35
"The aim of this study was to measure the cumulative incidence of adverse events (AEs) related to nevirapine in patients switched from efavirenz to immediate full-dose nevirapine (FDN)."( Efavirenz replacement by immediate full-dose nevirapine is safe in HIV-1-infected patients in Cambodia.
Chhneang, V; Fernandez, M; Laureillard, D; Moeung, S; Ngeth, C; Piketty, C; Prak, N; Quillet, C; Riel, V; Song, S, 2008
)
0.82
" However, while NVP is a safe treatment in immunocompromised patients, NVP-containing regimens have been associated with severe immune-mediated toxicities in non-HIV individuals."( Nevirapine toxicity in non-HIV cancer patients.
Barone, C; Cignarelli, M; De Vis, K; Fabiano, A; Fersini, A; Landriscina, M; Lombardi, V; Piscazzi, A; Santodirocco, M, 2008
)
1.79
" The incidence of adverse hepatic and/or cutaneous effects was determined and correlated to the CD4 cells count."( [Evaluation of the adverse effects of nevirapine in HIV-infected pregnant women in a South Brazilian University Hospital].
Astori, Ade A; Fernandes, Rde B; Gomes, Sel-K; Kondo, W; Sasaki, Md; Sbalqueiro, RL, 2008
)
0.62
" Baseline CD4 counts, viral loads and transaminases were similar in pregnant women with nevirapine adverse effects and those without reaction."( [Evaluation of the adverse effects of nevirapine in HIV-infected pregnant women in a South Brazilian University Hospital].
Astori, Ade A; Fernandes, Rde B; Gomes, Sel-K; Kondo, W; Sasaki, Md; Sbalqueiro, RL, 2008
)
0.84
"The incidence of adverse events with nevirapine in our study was high, but most of them were cutaneous."( [Evaluation of the adverse effects of nevirapine in HIV-infected pregnant women in a South Brazilian University Hospital].
Astori, Ade A; Fernandes, Rde B; Gomes, Sel-K; Kondo, W; Sasaki, Md; Sbalqueiro, RL, 2008
)
0.89
" Sources included adverse event reports from pharmaceutical manufacturers and the US FDA, reports from peer-reviewed journals/scientific meetings and the Research on Adverse Drug events And Reports (RADAR) project."( Hepatotoxicity associated with long- versus short-course HIV-prophylactic nevirapine use: a systematic review and meta-analysis from the Research on Adverse Drug events And Reports (RADAR) project.
Bennett, CL; Chandler, KL; Differding, V; Johnson, S; McKoy, JM; Obadina, E; Palella, F; Parada, JP; Raisch, DW; Scarsi, KK; Scheetz, MH; Sutton, S; Yarnold, PR, 2009
)
0.58
" Grade 3-4 adverse events occurred in 3 cases (2 peripheral neuropathy, and 1 suspected lactic acidosis)."( [Therapeutic effect and safety evaluation on 6-year highly active antiretroviral therapy for Chinese HIV-1 infected patients].
Chen, Z; Gong, G; He, Y; Liu, C; Liu, M; Yin, W; Zheng, Y; Zhou, H, 2009
)
0.35
"Antiretroviral therapy with NVP-based regimens is safe and effective by suppressing HIV viremia and producing continued CD4 cell increases in subjects with HIV or AIDS for 6 years."( [Therapeutic effect and safety evaluation on 6-year highly active antiretroviral therapy for Chinese HIV-1 infected patients].
Chen, Z; Gong, G; He, Y; Liu, C; Liu, M; Yin, W; Zheng, Y; Zhou, H, 2009
)
0.35
" Hepatitis C virus (HCV) coinfection, adverse events, and reasons for using nevirapine were also recorded."( Long-term effectiveness and safety outcomes in HIV-1-infected patients after a median time of 6 years on nevirapine.
Aguirrebengoa, K; Clotet, B; García, MA; Goikoetxea, J; Iribarren, JA; Martínez, E; Muñoz, J; Negredo, E; Perez-Alvarez, N; Portu, J; Rodríguez-Arrondo, F, 2009
)
0.8
"Nevirapine is widely used to treat HIV-1 infection to prevent mother-to-child transmission; unfortunately adverse drug reactions have been reported."( Nevirapine-induced hepatotoxicity and pharmacogenetics: a retrospective study in a population from Mozambique.
Altan, AM; Borgiani, P; Bramanti, P; Ceffa, S; Ciccacci, C; Marazzi, MC; Novelli, G; Palombi, L; Paturzo, G; Sirianni, E, 2010
)
3.25
"Patients from Mozambique, 78 with nevirapine-induced hepatotoxicity and 78 without adverse events, were genotyped for ABCB1, CYP2B6, CYP3A4 and CYP3A5 gene variants."( Nevirapine-induced hepatotoxicity and pharmacogenetics: a retrospective study in a population from Mozambique.
Altan, AM; Borgiani, P; Bramanti, P; Ceffa, S; Ciccacci, C; Marazzi, MC; Novelli, G; Palombi, L; Paturzo, G; Sirianni, E, 2010
)
2.08
"In AIDS Clinical Trials Group A5095, 9% of participants who experienced an adverse event related to efavirenz substituted nevirapine."( Substitution of nevirapine because of efavirenz toxicity in AIDS clinical trials group A5095.
Gulick, RM; Kmack, A; Krambrink, A; Kuritzkes, DR; Ribaudo, HJ; Schouten, JT; Shikuma, C; Webb, N, 2010
)
0.91
"To investigate uptake and provision of antenatal care (ANC) services in the Uzazi Bora project: a demonstration-intervention project for Safe Motherhood and prevention of mother-to-child transmission of HIV in Kenya."( A Safe Motherhood project in Kenya: assessment of antenatal attendance, service provision and implications for PMTCT.
Chersich, MF; Delva, W; Luchters, S; Muigai, E; Oyier, V; Temmerman, M; Yard, E, 2010
)
0.36
" However, reports of severe NVP-induced hepatotoxicity and serious adverse cutaneous effects have raised concerns about its use."( Amino acid adduct formation by the nevirapine metabolite, 12-hydroxynevirapine--a possible factor in nevirapine toxicity.
Antunes, AM; Beland, FA; Godinho, AL; Justino, GC; Marques, MM; Martins, IL, 2010
)
0.64
"The chewable FDC was safe and provided therapeutically adequate plasma drug exposures in human immunodeficiency virus-infected children."( A chewable pediatric fixed-dose combination tablet of stavudine, lamivudine, and nevirapine: pharmacokinetics and safety compared with the individual liquid formulations in human immunodeficiency virus-infected children in Thailand.
Capparelli, E; Chokephaibulkit, K; Chotpitayasunondh, T; Cressey, TR; Eksaengsri, A; Hongsiriwan, S; McIntosh, K; Muresan, P; Plipat, N; Prasitsuebsai, W; Sirisanthana, V; Smith, ME; Toye, M; Vanprapar, N; Yogev, R, 2010
)
0.59
"In resource-limited settings where nevirapine-containing regimen is the preferred regimen in women, data on severe adverse events (SAEs) according to CD4 cell count are limited."( Incidence and risk factors of severe adverse events with nevirapine-based antiretroviral therapy in HIV-infected women. MTCT-Plus program, Abidjan, Côte d'Ivoire.
Abrams, EJ; Amani-Bosse, C; Bédikou, G; Coffie, PA; Dabis, F; Ekouevi, DK; Tanon, AK; Tonwe-Gold, B, 2010
)
0.88
" Despite its clinical efficacy, NVP administration is associated with a variety of toxic responses that include hepatotoxicity and skin rash."( Protein adducts as prospective biomarkers of nevirapine toxicity.
Antunes, AM; Beland, FA; Coelho, AV; Godinho, AL; Gomes, RA; Marques, MM; Martins, IL; Oliveira, MC, 2010
)
0.62
"Predictors of adverse events (AE) associated with nevirapine use are needed to better understand reports of severe rash or liver enzyme elevation (LEE) in HIV+ women."( Adverse events in a cohort of HIV infected pregnant and non-pregnant women treated with nevirapine versus non-nevirapine antiretroviral medication.
Aaron, E; Bachmann, LH; Criniti, S; Gracely, E; Kempf, MC; Kumar, R; Tedaldi, E; Warriner, A, 2010
)
0.84
" We analyzed patients' age, gender, HIV transmission route, HIV disease stage, pregnancy, alcohol intake, adverse events, coinfection with hepatitis B or C virus, time until toxicity, and withdrawal rates."( Nevirapine-associated toxicity in clinical practice in Buenos Aires, Argentina.
Antonelli, L; Bottaro, EG; Cassetti, LI; Errea, S; Huberman, MJ; Iannella, Mdel C; Scapellato, PG; Vesperoni, FA,
)
1.57
" Rash was the most frequently observed adverse event; it was more frequent in women."( Nevirapine-associated toxicity in clinical practice in Buenos Aires, Argentina.
Antonelli, L; Bottaro, EG; Cassetti, LI; Errea, S; Huberman, MJ; Iannella, Mdel C; Scapellato, PG; Vesperoni, FA,
)
1.57
" Multivariate analyses were performed to compare, between the ddI and ZDV groups, the proportion of patients with a viral load <500 copies/ml during follow-up; the increase in the CD4 cell count; survival; treatment changes and severe adverse events."( Long-term effectiveness and safety of didanosine combined with lamivudine and efavirenz or nevirapine in antiretroviral-naive patients: a 9-year cohort study in Senegal.
Delaporte, E; Diouf, A; Etard, JF; Girard, PM; Landman, R; Laurent, C; Molinari, N; Ndoye, I; Ngom Guèye, NF; Sow, PS; Tchatchueng Mbougua, JB, 2011
)
0.59
"There are few studies from India documenting the adverse effects of generic HAART (Highly Active Anti-retroviral Therapy)."( Adverse effects after HAART Initiation in resource-limited settings: a prospective study from Mysore, India.
Dasegowda, V; Sreenivasan, S, 2010
)
0.36
"A prospective study was conducted at Mysore, India, to study the adverse effects after HAART initiation in a cohort of 100 antiretroviral therapy (ART)-naive patients, who were evaluated prospectively every three months by clinical and laboratory monitoring for adverse effects after HAART initiation for one year."( Adverse effects after HAART Initiation in resource-limited settings: a prospective study from Mysore, India.
Dasegowda, V; Sreenivasan, S, 2010
)
0.36
" The most common reasons for modifying therapy were development of an adverse effect (eight cases; 57."( Adverse effects after HAART Initiation in resource-limited settings: a prospective study from Mysore, India.
Dasegowda, V; Sreenivasan, S, 2010
)
0.36
"A significant proportion of patients had adverse effects of a lower grade severity after HAART."( Adverse effects after HAART Initiation in resource-limited settings: a prospective study from Mysore, India.
Dasegowda, V; Sreenivasan, S, 2010
)
0.36
" We characterized relationships between nevirapine-associated cutaneous and hepatic adverse events and genetic variants among HIV-infected adults."( Toxicogenomics of nevirapine-associated cutaneous and hepatic adverse events among populations of African, Asian, and European descent.
Cammett, AM; Distel, M; Guo, S; Haas, DW; Hall, D; Huang, Z; Jayadev, S; Mootsikapun, P; Podzamczer, D; Ruxrungtham, K; Storfer, S; Yuan, J, 2011
)
0.97
" Cases experienced symptomatic nevirapine-associated severe (grade III/IV) cutaneous and/or hepatic adverse events within 8 weeks of initiating nevirapine."( Toxicogenomics of nevirapine-associated cutaneous and hepatic adverse events among populations of African, Asian, and European descent.
Cammett, AM; Distel, M; Guo, S; Haas, DW; Hall, D; Huang, Z; Jayadev, S; Mootsikapun, P; Podzamczer, D; Ruxrungtham, K; Storfer, S; Yuan, J, 2011
)
0.99
"We studied 276 evaluable cases (175 cutaneous adverse events, 101 hepatic adverse events) and 587 controls."( Toxicogenomics of nevirapine-associated cutaneous and hepatic adverse events among populations of African, Asian, and European descent.
Cammett, AM; Distel, M; Guo, S; Haas, DW; Hall, D; Huang, Z; Jayadev, S; Mootsikapun, P; Podzamczer, D; Ruxrungtham, K; Storfer, S; Yuan, J, 2011
)
0.7
"Among patients with at least 150 CD4 T cells/μl, polymorphisms in drug metabolism and immune response pathways were associated with greater likelihood of risk for nevirapine-related adverse events."( Toxicogenomics of nevirapine-associated cutaneous and hepatic adverse events among populations of African, Asian, and European descent.
Cammett, AM; Distel, M; Guo, S; Haas, DW; Hall, D; Huang, Z; Jayadev, S; Mootsikapun, P; Podzamczer, D; Ruxrungtham, K; Storfer, S; Yuan, J, 2011
)
0.9
" Ten percent (13/123) of the subjects discontinued the treatment due to adverse events."( Evaluation of the safety and effectiveness of nevirapine plus coformulated tenofovir/emtricitabine as first-line therapy in routine clinical practice.
Blanch, J; Cervantes, M; Domingo, P; Ferrer, E; Knobel, H; Llibre, JM; Mallolas, J; Pedrol, E; Vallecillo, G, 2012
)
0.64
" The safety profile of NVP XR was similar to NVP IR, but showed numerically fewer treatment-related adverse events."( Efficacy and safety of nevirapine extended-release once daily versus nevirapine immediate-release twice-daily in treatment-naive HIV-1-infected patients.
Andrade-Villanueva, J; Bogner, J; Cahn, P; Drulak, M; Gathe, J; Horban, A; Nelson, M; Nguyen, T; Podzamczer, D; Quinson, AM; Santiago, S; Spencer, D; Yong, CL; Zhang, W, 2011
)
0.68
"NVP XR in combination with TDF and emtricitabine was shown to be non-inferior in efficacy to NVP IR with a similar safety and adverse event profile, with the potential for the added convenience of once-daily dosing."( Efficacy and safety of nevirapine extended-release once daily versus nevirapine immediate-release twice-daily in treatment-naive HIV-1-infected patients.
Andrade-Villanueva, J; Bogner, J; Cahn, P; Drulak, M; Gathe, J; Horban, A; Nelson, M; Nguyen, T; Podzamczer, D; Quinson, AM; Santiago, S; Spencer, D; Yong, CL; Zhang, W, 2011
)
0.68
" Similarly, the proportion of serious adverse events in the HIVIGLOB/sdNVP and sdNVP arms, respectively, for mothers (18."( Safety and efficacy of HIV hyperimmune globulin for prevention of mother-to-child HIV transmission in HIV-1-infected pregnant women and their infants in Kampala, Uganda (HIVIGLOB/NVP STUDY).
Antelman, G; Falksveden, L; Fowler, MG; Guay, L; Jackson, JB; Mmiro, F; Moulton, LH; Mubiru, M; Musoke, P; Nakabiito, C; Omer, SB; Onyango-Makumbi, C; Wahren, B; Wigzell, H; Zwerski, S, 2011
)
0.37
"Giving mother-infant pairs an infusion of peripartum HIV hyperimmune globulin in addition to sdNVP for preventing maternal-to-child transmission was as safe as sdNVP alone but was no more effective than sdNVP alone in preventing HIV transmission."( Safety and efficacy of HIV hyperimmune globulin for prevention of mother-to-child HIV transmission in HIV-1-infected pregnant women and their infants in Kampala, Uganda (HIVIGLOB/NVP STUDY).
Antelman, G; Falksveden, L; Fowler, MG; Guay, L; Jackson, JB; Mmiro, F; Moulton, LH; Mubiru, M; Musoke, P; Nakabiito, C; Omer, SB; Onyango-Makumbi, C; Wahren, B; Wigzell, H; Zwerski, S, 2011
)
0.37
" Primary outcome was a composite of death, virological failure, default, or serious adverse event (SAE) at 24 weeks."( Efficacy and safety of once-daily nevirapine- or efavirenz-based antiretroviral therapy in HIV-associated tuberculosis: a randomized clinical trial.
Bhavani, PK; Dilip, M; Iliayas, S; Menon, PA; Narendran, G; Padmapriyadarsini, C; Ponnuraja, C; Pooranagangadevi, NP; Ramachandran, R; Ramesh Kumar, S; Selvaraju, S; Swaminathan, S; Venkatesan, P, 2011
)
0.65
" Frequency of adverse events (AEs) was similar between arms, with 88."( A randomised comparison of safety and efficacy of nevirapine vs. atazanavir/ritonavir combined with tenofovir/emtricitabine in treatment-naïve patients.
Bhatti, L; Conner, C; Dejesus, E; Mills, A; Storfer, S, 2011
)
0.62
" Adverse events (AEs) were recorded."( Twenty-four-week efficacy and safety of switching virologically suppressed HIV-1-infected patients from nevirapine immediate release 200 mg twice daily to nevirapine extended release 400 mg once daily (TRANxITION).
Arasteh, K; Cordes, C; Guo, J; Livrozet, JM; Orkin, C; Plettenberg, A; Quinson, A; Robinson, P; Wang, E; Ward, D; Yong, CL, 2012
)
0.59
" The primary efficacy endpoint was HIV-1 infection in infants at 6 months and safety endpoints were adverse reactions in both groups."( Efficacy and safety of an extended nevirapine regimen in infant children of breastfeeding mothers with HIV-1 infection for prevention of postnatal HIV-1 transmission (HPTN 046): a randomised, double-blind, placebo-controlled trial.
Andrew, P; Brown, ER; Chetty, V; Chipato, T; Coovadia, HM; Eshleman, SH; Fawzi, W; Fowler, MG; George, K; Guay, L; Kisenge, R; Lynn, DJ; Maldonado, Y; Manji, K; Mofenson, LM; Moodley, D; Msweli, L; Musoke, P; Mwatha, A; Nakabiito, C; Richardson, P; Stranix-Chibanda, L; Zwerski, S, 2012
)
0.66
" 125 (16%) of 758 infants given extended nevirapine and 116 (15%) of 761 controls had serious adverse events, but frequency of adverse events, serious adverse events, and deaths did not differ significantly between treatment groups."( Efficacy and safety of an extended nevirapine regimen in infant children of breastfeeding mothers with HIV-1 infection for prevention of postnatal HIV-1 transmission (HPTN 046): a randomised, double-blind, placebo-controlled trial.
Andrew, P; Brown, ER; Chetty, V; Chipato, T; Coovadia, HM; Eshleman, SH; Fawzi, W; Fowler, MG; George, K; Guay, L; Kisenge, R; Lynn, DJ; Maldonado, Y; Manji, K; Mofenson, LM; Moodley, D; Msweli, L; Musoke, P; Mwatha, A; Nakabiito, C; Richardson, P; Stranix-Chibanda, L; Zwerski, S, 2012
)
0.92
" The ultimate goal is to develop diagnostic methods for predicting the onset of nevirapine-induced toxic reactions."( Evidence for nevirapine bioactivation in man: searching for the first step in the mechanism of nevirapine toxicity.
Antunes, AM; Branco, T; Caixas, U; Godinho, AL; Grilo, NM; Marinho, AT; Marques, MM; Monteiro, EC; Oliveira, MC; Pereira, SA, 2012
)
0.98
"We compared adverse events among breast-feeding neonates born to Kenyan mothers receiving triple-antiretroviral therapy, including either nevirapine or nelfinavir."( Rash, hepatotoxicity and hyperbilirubinemia among Kenyan infants born to HIV-infected women receiving triple-antiretroviral drugs for the prevention of mother-to-child HIV transmission.
Akoth, B; Angira, F; Masaba, R; Mills, LA; Minniear, TD; Ndivo, R; Oyaro, B; Peters, PJ; Polle, N; Thomas, TK; Zeh, C, 2012
)
0.58
"Hepatotoxicity was a common adverse effect of NVP among men and women with CD4 >250 cells per microliter."( The interaction of CD4 T-cell count and nevirapine hepatotoxicity in China: a change in national treatment guidelines may be warranted.
Ghanem, KG; Guo, F; Han, Y; Li, T; Li, Y; Qiu, Z; Wang, H; Wang, W; Xie, J; Zhang, C; Zhou, M, 2013
)
0.66
"The risk of adverse drug events associated with nevirapine (NVP) is suggested to be greater in pregnant women."( Adverse events associated with nevirapine use in pregnancy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Shubber, Z, 2013
)
0.93
"We searched six databases for studies reporting adverse events among HIV-positive pregnant women who had received NVP-based antiretroviral therapy for at least 7 days."( Adverse events associated with nevirapine use in pregnancy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Shubber, Z, 2013
)
0.68
"3%) of patients discontinued NVP due to an adverse event."( Adverse events associated with nevirapine use in pregnancy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Shubber, Z, 2013
)
0.68
"These results suggest that the frequency of adverse events associated with NVP use in pregnant women, although high, is no higher than reported for NVP in the general adult population."( Adverse events associated with nevirapine use in pregnancy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Shubber, Z, 2013
)
0.68
"We systematically reviewed adverse events among treatment-naive HIV-positive adults and children receiving either NVP or EFV as part of first-line antiretroviral therapy."( Adverse events associated with nevirapine and efavirenz-based first-line antiretroviral therapy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Renaud-Théry, F; Shaffer, N; Shubber, Z; Vitoria, M, 2013
)
0.68
"Compared to NVP, EFV is associated with a lower frequency of severe adverse events, in particular treatment discontinuations."( Adverse events associated with nevirapine and efavirenz-based first-line antiretroviral therapy: a systematic review and meta-analysis.
Andrieux-Meyer, I; Calmy, A; Ford, N; Hargreaves, S; Mills, EJ; Renaud-Théry, F; Shaffer, N; Shubber, Z; Vitoria, M, 2013
)
0.68
" Pressure of work and insufficient perceived benefit of side-effect recording are suspected causes."( Underreporting of side effects of standard first-line ART in the routine setting in Blantyre, Malawi.
Lungu, M; Mathews, T; Tapsfield, J; van Oosterhout, JJ, 2011
)
0.37
"Nevirapine (NVP) is a non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV infections and has been reported to be toxic to the male reproductive system."( Nevirapine induces testicular toxicity in Wistar rats: reversal effect of kolaviron (biflavonoid from Garcinia kola seeds).
Adaramoye, OA; Akanni, OO; Farombi, EO, 2013
)
3.28
" In contrast, NVP-2T did not produce an adverse effect on the biochemical indices studied in testes and sperm of rats."( Nevirapine induces testicular toxicity in Wistar rats: reversal effect of kolaviron (biflavonoid from Garcinia kola seeds).
Adaramoye, OA; Akanni, OO; Farombi, EO, 2013
)
1.83
"Taken together, KV reversed the adverse effects of NVP-4T on testicular antioxidant enzymes and markers of oxidative stress in the rats."( Nevirapine induces testicular toxicity in Wistar rats: reversal effect of kolaviron (biflavonoid from Garcinia kola seeds).
Adaramoye, OA; Akanni, OO; Farombi, EO, 2013
)
1.83
" There were no differences in adverse events between study arms."( Efficacy and safety of an extended nevirapine regimen in infants of breastfeeding mothers with HIV-1 infection for prevention of HIV-1 transmission (HPTN 046): 18-month results of a randomized, double-blind, placebo-controlled trial.
Aizire, J; Allen, M; Andrew, P; Brown, E; Chetty, V; Chipato, T; Coovadia, H; Eshleman, SH; Fawzi, W; Fowler, MG; George, K; Herron, CM; Jackson, JB; Kisenge, R; Maldonado, Y; Manji, K; Mofenson, LM; Moodley, D; Msweli, L; Musoke, P; Mwatha, A; Richardson, P; Stranix-Chibanda, L; Zwerski, S, 2014
)
0.68
" 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
)
0.4
" Both ACT regimens were safe and well tolerated."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
"Treatment of uncomplicated malaria with AL or DP was efficacious and safe in HIV-infected children taking ART."( Artemisinin-based combination therapies are efficacious and safe for treatment of uncomplicated malaria in HIV-infected Ugandan children.
Achan, J; Arinaitwe, E; Charlebois, E; Clark, TD; Dorsey, G; Havlir, D; Ikilezi, G; Kakuru, A; Kamya, MR; Muhindo, MK; Mwangwa, F; Rosenthal, PJ; Ruel, T; Tappero, JW, 2014
)
0.4
" Hepatotoxicity was rated according to the AIDS Table for Grading the Severity of Adult and Pediatric Adverse Events (DAIDS)."( [Hepatotoxicity in healthy infants exposed to nevirapine during pregnancy].
Figueras-Nadal, C; Fortuny-Guasch, C; Iveli, P; Martín-Nalda, A; Noguera-Julian, A; Rovira-Girabal, N; Soler-Palacín, P, 2016
)
0.69
" We investigated the frequency and severity of adverse events (AE) in infants receiving multiple drug prophylaxis compared to ZDV alone."( Serious adverse events are uncommon with combination neonatal antiretroviral prophylaxis: a retrospective case review.
Barr, E; Davies, J; Forster, JE; Kinzie, K; Levin, MJ; McFarland, EJ; Pappas, J; Paul, S; Smith, C; Weinberg, A, 2015
)
0.42
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
" The aim of this study was to compare the rate of any discontinuation of antiretroviral (ARV) regimen because of virologic failure (VF), and/or adverse drug reaction (ADR) among patients receiving stable ARV regimens for at least 6 months."( Long-term efficacy and toxicity of abacavir/lamivudine/nevirapine compared to the most prescribed ARV regimens before 2013 in a French Nationwide Cohort Study.
Bani-Sadr, F; Cabie, A; Cotte, L; de Boissieu, P; Delobel, P; Dramé, M; Garraffo, R; Huleux, T; Poizot-Martin, I; Raffi, F; Rey, D, 2016
)
0.68
" The most common adverse events potentially attributable to combination antiretroviral therapy were transient asymptomatic hyperlactatemia (26%), anemia (24."( Nevirapine Pharmacokinetics and Safety in Neonates Receiving Combination Antiretroviral Therapy for Prevention of Vertical HIV Transmission.
Bitnun, A; Brophy, J; Campbell, DM; Colantonio, D; Kakkar, F; Lau, E; Murphy, K; Read, SE; Samson, L; Seto, W; Yudin, MH, 2017
)
1.9
" Secondary endpoints were time to loss of virological response and adverse events."( Efficacy and safety of switching from nevirapine immediate-release twice daily to nevirapine extended-release once daily in virologically suppressed HIV-infected patients: a retrospective cohort study in Taiwan.
Chang, HM; Chen, YS; Kunin, CM; Lee, CY; Lee, SS; Tsai, HC, 2017
)
0.73
" Furthermore, there were no significant differences in adverse events between these two groups."( Efficacy and safety of switching from nevirapine immediate-release twice daily to nevirapine extended-release once daily in virologically suppressed HIV-infected patients: a retrospective cohort study in Taiwan.
Chang, HM; Chen, YS; Kunin, CM; Lee, CY; Lee, SS; Tsai, HC, 2017
)
0.73
" The form is designed to obtain information on the demographics of the patients, WHO clinical stage of their HIV infection, HAART regimen for the patients, and suspected adverse events associated with the antiretroviral drugs used by the patients."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
" About half (57%) of the participants reported clinical adverse events; 92% of which were reported within two weeks of HAART initiation."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
"Antiretroviral drugs exposure often presents with adverse events, an observation similar to other studies."( A prospective study of adverse events to antiretroviral therapy in HIV- infected adults in Ekiti State, Nigeria.
Awodele, O; Oshikoya, KA; Popoola, TD, 2016
)
0.43
"Our findings suggest that ART drugs are not associated with an increased risk of CMs, yet some may increase adverse birth events."( Comparative safety and effectiveness of perinatal antiretroviral therapies for HIV-infected women and their children: Systematic review and network meta-analysis including different study designs.
Antony, J; Ashoor, HM; Blondal, E; Finkelstein, Y; Ghassemi, M; Gough, K; Hemmelgarn, BR; Hutton, B; Ivory, JD; Khan, PA; Lillie, E; Straus, SE; Tricco, AC; Vafaei, A; Veroniki, AA, 2018
)
0.48
" This antiretroviral is one of the scarce examples of drugs with prescription criteria based on sex, in order to prevent adverse reactions."( Singularities of nevirapine metabolism: from sex-dependent differences to idiosyncratic toxicity.
Antunes, AMM; Caixas, U; Charneira, C; Gonçalves-Dias, C; Marinho, AT; Marques, MM; Miranda, JP; Monteiro, EC; Pereira, SA, 2019
)
0.85
" We evaluated the adverse events associated with the use of zidovudine (ZDV)/lamivudine (3TC)/nevirapine (NVP) for neonatal PEP during the first 6 weeks of life."( Safety of 6-week Neonatal Triple-combination Antiretroviral Postexposure Prophylaxis in High-risk HIV-exposed Infants.
Anugulruengkitt, S; Chokephaibulkit, K; Cressey, TR; Jantarabenjakul, W; Ounchanum, P; Pancharoen, C; Punnahitanon, S; Puthanakit, T; Sophonphan, J; Srirompotong, U; Suntarattiwong, P, 2019
)
0.73
" They received a directly-observed 3-day standard treatment of DPQ and were followed up until day 63 for malaria infection and adverse events."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.51
"DPQ was highly efficacious and safe for the treatment of malaria in HIV-infected patients concurrently taking efavirenz- or nevirapine-based ART, despite known pharmacokinetic interactions between dihydroartemisinin-piperaquine and efavirenz- or nevirapine-based ART regimens."( Efficacy and safety of dihydroartemisinin-piperaquine for treatment of Plasmodium falciparum uncomplicated malaria in adult patients on antiretroviral therapy in Malawi and Mozambique: an open label non-randomized interventional trial.
Banda, CG; Kalilani-Phiri, L; Khoo, SH; Lalloo, DG; Macuacua, S; Maculuve, S; Mallewa, J; Mukaka, M; Mwapasa, V; Piqueras, M; Sevene, E; Terlouw, DJ; Vala, A, 2019
)
0.72
"NVP/ZDV/3TC started in the first week of life was safe and effective, even when trough NVP levels were below target."( Safety and Efficacy of Starting Antiretroviral Therapy in the First Week of Life.
Ajibola, G; Batlang, O; Bennett, K; Capparelli, EV; Hughes, MD; Jean-Philippe, P; Kuritzkes, DR; Lichterfeld, M; Lockman, S; Makhema, J; Maswabi, K; Mohammed, T; Moyo, S; Sakoi, M; Shapiro, RL, 2021
)
0.62
" There were no clinically relevant toxicities nor adverse events in both control and test arms."( Effect of nevirapine, efavirenz and lopinavir/ritonavir on the therapeutic concentration and toxicity of lumefantrine in people living with HIV at Lagos University Teaching Hospital, Nigeria.
Abideen, G; Adeniji, H; Adeuja, O; Agbaje, EO; Akanmu, AS; Akinleye, MO; Akinyede, AA; Busari, AW; Hassan, OO; Ken-Owotor, C; Kogbe, S; Ogunfowokan, T; Onwujuobi, AG; Oreagba, IA; Owolabi, ET; Usman, SO, 2020
)
0.96
" DAIDS grade 3 or 4 adverse events at least possibly related to antiretrovirals occurred in 30 (7%, 95% CI 5-10) of 438 infants but did not lead to nevirapine cessation in any neonates; neutropenia (25 [6%] neonates) and anaemia (six [1%]) were most common."( Pharmacokinetics and safety of early nevirapine-based antiretroviral therapy for neonates at high risk for perinatal HIV infection: a phase 1/2 proof of concept study.
Bryson, Y; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Coletti, A; Cotton, MF; Hazra, R; Jean-Philippe, P; LeBlanc, R; Mirochnick, M; Naidoo, KL; Nelson, BS; Persaud, D; Reding, C; Ruel, TD; Spector, SA; Tierney, C; Zimmer, B, 2021
)
1.09
"Nevirapine at the dose studied was confirmed to be safe and provides therapeutic exposure concentrations."( Pharmacokinetics and safety of early nevirapine-based antiretroviral therapy for neonates at high risk for perinatal HIV infection: a phase 1/2 proof of concept study.
Bryson, Y; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Coletti, A; Cotton, MF; Hazra, R; Jean-Philippe, P; LeBlanc, R; Mirochnick, M; Naidoo, KL; Nelson, BS; Persaud, D; Reding, C; Ruel, TD; Spector, SA; Tierney, C; Zimmer, B, 2021
)
2.34

Pharmacokinetics

The aim of this 2NN pharmacokinetic substudy was to investigate the population pharmacokinetics of nevirapine and efavirenz. Nevirapine significantly reduced median indinavir Cmin (47.5 mg/kg) Here we aimed to quantify nevirabine and LPV/r drug-drug interaction effects on bedaquiline and M2.

ExcerptReferenceRelevance
" The terminal half-life and mean residence time exceeded 24 h in all but one subject, indicating a prolonged disposition time in this population."( Pharmacokinetics of nevirapine: initial single-rising-dose study in humans.
Andrews, C; Bova, CA; Cheeseman, SH; Hattox, SE; Keirns, JJ; Koup, RA; McLaughlin, MM; Pav, JW; Roy, T; Sullivan, JL, 1993
)
0.61
" Nevirapine significantly reduced median indinavir Cmin (47."( Antiviral effect and pharmacokinetic interaction between nevirapine and indinavir in persons infected with human immunodeficiency virus type 1.
Dusek, A; Hall, DB; Lamson, M; Murphy, RL; Myers, M; Sommadossi, JP, 1999
)
1.46
" The median half-life in women was 61."( A phase I/II study of the safety and pharmacokinetics of nevirapine in HIV-1-infected pregnant Ugandan women and their neonates (HIVNET 006).
Allen, M; Bagenda, D; Dransfield, K; Elliott, T; Fleming, T; Fowler, MG; Guay, LA; Hom, D; Horton, S; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, L; Murarka, A; Musoke, P; Nakabiito, C; Pav, JW, 1999
)
0.55
" Overall, comparison of the pharmacokinetic parameters between the 50 and 200 mg doses indicates that nevirapine is well absorbed at clinically relevant doses."( Single dose pharmacokinetics and bioavailability of nevirapine in healthy volunteers.
Cappola, M; Hawi, A; Lamson, MJ; MacGregor, TR; Pav, JW; Robinson, P; Rowland, L; Sabo, JP, 1999
)
0.77
"The dNN study evaluated the safety, efficacy and pharmacokinetic interactions of the combination of stavudine (2',3'-didehydro-2',3'-dideoxythymidine; D4T), nelfinavir and nevirapine in 25 HIV-infected subjects who received treatment for up to 29 weeks."( dNN study: stavudine, nelfinavir and nevirapine. Preliminary safety, activity and pharmacokinetic interactions.
Skowron, G, 1998
)
0.77
" Non-compartmental methods were used to calculate the area under the plasma concentration versus time curve (AUC[24h]), and the maximal (Cmax) and minimal plasma concentration (Cmin), the time to Cmax (t(max)), the plasma elimination half-life (t1/2), the apparent oral clearance (Cl/F) and the apparent volume of distribution (V/F)."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.58
" However, Cmax and Cmin were higher and lower, respectively, when nevirapine was used in the once daily regimen as compared with the twice daily regimen."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.82
" However, Cmax and Cmin are higher and lower, respectively, for the once daily regimen as compared with the twice daily regimen."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.58
" The differences between the pharmacokinetic parameters of efavirenz with and without nevirapine were analyzed, and the pharmacokinetics of nevirapine were compared with those in historical control patients."( The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons.
Beijnen, JH; Carlier, H; Gazzard, B; Harris, M; Hoetelmans, RM; Johnson, M; Kwakkelstein, MO; Lange, JM; Montaner, JS; Moyle, G; Reiss, P; van Leeuwen, R; Veldkamp, AI; Youle, M, 2001
)
0.79
" Initial dose pharmacokinetic profiles in the pregnant women were similar to those seen in nonpregnant adults."( Nevirapine pharmacokinetics in pregnant women and in their infants after in utero exposure.
Fenton, T; Lugo, M; Mirochnick, M; Siminski, S; Sullivan, JL, 2001
)
1.75
" Although possessing a common mechanism of action, these agents can be differentiated by both molecular and pharmacokinetic characteristics."( Clinical pharmacokinetics of non-nucleoside reverse transcriptase inhibitors.
DiCenzo, R; Morse, GD; Smith, PF, 2001
)
0.31
" This pharmacokinetic interaction study was nested within a larger Phase III clinical trial conducted to characterize the safety and efficacy of coadministered nevirapine and lamivudine."( Pharmacokinetics of nevirapine and lamivudine in patients with HIV-1 infection.
Lamson, MJ; Leitz, G; MacGregor, TR; Sabo, JP; Yong, CL, 2000
)
0.83
"Concomitant administration of NVP at steady state with EE/NET resulted in a significant (29%) median reduction in the area under the plasma concentration time curve (AUC(infinity)) and a significant reduction in mean residence time (MRT) and half-life (t(1/2)) of EE."( Pharmacokinetic interaction between nevirapine and ethinyl estradiol/norethindrone when administered concurrently to HIV-infected women.
Hutman, HW; Lamson, M; Marshak, A; McDonough, M; Mildvan, D; Robinson, P; Yarrish, R, 2002
)
0.59
" Population pharmacokinetic parameters (apparent clearance (CL/F), volume of distribution (V/F), absorption rate constant (k a)) were estimated, as were interindividual, interoccasion, and residual variability in the pharmacokinetics."( Population pharmacokinetics of nevirapine in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; de Maat, MM; Huitema, AD; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2002
)
0.6
"From 173 outpatients a total number of 757 nevirapine plasma concentrations at a single random time point and full pharmacokinetic curves for 13 patients were available resulting in a database of 1329 nevirapine plasma concentrations."( Population pharmacokinetics of nevirapine in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; de Maat, MM; Huitema, AD; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2002
)
0.86
"The pharmacokinetics of nevirapine were adequately described by our population pharmacokinetic model."( Population pharmacokinetics of nevirapine in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; de Maat, MM; Huitema, AD; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2002
)
0.91
" The objective of this study was to assess the impact of body weight on the pharmacokinetic disposition of nelfinavir (NFV) in the absence and presence of nevirapine (NVP) and compare the pharmacokinetic profiles of twice-daily (BID) and three-times-daily (TID) NFV regimens."( Nelfinavir pharmacokinetics in stable human immunodeficiency virus-positive children: Pediatric AIDS Clinical Trials Group Protocol 377.
Aweeka, FT; Floren, LC; Hayashi, S; Jayewardene, A; Johnson, G; Krogstad, P; Nachman, S; Stanley, K; Wiznia, A, 2003
)
0.52
"This was an intensive pharmacokinetic substudy nested in a phase II, multicenter, randomized, open-label trial."( Nelfinavir pharmacokinetics in stable human immunodeficiency virus-positive children: Pediatric AIDS Clinical Trials Group Protocol 377.
Aweeka, FT; Floren, LC; Hayashi, S; Jayewardene, A; Johnson, G; Krogstad, P; Nachman, S; Stanley, K; Wiznia, A, 2003
)
0.32
"Evaluate pharmacokinetic interaction, short-term safety, and antiretroviral activity of stavudine (d4T), nevirapine (NVP), and nelfinavir (NFV) as combination HIV-1 therapy."( Pharmacokinetic evaluation and short-term activity of stavudine, nevirapine, and nelfinavir therapy in HIV-1-infected adults.
Fisher, A; Grosso, R; Hall, DB; Jacobs, M; Kerr, B; Leoung, G; Lewis, R; MacGregor, T; Odgen, R; Robinson, P; Skowron, G; Stevens, M; Yen-Lieberman, B, 2004
)
0.78
"Prospective, open-label study investigating the pharmacokinetic interactions between d4T, NVP, and NFV and documenting short-term tolerability and virologic and immunologic activity."( Pharmacokinetic evaluation and short-term activity of stavudine, nevirapine, and nelfinavir therapy in HIV-1-infected adults.
Fisher, A; Grosso, R; Hall, DB; Jacobs, M; Kerr, B; Leoung, G; Lewis, R; MacGregor, T; Odgen, R; Robinson, P; Skowron, G; Stevens, M; Yen-Lieberman, B, 2004
)
0.56
" Steady-state pharmacokinetic parameters of NFV, AG1402 (metabolite of NFV), and d4T were compared before and after the addition of NVP."( Pharmacokinetic evaluation and short-term activity of stavudine, nevirapine, and nelfinavir therapy in HIV-1-infected adults.
Fisher, A; Grosso, R; Hall, DB; Jacobs, M; Kerr, B; Leoung, G; Lewis, R; MacGregor, T; Odgen, R; Robinson, P; Skowron, G; Stevens, M; Yen-Lieberman, B, 2004
)
0.56
"NVP administration did not significantly affect the steady-state pharmacokinetic parameters of NFV or d4T."( Pharmacokinetic evaluation and short-term activity of stavudine, nevirapine, and nelfinavir therapy in HIV-1-infected adults.
Fisher, A; Grosso, R; Hall, DB; Jacobs, M; Kerr, B; Leoung, G; Lewis, R; MacGregor, T; Odgen, R; Robinson, P; Skowron, G; Stevens, M; Yen-Lieberman, B, 2004
)
0.56
"The prolonged elimination half-life of NVP compared with NRTIs, which persists even after 20 weeks of therapy, raises concern over the development of NNRTI resistance if all three drugs are stopped together."( Clinical implications of stopping nevirapine-based antiretroviral therapy: relative pharmacokinetics and avoidance of drug resistance.
Back, D; Clarke, JR; Fidler, S; Mackie, NE; Tamm, N; Taylor, GP; Weber, JN, 2004
)
0.6
" Population pharmacokinetic parameters [clearance (CL/F), volume of distribution (V/F), absorption rate constant (ka)] and interindividual (IIV) and interoccasion variability (IOV) were estimated."( Race is not associated with nevirapine pharmacokinetics.
Beijnen, JH; de Maat, MM; Huitema, AD; Mulder, JW; Nellen, JF; Prins, JM; Wit, FW, 2004
)
0.62
"The aim of this 2NN pharmacokinetic substudy was to investigate the population pharmacokinetics of nevirapine and efavirenz."( Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, J; MacGregor, TR; van Leth, F, 2005
)
1.99
"We have investigated the pharmacokinetics of nevirapine and paclitaxel in a patient who used both drugs concomitantly, as there are strong theoretical indications for a potential pharmacokinetic drug-drug interaction."( No pharmacokinetic drug-drug interaction between nevirapine and paclitaxel.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Schellens, JH, 2005
)
0.84
" Intensive pharmacokinetic sampling occurred after 4 weeks of therapy."( Efficacy, tolerability and pharmacokinetics of two nelfinavir-based regimens in human immunodeficiency virus-infected children and adolescents: pediatric AIDS clinical trials group protocol 403.
Acosta, EP; Aldrovandi, G; Chen, J; Damle, B; Hodge, J; Hughes, MD; King, JR; Nachman, S; Wiznia, A; Yogev, R, 2005
)
0.33
" NFV pharmacokinetic measurements were not statistically different between the treatment groups, yet exposure to the NFV metabolite, M8, was significantly higher in subjects receiving RTV."( Efficacy, tolerability and pharmacokinetics of two nelfinavir-based regimens in human immunodeficiency virus-infected children and adolescents: pediatric AIDS clinical trials group protocol 403.
Acosta, EP; Aldrovandi, G; Chen, J; Damle, B; Hodge, J; Hughes, MD; King, JR; Nachman, S; Wiznia, A; Yogev, R, 2005
)
0.33
" A randomized, two-way, crossover study was conducted in 24 fasting, healthy, Indian male subjects to compare plasma pharmacokinetic profile and single-dose tolerability of a new nevirapine tablet formulation (test, T) with that of a reference (R) tablet."( Pharmacokinetic profiling and bioequivalence assessment of two marketed brands of nevirapine tablets in healthy Indian volunteers.
Lulla, A; Malhotra, G; Narang, VS; Purandare, S, 2005
)
0.75
" Dosage and dosing frequency did not influence clearance or volume of distribution of nevirapine, indicating linear pharmacokinetic behavior of nevirapine whether given as a single daily dose or as divided doses over 24 hours."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.68
" The Cmin of nevirapine is lower and the Cmax of nevirapine is higher for the once-daily regimen as compared to the twice-daily regimen."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.82
" The objective was to find cutoff values of the Cmin and AUC24 below which the risk of virologic failure increased."( Pharmacokinetic parameters of nevirapine and efavirenz in relation to antiretroviral efficacy.
Beijnen, JH; Boron-Kaczmarska, A; Hall, DB; Huitema, AD; Johnson, D; Kappelhoff, BS; Lange, JM; Leith, J; Leth, FV; Livrozet, JM; Losso, MH; Saag, MS; Wit, FW, 2006
)
0.62
"A population pharmacokinetic analysis was performed in the context of therapeutic drug monitoring (87 patients, 121 samples)."( Influence of tenofovir, nevirapine and efavirenz on ritonavir-boosted atazanavir pharmacokinetics in HIV-infected patients.
Arvieux, C; Dailly, E; Jolliet, P; Perré, P; Raffi, F; Tattevin, P; Tribut, O, 2006
)
0.64
" A pre-dose to 6 h post-dose steady-state pharmacokinetic analysis (n = 35) of the drugs on the day of the scheduled Caesarean section was performed."( Placental transfer and pharmacokinetics of lopinavir and other protease inhibitors in combination with nevirapine at delivery.
Belohradsky, BH; Eberle, J; Friese, K; Gingelmaier, A; Grubert, TA; Kästner, R; Kurowski, M; Mylonas, I, 2006
)
0.55
" The influence of gender, age, body weight and comedication on minimum and maximum concentrations (C(min), C(max)), area under the concentration-time curve (AUC), total clearance (CL(tot)), half-life (t(1/2)) and volume of distribution (V(d)) was analysed by multivariate techniques."( A comparison of the steady-state pharmacokinetics of nevirapine in men, nonpregnant women and women in late pregnancy.
Carlebach, A; Gute, P; Haberl, A; Harder, S; Klauke, S; Knecht, G; Kurowski, M; Rohrbacher, M; Staszewski, S; Stocker, H; von Hentig, N, 2006
)
0.58
" We determined the pharmacokinetic profiles of stavudine, lamivudine and nevirapine in Pedimune and compared these with the branded products."( Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults.
Burger, DM; Dijkema, T; Gibb, DM; L'homme, RF; van der Ven, AJ; Warris, A, 2007
)
0.57
" An 8 h pharmacokinetic curve was recorded at day 1 of every cycle after medication intake."( Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults.
Burger, DM; Dijkema, T; Gibb, DM; L'homme, RF; van der Ven, AJ; Warris, A, 2007
)
0.34
"Non-parametric statistical tests revealed no statistically significant differences in Cmax (0."( Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults.
Burger, DM; Dijkema, T; Gibb, DM; L'homme, RF; van der Ven, AJ; Warris, A, 2007
)
0.34
"The pharmacokinetic profiles of stavudine, lamivudine and nevirapine in Pedimune Baby and Junior are comparable to the branded products."( Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults.
Burger, DM; Dijkema, T; Gibb, DM; L'homme, RF; van der Ven, AJ; Warris, A, 2007
)
0.58
" Patients taking Triomune had notably higher stavudine Cmax values."( Pharmacokinetic comparison of generic and trade formulations of lamivudine, stavudine and nevirapine in HIV-infected Malawian adults.
Corbett, AH; Hosseinipour, MC; Kanyama, C; Kashuba, AD; Mshali, I; Phakati, S; Rezk, NL; van der Horst, C, 2007
)
0.56
" Both drugs have demonstrated interindividual pharmacokinetic variability."( Efavirenz and nevirapine in HIV-1 infection : is there a role for clinical pharmacokinetic monitoring?
Dahri, K; Ensom, MH, 2007
)
0.7
" Nevirapine has a long half-life and achieves high steady-state plasma concentrations relative to the concentration required to inhibit 50% viral replication in vitro (IC(50)) in patients."( Once-daily nevirapine dosing: a pharmacokinetics, efficacy and safety review.
Cooper, CL; van Heeswijk, RP, 2007
)
1.64
" Nevirapine pharmacokinetic studies were carried out starting with the seventh dose of nevirapine in the nevirapine regimen (on days 7-10 or 28-31) and the combination regimen (on days 49-52)."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
1.49
"There was no significant difference in nevirapine pharmacokinetic parameters between the nevirapine and combination regimens."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
0.85
" Noncompartmental pharmacokinetic analysis was performed."( Pharmacokinetics of methadone in human-immunodeficiency-virus-infected patients receiving nevirapine once daily.
Arroyo, E; Climent-Grana, E; Merino, E; Pérez-Ruixo, JJ; Portilla, J; Valenzuela, B, 2007
)
0.56
" Pharmacokinetic parameters were calculated using noncompartmental methods, and bioequivalence was assessed using an analysis of variance model."( Pharmacokinetics of lamivudine, zidovudine, and nevirapine administered as a fixed-dose combination formulation versus coadministration of the individual products.
Dimarco, M; Dodard, C; Guilbaud, R; Marier, JF; Monif, T; Morelli, G; Singla, AK; Thudi, NR; Tippabhotla, SK, 2007
)
0.6
" Blood samples were collected from 1 to 144 hours post-dose for pharmacokinetic analysis."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.59
" Pharmacokinetic variables were compared between patients divided based on CD4 cell counts, sex, and BMI."( Steady-State Pharmacokinetics of Nevirapine in HIV-1 Infected Adults in India.
Anitha, S; Hemanthkumar, AK; Kumaraswami, V; Narendran, G; Padmapriyadarsini, C; Rajasekaran, S; Ramachandran, G; Subramanyam, S; Swaminathan, S, 2007
)
0.62
"Patients with higher BMI had lower peak and trough concentration and exposure of nevirapine than those with lower BMI; none of the differences in the pharmacokinetic variables of nevirapine between the various patient groups was statistically significant."( Steady-State Pharmacokinetics of Nevirapine in HIV-1 Infected Adults in India.
Anitha, S; Hemanthkumar, AK; Kumaraswami, V; Narendran, G; Padmapriyadarsini, C; Rajasekaran, S; Ramachandran, G; Subramanyam, S; Swaminathan, S, 2007
)
0.85
"The influence of nevirapine or efavirenz co-administration on ritonavir-boosted amprenavir pharmacokinetics was investigated in HIV-infected patients with a population pharmacokinetic approach."( Impact of nevirapine or efavirenz co-administration on ritonavir-boosted amprenavir pharmacokinetics in HIV-infected patients.
Allavena, C; Biron, C; Dailly, E; Jolliet, P; Raffi, F, 2008
)
1.09
" After 4 weeks or more, a 12-h pharmacokinetic curve was recorded."( Nevirapine, stavudine and lamivudine pharmacokinetics in African children on paediatric fixed-dose combination tablets.
Burger, DM; Chintu, C; Ewings, FM; Gibb, DM; Kabamba, D; Kankasa, C; L'homme, RF; Mulenga, V; Thomason, MJ; Walker, AS, 2008
)
1.79
"Nevirapine concentrations were higher but more variable than in adults; the pharmacokinetic parameters of stavudine and lamivudine were comparable to adults."( Nevirapine, stavudine and lamivudine pharmacokinetics in African children on paediatric fixed-dose combination tablets.
Burger, DM; Chintu, C; Ewings, FM; Gibb, DM; Kabamba, D; Kankasa, C; L'homme, RF; Mulenga, V; Thomason, MJ; Walker, AS, 2008
)
3.23
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
"The aim of this study was to develop and validate a population pharmacokinetic model for nevirapine in a population of HIV-infected adults and to evaluate the influence of nevirapine dosing regimen and patient characteristics on nevirapine trough concentration."( Once- or twice-daily dosing of nevirapine in HIV-infected adults: a population pharmacokinetics approach.
Cedeño, S; Clotet, B; Costa, J; Miranda, C; Miranda, J; Moltó, J; Negredo, E; Santos, JR; Valle, M; Vilaró, J, 2008
)
0.85
" Pharmacokinetic parameters, inter-individual variability and residual error were estimated using non-linear mixed effects modelling."( Once- or twice-daily dosing of nevirapine in HIV-infected adults: a population pharmacokinetics approach.
Cedeño, S; Clotet, B; Costa, J; Miranda, C; Miranda, J; Moltó, J; Negredo, E; Santos, JR; Valle, M; Vilaró, J, 2008
)
0.63
"We aimed to compare the steady-state pharmacokinetic parameters and tolerability of Triomune 40 (stavudine 40 mg, lamivudine 150 mg and nevirapine 200 mg) and branded formulations of these drugs in HIV-infected Ugandans."( Steady-state pharmacokinetic comparison of generic and branded formulations of stavudine, lamivudine and nevirapine in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; D'Avolio, A; Di Perri, G; Kalemeera, F; Khoo, S; Lamorde, M; Mauro, S; Mayanja-Kizza, H; Merry, C; Ryan, M, 2008
)
0.76
" Similarity between steady-state pharmacokinetic parameters was assessed using the US Food and Drug Administration standards for bioequivalency testing."( Steady-state pharmacokinetic comparison of generic and branded formulations of stavudine, lamivudine and nevirapine in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; D'Avolio, A; Di Perri, G; Kalemeera, F; Khoo, S; Lamorde, M; Mauro, S; Mayanja-Kizza, H; Merry, C; Ryan, M, 2008
)
0.56
" Pharmacokinetic parameter inter-individual variability ranged from 29% to 99%."( Steady-state pharmacokinetic comparison of generic and branded formulations of stavudine, lamivudine and nevirapine in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; D'Avolio, A; Di Perri, G; Kalemeera, F; Khoo, S; Lamorde, M; Mauro, S; Mayanja-Kizza, H; Merry, C; Ryan, M, 2008
)
0.56
" Capacity building for pharmacokinetic research in resource-limited settings is a priority."( Steady-state pharmacokinetic comparison of generic and branded formulations of stavudine, lamivudine and nevirapine in HIV-infected Ugandan adults.
Back, D; Boffito, M; Byakika-Kibwika, P; D'Avolio, A; Di Perri, G; Kalemeera, F; Khoo, S; Lamorde, M; Mauro, S; Mayanja-Kizza, H; Merry, C; Ryan, M, 2008
)
0.56
" The effect of three routinely prescribed antiretroviral (ARV) drugs on the pharmacokinetic profile of an antidiabetic drug, chlorpropamide, was investigated in 18 human subjects, who had recently been diagnosed positive for human immunodeficiency virus (HIV) infection."( The influence of lamivudine, stavudine and nevirapine on the pharmacokinetics of chlorpropamide in human subjects.
Bakare-Odunola, MT; Enemali, I; Garba, M; Mustapha, KB; Obodozie, OO,
)
0.39
" A 600-mg oral dose of efavirenz was subsequently administered, and pharmacokinetic sampling was repeated."( Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African americans.
Acosta, EP; Floyd, M; Gebretsadik, T; Haas, DW; Mayo, G; Menon, UN; Shintani, A; Stein, CM; Wilkinson, GR, 2009
)
0.58
"A 12 h pharmacokinetic analysis was performed in 18 patients: 7 HIV/HCV-coinfected and 11 HIV-monoinfected."( Nevirapine pharmacokinetics in HIV-infected and HIV/HCV-coinfected individuals.
Bertram, N; Fätkenheuer, G; Reichel, C; Rockstroh, JK; Schwarze-Zander, C; Sudhop, T; Vogel, M; Voigt, E; Wasmuth, JC; Wyen, C, 2009
)
1.8
"Small intensive pharmacokinetic (PK) studies of medications in early-phase trials cannot identify the range of factors that influence drug exposure in heterogenous populations."( Nonnucleoside reverse transcriptase inhibitor pharmacokinetics in a large unselected cohort of HIV-infected women.
Anastos, K; Bacchetti, P; Benet, LZ; Cohen, M; Gandhi, M; Gange, SJ; Greenblatt, RM; Kalinowski, A; Minkoff, H; Wolfe, AR; Young, M, 2009
)
0.35
"To investigate the pharmacokinetic interaction between darunavir/ritonavir (DRV/r) and nevirapine (NVP) in 19 HIV-infected patients."( Pharmacokinetic interaction between nevirapine and darunavir with low-dose ritonavir in HIV-1-infected patients.
De Pauw, M; Hoetelmans, RM; Lefebvre, E; Mariën, K; Pozniak, A; Sekar, V; Vangeneugden, T, 2009
)
0.85
"A highly sensitive and specific LC-MS/MS assay was developed and validated to quantify nevirapine (NVP) and its five metabolites [2-, 3-, 8-, 12-hydroxyl NVP (OHNVP) and 4-carboxyl NVP (CANVP)] simultaneously in baboon serum and the assay was used to characterize their pharmacokinetic studies of an oral-dose escalation study in baboon."( A sensitive and specific liquid chromatography/tandem mass spectrometry method for quantification of nevirapine and its five metabolites and their pharmacokinetics in baboons.
Chan, KK; Fan-Havard, P; Ling, Y; Liu, Z; Ren, C; Schlabritz-Loutsevitch, N, 2010
)
0.8
" The method has been successfully applied to the pharmacokinetic study of a combination treatment of 300 mg lamivudine, 30 mg stavudine and 200 mg nevirapine in 22 healthy male volunteers under fasting conditions."( Simultaneous determination of lamivudine, stavudine and nevirapine in human plasma by LC-MS/MS and its application to pharmacokinetic study in clinic.
Ding, C; Ge, Q; Li, Z; Liu, X; Zhi, X; Zhou, Z, 2010
)
0.81
" After 10 days of one formulation, 6-h pharmacokinetic sampling was performed, and patients were crossed over to subsequent formulations."( Pharmacokinetics of generic and trade formulations of lamivudine, stavudine and nevirapine in HIV-infected Malawian children.
Corbett, AH; Hosseinipour, MC; Kanyama, C; Kashuba, AD; Kazembe, P; Mkupani, P; Mwansambo, C; Nyirenda, J; Rezk, NL; Sichali, D; Tien, H; Weigel, R, 2010
)
0.59
"Full 12-hour pharmacokinetic profiles of nevirapine, stavudine, and lamivudine in HIV-infected children taking fixed-dose combination antiretroviral tablets have been reported previously by us."( Limited sampling models to predict the pharmacokinetics of nevirapine, stavudine, and lamivudine in HIV-infected children treated with pediatric fixed-dose combination tablets.
Burger, D; Chintu, C; Ewings, F; Gibb, DM; Kabamba, D; Kankasa, C; L'homme, R; Mulenga, V; Thomason, M; Walker, AS, 2010
)
0.87
" Six-point pharmacokinetic sampling (0, 2, 4, 6, 8, and 12 h) was undertaken after observed intake with a standardized breakfast."( Pharmacokinetics of lopinavir-ritonavir with and without nonnucleoside reverse transcriptase inhibitors in Ugandan HIV-infected adults.
Dickinson, L; Gibb, DM; Gilks, CF; Kayiwa, J; Khoo, S; Kityo, C; Lutwama, F; Munderi, P; Nalumenya, R; Reid, A; Ssali, F; Tumukunde, D; Walker, AS, 2010
)
0.36
"The International Maternal Pediatric Adolescent AIDS Clinical Trials group (IMPAACT) P1056 study was a phase I/II, 2-arm, randomized, open-label, multidose pharmacokinetic cross-over study."( A chewable pediatric fixed-dose combination tablet of stavudine, lamivudine, and nevirapine: pharmacokinetics and safety compared with the individual liquid formulations in human immunodeficiency virus-infected children in Thailand.
Capparelli, E; Chokephaibulkit, K; Chotpitayasunondh, T; Cressey, TR; Eksaengsri, A; Hongsiriwan, S; McIntosh, K; Muresan, P; Plipat, N; Prasitsuebsai, W; Sirisanthana, V; Smith, ME; Toye, M; Vanprapar, N; Yogev, R, 2010
)
0.59
" The developed assay method was successfully applied to a pharmacokinetic study in human male volunteers."( Simultaneous determination of atorvastatin, amlodipine, ramipril and benazepril in human plasma by LC-MS/MS and its application to a human pharmacokinetic study.
Inamadugu, JK; Karra, VK; Mullangi, R; Pilli, NR; Rao, JV; Vaidya, JR, 2011
)
0.37
"The aims of this ANRS12154 open-label, single-center, multiple-dose pharmacokinetic study were to characterize nevirapine pharmacokinetics in a Cambodian population of HIV-infected patients and to identify environmental and genetic factors of variability, focusing on the CYP2B6, CYP3A5, and ABCB1 (MDR1) genes."( Population pharmacokinetic-pharmacogenetic study of nevirapine in HIV-infected Cambodian patients.
Becquemont, L; Bertrand, J; Borand, L; Chou, M; Comets, E; Le Tiec, C; Mentre, F; Ouk, V; Segeral, O; Taburet, AM; Verstuyft, C, 2010
)
0.82
" The method was sensitive, specific, precise, accurate and suitable for bioequivalence and pharmacokinetic studies."( Simultaneous determination of niacin and its metabolites--nicotinamide, nicotinuric acid and N-methyl-2-pyridone-5-carboxamide--in human plasma by LC-MS/MS and its application to a human pharmacokinetic study.
Damaramadugu, R; Inamadugu, JK; Mullangi, R; Ponneri, V, 2010
)
0.36
" Subjects underwent 12 h intensive pharmacokinetic sampling on Days 7, 14 and 21 of nevirapine treatment."( Nevirapine pharmacokinetics when initiated at 200 mg or 400 mg daily in HIV-1 and tuberculosis co-infected Ugandan adults on rifampicin.
Back, D; Boffito, M; Byakika-Kibwika, P; Coakley, P; Colebunders, R; Kalemeera, F; Khoo, S; Lamorde, M; Merry, C; Namakula, R; Okaba-Kayom, V; Ryan, M, 2011
)
2.04
"Non-linear mixed-effects modelling was used to estimate pharmacokinetic parameters from 275 patients."( Integration of population pharmacokinetics and pharmacogenetics: an aid to optimal nevirapine dose selection in HIV-infected individuals.
Back, DJ; Brockmeyer, NH; Davies, G; Egan, D; Fätkenheuer, G; Hendra, H; Johnson, MA; Khoo, S; Mahungu, T; Owen, A; Rockstroh, J; Schipani, A; Siccardi, M; Wyen, C; Youle, M, 2011
)
0.59
" No significant difference in the pharmacokinetic parameters of NVP was found upon short-term co-administration of Sutherlandia."( Effect of short term and chronic administration of Sutherlandia frutescens on pharmacokinetics of nevirapine in rats.
Earla, R; Folk, WR; Kwatra, D; Mandava, NK; Minocha, M; Mitra, AK; Pal, D, 2011
)
0.59
"Patients, who participated in the 2NN pharmacokinetic sub study, were reconsented and reenrolled into a clinical trial for genotyping analysis."( Integration of absorption, distribution, metabolism, and elimination genotyping data into a population pharmacokinetic analysis of nevirapine.
Hall, D; Jayadev, S; Lehr, T; MacGregor, TR; Schaefer, HG; Staab, A; Yuan, J; Zimdahl-Gelling, H, 2011
)
0.57
" Pharmacokinetic parameter estimates and model-predicted HIV-1 transmission rates were very consistent with other studies."( Quantifying the impact of nevirapine-based prophylaxis strategies to prevent mother-to-child transmission of HIV-1: a combined pharmacokinetic, pharmacodynamic, and viral dynamic analysis to predict clinical outcomes.
Frank, M; Harms, G; Kloft, C; Kunz, A; Schütte, C; von Kleist, M, 2011
)
0.67
" More comprehensive in vivo pharmacokinetic data are required to justify the potential use of these agents as safe and effective options during pregnancy."( Pharmacokinetics of antiretroviral drugs in anatomical sanctuary sites: the fetal compartment (placenta and amniotic fluid).
Back, DJ; Else, LJ; Khoo, SH; Taylor, S, 2011
)
0.37
"In this Phase I/II open-label pharmacokinetic study, 42 children weighing 6-30 kg treated with NVP-based HAART for ≥4 weeks were randomized to receive the FDC tablets (GPO-VIR Z30) or the liquid formulations."( Pharmacokinetics and safety of a new paediatric fixed-dose combination of zidovudine/lamivudine/nevirapine in HIV-infected children.
Aurpibul, L; Capparelli, E; Chokephaibulkit, K; Cressey, TR; Eksaengsri, A; Hongsiriwon, S; Kabat, B; Limwongse, C; McIntosh, K; Muresan, P; Ngampiyaskul, C; Sirisanthana, V; Smith, ME; Toye, M; Wittawatmongkol, O; Yogev, R, 2011
)
0.59
"To propose a modelling strategy to efficiently integrate data from different sources in one simultaneous analysis, using nevirapine population pharmacokinetic data as an example."( Integration of data from multiple sources for simultaneous modelling analysis: experience from nevirapine population pharmacokinetics.
Barnes, KI; Cohen, K; Denti, P; Huitema, A; Karlsson, MO; Kredo, T; Nachega, JB; Svensson, E; van der Walt, JS, 2012
)
0.81
"NVP pharmacokinetics were modeled by population pharmacokinetic analysis."( Nevirapine pharmacokinetics and risk of rash and hepatitis among HIV-infected sub-Saharan African women.
Aweeka, FT; Currier, JS; Dong, BJ; Frymoyer, A; Hughes, MD; Lizak, P; Lockman, S; Sawe, F; Verotta, D; Zheng, Y, 2012
)
1.82
" The method was successfully applied to quantify them in a rat pharmacokinetic study in whole blood, plasma and DBS cards after a single oral co-administration at the dose of 10, 2 and 13 mg/kg for lamivudine, stavudine and nevirapine, respectively, to male Wistar rats."( Exploring dried blood spot sampling technique for simultaneous quantification of antiretrovirals: lamivudine, stavudine and nevirapine in a rodent pharmacokinetic study.
Aleti, R; Bhyrapuneni, G; Kalaikadhiban, I; Kandikere, V; Komarneni, P; Muddana, N; Nirogi, R; Padala, N, 2012
)
0.77
" The developed and validated method was successfully applied to quantitative determination of the three analytes in plasma for pharmacokinetic study in 12 healthy human volunteers."( Development and validation of an HPLC-UV method for simultaneous determination of zidovudine, lamivudine, and nevirapine in human plasma and its application to pharmacokinetic study in human volunteers.
Choudhury, H; Das, A; Gorain, B; Nandi, U; Pal, TK; Roy, B, 2013
)
0.6
" The developed assay method was successfully applied to a pharmacokinetic study in humans."( Simultaneous determination of atorvastatin and niacin in human plasma by LC-MS/MS and its application to a human pharmacokinetic study.
Gajula, R; Inamadugu, JK; Mullangi, R; Pilli, NR; Ponneri, V; Ravi, VB, 2012
)
0.38
"Twenty-two children received antituberculosis and antiretroviral therapy (ART) concurrently for 4 weeks before pharmacokinetic sampling."( Pharmacokinetics of nevirapine in HIV-infected children under 3 years on rifampicin-based antituberculosis treatment.
Burger, DM; Chintu, C; Cook, A; Gibb, DM; McIlleron, H; Merry, C; Mulenga, V; Oudijk, JM; Walker, AS, 2012
)
0.7
"Co-administration of artemether/lumefantrine with antiretroviral therapy has potential for pharmacokinetic drug interactions."( Significant pharmacokinetic interactions between artemether/lumefantrine and efavirenz or nevirapine in HIV-infected Ugandan adults.
Back, D; Byakika-Kibwika, P; de Vries, PJ; Hanpithakpong, W; Katabira, E; Khoo, S; Lamorde, M; Lindegardh, N; Mayanja-Kizza, H; Mayito, J; Merry, C; Nabukeera, L; Namakula, R; Ntale, M; Pakker, N; Ryan, M; Tarning, J, 2012
)
0.6
" Clinical data from population pharmacokinetic and pharmacodynamic trials evaluating the impact of these drug interactions are urgently needed."( Significant pharmacokinetic interactions between artemether/lumefantrine and efavirenz or nevirapine in HIV-infected Ugandan adults.
Back, D; Byakika-Kibwika, P; de Vries, PJ; Hanpithakpong, W; Katabira, E; Khoo, S; Lamorde, M; Lindegardh, N; Mayanja-Kizza, H; Mayito, J; Merry, C; Nabukeera, L; Namakula, R; Ntale, M; Pakker, N; Ryan, M; Tarning, J, 2012
)
0.6
" The population pharmacokinetic approach represents a very useful tool for the description of the dose-concentration relationship, the quantification of variability in the target population of patients and the identification of influencing factors."( Dosage optimization of treatments using population pharmacokinetic modeling and simulation.
Aouri, M; Arab-Alameddine, M; Buclin, T; Csajka, C; Decosterd, LA; Guidi, M; Rotger, M; Telenti, A, 2012
)
0.38
" NVP pharmacokinetic data were combined from eight pediatric clinical trials (Pediatric AIDS Clinical Trials Group [PACTG] studies 245, 356, 366, 377, 403, 1056, and 1069 and Children with HIV in Africa Pharmacokinetics and Adherence of Simple Antiretroviral Regimens [CHAPAS]) representing subjects from multiple continents and across the pediatric age continuum."( Nevirapine exposure with WHO pediatric weight band dosing: enhanced therapeutic concentrations predicted based on extensive international pharmacokinetic experience.
Acosta, EP; Aweeka, FT; Burger, D; Capparelli, EV; Cressey, TR; Kabamba, D; Nikanjam, M; Spector, SA, 2012
)
1.82
" In a pharmacokinetic investigation, breast milk and plasma samples of mothers and newborns were collected."( Population pharmacokinetic analysis of a nevirapine-based HIV-1 prevention of mother-to-child transmission program in Uganda to assess the impact of different dosing regimens for newborns.
Frank, M; Harms, G; Kloft, C; Kunz, A, 2013
)
0.66
" Pharmacokinetic parameters were calculated by noncompartmental analysis."( Pharmacokinetics of phase I nevirapine metabolites following a single dose and at steady state.
Barrail-Tran, A; Chou, M; Fan-Havard, P; Haas, DW; Ling, Y; Liu, Z; Taburet, AM, 2013
)
0.68
" Median distribution half-life was 24 min (range 6-42 min) and 39 min (range 33."( Pharmacokinetics of midazolam after intravenous administration to horses.
Aarnes, TK; Bednarski, RM; Hubbell, JA; Kelly, EM; Lakritz, J; Lerche, P; Liu, Z, 2013
)
0.39
" We conducted a cross-sectional study of HIV-positive women to determine if protease inhibitor (PI) and non-nucleoside reverse transcriptase inhibitor (NNRTI) C(min) and Cmax values were significantly different than historical general population (predominantly male) averages and to evaluate correlates of higher concentrations."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
" Timed blood samples for C(min) and Cmax were drawn weekly for 3 weeks."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
"Compared to historical control data, C(min) in the women enrolled was significantly higher whereas Cmax was significantly lower."( Factors affecting antiretroviral pharmacokinetics in HIV-infected women with virologic suppression on combination antiretroviral therapy: a cross-sectional study.
Angel, JB; Blitz, SL; Burdge, D; Cohen, J; Conway, B; de Pokomandy, A; Gough, K; Haase, D; Klein, MB; la Porte, CJ; Loemba, H; Loutfy, MR; Pick, N; Raboud, J; Rachlis, AR; Smaill, FM; Trottier, S; Tseng, AL; Walmsley, SL, 2013
)
0.39
"To confirm whether 7 days of phenytoin, an enzyme inducer, would decrease the elimination half-life of single-dose nevirapine and to investigate its effect on the development of nevirapine resistance in pregnant, HIV-infected women."( Effect of 7 days of phenytoin on the pharmacokinetics of and the development of resistance to single-dose nevirapine for perinatal HIV prevention: a randomized pilot trial.
Aitken, S; Burger, DM; Chunda, C; Fillekes, Q; Gibb, DM; Kankasa, C; Kisanga, ER; Muro, EP; Thomason, MJ; Walker, AS, 2013
)
0.81
"In a pharmacokinetic pilot trial (NCT01187719), HIV-infected, antiretroviral (ARV)-naive pregnant women ≥18 years old from Zambia and Tanzania and with CD4 cell counts >350 cells/mm(3) were randomized 1 : 1 to a control (zidovudine pre-delivery, single-dose nevirapine/zidovudine/lamivudine at delivery and zidovudine/lamivudine for 7 days post-delivery) or an intervention (control plus 184 mg of phenytoin once daily for 7 days post-delivery) group."( Effect of 7 days of phenytoin on the pharmacokinetics of and the development of resistance to single-dose nevirapine for perinatal HIV prevention: a randomized pilot trial.
Aitken, S; Burger, DM; Chunda, C; Fillekes, Q; Gibb, DM; Kankasa, C; Kisanga, ER; Muro, EP; Thomason, MJ; Walker, AS, 2013
)
0.78
" The GM (95% CI) half-life of nevirapine was 63."( Effect of 7 days of phenytoin on the pharmacokinetics of and the development of resistance to single-dose nevirapine for perinatal HIV prevention: a randomized pilot trial.
Aitken, S; Burger, DM; Chunda, C; Fillekes, Q; Gibb, DM; Kankasa, C; Kisanga, ER; Muro, EP; Thomason, MJ; Walker, AS, 2013
)
0.89
"Adding 7 days of an enzyme inducer to single-dose nevirapine to prevent mother-to-child transmission of HIV significantly reduced subtherapeutic nevirapine levels by shortening the half-life of nevirapine."( Effect of 7 days of phenytoin on the pharmacokinetics of and the development of resistance to single-dose nevirapine for perinatal HIV prevention: a randomized pilot trial.
Aitken, S; Burger, DM; Chunda, C; Fillekes, Q; Gibb, DM; Kankasa, C; Kisanga, ER; Muro, EP; Thomason, MJ; Walker, AS, 2013
)
0.86
"To compare steady-state (ss) pharmacokinetic targets of nevirapine extended-release (NVP-XR) tablets once-daily (QD) with immediate-release (NVP-IR) tablet or oral suspension twice-daily in HIV-1-infected children and adolescents."( Steady-state pharmacokinetics of nevirapine extended-release tablets in HIV-1-infected children and adolescents: an open-label, multiple-dose, cross-over study.
Anabwani, G; Feiterna-Sperling, C; Giaquinto, C; Königs, C; MacGregor, TR; Mensa, FJ; Mompati, K; Nguyen, T; Nuttall, J; Quinson, AM; Sabo, JP; Yong, CL, 2014
)
0.93
" Cpre,ss (steady-state, predose concentrations) was obtained from all, and 12-hour NVP-IR and 24-hour NVP-XR steady-state pharmacokinetic profiles were obtained in the pharmacokinetic substudy."( Steady-state pharmacokinetics of nevirapine extended-release tablets in HIV-1-infected children and adolescents: an open-label, multiple-dose, cross-over study.
Anabwani, G; Feiterna-Sperling, C; Giaquinto, C; Königs, C; MacGregor, TR; Mensa, FJ; Mompati, K; Nguyen, T; Nuttall, J; Quinson, AM; Sabo, JP; Yong, CL, 2014
)
0.68
" The purpose of the current study was to determine the population mean pharmacokinetic parameters and identify factors that influence pharmacokinetic parameters of nevirapine in Thai HIV-infected patients."( Population pharmacokinetics of nevirapine in Thai HIV-infected patients.
Avihingsanon, A; Manosuthi, W; Punyawudho, B; Wattanakul, T, 2014
)
0.88
"This population-based pharmacokinetic model can be used for optimizing nevirapine dosage regimens for individual patients to improve efficacy and safety of nevirapine therapy in this population."( Population pharmacokinetics of nevirapine in Thai HIV-infected patients.
Avihingsanon, A; Manosuthi, W; Punyawudho, B; Wattanakul, T, 2014
)
0.92
"Nevirapine (NVP) extensive data obtained after oral single dose administration of 200 mg in a crossover study involving 16 healthy subjects was used to develop a descriptive population pharmacokinetic model including drug recirculation, since secondary peaks were observed in plasma concentration-time profiles for all subjects."( Population pharmacokinetic model to analyze nevirapine multiple-peaks profile after a single oral dose.
Fagiolino, P; Ibarra, M; Vázquez, M, 2014
)
2.11
" Therefore, it was decided to study a potential pharmacokinetic interaction between the nonnucleoside reverse transcriptase inhibitor nevirapine (NVP) and the tricyclic antidepressant nortriptyline (NT)."( Pharmacokinetic interaction between nevirapine and nortriptyline in rats: inhibition of nevirapine metabolism by nortriptyline.
Gandía, P; Melis, V; Peris, JE; Usach, I, 2014
)
0.88
" Substituting nevirapine for rilpivirine resulted in ongoing virological suppression and did not have clinically relevant pharmacokinetic effects by cytochrome P450 interactions."( The efficacy, pharmacokinetics, and safety of a nevirapine to rilpivirine switch in virologically suppressed HIV-1-infected patients.
Blonk, M; Burger, D; Rijnders, BJ; Rokx, C; Verbon, A, 2015
)
1.03
" Pharmacokinetic analysis of the rat plasma NVP concentration-time data allowed absorption rate constants to be calculated."( Pharmacokinetics of injectable, long-acting nevirapine for HIV prophylaxis in breastfeeding infants.
Baum, MM; Beliveau, M; Cortez, JM; Moss, JA; Quintero, R; Smith, TJ, 2015
)
0.68
" The effect of EFV and/or NVP on lumefantrine pharmacokinetic profile among HIV-malaria co-infected patients on ART and treated with AL was investigated."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
" Pharmacokinetic analysis of lumefantrine was done using non-linear mixed effect modelling."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
"Of the evaluated models, a two-compartment pharmacokinetic model with first order absorption and lag-time described well lumefantrine plasma concentrations time profile."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
"The metabolic pathways of dolutegravir and nevirapine suggest a potential pharmacokinetic interaction between these drugs."( Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
Allavena, C; Billaud, E; Bouchez, S; Bouquié, R; Dailly, E; Deslandes, G; Grégoire, M; Hall, N; Hernando, H; Jolliet, P; Raffi, F; Reliquet, V, 2015
)
1.05
" Full pharmacokinetic profiles were assessed on the day of nevirapine discontinuation and 2 weeks after discontinuation of nevirapine."( Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
Allavena, C; Billaud, E; Bouchez, S; Bouquié, R; Dailly, E; Deslandes, G; Grégoire, M; Hall, N; Hernando, H; Jolliet, P; Raffi, F; Reliquet, V, 2015
)
1.03
"018) and terminal half-life (-15%, P = 0."( Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
Allavena, C; Billaud, E; Bouchez, S; Bouquié, R; Dailly, E; Deslandes, G; Grégoire, M; Hall, N; Hernando, H; Jolliet, P; Raffi, F; Reliquet, V, 2015
)
0.79
" Plasma concentrations were measured as therapeutic drug monitoring while a subset of patients underwent intensive 12-hour pharmacokinetic evaluation."( Raltegravir Plus Nevirapine as Maintenance Antiretroviral Therapy in HIV-Positive Patients: Safety, Efficacy and Pharmacokinetics.
Bonora, S; Calcagno, A; Calza, L; Capetti, A; Cenderello, G; D'Avolio, A; Di Perri, G; Guaraldi, G; Lanzafame, M; Marinaro, L; Montrucchio, C; Tettoni, MC; Trentini, L, 2016
)
0.77
" Median trough raltegravir and nevirapine concentrations were 83 ng/ml (32-227) and 5460 ng/ml (4037-7221); intensive 12-hours pharmacokinetic parameters (n=7) were similar to published data."( Raltegravir Plus Nevirapine as Maintenance Antiretroviral Therapy in HIV-Positive Patients: Safety, Efficacy and Pharmacokinetics.
Bonora, S; Calcagno, A; Calza, L; Capetti, A; Cenderello, G; D'Avolio, A; Di Perri, G; Guaraldi, G; Lanzafame, M; Marinaro, L; Montrucchio, C; Tettoni, MC; Trentini, L, 2016
)
1.06
"This nonrandomized, parallel group, pharmacokinetic evaluation was conducted in three groups of human immunodeficiency virus-infected Ugandan women: ART-naive (n = 17), efavirenz-based ART (n = 20), and nevirapine-based ART (n = 20)."( Unintended Pregnancies Observed With Combined Use of the Levonorgestrel Contraceptive Implant and Efavirenz-based Antiretroviral Therapy: A Three-Arm Pharmacokinetic Evaluation Over 48 Weeks.
Back, DJ; Buzibye, A; Byakika-Kibwika, P; Cohn, SE; Darin, KM; Dilly Penchala, S; Else, LJ; Lamorde, M; Merry, C; Nakalema, S; Scarsi, KK, 2016
)
0.62
" Hence, this study was aimed to determine population pharmacokinetic parameters in Malaysian HIV-infected patients with a non-parametric approach which allows detection of outliers or non-normal distribution contrary to the parametric approach."( Population pharmacokinetics of nevirapine in Malaysian HIV patients: a non-parametric approach.
Choon, TS; Hassan, NB; Mustafa, S; Woillard, JB; Yusuf, WN, 2016
)
0.72
" In the intensive pharmacokinetic phase, apparent clearance (CL/F) was higher in pregnant (n=31) than postpartum (n=28) women (P=0."( Pregnancy affects nevirapine pharmacokinetics: evidence from a CYP2B6 genotype-guided observational study.
Back, D; Bolaji, O; Khoo, S; Neary, M; Olagunju, A; Owen, A, 2016
)
0.77
" The pharmacodynamic consequences in patients at risk of suboptimal exposure and potential dose optimization strategies warrant further investigation."( Pregnancy affects nevirapine pharmacokinetics: evidence from a CYP2B6 genotype-guided observational study.
Back, D; Bolaji, O; Khoo, S; Neary, M; Olagunju, A; Owen, A, 2016
)
0.77
"A physiologically-based pharmacokinetic (PBPK) model for nevirapine, which is metabolized by the cytochrome P450 (CYP) 3A4, 2B6 and 2D6 pathways, was developed to predict maternal and fetal pharmacokinetics (PK)."( A Physiologically-Based Pharmacokinetic Model to Predict Human Fetal Exposure for a Drug Metabolized by Several CYP450 Pathways.
Benaboud, S; Blanche, S; Bouazza, N; De Sousa Mendes, M; Foissac, F; Hirt, D; Lui, G; Pressiat, C; Treluyer, JM; Urien, S; Valade, E; Zheng, Y, 2017
)
0.7
" Here we aimed to quantify nevirapine and LPV/r drug-drug interaction effects on bedaquiline and M2 in patients co-infected with HIV and multidrug-resistant tuberculosis (MDR-TB) using population pharmacokinetic (PK) analysis and compare these with model-based predictions from single-dose studies in subjects without TB."( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis.
Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017
)
0.97
"Traditional medication adherence measures do not account for the pharmacokinetic (PK) properties of the drugs, potentially misrepresenting true therapeutic exposure."( Pharmacokinetics-based adherence measures for antiretroviral therapy in HIV-infected Kenyan children.
Ayaya, SO; Liu, H; Nyandiko, WM; Scanlon, ML; Slaven, JE; Tu, W; Vreeman, RC, 2017
)
0.46
"Sparse pharmacokinetic sampling of ENG, NVP, or EFV were performed at screening, entry, and then 1, 4, 12, and 24-week postimplant insertion."( Efavirenz decreases etonogestrel exposure: a pharmacokinetic evaluation of implantable contraception with antiretroviral therapy.
Achilles, SL; Chappell, CA; Chen, BA; Cohn, SE; Darin, KM; Lamorde, M; Mackline, H; Nakalema, S; Riddler, SA; Scarsi, KK, 2017
)
0.46
" Pharmacokinetic parameters (area under the plasma concentration vs."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
0.83
" Fifteen of the 16 (aged 4 to 11 years) on nevirapine-based ART were included in the pharmacokinetic analysis."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
1.1
" NVP was administered orally to male and female rats and sex differences in plasma levels and pharmacokinetic parameters were analysed."( Sex-dependent metabolism of nevirapine in rats: impact on plasma levels, pharmacokinetics and interaction with nortriptyline.
Compañ, P; Peris, JE; Usach, I, 2018
)
0.77
" Associations between patient genotype and etonogestrel pharmacokinetic parameters were determined through univariate and multivariate linear regression."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.73
"Within the control group, CYP2B6 983 T>C was associated with 27% higher etonogestrel Cmax and 28% higher AUC0-24weeks."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.73
" Participants provided sparse pharmacokinetic (PK) sampling at baseline and weeks 2 and 4 for trough nevirapine determination."( Nevirapine pharmacokinetics in HIV-infected persons receiving rifapentine and isoniazid for TB prevention.
Benson, CA; Chaisson, RE; Fletcher, CV; Gupta, A; Hakim, J; Kanyama, C; Langat, D; Leon-Cruz, J; Mwelase, N; Omoz-Oarhe, A; Podany, AT; Supparatpinyo, K; Swindells, S, 2021
)
2.28
" However, pharmacokinetic knowledge is lacking for specific populations, especially patients with neglected tropical diseases and severe malnutrition."( Influence of Malnutrition on the Pharmacokinetics of Drugs Used in the Treatment of Poverty-Related Diseases: A Systematic Review.
Beijnen, JH; Dorlo, TPC; Huitema, ADR; Verrest, L; Wilthagen, EA, 2021
)
0.62
" A linear one-compartment population pharmacokinetic model with first-order conditional estimation with interaction was used to evaluate methadone clearance (CL/F) and volume of distribution (V/F)."( Effect of HIV, antiretrovirals, and genetics on methadone pharmacokinetics: Results from the methadone antiretroviral pharmacokinetics study.
Bart, G; Brundage, RC; Giang, LM; Hodges, JS; Yen, H, 2021
)
0.62
" This study aimed to develop a population pharmacokinetic model to characterize the disposition of maraviroc in neonates to inform dosing regimens and expand available options."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
"Using maraviroc concentrations from neonates who received either a single dose or multiple doses of 8 mg/kg of maraviroc in the first 6 weeks of life, a population pharmacokinetic model was developed to determine the effects of age, sex, maternal efavirenz exposure and concomitant ARV therapy on maraviroc disposition."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" There are few pharmacokinetic models of buprenorphine across diverse populations."( Findings from a pilot study of buprenorphine population pharmacokinetics: A potential effect of HIV on buprenorphine bioavailability.
Bart, G; Brundage, RC; Giang, LM; Jaber, M; Korthuis, PT, 2022
)
0.72

Compound-Compound Interactions

ARTEN is a randomized, open-label, non-inferiority trial that compares nevirapine (NVP) 200 mg twice daily or  efavirenz once daily. Single-dose drug-drug interaction studies found no significant interactions with nevirAPine or lopinavir/ritonavir.

ExcerptReferenceRelevance
"5, 50, and 200 mg/day, alone or in combination with zidovudine, 200 mg q8h."( Phase I/II evaluation of nevirapine alone and in combination with zidovudine for infection with human immunodeficiency virus.
Cheeseman, SH; Greenough, TC; Hall, D; Hattox, SE; Havlir, D; McLaughlin, MM; Myers, M; Spector, SA; Stein, DS; Sullivan, JL, 1995
)
0.59
" MKC-442 was evaluated in combination with the nucleoside analogues AZT, ddI and ddC, the non-nucleoside RT inhibitor nevirapine, the HIV-1 proteinase inhibitor Ro-31-8959, and the alpha-glucosidase 1 inhibitor, MDL-28,574, using a cell viability assay."( The inhibition of human immunodeficiency virus type 1 in vitro by a non-nucleoside reverse transcriptase inhibitor MKC-442, alone and in combination with other anti-HIV compounds.
Brennan, TM; Bridges, CG; Leyda, JP; Taylor, DL; Tyms, AS, 1995
)
0.5
"To determine whether synergistic inhibition of HIV-1 replication would result from the in vitro use of nevirapine in combination with zidovudine, interferon (IFN)-alpha 2C, and CD4 immunoadhesin."( Nevirapine synergistically inhibits HIV-1 replication in combination with zidovudine, interferon or CD4 immunoadhesin.
Brewster, F; Grob, P; Koup, RA; Sullivan, JL, 1993
)
1.94
"The non-nucleoside reverse transcriptase inhibitor nevirapine (formerly BI-RG-587) was tested in combination with the other antiretrovial agents."( Nevirapine synergistically inhibits HIV-1 replication in combination with zidovudine, interferon or CD4 immunoadhesin.
Brewster, F; Grob, P; Koup, RA; Sullivan, JL, 1993
)
1.98
"Zidovudine, IFN-alpha 2C and CD4 immunoadhesin, when used in combination with nevirapine, synergistically inhibited HIV-1 replication in human peripheral blood lymphocytes compared with each agent used alone."( Nevirapine synergistically inhibits HIV-1 replication in combination with zidovudine, interferon or CD4 immunoadhesin.
Brewster, F; Grob, P; Koup, RA; Sullivan, JL, 1993
)
1.96
"Antiretroviral therapy including zidovudine may yield replicating viruses with a two amino-acid insertion in RT in combination with amino-acid changes at codons 67 and 215, which are highly resistant to lamivudine and stavudine on top of zidovudine and have unpredictable susceptibility to didanosine and zalcitabine despite lack of previously reported corresponding resistance-associated amino-acid changes."( Insertion of two amino acids combined with changes in reverse transcriptase containing tyrosine-215 of HIV-1 resistant to multiple nucleoside analogs.
Baan, E; Danner, SA; de Jong, JJ; de Wolf, F; Goudsmit, J; Hillebrand, ME; Huismans, R; Jurriaans, S; Lukashov, VV; ten Veen, JH, 1999
)
0.3
"The purpose of the current study was to determine the efficacy and safety of nevirapine combined with nelfinavir and two nucleoside reverse transcriptase inhibitors (NRTIs) in patients previously exposed to highly active antiretroviral therapy (HAART)."( The effect of nevirapine in combination with nelfinavir in heavily pretreated HIV-1-infected patients: a prospective, open-label, controlled, randomized study.
Black, FT; Jensen-Fangel, S; Larsen, L; Obel, N; Thomsen, HF, 2001
)
0.9
" Efavirenz, DPC082, DPC083, DPC961, and DPC963 used in combination with the NRTIs zidovudine and lamivudine acted synergistically to inhibit RT activity in the HIV-1 RT enzyme assay and additively to slightly synergistically to inhibit HIV-1 (RF) replication in the yield reduction assay."( Potency of nonnucleoside reverse transcriptase inhibitors (NNRTIs) used in combination with other human immunodeficiency virus NNRTIs, NRTIs, or protease inhibitors.
Erickson-Viitanen, SK; King, RW; Klabe, RM; Reid, CD, 2002
)
0.31
"To evaluate the sustained efficacy of nevirapine in combination with two nucleoside analogues in the treatment of HIV-infected patients in routine clinical practice."( Sustained efficacy of nevirapine in combination with two nucleoside analogues in the treatment of HIV-infected patients: a 48-week retrospective multicenter study.
Allan, PS; Arumainayagam, J; Browning, M; Das, S; Harindra, V; Tobin, J; Wade, A; Yoganathan, K,
)
0.72
" To have any understanding of drug-drug interactions in HIV treatment we need to appreciate the importance of key pharmacological areas including: 1) how each drug in a regimen is eliminated; 2) the potential for a drug to either induce or inhibit metabolic enzymes and/or transporters; 3) the therapeutic index of each drug."( Pharmacokinetic drug interactions with nevirapine.
Back, D; Gibbons, S; Khoo, S, 2003
)
0.59
"Randomized, controlled, open-label trial of 233 protease inhibitor- and non-nucleoside reverse transcriptase inhibitor-naive HIV-infected patients allocated to a regimen of nelfinavir and nevirapine (1250/200 mg twice daily; n = 118) or ritonavir and saquinavir (400/400 mg twice daily; n = 115), both in combination with two nucleoside reverse transcriptase inhibitors."( A randomized trial comparing initial HAART regimens of nelfinavir/nevirapine and ritonavir/saquinavir in combination with two nucleoside reverse transcriptase inhibitors.
Gerstoft, J; Katzenstein, TL; Kirk, O; Lundgren, JD; Mathiesen, LR; Nielsen, H; Obel, N; Pedersen, C, 2003
)
0.75
"A regimen of nelfinavir/nevirapine had a favourable virological effect and tolerability over a 48-week period compared with ritonavir/saquinavir, when administered in combination with two nucleoside reverse transcriptase inhibitors."( A randomized trial comparing initial HAART regimens of nelfinavir/nevirapine and ritonavir/saquinavir in combination with two nucleoside reverse transcriptase inhibitors.
Gerstoft, J; Katzenstein, TL; Kirk, O; Lundgren, JD; Mathiesen, LR; Nielsen, H; Obel, N; Pedersen, C, 2003
)
0.86
"We have investigated the pharmacokinetics of nevirapine and paclitaxel in a patient who used both drugs concomitantly, as there are strong theoretical indications for a potential pharmacokinetic drug-drug interaction."( No pharmacokinetic drug-drug interaction between nevirapine and paclitaxel.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Mairuhu, AT; Schellens, JH, 2005
)
0.84
"Tenofovir disoproxil fumarate (DF) has been studied in combination with efavirenz in healthy volunteers and no interaction was found."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.54
" Six different groups were studied: 200 mg nevirapine twice daily, 400 mg nevirapine once daily, 600 mg efavirenz once daily, all without tenofovir DF (groups 1, 2, and 3, respectively), and the same groups with the drugs combined with tenofovir 300 mg once daily (groups 4, 5, and 6, respectively)."( Assessment of drug-drug interactions between tenofovir disoproxil fumarate and the nonnucleoside reverse transcriptase inhibitors nevirapine and efavirenz in HIV-infected patients.
Burger, DM; Droste, JA; Hekster, YA; Kearney, BP, 2006
)
0.8
"We assessed the 18-month effectiveness of short-course (sc) antiretroviral peripartum regimens combined with alternatives to prolonged breastfeeding to prevent mother-to-child transmission (MTCT) of HIV-1 in Abidjan, Côte d'Ivoire."( 18-month effectiveness of short-course antiretroviral regimens combined with alternatives to breastfeeding to prevent HIV mother-to-child transmission.
Becquet, R; Dabis, F; Dequae-Merchadou, L; Ekouevi, DK; Horo, A; Leroy, V; Rouet, F; Rouzioux, C; Sakarovitch, C; Timité-Konan, M; Tonwe-Gold, B; Viho, I, 2008
)
0.35
" Patients with HIV may also have simultaneous chronic medical conditions, resulting in the possibility of complex drug-drug interactions."( Possible antiretroviral therapy-warfarin drug interaction.
Fulco, PP; Higginson, RT; Zingone, MM, 2008
)
0.35
" These mt-QSARs offer also a good opportunity to construct drug-drug Complex Networks (CNs) that can be used to explore large and complex drug-viral species databases."( Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
Chou, KC; González-Díaz, H; Martinez de la Vega, O; Prado-Prado, FJ; Ubeira, FM; Uriarte, E, 2009
)
0.35
"To determine which NNRTI, EFV or NVP, is more efficacious when given in combination with two NRTIs as part of initial ART for HIV infection in adults and children."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.73
"Both drugs have equivalent efficacies in initial treatment of HIV infection when combined with two NRTIs, but different side effects."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.73
"We retrospectively evaluated the durability and reasons for discontinuation of nevirapine (NVP) in combination with a tenofovir (TDF) and emtricitabine (FTC) or lamivudine (3TC)-containing antiretroviral therapy (ART) regimen in an Australian outpatient setting."( Clinical experience with nevirapine combined with tenofovir plus emtricitabine or lamivudine-containing regimens in HIV-infected subjects.
Chan, DJ; Jeganathan, S; Maruszak, H; Smith, DE, 2011
)
0.9
" nevirapine on the same background, in naïve HIV-1-infected patients) study compared prospectively ritonavir-boosted atazanavir (ATZ/r) 300 mg/100 mg once daily (qd) with immediate release nevirapine (NVP) 200 mg twice daily or 400 mg qd, each combined with fixed-dose tenofovir 300 mg/emtricitabine 200 mg qd in 569 ARV-naïve HIV-1-infected patients."( Lipid profiles for nevirapine vs. atazanavir/ritonavir, both combined with tenofovir disoproxil fumarate and emtricitabine over 48 weeks, in treatment-naïve HIV-1-infected patients (the ARTEN study).
Andrade-Villanueva, J; Cairns, V; Clotet, B; de Rossi, L; Domingo, P; Gellermann, HJ; Podzamczer, D; Reiss, P; Rockstroh, JK; Soriano, V; Taylor, S, 2011
)
1.61
"ARTEN is a randomized, open-label, non-inferiority trial that compares nevirapine (NVP) 200 mg twice daily or 400 mg once daily to atazanavir/ritonavir (ATZ/r) 300 mg/100 mg once daily, each combined with fixed-dose tenofovir disoproxil fumarate (TDF) 300 mg/emtricitabine (FTC) 200 mg once daily, in antiretroviral-naive HIV-1 patients with CD4(+) T-cell counts <400 (men) and <250 cells/mm(3) (women)."( Nevirapine versus atazanavir/ritonavir, each combined with tenofovir disoproxil fumarate/emtricitabine, in antiretroviral-naive HIV-1 patients: the ARTEN Trial.
Andrade-Villanueva, J; Antunes, F; Arastéh, K; de Rossi, L; Di Perri, G; Domingo, P; Gellermann, H; Lutz, T; Migrone, H; Opravil, M; Podzamczer, D; Soriano, V; Taylor, S, 2011
)
2.05
"NVP demonstrated at week 48 non-inferior antiviral efficacy compared with ATZ/r when given along with TDF/FTC, despite more drug-related discontinuations with NVP than ATZ/r."( Nevirapine versus atazanavir/ritonavir, each combined with tenofovir disoproxil fumarate/emtricitabine, in antiretroviral-naive HIV-1 patients: the ARTEN Trial.
Andrade-Villanueva, J; Antunes, F; Arastéh, K; de Rossi, L; Di Perri, G; Domingo, P; Gellermann, H; Lutz, T; Migrone, H; Opravil, M; Podzamczer, D; Soriano, V; Taylor, S, 2011
)
1.81
"Efficacy results were consistent with the ARTEN study demonstrating that NVP was non-inferior to ATV/r when taken in combination with TDF/FTC."( A randomised comparison of safety and efficacy of nevirapine vs. atazanavir/ritonavir combined with tenofovir/emtricitabine in treatment-naïve patients.
Bhatti, L; Conner, C; Dejesus, E; Mills, A; Storfer, S, 2011
)
0.62
"Drugs most likely to interact with combined oral contraceptives, transdermal and implant contraceptives include protease inhibitors, the NNRTIs efavirenz and nevirapine, and cobicistat-boosted elvitegravir."( Drug interactions between antiretrovirals and hormonal contraceptives.
Hills-Nieminen, C; Tseng, A, 2013
)
0.59
"Compared with zidovudine-lamivudine, the use of tenofovir-lamivudine or emtricitabine in combination with nevirapine was a strong predictor of virologic failure in our cohort, which was not explained by other risk factors or criteria for regimen selection."( Superior Effectiveness of Zidovudine Compared With Tenofovir When Combined With Nevirapine-based Antiretroviral Therapy in a Large Nigerian Cohort.
Agbaji, OO; Darin, KM; Eisen, G; Gashau, W; Kanki, PJ; Meloni, ST; Murphy, RL; Nkado, R; Okonkwo, P; Onwujekwe, DI; Rawizza, HE; Scarsi, KK; Tchetgen Tchetgen, EJ, 2016
)
0.87
" Single-dose drug-drug interaction studies found no significant interactions with nevirapine or lopinavir/ritonavir, but these findings could be misleading, especially because of bedaquiline's long terminal t1/2."( Drug-drug interactions between bedaquiline and the antiretrovirals lopinavir/ritonavir and nevirapine in HIV-infected patients with drug-resistant TB.
Conradie, F; Hughes, J; Maartens, G; McIlleron, H; Pandie, M; Siwendu, S; Variava, E; Wiesner, L, 2016
)
0.88
"To determine which non-nucleoside reverse transcriptase inhibitor, either EFV or NVP, is more effective in suppressing viral load when given in combination with two nucleoside reverse transcriptase inhibitors as part of initial antiretroviral therapy for HIV infection in adults and children."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.8
"Both drugs have similar benefits in initial treatment of HIV infection when combined with two NRTIs."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.8
"To investigate the genetic contribution to this previously observed drug-drug interaction through studying SNPs in genes known to be involved in efavirenz, nevirapine or etonogestrel metabolism in the same group of women."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.93
"This study demonstrates the influence of pharmacogenetics on the extent of drug-drug interactions between etonogestrel and efavirenz- or nevirapine-based ART."( Effect of patient genetics on etonogestrel pharmacokinetics when combined with efavirenz or nevirapine ART.
Achilles, SL; Chappell, CA; Chen, BA; Lamorde, M; Matovu, J; Nakalema, S; Neary, M; Owen, A; Scarsi, KK; Siccardi, M, 2019
)
0.94

Bioavailability

Nevirapine (NVP) is used for the management of HIV/AIDS. Bioavailability of lumefantrine, sulfadoxine, pyrimethamine, lopinavir, and efavirenz was decreased in severely malnourished patients.

ExcerptReferenceRelevance
" Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel."( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993
)
0.29
" The relative bioavailability (F) of ZDV and ddI in the triple combination compared to that in the double combination was also evaluated."( Population pharmacokinetics of nevirapine, zidovudine, and didanosine in human immunodeficiency virus-infected patients. The National Institute of Allergy and Infectious Diseases AIDS Clinical Trials Group Protocol 241 Investigators.
D'Aquila, RT; Fischl, MA; Hirsch, MS; Hughes, MD; Johnson, VA; Myers, M; Sheiner, LB; Sommadossi, JP; Zhou, XJ, 1999
)
0.59
" Preliminary pharmacokinetics in rats showed that compound 18 is orally bioavailable and penetrates well into the brain."( Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Bäckbro, K; Engelhardt, P; Fridborg, K; Högberg, M; Johansson, NG; Kangasmetsä, J; Lövgren, S; Noréen, R; Oberg, B; Sahlberg, BL; Sahlberg, C; Unge, T; Vrang, L; Zhang, H, 1999
)
0.3
"The results of two randomized, single-dose, crossover bioavailability studies are presented which describe the pharmacokinetics and oral bioavailability of nevirapine, a novel nonnucleoside antiretroviral drug."( Single dose pharmacokinetics and bioavailability of nevirapine in healthy volunteers.
Cappola, M; Hawi, A; Lamson, MJ; MacGregor, TR; Pav, JW; Robinson, P; Rowland, L; Sabo, JP, 1999
)
0.75
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" Nevirapine is well absorbed during labor, and sufficient drug for prophylaxis against perinatal transmission crosses the placenta if an oral dose is administered to the mother at least 1 hour before delivery."( Antiretroviral pharmacology in pregnant women and their newborns.
Mirochnick, M, 2000
)
1.22
" Through an integrated effort involving synthesis, docking studies, and biological and pharmacokinetic evaluation, we investigated the structural dependence of the poor bioavailability and rapid clearance within the thioureidic series of antivirals."( Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
Aiello, F; Armaroli, S; Bergamini, A; Bolacchi, F; Bongiovanni, B; Caccia, S; Campiani, G; Capozzi, M; Coletta, M; Fabbrini, M; Garofalo, A; Greco, G; Guiso, G; Maga, G; Marini, S; Morelli, E; Nacci, V; Novellino, E; Ramunno, A; Spadari, S; Ventura, L, 2001
)
0.31
" Population pharmacokinetic parameters (apparent clearance (CL/F), volume of distribution (V/F), absorption rate constant (k a)) were estimated, as were interindividual, interoccasion, and residual variability in the pharmacokinetics."( Population pharmacokinetics of nevirapine in an unselected cohort of HIV-1-infected individuals.
Beijnen, JH; de Maat, MM; Huitema, AD; Meenhorst, PL; Mulder, JW; van Gorp, EC, 2002
)
0.6
" Population pharmacokinetic parameters [clearance (CL/F), volume of distribution (V/F), absorption rate constant (ka)] and interindividual (IIV) and interoccasion variability (IOV) were estimated."( Race is not associated with nevirapine pharmacokinetics.
Beijnen, JH; de Maat, MM; Huitema, AD; Mulder, JW; Nellen, JF; Prins, JM; Wit, FW, 2004
)
0.62
" Volume of distribution and absorption rate constant were 77."( Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, J; MacGregor, TR; van Leth, F, 2005
)
1.77
"Ideally, an anti-HIV drug should (1) be highly active against wild-type and mutant HIV without allowing breakthrough; (2) have high oral bioavailability and long elimination half-life, allowing once-daily oral treatment at low doses; (3) have minimal adverse effects; and (4) be easy to synthesize and formulate."( In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
Andries, K; Arnold, E; Bohets, H; Clark, AD; Daeyaert, F; Das, K; de Béthune, MP; De Clerck, F; de Jonge, M; De Knaep, F; Frenkel, YV; Guillemont, J; Heeres, J; Hughes, SH; Janssen, PA; Koymans, L; Kukla, M; Lampo, A; Lewi, PJ; Ludovici, D; Medaer, B; Pasquier, E; Pauwels, R; Stoffels, P; Vinkers, M; Williams, P, 2005
)
0.33
" Our findings suggest that decreased bioavailability of nevirapine because of rifampicin coadministration could be overcome by increasing the dose of nevirapine from 200 to 300 mg twice daily without short-term adverse events."( Increasing nevirapine dose can overcome reduced bioavailability due to rifampicin coadministration.
Hemanthkumar, AK; Kumaraswami, V; Narendran, G; Padmapriyadarsini, C; Raja, K; Rajasekaran, S; Ramachandran, G; Sathishnarayan, S; Sukumar, B; Swaminathan, S, 2006
)
0.97
"An open-label, balanced, randomized, 2-treatment, 2-period, 2-sequence, single-dose, crossover bioavailability study was conducted in 40 subjects with 21-day washout period between each treatment."( Nevirapine/lamivudine/stavudine as a combined-formulation tablet: bioequivalence study compared with each component administered concurrently under fasting condition.
Garg, M; Monif, T; Singla, AK; Tippabhotla, SK; Vijan, T, 2006
)
1.78
"Nevirapine has been widely used in pregnancy for its efficacy, low pill burden, bioavailability and rapid transplacental transfer."( Safety of nevirapine in pregnancy.
Anderson, J; de Ruiter, A; Edwards, SG; Hay, P; McDonald, C; Natarajan, U; Pym, A; Taylor, GP; Velisetty, P; Welch, J, 2007
)
2.18
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
0.34
" There are indications that piperine inhibits, rather than stimulates, drug metabolism in most cases, thus increasing the bioavailability and effect of some drugs."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.59
"This pilot study provided evidence for enhanced bioavailability of nevirapine when administered with piperine."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.83
"Hypoxis hemerocallidea and l-canavanine interact with the efflux of nevirapine across intestinal epithelial cells and therefore can potentially increase the bioavailability of this antiretroviral drug when taken concomitantly."( Impact of traditional medicinal plant extracts on antiretroviral drug absorption.
Brown, D; Brown, L; Hamman, JH; Heyneke, O; van Wyk, JP, 2008
)
0.58
"4% and reduced the absorption rate constant (k(a)) by almost sixfold."( Population pharmacokinetics of nevirapine in combination with rifampicin-based short course chemotherapy in HIV- and tuberculosis-infected South African patients.
Cohen, K; Elsherbiny, D; Jansson, B; McIlleron, H; Simonsson, US; Smith, P, 2009
)
0.64
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
"This study compared the pharmacokinetics and relative bioavailability of a test and reference formulation of nevirapine 200-mg tablets after single oral doses in healthy Chinese men to meet regulatory criteria for marketing of the new generic formulation."( Relative bioavailability of two formulations of nevirapine 200-mg tablets in healthy Chinese male volunteers: a single-dose, randomized-sequence, open-label, two-way crossover study.
Hu, Y; Yang, X; Yu, C; Zhang, Q; Zhu, Y; Zou, J, 2010
)
0.83
" Mean relative bioavailability was 103."( Relative bioavailability of two formulations of nevirapine 200-mg tablets in healthy Chinese male volunteers: a single-dose, randomized-sequence, open-label, two-way crossover study.
Hu, Y; Yang, X; Yu, C; Zhang, Q; Zhu, Y; Zou, J, 2010
)
0.62
" Therefore, this investigation aimed at screening the effects of short term and chronic exposure of sutherlandia on oral bioavailability and pharmacokinetics of nevirapine (NVP), a non-nucleoside reverse transcriptase inhibitor, in Sprague Dawley rats."( Effect of short term and chronic administration of Sutherlandia frutescens on pharmacokinetics of nevirapine in rats.
Earla, R; Folk, WR; Kwatra, D; Mandava, NK; Minocha, M; Mitra, AK; Pal, D, 2011
)
0.78
" However, there are no studies about its bioavailability in rats and hardly any about its pharmacokinetic."( Bioavailability of nevirapine in rats after oral and subcutaneous administration, in vivo absorption from gastrointestinal segments and effect of bile on its absorption from duodenum.
Peris, JE; Usach, I, 2011
)
0.7
"The aim of this study was to investigate the steady-state bioavailability of 2 once-daily tablet formulations of NVP XR (containing 25% or 20% hypromellose; NVP XR25 and NVP XR20, respectively) in 400- or 300-mg tablets compared with twice-daily immediate-release (IR) NVP 200-mg tablets."( Bioavailability of extended-release nevirapine 400 and 300 mg in HIV-1: a multicenter, open-label study.
Arasteh, K; Battegay, M; Berger, F; Bogner, JR; Livrozet, JM; Macha, S; Mossdorf, E; Plettenberg, A; Quinson, AM; Robinson, P; Stern, J; Witt, MD; Yong, CL; Zhang, W, 2011
)
0.64
" The relative bioavailability of NVP XR25 was greater compared with that of NVP XR20."( Bioavailability of extended-release nevirapine 400 and 300 mg in HIV-1: a multicenter, open-label study.
Arasteh, K; Battegay, M; Berger, F; Bogner, JR; Livrozet, JM; Macha, S; Mossdorf, E; Plettenberg, A; Quinson, AM; Robinson, P; Stern, J; Witt, MD; Yong, CL; Zhang, W, 2011
)
0.64
"Extent of bioavailability was lower and t(max,ss) was delayed with all NVP XR formulations compared with NVP IR."( Bioavailability of extended-release nevirapine 400 and 300 mg in HIV-1: a multicenter, open-label study.
Arasteh, K; Battegay, M; Berger, F; Bogner, JR; Livrozet, JM; Macha, S; Mossdorf, E; Plettenberg, A; Quinson, AM; Robinson, P; Stern, J; Witt, MD; Yong, CL; Zhang, W, 2011
)
0.64
" Higher MRT values of surface coated nanosuspension in brain, liver and spleen as compared to pure drug solution ensured enhanced bioavailability and prolonged residence of the drug at the target site."( Surface modified nevirapine nanosuspensions for viral reservoir targeting: In vitro and in vivo evaluation.
Shegokar, R; Singh, KK, 2011
)
0.71
" We report the bioavailability and short-term safety of a novel paediatric FDC tablet of zidovudine (ZDV)/lamivudine (3TC)/nevirapine (NVP; 30/15/28 mg) in HIV-infected children."( Pharmacokinetics and safety of a new paediatric fixed-dose combination of zidovudine/lamivudine/nevirapine in HIV-infected children.
Aurpibul, L; Capparelli, E; Chokephaibulkit, K; Cressey, TR; Eksaengsri, A; Hongsiriwon, S; Kabat, B; Limwongse, C; McIntosh, K; Muresan, P; Ngampiyaskul, C; Sirisanthana, V; Smith, ME; Toye, M; Wittawatmongkol, O; Yogev, R, 2011
)
0.79
" Concomitant antitubercular treatment including rifampicin typically decreased bioavailability by 39%, with significant between-subject variability."( Integration of data from multiple sources for simultaneous modelling analysis: experience from nevirapine population pharmacokinetics.
Barnes, KI; Cohen, K; Denti, P; Huitema, A; Karlsson, MO; Kredo, T; Nachega, JB; Svensson, E; van der Walt, JS, 2012
)
0.6
" The Triomune fixed-dose tablet was an independent predictor of bioavailability compared to the liquid and other tablet formulations."( Nevirapine exposure with WHO pediatric weight band dosing: enhanced therapeutic concentrations predicted based on extensive international pharmacokinetic experience.
Acosta, EP; Aweeka, FT; Burger, D; Capparelli, EV; Cressey, TR; Kabamba, D; Nikanjam, M; Spector, SA, 2012
)
1.82
" Subjects taking concomitant PIs exhibited increases in CsA and TAC exposure (AUC/dose) due to the increased apparent oral bioavailability and decreased apparent oral clearance."( Changes in clearance, volume and bioavailability of immunosuppressants when given with HAART in HIV-1 infected liver and kidney transplant recipients.
Barin, B; Benet, L; Browne, M; Carlson, L; Christians, U; Floren, L; Frassetto, L; Roland, M; Stock, P; Wolfe, A, 2013
)
0.39
" Oral bioavailability of nevirapine SEDDS was checked by using rat model."( Role of lipid-based excipients and their composition on the bioavailability of antiretroviral self-emulsifying formulations.
Chudasama, A; Nivsarkar, M; Patel, V; Shishoo, C; Vasu, K, 2015
)
0.72
" Finally, oral bioavailability of the NVP-loaded micellar systems (2mg/mL) was assessed in male Wistar rats (8mg/kg) and compared with a pediatric commercially available formulation (Viramune(®))."( Enhanced oral bioavailability of nevirapine within micellar nanocarriers compared with Viramune(®).
Bernabeu, E; Chiappetta, DA; Cohen, L; Höcht, C; Lepera, L; Moretton, MA; Taira, C, 2014
)
0.68
" Pharmacokinetic analysis of the rat plasma NVP concentration-time data allowed absorption rate constants to be calculated."( Pharmacokinetics of injectable, long-acting nevirapine for HIV prophylaxis in breastfeeding infants.
Baum, MM; Beliveau, M; Cortez, JM; Moss, JA; Quintero, R; Smith, TJ, 2015
)
0.68
" However, the data obtained from IDR testing indicate that dissolution is the critical factor for the bioavailability of this drug."( Compatibility studies of nevirapine in physical mixtures with excipients for oral HAART.
de Oliveira, GG; Ferraz, HG; Severino, P; Souto, EB, 2013
)
0.69
" Compared to RRC, Ugandan children exhibited reduced bioavailability of EFV and LPV; 11% (P=0."( The effect of malnutrition on the pharmacokinetics and virologic outcomes of lopinavir, efavirenz and nevirapine in food insecure HIV-infected children in Tororo, Uganda.
Achan, J; Aweeka, F; Bartelink, IH; Capparelli, E; Charlebois, E; Dorsey, G; Gingrich, D; Havlir, D; Jullien, V; Kamya, M; Plenty, A; Ruel, T; Savic, RM; Scherpbier, HJ; Young, SL, 2015
)
0.63
" Patients in the EFV-arm but not in the NVP-arm had significantly lower lumefantrine bioavailability compared to that in the control-arm."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
"Co-treatment of AL with EFV-based ART but not NVP-based ART significantly reduces lumefantrine bioavailability and consequently total exposure."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
"It was concluded that the concept of mixed hydrotropic solid dispersion is a safe, novel and cost-effective technique for enhancing the bioavailability of poorly water-soluble drugs by dissolving the drug in a nonionized form."( Improving the solubility of nevirapine using A hydrotropy and mixed hydrotropy based solid dispersion approach.
Awasthi, R; Dua, K; Kamate, VJ; Madan, JR,
)
0.43
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Nevirapine (NVP) is used for the management of HIV/AIDS but must be dosed frequently, exhibits unpredictable bioavailability and a side effect profile that includes hepato- and dermo-toxicity."( Preformulation characterization and identification of excipients for nevirapine loaded niosomes.
Walker, RB; Witika, BA, 2021
)
2.3
" Bioavailability of lumefantrine, sulfadoxine, pyrimethamine, lopinavir, and efavirenz was decreased in severely malnourished patients, but increased for the P-glycoprotein substrates abacavir, saquinavir, nevirapine, and ivermectin."( Influence of Malnutrition on the Pharmacokinetics of Drugs Used in the Treatment of Poverty-Related Diseases: A Systematic Review.
Beijnen, JH; Dorlo, TPC; Huitema, ADR; Verrest, L; Wilthagen, EA, 2021
)
0.81
" Proportionate changes in CL/F and V/F might indicate a primary effect on bioavailability (F) rather than two separate effects."( Findings from a pilot study of buprenorphine population pharmacokinetics: A potential effect of HIV on buprenorphine bioavailability.
Bart, G; Brundage, RC; Giang, LM; Jaber, M; Korthuis, PT, 2022
)
0.72

Dosage Studied

Study compared the efficacy and safety of the new nevirapine extended-release (NVP XR) formulation dosed once daily with NVP immediate release (IR) twice daily in treatment-naive patients. Plasma trough levels of nelfinavir (NFV) and saquinavir (SQV), in a twice daily dosing regimen, were above the protein-corrected IC(95) in most patients.

ExcerptRelevanceReference
" Good oral bioavailability was observed in rhesus monkeys upon oral dosing of 1 as a suspension in methocel."( 5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
Balani, SK; Ciccarone, TM; Condra, JH; Emini, EA; Goldman, ME; Greenlee, WJ; Kauffman, LR; MacTough, SC; Rooney, CS; Williams, TM, 1993
)
0.29
" Clearance was more rapid in chronic dosing studies than predicted by single-dose studies and was more rapid in younger children than in adolescent children."( Pharmacokinetics, safety, and activity of nevirapine in human immunodeficiency virus type 1-infected children.
Bryson, Y; Cort, S; Lamson, M; Luzuriaga, K; McSherry, G; Robinson, J; Scott, G; Stechenberg, B; Sullivan, JL, 1996
)
0.56
" This small-animal model should be particularly useful in the preclinical prioritization of lead compounds within a common chemical class, in the evaluation of alternative in vivo dosing regimens, and in the determination of appropriate combination therapy in vivo."( Use of standardized SCID-hu Thy/Liv mouse model for preclinical efficacy testing of anti-human immunodeficiency virus type 1 compounds.
Charpiot, B; Datema, R; Hincenbergs, M; Kaneshima, H; Linquist, V; McCune, JM; Moreno, MB; Rabin, L; Seifert, J; Warren, S, 1996
)
0.29
"Blood samples were obtained at 0, 1, 2, 3, 4, 6 and 8 h after dosing on both study days."( The pharmacokinetics of combination therapy with nelfinavir plus nevirapine.
Back, DJ; Barry, MG; Breckenridge, AM; Halifax, KL; Merry, C; Mulcahy, F; Ryan, M; Tjia, JF, 1998
)
0.54
" In the absence of therapeutic drug monitoring we suggest that an increase in the standard NFV dosage of 750 mg three times daily will be required to ensure satisfactory NFV plasma concentrations, thereby maintaining antiviral efficacy."( The pharmacokinetics of combination therapy with nelfinavir plus nevirapine.
Back, DJ; Barry, MG; Breckenridge, AM; Halifax, KL; Merry, C; Mulcahy, F; Ryan, M; Tjia, JF, 1998
)
0.54
" Following maternal dosing with 200 mg during labor, concentrations exceeding 100 ng/mL (10 times the in vitro IC50) were achieved in the newborns."( Pharmacokinetics of nevirapine in human immunodeficiency virus type 1-infected pregnant women and their neonates. Pediatric AIDS Clinical Trials Group Protocol 250 Team.
Beckerman, K; Fenton, T; Gagnier, P; Gwynne, M; Jimenez, E; Mirochnick, M; Pav, J; Siminski, S; Spector, SA; Sperling, RS; Sullivan, JL; Yogev, R, 1998
)
0.62
" These data suggest that indinavir dosing should be dependent on drug exposure and not on cotherapy with nevirapine."( Antiviral effect and pharmacokinetic interaction between nevirapine and indinavir in persons infected with human immunodeficiency virus type 1.
Dusek, A; Hall, DB; Lamson, M; Murphy, RL; Myers, M; Sommadossi, JP, 1999
)
0.76
"The administration of a single dose of nevirapine to women during labor and to their newborns at 72 h was well tolerated and showed potent antiretroviral activity in the women at 1 week after dosing without rebound above baseline 6 weeks after a single dose."( A phase I/II study of the safety and pharmacokinetics of nevirapine in HIV-1-infected pregnant Ugandan women and their neonates (HIVNET 006).
Allen, M; Bagenda, D; Dransfield, K; Elliott, T; Fleming, T; Fowler, MG; Guay, LA; Hom, D; Horton, S; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, L; Murarka, A; Musoke, P; Nakabiito, C; Pav, JW, 1999
)
0.82
" Although the currently used protease inhibitors (PIs) may undergo more rapid rates of metabolism because NVP induces CYP3A, No dosage adjustments are required when NVP is taken in combination with PIs so far."( [Antiretroviral agent nevirapine: its pharmacological action and potential for clinical use].
Osugi, T; Takeuchi, S, 1999
)
0.62
"To investigate and to compare the steady-state plasma pharmacokinetics of nevirapine in a dosing regimen of 400 mg once daily versus 200 mg twice daily in HIV-1-infected individuals."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.81
" Differences in these pharmacokinetic parameters for the two dosing regimens were tested using ANOVA."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.58
"These data show that the daily exposure to nevirapine, as measured by the plasma AUC[24h], is not different between a 400 mg once daily and a 200 mg twice daily dosing regimen."( The steady-state pharmacokinetics of nevirapine during once daily and twice daily dosing in HIV-1-infected individuals.
Beijnen, JH; Danner, SA; Foudraine, NA; Hoetelmans, RM; Kwakkelstein, MO; Lange, JM; Meenhorst, PL; Mulder, JW; Reiss, P; van Heeswijk, RP; Veldkamp, AI; Wit, FW, 2000
)
0.84
" Oral dosing is administered three times daily for delavirdine (DLV), twice daily for nevirapine (NVP), and once daily for efavirenz (EFV)."( Clinical uses of non-nucleoside reverse transcriptase inhibitors.
Harris, M; Montaner, JS,
)
0.35
" RT sequences from plasma collected prior to NVP dosing were also analyzed."( Identification of the K103N resistance mutation in Ugandan women receiving nevirapine to prevent HIV-1 vertical transmission.
Becker-Pergola, G; Eshleman, SH; Fowler, MG; Guay, LA; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, LM; Mracna, M; Musoke, P, 2000
)
0.54
" Pharmacokinetic data suggested that a more prolonged exposure to NVP after dosing may favor selection of NVP-resistant HIV-1."( Identification of the K103N resistance mutation in Ugandan women receiving nevirapine to prevent HIV-1 vertical transmission.
Becker-Pergola, G; Eshleman, SH; Fowler, MG; Guay, LA; Jackson, JB; Mirochnick, M; Mmiro, F; Mofenson, LM; Mracna, M; Musoke, P, 2000
)
0.54
"NVP reaches concentrations in the semen approximately 60% of those in the blood plasma throughout the 12 h dosing period."( Concentrations of nevirapine, lamivudine and stavudine in semen of HIV-1-infected men.
Drake, SM; Hoetelmans, RM; Pillay, D; Taylor, S; van Heeswijk, RP; White, DJ; Workman, J, 2000
)
0.64
" Dosing regimens must take into account developmental changes in clearance and appropriate scaling for size."( Antiretroviral pharmacology in pregnant women and their newborns.
Mirochnick, M, 2000
)
0.31
" Plasma trough levels of nelfinavir (NFV) and saquinavir (SQV), in a twice daily dosing regimen, were above the protein-corrected IC(95) in most patients despite the addition of an enzymatic inducer such as nevirapine, and peak levels were 2- and 5-fold increased with respect to standard doses."( Efficacy, tolerance, and pharmacokinetics of the combination of stavudine, nevirapine, nelfinavir, and saquinavir as salvage regimen after ritonavir or indinavir failure.
Antela, A; Casado, JL; Dehertogh, P; Dronda, F; Hertogs, K; Martí-Belda, P; Moreno, S; Sabido, R, 2001
)
0.73
" Clinicians should use recommended PEP guidelines and dosing instructions to reduce the risk for serious adverse events."( Serious adverse events attributed to nevirapine regimens for postexposure prophylaxis after HIV exposures--worldwide, 1997-2000.
, 2001
)
0.58
" The pharmacokinetics of nevirapine in plasma and saliva during a dosing interval was assessed in HIV-1-infected patients taking nevirapine (200 mg twice daily) to explore the relation between the concentration of nevirapine in plasma and saliva."( Saliva as an alternative body fluid for therapeutic drug monitoring of the nonnucleoside reverse transcription inhibitor nevirapine.
Beijnen, JH; Hoetelmans, RM; Lange, JM; Meenhorst, PL; Mulder, JW; van Heeswijk, RP; Veldkamp, AI, 2001
)
0.82
" Information on each drug, such as the name of the drug, the dosage normally prescribed, and cost of treatment is listed."( What they say about: non-nucleoside drugs.
,
)
0.13
" Several studies of regimens that include protease inhibitors compare dosing twice daily to three times a day."( Antivirals update.
, 1998
)
0.3
" Dosage and cost data are included."( What they say about non-nucleoside drugs.
,
)
0.13
" Finally, nevirapine-containing regimens have a simpler dosing schedule, and this facilitates high adherence and improves QOL."( Antiretroviral treatment simplification with nevirapine in protease inhibitor-experienced patients with hiv-associated lipodystrophy: 1-year prospective follow-up of a multicenter, randomized, controlled study.
Balagué, M; Bonjoch, A; Clotet, B; Domingo, P; Francia, E; Fumaz, CR; Gel, S; Johnston, S; Lange, J; Negredo, E; Paredes, R; Romeu, J; Ruiz, L, 2001
)
0.97
"Limited data are available on antiretroviral drug concentrations in seminal plasma during a dosing interval."( Pharmacokinetic profiles of nevirapine and indinavir in various fractions of seminal plasma.
de Vries, JW; Hoetelmans, RM; Lange, JM; Prins, JM; Repping, S; van Praag, RM, 2001
)
0.6
" Given that the lowest trough serum concentration of nevirapine exceeded by more than 40 times the protein binding adjusted median infective dose (IC(50)) of wild-type HIV in all patients, we suggest that there is no need to increase nevirapine dosage when it is given with rifampicin."( Pharmacokinetic interaction between nevirapine and rifampicin in HIV-infected patients with tuberculosis.
Crespo, M; Falco, V; Lopez, RM; Ocaña, I; Pahissa, A; Pou, L; Ribera, E; Ruiz, I, 2001
)
0.84
"The objective of this study was to develop and validate a limited sampling strategy (LSS) that allows accurate and precise estimation of the area under the plasma concentration versus time curve (AUC) of nevirapine, when used in the licensed dosage of 200 mg twice daily."( Limited sampling strategies for the estimation of the systemic exposure to the HIV-1 nonnucleoside reverse transcriptase inhibitor nevirapine.
Beijnen, JH; Hoetelmans, RM; Lange, JM; Meenhorst, PL; Mulder, JW; van Heeswijk, RP; Veldkamp, AI, 2001
)
0.7
"As part of an on-going clinical trial in Malawi, infants born to women who received (early presenters) or did not receive (late presenters) standard intrapartum nevirapine (NVP) dosing were randomized to receive orally either single dose NVP alone or NVP plus zidovudine (twice daily for 1 week)."( Effect of HIV-1 antiretroviral prophylaxis on hepatic and hematological parameters of African infants.
Broadhead, R; Fiscus, S; Gibbons, A; Hoover, D; Kumwenda, N; Lema, V; Liomba, G; Mukiibi, J; Taha, TE, 2002
)
0.51
"The complexity of highly active antiretroviral therapy (HAART), with multiple medications, formulations, and dosing intervals, makes adherence challenging."( Reported adherence as a determinant of response to highly active antiretroviral therapy in children who have human immunodeficiency virus infection.
Johnson, GM; Krogstad, PA; Lee, S; Mohan, K; Morse, EV; Nachman, S; Stanley, K; Van Dyke, RB; Wiznia, A, 2002
)
0.31
" Nevirapine was administered at the lead-in dosage of 200 mg once daily."( Randomized, controlled study of the effects of a short course of prednisone on the incidence of rash associated with nevirapine in patients infected with HIV-1.
Cahn, P; Casssetti, LI; Gigliotti, M; Hall, DB; Losso, M; McDonough, M; Montaner, JS; Robinson, PA; Wruck, J; Zala, C, 2003
)
1.44
" Lower predose nevirapine concentrations were associated with lower cord blood concentrations and a shorter interval between maternal dosing and delivery."( Predose infant nevirapine concentration with the two-dose intrapartum neonatal nevirapine regimen: association with timing of maternal intrapartum nevirapine dose.
Blanchard, S; Culnane, M; Cunningham, CK; Dorenbaum, A; Gelber, RD; Mirochnick, M; Mofenson, L; Sullivan, JL, 2003
)
1.02
"Infants born less than 2 hours after maternal nevirapine dosing during labor should receive a dose of nevirapine immediately after birth in addition to the standard infant dose at 48 to 72 hours."( Predose infant nevirapine concentration with the two-dose intrapartum neonatal nevirapine regimen: association with timing of maternal intrapartum nevirapine dose.
Blanchard, S; Culnane, M; Cunningham, CK; Dorenbaum, A; Gelber, RD; Mirochnick, M; Mofenson, L; Sullivan, JL, 2003
)
0.93
" Nevirapine was dosed according to the manufacturer's guidelines."( Nevirapine use in HIV-1-infected children.
Ball, C; Dumont, G; Gibb, DM; Lyall, H; Novelli, V; Sharland, M; Tudor-Williams, G; Verweel, G; Walters, S; Wilkins, E, 2003
)
2.67
" NFV dosed at 55 mg/kg BID in children who are <30 kg provides comparable exposure to that measured in children who are >25 kg and receiving NFV 30 mg/kg TID."( Nelfinavir pharmacokinetics in stable human immunodeficiency virus-positive children: Pediatric AIDS Clinical Trials Group Protocol 377.
Aweeka, FT; Floren, LC; Hayashi, S; Jayewardene, A; Johnson, G; Krogstad, P; Nachman, S; Stanley, K; Wiznia, A, 2003
)
0.32
" Using the recommended lead-in dosing schedule in conjunction with good health care management, this adverse event can be controlled in the vast majority of patients."( Defining the toxicity profile of nevirapine and other antiretroviral drugs.
Murphy, RL, 2003
)
0.6
" Following maternal dosing with 200 mg NVP orally at onset of labor, breast-feeding infants were randomized within 48 hours of birth to 1 of 3 regimens: arm 1, NVP given OW (4 mg/kg from birth to 14 days, upward arrow to 8 mg/kg from 15 days to 24 weeks), arm 2, NVP given TW (4 mg/kg from birth to 14 days, upward arrow to 8 mg/kg from 15 days to 24 weeks), and arm 3, NVP given OD (2 mg/kg from birth to 14 days, upward arrow to 4 mg/kg from 15 days to 24 weeks)."( Safety and trough concentrations of nevirapine prophylaxis given daily, twice weekly, or weekly in breast-feeding infants from birth to 6 months.
Abdool Karim, SS; Bassett, MT; Coovadia, HM; Emel, L; Eshleman, SH; Fleming, T; George, K; Jones, SA; Katzenstein, DA; Maldonado, Y; Maponga, CC; Mirochnick, MM; Mofenson, LM; Mwatha, A; Shetty, AK; Wells, J, 2003
)
0.59
" Labor ward dosing to enhance nevirapine coverage should be considered as an adjunct to antenatal nevirapine administration for prevention of mother-to-child transmission of HIV."( Universal nevirapine upon presentation in labor to prevent mother-to-child HIV transmission in high prevalence settings.
Acosta, EP; Aldrovandi, GM; Goldenberg, RL; Kumwenda, R; Sinkala, M; Stout, JP; Stringer, JS; Vermund, SH, 2004
)
1.01
" PI-based therapies often fail due to poor adherence caused by heavy pill burden, complex dosing schedules and undesirable side effects."( Clinical utility of current NNRTIs and perspectives of new agents in this class under development.
Hamatake, R; Hong, Z; Zhang, Z, 2004
)
0.32
" Adjusting dosage by means of therapeutic drug monitoring would appear to be a reasonable way of maximising patient benefit from treatment."( Follow-up measurements of Nevirapine plasma levels over a prolonged period.
Ebigbo, A; Klinker, H; Knipper, A; Langmann, P; Sienz, M; Winzer, R; Zilly, M, 2004
)
0.62
"In antiretroviral-experienced subjects with sustained viral suppression, dual therapy with NVP plus LPV/rtv at standard dosage was as potent and safe as standard-of-care HAART at 48 weeks of follow-up."( Lopinavir/ritonavir plus nevirapine as a nucleoside-sparing approach in antiretroviral-experienced patients (NEKA study).
Burger, D; Clotet, B; Côté, H; López, S; Martínez, E; Miró, O; Moltó, J; Montaner, J; Negredo, E; Puig, J; Rey-Joly, C; Ribalta, J; Ruiz, L; Salazar, J, 2005
)
0.63
"The median NVP level fell to 68 ng/mL (range: <50-228, n = 43) 8 to 14 days after dosing and to 51 ng/mL (range: <50-166, n = 25) between 15 and 21 days."( Persistence of nevirapine exposure during the postpartum period after intrapartum single-dose nevirapine in addition to zidovudine prophylaxis for the prevention of mother-to-child transmission of HIV-1.
Capparelli, E; Cressey, TR; Jackson, JB; Jourdain, G; Kunkeaw, S; Lallemant, MJ; Mirochnick, M; Musoke, P, 2005
)
0.68
" Our objective was to determine intracellular (or cell-associated) nevirapine concentrations over the full dosing interval and to relate protein binding and P-glycoprotein (P-gp) expression to intracellular exposure."( Intracellular and plasma pharmacokinetics of nevirapine in human immunodeficiency virus-infected individuals.
Almond, LM; Back, DJ; Bonington, A; Dalton, M; Edirisinghe, D; Khoo, SH, 2005
)
0.82
"054) and remained unchanged over the dosing interval."( Intracellular and plasma pharmacokinetics of nevirapine in human immunodeficiency virus-infected individuals.
Almond, LM; Back, DJ; Bonington, A; Dalton, M; Edirisinghe, D; Khoo, SH, 2005
)
0.59
"The intracellular accumulation of nevirapine was low, did not change over the dosing interval, and was not related to protein binding."( Intracellular and plasma pharmacokinetics of nevirapine in human immunodeficiency virus-infected individuals.
Almond, LM; Back, DJ; Bonington, A; Dalton, M; Edirisinghe, D; Khoo, SH, 2005
)
0.87
" The method has been successfully used to analyze commercial solid dosage form to assess the chromatographic performance of SFC system."( Effect of system variables involved in packed column SFC of nevirapine as model analyte using response surface methodology: application to retention thermodynamics, solute transfer kinetic study and binary diffusion coefficient determination.
Agrawal, H; Kaul, N; Mahadik, KR; Paradkar, AR, 2005
)
0.57
" Daily drug dosage was 250 or 400 mg didanosine, 300mg lamivudine and 400 mg nevirapine."( Efficacy and safety of once-daily combination therapy with didanosine, lamivudine and nevirapine in antiretroviral-naive HIV-infected patients.
Blanco, JL; Crespo, M; Deig, E; Falcó, V; González, A; Miró, JM; Ocaña, I; Pahissa, A; Pedrol, E; Ribera, E; Rodríguez-Pardo, D; Rubio, M; Soler, A, 2005
)
0.78
" One patient erroneously took double dosing of nevirapine, while the other patient did not attend the scheduled laboratory control two weeks after the initiation of nevirapine treatment."( [Hepatic failure due to nevirapine treatment for HIV infection].
Katzenstein, TL; Mens, H, 2005
)
0.89
"To improve the dosing frequency and pill burden of antiretroviral therapy, we compared two once-daily dosed regimens to a twice-daily dosed regimen."( Comparison of two once-daily regimens with a regimen consisting of nelfinavir, didanosine, and stavudine in antiretroviral therapy-naïve adults: 48-week results from the Antiretroviral Regimen Evaluation Study (ARES).
Borleffs, JC; Hassink, EA; Juttmann, JR; Koopmans, PP; Lange, JM; Lowe, SH; Richter, C; Schreij, G; ten Kate, RW; van der Tweel, I; Wensing, AM,
)
0.13
"HIV-1-infected, antiretroviral drug-naïve adults were randomized to either twice-daily nelfinavir and stavudine and once-daily didanosine (regimen A) or simplified once-daily dosed antiretroviral regimens consisting of nevirapine, didanosine, and lamivudine (regimen B) or saquinavir, ritonavir, didanosine, and lamivudine (regimen C)."( Comparison of two once-daily regimens with a regimen consisting of nelfinavir, didanosine, and stavudine in antiretroviral therapy-naïve adults: 48-week results from the Antiretroviral Regimen Evaluation Study (ARES).
Borleffs, JC; Hassink, EA; Juttmann, JR; Koopmans, PP; Lange, JM; Lowe, SH; Richter, C; Schreij, G; ten Kate, RW; van der Tweel, I; Wensing, AM,
)
0.32
"No statistically significant difference in efficacy was found between the two investigated once-daily dosed treatment regimens (B and C) and the reference (A)."( Comparison of two once-daily regimens with a regimen consisting of nelfinavir, didanosine, and stavudine in antiretroviral therapy-naïve adults: 48-week results from the Antiretroviral Regimen Evaluation Study (ARES).
Borleffs, JC; Hassink, EA; Juttmann, JR; Koopmans, PP; Lange, JM; Lowe, SH; Richter, C; Schreij, G; ten Kate, RW; van der Tweel, I; Wensing, AM,
)
0.13
"As part of the large international, randomized 2NN trial, the pharmacokinetics of nevirapine in once-daily 400 mg and twice-daily 200 mg dosing regimens were investigated."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.68
" Differences in pharmacokinetics between once- versus twice-daily dosing were investigated with nonlinear mixed effects modelling (NONMEM)."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.45
" Dosage and dosing frequency did not influence clearance or volume of distribution of nevirapine, indicating linear pharmacokinetic behavior of nevirapine whether given as a single daily dose or as divided doses over 24 hours."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.68
"The daily exposure to nevirapine (AUC24h) was similar for the 400 mg once-daily and the 200 mg twice-daily dosing regimens."( Pharmacokinetics of nevirapine: once-daily versus twice-daily dosing in the 2NN study.
Beijnen, JH; Huitema, AD; Kappelhoff, BS; Lange, JM; MacGregor, TR; Robinson, PA; van Leth, F,
)
0.77
" To minimize toxicity, clinicians must adhere to dosing guidelines, avoid prescribing the drug in patients with known increased risk of toxicity, and promptly recognize toxicities, which are mainly cutaneous and hepatic."( Nevirapine toxicity.
Taiwo, BO, 2006
)
1.78
" In a multivariate model, K103N detection was associated with HIV-1 subtype (C > A), after adjusting for log10 delivery viral load, the number of days between NVP dosing and sample collection, age, and parity."( Quantitative analysis of HIV-1 variants with the K103N resistance mutation after single-dose nevirapine in women with HIV-1 subtypes A, C, and D.
Chen, S; Church, JD; Eshleman, SH; Fiscus, SA; Flys, TS; Guay, LA; Hoover, DR; Jackson, JB; Jones, DC; Kumwenda, N; Mmiro, F; Musoke, P; Mwatha, A; Taha, TE, 2006
)
0.55
"To reduce mother-to-child transmission (MTCT) of HIV, we assessed the stability of nevirapine suspension in an oral dosing syringe over a range of storage conditions."( Stability of nevirapine suspension in prefilled oral syringes used for reduction of mother-to-child HIV transmission.
Dreyfuss, ML; Gray, RH; Hamzeh, FM; Li, X; Parsons, TL; Rexroad, VE; Stamper, PD, 2006
)
0.93
"A mother-to-child transmission dosing kit, containing a maternal nevirapine tablet and infant nevirapine suspension in an oral syringe that can be dispensed to the pregnant woman to use at delivery."( Stability of nevirapine suspension in prefilled oral syringes used for reduction of mother-to-child HIV transmission.
Dreyfuss, ML; Gray, RH; Hamzeh, FM; Li, X; Parsons, TL; Rexroad, VE; Stamper, PD, 2006
)
0.94
" Based on these results, it is acceptable to test the pharmacokinetics and dosing requirements of Pedimune in HIV-infected children."( Pharmacokinetics of two generic fixed-dose combinations for HIV-infected children (Pedimune Baby & Pedimune Junior) are similar to the branded products in healthy adults.
Burger, DM; Dijkema, T; Gibb, DM; L'homme, RF; van der Ven, AJ; Warris, A, 2007
)
0.34
"Despite the benefits of protease inhibitor (PI)-based HIV treatment, issues of tolerability, dosing frequency, pill count and long-term metabolic complications necessitate evaluation of alternate treatment strategies."( Evaluation of nevirapine-switch strategies for HIV treatment.
Cooper, CL, 2006
)
0.69
" The first trial began in April 1991 and assessed zidovudine (ZDV) versus placebo and since then, the type, dosage and duration of drugs to be compared has been modified in each subsequent trial."( Antiretrovirals for reducing the risk of mother-to-child transmission of HIV infection.
Brocklehurst, P; Siegfried, NL; van der Merwe, L; Volmink, J, 2007
)
0.34
"0001 in both cases) influenced by the patient's status (mean KM estimate of 812 days for virological failures, 1294 for naive patients and 1657 for treatment simplifications) and by the dosing schedule (once-daily 1315 days; twice-daily 1198 days)."( Reasons for discontinuation of nevirapine-containing HAART: results from an unselected population of a large clinical cohort.
Airoldi, M; Arici, C; Bombana, E; Gregis, G; Maggiolo, F; Quinzan, G; Ravasio, V; Ripamonti, D; Suter, F, 2007
)
0.63
"In the context of attempts to simplify treatment regimens and enhance adherence, there is great interest in once-daily dosing regimens for the treatment of HIV-1 infection."( Once-daily nevirapine dosing: a pharmacokinetics, efficacy and safety review.
Cooper, CL; van Heeswijk, RP, 2007
)
0.73
"Most antiretrovirals are metabolized in the liver, and lower dosing could be advisable in patients with severe liver insufficiency."( Influence of liver fibrosis stage on plasma levels of antiretroviral drugs in HIV-infected patients with chronic hepatitis C.
Barreiro, P; Gonzalez-Lahoz, J; Jiménez-Nácher, I; Labarga, P; Martín-Carbonero, L; Rodríguez-Novoa, S; Ruiz, A; Soriano, V, 2007
)
0.34
" However, a higher daily dosage of itraconazole might have an inhibitory effect."( Pharmacokinetic study of the interaction between itraconazole and nevirapine.
Jaruratanasirikul, S; Sriwiriyajan, S, 2007
)
0.58
"Co-administration of NVP and daily dosage of FLU (200 mg/day and 400 mg/day) results in markedly increased trough plasma NVP level when compared to the administration of NVP alone."( Plasma nevirapine levels, adverse events and efficacy of antiretroviral therapy among HIV-infected patients concurrently receiving nevirapine-based antiretroviral therapy and fluconazole.
Athichathanabadi, C; Manosuthi, W; Phoorisri, T; Sungkanuparph, S; Uttayamakul, S, 2007
)
0.79
"The effect of nevirapine once-daily dosing on the pharmacokinetics of methadone and its main metabolite, 2-ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine, was evaluated in ten HIV positive patients on stable methadone therapy."( Pharmacokinetics of methadone in human-immunodeficiency-virus-infected patients receiving nevirapine once daily.
Arroyo, E; Climent-Grana, E; Merino, E; Pérez-Ruixo, JJ; Portilla, J; Valenzuela, B, 2007
)
0.92
" In conclusion, with the persistence of 4'-Ed4TTP and persistent anti-HIV activity in cells, we anticipate less frequent dosing and fewer patient compliance issues than for D4T."( Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
Baba, M; Cheng, YC; Dutschman, GE; Grill, SP; Hu, R; Lam, W; Paintsil, E; Tanaka, H, 2007
)
0.34
" Further in-depth studies in a large number of patients receiving different dosage regimens are required to confirm these results and further our understanding of a possible clinical advantage arising from the bioenhancement capabilities of piperine in the treatment of HIV infection."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.59
" Simplification of dosing schedules has prompted investigations into once-daily dosing regimens; nevirapine once-daily dosing strategies are currently under investigation."( Once-daily dosing of nevirapine in HAART.
Clotet, B, 2008
)
0.88
"For optimal adherence, once-daily dosing is best."( Effect of twice-daily nevirapine on adherence in HIV-1-infected patients: a randomized controlled study.
Arvieux, C; Chaillot, F; Le Moal, G; Massari, V; Parienti, JJ; Reliquet, V; Vabret, A; Verdon, R, 2007
)
0.65
" Newer HAART regimens have less toxicity and better dosing characteristics than first-generation regimens, but it is not known whether they are associated with improved clinical outcomes."( Initiating highly active antiretroviral therapy with newer protease inhibitors is associated with better survival compared to first-generation protease inhibitors or nevirapine.
Crane, HM; Kitahata, MM; Van Rompaey, SE, 2007
)
0.53
" The results of the calculations revealed that the variant that survives in patients dosed with either nevirapine or efavirenz had a more positive Delta Delta G value than other variants that were not observed in patients."( Energetic effects for observed and unobserved HIV-1 reverse transcriptase mutations of residues L100, V106, and Y181 in the presence of nevirapine and efavirenz.
Franklin, AM; Jorgensen, WL; Rader, LH; Smith, KD; Smith, MB; Smith, RH; Taylor, EV; Tirado-Rives, J, 2008
)
0.76
" TDM is useful to determine the best dosage regimen adapted to each patient."( Determination of abacavir, amprenavir, didanosine, efavirenz, nevirapine, and stavudine concentration in human plasma by MALDI-TOF/TOF.
Alonzi, T; Ascenzi, P; Mancone, C; Narciso, P; Notari, S; Tripodi, M, 2008
)
0.59
"Seventy-one Zambian children were treated with Triomune Baby or Junior dosed according to weight bands."( Nevirapine, stavudine and lamivudine pharmacokinetics in African children on paediatric fixed-dose combination tablets.
Burger, DM; Chintu, C; Ewings, FM; Gibb, DM; Kabamba, D; Kankasa, C; L'homme, RF; Mulenga, V; Thomason, MJ; Walker, AS, 2008
)
1.79
"To determine the impact of pregnancy on the pharmacokinetics (PK) of nevirapine (NVP) during chronic dosing in HIV-infected women and appropriate NVP dosing in this population."( Chronic administration of nevirapine during pregnancy: impact of pregnancy on pharmacokinetics.
Aweeka, F; Best, B; Burchett, SK; Capparelli, EV; Foca, M; Hitti, J; Hu, C; Jimenez, E; Mirochnick, M; Nachman, S; Read, JS; Shearer, WT; Smith, E; Spector, SA; Stek, A; Thorpe, EM; Watts, H, 2008
)
0.88
"The aim of this study was to develop and validate a population pharmacokinetic model for nevirapine in a population of HIV-infected adults and to evaluate the influence of nevirapine dosing regimen and patient characteristics on nevirapine trough concentration."( Once- or twice-daily dosing of nevirapine in HIV-infected adults: a population pharmacokinetics approach.
Cedeño, S; Clotet, B; Costa, J; Miranda, C; Miranda, J; Moltó, J; Negredo, E; Santos, JR; Valle, M; Vilaró, J, 2008
)
0.85
"0 mg/L when nevirapine was dosed once daily."( Once- or twice-daily dosing of nevirapine in HIV-infected adults: a population pharmacokinetics approach.
Cedeño, S; Clotet, B; Costa, J; Miranda, C; Miranda, J; Moltó, J; Negredo, E; Santos, JR; Valle, M; Vilaró, J, 2008
)
1.01
" The latter association was maintained with both 200 mg twice daily (bid) and 400 mg once daily (qd) dosing [GG, 3527 ng/mL (n=30); GT, 4525 ng/mL (n=32); TT, 7020 ng/mL (n=2); P(anova)=0."( Cytochrome P450 2B6 516G-->T is associated with plasma concentrations of nevirapine at both 200 mg twice daily and 400 mg once daily in an ethnically diverse population.
Back, Dj; Egan, D; Johnson, M; Khoo, S; Mahungu, T; Owen, A; Smith, C; Turner, F; Youle, M, 2009
)
0.58
"01) in the total area under the concentration-time curve (AUC(T)), maximum plasma concentration (C(max)) and terminal elimination half-life (T((1/2)beta)) of quinine compared with values with quinine dosing alone (AUC: 53."( Effects of concurrent administration of nevirapine on the disposition of quinine in healthy volunteers.
Cook, JM; Omoruyi, SI; Onyeji, CO; Owolabi, AR; Sarma, PV; Soyinka, JO, 2009
)
0.62
" Efavirenz and nevirapine concentrations at 12 h after dosing (C12) were monitored at weeks 6 and 12."( A randomized trial comparing plasma drug concentrations and efficacies between 2 nonnucleoside reverse-transcriptase inhibitor-based regimens in HIV-infected patients receiving rifampicin: the N2R Study.
Burapatarawong, S; Likanonsakul, S; Lueangniyomkul, A; Mankatitham, W; Manosuthi, W; Prasithsirskul, W; Prommool, V; Ruxrungtham, K; Sungkanuparph, S; Tantanathip, P; Thawornwa, U; Thongyen, S, 2009
)
0.71
" Significant autoinduction of cytochrome P450 3A4 and 2B6 following multiple dosing prompted an assessment of the metabolic profiles in patients with liver disease receiving chronic nevirapine therapy."( Pharmacokinetic assessment of nevirapine and metabolites in human immunodeficiency virus type 1-infected patients with hepatic fibrosis.
Cammett, AM; Felizarta, F; MacGregor, TR; Mallolas, J; Miailhes, P; Piliero, PJ; Wruck, JM, 2009
)
0.83
"Children were recruited in weight-based dosage bands and nutritional status classified according to weight for height."( Pharmacokinetics of nevirapine in HIV-infected children with and without malnutrition receiving divided adult fixed-dose combination tablets.
Back, D; Else, L; Fraser, W; Khoo, S; Molyneux, E; Moons, P; Poerksen, G; Pollock, L; Walker, S, 2009
)
0.68
" We investigated the relationship of NVP dosing with safety and efficacy."( Safety and efficacy of once-daily nevirapine dosing: a multicohort study.
Battegay, M; Calmy, A; de Wolf, F; Hirschel, B; Hogg, RS; Lange, JM; Lima, VD; Montaner, JS; Nguyen, A; Reiss, P; Vallier, N; Wit, FW; Yip, B, 2009
)
0.63
" Daily drug dosage was 300 mg Tenofovir, 200mg Emtricitabine and 400 mg Nevirapine once daily."( Long-term efficacy and safety of once-daily nevirapine in combination with tenofovir and emtricitabine in the treatment of HIV-infected patients: a 72-week prospective multicenter study (TENOR-trial).
Flux, K; Gholam, P; Hartmann, M; Hueter, E; Weberschock, T, 2009
)
0.85
" These data suggest that 2 tablets of lopinavir-ritonavir BD may be inadequate when dosed with NNRTIs in Ugandan adults, and the dosage should be increased by the addition of an additional adult tablet or a half-dose tablet (100/25 mg), where available."( Pharmacokinetics of lopinavir-ritonavir with and without nonnucleoside reverse transcriptase inhibitors in Ugandan HIV-infected adults.
Dickinson, L; Gibb, DM; Gilks, CF; Kayiwa, J; Khoo, S; Kityo, C; Lutwama, F; Munderi, P; Nalumenya, R; Reid, A; Ssali, F; Tumukunde, D; Walker, AS, 2010
)
0.36
" Children were stratified by weight and dosing was weight-based."( A chewable pediatric fixed-dose combination tablet of stavudine, lamivudine, and nevirapine: pharmacokinetics and safety compared with the individual liquid formulations in human immunodeficiency virus-infected children in Thailand.
Capparelli, E; Chokephaibulkit, K; Chotpitayasunondh, T; Cressey, TR; Eksaengsri, A; Hongsiriwan, S; McIntosh, K; Muresan, P; Plipat, N; Prasitsuebsai, W; Sirisanthana, V; Smith, ME; Toye, M; Vanprapar, N; Yogev, R, 2010
)
0.59
"CHAP2 (Children with HIV Antibiotic Prophylaxis 2) is a prospective cohort of Zambian children using d4T/3TC/NVP adult Triomune30 dosed according to WHO guidelines."( Drug resistance in human immunodeficiency virus type-1 infected Zambian children using adult fixed dose combination stavudine, lamivudine, and nevirapine.
Chintu, C; Ferrier, A; Ford, D; Gibb, DM; Grant, PR; Gupta, RK; Kabamba, D; Kalumbi, M; Mulenga, V; Pillay, D; Walker, AS, 2010
)
0.56
" Children taking T30 for > 6 weeks from each dosing weight band (<5, 5-<8, 8-<12, 12-<14, 14-<19, 19-<26, 26-<30 and > or = 30 kg) were recruited."( Steady-state nevirapine, lamivudine and stavudine levels in Malawian HIV-infected children on antiretroviral therapy using split Triomune 30 tablets.
Burger, D; Chesshyre, E; Khoo, S; Molyneux, E; Moons, P; Poerksen, G; Pollock, L, 2010
)
0.73
" Nevirapine trough concentrations were measured after 18 and 36 months of starting antiretroviral treatment and in samples drawn during a dosing interval in a subset of 10 patients."( Population pharmacokinetic-pharmacogenetic study of nevirapine in HIV-infected Cambodian patients.
Becquemont, L; Bertrand, J; Borand, L; Chou, M; Comets, E; Le Tiec, C; Mentre, F; Ouk, V; Segeral, O; Taburet, AM; Verstuyft, C, 2010
)
1.52
"Children were randomized to initiate antiretroviral therapy with full-dose (FD) nevirapine (Triomune Baby or Junior in the morning and evening) versus DE (half-dose nevirapine for 14 days [Triomune in the morning and stavudine-lamivudine {Lamivir-S} in the evening], then FD), in accordance with World Health Organization weight-band dosing tables."( Strategies for nevirapine initiation in HIV-infected children taking pediatric fixed-dose combination "baby pills" in Zambia: a randomized controlled trial.
Burger, D; Chijoka, C; Chintu, C; Cook, A; Ferrier, A; Gibb, DM; Kabamba, D; Kalengo, C; Kankasa, C; Kityo, C; Mulenga, V; Thomason, M; Walker, AS, 2010
)
0.94
"This study assessed the effect of stavudine (d4T) 30 mg dosage on lipoatrophy in HIV-infected patients on antiretroviral treatment."( Reduced dose of stavudine and lipoatrophy in HIV-infected patients in Cameroon.
Biwolé-Sida, M; Bork, K; Coudray, M; Cournil, A; Delaporte, E; Essomba, CN; Kouanfack, C; Laurent, C; Tonfack, CA, 2010
)
0.36
"The use of d4T at a lower dosage might increase safety with regard to its effect on lipoatrophy."( Reduced dose of stavudine and lipoatrophy in HIV-infected patients in Cameroon.
Biwolé-Sida, M; Bork, K; Coudray, M; Cournil, A; Delaporte, E; Essomba, CN; Kouanfack, C; Laurent, C; Tonfack, CA, 2010
)
0.36
" A minimum effective concentration (MEC) of 3000 ng/mL was used to interpret nevirapine concentrations 12 h after dosing (C(12))."( Nevirapine pharmacokinetics when initiated at 200 mg or 400 mg daily in HIV-1 and tuberculosis co-infected Ugandan adults on rifampicin.
Back, D; Boffito, M; Byakika-Kibwika, P; Coakley, P; Colebunders, R; Kalemeera, F; Khoo, S; Lamorde, M; Merry, C; Namakula, R; Okaba-Kayom, V; Ryan, M, 2011
)
2.04
"All randomised controlled trials comparing EFV to NVP in HIV-infected individuals without prior exposure to ART, irrespective of the dosage or NRTI backbone."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.73
" Data were analysed on an intention-to-treat basis and reported as per dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.73
"The trials were pooled as per dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, LC; Rutherford, GW; Siegfried, N; Spaulding, A, 2010
)
0.73
" For analysis of nevirapine pharmacokinetic parameters, blood samples were obtained before dosing and at regularly scheduled intervals over 168 hours after administration."( Relative bioavailability of two formulations of nevirapine 200-mg tablets in healthy Chinese male volunteers: a single-dose, randomized-sequence, open-label, two-way crossover study.
Hu, Y; Yang, X; Yu, C; Zhang, Q; Zhu, Y; Zou, J, 2010
)
0.96
" Dosing recommendations for children should be reviewed in the light of these findings."( Factors influencing plasma nevirapine levels: a study in HIV-infected children on generic antiretroviral treatment in India.
Agibothu Kupparam, HK; Karunaianandham, R; Mahalingam, V; Navaneethapandian, PG; Perumal Kannabiran, B; Ramachandran, G; Shah, I; Sikhamani, R; Soundararajan, L; Swaminathan, S, 2011
)
0.67
" Currently, twice-a-day dosing is required for the successful application of NVP immediate release (IR), but there is potential for a more convenient once-a-day antiretroviral combination."( Nevirapine once daily: pharmacology, metabolic profile and efficacy data of the new extended-release formulation.
Parienti, JJ; Peytavin, G, 2011
)
1.81
" Simulations of the nevirapine concentration profile were performed with dosing regimens of 200 mg twice daily and 400 mg once daily for individuals with body weights of 50, 70 and 90 kg in combination with CYP2B6 genetic variation."( Integration of population pharmacokinetics and pharmacogenetics: an aid to optimal nevirapine dose selection in HIV-infected individuals.
Back, DJ; Brockmeyer, NH; Davies, G; Egan, D; Fätkenheuer, G; Hendra, H; Johnson, MA; Khoo, S; Mahungu, T; Owen, A; Rockstroh, J; Schipani, A; Siccardi, M; Wyen, C; Youle, M, 2011
)
0.92
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
0.37
" The first trial began in April 1991 and assessed zidovudine (ZDV) versus placebo and since then, the type, dosage and duration of drugs to be compared has been modified in each subsequent trial."( Antiretrovirals for reducing the risk of mother-to-child transmission of HIV infection.
Brocklehurst, P; Siegfried, N; Sint, TT; van der Merwe, L, 2011
)
0.37
"This study (VERxVE) compared the efficacy and safety of the new nevirapine extended-release (NVP XR) formulation dosed once daily with NVP immediate release (IR) twice daily in treatment-naive patients."( Efficacy and safety of nevirapine extended-release once daily versus nevirapine immediate-release twice-daily in treatment-naive HIV-1-infected patients.
Andrade-Villanueva, J; Bogner, J; Cahn, P; Drulak, M; Gathe, J; Horban, A; Nelson, M; Nguyen, T; Podzamczer, D; Quinson, AM; Santiago, S; Spencer, D; Yong, CL; Zhang, W, 2011
)
0.92
" The usual dosing regimen is 200 mg twice/day."( Bioavailability of nevirapine in rats after oral and subcutaneous administration, in vivo absorption from gastrointestinal segments and effect of bile on its absorption from duodenum.
Peris, JE; Usach, I, 2011
)
0.7
" Lopinavir was active at levels well below those achieved with standard dosing of coformulated lopinavir-ritonavir."( In vitro activity of antiretroviral drugs against Plasmodium falciparum.
Nsanzabana, C; Rosenthal, PJ, 2011
)
0.37
" Our study suggests that NVP dosing of preterm infants as soon as possible after birth without maternal intrapartum dosing may be as effective as combined maternal and infant dosing."( Nevirapine plasma concentrations in premature infants exposed to single-dose nevirapine for prevention of mother-to-child transmission of HIV-1.
Cotton, MF; Els, I; Hall, D; Madsen, R; Mirochnick, M; Mugabo, P; Rabie, H; Smith, J; Smith, P; Steyn, W, 2011
)
1.81
" It is expected that patients who are on NVP IR at present will consider switching to NVP XR to achieve regimen simplification by reducing their daily dosing and pill burden."( Guidelines for the use of extended-release nevirapine in HIV-infected patients.
Corbett, AH; Heil, EL, 2011
)
0.63
" The correlation between nevirapine concentrations, efficacy and hepatotoxicity suggests the benefit of dosage adjustment based on therapeutic drug monitoring among Chinese HIV-infected patients to optimize nevirapine containing antiretroviral therapy."( Nevirapine plasma concentrations are associated with virologic response and hepatotoxicity in Chinese patients with HIV infection.
Fu, Q; Han, Y; Kou, H; Li, T; Li, Y; Ma, Q; Qiu, Z; Wang, J; Ye, M; Zhu, Z; Zuo, L, 2011
)
2.12
" Dosing was weight-based."( Pharmacokinetics and safety of a new paediatric fixed-dose combination of zidovudine/lamivudine/nevirapine in HIV-infected children.
Aurpibul, L; Capparelli, E; Chokephaibulkit, K; Cressey, TR; Eksaengsri, A; Hongsiriwon, S; Kabat, B; Limwongse, C; McIntosh, K; Muresan, P; Ngampiyaskul, C; Sirisanthana, V; Smith, ME; Toye, M; Wittawatmongkol, O; Yogev, R, 2011
)
0.59
" Factors that may have contributed to the suboptimal results with nevirapine include elevated viral load at baseline, selection for nevirapine resistance, background regimen of nucleoside reverse-transcriptase inhibitors, and the standard ramp-up dosing strategy."( Nevirapine versus ritonavir-boosted lopinavir for HIV-infected children.
Abrams, EJ; Barlow-Mosha, L; Bobat, R; Chi, BH; Cotton, MF; Eshleman, SH; Hughes, MD; Jean-Philippe, P; Kamthunzi, P; Khadse, S; Lindsey, JC; Millar, L; Mofenson, LM; Moultrie, H; Mujuru, HA; Palumbo, P; Petzold, E; Purdue, L; Schimana, W; Violari, A, 2012
)
2.06
" However, there are challenges to initiate ART in early life, including the possibility of drug resistance in the context of prevention of mother-to-child transmission (PMTCT) programs, a paucity of drug choices , uncertain dosing for some medications and long-term toxicities."( Effectiveness of antiretroviral therapy in HIV-infected children under 2 years of age.
Cotton, M; Gibb, D; Penazzato, M; Prendergast, A; Tierney, J, 2012
)
0.38
" Male Cbl-b(-/-) mice dosed with NVP had an increase in ALT of >200 U/L, which also resolved despite continued treatment."( Bioactivation of nevirapine to a reactive quinone methide: implications for liver injury.
Hayes, MA; Li, Y; Novalen, M; Sharma, AM; Uetrecht, J, 2012
)
0.72
" It can thus be used to make predictions and dosage adjustment optimization based on Bayesian therapeutic drug monitoring (TDM)."( Dosage optimization of treatments using population pharmacokinetic modeling and simulation.
Aouri, M; Arab-Alameddine, M; Buclin, T; Csajka, C; Decosterd, LA; Guidi, M; Rotger, M; Telenti, A, 2012
)
0.38
" An extended-release (XR) formulation of NVP was developed since QD dosing and reduced pill burdens have been shown to improve regimen adherence."( Once-daily nevirapine XR: a brief overview of the safety and efficacy of a new formulation.
Bhatti, L; Gladstein, J,
)
0.52
"In this highly adherent population, the number of daily pills was related to self-reported health status but not to self-reported adherence, whereas the dosing interval did not influence self-reported adherence or health status."( Number of daily pills, dosing schedule, self-reported adherence and health status in 2010: a large cross-sectional study of HIV-infected patients on antiretroviral therapy.
Bocchiola, B; Cahua, T; Castagna, A; Danise, A; Galli, L; Gianotti, N; Lazzarin, A; Maillard, M; Panzini, P; Pazzi, A; Salpietro, S; Zandonà, D, 2013
)
0.39
" Through dose-response experiments, we established relative inhibitory potencies of NRTIs on in vitro telomerase activity as compared to the inhibitory potencies of the corresponding dideoxynucleotide triphosphates."( In vitro and ex vivo inhibition of human telomerase by anti-HIV nucleoside reverse transcriptase inhibitors (NRTIs) but not by non-NRTIs.
Côté, HC; Hukezalie, KR; Thumati, NR; Wong, JM, 2012
)
0.38
"Standard LPV dosing achieved therapeutic levels in pregnancy and no appreciable concentrations in breast milk."( Therapeutic levels of lopinavir in late pregnancy and abacavir passage into breast milk in the Mma Bana Study, Botswana.
Capparelli, E; Essex, M; Leidner, J; Lockman, S; Makhema, J; Moffat, C; Moss, M; Moyo, S; Ogwu, A; Rossi, S; Shapiro, RL, 2013
)
0.39
" The aims of this study were to investigate the population pharmacokinetics of NVP in children, establish factors that influence NVP pharmacokinetics and evaluate the current dosing recommendations."( Evaluation of nevirapine dosing recommendations in HIV-infected children.
Benaboud, S; Blanche, S; Bouazza, N; Dollfus, C; Faye, A; Foissac, F; Frange, P; Hirt, D; Lachassinne, E; Treluyer, JM; Urien, S, 2013
)
0.75
" Based on simulations of European Medicines Agency (EMA) and World Health Organization (WHO) dosing recommendations, the probability of observing minimal concentrations below the efficacy target of 3 mg l(-1) is higher following the EMA recommendations than the WHO recommendations."( Evaluation of nevirapine dosing recommendations in HIV-infected children.
Benaboud, S; Blanche, S; Bouazza, N; Dollfus, C; Faye, A; Foissac, F; Frange, P; Hirt, D; Lachassinne, E; Treluyer, JM; Urien, S, 2013
)
0.75
" Simulations revealed that newborns born early (<1 hour) after maternal nevirapine intake would benefit from a 3-fold higher nevirapine dosage (6 mg/kg) after birth for analogous protective plasma concentrations over the first 2 weeks."( Population pharmacokinetic analysis of a nevirapine-based HIV-1 prevention of mother-to-child transmission program in Uganda to assess the impact of different dosing regimens for newborns.
Frank, M; Harms, G; Kloft, C; Kunz, A, 2013
)
0.89
" Formulations allowing once-daily dosing of antiretrovirals can significantly improve regimen adherence, which is important for maintaining virologic control, especially for NNRTI-based regimens with low barriers for genetic resistance."( Considerations on the new nevirapine: switching patients from twice-daily to once-daily.
Slim, J; Ward, D,
)
0.43
" Fixed-dose combination anti-retroviral therapy provides adequate suppression of HIV-1 replication, provides barrier to the development of resistance, simplifies dosage regimen and improves adherence."( A randomized pahse I bioequivalence clinincal trial of a paediatric fixed-dose combination antiretroviral reconstitutable suspension in healthy adult volunteers.
Adeyeye, M; Edowhorhu, G; Esseku, F; Gbadero, D; Joshi, A; Oyegbile, Y, 2013
)
0.39
" A total of 15 blood samples were collected before dosing and up to 96 h post dosing."( A randomized pahse I bioequivalence clinincal trial of a paediatric fixed-dose combination antiretroviral reconstitutable suspension in healthy adult volunteers.
Adeyeye, M; Edowhorhu, G; Esseku, F; Gbadero, D; Joshi, A; Oyegbile, Y, 2013
)
0.39
"Regimen simplification can be defined as a change in established effective therapy to reduce pill burden and dosing frequency, to enhance tolerability, or to decrease specific food and fluid requirements."( Abacavir-based triple nucleoside regimens for maintenance therapy in patients with HIV.
Bosco, O; Cruciani, M; Malena, M; Mengoli, C; Parisi, SG; Serpelloni, G, 2013
)
0.39
" SJS can occur in children at any age, with any level of immunosuppression, and can occur during the lead-in dosing period of NVP."( Stevens-Johnson syndrome and HIV in children in Swaziland.
Blank, DA; Draper, HR; Dziuban, EJ; Hughey, AB; Kochelani, D; Schutze, GE; Stewart, DA, 2013
)
0.39
" As prolonged subtherapeutic nevirapine dosage leads to the emergence of resistance, single-dose nevirapine could be used with phenytoin as an alternative if other ARVs were unavailable."( Effect of 7 days of phenytoin on the pharmacokinetics of and the development of resistance to single-dose nevirapine for perinatal HIV prevention: a randomized pilot trial.
Aitken, S; Burger, DM; Chunda, C; Fillekes, Q; Gibb, DM; Kankasa, C; Kisanga, ER; Muro, EP; Thomason, MJ; Walker, AS, 2013
)
0.89
" Our results demonstrate that the HIV PI lopinavir inhibits liver stage parasites at clinically relevant concentrations, that is, at drug levels achieved in HIV-infected patients on standard dosing regimens."( The effect of antiretrovirals on Plasmodium falciparum liver stages.
Borkowsky, W; De La Vega, P; Duffy, PE; Hobbs, CV; Krzych, U; Penzak, SR; Sinnis, P; Van Vliet, J, 2013
)
0.39
" We set out to demonstrate that in-home HIV testing and NVP dosing by traditional birth attendants (TBAs) is feasible and acceptable by women in rural Zambia."( In-home HIV testing and nevirapine dosing by traditional birth attendants in rural Zambia: a feasibility study.
Botha, B; Brennan, AT; Goggin, C; Hamomba, L; Mazimba, A; Pilingana, P; Scott, N; Seidenberg, P; Semrau, K; Thea, DM,
)
0.44
"3%) took single-dose NVP administered by a TBA between 1 and 24 hours prior to birth and 100% of exposed newborns (16 of 16) received NVP syrup within 72 hours after birth, 80% of whom were dosed in the first 24 hours of life."( In-home HIV testing and nevirapine dosing by traditional birth attendants in rural Zambia: a feasibility study.
Botha, B; Brennan, AT; Goggin, C; Hamomba, L; Mazimba, A; Pilingana, P; Scott, N; Seidenberg, P; Semrau, K; Thea, DM,
)
0.44
" Mice were dosed twice daily until PND 28."( Toxicology and Carcinogenesis Studies of Mixtures of 3'-Azido-3'-Deoxythymidine (AZT), Lamivudine (3TC), and Nevirapine (NVP) (CAS Nos. 30516-87-1, 134678-17-4, 129618-40-2) in Genetically Modified C3B6.129F1-Trp53(tm1Brd) N12 Haploinsufficient Mice (in u
, 2013
)
0.6
" Additionally, nevirapine plasma concentrations of 200 mg twice daily (NVPBID) and 400 mg once daily (NVPOD) were simulated using the final model to investigate the impact of the covariates and different dosage regimens on nevirapine steady state concentrations."( Population pharmacokinetics of nevirapine in Thai HIV-infected patients.
Avihingsanon, A; Manosuthi, W; Punyawudho, B; Wattanakul, T, 2014
)
1.04
"This population-based pharmacokinetic model can be used for optimizing nevirapine dosage regimens for individual patients to improve efficacy and safety of nevirapine therapy in this population."( Population pharmacokinetics of nevirapine in Thai HIV-infected patients.
Avihingsanon, A; Manosuthi, W; Punyawudho, B; Wattanakul, T, 2014
)
0.92
" However, there are challenges to initiation of ART in early life, including the possibility of drug resistance in the context of prevention of mother-to-child transmission (PMTCT) programs, a paucity of drug choices , uncertain dosing for some medications and long-term toxicities."( Optimisation of antiretroviral therapy in HIV-infected children under 3 years of age.
Abrams, E; Muhe, LM; Penazzato, M; Prendergast, AJ; Tindyebwa, D, 2014
)
0.4
"The aim of the present research work was to formulate and evaluate the extended release matrix pellets of nevirapine using extrusion and spheronization technique which will be an alternative technique for making extended release dosage forms and to compare the drug release profiles of the formulations with the reference product."( Effect of combination of acrylic polymers on the release of nevirapine formulated as extended release matrix pellets using extrusion and spheronization technique.
Dua, K; Prasad, A; Sharma, A; Singh, G, 2014
)
0.86
" Efficacious, safe bedaquiline dosing for MDR-TB patients receiving antiretrovirals is important."( Impact of lopinavir-ritonavir or nevirapine on bedaquiline exposures and potential implications for patients with tuberculosis-HIV coinfection.
Dooley, KE; Karlsson, MO; Svensson, EM, 2014
)
0.68
" This modelling technique is able to inform the design of clinical studies, and allows assessment of pragmatic dosing strategies under complex therapeutic scenarios."( Use of in vitro to in vivo extrapolation to predict the optimal strategy for patients switching from efavirenz to maraviroc or nevirapine.
Back, D; Davies, G; Khoo, S; Owen, A; Schipani, A; Siccardi, M, 2015
)
0.62
"We document our experience with therapeutic drug monitoring (TDM) of antiretroviral agents (1807 determinations) carried out as day-by-day clinical practice for the optimization of drug dosing in HIV-infected patients."( Is it time to revise antiretrovirals dosing? a pharmacokinetic viewpoint.
Baldelli, S; Castoldi, S; Cattaneo, D; Charbe, N; Clementi, E; Cozzi, V; Fucile, S, 2014
)
0.4
" Nevirapine has low solubility, an acid medium being the most appropriate medium for assessing the release of the drug from dosage forms."( Compatibility studies of nevirapine in physical mixtures with excipients for oral HAART.
de Oliveira, GG; Ferraz, HG; Severino, P; Souto, EB, 2013
)
1.6
" In conclusion, this genotypic resistance analysis strongly suggests that the latest NNRTI, rilpivirine, may retain activity in a large proportion of HIV-1 patients in whom resistance failed while they were on an efavirenz- or nevirapine-containing regimen, and may present an attractive option for second-line treatment given its good safety profile and dosing convenience."( Predicted residual activity of rilpivirine in HIV-1 infected patients failing therapy including NNRTIs efavirenz or nevirapine.
Camacho, RJ; Gomes, P; Rhee, SY; Theys, K; Vandamme, AM, 2015
)
0.81
" Optimal lumefantrine dosage regimen for patients on EFV-based ART was determined by population pharmacokinetics and simulation."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
" The predictive model through simulation of lumefantrine exposure at different dosage regimen scenarios for patients on EFV-based ART, suggest that AL taken twice daily for five days using the current dose could improve lumefantrine exposure and consequently malaria treatment outcomes."( The influence of nevirapine and efavirenz-based anti-retroviral therapy on the pharmacokinetics of lumefantrine and anti-malarial dose recommendation in HIV-malaria co-treatment.
Aklillu, E; Kamuhabwa, AA; Maganda, BA; Minzi, OM; Ngaimisi, E, 2015
)
0.76
" Stavudine and lamivudine are administered as fixed combination while nevirapine as separate dosage form which often results in poor compliance and adherence to therapy by patients and therefore, there is a need to develop dosage forms that can overcome the problems of currently available dosage forms for treatment of HIV infection."( Simultaneous And Extended Delivery Of Stavudine, Lamivudine And Nevirapine In Fixed Dose Combination Using Sandwiched Osmotic Tablets For Hiv Therapy.
Priya, MR; Rajendran, NN, 2015
)
0.89
"05) in the area under the plasma concentration-time curve for dolutegravir from the time the dose was administered until the end of the dosing interval (-19%, P = 0."( Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
Allavena, C; Billaud, E; Bouchez, S; Bouquié, R; Dailly, E; Deslandes, G; Grégoire, M; Hall, N; Hernando, H; Jolliet, P; Raffi, F; Reliquet, V, 2015
)
0.79
" According to therapeutic drug monitoring for dolutegravir, some patients may need a higher dose than 50 mg of dolutegravir once daily to maintain the therapeutic plasma concentration throughout the dosing interval."( Influence of nevirapine administration on the pharmacokinetics of dolutegravir in patients infected with HIV-1.
Allavena, C; Billaud, E; Bouchez, S; Bouquié, R; Dailly, E; Deslandes, G; Grégoire, M; Hall, N; Hernando, H; Jolliet, P; Raffi, F; Reliquet, V, 2015
)
0.79
" Absence of hypersensitivity reactions, superior resistance profile and once-daily dosing favours abacavir for African children, supporting WHO 2013 guidelines."( Abacavir, zidovudine, or stavudine as paediatric tablets for African HIV-infected children (CHAPAS-3): an open-label, parallel-group, randomised controlled trial.
Abongomera, G; Asiimwe, A; Burger, D; Chabala, C; Chintu, C; Cook, AD; Gibb, DM; Kekitiinwa, A; Kenny, J; Kityo, C; Klein, N; McIlleron, H; Mirembe, G; Mulenga, V; Musiime, V; Owen-Powell, E; Thomason, MJ; Walker, AS, 2016
)
0.43
" Only zidovudine has adequate dosing recommendations for treating term and preterm infants and has an intravenous formulation, essential if feeding intolerance occurs."( The last and first frontier--emerging challenges for HIV treatment and prevention in the first week of life with emphasis on premature and low birth weight infants.
Cotton, MF; Holgate, S; Mirochnick, M; Nelson, A; Rabie, H; Wedderburn, C, 2015
)
0.42
" In an effort to understand whether NVP is metabolized differently in a transiently inflamed liver and whether a heightened immune response alters NVP-induced hepatic responses, female brown Norway rats were dosed with either vehicle or NVP alone (75 mg/kg/day for 15 days) or galactosamine alone (single intraperitoneal [ip] injection on day 7 to mimic viral hepatitis) or a combination of NVP (75/100/150 mg/kg/day for 15 days) and galactosamine (single 750 mg/kg ip on day 7)."( Drug-induced Liver Fibrosis: Testing Nevirapine in a Viral-like Liver Setting Using Histopathology, MALDI IMS, and Gene Expression.
Arrington-Brown, L; Bailey, D; Brown, HR; Cariello, NF; Castellino, S; Elangbam, CS; Fowler, S; Gates, LD; Groseclose, MR; Krull, DL; Mellon-Kusibab, K; Miller, RT; Shah, V; Tillman, T; Yoon, LW, 2016
)
0.71
"The PBPK approach is a useful tool for quantifying a priori the drug exposure of metabolized drugs during pregnancy, and can be applied to evaluate alternative dosing regimens to optimize drug therapy."( A Physiologically-Based Pharmacokinetic Model to Predict Human Fetal Exposure for a Drug Metabolized by Several CYP450 Pathways.
Benaboud, S; Blanche, S; Bouazza, N; De Sousa Mendes, M; Foissac, F; Hirt, D; Lui, G; Pressiat, C; Treluyer, JM; Urien, S; Valade, E; Zheng, Y, 2017
)
0.46
"We included all randomized controlled trials (RCTs) that compared EFV to NVP in people with HIV without prior exposure to ART, irrespective of the dosage or NRTI's given in combination."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.8
" We performed subgroup analyses for concurrent treatment for tuberculosis and dosage of NVP."( Efavirenz or nevirapine in three-drug combination therapy with two nucleoside or nucleotide-reverse transcriptase inhibitors for initial treatment of HIV infection in antiretroviral-naïve individuals.
Irlam, JH; Mbuagbaw, L; Mursleen, S; Rutherford, GW; Siegfried, N; Spaulding, AB, 2016
)
0.8
" To normalise bedaquiline exposure in patients with concomitant LPV/r therapy, an adjusted bedaquiline dosing regimen is proposed for further study."( Confirming model-predicted pharmacokinetic interactions between bedaquiline and lopinavir/ritonavir or nevirapine in patients with HIV and drug-resistant tuberculosis.
Brill, MJ; Karlsson, MO; Maartens, G; Pandie, M; Svensson, EM, 2017
)
0.67
" NVP was dosed at 150 mg/m daily for 14 days, then twice daily for 14 days."( Nevirapine Pharmacokinetics and Safety in Neonates Receiving Combination Antiretroviral Therapy for Prevention of Vertical HIV Transmission.
Bitnun, A; Brophy, J; Campbell, DM; Colantonio, D; Kakkar, F; Lau, E; Murphy, K; Read, SE; Samson, L; Seto, W; Yudin, MH, 2017
)
1.9
" Lower empiric dosing is recommended for infants <34 weeks of GA."( Nevirapine Pharmacokinetics and Safety in Neonates Receiving Combination Antiretroviral Therapy for Prevention of Vertical HIV Transmission.
Bitnun, A; Brophy, J; Campbell, DM; Colantonio, D; Kakkar, F; Lau, E; Murphy, K; Read, SE; Samson, L; Seto, W; Yudin, MH, 2017
)
1.9
" Blood plasma was collected at 1, 4 and 24 hours post-ART dosing from 58 subjects receiving NVP-containing ART and used to determine cNVP and viral load (VL)."( Plasma nevirapine concentrations predict virological and adherence failure in Kenyan HIV-1 infected patients with extensive antiretroviral treatment exposure.
Aman, RA; Kimulwo, MJ; Kokwaro, GO; Muigai, AW; Ochieng, DJ; Ochieng, W; Ogutu, BR; Okendo, J; Oloo, FA, 2017
)
0.91
" We evaluated current World Health Organization (WHO) weight-band NVP prophylactic dosing recommendations and investigated optimal therapeutic NVP dosing for neonates."( Assessment of Nevirapine Prophylactic and Therapeutic Dosing Regimens for Neonates.
Aarons, L; Borkird, T; Capparelli, EV; Cressey, TR; Jittayanun, K; Jourdain, G; Lallemant, M; Le Coeur, S; Luvira, A; Phanomcheong, S; Puangsombat, A; Punyawudho, B; Saenjum, C; Sukrakanchana, PO; Urien, S, 2017
)
0.82
"0 mg/L) using different infant dosing strategies."( Assessment of Nevirapine Prophylactic and Therapeutic Dosing Regimens for Neonates.
Aarons, L; Borkird, T; Capparelli, EV; Cressey, TR; Jittayanun, K; Jourdain, G; Lallemant, M; Le Coeur, S; Luvira, A; Phanomcheong, S; Puangsombat, A; Punyawudho, B; Saenjum, C; Sukrakanchana, PO; Urien, S, 2017
)
0.82
"In a population of HIV-infected Kenyan children on antiretroviral therapy including nevirapine (NVP), we used a one-compartment model with previously established PK parameters and Medication Event Monitoring Systems (MEMS®)-recorded dosing times to estimate the mean plasma concentration of NVP (Cp) in individual patients during 1 month of follow-up."( Pharmacokinetics-based adherence measures for antiretroviral therapy in HIV-infected Kenyan children.
Ayaya, SO; Liu, H; Nyandiko, WM; Scanlon, ML; Slaven, JE; Tu, W; Vreeman, RC, 2017
)
0.68
" However, studies have shown that this dosing strategy based on adult studies may not be appropriate in children, given that younger children have higher drug clearance rates."( Sub-therapeutic nevirapine concentration during antiretroviral treatment initiation among children living with HIV: Implications for therapeutic drug monitoring.
A K, HK; D'souza, RR; Gopalan, BP; Mehta, K; Rajnala, N; Ramachandran, G; Shet, A, 2017
)
0.8
" However, the reduction in artemisinin exposure may warrant further study, and suggests that dosage adjustment of artemether-lumefantrine with nevirapine-based ART in children is likely warranted."( Concomitant nevirapine impacts pharmacokinetic exposure to the antimalarial artemether-lumefantrine in African children.
Aweeka, FT; Barlow-Mosha, L; Carey, V; Gingrich, D; Graham, B; Huang, L; Kamthunzi, P; Lindsey, JC; Marzan, F; Nachman, S; Parikh, S; Ssemambo, PK, 2017
)
1.03
"The development of antiretroviral associations in a single dosage form aims to ensure improved efficacy, low costs and better adherence to treatment."( Formulation, Development and Scale-Up of Fixed-Dose Combination Tablets Containing Zidovudine, Lamivudine and Nevirapine.
Barros Silva, LCPB; da Silva, RMF; de Lima, LG; de Medeiros, FPM; de Sousa, ALMD; Lavra, ZMM; Neto, PJR; Rolim, LA; Rosa, TA; Wanderley Sales, VA, 2019
)
0.73
" Lopinavir TDM excluded pharmacokinetic reasons for failure in patients failing treatment when lopinavir dosing was supervised."( Pediatric Antiretroviral Therapeutic Drug Monitoring: A Five and a Half Year Experience from a South African Tertiary Hospital.
Decloedt, EH; Engelbrecht, AE; Norman, J; Rabie, H; Wiesner, L, 2020
)
0.56
" This study aims to establish dosing of nevirapine for very early treatment of HIV-exposed neonates at high risk of HIV acquisition."( Pharmacokinetics and safety of early nevirapine-based antiretroviral therapy for neonates at high risk for perinatal HIV infection: a phase 1/2 proof of concept study.
Bryson, Y; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Coletti, A; Cotton, MF; Hazra, R; Jean-Philippe, P; LeBlanc, R; Mirochnick, M; Naidoo, KL; Nelson, BS; Persaud, D; Reding, C; Ruel, TD; Spector, SA; Tierney, C; Zimmer, B, 2021
)
1.16
" The regimen consisted of two nucleoside reverse transcriptase inhibitors plus nevirapine dosed at 6 mg/kg twice daily for term neonates (≥37 weeks gestational age) or 4 mg/kg twice daily for 1 week and 6 mg/kg twice daily thereafter for preterm neonates (34 to <37 weeks gestational age)."( Pharmacokinetics and safety of early nevirapine-based antiretroviral therapy for neonates at high risk for perinatal HIV infection: a phase 1/2 proof of concept study.
Bryson, Y; Bwakura-Dangarembizi, M; Capparelli, EV; Chadwick, EG; Coletti, A; Cotton, MF; Hazra, R; Jean-Philippe, P; LeBlanc, R; Mirochnick, M; Naidoo, KL; Nelson, BS; Persaud, D; Reding, C; Ruel, TD; Spector, SA; Tierney, C; Zimmer, B, 2021
)
1.12
"Nevirapine (NVP) is used for the management of HIV/AIDS but must be dosed frequently, exhibits unpredictable bioavailability and a side effect profile that includes hepato- and dermo-toxicity."( Preformulation characterization and identification of excipients for nevirapine loaded niosomes.
Walker, RB; Witika, BA, 2021
)
2.3
"2% (30/185) with improper dosage or prescription errors."( Adverse Reactions to Antiretrovirals in Cuban Patients Living with HIV/AIDS.
Morales-Pérez, M, 2021
)
0.62
" This study aimed to develop a population pharmacokinetic model to characterize the disposition of maraviroc in neonates to inform dosing regimens and expand available options."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" The final model was used in Monte Carlo simulations to generate expected exposures with recommended dosing regimens."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
" Monte Carlo simulations with FDA-approved weight band dosing resulted in the majority of simulated patients (84."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
"While maraviroc apparent clearance is decreased in the first few days of life, the current FDA-approved maraviroc weight band dosing provides maraviroc exposures for neonates in the first 6 weeks of life, which were consistent with adult maraviroc exposure range."( Maraviroc Population Pharmacokinetics Within the First 6 Weeks of Life.
Best, BM; Bradford, S; Capparelli, EV; Chadwick, EG; Jean-Philippe, P; Liyanage, M; McFadyen, L; Mirochnick, M; Moye, J; Nikanjam, M; Rogg, L; Vourvahis, M; Whitson, K, 2022
)
0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
HIV-1 reverse transcriptase inhibitorAn entity which inhibits the activity of HIV-1 reverse transcriptase.
[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]

Drug Classes (2)

ClassDescription
dipyridodiazepineAn organic heterotricyclic compound whose skeleton consists of a diazepine ring which is fused to two pyridine rings.
cyclopropanesCyclopropane and its derivatives formed by substitution.
[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]

Pathways (1)

PathwayProteinsCompounds
Nevirapine Metabolism Pathway821

Protein Targets (50)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency47.39350.003245.467312,589.2998AID2517
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.45070.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency0.63100.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency7.35630.000811.382244.6684AID686978; AID686979
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency35.48130.011212.4002100.0000AID1030
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency31.90930.003041.611522,387.1992AID1159552
retinoid X nuclear receptor alphaHomo sapiens (human)Potency16.25950.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency63.66750.001530.607315,848.9004AID1224848; AID1224849
pregnane X nuclear receptorHomo sapiens (human)Potency63.66750.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency15.99260.000229.305416,493.5996AID743080
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency50.11870.001019.414170.9645AID588537
importin subunit beta-1 isoform 1Homo sapiens (human)Potency5.62345.804836.130665.1308AID540263
DNA polymerase betaHomo sapiens (human)Potency35.48130.022421.010289.1251AID485314
mitogen-activated protein kinase 1Homo sapiens (human)Potency6.23030.039816.784239.8107AID1454
snurportin-1Homo sapiens (human)Potency5.62345.804836.130665.1308AID540263
gemininHomo sapiens (human)Potency23.72460.004611.374133.4983AID624296; AID624297
lamin isoform A-delta10Homo sapiens (human)Potency0.03550.891312.067628.1838AID1487
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain B, Hiv-1 Reverse TranscriptaseHuman immunodeficiency virus 1IC50 (µMol)0.08000.08008.540017.0000AID977608
Chain A, Hiv-1 Reverse TranscriptaseHuman immunodeficiency virus 1IC50 (µMol)0.08000.08008.540017.0000AID977608
Chain A, Hiv-1 Reverse TranscriptaseHuman immunodeficiency virus 1IC50 (µMol)0.08000.08008.540017.0000AID977608
Chain A, Hiv-1 Reverse TranscriptaseHuman immunodeficiency virus 1IC50 (µMol)0.08000.08008.540017.0000AID977608
Chain B, Hiv-1 Reverse TranscriptaseHuman immunodeficiency virus 1IC50 (µMol)0.08000.08008.540017.0000AID977608
Chain A, Reverse transcriptase/ribonuclease HHuman immunodeficiency virus 1IC50 (µMol)1.16501.16501.16501.1650AID977608
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)187.53330.11007.190310.0000AID1443980; AID1449628; AID1473738
Prothrombin Bos taurus (cattle)IC50 (µMol)1.15000.00890.88576.0000AID1191671
ReninHomo sapiens (human)Ki7.00000.00001.80787.4000AID198779
Gag-Pol polyproteinHuman immunodeficiency virus type 1 BH10IC50 (µMol)17.29580.08001.71283.9300AID1795322; AID1795327; AID1795330; AID1795355; AID1795358; AID1797479
Gag-Pol polyproteinHuman immunodeficiency virus type 2 (ISOLATE ROD)IC50 (µMol)11.02500.00261.43523.5000AID1795385
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)19.15340.00060.91418.3200AID1795311; AID1795346; AID1795349; AID1795367; AID1795381; AID1795382; AID1795384; AID1795385; AID1795386; AID1795388; AID1795390; AID1795394; AID1795395; AID1795423; AID1795433; AID1795743; AID1796564; AID1796846; AID1802330; AID1802585; AID1803151
Gag-Pol polyproteinHIV-1 M:B_HXB2RKi11.77140.00000.51449.0000AID1798816
Imidazoleglycerol-phosphate dehydrataseSaccharomyces cerevisiae S288CIC50 (µMol)59.63331.70001.70001.7000AID1797479
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)0.18100.00011.753610.0000AID1583030
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)0.18100.00002.800510.0000AID1583030
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)IC50 (µMol)0.69000.00020.10421.7000AID1801807
Ryanodine receptor 1Homo sapiens (human)Ki7.00007.00007.00007.0000AID198779
Kappa-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.70000.00030.71237.0700AID573468
Cannabinoid receptor 1Mus musculus (house mouse)Ki7.20000.00060.72467.2000AID736440
Microsomal triglyceride transfer protein large subunitHomo sapiens (human)IC50 (µMol)5.75000.00000.72635.7500AID266346
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC50 (µMol)0.18000.00021.014010.0000AID299022
Exoribonuclease H Human immunodeficiency virus 2IC50 (µMol)20.00000.00050.01520.0300AID199097
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)32.37100.00011.076810.0000AID104448; AID1057035; AID1059142; AID1060625; AID1069710; AID1072797; AID1124998; AID1126511; AID1141975; AID1141976; AID1141978; AID1161108; AID1165079; AID1171593; AID1171594; AID1171595; AID1171596; AID1171598; AID1175435; AID1187998; AID1191404; AID1191671; AID1197835; AID1200848; AID1206939; AID1231487; AID1235381; AID1248227; AID1249724; AID1275539; AID1290408; AID1292014; AID1292366; AID1298247; AID1298248; AID1298249; AID1298250; AID1298251; AID1298253; AID1304407; AID1320869; AID1352323; AID1373153; AID1379964; AID1391076; AID1410405; AID1410486; AID1418468; AID143385; AID143387; AID1457063; AID1457064; AID1457065; AID1485966; AID1485969; AID1485970; AID1485971; AID1485972; AID1485973; AID1485974; AID1485975; AID1504705; AID1520066; AID1535529; AID1537494; AID1558858; AID1565088; AID1572530; AID1583030; AID1594863; AID1596756; AID1609110; AID1627029; AID1636131; AID1637387; AID1655526; AID1657475; AID1685253; AID1705194; AID1705195; AID1729163; AID1731753; AID1750722; AID1769793; AID1773463; AID1775803; AID1811038; AID1815396; AID1819220; AID1822283; AID1877036; AID1880369; AID1884494; AID197775; AID197776; AID197779; AID197780; AID197782; AID197787; AID197788; AID197792; AID197794; AID197795; AID197796; AID197797; AID197798; AID197799; AID197800; AID197803; AID197807; AID197925; AID197931; AID197932; AID197933; AID197934; AID197941; AID197943; AID197944; AID197946; AID197948; AID198067; AID198068; AID198073; AID198074; AID198075; AID198077; AID198078; AID198080; AID198086; AID198094; AID198228; AID198229; AID198231; AID198234; AID198235; AID198236; AID198239; AID198247; AID198257; AID198258; AID198259; AID198260; AID198396; AID198400; AID198409; AID198410; AID198411; AID198563; AID199102; AID199242; AID199243; AID199521; AID200150; AID200161; AID240924; AID241996; AID242064; AID242248; AID242545; AID266345; AID266346; AID266347; AID266348; AID279321; AID279324; AID279325; AID282736; AID282737; AID282738; AID282739; AID282740; AID286999; AID287002; AID294633; AID294634; AID299022; AID301928; AID317728; AID318120; AID342718; AID360704; AID360705; AID360706; AID360707; AID360708; AID360709; AID360710; AID360711; AID391687; AID391688; AID391690; AID430054; AID457955; AID457959; AID457960; AID457961; AID479214; AID481177; AID510360; AID518734; AID518735; AID518737; AID518738; AID557019; AID557043; AID557044; AID566904; AID573464; AID573465; AID573466; AID573468; AID573469; AID573470; AID606671; AID606672; AID606673; AID606674; AID607877; AID608390; AID619628; AID648425; AID666410; AID698144; AID698145; AID698146; AID717253; AID718366; AID734270; AID735329; AID738336; AID757621; AID779524; AID781021
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Ki348.44320.00031.552310.0000AID198779; AID198906; AID198907; AID198908; AID198909; AID198910; AID198911; AID198912; AID198913; AID198915; AID198916; AID198917; AID302259; AID302260; AID302261; AID302262; AID302263; AID302265; AID368564; AID368565; AID368566; AID368567; AID368568; AID368569; AID370724; AID370725; AID370726; AID370727; AID622047; AID622049; AID622052; AID736038; AID736040; AID736041; AID736438; AID736439; AID736440
Protease Human immunodeficiency virus 1IC50 (µMol)23.10030.00010.22487.3200AID200169; AID200170; AID200171
Cardiac ryanodine receptor 2 Canis lupus familiaris (dog)Ki7.00007.00007.00007.0000AID198779
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Reverse transcriptase Human immunodeficiency virus 1IC50 (µMol)198.67000.01000.53567.1300AID1815391; AID1815397; AID1815398; AID1815399; AID1815400; AID1815401; AID1815402
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC50 (µMol)5.95050.00040.61539.7000AID1056583; AID1373152; AID1373158; AID1373159; AID1373160; AID1373161; AID1373162; AID1373163; AID1410481; AID1410482; AID1456307; AID1456308; AID1483271; AID1483272; AID1483273; AID1483274; AID1483275; AID1483276; AID1483277; AID1750717; AID1750718; AID1750719; AID199992; AID199993; AID199994; AID199995; AID199997; AID199998; AID199999; AID200000; AID240140; AID267854; AID267855; AID267856; AID267858; AID460296; AID757627
Reverse transcriptase Human immunodeficiency virus 1EC50 (µMol)247.83730.00021.16839.0740AID1731746; 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]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)ID5020.00000.40000.40000.4000AID298089
AcetylcholinesteraseRattus norvegicus (Norway rat)ID5035.00000.08000.08000.0800AID650690
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Activity3.26500.00091.30738.0000AID199980; AID279322
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ED503.06520.00020.99359.8000AID105522; AID105535; AID105537; AID105539; AID105543
Reverse transcriptase/RNaseH Human immunodeficiency virus 1ID5011.68210.00602.18989.0000AID1155813; AID1155814; AID1155815; AID1155816; AID1574384; AID1574385; AID1574386; AID1574387; AID242820; AID253490; AID253492; AID253493; AID253494; AID253495; AID257163; AID257164; AID257165; AID267851; AID267862; AID267863; AID298087; AID298088; AID298089; AID298090; AID366526; AID366527; AID366529; AID366531; AID368555; AID368556; AID368557; AID650688; AID650689; AID650690; AID650691; AID650692; AID663305; AID663306; AID663308
Fructose-1,6-bisphosphatase 1 Mus musculus (house mouse)ID508.00000.40004.20008.0000AID368556
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (156)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
proteolysisProthrombin Bos taurus (cattle)
acute-phase responseProthrombin Bos taurus (cattle)
positive regulation of blood coagulationProthrombin Bos taurus (cattle)
protein polymerizationProthrombin Bos taurus (cattle)
kidney developmentReninHomo sapiens (human)
mesonephros developmentReninHomo sapiens (human)
angiotensin maturationReninHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionReninHomo sapiens (human)
proteolysisReninHomo sapiens (human)
regulation of blood pressureReninHomo sapiens (human)
male gonad developmentReninHomo sapiens (human)
hormone-mediated signaling pathwayReninHomo sapiens (human)
response to lipopolysaccharideReninHomo sapiens (human)
response to immobilization stressReninHomo sapiens (human)
drinking behaviorReninHomo sapiens (human)
regulation of MAPK cascadeReninHomo sapiens (human)
cell maturationReninHomo sapiens (human)
amyloid-beta metabolic processReninHomo sapiens (human)
response to cAMPReninHomo sapiens (human)
response to cGMPReninHomo sapiens (human)
cellular response to xenobiotic stimulusReninHomo sapiens (human)
juxtaglomerular apparatus developmentReninHomo sapiens (human)
viral life cycleGag-Pol polyproteinHIV-1 M:B_HXB2R
establishment of integrated proviral latencyGag-Pol polyproteinHIV-1 M:B_HXB2R
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
response to hypoxiaRyanodine receptor 1Homo sapiens (human)
outflow tract morphogenesisRyanodine receptor 1Homo sapiens (human)
calcium ion transportRyanodine receptor 1Homo sapiens (human)
muscle contractionRyanodine receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosol by sarcoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
calcium-mediated signalingRyanodine receptor 1Homo sapiens (human)
response to caffeineRyanodine receptor 1Homo sapiens (human)
skin developmentRyanodine receptor 1Homo sapiens (human)
ossification involved in bone maturationRyanodine receptor 1Homo sapiens (human)
skeletal muscle fiber developmentRyanodine receptor 1Homo sapiens (human)
release of sequestered calcium ion into cytosolRyanodine receptor 1Homo sapiens (human)
protein homotetramerizationRyanodine receptor 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationRyanodine receptor 1Homo sapiens (human)
cellular response to calcium ionRyanodine receptor 1Homo sapiens (human)
cellular response to caffeineRyanodine receptor 1Homo sapiens (human)
striated muscle contractionRyanodine receptor 1Homo sapiens (human)
lipid metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
circadian rhythmMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein secretionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
sterol transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
low-density lipoprotein particle remodelingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
plasma lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
chylomicron assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
very-low-density lipoprotein particle assemblyMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
response to calcium ionMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
establishment of localization in cellMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
intermembrane lipid transferMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transportMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipoprotein metabolic processMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol homeostasisMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (91)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
serine-type endopeptidase activityProthrombin Bos taurus (cattle)
calcium ion bindingProthrombin Bos taurus (cattle)
protein bindingProthrombin Bos taurus (cattle)
fibrinogen bindingProthrombin Bos taurus (cattle)
aspartic-type endopeptidase activityReninHomo sapiens (human)
signaling receptor bindingReninHomo sapiens (human)
insulin-like growth factor receptor bindingReninHomo sapiens (human)
protein bindingReninHomo sapiens (human)
peptidase activityReninHomo sapiens (human)
peptidase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
integrase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome 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 oxygenCytochrome P450 2C9 Homo sapiens (human)
ryanodine-sensitive calcium-release channel activityRyanodine receptor 1Homo sapiens (human)
voltage-gated calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium ion bindingRyanodine receptor 1Homo sapiens (human)
calmodulin bindingRyanodine receptor 1Homo sapiens (human)
ATP bindingRyanodine receptor 1Homo sapiens (human)
intracellularly gated calcium channel activityRyanodine receptor 1Homo sapiens (human)
calcium-induced calcium release activityRyanodine receptor 1Homo sapiens (human)
lipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
lipid bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
apolipoprotein bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein-containing complex bindingMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
protein heterodimerization activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylcholine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cholesterol transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
triglyceride transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
ceramide 1-phosphate transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phosphatidylethanolamine transfer activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
phospholipid transporter activityMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (48)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
plasma membraneReninHomo sapiens (human)
apical part of cellReninHomo sapiens (human)
extracellular spaceReninHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmRyanodine receptor 1Homo sapiens (human)
plasma membraneRyanodine receptor 1Homo sapiens (human)
cell cortexRyanodine receptor 1Homo sapiens (human)
junctional sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
terminal cisternaRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
organelle membraneRyanodine receptor 1Homo sapiens (human)
I bandRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
extracellular exosomeRyanodine receptor 1Homo sapiens (human)
ryanodine receptor complexRyanodine receptor 1Homo sapiens (human)
Z discRyanodine receptor 1Homo sapiens (human)
sarcolemmaRyanodine receptor 1Homo sapiens (human)
smooth endoplasmic reticulumRyanodine receptor 1Homo sapiens (human)
sarcoplasmic reticulum membraneRyanodine receptor 1Homo sapiens (human)
calcium channel complexRyanodine receptor 1Homo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulum lumenMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
cytosolMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
brush border membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
microvillus membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
vesicleMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
receptor complexMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
Golgi apparatusMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
endoplasmic reticulumMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
basolateral plasma membraneMicrosomal triglyceride transfer protein large subunitHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2791)

Assay IDTitleYearJournalArticle
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID622057Ratio of Ki for HIV1 RT p66/p66 homodimer G190A mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID106053Inhibitory activity against 100I strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID82462Antiviral activity against K103N/P225H strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID248264In vitro inhibitory concentration against HIV Y188L mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID279480Antiviral activity against HIV1 isolate with RT 100F mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279463Antiviral activity against HIV1 isolate with RT 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1574373Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2019Journal 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.
AID1637393Antiviral 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 assay2016Bioorganic & 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.
AID557045Antiviral activity against HIV1 CRF17_BF harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID440071Antiviral activity against HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1574390Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p512019Journal 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.
AID508644Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID1161105Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID226239Fold resistance (L100I/ WT) (as per ref 7 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID632800Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection2011Journal 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.
AID1654213Drug metabolism in human primary hepatocytes assessed as Cytochrome P450-mediated formation of 2-OHNVP at 10 uM incubated for 24 to 48 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID302267Resistance index, ratio of Ki for HIV1 reverse transcriptase L100I mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID248880Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID298079Antiviral activity against HIV1 RT 112 mutant in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID106769Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50%2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID499278Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV1 3B2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
AID1197831Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID523356Antiviral activity against HIV1 with RT connection domain Y181C/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID279411Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID248846Inhibitory concentration against human immunodeficiency virus type 1 (with Y188C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID573475Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay2009Antimicrobial 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.
AID1335201Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID279437Antiviral activity against HIV1 isolate with RT 103N, 108I, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID557047Antiviral activity against HIV1 clade D harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1750722Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal 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
AID1457066Inhibition 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 scintilla2017Journal 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.
AID1565095Antiviral 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
AID361906Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1574378Antiviral 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 assay2019Journal 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.
AID82460Antiviral activity against K103N/G190A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID198911Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID1124992Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2014Bioorganic & 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.
AID105716Antiviral activity against HIV-1 (strain RF) infected MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID244633Selective index value (ratio of CC50 to IC50 value)against HIV LAI cell line2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1729156Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID1729152Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID1249715Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269798Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1485973Inhibition of HIV-1 reverse transcriptase Y181C mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1773455Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells
AID297137Antiviral activity against wild type HIV1 NL4-3 by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID666414Antiviral activity against NNRTI-resistant HIV1 A17 expressing reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral p24 antigen production after 7 days by ELISA2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID1163254Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1303216Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Design, synthesis and anti-HIV activity of novel quinoxaline derivatives.
AID198078Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID725390Cytotoxicity against human CEmx174 cells expressing LTR-GFP2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors.
AID1141978Inhibition of HIV1 wild-type reverse transcriptase L1001 mutant using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID299022Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID105693Anti-HIV-1 activity against K1001 strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID257917Antiviral activity against HIV1 Y181C mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID1357783Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1485974Inhibition of HIV-1 reverse transcriptase Y188L mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1391081Antiviral 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 assay2018Bioorganic & 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.
AID226240Fold resistance (L100I/ WT) (as per ref 8 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID342721Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID522377Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A/V179D mutant clone to EC50 for wild type HIV12010Antimicrobial 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.
AID1761020Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID198247Inhibitory concentration against HIV-1 wild type Reverse transcriptase (RT)1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID279396Antiviral activity against HIV1 isolate with RT 103N, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1443668Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID297141Antiviral activity against HIV1 with RT V108I mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID413566Ratio of EC50 for multidrug-resistant HIV1with reverse transcriptase clone 7324-1 to EC50 for wild type HIV1 3B2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID1200845Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID248841Inhibitory concentration against human immunodeficiency virus type 1 (with G190A resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID322392Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs).
AID1171598Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity2014Journal 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.
AID586904Activity at BCRP2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1191403Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2015Bioorganic & 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.
AID281489Selectivity index, CC50 for MT4 cells/IC50 for HIV1 3B2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID298078Antiviral activity against wild type HIV1 3B in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1637404Selectivity 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 cells2016Bioorganic & 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.
AID1741400Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based fluorescence assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID492287Antiviral activity against HIV1 with reverse transcriptase F227L, V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID573480Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial 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.
AID282738Inhibition of HIV1 RT V106A mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1171588Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32014Journal 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.
AID1292366Inhibition of HIV1 reverse transcriptase using 234-nt long RNA/18-mer DNA oligonucleotide as template/primer preincubated for 15 mins followed by incubation with template/primer for 40 mins by liquid scintillation counting in presence of alpha[P33]-dCTP2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1483281Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B2017Journal 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.
AID1565099Antiviral 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
AID322394Selectivity index, Ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs).
AID508783Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1736356Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID650693Ratio of ID50 for HIV 1 reverse transcriptase Y188L mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1610053Antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID1357793Antiviral 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 assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID361905Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/P225H mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID726437Antiviral 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 method2013Bioorganic & 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.
AID279430Antiviral activity against HIV1 isolate with RT 103N, 106I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1320864Antiviral 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 assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID28979Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1290408Inhibition of recombinant HIV1 His-tagged p66/p51 reverse transcriptase expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)-oligo(dT) (12 to 18 bp) as template/primer incubated for 20 mins by scintillation counting2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID1056578Antiviral activity against HIV-1 expressing reverse transcriptase K103N/P225H double mutant infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1636135Inhibition of Escherichia coli RNA polymerase2016Journal 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.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1637388Antiviral 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 assay2016Bioorganic & 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.
AID607875Cytotoxic activity against human MT4 cells assessed as viability of mock-infected cells after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1316806Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-1 3B infected in human MT-4 cells2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity.
AID443757Antiviral activity against HIV1 with reverse transcriptase Y181L mutation2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID247496Inhibitory activity against HIV-1 mutant strain 101E2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1059146Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID476469Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus replication by MTT assay2010Bioorganic & 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.
AID246153Concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID717257Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1574384Inhibition 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 analysis2019Journal 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.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263153Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID391991Inhibition of HIV1 reverse transcriptase at 100 ug/ml after 1 hr by microtiter plate ELISA2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID735329Inhibition of HIV-1 reverse transcriptase assessed as decrease in incorporation of [3H]TTP into polyA template2013Journal of natural products, Apr-26, Volume: 76, Issue:4
Cytotoxic, antitopoisomerase IIα, and anti-HIV-1 activities of triterpenoids isolated from leaves and twigs of Gardenia carinata.
AID105540Inhibitory activity against HIV-1 Wild Type in MT-4 cell culture (human T-cell line with 50% human AB serum)1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1558853Antiviral 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1483269Antiviral 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 assay2017Journal 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.
AID573474Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay2009Antimicrobial 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.
AID518742Selectivity 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 transcriptase2010Antimicrobial 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.
AID666413Antiviral activity against HIV1 SF33 infected in human MT4 cells assessed as inhibition of viral p24 antigen production after 7 days by ELISA2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID587747Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID587755Antiviral activity against HIV1 NL4-3.Luc in human MDM assessed as infectivity treated for 24 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID246786Concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1077220Cytotoxicity against human MT4 cells assessed as growth inhibition after 5 days by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID508795Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID197933HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1880372Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID632804Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay2011Journal 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.
AID1637401Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y181C mutant infected in human MT4 cells2016Bioorganic & 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.
AID405582Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID571978Antiviral activity against HIV-1 subtype B V022810 harboring NNRTI A98S andK101R mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID46376Antiviral activity against site directed resistant isolate HIV-1 K101E in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID663306Inhibition of HIV1 recombinant reverse transcriptase K103N mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID496616Antiviral 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 control2010Antimicrobial 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.
AID1687687Selectivity 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 cytopa2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID734261Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 A17 infected in human MT4 cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1822273Antiviral 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 assay2022Journal 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.
AID293562Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1565100Antiviral 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
AID1877038Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 3 days by XTT assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
AID508655Selectivity index, ratio of CC50 human MT4 cells to EC50 for Human immunodeficiency virus 12010Antimicrobial 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.
AID525105Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID287003Inhibition of drug-resistant reverse transcriptase T181C mutant2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID82465Antiviral activity against L100I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1171590Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-32014Journal 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.
AID1743637Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID395597Selectivity index, ratio of CC50 for human CEM cells to EC50 for HIV1 3B2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
AID257918Antiviral activity against HIV1 V106A mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID492282Antiviral activity against HIV1 with reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID279426Antiviral activity against HIV1 isolate with RT 227L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID368559Antiviral activity against HIV1 reverse transcriptase K103N mutant infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID293563Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID232981Selectivity index; ND = Not determined2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
AID1435517Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase F227L/V106A double mutant
AID1316344Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells2016Journal 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.
AID481177Inhibition of HIV1 reverse transcriptase by ELISA2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID197800Compound was tested for inhibitory activity against HIV-1 wild type reverse transcriptase1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
AID1460929Antiviral activity against HIV-1 Bal infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID571971Antiviral activity against HIV-1 subtype CRF01_AE V022820 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID391678Antiviral activity against HIV1 infected in human 293T cells assessed as inhibition of pseudovirus infection2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID650694Ratio of ID50 for HIV 1 reverse transcriptase Y181I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1069707Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248316In vitro inhibitory concentration against HIV-1 Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID527562Antiviral activity against HIV1 NL4-3 containing reverse transcriptase K103N mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID279412Antiviral activity against HIV1 isolate with RT 103N, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279403Antiviral activity against HIV1 isolate with RT 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1316336Antiviral 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 assay2016Journal 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.
AID1565097Antiviral 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
AID361917Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1303215Cytotoxicity against human MT4 cells infected with HIV1 3B assessed as cell growth inhibition after 5 days by MTT assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Design, synthesis and anti-HIV activity of novel quinoxaline derivatives.
AID257165Inhibition of Y181I mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID279418Antiviral activity against HIV1 isolate with RT 98G, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID619641Ratio 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 cells2011European 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.
AID1483278Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2017Journal 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.
AID573470Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay2009Antimicrobial 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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID698294Antiviral activity against HIV1 IRLL98 containing reverse transcriptase K101Q, Y181C and G190A mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal 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.
AID299023Antiviral activity against HIV1 assessed as reduction of virus-induced cytopathic effect in MT4 cells2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1880377Antiviral activity against HIV-1 IIIB harboring reverse transcriptase K103N mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID267648Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID370725Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID558379Drug level in HIV-infected pregnant woman cord blood plasma at 200 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID1162261Antiviral activity against X4 tropic HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 2 to 3 days by MTT assay2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Semi-synthesis of oxygenated dolabellane diterpenes with highly in vitro anti-HIV-1 activity.
AID1171586Antiviral 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 assay2014Journal 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.
AID1282049Cytotoxicity against human U2OS cells assessed as cell viability at highest non-toxic concentration2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Antiretroviral (HIV-1) activity of azulene derivatives.
AID348907Ratio of ED50 for drug resistant HIV1 with reverse transcriptase K103N mutant to wild type HIV1 NL4-32008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID105123Dose required to achieve 50% protection of MT-4 cells from the HIV-1 induced cytopathogenicity in mock-infected MT-4 cells1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID586319Antiviral activity against Human T-cell leukemia/lymphoma virus type 1 infected in human PBMC assessed as inhibition of tax/rex gene expression after 3 weeks post infection by quantitative real time RT-PCR2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID1627026Cytotoxicity against HIV1 infected human PBMC cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1591876Solubility of the compound in water at pH 72019Bioorganic & 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.
AID1636929Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID718369Selectivity index, ratio of CC50 for HIV1 3B infected in human MT4 cells to EC50 for HIV1 3B2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID1754639Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Antiviral activity against HIV-1 IIIB infected in human MT4 cells2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1185993Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV12014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1186004Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID226238Fold resistance (L100I/ WT) (as per ref 6 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID1197830Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID1316342Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells2016Journal 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.
AID1736364Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID443755Antiviral activity against HIV1 with reverse transcriptase K103N mutation2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID443756Antiviral activity against HIV1 with reverse transcriptase Y181C mutation2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID234267Selectivity index, ratio of CC50 to EC502000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
AID557039Antiviral 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% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID279322Inhibition of reverse transcriptase in HIV1 Z6gpt assessed as inhibition of ssDNA synthesis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID508642Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID551464Antiviral activity against HIV1 3B infected in human C8166 cells assessed as protection against virus-induced cytopathogenicity after 3 days2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents.
AID566899Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by microtiter plate analysis2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.
AID1457054Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2017Journal 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.
AID1072802Cytotoxicity against human MT4 cells after 5 days by MTT assay2014Bioorganic & 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.
AID1483276Inhibition of HIV1 3B reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal 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.
AID371909Antiviral activity against HIV1 NL4-3 with L100I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID368567Inhibition of HIV1 recombinant free reverse transcriptase K103N mutant expressed in Escherichia coli BL212009Journal 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.
AID1357789Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1862267Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.
AID1754641Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID650544Antiviral 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 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1072801Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2014Bioorganic & 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.
AID508654Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID391992Antiviral activity against HIV1 3B replication in human CEM cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID650541Resistance ratio of EC50 for multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID572175Antiviral activity against HIV-1 subtype F V029522 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID371904Antiviral activity against HIV1 NL4-3 with K103N/L100I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID363038Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV1 3B2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
AID1248227Inhibition of recombinant HIV1 Reverse transcriptase p66/p51 using poly (rA)-oligo (dT) as template primer after 40 mins by spectrofluorometric analysis2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1888700Resistance 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
AID666973Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID1460943Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase Y181C mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1446814Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID104944Concentration which reduced the viability of the HIV-1 infected MT-4 cells to 50% compared to untreated control cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID198746In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) at a concentration of 10 ug/mL.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
AID373574Half life in plasma of HIV1-infected patient administered as single dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID279478Antiviral activity against HIV1 isolate with RT 106L, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1773459Resistance factor, ratio of EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID508761Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, F227L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1443664Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID246266Effective concentration against human immunodeficiency virus type 1 K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID293564Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1743627Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID346973Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 3B2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Studies on anti-HIV quinolones: new insights on the C-6 position.
AID88364Antiviral activity against E138K mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID630953Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 subtype B-ADA52011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1352315Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID698300Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-32012Journal 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.
AID391995Antiviral activity against HIV2 ROD replication in human CEM cells assessed as inhibition of virus-induced cytopathic effect at subtoxic concentration after 5 days by tetrazolium-based colorimetric assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID1443660Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID279457Antiviral activity against HIV1 isolate with RT 98G, 101E, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1155814Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1654219Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as 12-O-GlucD2NVP metabolite formation at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID1815393Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID263516Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1357792Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID571977Antiviral activity against HIV-1 subtype B V022809 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1610045Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells measured upto 24 hrs by bright Glo-luciferase reporter gene assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269796Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1298251Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID1811039Anti-viral activity against HIV1 harboring RT L100I mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID1729151Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID1304407Inhibition 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 primer2016Bioorganic & 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.
AID282737Inhibition of HIV1 RT K103N mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID430055Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID1457056Antiviral 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 assay2017Journal 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.
AID587754Antiviral activity against HIV1 NL4-3.Luc in human PBMC assessed as infectivity treated for 24 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID105572Antiviral activity was determined against wild type HIV-1 in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1163255Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID82458Antiviral activity against K101E strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID779524Inhibition 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 analysis2013Bioorganic & 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.
AID508765Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M236L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1217709Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID279470Antiviral activity against HIV1 isolate with RT 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1316328Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells2016Journal 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.
AID105547Tested for the inhibition of wild type HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1574388Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p512019Journal 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.
AID1460931Antiviral activity against HIV-1 Bal infected in human PBMC by MTS assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID248354Concentration required to inhibit 50% viral production of human immunodeficiency virus type 1 (HIV-1-IIIB)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269794Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID734267Cytotoxicity against human MT4 cells after 3 days by XTT assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1435503Antiviral 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
AID199242Inhibitory effect on recombinant HIV- 1 reverse transcriptase which has a mutation Leu 100 to Ile 100 (clone 118)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID496618Antiviral 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 control2010Antimicrobial 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.
AID523486Antiviral activity against HIV1 with RT connection domain L100I/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID587757Ratio of EC50 for HIV1 NL4-3.Luc assessed as infectivity using human MDM pretreated for 24 hrs followed by exposed to virus after compound washout to standard EC50 for HIV1 NL4-3.Luc2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID1267611Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1057036Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID248261In vitro inhibitory concentration against HIV L100I mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID253493Dose required to inhibit HIV-1 reverse transcriptase activity (Y181I mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID779527Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & 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.
AID257166Antiviral activity against wild type HIV1 NL4-3 infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1069708Cytotoxicity against human MT4 cells assessed as cell viability2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248260In vitro inhibitory concentration against HIV K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1457057Antiviral 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 assay2017Journal 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.
AID1298245Cytotoxicity against human MT4 cells after 5 days MTT assay2016Bioorganic & 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.
AID1815384Antiviral 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 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1736368Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID1390713Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells2018Bioorganic & 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.
AID1056577Ratio of EC50 for HIV-1 expressing reverse transcriptase K103N mutant to EC50 for wild-type HIV-12013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1391077Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & 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.
AID247619Inhibitory activity against HIV-1 double mutants strain 103N and 181C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID279451Antiviral activity against HIV1 isolate with RT 101E, 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID395594Antiviral activity against HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
AID482695Antiviral activity against HIV1 NL4-3 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID279325Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID584081Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, H221Y, F227F/L, M230M/I mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID199992Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 12 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID106609Cytotoxic concentration that reduces the MT-4 cell viability by 50%2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID1249721Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID571984Antiviral activity against HIV-1 subtype C V022816 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID361922Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID198231Inhibition of purified recombinant HIV-1 reverse transcriptase1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID29361Dissociation constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1157587Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID294631Cytotoxicity against CEM cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID267862Inhibition of HIV1 reverse transcriptase K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID1186685Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection from viral cytopathicity after 5 days by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID440638Antiviral activity against NNRTI-resistant HIV1 NL4-3 with reverse transcriptase K103N mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
AID1822277Antiviral 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 assay2022Journal 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.
AID1773444Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells
AID523484Antiviral activity against HIV1 with RT connection domain L100I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID106065Inhibitory activity against 181C strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1520037Antiviral activity against VSV-G pseudotyped HIV1 transfected in human 293T cells co-transfected with NL4-3 HIV1 supernatant infected in human SupT1 cells treated with compound for 48 hrs assessed as inhibition of viral infection at 100 nM after 48 hrs by2020European journal of medicinal chemistry, Jan-01, Volume: 185Preliminary SAR and biological evaluation of potent HIV-1 protease inhibitors with pyrimidine bases as novel P2 ligands to enhance activity against DRV-resistant HIV-1 variants.
AID1815386Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1435502Antiviral 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
AID650689Inhibition of HIV 1 reverse transcriptase K103N mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID523347Antiviral activity against HIV1 with RT connection domain N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID82470Antiviral activity against V106I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1729149Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID267859Cytotoxicity against MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID302254Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID449491Cytotoxicity against human MT4 cells as reduction in cell viability after 5 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID198235Inhibitory activity against HIV rRT activity in mutant HIV-1 strain resistant to Nevirapine (Y181C)1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID1373152Inhibition of reverse transcriptase Y181C mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID361928Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1157582Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID660088Inhibition of HIV-1 reverse transcriptase at 20 ug after 1 hr by colorimetry2012Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9
Synthesis, biological activity and docking study of imidazol-5-one as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508785Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1186002Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1565093Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID734256Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 harboring reverse transcriptase Y181C mutation infected in human TZM-bl cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID246359Protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID226250Y181C/WTIIIB ratio of the compound2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1410488Inhibition of HIV1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay2018ACS 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.
AID263522Antiviral activity against HIV1 F227L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID698145Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal 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.
AID82474Antiviral activity against Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID279472Antiviral activity against HIV1 isolate with RT 103S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID302621Cytotoxicity against human MT2 cells by MTT assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
From docking false-positive to active anti-HIV agent.
AID1743630Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID371907Antiviral activity against HIV1 NL4-3 with Y181L mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID198094Inhibitory activity against HIV-1 recombinant reverse transcriptase.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID443758Antiviral activity against HIV1 with reverse transcriptase G190A mutation2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID440084Antiviral activity against HIV1 HXB2 harboring 100I and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1572530Inhibition 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
AID1574387Inhibition 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 analysi2019Journal 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.
AID1175436Antiviral activity against wild-type HIV-1 SF33 infected in human TZM-bl cells after 7 days by ELISA2015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.
AID298074Antiviral activity against HIV1 3B in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID246274Effective concentration against rhuman immunodeficiency virus type 1 L100I mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID508787Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID491827Antiviral activity against HIV1 with reverse transcriptase 8605MR mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1418464Antiviral 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 assay2018Bioorganic & 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.
AID246481Effective concentration against human immunodeficiency virus type 1 mutated at 227C; ND:Not determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1483280Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B2017Journal 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.
AID360706Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID46377Antiviral activity against site directed resistant isolate HIV-1 K103N in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1636146Antiviral activity against wild type HIV1 NL4-32016Journal 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.
AID1304401Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2016Bioorganic & 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.
AID248843Inhibitory concentration against human immunodeficiency virus type 1 (with V106A resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1591874Antiviral activity against HIV1 NL4-3 harboring Y181C mutant infected in human MT2 cells measured 48 hrs post-infection by MTT assay2019Bioorganic & 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.
AID105143Concentration required to achieve 50% protection of MT-4 cells from HIV-1-induced cytopathogenicity.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1736154Inhibition of wild type recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodimer expressed in Escherichia coli BL21 (DE3) assessed as inhibition of dTTP incorporation on poly(rA)-oligo(dT) template primer duplex at 100 uM preincubated wi2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID735082Antiviral activity against wild type HIV by cell based assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID1443666Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID246779Concentration required to reduce the amount of p24 by 90% in wtIIIB-HIV-1-infected C8166 cells2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID371896Antiviral activity against wild type HIV1 NL4-3 in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1884541Fold 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 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1442776Inhibition of HIV1 reverse transcriptase by colorimetric assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Synthesis, Antiviral Potency, in Vitro ADMET, and X-ray Structure of Potent CD4 Mimics as Entry Inhibitors That Target the Phe43 Cavity of HIV-1 gp120.
AID248842Inhibitory concentration against human immunodeficiency virus type 1 (with K103N resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1888701Resistance 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
AID1357785Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1637390Cytotoxicity against mock-infected human MT4 cells assessed as reduction of cell viability after 5 days by MTT assay2016Bioorganic & 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.
AID522373Antiviral 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 microscopy2010Antimicrobial 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.
AID443754Antiviral activity against HIV1 PNL4-32010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID1155809Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID346972Cytotoxicity against mock-infected human MT4 cells by MTT assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Studies on anti-HIV quinolones: new insights on the C-6 position.
AID1880376Antiviral activity against HIV-1 IIIB harboring reverse transcriptase L1001 mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID496622Antiviral 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 control2010Antimicrobial 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.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269801Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1056575Ratio of EC50 for HIV-1 expressing reverse transcriptase K103N/V108I double mutant to EC50 for wild-type HIV-12013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID586321Inhibition of HIV1 3B reverse transcriptase activity infected in human H9 cells assessed as level of p24 antigen2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID1884488Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1485967Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID614141Antiviral 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 assay2011Bioorganic & 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.
AID1418466Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2018Bioorganic & 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.
AID279417Antiviral activity against HIV1 isolate with RT 106A, F227L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID305057Antiviral activity against HIV in HEK293T cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
4-Aminopyrimidines as novel HIV-1 inhibitors.
AID718368Cytotoxicity against HIV2 ROD infected in human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID199997Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 12 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID440075Antiviral activity against HIV1 HXB2 harboring Y188L mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269689Antiviral activity against HIV1 NNTRI resistant L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1057037Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in MT4 cells2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID508786Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1191400Antiviral 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 assay2015Bioorganic & 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.
AID199995Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 8 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID478386Inhibition of HIV1 RT after 1 hr by ELISA relative to control2010Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9
Design of potential reverse transcriptase inhibitor containing Isatin nucleus using molecular modeling studies.
AID1249723Antiviral activity against HIV1 expressing reverse transcriptase F227L + V106A mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID361908Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID518735Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay2010Antimicrobial 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.
AID371897Selectivity index, ratio of CC50 for human TZM-b1 cells to EC50 for HIV1 NL4-32009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID361924Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/V108I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID440074Antiviral activity against HIV1 HXB2 harboring Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID508778Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID197779Ability to inhibit HIV-1 Reverse Transcriptase (RT) using an rC-dG template/primer1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID606674Inhibition of HIV1 reverse transcriptase V179D mutant2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID496620Antiviral 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 control2010Antimicrobial 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.
AID198228Inhibitory activity against recombinant HIV-1 reverse transcriptase (rRT)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID279467Antiviral activity against HIV1 isolate with RT 106A, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID263517Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID198411Tested for the inhibition of wild type HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1267612Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-2 ROD2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1517761Inhibition of HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in biotin-dUTP incorporation at 500 nM using poly(A)/oligo (dT)15 as template/primer by ELISA2019European journal of medicinal chemistry, Dec-01, Volume: 183Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity.
AID1882468Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal 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.
AID248844Inhibitory concentration against human immunodeficiency virus type 1 (with V108I resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID267863Inhibition of HIV1 reverse transcriptase Y181I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID265467Antiviral activity against HIV1 3B in MT4 cell line2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID366524Antiviral activity against HIV1 isolates with reverse transcriptase Y188L mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID371911Antiviral activity against HIV1 NL4-3 with Y181C mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID738335Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1483277Inhibition 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 assay2017Journal 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.
AID248493In vitro inhibitory concentration value against HIV K103N and Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1171585Antiviral 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 assay2014Journal 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.
AID757625Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID373561Half life in plasma of HIV1-infected patient2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID508764Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1773452Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells
AID198236Inhibitory activity against HIV rRT activity in wild type IIIB strain1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID1304403Cytotoxicity against mock-infected human MT4 cells2016Bioorganic & 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.
AID1373156Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID663299Cytotoxicity against human MT4 cells after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID685331Antiviral activity against HIV-1 3B infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID693583Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID522372Antiviral 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 microscopy2010Antimicrobial 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.
AID1743629Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID82463Antiviral activity against K103N/V108I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1235381Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin deoxyuridine triphosphate (biotin-dUTP) incorporation using poly(rA)/oligo (dT)16 template and primer by spectrofluorometry2015Bioorganic & 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.
AID106967Concentration required to inhibit HIV-1 induced cytopathicity in MT-4 cells by 50%1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro -5''- (4''-amino-1'',2''-oxathiole 2'',2''-dioxide) pyrimidine and pyrimidine-modified nucleosides.
AID1763904Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1304408Antiviral 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 assay2016Bioorganic & 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.
AID1729150Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID592540Cytotoxicity against human CEM cells by coulter counter analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID247502Inhibitory activity against HIV-1 mutant strain 188L2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID613685Induction of human A375 cell differentiation assessed as formation of vimentin intermediate filament at 20 uM after 96 hrs by immunofluorescence analysis2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID734265Antiviral activity against Human immunodeficiency virus 1 SF33 infected in human MT4 cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1561720Resistance 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
AID584082Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase L100I, K103Q, H221H/Y mutant infected in human SupT1 cells derived from 11 viral passages with efavirenz assessed as inhibition of viral replication after 21 days relative to drug sensi2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1822278Antiviral 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 assay2022Journal 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.
AID614139Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 IIIB infected in human MT4 cells2011Bioorganic & 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.
AID106977Effective concentration against HIV-1 induced cytopathicity in MT-4 cells using MTT method2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
AID1390712Cytotoxicity against human MT4 cells after 5 days by MTT assay2018Bioorganic & 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.
AID1056576Ratio of EC50 for HIV-1 expressing reverse transcriptase L100I/K103N double mutant to EC50 for wild-type HIV-12013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1627027Cytotoxicity against HIV1 infected human CEM cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1609104Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1059145Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1761008Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1165076Antiviral 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 assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID351446Antiviral activity against HIV2 ROD in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by MTT assay2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1357791Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1884539Fold 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 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID523348Antiviral activity against HIV1 with RT connection domain T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID94314Antiviral activity against HIV-1 K103N mutant virus.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID198563The compound was evaluated for the inhibition of HIV-1 reverse transcriptase2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
AID1171584Antiviral 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 assay2014Journal 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.
AID297134Inhibition of HIV1 NL4-3 reverse transcriptase2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID279466Antiviral activity against HIV1 isolate with RT 103N, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508638Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID279458Antiviral activity against HIV1 isolate with RT 103Q mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID571972Antiviral activity against HIV-1 subtype CRF01_AE V022821 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID457960Inhibition of HIV1 reverse transcriptase Y181I mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID279432Antiviral activity against HIV1 isolate with RT 181I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID572184Antiviral activity against HIV-1 SM026 harboring NNTRI 103N and 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID781026Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against viral-induced cytotoxicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
AID607873Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1574377Antiviral 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 assay2019Journal 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.
AID279454Antiviral activity against HIV1 isolate with RT 100I, 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID302253Antiviral activity against HIV1 with reverse transcriptase K103N mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID265472Activity against HIV-112 assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID263518Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID619636Antiviral 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 assay2011European 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.
AID572183Antiviral activity against HIV-1 SM024 harboring NNTRI 190A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID622048Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer V106A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1235383Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity added 3 to 5 hrs post infection and measured 31 hrs post infection by p24 enzyme-linked immunosorbent assay2015Bioorganic & 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.
AID1811035Anti-viral activity against HIV1 harboring RT Y188L mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID440632Antiviral activity against HIV1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
AID734258Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 harboring reverse transcriptase K103N mutation infected in human TZM-bl cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1691437Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID734264Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for Human immunodeficiency virus 1 SF33 infected in human TZM-bl cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1316346Selectivity 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 cells2016Journal 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.
AID1888689Antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID298077Cytotoxicity against lymphocytes2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID88367Antiviral activity against K103N/L100I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID622050Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y188L mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID88368Antiviral activity against K103N/P225H mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1636131Inhibition of HIV1 reverse transcriptase using T19-Cy5 labeled 23-mer DNA/T2-TAMRA labeled 63-mer DNA as primer/template assessed as inhibition of dNTP incorporation into primer/template2016Journal 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.
AID1754643Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID586325Cytotoxicity against human MOLT3 cells after 24 hrs by MTS assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID368566Inhibition of wild type HIV1 reverse transcriptase-DNA-dNTP ternary complex2009Journal 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.
AID619638Antiviral 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 assay2011European 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.
AID279439Antiviral activity against HIV1 isolate with RT 101P, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1558855Antiviral 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1811034Anti-viral activity against HIV1 harboring RT E138K mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID440670Antiviral activity against NNRTI-resistant HIV1 N119 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID523345Antiviral activity against HIV1 with RT connection domain T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID591356Antiviral activity against wild type HIV1 3B infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID1736357Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID606671Inhibition of HIV1 wild type reverse transcriptase2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
AID1126511Inhibition of wild-type HIV1 reverse transcriptase p66/p51 after 40 mins by spectrophotometry2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID650542Antiviral activity against multidrug-resistant HIV 1 IRLL98 harboring reverse transcriptase K101Q/Y181C/G190a mutant infected in human MT4 cells assessed as virus-induced cytopathic effect after 5 days by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID155278Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain HTLV IIIB in peripheral blood mononuclear cells (PBMC)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID83547Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala2004Journal 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
AID1504705Inhibition 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 ELISA2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Discovery of Thiophene[3,2-
AID440072Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID361911Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase L100I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID46383Antiviral activity against site directed resistant isolate HIV-1 Y188C in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1163230Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID302269Resistance index, ratio of Ki for NNRTI-resistant HIV1 reverse transcriptase V179D mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1249713Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID88370Antiviral activity against K103N/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID623212Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1248223Cytotoxicity against uninfected human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID235446Selective index (CD50 compared to ED50 against HIV-1 IIIB strain).2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1743631Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269800Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID200000Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 8 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID298088Inhibition of HIV1 RT K103N mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1880374Selectivity 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 cells2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID248255In vitro inhibitory concentration against HIV E138K mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID279462Antiviral activity against HIV1 isolate with RT 103N, 108I, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1446818Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1155818Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID551465Cytotoxicity against human C1866 cells after 72 hrs by MTT assay2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents.
AID1736352Cytotoxicity against human HEK 293T cells assessed as cell viability at 30 uM measured after 48 hrs by Celltiter-glo assay
AID1152242Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 3B subtype B2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID198258Inhibitory concentration against mutant reverse transcriptase of K103N was determined which is in turn resistant to pyridinones1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID106978Effective concentration against HIV-1 induced cytopathogenicity in MT-4 cells2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1815398Inhibition of HIV1 reverse transcriptase K103N mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID46205Tested for the inhibitory activity of virus induced giant cell formation in HIV-2 infected CEM cells1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID1380570Resistance index, ratio of IC50 for antiviral activity against HIV1 virions containing reverse transcriptase K103N mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells to IC50 for antiviral activity ag2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID510359Inhibition of HIV1 recombinant protease2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.
AID1729153Selectivity 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 cells2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID279413Antiviral activity against HIV1 isolate with RT 106A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279424Antiviral activity against HIV1 isolate with RT 103N, 106A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID655386Antiviral activity against HIV1 LAI infected in CEMx174 cells coexpressing GFP after 5 days by fluorimetry2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability.
AID279438Antiviral activity against HIV1 isolate with RT 98G, 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279456Antiviral activity against HIV1 isolate with RT 188H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1657475Inhibition of wild type recombinant HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by picogreen dye-based spectrofluorometric method2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1267619Cytotoxicity against human HUT78 cells assessed as reduction in cell viability after 5 days by MTT assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1443662Antiviral 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 assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1292375Cytotoxicity against human U2OS cells assessed as cell viability at 50 uM after 48 hrs relative to control2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1446811Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1657477Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity againstHIV1 infected in human MT4 cells2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.
AID508636Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID1815399Inhibition of HIV1 reverse transcriptase Y181C mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID587738Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID1267618Antiviral activity against HIV1 3B persistently infected in HUT78 cells assessed as reduction of p24 production after 43 hrs by ELISA2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID293560Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID491826Antiviral activity against HIV1 with reverse transcriptase 6005MR mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID431622Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1884225Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID298075Antiviral activity against HIV1 RT Y181C mutant in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1290399Antiviral activity against HIV1 NL4.3 infected in human TZM-bl cells incubated for 30 mins prior to infection measured after 48 hrs by luciferase assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID1275548Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1298249Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID522374Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106A mutant clone to EC50 for wild type HIV12010Antimicrobial 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.
AID1057040Antiviral activity against wild-type HIV1 3B infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID1705183Antiviral activity against HIV-1 NL4-3 infected in human MT-4 cells assessed as virus induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID318122Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID767499Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID198229Inhibition of recombinant reverse transcriptase (RT) in cell-free Quan-T-RT assay system1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID105526Inhibition of HIV-1(IIIB) variants (Ile100/Cys181) in HIV-1 MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1754646Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1761007Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 1 day by CytoTox-Glo assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1636140Binding affinity to bodipy-labeled HIV1 reverse transcriptase p66 W24C/K287C double mutant assessed as induction of p66 thumb and finger domain open conformation by measuring increase in bodipy fluorescence at 10 uM by stopped flow kinetic analysis2016Journal 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.
AID1882469Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal 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.
AID279397Antiviral activity against HIV1 isolate with RT 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID302620Antiviral activity against HIV1 3B in human MT2 cells by MTT assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
From docking false-positive to active anti-HIV agent.
AID279431Antiviral activity against HIV1 isolate with RT 103S, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1754645Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID525111Antiviral activity against HIV 1 NL4.3 assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1391080Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2018Bioorganic & 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.
AID1687682Antiviral activity against HIV-1 Y181C mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID246482Effective concentration for the inhibition of wild type human immunodeficiency virus type 1 LAI strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID508788Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID587748Ratio of EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to virus immed2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID1191971Antiviral activity against HIV1 3B infected infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity.
AID1574371Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 NL4-3 infected in human MT4 cells2019Journal 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.
AID104602Concentration which inhibited >95% spread of HIV-1 strain IIIb infection in susceptible MT-4 cell culture1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
AID1811037Anti-viral activity against HIV1 harboring RT K103N mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID557043Inhibition of HIV1 isolate R8 reverse transcriptase Y181C mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1561716Antiviral 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
AID1750725Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase Y181C mutant2021Journal 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
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1743638Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID279414Antiviral activity against HIV1 isolate with RT 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID779525Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2013Bioorganic & 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.
AID297140Antiviral activity against HIV1 with RT K103N mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID199521In vitro for inhibitory activity against HIV-1 Reverse Transcriptase1993Journal of medicinal chemistry, Mar-19, Volume: 36, Issue:6
Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and X-ray structure investigations.
AID613683Induction of apoptosis in human A375 cells seeded as low density at 20 uM after 96 hrs by DAPI staining-based FACS analysis2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID155270Ability to inhibit the replication of A17 variant (Y181C,K103N) strain of HIV-1 p24 antigen production in PBMC1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID279324Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells after dialysis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID1456310Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID440664Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID1754637Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID197788In vitro ability to inhibit wild type resistant (WT) reverse transcriptase2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID105205Potency against non nucleoside reverse transcriptor was determined in MT-4 cells2004Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
Threshold interaction energy of NRTI's (2'-deoxy 3'-substituted nucleosidic analogs of reverse transcriptase inhibitors) to undergo competitive inhibition.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1572554Solubility in water at pH 7
AID373390Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.14 uM after 24 hrs by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID1574375Antiviral 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 assay2019Journal 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.
AID232750Selectivity index is the ratio between CC50 for MT-4 cells and IC50 against HIV-1 infection2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID413564Ratio of EC50 for multidrug-resistant HIV1 with reverse transcriptase 41 L, 67N, 210W, 215Y, 184V, 103N mutation to EC50 for wild type HIV1 3B2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID82456Antiviral activity against E138K strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1316338Antiviral 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 assay2016Journal 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.
AID105349Tested for the inhibitory activity of HIV-2 infected MT-4 cells1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID1705195Inhibition 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 cou2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID298059Inhibition of HIV1 reverse transcriptase2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID305058Cytotoxicity against HEK293T cells after 48 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
4-Aminopyrimidines as novel HIV-1 inhibitors.
AID430054Inhibition of HIV1 recombinant RNA-dependent DNA polymerase activity of reverse transcriptase assessed as incorporation of radioactive dTTP into poly(rA)/oligo(dT)2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID1410482Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay2018ACS 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.
AID1773463Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA
AID522378Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone to EC50 for wild type HIV12010Antimicrobial 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.
AID734260Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 A17 double mutant infected in human TZM-bl cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1460937Antiviral activity against wild type HIV-1 NL4-3 infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID1290401Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 2 days by WST-1 assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development and in Vitro Evaluation of a Microbicide Gel Formulation for a Novel Non-Nucleoside Reverse Transcriptase Inhibitor Belonging to the N-Dihydroalkyloxybenzyloxopyrimidines (N-DABOs) Family.
AID279449Antiviral activity against HIV1 isolate with RT 98G, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID299026Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID231368Ratio of wild type IIIB to that of Y181C HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID1594862Lipophilicity, log P of the compound2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID1373154Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID527563Antiviral activity against HIV1 NL4-3 containing reverse transcriptase Y181C mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID106589Concentration required to reduce human MT-4 cell viability by 50%.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2'-5'-bis-O-(tert-butyldimethylsilyl)-beta-D-xylo- and -ribofuranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (
AID297136Toxicity against CEM cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID586901Activity at MRP12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID571983Antiviral activity against HIV-1 subtype B V022815 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID247501Inhibitory activity against HIV-1 mutant strain 181C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID265473Activity against HIV-AB1 assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID1446815Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID328843Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID556527Antiviral activity against Human immunodeficiency virus 1 clone 14682 harboring 122E, 135V, Q145V, 200A mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID482691Antiviral activity against HIV1 3B infected in human MT4 cells assessed as time-of-addition prolongation at 2 ug/ml after 31 hrs post infection by ELISA2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID1884486Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1769793Inhibition of recombinant HIV1 reverse transcriptase by colorimetric assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Design of gp120 HIV-1 entry inhibitors by scaffold hopping via isosteric replacements.
AID248881Inhibitory concentration against human immunodeficiency virus type 1 (with V106A/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID279469Antiviral activity against HIV1 isolate with RT 238N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID279465Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID82467Antiviral activity against P236L strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID525107Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID266348Inhibition of HIV1 reverse transcriptase Y188C mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID198239Inhibitory activity against HIV-1 reverse transcriptase1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
All-atom models for the non-nucleoside binding site of HIV-1 reverse transcriptase complexed with inhibitors: a 3D QSAR approach.
AID328881Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 200 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID1357784Antiviral 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 assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1248225Antiviral 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 assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID360708Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID1171581Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay2014Journal 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.
AID689697Antiviral activity against wild type HIV1 LAI infected in human CEM174 cells assessed as inhibition of viral replication preincubated for 1 hr prior to viral infection measured after 5 days2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID431621Cytotoxicity against human MT4 cells by MTT assay2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1736345Cytotoxicity against human HEK 293T cells assessed as reduction in cell viability measured after 48 hrs by Celltiter-glo assay
AID1654238Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 12-OHNVP by measuring Kcat/Km ratio in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID267649Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID304872Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells after 5 days by MTT method relative to wild type NL4-32007Journal of medicinal chemistry, Dec-27, Volume: 50, Issue:26
Dihydro-alkylthio-benzyl-oxopyrimidines as inhibitors of reverse transcriptase: synthesis and rationalization of the biological data on both wild-type enzyme and relevant clinical mutants.
AID510361Inhibition of HIV1 integrase after 1 hr2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.
AID105906Effective dose required to achieve protection of MT-4 cells from wild type IIIB HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID1244339Spermicidal activity in liquefied human semen assessed as reduction in motile spermatozoa incubated at 37 degC for 30 mins2015European journal of medicinal chemistry, Aug-28, Volume: 101N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition.
AID1691436Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID561949Antibacterial activity against Staphylococcus aureus after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID198234Inhibitory activity against HIV rRT activity in HIV-1 mutant resistant to TIBO(L100I) strain1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID1155804Antiviral activity against wild type HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1884229Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID279434Antiviral activity against HIV1 isolate with RT 101E, 181C, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1373163Inhibition of reverse transcriptase K103N/Y181C double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1763898Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID302271Resistance index, ratio of Ki for HIV1 reverse transcriptase Y188L mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1380567Antiviral activity against HIV1 virions derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed virions followed by incubation with target cel2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID1157583Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID82472Antiviral activity against V108I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID82471Antiviral activity against V106I/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1141959Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID443752Selectivity index, ratio of IC50 for African green monkey Vero cells to EC50 for HIV12010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID1888696Antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID83549Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile2004Journal 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
AID1558849Selectivity 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID318126Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis at 100 uM2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1743639Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1763899Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID606673Inhibition of HIV1 reverse transcriptase L100I mutant2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
AID279390Antiviral activity against HIV1 isolate with RT 103N, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1884222Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 to 7 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1773440Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID279416Antiviral activity against HIV1 isolate with RT 179A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1457060Ratio 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 cells2017Journal 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.
AID650687Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 1 NL4-32011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID734255Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 harboring reverse transcriptase Y181C mutation infected in human MT4 cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID279445Antiviral activity against HIV1 isolate with RT 101E, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID317733Cytotoxicity against mock-infected human MT4 cells by MTT assay2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1292009Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1157593Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID267851Inhibition of wild type HIV1 reverse transcriptase2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID1275547Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1610041Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 N119 infected in human TZM-bl cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID1654239Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 3-OHNVP formation at 5 to 400 uM in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID105341Inhibitory activity against resistant HIV-1 strain MC639r was determined.1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID373565Antiviral activity against 0.1 MOI HIV1 3B in 24 hrs pretreated human TZM-b1 cells infected 24 hrs post drug removal assessed as inhibition of viral replication at 0.04 to 0.18 uM measured 24 hrs postinfection by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID1535529Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA2019Bioorganic & 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.
AID1822283Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2022Journal 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.
AID1056581Antiviral activity against HIV-1 expressing reverse transcriptase L100I/K103N double mutant infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID198770Binding affinity against HIV reverse transcriptase (Estimated Ki)2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID508650Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID573465Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay2009Antimicrobial 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.
AID508791Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID287005Inhibition of DNA polymerase activity of reverse transcriptase pre-incubated with drug assessed as impairment of primer elongation by DNA polymerase primer-extension assay2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID622055Ratio of Ki for HIV1 RT p66/p66 homodimer Y181C mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID279474Antiviral activity against HIV1 isolate with RT 101R, 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID635345Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1654199Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as Cytochrome P450-mediated formation of 2-OHNVP at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID198067Inhibition of HIV-1 reverse transcriptase at 37 degree Centigrade2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Estimation of binding affinities for HEPT and nevirapine analogues with HIV-1 reverse transcriptase via Monte Carlo simulations.
AID298064Cytotoxicity against human MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1171594Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity2014Journal 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.
AID738334Antiviral 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 assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID198077Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
AID508781Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1736157Selectivity index, ratio of CC50 for human MT2 cells to EC50 for anti-HIV-1 activity against HTLV-3B infected in human MT2 cells2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID508763Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1323001Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
AID1320868Solubility of the compound2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1335206Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID10657950% cytotoxic concentration against mock-infected MT-4 cells using MTT method2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
AID1304409Antiviral 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 assay2016Bioorganic & 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.
AID228281Compound was evaluated for the cytotoxic activity by using Microculture Tetrazolium assay (MTA)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID1736366Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID1267628Antiviral activity against nevirapine-resistant SIV mac251 infected in human MT4 cells2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1435512Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase L100I mutant
AID267647Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID508647Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID302263Inhibition of HIV1 reverse transcriptase V179D mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID253490Dose required to inhibit HIV-1 reverse transcriptase activity (K103N mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID1141962Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID82272Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected wild type cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1773441Antiviral activity against wild type HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID240140Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID342720Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID1457053Antiviral 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 assay2017Journal 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.
AID508767Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1275539Inhibition 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 ELISA2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1418463Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay2018Bioorganic & 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.
AID232055Selectivity index (Ratio of CC50/EC50).2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID279443Antiviral activity against HIV1 isolate with RT 106A, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID199097Inhibitory activity against HIV rRT activity in HIV-21996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID1141976Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1884494Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1410481Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay2018ACS 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.
AID1877040Potency index, ratio of test compound EC50 to NBD-14189 EC50 for antiviral activity against HIV1 pseudovirus infected in human TZM-bl cells preincubated with virus for 30 mins followed by cell infection and measured after 3 days by luciferase assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
AID508753Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1155819Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID105325Inhibition of Efavirenz resistant HIV-1 (Y181C) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID197944In vitro inhibition of recombinant reverse transcriptase (WT) of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID572180Antiviral activity against HIV-1 SM002 harboring NNTRI 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1185995Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV12014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1743636Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID572187Antiviral activity against HIV-1 SM051 harboring NNTRI 100I and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1077223Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID82271Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1687685Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1736155Anti-HIV-1 activity against HTLV-3B infected in human MT2 cells assessed as reduction in syncytium formation by measuring reduction in p24 antigen production measured after 4 days by ELISA method2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID279444Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID263514Antiviral activity against HIV1 V106A mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1574376Antiviral 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 assay2019Journal 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.
AID88377Antiviral activity against V106A mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1155805Cytotoxicity against human MT4 cells assessed as induction of cell death by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID210590In vitro metabolism in human liver microsomes1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID518738Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay2010Antimicrobial 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.
AID1687684Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID635302Antiviral 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 assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID88371Antiviral activity against P236L mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID152641Cytotoxic concentration was evaluated against human peripheral blood mononuclear cells (PBMC); ND = Not determined2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
AID105858Compound was tested for potency to achieve protection of MT-4 cells from 100I strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID302248Cytotoxicity against MT4 cells after 4 days by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID572172Antiviral activity against HIV-1 subtype CRF05_DF V022823 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1173646Therapeutic index, ratio of CC50 for human CEmx174 cells expressing GFP to IC50 for HIV-1 LAI infected in human CEMx174-LTR-GFP CG8 cells2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Serendipitous discovery of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine derivatives as novel HIV-1 replication inhibitors.
AID736040Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID561946Antibacterial activity against Streptococcus pneumoniae after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID248494In vitro inhibitory concentration against HIV L100I and K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID294634Inhibition of HIV1 reverse transcriptase using Poly rA.dT template2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID1228841Selectivity index, ratio of CC50 against human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Limonoids with Anti-HIV Activity from Cipadessa cinerascens.
AID247617Inhibitory activity against HIV-1 double mutants strain 100I and 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID342719Antiviral activity against HIV1 3B in human MT4 cells assessed as virus-induced cytopathogenicity after 5 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID298089Inhibition of HIV1 RT Y181I mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID361923Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/G190A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID523477Antiviral activity against HIV1 with RT connection domain G190A/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID294629Antiviral activity against HIV1 3B in CEM cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID1231489Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID106745Cytotoxicity against MT-4 cells.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID561947Antibacterial activity against Haemophilus influenzae after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID1882471Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay2022Journal 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.
AID1157592Antiviral 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-in2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1316335Selectivity 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 cells2016Journal 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.
AID246511Compound concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C strain was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID566904Inhibition of HIV1 reverse transcriptase2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.
AID1335218Antiviral activity against wild-type HIV-1 NL4-3 harboring vesicular stomatitis virus glycoprotein infected in HEK293T cells pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene assay2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1141966Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID328844Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID366530Resistance index, ratio of ID50 for reverse transcriptase Y181I mutant to IC50 for wild-type HIV1 reverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID413267Antiviral activity against multidrug-resistant HIV1 with reverse transcriptase clone 7324-1 infected human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID1457052Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2017Journal 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.
AID1558857Antiviral 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1610043Antiviral activity against HIV1 VB51 infected in human PBMC cells incubated for 5 days by bright Glo-luciferase reporter gene assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID232053Selectivity index is the ratio of CC50 to EC501997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID1335205Ratio of IC50 for HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID389380Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID525109Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID619630Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European 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.
AID106074Inhibitory activity against LAI strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1152241Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID247504Inhibitory activity against HIV-1 mutant strain 190S2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1156485Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID1773443Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells
AID1352317Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1561719Antiviral 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
AID736442Cytotoxicity against human MT4 cells after 4 days by MTT assay2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID496621Antiviral 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 control2010Antimicrobial 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.
AID279326Decrease in reverse transcriptase activity in HIV1 infected HeLa MAGI cells assessed as decrease in number of blue foci after dialysis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID82461Antiviral activity against K103N/L100I strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1141963Antiviral activity against HIV-2 ROD infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248882Inhibitory concentration against human immunodeficiency virus type 1 (with V108I/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID767496Solubility of the compound in water by HPLC analysis2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1155808Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID104800Dose required to reduce the viability of mock-infected cells by 50%, determined by MTT method.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
AID1124991Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2014Bioorganic & 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.
AID88382Antiviral activity against Y188C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID294632Selectivity index, ratio of CC50 for CEM cells to EC50 for HIV1 infected CEM cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID371905Antiviral activity against HIV1 NL4-3 with K103N/Y181C double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID246283Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells2005Journal 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.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID88378Antiviral activity against V106A/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID558393Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 200 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID663298Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1901048Inhibition of HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in biotin-dUTP incorporation at 500 nM using poly(A)/oligo (dT)15 as template/primer by ELISA relative to control2022Bioorganic & medicinal chemistry, 02-15, Volume: 56Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs.
AID698304Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2012Journal 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.
AID1077222Antiviral 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 assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID523357Antiviral activity against HIV1 with RT connection domain G190A mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID525106Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1736151Inhibition of wild type recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodimer expressed in Escherichia coli BL21 (DE3) assessed as inhibition of dTTP incorporation on poly(rA)-oligo(dT) template primer duplex preincubated with enzyme 2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID1750716Selectivity index, ratio of CC50 for human MT-4 cells to EC50 for HIV-1 infected in MT-4 cells2021Journal 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
AID557040Antiviral 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% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID104757Compound dose required to reduce the viability of mock-infected cells by 50%1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID198915Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y181I2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID1654218Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as O-GlucNVP metabolite formation at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID1594863Inhibition of HIV1 reverse transcriptase derived from HIV patient plasma by LC/MS/MS analysis2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID247499Inhibitory activity against HIV-1 mutant strain 138K2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID573464Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay2009Antimicrobial 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.
AID1152372Antiviral 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 assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID523355Antiviral activity against HIV1 with RT connection domain Y181C/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID82473Antiviral activity against V108I/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1884542Fold 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 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID527376Toxicity in human CEM-SS cells2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID650696Ratio of ID50 for HIV 1 reverse transcriptase K103N mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1126508Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1185997Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID572188Antiviral activity against HIV-1 SM052 harboring NNTRI 101E and 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID279419Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID496619Antiviral 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 control2010Antimicrobial 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.
AID252950Selectivity index of cytotoxic activity (CC50) to inhibitory activity (IC50) relative to LAI cell line2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID666410Inhibition of HIV1 reverse transcriptase using poly(ra)/oligo(dT)15 homopolymer template as substrate after 1 hr2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID698146Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal 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.
AID1059141Selectivity index, ratio of CC50 for human MT4 cells to EC50 for drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID665547Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Bioorganic & 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.
AID571980Antiviral activity against HIV-1 subtype B V022812 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID263508Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID666971Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days2012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID198260Inhibitory concentration against mutant reverse transcriptase of P236L was determined which is in turn resistant to BHAP1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID718370Cytotoxicity against HIV1 3B infected in human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID197925Concentration required to inhibit the HIV-1 reverse transcriptase activity by 50%.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
AID1171595Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity2014Journal 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.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID1446813Cytotoxicity against human MT4 cells after 5 days by MTT assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1636138Binding affinity to bodipy-labeled HIV1 reverse transcriptase p66 W24C/K287C double mutant assessed as induction of p66 thumb and finger domain open conformation by measuring increase in bodipy fluorescence at 10 uM by fluorescence spectroscopic analysis 2016Journal 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.
AID1822332Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity at 2 uM incubated for 5 days by MTT assay2022Journal 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.
AID361927Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID363036Antiviral activity against HIV 3B in human MT4 cells assessed as inhibition of viral replication by MTT assay2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
AID279476Antiviral activity against HIV1 isolate with RT 101N, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1056574Ratio of EC50 for HIV-1 expressing reverse transcriptase K103N/G190A double mutant to EC50 for wild-type HIV-12013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID717258Cytotoxicity against human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1761009Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID648421Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1565090Antiviral 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
AID586322Inhibition of Human T-cell leukemia/lymphoma virus type 1 reverse transcriptase activity infected in human MT2 cells assessed as level of p19 antigen2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID648420Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1292367Antiviral activity against HIV1 virion infected in human TZM-bl cells after 48 hrs by firefly luciferase assay2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1888692Selectivity 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
AID1435513Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase K103N mutant
AID523353Antiviral activity against HIV1 with RT connection domain Y181C mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1763900Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID395596Cytotoxicity against HIV-infected human CEM cells2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID583848Antiviral activity against HIV1 NL4-3 infected in human SupT1 cells derived from 11 viral passages assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV1 NL4-32010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1057038Antiviral activity against HIV2 ROD infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID556524Antiviral activity against Human immunodeficiency virus 1 clone pNL4-3-Q145M harboring K102Q, Q145M, S162C, K277R, I293V mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID104804Tested for the cytotoxic concentration required to reduce the number of viable mock infected MT-4 cells1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID370729Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V179D mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID298080Antiviral activity against HIV1 RT AB1 mutant in lymphocytes assessed as reduction of p24 antigen production2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID557042Antiviral 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% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID608393Selectivity index, ratio of CC50 for MAGI-CCR5 cells to IC50 for HIV13B infected in human MAGI-CCR5 cells2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID366526Inhibition of RNA dependent DNA polymerase activity of wild-type HIV1 reverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1705194Inhibition 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 scintilla2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID242820Dose required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID1162263Selectivity index, ratio of CC50 for human MT2 cells to EC50 for X4 tropic HIV1 3B infected in human MT2 cells2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Semi-synthesis of oxygenated dolabellane diterpenes with highly in vitro anti-HIV-1 activity.
AID1485968Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID557044Inhibition of HIV1 isolate R8 reverse transcriptase K103N mutant after 90 mins by electrochemiluminescence analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1197832Antiviral 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 assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID1162262Cytotoxicity against human MT2 cells after 4 to 5 days by MTT assay2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Semi-synthesis of oxygenated dolabellane diterpenes with highly in vitro anti-HIV-1 activity.
AID630957Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 subtype C-VB592011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279391Antiviral activity against HIV1 isolate with RT 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1141968Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573478Antiviral activity of Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial 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.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269804Antiviral activity against HIV1 Y181H mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1761018Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID246301Effective concentration of the compound to inhibit HIV-1 mutant Y188L replication in HIV-infected MT-4 cells2005Journal 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.
AID391676Inhibition of RNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity at 50 ug/ml relative to control2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID88365Antiviral activity against G190A mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID523350Antiviral activity against HIV1 with RT connection domain K103N/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID248263In vitro inhibitory concentration against HIV V179E mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID360704Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID1171597Inhibition of wild type HIV1 reverse transcriptase V106A mutant assessed as reduction in enzyme activity2014Journal 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.
AID1206939Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin-labeled dUTP incorporation into DNA using polyr(A) x oligo(dT)16 template/primer hybrid2015European journal of medicinal chemistry, Jun-05, Volume: 97Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1731743Antiviral 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
AID279402Antiviral activity against HIV1 isolate with RT 103N, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1320867Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID197796Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (K103N)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
AID279415Antiviral activity against HIV1 isolate with RT 101E, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1072799Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES0562014Bioorganic & 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.
AID228280Compound dose required to reduce viability of mock infected cells using MTT method2000Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.
AID361920Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P225H mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID105535Inhibitory activity against HIV-1 Asn 103 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1705186Antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID293565Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID665273Antiviral activity against HIV2 ROD mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID302266Resistance index, ratio of Ki for HIV1 RT K103N mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1228736Antiviral activity against HIV2-ROD infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata.
AID247620Inhibitory activity against HIV-1 double mutants strain 227L and 106A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID104448Concentration required to protect the cell against HIV-1 strain IIIB viral cytopathogenicity by 50% in MT-4 cells2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID591355Antiviral activity against HIV2 isolate ROD infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days by microscopic analysis2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID1784207Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID607877Inhibition of HIV1 wild type RT using poly(rA)/oligo(dT)15 homopolymer template after 1 hrs by ELISA2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1815390Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 of Anti-HIV activity against HIV-1 IIIB infected in human MT42021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1750723Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase L100I mutant2021Journal 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
AID267855Antiviral activity against HIV1 IRLL98 in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID105155Effective concentration against HIV-1 induced cytopathogenicity in MT-4 cells1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID650691Inhibition of wild type HIV1 NL4-3 reverse transcriptase assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1435507Antiviral 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
AID232050Selectivity index expressed as the ratio of CC50/ EC501996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID368568Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA binary complex expressed in Escherichia coli BL212009Journal 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.
AID1352323Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 using poly (rA)/anoligo (dT)16 as template/primer assessed as inhibition of biotin-dUTP incorporation after 40 mins by Pico-Green staining based fluorescence assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID301928Inhibition of HIV1 reverse transcriptase by ELISA2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.
AID1072800Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2014Bioorganic & 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.
AID508779Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1249722Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID155276Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 variant (Y181C,K103N) in peripheral blood mononuclear cells (PBMC)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID1888691Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay
AID1435504Antiviral 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
AID1316345Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells2016Journal 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.
AID1322999Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1888704Resistance 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
AID46381Antiviral activity against site directed resistant isolate HIV-1 V179D in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID508649Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID391687Inhibition of RNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID1155813Inhibition of wild type HIV-1 recombinant reverse transcriptase assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID240924Inhibitory concentration against HIV-Reverse transcriptase2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Human immunodeficiency virus-reverse transcriptase inhibition and hepatitis C virus RNA-dependent RNA polymerase inhibition activities of fullerene derivatives.
AID198068Inhibition of reverse transcriptase activity of HIV-1 in the presence of [alpha35 S] TTP as cosubstrate1993Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
AID557048Antiviral activity against HIV1 clade F1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID717261Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID508640Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID1191974Selectivity index, ratio of CC50 for mock-infected human HeLa cells to EC50 for HIV2 ROD infected in human MT4 cells2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity.
AID247498Inhibitory activity against HIV-1 mutant strain 106A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID391690Inhibition of DNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant expressed in Escherichia coli BL212008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID1888694Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID106949Anti-HIV-1 activity against WTIIIB HIV-1 strain in MT-4 cells2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1446819Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID698301Antiviral activity against HIV1 containing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal 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.
AID1446817Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1446826Inhibition 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 ELISA2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID299025Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV12007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID619629Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2011European 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.
AID1249720Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1483273Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal 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.
AID1731749Inhibition 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
AID508641Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID253492Dose required to inhibit HIV-1 reverse transcriptase activity (V179D mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID1418467Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells2018Bioorganic & 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.
AID1822274Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2022Journal 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.
AID1485966Inhibition of recombinant wild-type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by Pi2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID246351Effective concentration against human immunodeficiency virus type 1 mutated at 188L2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1056579Antiviral activity against HIV-1 expressing reverse transcriptase K103N/G190A double mutant infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1877036Inhibition of recombinant HIV-1 reverse transcriptase incubated for 2 hrs by colorimetric assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
AID1731744Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1654236Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 12-OHNVP at 1 to 400 uM in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID635301Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID518740Antiviral 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 assay2010Antimicrobial 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.
AID523354Antiviral activity against HIV1 with RT connection domain Y181C/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID265474Selectivity index, TC50 for human lymphocytes/EC50 for HIV1 3B2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID1316805Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity.
AID673926Antiviral activity against Human immunodeficiency virus 1 infected in human 293T cells assessed as inhibition of viral replication after 48 hrs by luminescence analysis2012ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6
Novel Cyclopropyl-Indole Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
AID1572527Antiviral 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
AID253495Dose required to inhibit HIV-1 reverse transcriptase activity ( L100I mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID1561717Antiviral 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
AID523358Antiviral activity against HIV1 with RT connection domain G190A/N348Ib mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID105522Concentration which reduced the cytopathic effect of HIV-1 in MT-4 infected cells1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID198259Inhibitory concentration against mutant reverse transcriptase of L100I was determined which is in turn resistant TIBO1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID1565091Antiviral 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
AID1457058Antiviral 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 assay2017Journal 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.
AID282740Inhibition of HIV1 RT Y188L mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID342718Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT)2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
AID1298243Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016Bioorganic & 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.
AID46204Tested for the inhibitory activity of virus induced giant cell formation in HIV-1 infected CEM cells1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID1072798Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD2014Bioorganic & 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.
AID1155806Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1435509Antiviral 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
AID1185998Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1784213Antiviral 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 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID299029Antiviral activity against HIV1 with reverse transcriptase E138K mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID508774Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1565088Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template incubated for 1 hr by ELISA
AID287001Cytotoxicity against Jurkat cells by XTT assay2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1731751Inhibition 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
AID586908Induction of MRP1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID665553Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B2012Bioorganic & 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.
AID248259In vitro inhibitory concentration against HIV K101E mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID276232Cytotoxicity against MT2 cells2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1244338Inhibition of HIV1 reverse transcriptase at 100 ug/ml incubated for 1 hr by ELISA method2015European journal of medicinal chemistry, Aug-28, Volume: 101N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition.
AID279392Antiviral activity against HIV1 isolate with RT 100I, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1357795Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1565096Antiviral 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
AID473117Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID1152245Antiviral activity against X4 tropic Human immunodeficiency virus 1 UG070 subtype D infected in human TZM-bl cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by luminescence assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID449489Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus induced cytotoxicity after 5 days by MTT assay2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID621978Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1636149Ratio 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 cells2016Journal 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.
AID557036Antiviral 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 serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269803Antiviral activity against HIV1 V179E mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1191404Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometry2015Bioorganic & 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.
AID104802In vitro cytotoxicity against mock infected MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID256329Percentage inhibition of proliferation against alive human A-375 cells treated with DMSO (control) at a concentration of 350 uM2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
6-[1-(2,6-difluorophenyl)ethyl]pyrimidinones antagonize cell proliferation and induce cell differentiation by inhibiting (a nontelomeric) endogenous reverse transcriptase.
AID361909Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID443759Antiviral activity against HIV1 with reverse transcriptase G139I mutation2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID106956Compound dose required to achieve protection of MT-4 cells from HIV-1 induced cytopathicity using MTT method2000Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.
AID1572528Antiviral 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
AID663307Inhibition of HIV1 recombinant reverse transcriptase L100I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID572185Antiviral activity against HIV-1 SM030 harboring NNTRI 100I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID293557Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 LAI2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID1822275Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells2022Journal 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.
AID222294Effect of human plasma protein binding on antiviral efficacy.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1815387Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID297135Antiviral activity against HIV1 infected CEM cells2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID105700Anti-HIV-1 activity against K103N+Y181C strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1446816Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID391683Antiviral activity against HIV1 infected in 8186 T cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID1761017Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1141972Ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1443670Antiviral 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 assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID693584Antiviral 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 assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID279433Antiviral activity against HIV1 isolate with RT 179T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID449492Selective index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID198909In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y188L1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID1155817Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1591873Antiviral activity against wild-type HIV1 NL4-3 infected in human MT2 cells measured 48 hrs post-infection by MTT assay2019Bioorganic & 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.
AID299030Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1815400Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1173644Antiviral activity against HIV-1 LAI infected in human CEMx174-LTR-GFP CG8 cells assessed as inhibition of viral replication after 5 days2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Serendipitous discovery of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine derivatives as novel HIV-1 replication inhibitors.
AID557035Antiviral 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 serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID757623Cytotoxicity against human MT4 cells after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1171582Antiviral activity against HIV2 ROD infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay2014Journal 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.
AID460296Inhibition of HIV1 reverse transcriptase by EIA2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1275552Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1637398Antiviral 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 assay2016Bioorganic & 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.
AID621980Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1750717Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal 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
AID361914Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190E mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1654201Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as Cytochrome P450-mediated formation of 12-OHNVP at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID82276Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C+K103N strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID492286Antiviral activity against HIV1 with reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID767501Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1379964Inhibition 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 spectrofluorometry2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID655387Cytotoxicity against human CEmx174 cells2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability.
AID197780Compound was evaluated for its inhibitory activity against recombinant HIV-1 Reverse transcriptase using cell free RT inhibition assay2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1784214Antiviral 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 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1267625Antiviral activity against NRTI/NNRTI-resistant HIV1 L6 harboring reverse transcriptase V75I/F77L/K103N/F116Y/Q151M/M184V mutant infected in human MT4 cells2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1152246Antiviral activity against R5 tropic Human immunodeficiency virus 1 VB59 subtype C infected in human TZM-bl cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by luminescence assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1357798Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID279323Inhibition of reverse transcriptase RTY18C mutant in HIV1 Z6gpt assessed as inhibition of ssDNA synthesis2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID267856Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID571968Antiviral activity against HIV-1 subtype CRF02_AG V022825 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1352319Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID82606The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of acid glycoprotein in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID105859Compound was tested for potency to achieve protection of MT-4 cells from 101E strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID1773457Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1884491Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID572169Antiviral activity against HIV-1 subtype D V022832 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID557052Antiviral activity against NRTI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID82476Antiviral activity against wild-type HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1157595Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1483272Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal 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.
AID779529Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & 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.
AID1141977Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1390711Antiviral 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 assay2018Bioorganic & 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.
AID561944Antibacterial activity against Shigella sonnei ATCC 111060 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID1565092Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
AID1685255Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID1705193Resistance 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 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID395595Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days2009European journal of medicinal chemistry, Jan, Volume: 44, Issue:1
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
AID1157581Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID571986Antiviral activity against HIV-1 subtype C V022829 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID735081Antiviral activity against HIV harboring reverse transcriptase Y181C mutant by cell based assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID1316337Antiviral 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 assay2016Journal 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.
AID508752Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID619643Ratio 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 cells2011European 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.
AID1729160Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID317734Inhibition of tubulin polymerization after 20 mins2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID346970Antiviral activity against HIV 3B in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Studies on anti-HIV quinolones: new insights on the C-6 position.
AID368558Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID198913Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID1636932Aqueous solubility of compound in water at pH 7 by HPLC analysis2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID416759Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID391996Antiviral activity against HIV2 ROD replication in human MT4 cells assessed as inhibition of virus-induced cytopathic effect at subtoxic concentration after 5 days by tetrazolium-based colorimetric assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID105546Inhibition of mutant type (Ile100) HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1888703Resistance 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
AID1862268Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.
AID1186005Antiviral activity against HIV1 harboring reverse transcriptase K103N/V108I double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID226237Fold resistance (L100I/ WT) (as per ref 12 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID689698Cytotoxicity against human CEM174 cells assessed as cell viability2012ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
AID391677Inhibition of DNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity at 50 ug/ml relative to control2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID360707Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID83554Potency evaluated against wild type HIV-1 strain IIIB2004Journal 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
AID571985Antiviral activity against HIV-1 subtype C V022817 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID348906Antiviral activity against drug-resistant HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID1763901Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID572179Antiviral activity against HIV-1 subtype O V029524 harboring NNRTI A98G, V179E and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID666412Cytotoxicity against human MT4 cells after 3 days by XTT assay2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID1729159Antiviral activity against HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID572177Antiviral activity against HIV-1 subtype H V022828 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID104980Dose required to achieve 50% protection of MT-4 cells from HIV-1 induced cytopathogenicity1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.
AID586320Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of gag gene expression after 5 days post infection by quantitative real time RT-PCR2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID260237Antiviral activity against HIV1 3B in MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1609109Antiviral 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID198906In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution L100I1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID266346Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID368561Antiviral activity against HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID1292363Antiviral activity against HIV1 virus-like particles harboring wild type reverse transcriptase infected in human U2OS cells assessed as remaining viral activity at 5 uM after 24 hrs by Renilla luciferase assay relative to control2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID391692Inhibition of DNA dependent DNA polymerase activity of HIV2 recombinant reverse transcriptase at 140 uM2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID586902Activity at MRP22011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1773442Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
AID557038Antiviral 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 serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1591875Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay2019Bioorganic & 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.
AID197932HIV-1 reverse transcriptase inhibitory activity against Cys181 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID198409Tested for the inhibition of mutant type (Cys181) HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1380573Antiviral activity against HIV1 virions containing reverse transcriptase E138K/M184V mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID1059142Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1877039Potency index, ratio of test compound IC50 to NBD-14189 IC50 for inhibition of recombinant HIV-1 reverse transcriptase incubated for 2 hrs by colorimetric assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
AID1884227Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID556525Antiviral activity against Human immunodeficiency virus 1 clone 38086 harboring K49R, V60I, I135V, Q145M, Q174H, G196E, Q207E, R211K, V245K mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID279477Antiviral activity against HIV1 isolate with RT 181V mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID460295Inhibition of HIV1 reverse transcriptase at 20 ug/mL by EIA2010Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols.
AID279319Inhibition of reverse transcriptase assessed as decrease in ssDNA level in cell free virion HIV1 by NERT-based real-time PCR at 10 uM2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID83552Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu2004Journal 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
AID1231487Inhibition of wild-type HIV1 Reverse transcriptase p66/p51 assessed as relative fluorescence signal after 40 mins2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID287004Inhibition of drug-resistant reverse transcriptase L100I-K103 mutant2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1736363Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y181C mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID317729Antiviral activity against HIV1RF infected in human CEM-SS cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1316333Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2016Journal 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.
AID81255Concentration required to inhibit HIV-1 induced cytopathicity in human MT-4 lymphocyte cells.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2'-5'-bis-O-(tert-butyldimethylsilyl)-beta-D-xylo- and -ribofuranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (
AID263507Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID665272Antiviral 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 assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1609103Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID244306Fold increase in inhibitory concentration against HIV 1 reverse transcriptase mutant type Cys181 over wild type HIV 1 reverse transcriptase2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID586900Activity at ABCB12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID263521Antiviral activity against HIV1 F227C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID482696Antiviral activity against AZT-resistant HIV infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID294630Antiviral activity against HIV2 ROD in CEM cells2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID265471Activity against HIV1 3B assessed by inhibition of p24 production in human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID281485Antiviral activity against wild type HIV1 3B in MT4 cells after 4 days by MTT method2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1298253Inhibition of HIV1 3B reverse transcriptase p66/p51 K103N/Y181C mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID648422Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1373158Inhibition of reverse transcriptase L100I mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1379963Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1292376Cytotoxicity against human U2OS cells assessed as cell viability at 5 uM after 48 hrs relative to control2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1657476Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.
AID1199054Antiviral activity against Human immunodeficiency virus type 2 ROD infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead.
AID318121Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID366532Resistance index, ratio of ID50 for reverse transcriptase L100I mutant to IC50 for wild-type HIV1 reverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID282735Inhibition of HIV1 RT2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID608389Inhibition of HIV1 reverse transcriptase assessed as residual enzyme activity at 50 uM after 1 hr by ELISA relative to control2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID299028Antiviral activity against HIV1 with reverse transcriptase K103N mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID557022Antiviral activity against HIV1 CRF01_AE harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID263152Antiviral activity against HIV1 in HEK293T cells2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1335207Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID614142Antiviral 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 assay2011Bioorganic & 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.
AID1596756Inhibition of recombinant wild-type HIV1 3B reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template primer incubated for 1 hr followed by the addition of (DIG)-dUTP and biotin-labeled dNTPs by ELISA2019European journal of medicinal chemistry, Aug-15, Volume: 176Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains.
AID366517Antiviral activity against HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID413265Antiviral activity against multidrug-resistant HIV1 with reverse transcriptase 41L, 67N, 210W, 215Y, 184V, 103N mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID1077218Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID391691Inhibition of DNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I/K103N mutant expressed in Escherichia coli DH5alpha2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID328845Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID263515Antiviral activity against HIV1 I135T mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1152247Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 UG070 subtype D2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246275Effective concentration against rhuman immunodeficiency virus type 1 Y181C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1761015Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1357797Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID573481Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8117 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial 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.
AID1197833Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID1574386Inhibition 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 analysi2019Journal 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.
AID1316341Antiviral 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 assay2016Journal 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.
AID302252Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT IRLL98 mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID650540Antiviral 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 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID586326Cytotoxicity against PHA-stimutated human PBMC after 24 hrs by MTS assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID105539Inhibitory activity against HIV-1 Ile 100 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID523349Antiviral activity against HIV1 with RT connection domain K103N mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID508643Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID197795Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID1161104Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1736152Selectivity for inhibition of wild type recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodimer expressed in Escherichia coli BL21 (DE3) at 50 uM over inhibition of recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodi2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID246799Compound concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR carrying mutations K103R, V179D, and P225H2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID522371Antiviral 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 microscopy2010Antimicrobial 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.
AID82275Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1175438Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild-type HIV-1 SF332015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.
AID299027Antiviral activity against HIV1 with reverse transcriptase L100I mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID152657Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17 variant.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID391689Inhibition of HIV1 BH10 recombinant reverse transcriptase p66/p51 RNase H activity assessed as residual enzyme activity2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID1884221Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1460940Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in MAGI-CCR5 cells2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID361910Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188L mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID586905Inhibition of ABCB1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID650543Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID557051Antiviral activity against PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1191973Cytotoxicity against mock-infected human HeLa cells by MTT assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity.
AID302251Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID366518Cytotoxicity against human MT4 cells by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1323000Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
AID328885Toxicity in human HeLa cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID1126507Antiviral 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 assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID685333Cytotoxicity against mock-infected human MT4 cells by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1736359Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase Y188L mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID1773451Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells
AID46375Antiviral activity against site directed 4X AZT resistant isolate HIV-1 in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID106600Cytotoxic concentration required to reduce MT-4 cell viability by 50%1992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro -5''- (4''-amino-1'',2''-oxathiole 2'',2''-dioxide) pyrimidine and pyrimidine-modified nucleosides.
AID718372Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID105905Effective dose required to achieve protection of MT-4 cells from Y181C HIV-1 induced cytopathogenicity2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Computer-aided design, synthesis, and anti-HIV-1 activity in vitro of 2-alkylamino-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as novel potent non-nucleoside reverse transcriptase inhibitors, also active against the Y181C varia
AID1352322Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID318120Inhibition of HIV1 reverse transcriptase2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID523478Antiviral activity against HIV1 with RT connection domain G190A/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID665551Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Bioorganic & 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.
AID571967Antiviral activity against HIV-1 subtype CRF02_AG V022808 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID391994Selectivity index, ratio of CC50 for human CEM cells to EC50 for HIV1 3B2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID571976Antiviral activity against HIV-1 subtype B V022807 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID197776Compound was evaluated for inhibition of Y181C HIV type I reverse transcriptase.1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.
AID370726Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1352312Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID622058Ratio of Ki for HIV1 RT p66/p66 homodimer K103N/Y181C double mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID738331Cytotoxicity against mock-infected human MT4 cells assessed as cell viability after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID105537Inhibitory activity against HIV-1 Cys 181 mutant in MT-4 cells.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1729158Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID1457055Antiviral 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 assay2017Journal 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.
AID1357786Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID496633Antiviral 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 control2010Antimicrobial 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.
AID558372Drug level in HIV-infected pregnant woman maternal blood plasma at 200 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID1743626Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID1185996Antiviral activity against HIV1 harboring reverse transcriptase L1001/K103N double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1761011Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID522368Antiviral activity against wild type HIV1 infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy2010Antimicrobial 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.
AID46380Antiviral activity against site directed resistant isolate HIV-1 V106A in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1888705Resistance 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
AID734259Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 A17 double mutant infected in human MT4 cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1357796Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID508652Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1729157Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID105891Cytotoxicity against uninfected MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID153130Effective dose for inhibition of viral replication in cell culture of 0.1 uM2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID1460930Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 Bal infected in MAGI-CCR5 cells2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID318123Antiviral activity against HIV2 ROD in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1391087Antiviral 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 assay2018Bioorganic & 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.
AID1520058Antiviral 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 assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1057039Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID263512Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID619635Antiviral 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 assay2011European 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.
AID665271Antiviral 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 assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID508797Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay2010Antimicrobial 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.
AID698144Inhibition of HIV1 reverse transcriptase L100I mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate2012Journal 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.
AID155273Ability to inhibit the replication of RT-MDR (V106A) strain of HIV-1 p24 antigen production in PBMC1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID279464Antiviral activity against HIV1 isolate with RT 101Q, 103N, 225H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID366528Resistance index, ratio of ID50 for reverse transcriptase K103N mutant to IC50 for wild-type HIV1 sreverse transcriptase2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1520057Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID508634Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID287000Inhibition of RNase H activity of HIV1 reverse transcriptase2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID198080Inhibitory activity against HIV-1 Mutant Reverse transcriptase V106A1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID266345Inhibition of wild type HIV1 reverse transcriptase in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID197934HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID302268Resistance index, ratio of Ki for HIV1 reverse transcriptase V106A mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1731748Inhibition 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
AID1171578Cytotoxic activity against human MT4 cells by MTT assay2014Journal 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.
AID1483275Inhibition 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 assay2017Journal 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.
AID735080Ratio of EC50 for HIV harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID573468Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay2009Antimicrobial 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.
AID1572526Antiviral 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
AID457959Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1072797Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA2014Bioorganic & 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.
AID1775803Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template2021Journal 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.
AID1335212Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1610039Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 92/BR/018 infected in human TZM-bl cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID1763903Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID405412Antiviral activity against PERV infected in human 293T cells assessed as inhibition of proximal DNA synthesis after 24 hrs by RT-PCR2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
AID586906Inhibition of BCRP activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1822276Antiviral 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 assay2022Journal 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.
AID1460941Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase K103N mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID197807In vitro inhibition of HIV-1 reverse transcriptase1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID508782Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1390715Resistance 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 cells2018Bioorganic & 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.
AID1761019Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID247495Inhibitory activity against HIV-1 mutant strain 100I2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID298061Antiviral activity against HIV1 3B in human MT4 cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID632799Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection2011Journal 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.
AID1743618Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID105523Inhibition of HIV-1(IIIB) variants (Ile100/Asn103) in HIV-1 MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1191668Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID482700Cytotoxicity against human Jurkat A72 cells by MTT assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID247505Inhibitory activity against HIV-1 mutant strain 227C2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID622049Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1811036Anti-viral activity against HIV1 harboring RT Y181C mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID281486Cytotoxicity against MT4 cells after 4 days by MTT method2007Journal of medicinal chemistry, Apr-19, Volume: 50, Issue:8
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID492278Antiviral activity against HIV1 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID1435514Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y181C mutant
AID1141975Inhibition of HIV1 wild-type reverse transcriptase using [3H]dTTP by scintillation counting2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1163253Trypanocidal 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 assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID105866Compound was tested for potency to achieve protection of MT-4 cells from LAI strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID1636147Antiviral 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 assay2016Journal 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.
AID366531Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1335217Inhibition of wild-type HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in digoxigenin-11-dUTP incorporation using poly(rA)/oligo(dT) as template/primer incubated for 1 hr2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID556526Antiviral activity against Human immunodeficiency virus 1 clone Q9016 harboring K122E, Q145M, I202V, F214L mutation in reverse transcriptase by phenosense assay relative to wild type2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Human immunodeficiency virus type 1 isolates with the reverse transcriptase (RT) mutation Q145M retain nucleoside and nonnucleoside RT inhibitor susceptibility.
AID523480Antiviral activity against HIV1 with RT connection domain G190S/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1763906Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269688Antiviral activity against HIV1 NNTRI resistant K103N mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1784209Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1249716Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID199993Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 6 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID1316340Antiviral 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 assay2016Journal 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.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID622053Ratio of Ki for HIV1 RT p66/p66 homodimer L100I mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID198910In vitro inhibitory activity against HIV-1 wild type reverse transcriptase (RT)1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID586911Induction of SLCO1B1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID105326Inhibition of HIV-1 (IIIB) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID105862Compound was tested for potency to achieve protection of MT-4 cells from 181C strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID298090Inhibition of HIV1 RT L100I mutant2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID440083Antiviral activity against HIV1 HXB2 harboring 227C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID508637Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID96296Compound was evaluated for antiviral activity against L100I mutant virus; ND is Not Determined.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1316803Antiviral activity against HIV-1 3B infected in human MT-4 cells assessed as protection against virus induced cytopathic effect after 5 days by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity.
AID726439Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method2013Bioorganic & 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.
AID482694Antiviral activity against HIV2 ROD infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID235264Selectivity index is ratio of CC50 to that of EC502000Bioorganic & medicinal chemistry letters, Feb-07, Volume: 10, Issue:3
1-[2-(Diphenylmethoxy)ethyl]-2-methyl-5-nitroimidazole: a potent lead for the design of novel NNRTIs.
AID1773454Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells
AID253494Dose required to inhibit HIV-1 reverse transcriptase activity (Y188L mutant) by 50%2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
AID508789Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1687686Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1157586Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID583847Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K mutant infected in human SupT1 cells derived from 9 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sensitive HIV2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID371903Antiviral activity against HIV1 NL4-3 with L100I/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1594864Oral bioavailability in human2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID302250Selectivity index, ratio of CC50 for MT4 cells to EC50 for HIV1 NL43 infected MT4 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID508798Ratio of EC50 for HIV1 in presence of 50% human serum to EC50 for HIV1 in absence of serum proteins by GFP assay2010Antimicrobial 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.
AID1157584Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID252955Ratio of CC50 and EC50 against wild type human immunodeficiency virus type 1 LAI strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID717260Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID1880379Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y188L mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1228735Antiviral activity against HIV1-3B infected in human MT4 cells assessed as inhibition of virus induced cell death measured after 5 days of infection by MTT assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata.
AID525108Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1141965Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1537495Cytotoxicity against HEK293T cells assessed as reduction in cell viability after 48 hrs by CellTiter 96 aqueous one solution assay2019ACS medicinal chemistry letters, Feb-14, Volume: 10, Issue:2
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
AID1731750Inhibition 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
AID198410Tested for the inhibition of mutant type (Ile100) HIV-1 (IIIB) RT1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID279468Antiviral activity against HIV1 isolate with RT 98G, 108I, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID246393Effective concentration against human immunodeficiency virus type 1 mutated at 103N+181C2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID557023Antiviral activity against HIV1 clade A harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID198396Inhibitory activity against HIV-1 reverse transcriptase (HIV-RT)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID1456306Inhibition 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 assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID508776Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID518739Selectivity 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 transcriptase2010Antimicrobial 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.
AID293555Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID586324Inhibition of HIV1 3B reverse transcriptase activity2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID1141973Ratio of EC50 for HIV1 harboring reverse transcriptase L1001 mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID82604The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1357805Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1446812Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID1636930Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID1736362Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cells
AID1228737Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1-3B2015Journal of natural products, May-22, Volume: 78, Issue:5
Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID82469Antiviral activity against V106A/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID279479Antiviral activity against HIV1 isolate with RT 179D, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1784212Antiviral 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 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1171593Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity2014Journal 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.
AID389379Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435525Inhibition 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
AID44798In vitro concentration required to reduce the amount of p24 by 90% in WTIIIB infected C8166 cells2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269687Antiviral activity against HIV1 NNTRI resistant Y181C mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID257167Antiviral activity against HIV1 IRLL98 mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID235708Selectivity index measured as the ratio of CC50 / EC50.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
AID82464Antiviral activity against K103N/Y181C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID757622Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1485965Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID83551Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys2004Journal 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
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1391082Antiviral 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 assay2018Bioorganic & 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.
AID1705187Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1741396Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID242545Fold increase in inhibitory concentration against HIV 1 reverse transcriptase mutant type Ile100 over wild type HIV 1 reverse transcriptase2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID482701Selectivity index, ratio of CC50 for human Jurkat A72 cells to EC50 for HIV1 3B2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID767497Cytotoxicity against human MT2 cells assessed as growth inhibition2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1186689Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV-1 RES056 harboring RT K103N/Y181C double mutant infected in human MT4 cells2014European journal of medicinal chemistry, Oct-06, Volume: 85Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
AID496627Antiviral 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 control2010Antimicrobial 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.
AID522577Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I mutant clone to EC50 for wild type HIV12010Antimicrobial 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.
AID482697Antiviral activity against HIV S056 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID199994Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 7 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1267609Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID79121Inhibitory activity against multidrug resistant HIV-1 strain RT-MDR2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID105715Antiviral activity against HIV-1 resistant to 2-(2-Benzoyl-4-chloro-phenyl)-N-[4-(3-dimethylamino-propoxy)-2-methyl-phenyl]-acetamide in MT-4 cells1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Benzophenone derivatives: a novel series of potent and selective inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
AID105704Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID297139Antiviral activity against HIV1 with RT K101E mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID360710Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID373387Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.18 uM after 24 hrs by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID522376Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V179D mutant clone to EC50 for wild type HIV12010Antimicrobial 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.
AID1685254Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID1171592Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant to EC50 for wild type HIV1 NL4-32014Journal 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.
AID1574389Resistance index, ratio of ID50 for recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant to ID50 for recombinant wild type HIV-1 reverse transcriptase His-tagged p66/p512019Journal 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.
AID246203Concentration required to achieve 50% protection of infected MT-4 cells from Y181C-HIV-1 strain2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID1741393Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID1141967Antiviral activity against HIV1 harboring reverse transcriptase L1001 mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279481Antiviral activity against HIV1 isolate with RT 101E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1741399Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID650695Ratio of ID50 for HIV 1 reverse transcriptase L100I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID1244340Anti-trichomonas activity against MTZ-susceptible Trichomonas vaginalis incubated for 3 to 48 hrs by trypan blue exclusion assay2015European journal of medicinal chemistry, Aug-28, Volume: 101N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition.
AID557021Antiviral activity against HIV1 CRF02_AG harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID573482Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type2009Antimicrobial 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.
AID366529Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181I mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1275543Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID235859CC50/EC50 ratio of the compound2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID391686Antiviral activity against HIV1 infected in human 293T cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID678721Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1231485Antiviral 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 assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID360709Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID557050Antiviral activity against HIV1 clade H harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID663308Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID630787Antiviral activity against X4 tropic Human immunodeficiency virus 1 subtype B-3B infected in human TZM-bl cells assessed as inhibition of virus-induced cytopathic effect after 2 days by luciferase assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID297143Antiviral activity against HIV1 with RT Y188C mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID522370Antiviral 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 microscopy2010Antimicrobial 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.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1316804Antiviral activity against HIV-2 ROD infected in human MT-4 cells assessed as protection against virus induced cytopathic effect after 5 days by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity.
AID619637Antiviral 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 assay2011European 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.
AID366522Antiviral activity against HIV1 isolates with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1141960Antiviral activity against HIV1 NL4.3 infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID246519Effective concentration against human immunodeficiency virus type 1 mutated at 227L+106A; ND:Not determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1815382Antiviral 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 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID298081Selectivity index, ratio of TC50 for lymphocytes to ED50 for HIV1 3B2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1731753Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into wild type RT measured after 1 hr by ELISA
AID235503Selectivity index calculated as the ratio between CC50 and EC501995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines.
AID1249707Antiviral activity against wild-type HIV-1 infected in human MT4 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors from arylthioacetanilide structural motif.
AID1435508Antiviral 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
AID1520061Selectivity 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 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID82468Antiviral activity against V106A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1200844Antiviral 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 assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID279461Antiviral activity against HIV1 isolate with RT 179D, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID635346Cytotoxicity against human MT4 cells measured by MTT assay2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1228840Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 3 to 4 days by MTT assay2015Journal of natural products, Jun-26, Volume: 78, Issue:6
Limonoids with Anti-HIV Activity from Cipadessa cinerascens.
AID1743621Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID499279Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV2 ROD2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID499275Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
AID1157594Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID698298Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32012Journal 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.
AID1435506Antiviral 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
AID368569Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA-dNTP ternary complex expressed in Escherichia coli BL212009Journal 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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1320866Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1171579Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay2014Journal 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.
AID1485971Inhibition of HIV-1 reverse transcriptase V106A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1152248Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 VB59 subtype C2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID736443Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID649827Cytotoxicity against human CEMx174 cells2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID279460Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID348905Antiviral activity against drug-resistant HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID152788Tested for the ability to inhibit the replication of HIV-1 strain HTLV IIIB in human peripheral blood mononuclear cells (PBMC)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
AID1322998Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
AID1377175Antiviral activity against NNRTI-resistant HIV1 isolate N119 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA2017Journal of natural products, 06-23, Volume: 80, Issue:6
Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa.
AID370727Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269802Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID630955Antiviral activity against R5 tropic Human immunodeficiency virus 1 subtype C-VB59 infected in human TZM-bl cells assessed as inhibition of virus-induced cytopathic effect after 2 days by luciferase assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID248492In vitro inhibitory concentration against HIV K101E and K103N mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1572521Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells
AID608390Inhibition of HIV1 reverse transcriptase assessed as residual enzyme activity at 50 uM after 1 hr by ELISA2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508751Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1884489Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID197792Compound was tested for Inhibition of HIV-1 RT activity.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Pyrrolobenzothiazepinones and pyrrolobenzoxazepinones: novel and specific non-nucleoside HIV-1 reverse transcriptase inhibitors with antiviral activity.
AID430056Cytotoxicity against human MT4 cells after 5 days2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID199999Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 7 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID106777Compound was evaluated for antiviral activity in MT-4 cells. Cell culture inhibitor concentration (CIC95) is defined as concentration which inhibited >95% the spread of HIV-1 IIIb infection in susceptible cell culture1992Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21
Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 2. Analogues of 3-aminopyridin-2(1H)-one.
AID198400Tested for inhibitory concentration on HIV-1 Reverse transcriptase in the presence of poly(c)-oligo-(dG)2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
AID1460944Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 harboring reverse transcriptase K103N mutant infected in MAGI-CCR5 cells2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID299024Cytotoxicity against MT4 cells assessed as reduction of cell viability2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1705188Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID619632Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells2011European 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.
AID496615Antiviral 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 control2010Antimicrobial 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.
AID279410Antiviral activity against HIV1 isolate with RT 179E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID104785Cytotoxic concentration based on the reduction of viability of mock-infected cells1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
AID248256In vitro inhibitory concentration against HIV F227C mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID561941Antibacterial activity against Haemophilus influenzae ATCC 4927 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID1687681Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1460938Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 infected in MAGI-CCR5 cells2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID523483Antiviral activity against HIV1 with RT connection domain L100I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1811046Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells2021Journal 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.
AID496617Antiviral 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 control2010Antimicrobial 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.
AID1572522Selectivity 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
AID246517Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N; ND:Not determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID279321Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Development of a new methodology for screening of human immunodeficiency virus type 1 microbicides based on real-time PCR quantification.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1357790Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1156487Cytotoxicity against human MT4 cells after 5 days by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID1609110Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1815381Antiviral 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 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1186684Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection from viral cytopathicity after 5 days by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
AID267645Antiviral activity against wild type HIV1 virus2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID698302Antiviral activity against HIV1 containing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal 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.
AID1357799Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1304400Antiviral activity against HIV-1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2016Bioorganic & 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.
AID476468Cytotoxicity against human MT2 cells by MTT assay2010Bioorganic & 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.
AID105571Antiviral activity was determined against wild type HIV-1 in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1572525Antiviral 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
AID1171580Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells2014Journal 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.
AID1435505Antiviral 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
AID1736150Inhibition of recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodimer K103N mutant assessed as inhibition of dTTP incorporation on poly(rA)-oligo(dT) template primer duplex at 50 uM preincubated with enzyme for 2 mins followed by incuba2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID1292365Inhibition of recombinant HIV1 reverse transcriptase using 234-nt long RNA/18-mer DNA oligonucleotide as template/primer assessed as remaining activity at 50 uM preincubated for 15 mins followed by incubation with template/primer for 40 mins by liquid sci2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1141970Ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1152371Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1156484Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID1249717Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID287006Inhibition of reverse transcriptase binding to DNA assessed as formation of RT-DNA complex by gel mobility shift assay2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1460933Therapeutic index, ratio of TC50 for human PBMC to IC50 for HIV-1 Bal infected in human PBMC2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID391685Antiviral activity against HIV1 infected in human CEM cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID557037Antiviral 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 serum2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID242248Concentration required for 50% inhibition of human immunodeficiency virus type 1 reverse transcriptase mutant type Cys1812004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID666416Selectivity index, ratio of CC50 for human MT4 cells to EC50 for NNRTI-resistant HIV1 A17 expressing reverse transcriptase K103N and Y181C mutant2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID632795Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection2011Journal 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.
AID586907Induction of ABCB1 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID297138Antiviral activity against HIV1 with RT L100I mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID508653Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID246300Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells2005Journal 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.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID105863Compound was tested for potency to achieve protection of MT-4 cells from 188L strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID1175435Inhibition of HIV-1 recombinant reverse transcriptase after 1 hr by streptavidinalkaline phosphatase reporter system2015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.
AID282736Inhibition of HIV1 RT L100I mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1152243Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 ADA5 subtype B2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1705191Resistance 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 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID665275Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID518734Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay2010Antimicrobial 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.
AID105543Inhibition of wild type HIV-1 in MT-4 cell culture (human T cell line)1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID586903Activity at MRP32011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID1069710Inhibition of GST-tagged recombinant wild type HIV-1 reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 using dTTP as substrate after 40 mins by spectrofluorometric analysis2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID457956Antiviral activity against HIV1 3B infected in human MT4 cells assessed inhibition of viral-induced cytopathic effect after 5 days2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1231488Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID440081Antiviral activity against HIV1 HXB2 harboring 190A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID717256Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID155290Inhibit the replication of the HIV-1 strain HTLV111B in human peripheral blood mononuclear cell2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID235701Selectivity index is the ratio of CC50 and EC50 in MT-4 cells.1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
AID440082Antiviral activity against HIV1 HXB2 harboring 190S mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID572181Antiviral activity against HIV-1 SM007 harboring NNTRI 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID591001Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Asymmetric total synthesis of (+)- and (-)-clusianone and (+)- and (-)-clusianone methyl enol ether via ACC alkylation and evaluation of their anti-HIV activity.
AID279409Antiviral activity against HIV1 isolate with RT 101P, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1773448Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1822279Antiviral 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 assay2022Journal 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.
AID491828Antiviral 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 ELISA2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1736360Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID351451Hydrolytic stability in rat plasma assessed as half life by electrospray ionization mass spectrometry2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1729163Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID1761016Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID561943Antibacterial activity against Staphylococcus aureus ATCC 29213 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID1888697Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1320869Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1884493Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1565098Antiviral 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
AID373571Antiviral activity against 0.1 MOI HIV1 3B in 24 hrs pretreated human TZM-b1 cells infected 48 hrs post drug removal assessed as inhibition of viral replication at 0.04 to 0.18 uM measured 24 hrs postinfection by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID496623Antiviral 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 control2010Antimicrobial 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.
AID496626Antiviral 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 control2010Antimicrobial 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.
AID1456311Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID267650Antiviral activity against HIV1 K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID482693Antiviral activity against HIV1 3B infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID198758Percent inhibitory activity against wild type (WT) HIV type I reverse transcriptase at a concentration of 1 uM1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.
AID371908Antiviral activity against HIV1 NL4-3 with V108I mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID82475Antiviral activity against Y188C strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID525102Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID81597Inhibitory activity against NNI-resistant HIV-1 strain A17 with Y181C,K103N mutation2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID88384Antiviral activity against wild-type HIV-1 in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID279404Antiviral activity against HIV1 isolate with RT 103N, 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1352321Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID302270Resistance index, ratio of Ki for HIV1 reverse transcriptase Y181I mutant to Ki for wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1165078Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1335210Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID368565Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex2009Journal 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.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID622056Ratio of Ki for HIV1 RT p66/p66 homodimer Y188L mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1741391Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID492045Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1558858Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID267858Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID1175437Cytotoxicity against human TZM-bl cells after 3 days by XTT assay2015Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.
AID197799Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (Y181C)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
AID279446Antiviral activity against HIV1 isolate with RT 101Q, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1637387Inhibition 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 ELISA2016Bioorganic & 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.
AID525104Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID491834Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573476Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay2009Antimicrobial 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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1077219Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2014European journal of medicinal chemistry, Apr-09, Volume: 76Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.
AID572176Antiviral activity against HIV-1 subtype H V022827 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1380572Resistance index, ratio of IC50 for antiviral activity against HIV1 virions containing reverse transcriptase Y181C mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells to IC50 for antiviral activity ag2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID1391076Inhibition 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 ELISA2018Bioorganic & 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.
AID492285Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID1335209Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/V108I double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID259754Antiviral activity against wild-type HIV1 in MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1761006Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID279406Antiviral activity against HIV1 isolate with RT 103N, 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1171591Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase L100I mutant to EC50 for wild type HIV1 NL4-32014Journal 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.
AID1884538Fold 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 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1736348Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase K103N mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infect
AID248491In vitro inhibitory concentration against HIV F227L and V106A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID734266Antiviral activity against Human immunodeficiency virus 1 SF33 infected in human TZM-bl cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID82608The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1773456Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells
AID1687680Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID1126510Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1627029Inhibition of HIV1 RT using 17-mer DNA/Alexa Fluor 488 5'-end labeled DNA/Alexa Fluor 555-aha-dUTP as primer/template/substrate preincubated for 10 mins followed substarte addition measured after 30 mins by FRET assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID267854Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors.
AID282739Inhibition of HIV1 RT Y181I mutant2005Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity.
AID1379961Antiviral 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 assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID391684Antiviral activity against HIV1 infected in human MT4 cells2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID198075Inhibitory activity against HIV-1 Mutant Reverse transcriptase K103N1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
AID200150Activity of selected HIV-1 N-acylthiocarbamates in enzyme assay against Virion-Associated reverse transcriptase2003Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives.
AID1163231Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID94313Antiviral activity toward K103N mutant HIV-1 virus as protein binding adjusted (PB adj).2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID230127Tested for the ratio between CC50 (MT-4) to EC50 (MT-4)1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID621981Resistance index, ratio of EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant to EC50 for wild-type HIV1 3B2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1373162Inhibition of reverse transcriptase F227L/V106A double mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1155810Fold resistance, ratio of EC50 for HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1380574Resistance index, ratio of IC50 for antiviral activity against HIV1 virions containing reverse transcriptase E138K/M184V mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells to IC50 for antiviral activ2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID573479Antiviral activity of Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial 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.
AID1741392Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID197946In vitro inhibitory activity against human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT)1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
AID1773453Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells
AID779528Antiviral activity against HIV-1 RESO56 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2013Bioorganic & 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.
AID508770Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID491833Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2010Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508651Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID525113Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID279395Antiviral activity against HIV1 isolate with RT 101Q mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID368562Cytotoxicity against human MT4 cells by MTT assay2009Journal 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.
AID1171596Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity2014Journal 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.
AID246348Effective concentration against human immunodeficiency virus type 1 mutated at 100I2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID279441Antiviral activity against HIV1 isolate with RT 101Q, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1249718Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID663300Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID496624Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/A33E, V35T, T39A, D123E, S162A, Q174G, T200E, I202V, Q207E mutant relative to control2010Antimicrobial 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.
AID279425Antiviral activity against HIV1 isolate with RT 179G mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID81442Inhibition of HIV-1 D34 replication in human peripheral blood mononuclear cells.1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID1743619Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID197797Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (L1001)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
AID587751Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated at 102011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID619642Ratio 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 cells2011European 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.
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID1171583Antiviral 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 assay2014Journal 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.
AID525114Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID279420Antiviral activity against HIV1 isolate with RT 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID508769Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID368555Inhibition of wild type HIV1 reverse transcriptase-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal 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.
AID106950Anti-HIV-1 activity against Y181C HIV-1 strain in MT-4 cells2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID443750Antiviral activity against 100 TCID50 HIV1 infected in human TZM-b1 cells assessed as inhibition of viral replication by pseudovirus based assay2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID1072804Antiviral activity against HIV1 3B harboring wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2014Bioorganic & 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.
AID1731745Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB
AID46385Antiviral activity against site directed wild-type enzyme isolate HIV-1 NL4-3WT in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID685330Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C mutant gene infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1736365Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID523481Antiviral activity against HIV1 with RT connection domain G190S/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID246189Effective concentration against human immunodeficiency virus type 1 wild type2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1773461Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1736344Antiviral activity against VSVG/wild-type HIV-1 infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hrs post-infection by luciferase reporter gene ass
AID257169Antiviral activity against HIV1 Y188L mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1191402Cytotoxicity against human MT4 cells after 5 days MTT assay2015Bioorganic & 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.
AID1275554Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1654241Toxicity in C57BL/6J mouse primary hepatocytes assessed as reduction in cell viability by measuring EtBr-positive cell nuclei level at 400 uM incubated for 8 hrs by EtBr/AcrO staining based assay (Rvb = 19%)2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID82607The effect of protein binding on the antiviral activity versus wild type virus strain K103N was tested in the presence of both acid glycoprotein and human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID734271Cytotoxicity against human TZM-bl cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1335204Ratio of IC50 for HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID508758Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1163233Antiviral 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 by2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1520060Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID508771Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID302260Inhibition of HIV1 reverse transcriptase K103N mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1884224Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1249719Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1380571Antiviral activity against HIV1 virions containing reverse transcriptase Y181C mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed 2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID82459Antiviral activity against K103N strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1636927Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID587742Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID571987Antiviral activity against HIV-1 subtype C V022831 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1880369Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1654220Drug metabolism in human primary hepatocytes assessed as O-GlucNVP metabolite formation at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID302262Inhibition of HIV1 reverse transcriptase V106A mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1162233Antiviral activity against HIV12014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Novel indole based NNRTIs with improved potency against wild type and resistant HIV.
AID1654208Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as Cytochrome P450-mediated formation of 8-OHNVP at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1141961Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4.3 infected in human MT4 cells2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1373159Inhibition of reverse transcriptase K103N mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID496632Antiviral 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 control2010Antimicrobial 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.
AID1815391Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID328846Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID279408Antiviral activity against HIV1 isolate with RT 101Q, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1316343Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells2016Journal 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.
AID246298Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells2005Journal 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.
AID1435516Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase E138K mutant
AID246780Compound concentration required to reduce the amount of p24 by 90% in wtIIIBinfected C8166 cells2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID508762Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID572189Antiviral activity against HIV-1 SM058 harboring NNTRI 227L and 106A mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1380569Antiviral activity against HIV1 virions containing reverse transcriptase K103N mutant derived from HIV/VSG-G or HIV/HA virions infected 293T cells using human A549 cells as target cells assessed as inhibition of viral replication using compound pre-mixed 2018Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents.
AID266347Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells2006Bioorganic & medicinal chemistry letters, Jun-01, Volume: 16, Issue:11
New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
AID630786Inhibition of biotin-dNTP labeled HIV-1 reverse transcriptase using ABST as substrate at 100 ug/ml after 1 hr by ELISA2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID366519Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1773458Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID571974Antiviral activity against HIV-1 subtype CRF01_AE V029521 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID344815Antiviral activity against HIV1 NL4-3 infected in HEK293T cells assessed as inhibition of virion-associated p24 antigen production after 24 hrs by ELISA2008Bioorganic & medicinal chemistry, Nov-01, Volume: 16, Issue:21
Inhibition of the CRM1-mediated nucleocytoplasmic transport by N-azolylacrylates: structure-activity relationship and mechanism of action.
AID346971Antiviral activity against HIV ROD in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Studies on anti-HIV quinolones: new insights on the C-6 position.
AID104772Concentration required to reduce the viability of mock-infected MT-4 cells by 50%1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID457957Cytotoxicity in human MT4 cells assessed as reduction in cell viability2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1485969Inhibition of HIV-1 reverse transcriptase L100I mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID197803Inhibitory effect on wild type HIV- 1 reverse transcriptase using rCdG as template and dGTP as substrate.1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1637389Antiviral 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 assay2016Bioorganic & 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.
AID389378Antiviral activity against HIV1 3B in human MT4 cells assessed as protection of cell against virus-induced cytopathogenicity2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID766743Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV12013Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
Synthesis and evaluation of novel 3-(3,5-dimethylbenzyl)uracil analogs as potential anti-HIV-1 agents.
AID572170Antiviral activity against HIV-1 subtype D V022818 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID322393Cytotoxicity against human MT4 cells after 4 days by MTT assay2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs).
AID492043Inhibition of HIV1 reverse transcriptase2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1248226Antiviral activity against wild type HIV 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID199980Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.
AID518736Selectivity 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 transcriptase2010Antimicrobial 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.
AID663313Resistance ratio of ID50 for HIV1 reverse transcriptase Y181I mutant to ID50 HIV1 wild type reverse transcriptase2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID260238Cytotoxicity against human MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1705185Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1743620Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID317731Antiviral activity against HIV2ROD infected in human MT4 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1056586Antiviral activity against wild-type HIV-1 infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after 48 hrs by luciferase reporter gene assay2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1460932Cytotoxicity against human PBMC assessed as reduction in cell viability by MTS assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID1228734Cytotoxicity against human MT4 cells assessed as inhibition of cell metabolism after 72 hrs by MTS assay2015Journal of natural products, May-22, Volume: 78, Issue:5
Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata.
AID1815401Inhibition of HIV1 reverse transcriptase E138K mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1485970Inhibition of HIV-1 reverse transcriptase K103N mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1435515Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y188L mutant
AID1156488Selectivity index, ratio of CC50 for human MT4 cells to IC50 for wild type HIV1 3B2014European journal of medicinal chemistry, Jul-23, Volume: 82Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors.
AID650688Inhibition of HIV 1 reverse transcriptase L100I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID492279Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID279389Antiviral activity against HIV1 isolate with RT 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID253332Cytotoxic concentration against wild type human immunodeficiency virus type 1 LA1 strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1304399Inhibition of HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rC)/oligo(dG) as template primer2016Bioorganic & 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.
AID1410483Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2018ACS 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.
AID440087Antiviral activity against HIV1 HXB2 harboring 227L and 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1636148Ratio 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 cells2016Journal 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.
AID396620Cytotoxicity against human MT4 cells by MTT assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID1298250Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID508760Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V108I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID573467Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay2009Antimicrobial 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.
AID10431450% inhibitory concentration against HIV-1 rRT in MT-4 cells2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
AID587740Selectivity index, ratio of CC50 for human HeLa-T4 cells to EC50 for single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID1056573Ratio of EC50 for HIV-1 expressing reverse transcriptase K103N/P225H double mutant to EC50 for wild-type HIV-12013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID1705189Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID361907Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1741398Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID508648Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, T386A mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1784206Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1784211Antiviral activity against HIV1 L1001 infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1731747Inhibition 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
AID371910Antiviral activity against HIV1 NL4-3 with K103N mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID1654240Drug metabolism in human liver microsomes assessed as Cytochrome P450-mediated formation of 2-OHNVP formation at 5 to 400 uM in presence of NADPH regenerating reagents by uHPLC-MS/MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1200843Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1188001Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
AID1267623Antiviral activity against NNRTI-resistant HIV1 RES056 harboring reverse transcriptase K103N/181C double mutant infected in human MT4 cells2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1126506Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID199243Inhibitory effect on recombinant HIV- 1 reverse transcriptase which has a mutation Tyr 181 to Cys 181 (clone 90)1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID492044Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1152244Inhibition of HIV reverse transcriptase at 100 ug/ml after 1 hr by ELISA relative to control2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1888702Resistance 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
AID197782Inhibition of HIV-1 reverse transcriptase.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID757626Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID523485Antiviral activity against HIV1 with RT connection domain L100I/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID693587Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID561948Antibacterial activity against Escherichia coli after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1357801Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase K103N mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID630954Antiviral activity against X4 tropic Human immunodeficiency virus 1 subtype D-UG070 infected in human TZM-bl cells assessed as inhibition of virus-induced cytopathic effect after 2 days by luciferase assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1705192Resistance 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 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID198593In vitro inhibition of HIV-1 reverse transcriptase at 100 uM1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID199998Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 6 in the article)2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID298060Antiviral activity against HIV1 RF in human CEM-SS cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID508777Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID279436Antiviral activity against HIV1 isolate with RT 103R, 179D mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1754642Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1888693Resistance 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
AID1884223Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against wildtype HIV-1 3B infected in human MT4 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID328841Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID198757Percent inhibitory activity against Y181C HIV type I reverse transcriptase at a concentration of 10 uM1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.
AID302255Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1705196Inhibition 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 cou2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID1456307Inhibition 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 assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1316334Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells2016Journal 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.
AID1152240Antiviral activity against R5 tropic Human immunodeficiency virus 1 ADA5 subtype B infected in human TZM-bl cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by luminescence assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1191671Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 pre-incubated with compound before enzyme addition using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID328882Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 400 uM after 10 days by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID1754644Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID440073Antiviral activity against HIV1 HXB2 harboring K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID622051Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer G190A mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1558856Antiviral 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID738332Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for wild type HIV1 3B2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID665274Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, Jul, Volume: 53Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID81595Inhibitory activity against NNI-resistant HIV-1 strain A17 with Y181C mutation2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Stereochemistry of halopyridyl and thiazolyl thiourea compounds is a major determinant of their potency as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID279475Antiviral activity against HIV1 isolate with RT 101E, 103N, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105153Dose required to achieve 50% protection of MT-4 cells from HIV-1(IIIB) induced cytopathogenicity, determined by MIT method.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
AID1275544Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID257168Antiviral activity against HIV1 K103N mutant strain infected MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1298252Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID587750Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated residual infection in human HeLaT4 cells trea2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID105568Antiviral activity was determined against HIV-1 (clone 90) in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1741397Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID44664Ability to inhibit HIV-2 multiplication in acutely infected C8166 cells1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID1171411Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID738333Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID1244341Anti-trichomonas activity against MTZ-resistant Trichomonas vaginalis incubated for 3 to 48 hrs by trypan blue exclusion assay2015European journal of medicinal chemistry, Aug-28, Volume: 101N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition.
AID279459Antiviral activity against HIV1 isolate with RT 101H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1223492Oral bioavailability in human2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID584080Antiviral activity against HIV1 NL4-3 harboring reverse transcriptase V108I, E138K, F227F/L mutant infected in human SupT1 cells derived from 11 viral passages with lersivirine assessed as inhibition of viral replication after 21 days relative to drug sen2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.
AID1761012Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1736153Inhibition of wild type recombinant HIV-1 subtype B BH10 p66/p51 reverse transcriptase heterodimer expressed in Escherichia coli BL21 (DE3) assessed as inhibition of dTTP incorporation on poly(rA)-oligo(dT) template primer duplex at 10 uM preincubated wit2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID663309Inhibition of HIV1 recombinant reverse transcriptase V106A mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID492280Selectivity index, CC50 for human MT4 cells to EC50 for wild type HIV1 3B2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID88381Antiviral activity against Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID622054Ratio of Ki for HIV1 RT p66/p66 homodimer K103N mutant to Ki for wild-type HIV1 RT p66/p66 homodimer2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID152775Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain RT-MDR.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID1880378Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y181C mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1157585Antiviral 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 assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID1241792Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 infected in human MT4 cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase.
AID1197835Inhibition 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 nucleotides2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID293561Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID247503Inhibitory activity against HIV-1 mutant strain 190A2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID279455Antiviral activity against HIV1 isolate with RT 103N, 188H mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1655526Inhibition of recombinant HIV-1 BH10 reverse transcriptase p51/p66 expressed in Escherichia coli preincubated for 10 mins followed by D38/25PGA template-primer addition and measured after 10 to 30 secs by denaturing PAGE based single nucleotide incorporat2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Peptides Mimicking the β7/β8 Loop of HIV-1 Reverse Transcriptase p51 as "Hotspot-Targeted" Dimerization Inhibitors.
AID361912Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190A mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1191399Antiviral 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 assay2015Bioorganic & 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.
AID276231Antiviral activity against HIV1 3B in MT2 cells2006Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21
Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1784208Antiviral activity against HIV1 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID1443669Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1186008Antiviral activity against HIV1 infected in 293T cells assessed as time of 50% failure2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1357802Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase E138K mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID645832Cytotoxicity against human MT2 cells by MTT assay2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase.
AID623217Cytotoxicity against human MT4 cells after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID298087Inhibition of wild type HIV1 RT2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1186003Antiviral activity against HIV1 harboring reverse transcriptase K103N/G190A double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID650547Resistance ratio of EC50 for HIV 1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for wild type HIV 1 NL4-3 infected in human MT4 cells2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID360705Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID1754640Antiviral 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 assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID105566Antiviral activity was determined against HIV-1 (clone 118) in MT-4 cells infected with HIV-1 IIIB using an XTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246463Compound concentration required to achieve 50% protection of infected MT-4 cells from Y181C strain was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID508757Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1483271Inhibition of HIV1 3B reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal 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.
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1884540Fold 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 cells2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID767498Antiviral 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 assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID197775Compound was evaluated for inhibition of WT HIV type I reverse transcriptase.1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.
AID246269Effective concentration against human immunodeficiency virus type 1 Y188L mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1691438Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1056583Inhibition of HIV-1 reverse transcriptase after 1 hr by spectrophotometry2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID736441Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1637391Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B infected in human MT4 cells2016Bioorganic & 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.
AID650692Inhibition of HIV 1 reverse transcriptase Y188L mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID663295Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID587735Antiviral activity against HIV1 NL4-3.Luc assessed as infectivity using human PBMC pretreated for 24 hrs followed by exposed to virus after compound washout measured after 2 to 3 days by luciferase assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID1537494Inhibition of wild-type HIV1 reverse transcriptase in HIV1 infected HEK293T cells harboring luciferase gene assessed as reduction in viral infection after 48 hrs by Bright-Glo luciferase assay2019ACS medicinal chemistry letters, Feb-14, Volume: 10, Issue:2
Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.
AID302257Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y181C mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID361925Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1418468Inhibition 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 2018Bioorganic & 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.
AID246445Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells; Not determined2005Journal 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.
AID557020Antiviral activity against HIV1 clade B harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1456308Inhibition 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 assay2017Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8
Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR.
AID1320865Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID46585Inhibitory activity against the HIV-1 in CEM cells1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry.
AID1191401Antiviral 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 assay2015Bioorganic & 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.
AID198908In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y181I1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID1282050Antiretroviral activity against HIV-1 based virus like particles infected in U2OS cells assessed as Gluc activity at highest non-toxic concentration2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Antiretroviral (HIV-1) activity of azulene derivatives.
AID82603The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of acid glycoprotein in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID613686Induction of human A375 cell differentiation assessed as microtubule reorganization at 20 uM after 96 hrs by immunofluorescence analysis2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID1352320Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1410484Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells2018ACS 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.
AID368560Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID1373155Cytotoxicity against human MT4 cells after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1316807Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-2 ROD infected in human MT-4 cells2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity.
AID105701Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID373389Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication at 0.11 uM after 24 hrs by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID1231486Antiviral 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 assay2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action.
AID527375Antiviral activity against wild type HIV1 NL4-3 infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
Discovery and SAR of a series of 4,6-diamino-1,3,5-triazin-2-ol as novel non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID302258Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y188L mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1171413Antiviral 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 assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1357794Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID508759Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1292361Cytotoxicity against human TZM-bl cells assessed as reduction of cell viability after 48 hrs2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID317732Cytotoxicity against human HIV1RF infected CEM-SS cells by MTT assay2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID1743628Antiviral 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 assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID608392Cytotoxicity against human MAGI-CCR5 cells after 48 hrs by MTS cell viability assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1574374Antiviral 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 assay2019Journal 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.
AID1574385Inhibition 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 analysi2019Journal 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.
AID88366Antiviral activity against K103N mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1248222Antiviral activity against wild type HIV 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1637396Antiviral 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 assay2016Bioorganic & 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.
AID366521Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase K103N mutation to EC50 for wild type HIV1 NL4-32008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1610042Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 5 days by MTT assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID279394Antiviral activity against HIV1 isolate with RT 98G mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1275550Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1303217Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 24 hrs by MTT assay2016European journal of medicinal chemistry, Jul-19, Volume: 117Design, synthesis and anti-HIV activity of novel quinoxaline derivatives.
AID366520Antiviral activity against HIV1 isolates with reverse transcriptase K103N mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID557041Antiviral 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% FBS2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID104760Dose required to reduce the viability of mock-infected cells by 50%1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID1059144Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1822333Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity at 2 uM incubated for 5 days by MTT assay2022Journal 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.
AID46378Antiviral activity against site directed resistant isolate HIV-1 L100I in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID235444Selective index as the ratio of CD50 to that of ED50 against HIV-1 HxB2 strain.2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID106048Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cell was determined; Not determined2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID557019Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1217729Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID297144Antiviral activity against HIV1 with RT V106A mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID586910Induction of BCRP activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID525112Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID104963Compound was evaluated for the anti-viral activity against cultured MT-4 cells1994Journal of medicinal chemistry, Jul-22, Volume: 37, Issue:15
Synthesis of a series of 4-(arylethynyl)-6-chloro-4-cyclopropyl-3,4-dihydroquinazolin-2(1H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1460939Antiviral activity against HIV-1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MAGI-CCR5 cells after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID44808Inhibitory concentration against cell culture of Human T-cell line c8166 infected with HIV-1 IIIB strain was determined1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID1304406Inhibition 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 primer2016Bioorganic & 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.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1637395Antiviral 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 assay2016Bioorganic & 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.
AID1410411Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018ACS 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.
AID735083Inhibition of HIV reverse transcriptase2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and biological evaluation of phosphonate analogues of nevirapine.
AID473115Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID622052Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N/Y181C mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1610044Therapeutic index, ratio of CC50 for human PBMC cells to IC50 for antiviral activity against HIV1 VB51 infected in human TZM-bl cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269797Antiviral activity against HIV1 I135V mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID648425Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT)2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1705184Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID648424Antiviral 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 assay2012European journal of medicinal chemistry, May, Volume: 51Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID738336Inhibition of HIV 1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly rA.dT by ELISA2013Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
AID44797In vitro reduction of p24 by 90% in Efavirenz resistant HIV-1 (K103R, V179D, P225H) infected C8166 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID1736346Selectivity index, ratio of CC50 for human HEK 293T cells to EC50 for VSVG/wild type HIV1 infected in human HEK 293T cells
AID499277Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
AID649826Antiviral activity against HIV1 LAI infected in human CEMx174 cells coexpressing GFP preincubated for 1 hr measured after 5 days by fluorimetry2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication.
AID279428Antiviral activity against HIV1 isolate with RT 101E, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105860Compound was tested for potency to achieve protection of MT-4 cells from 103N strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID726438Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method2013Bioorganic & 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.
AID46384Antiviral activity against site directed resistant isolates in HIV-1 A98G CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1316339Antiviral 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 assay2016Journal 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.
AID1609108Antiviral 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID572186Antiviral activity against HIV-1 SM034 harboring NNTRI 188L mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1165074Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID523482Antiviral activity against HIV1 with RT connection domain G190S/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1292364Inhibition of recombinant HIV1 reverse transcriptase using 234-nt long RNA/18-mer DNA oligonucleotide as template/primer assessed as remaining activity at 200 uM preincubated for 15 mins followed by incubation with template/primer for 40 mins by liquid sc2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID523351Antiviral activity against HIV1 with RT connection domain K103N/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID586909Induction of MRP3 activity2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Interaction potential of etravirine with drug transporters assessed in vitro.
AID416755Antiviral activity against HIV1 with reverse transcriptase L100I mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID698306Antiviral activity against HIV1 containing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal 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.
AID561945Antibacterial activity against Salmonella group B ATCC 31194 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID1784216Antiviral activity against HIV1 harboring reverse transcriptase V106A/F227 mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID105695Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID246350Effective concentration against human immunodeficiency virus type 1 mutated at 181C2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID1141971Ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1304402Cytotoxicity against mock-infected human CEM-SS cells2016Bioorganic & 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.
AID197931HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer.1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID373562Antiviral activity against 0.1 MOI HIV1 3B in 24 hrs pretreated human TZM-b1 cells infected 0 hr post drug removal assessed as inhibition of viral replication at 0.18 uM measured 24 hrs postinfection by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID1637397Antiviral 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 assay2016Bioorganic & 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.
AID561951Antibacterial activity against Shigella flexneri group B after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID635347Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2011Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
AID1819220Inhibition of wild type HIV-1 reverse transcriptase using biotin-labelled dNTPs as substrate incubated for 2 hrs by ELISA
AID351450Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID246343Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells2005Journal 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.
AID457955Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1736347Inhibition of HIV-1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT) as template/primer incubated for 1 hr followed by transferring into streptavidin plate for 1 hr by absorba
AID247497Inhibitory activity against HIV-1 mutant strain 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1561722Resistance 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
AID1729161Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Exploiting 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
AID613676Antiproliferative activity against human A375 cells assessed as cell growth at 350 uM after 96 hrs by trypan blue assay2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID525110Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Mutations in human immunodeficiency virus type 1 integrase confer resistance to the naphthyridine L-870,810 and cross-resistance to the clinical trial drug GS-9137.
AID1217727Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID650545Antiviral 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 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID413266Antiviral activity against multidrug-resistant HIV1 with reverse transcriptase 41L, 74V, 184V, 210W, 215Y, ins SS, 98G mutation infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID1292014Inhibition 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 ELISA2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1884220Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1685253Covalent inhibition of recombinant wild type HIV-1 reverse transcriptase using poly(rA)350/oligo(dT)16 as template/primer preincubated followed by substrate addition measured after 1 hr by pico-green reagent based fluorescence analysis2021ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead.
AID1443663Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1773462Resistance 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
AID1056580Antiviral activity against HIV-1 expressing reverse transcriptase K103N/V108I double mutant infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID440086Antiviral activity against HIV1 HXB2 harboring K103N and Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1391085Antiviral 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 assay2018Bioorganic & 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.
AID622047Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer K103N mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID1457065Inhibition 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 2017Journal 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.
AID1197829Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID1435518Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase mutant
AID663305Inhibition of HIV1 wild type recombinant reverse transcriptase assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1292360Cytotoxicity against human U2OS cells assessed as reduction of cell viability after 48 hrs2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID351445Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by MTT assay2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID370728Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V106A mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID508796Ratio 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 assay2010Antimicrobial 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.
AID82277Inhibition of HIV-1 IIIB replication in MT-4-infected wild type cells.2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID1750721Inhibition of HIV-1 p66/p51 reverse transcriptase E138K mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal 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
AID523346Antiviral activity against HIV1 with RT connection domain T369V mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID1572518Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay
AID571975Antiviral activity against HIV-1 subtype CRF01_AE V029525 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1750715Cytotoxicity against in human MT-4 cells after 5 days by MTT assay2021Journal 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
AID457958Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1275546Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID1736156Cytotoxicity against human MT2 cells assessed as reduction in cell viability measured after 4 days by Trypan blue assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme.
AID1410405Inhibition 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 ELISA2018ACS 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.
AID1691435Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay2020European journal of medicinal chemistry, May-01, Volume: 193In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP.
AID1161108Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation using hybrid poly (A).oligo (dT)15 template primer incubated for 1 hr at 37 degC by ELISA method2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1657474Antiviral activity against HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2020Bioorganic & medicinal chemistry, 04-15, Volume: 28, Issue:8
Inhibition of HIV-1 RT activity by a new series of 3-(1,3,4-thiadiazol-2-yl)thiazolidin-4-one derivatives.
AID1199053Selectivity index, ratio of CC50 for human MT4 cells to IC50 for Human immunodeficiency virus 1 3b infected in human MT4 cells2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead.
AID105707Anti-HIV-1 activity against Y188L strain was determined in MT-4 cells by the MTT method2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1390710Antiviral 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 assay2018Bioorganic & 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.
AID1583030Inhibition of recombinant HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in to cDNA chain incubated for 1 hr by ELISA2020Journal 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.
AID279423Antiviral activity against HIV1 isolate with RT 106I, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID200161Compound concentration required to inhibit the HIV-1 recombinant Reverse transcriptase (rRT) activity by 50%.1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269799Antiviral activity against HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1391079Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay2018Bioorganic & 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.
AID155274Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 (Y181C) in peripheral blood mononuclear cells (PBMC)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID508793Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID361919Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase E138K mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1124998Inhibition of recombinant HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation in to poly [A] x oligo[dT]15 by ELISA2014Bioorganic & 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.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID105861Compound was tested for potency to achieve protection of MT-4 cells from 106A strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID717253Inhibition of HIV1 reverse transcriptase assessed as biotin-dUTP incorporation into enzyme using poly(rC)-oligo(dG) as template primer by colorimetric analysis2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
AID619634Antiviral 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 assay2011European 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.
AID198073Inhibitory activity against HIV-1 Mutant Reverse transcriptase G190A1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID1292359Antiviral activity against HIV1 virus-like particles harboring wild type reverse transcriptase infected in human U2OS cells after 24 hrs by Renilla luciferase assay2016Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11
Design, discovery, modelling, synthesis, and biological evaluation of novel and small, low toxicity s-triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID665550Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2012Bioorganic & 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.
AID197798Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (P236L)1998Bioorganic & medicinal chemistry letters, Aug-18, Volume: 8, Issue:16
A dipyrido [2,3-b:3',2'-f]azepine analog of the HIV-1 reverse transcriptase inhibitor nevirapine.
AID198907In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution V106A1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1457062Ratio 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 cells2017Journal 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.
AID235796Selectivity index was measured as the ratio of CC50(HIV-1) to that of EC50(HIV-1); SI Selectivity Index1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
AID1241795Selectivity index, ratio of IC50 for human CEM-SS cells to EC50 for HIV1 infected in human CEM-SS cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase.
AID104761Cytotoxicity against mock-infected MT-4 cells.1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
AID391679Inhibition of RNA dependent DNA polymerase activity of Escherichia coli DNA polymerase 1 Klenow fragment assessed as residual enzyme activity at 50 ug/ml relative to control2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID440076Antiviral activity against HIV1 HXB2 harboring 100I mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID440671Antiviral activity against NNRTI-resistant HIV1 A17 with reverse transcriptase K103N, Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID105545Inhibition of mutant type (Cys181) HIV-1 (IIIB) replication in MT-4 cells1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1187998Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 using dsDNA by microplate reader based assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
AID1298246Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells2016Bioorganic & 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.
AID757627Inhibition of HIV RT K103N/Y181C mutant by cell based assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1773450Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID1636150Ratio 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 cells2016Journal 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.
AID1186687Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
AID1298247Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID1687692Antiviral activity against wild type HIV1 infected in human SupT1 cells assessed as inhibitory effect at 100 nM by cell based inhibition assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase.
AID1457059Ratio 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 cells2017Journal 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.
AID666972Cytotoxicity against human MT4 cells after 5 days by MTT assay2012European journal of medicinal chemistry, Aug, Volume: 54Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors.
AID473114Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID1200848Inhibition 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 ELISA2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID1267610Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID153129Cytotoxic concentration was determined2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID263519Antiviral activity against HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID1822280Antiviral 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 assay2022Journal 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.
AID1057035Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin dUTP incorporation by primer extension assay2013Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs.
AID1161107Cytotoxicity against human MT4 cells by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID623214Antiviral activity against HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID370730Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y188L mutant expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1731752Inhibition 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
AID1377174Antiviral activity against NRTI-resistant HIV1 isolate 1617-1 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA2017Journal of natural products, 06-23, Volume: 80, Issue:6
Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa.
AID152777Inhibitory activity of compound won p24 production in peripheral blood mononuclear cells infected with HIV strain HTLV IIIB wild type.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID1171587Antiviral 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 assay2014Journal 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.
AID558386Drug level in HIV-infected pregnant woman amniotic fluid at 200 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID665549Cytotoxicity against human MT4 cells after 5 days by MTT assay2012Bioorganic & 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.
AID587737Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as time required to cause 50% loss in compound potency at 10 t2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID242064Concentration required for 50% inhibition of wild type human immunodeficiency virus type 1 reverse transcriptase2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID757621Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID298076Antiviral activity against HIV1 RT K103N-Y181C mutant in MT4 cells by MTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
AID1357788Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID492283Antiviral activity against HIV1 with reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID200171Inhibition single mutant of HIV-1 RT (Y181C)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID368557Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal 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.
AID632801Antiviral 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 infection2011Journal 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.
AID508775Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID572171Antiviral activity against HIV-1 subtype D V022819 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID587734Antiviral activity against HIV1 NL4-3.Luc assessed as infectivity using human MDM pretreated for 24 hrs followed by exposed to virus after compound washout measured after 2 to 3 days by luciferase assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID619628Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into enzyme by colorimetry2011European 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.
AID106057Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1654198Drug metabolism in human assessed as formation of 12-OH-NVP2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID1248224Selectivity index, ratio of CC50 for uninfected human MT4 cells to EC50 for wild type HIV 1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20
A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities.
AID1609105Selectivity index, ratio of CC50 for human MT4 cells to EC50 of antiviral activity against HIV-1 IIIB infected in human MT4 cells2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279398Antiviral activity against HIV1 isolate with RT 103N, 108I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID104244Cytotoxic concentration against MT-2 cells1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID558580Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 200 mg, po BID by HPLC/UV analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women.
AID1335219Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID82466Antiviral activity against P225H strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID440085Antiviral activity against HIV1 HXB2 harboring 101E and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID279405Antiviral activity against HIV1 isolate with RT 101E, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1124989Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay2014Bioorganic & 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.
AID293558Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID571969Antiviral activity against HIV-1 subtype CRF02_AG V022826 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID279401Antiviral activity against HIV1 isolate with RT 181C, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID621982Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer L100I mutant using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269685Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1610054Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID685335Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B2012Bioorganic & medicinal chemistry, Sep-15, Volume: 20, Issue:18
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
AID1155816Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1572520Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
AID1773439Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1750714Antiviral activity against HIV-1 infected in human MT-4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay2021Journal 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
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID1435511Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase
AID1558847Antiviral activity against HIV1 3B infected in human MT4 cells incubated assessed as reduction in virus-induced cytopathic effect for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID1152370Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID766432Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID1561718Antiviral 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
AID630951Cytotoxicity in human TZM-bl cells assessed as cell viability after 48 hrs by MTT assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID391688Inhibition of DNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID1574382Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV-1 NL4-32019Journal 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.
AID508639Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID1877037Antiviral activity against HIV-1 pseudovirus infected in human TZM-bl cells preincubated with virus for 30 mins followed by cell infection and measured after 3 days by luciferase assay2021Journal of medicinal chemistry, 11-25, Volume: 64, Issue:22
HIV-1 gp120 Antagonists Also Inhibit HIV-1 Reverse Transcriptase by Bridging the NNRTI and NRTI Sites.
AID88379Antiviral activity against V108I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1754638Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay2021Bioorganic & medicinal chemistry, 07-15, Volume: 42Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
AID1443661Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1316332Antiviral 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 assay2016Journal 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.
AID440078Antiviral activity against HIV1 HXB2 harboring 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID1188000Antiviral activity against HIV2 ROD acutely infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
AID1736367Selectivity index, ratio of EC50 for antiviral activity against VSVG/HIV-1 harboring reverse transcriptase G190A/K103N double mutant infected in human HEK 293T cells to EC50 for antiviral activity against VSVG/wild type HIV-1 infected in human HEK293T cel
AID572182Antiviral activity against HIV-1 SM012 harboring NNTRI 108I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID105864Compound was tested for potency to achieve protection of MT-4 cells from 190A strain of HIV-1 virus2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
AID1594856Half life in human serum at 200 mg, bid2019Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic.
AID1200847Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID586317Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of gag gene expression at 0.27 ug/ml after 5 days post infection by quantitative real time RT-PCR2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Antiviral activity of seed extract from Citrus bergamia towards human retroviruses.
AID1352314Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID302259Inhibition of wild type HIV1 3B reverse transcriptase2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID457961Inhibition of HIV1 reverse transcriptase K103N mutant by RNA-dependent DNA polymerase activity assay2010Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID508792Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1610038Antiviral activity against HIV1 92/BR/018 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID1162234Antiviral activity against HIV1 infected in HEK293T cells by p24 ELISA based phenotypic assay2014Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18
Novel indole based NNRTIs with improved potency against wild type and resistant HIV.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1460942Antiviral activity against HIV-1 NL4-3 harboring reverse transcriptase E138A mutant infected in human MAGI-CCR5 cells assessed as reduction in viral infection after 48 hrs by fluorescence based beta-galactosidase reporter gene assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID88380Antiviral activity against V108I/Y181C mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1357803Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y181C mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1373161Inhibition of reverse transcriptase E138K mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID361915Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106M mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID229259Antiviral activity was evaluated for the inhibition of wild-type RF strain of HIV-1 in an in vitro enzyme assay.2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1750727Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase E138K mutant2021Journal 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
AID663310Inhibition of HIV1 recombinant reverse transcriptase Y188L mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT)2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1750724Selectivity index, ratio of CC50 for cytotoxicity against human MT-4 cells to EC50 for inhibition of HIV-1 p66/51 reverse transcriptase K103N mutant2021Journal 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
AID200169Inhibition of HIV-1 RT using rC-dG as template1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID557053Antiviral activity against NRTI-, PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID413268Antiviral activity against wild type HIV1 3B in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID630956Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 subtype D-UG0702011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1558848Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID197794In vitro for inhibition of HIV-1 reverse transcriptase.1995Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones.
AID499276Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Anti-HIV and antiplasmodial activity of original flavonoid derivatives.
AID105342Inhibitory activity against resistant HIV-1 strain NevR was determined.1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID675274Inhibition of HIV reverse transcriptase activity at 10 ug/ml incubated at 37 degC for 1 hr by ELISA RT assay2012European journal of medicinal chemistry, Sep, Volume: 55One pot efficient diversity oriented synthesis of polyfunctional styryl thiazolopyrimidines and their bio-evaluation as antimalarial and anti-HIV agents.
AID1446820Antiviral 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 assay2017European journal of medicinal chemistry, Apr-21, Volume: 130Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.
AID650546Antiviral 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 assay2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID302264Inhibition of HIV1 reverse transcriptase Y1811 mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID587743Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID587756Ratio of EC50 for HIV1 NL4-3.Luc assessed as infectivity using human PBMC pretreated for 24 hrs followed by exposed to virus after compound washout to standard EC50 for HIV1 NL4-3.Luc2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID663301Resistance ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-32012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID440080Antiviral activity against HIV1 HXB2 harboring 179E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID496628Antiviral 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 control2010Antimicrobial 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.
AID105348Tested for the inhibitory activity of HIV-1 infected MT-4 cells1994Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
AID1249724Inhibition of HIV1 reverse transcriptase p66/p51 assessed as inhibition of biotin-dUTP incorporation using poly (rA)/oligo(dT)16 as template/primer incubated for 40 mins2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1773460Resistance factor, ratio of EC50 for HIV1 harboring Y188L mutant mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID361916Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1654212Drug metabolism in human primary hepatocytes assessed as Cytochrome P450-mediated formation of 3-OHNVP at 10 uM incubated for 24 to 48 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID508768Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1815377Anti-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 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID106061Inhibitory activity against 103N strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1884226Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID106775Inhibition of cell culture in MT-4 cells1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID368564Inhibition of wild type HIV1 free reverse transcriptase2009Journal 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.
AID46374Antiviral activity against site directed 4X AZT resistant isolate HIV-1 L100I in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1335215Antiviral activity against HIV-1 NL4-3 harboring RT-Y181C mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID557049Antiviral activity against HIV1 clade G harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID1175921Cytotoxicity against HEK293 cells infected with VSV-G protein pseudotyped HIV12014Journal of natural products, Dec-26, Volume: 77, Issue:12
Diterpenes from a Chinese collection of the brown alga Dictyota plectens.
AID297142Antiviral activity against HIV1 with RT Y181C mutation by cytopathic cell killing assay2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme.
AID279453Antiviral activity against HIV1 isolate with RT 98G, 100I, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID781024Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
AID1335211Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID106069Inhibitory activity against 188L strain of HIV-I in MT-4 cells2001Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17
Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues.
AID1862265Inhibition of wild-type recombinant HIV-1 group M subtype B BH10 reverse transcriptase RNase-associated RNase H activity expressed in Escherichia coli XL1 blue using 32P-labeled 5'-UUUUUUUUUAGGAUACAUAUGGUUAAAGUAU-3'/5'-ATACTTTAACCATATGTATCC-3' RNA/DNA tem2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.
AID396619Antiviral activity against HIV1 3B replication in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID1763902Antiviral 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 assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID1165075Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1185992Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1736349Inhibition of RNase H activity of HIV-1 reverse transcriptase using DNA/RNA hybrid as substrate incubated for 30 mins by fluorescence based analysis
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269795Antiviral activity against HIV1 E138K mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID726436Cytotoxicity in human MT2 cells assessed as inhibition of cell growth2013Bioorganic & 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.
AID373554Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication after 24 hrs by luciferase assay2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analog.
AID496742Antiviral 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 control2010Antimicrobial 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.
AID1483274Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2017Journal 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.
AID1822334Antiviral activity against HIV-1 harboring RES056 mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity at 2 uM incubated for 5 days by MTT assay2022Journal 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.
AID508646Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1637394Antiviral 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 assay2016Bioorganic & 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.
AID1773445Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1185999Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay relative HIV12014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1637399Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring L100I mutant infected in human MT4 cells2016Bioorganic & 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.
AID368556Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-mediated RNA-dependent DNA polymerase activity expressed in Escherichia coli BL21 assessed as [3H]dTTP incorporation by cell free-based scintillation counting2009Journal 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.
AID1773447Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1357804Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID1773446Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1884228Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features.
AID1161103Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID523352Antiviral activity against HIV1 with RT connection domain K103N/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID523479Antiviral activity against HIV1 with RT connection domain G190S mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-32010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Combinations of mutations in the connection domain of human immunodeficiency virus type 1 reverse transcriptase: assessing the impact on nucleoside and nonnucleoside reverse transcriptase inhibitor resistance.
AID79450Ability to inhibit HIV-1 multiplication in chronically infected H9/IIIB cells1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID371906Antiviral activity against HIV1 NL4-3 with K103N/V108I double mutant in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs by single round replication assay2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID473116Cytotoxicity against human MT4 cells after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
AID1298248Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry2016Bioorganic & 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.
AID248879Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/V108I resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID351448Cytotoxicity against human MT4 cells by MTT assay2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1157580Cytotoxicity against human MT4 cells after 96 hrs by MTT assay2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Synthesis of novel fluoro analogues of MKC442 as microbicides.
AID143387Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 with a Y181C mutation in RT (reverse transcriptase)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
AID1457063Inhibition 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 c2017Journal 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.
AID1609107Antiviral 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID663311Resistance ratio of ID50 for HIV1 reverse transcriptase K103N mutant to ID50 HIV1 wild type reverse transcriptase2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID608391Antiviral activity against HIV1 3B infected in human MAGI-CCR5 cells assessed as inhibition of viral replication after 48 hrs by beta-galactosidase reporter assay2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID227244The compound was evaluated for antiviral activity using whole cell assay2000Bioorganic & medicinal chemistry letters, Jan-17, Volume: 10, Issue:2
Novel 2,2-dioxide-4,4-disubstituted-1,3-H-2,1,3-benzothiadiazines as non-nucleoside reverse transcriptase inhibitors.
AID1750718Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal 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
AID736039Inhibition of HIV1 reverse transcriptase p66/p51 G190A mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID492276Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID287002Inhibition of HIV1 wild type p66/p51 reverse transcriptase2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID197787In vitro ability to inhibit mutant P236L reverse transcriptase2000Journal of medicinal chemistry, Mar-09, Volume: 43, Issue:5
Novel 1,5-diphenylpyrazole nonnucleoside HIV-1 reverse transcriptase inhibitors with enhanced activity versus the delavirdine-resistant P236L mutant: lead identification and SAR of 3- and 4-substituted derivatives.
AID1191669Cytotoxicity against human MT4 cells assessed as reduction in cell viability2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID153102Cytotoxic concentration against PBMC cells1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID665552Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant2012Bioorganic & 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.
AID508635Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity2010Antimicrobial 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.
AID508794Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1815402Inhibition of HIV1 reverse transcriptase F227L/V106A double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1267608Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Design and Synthesis of DiselenoBisBenzamides (DISeBAs) as Nucleocapsid Protein 7 (NCp7) Inhibitors with anti-HIV Activity.
AID1561721Resistance 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
AID361921Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P236L mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1460928Cytotoxicity against human MAGI-CCR5 cells assessed as reduction in cell viability after 48 hrs by MTS assay2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID1811045Cytotoxicity against mock infected human MT4 cells by MTT assay2021Journal 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.
AID263520Antiviral activity against HIV1 Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID198779In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution K103N1999Journal of medicinal chemistry, Oct-21, Volume: 42, Issue:21
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1163232Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID248845Inhibitory concentration against human immunodeficiency virus type 1 (with Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID1249714Antiviral 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 method2015European journal of medicinal chemistry, Sep-18, Volume: 102Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
AID1335220Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/Y188L double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1637400Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring K103N mutant infected in human MT4 cells2016Bioorganic & 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.
AID1862269Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay2022European journal of medicinal chemistry, Oct-05, Volume: 240Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors.
AID143385Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 variant with Y181C plus K103N mutations in RT (reverse transcriptase)2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds.
AID1572523Antiviral 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
AID571973Antiviral activity against HIV-1 subtype CRF01_AE V022822 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID198912Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution L10012001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID267652Selectivity for wild type HIV1 virus over HIV1 Y181C mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID1485972Inhibition of HIV-1 reverse transcriptase E138K mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID1743634Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID279400Antiviral activity against HIV1 isolate with RT 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID632797Antiviral 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 infection2011Journal 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.
AID279448Antiviral activity against HIV1 isolate with RT 101H, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID267654Selectivity for wild type HIV1 virus over HIV1 K103N/L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID630950Antiviral activity against R5 tropic Human immunodeficiency virus 1 subtype B-ADA5 infected in human TZM-bl cells assessed as inhibition of virus-induced cytopathic effect after 2 days by luciferase assay2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID302249Antiviral activity against HIV1 NL43 in MT4 cells assessed as inhibition of viral induced cytopathic effect after 4 days by MTT method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID298062Antiviral activity against HIV2 ROD in human MT4 cells by XTT assay2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID736438Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1888698Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID482699Antiviral activity against HIV S07 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID1736361Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase V108I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID757624Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2013European journal of medicinal chemistry, Jul, Volume: 65Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1373153Inhibition of recombinant wild-type HIV-1 3B reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli JM109 assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID1173645Cytotoxicity against human CEmx174 cells expressing GFP after 5 days by resazurin assay2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Serendipitous discovery of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine derivatives as novel HIV-1 replication inhibitors.
AID267646Cytotoxicity against HEK293T cells2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID619640Antiviral 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 assay2011European 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.
AID1199052Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead.
AID317730Antiviral activity against HIV13B infected in human MT4 cells2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID508754Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1763897Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs.
AID104450Concentration required to protect the cell against HIV-2 strain ROD viral cytopathogenicity by 50% in MT-4 cells; NA denotes not active2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
AID1335214Antiviral activity against HIV-1 NL4-3 harboring RT-L100I/K103N double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID781025Cytotoxicity against human MT4 cells after 5 days by MTT assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
AID279450Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID440077Antiviral activity against HIV1 HXB2 harboring 101E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269805Antiviral activity against HIV1 Y181S mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID551466Selectivity index, ratio of CC50 for human C1866 cells to EC50 for HIV1 3B infected in human C8166 cells2011Bioorganic & medicinal chemistry letters, Jan-15, Volume: 21, Issue:2
Synthesis and biological evaluation of novel dihydro-aryl/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents.
AID619639Antiviral 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 assay2011European 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.
AID1165079Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-/biotin-labeled dUTP nucleotides incubated for 1 hr2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID1335213Antiviral activity against HIV-1 NL4-3 harboring RT-Y188L mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1199051Cytotoxicity against human MT4 cells assessed as inhibition of overall cell metabolism after 5 days by MTT assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Jatrophane diterpenes as inhibitors of chikungunya virus replication: structure-activity relationship and discovery of a potent lead.
AID197943In vitro inhibition of mutant Y181C recombinant reverse transcriptase of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID1379959Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID1741390Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID734263Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 SF33 infected in human MT4 cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1352318Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1884492Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID492281Antiviral activity against wild type HIV1 LAI infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1335202Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/G190A double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID248262In vitro inhibitory concentration against HIV V106A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID247526Inhibitory activity against wild type HIV-1 LAI cell line2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID265470Cytotoxicity against human lymphocytes2006Journal of medicinal chemistry, Jun-01, Volume: 49, Issue:11
Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide.
AID496630Antiviral 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 control2010Antimicrobial 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.
AID200170Inhibition single mutant of HIV-1 RT (K103 N)1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID279473Antiviral activity against HIV1 isolate with RT 230L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID257916Antiviral activity against HIV1 K103N mutant using HeLa MAGI assay2006Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
Structure-activity relationship studies of novel benzophenones leading to the discovery of a potent, next generation HIV nonnucleoside reverse transcriptase inhibitor.
AID248257In vitro inhibitory concentration against HIV G190A mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID508772Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID246556Concentration required for 50% protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity was determined by the MTT method2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
Docking and 3-D QSAR studies on indolyl aryl sulfones. Binding mode exploration at the HIV-1 reverse transcriptase non-nucleoside binding site and design of highly active N-(2-hydroxyethyl)carboxamide and N-(2-hydroxyethyl)carbohydrazide derivatives.
AID155280Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain RT-MDR(V106A) in peripheral blood mononuclear cells (PBMC)1999Bioorganic & medicinal chemistry letters, Sep-20, Volume: 9, Issue:18
N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea and N'-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-chloropyridyl)]-thiourea as potent inhibitors of multidrug-resistant human immunodeficiency virus-1.
AID1705190Resistance 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 cells2020European journal of medicinal chemistry, Dec-15, Volume: 208New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
AID197941In vitro inhibition of mutant P236L recombinant reverse transcriptase of HIV-1 IIIB1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID492047Antiviral activity against HIV1 bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1165077Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.
AID561940Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID663297Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1815396Inhibition of wild type HIV1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites.
AID413565Ratio of EC50 for multidrug-resistant HIV1 with reverse transcriptase 41L, 74V, 184V, 210W, 215Y, ins SS, 98G mutation to EC50 for wild type HIV1 3B2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Development and preclinical studies of broad-spectrum anti-HIV agent (3'R,4'R)-3-cyanomethyl-4-methyl-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (3-cyanomethyl-4-methyl-DCK).
AID508766Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID734270Inhibition of HIV1 reverse transcriptase after 1 hr by colorimetric assay2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID279442Antiviral activity against HIV1 isolate with RT 98G, 190A mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID698299Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-32012Journal 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.
AID286999Inhibition of DNA polymerase activity of HIV1 reverse transcriptase2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1316330Antiviral 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 assay2016Journal 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.
AID1609106Antiviral 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 assay2019European journal of medicinal chemistry, Nov-15, Volume: 182Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1435510Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay
AID573477Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay2009Antimicrobial 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.
AID1815388Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1304405Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human MT4 cells to EC50 for antiviral activity against HIV-1 3B2016Bioorganic & 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.
AID1460947Inhibition of HIV1 NL4-3 reverse transcriptase assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 1 hr by microbeta scintillation counting analysis2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID279447Antiviral activity against HIV1 isolate with RT 236L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID105324Inhibition of Efavirenz resistant HIV-1 (K103N-Y181C) induced cytopathicity in MT-4 cells.2004Journal of medicinal chemistry, Jul-15, Volume: 47, Issue:15
Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
AID1161106Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
AID1815380Antiviral 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 assay2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID573471Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay2009Antimicrobial 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.
AID1811044Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay2021Journal 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.
AID279427Antiviral activity against HIV1 isolate with RT 103R, 179D, 188L mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID293559Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID650690Inhibition of HIV 1 reverse transcriptase Y181I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT)2011Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level.
AID370724Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 expressed in Escherichia coli JM1092009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID246265Effective concentration against human immunodeficiency virus type 1 G190S mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1056582Antiviral activity against HIV-1 expressing reverse transcriptase K103N mutant infected in human 293T cells co-transfected with VSVG protein assessed as inhibition of viral-replication incubated 15 mins prior to viral-infection measured after 48 hrs by lu2013Journal of natural products, Dec-27, Volume: 76, Issue:12
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
AID198086Inhibitory activity against HIV-1 Y181C Reverse transcriptase (RT)1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID360711Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay2007The Journal of biological chemistry, Mar-16, Volume: 282, Issue:11
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
AID1687683Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay2020European journal of medicinal chemistry, Jan-15, Volume: 186Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
AID510360Inhibition of HIV1 reverse transcriptase after 1 hr by ELISA2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.
AID1171589Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-32014Journal 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.
AID1457061Ratio 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 cells2017Journal 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.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269793Antiviral activity against HIV12006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID573466Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay2009Antimicrobial 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.
AID1152373Cytotoxicity against human MT4 cells by MTT assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID279452Antiviral activity against HIV1 isolate with RT 103N, 108I, 238T mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID572178Antiviral activity against HIV-1 subtype H V029523 harboring NNRTI K101Q and V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID734257Antiviral activity against NNRTI-resistant Human immunodeficiency virus 1 harboring reverse transcriptase K103N mutation infected in human MT4 cells assessed decrease in p24 level after 7 days by ELISA2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID566900Cytotoxicity against human MT4 cells after 5 days by spectrophotometry2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.
AID1163234Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1186000Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID571981Antiviral activity against HIV-1 subtype B V022813 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1773449Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay
AID1636928Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method2016Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20
Computer-aided discovery of anti-HIV agents.
AID736439Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID440079Antiviral activity against HIV1 HXB2 harboring 138K mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay2009Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-Iodopyridin-2(1H)-one type anti-HIV agents.
AID522369Antiviral 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 microscopy2010Antimicrobial 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.
AID298065Metabolic stability in rat plasma2007Journal of medicinal chemistry, Oct-04, Volume: 50, Issue:20
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
AID1292011Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID1352316Antiviral 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 assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
AID1637402Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y188L mutant infected in human MT4 cells2016Bioorganic & 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.
AID392513Antiviral activity against HIV12009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks.
AID1185994Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1410486Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation2018ACS 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.
AID247618Inhibitory activity against HIV-1 double mutants strain 101E and 103N2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID621974Inhibition of DNA-dependent DNA polymerase activity of HIV1 reverse transcriptase p66/p66 homodimer using activated DNA and [alpha-32P]dATP after 30 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
AID257163Inhibition of wild type HIV1 reverse transcriptase by [3H]dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1750719Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis2021Journal 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
AID572174Antiviral activity against HIV-1 subtype CRF05_DF V022833 harboring NNRTI V179I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID479214Inhibition of biotin-dUTP labeled HIV-1 reverse transcriptase after 30 mins colorimetric streptavidin alkaline phosphatase reporter system2010Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
Synthesis and biological evaluation of novel 2-arylalkylthio-4-amino-6-benzyl pyrimidines as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID496634Antiviral 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 control2010Antimicrobial 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.
AID508755Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID416757Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID1275545Antiviral 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 assay2016European journal of medicinal chemistry, Feb-15, Volume: 109Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
AID614140Cytotoxicity against human MT4 cells after 4 days by MTT assay2011Bioorganic & 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.
AID1741395Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID279440Antiviral activity against HIV1 isolate with RT 101R, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID82605The effect of protein binding on the antiviral activity versus wild type virus strain HXB2 was tested in the presence of human serum in HeLa MAGI assay2004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID257173Cytotoxicity against MT4 cells by MTT method2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID1197834Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant2015European journal of medicinal chemistry, Mar-06, Volume: 92Fused 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.
AID363037Cytotoxicity against human MT4 cells after 4 days by MTT assay2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
AID105202Antiviral activity against MT-4 cells infected with Nev-R strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1059143Cytotoxicity against human MT4 cells after 5 days by MTT assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID198074Inhibitory activity against HIV-1 Mutant Reverse transcriptase K103N1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID736041Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1483279Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells2017Journal 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.
AID1520066Inhibition 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 analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID83550Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn2004Journal 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
AID508780Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1060625Inhibition of wild-type HIV1 reverse transcriptase assessed as incorporation of biotin-labeled dUTP2014Bioorganic & 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.
AID1141964Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death measured after 5 days of infection by MTT method2014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1880373Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID613673Induction of apoptosis in human A375 cells seeded as high density at 20 uM after 96 hrs by DAPI staining-based FACS analysis2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID443751Toxicity in African green monkey Vero cells2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
AID693586Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID1815397Inhibition of HIV1 reverse transcriptase L100I mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis2021European journal of medicinal chemistry, Dec-15, Volume: 226Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel.
AID1373160Inhibition of reverse transcriptase Y188L mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay2018Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
Structural optimization of N
AID279429Antiviral activity against HIV1 isolate with RT 103N, 106M mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID561939Antiviral activity against HIV infected in human PBMC assessed as decrease in viral p24 antigen production at 0.25 to 4 ug/ml after 14 days by ELISA2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID198257Inhibitory concentration against mutant reverse transcriptase of E138K was determined which is in turn resistant to TSAO1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID279435Antiviral activity against HIV1 isolate with RT 101Q, 103R mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID155272Ability to inhibit the replication of HTLV IIIb strain of HIV-1 p24 antigen production in PBMC1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID1185990Antiviral activity against wild type HIV1 infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1171414Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID1457064Inhibition 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 2017Journal 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.
AID557046Antiviral activity against HIV1 clade C harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
AID476473Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase K103N/Y181C mutation by MTT assay2010Bioorganic & 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.
AID198916Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y188L2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID199102Inhibitory concentration against wild-type reverse transcriptase of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1292010Antiviral 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 assay2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID318125Cytotoxicity against human MT4 cells2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID152659Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17.1999Bioorganic & medicinal chemistry letters, Jun-07, Volume: 9, Issue:11
Rational design of N-[2-(2,5-dimethoxyphenylethyl)]-N'-[2-(5-bromopyridyl)]-thiourea (HI-236) as a potent non-nucleoside inhibitor of drug-resistant human immunodeficiency virus.
AID246349Effective concentration against human immunodeficiency virus type 1 mutated at 103N2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
AID508773Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181V mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID235889Ratio of effective concentration to that of cytotoxic concentration against HIV-1 induced cytopathogenicity in MT-4 cells1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2'-5'-bis-O-(tert-butyldimethylsilyl)-beta-D-xylo- and -ribofuranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID269686Antiviral activity against HIV1 NNTRI resistant Y188L mutant2006Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID698303Cytotoxicity against mock-infected human MT4 cells measured after 5 days by MTT assay2012Journal 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.
AID279393Antiviral activity against HIV1 isolate with RT 106I mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1335203Ratio of IC50 for HIV-1 NL4-3 harboring RT-K103N/P225H double mutant infected in HEK293T cells co-expressing vesicular stomatitis virus glycoprotein to IC50 for wild-type HIV-1 NL4-3 infected in HEK293T cells co-expressing vesicular stomatitis virus glyco2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID561950Antibacterial activity against Salmonella group D after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID318124Cytotoxicity against human CEM-SS cells2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID1572524Antiviral 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
AID1072803Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay2014Bioorganic & 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.
AID781021Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.
AID248648Inhibitory concentration against wild type human immunodeficiency virus type 1 was determined by recombinant virus assay2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 2.
AID46379Antiviral activity against site directed resistant isolate HIV-1 L74V in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1460945Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 harboring reverse transcriptase E138A mutant infected in MAGI-CCR5 cells2017Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23
An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors.
AID1186688Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells2014European journal of medicinal chemistry, Oct-06, Volume: 85Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
AID1483284Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B2017Journal 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.
AID571970Antiviral activity against HIV-1 subtype CRF02_AG V022830 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID496631Antiviral 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 control2010Antimicrobial 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.
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AID482698Antiviral activity against HIV S067 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
AID613681Antiproliferative activity against human A375 cells at 350 uM after 96 hrs by trypan blue assay2011Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16
Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors.
AID246362Effective concentration against rhuman immunodeficiency virus type 1 K103N and Y181C mutant strains2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine).
AID1377176Antiviral activity against HIV1 isolate LAV infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA2017Journal of natural products, 06-23, Volume: 80, Issue:6
Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa.
AID317728Inhibition of HIV1 reverse transcriptase2008Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
AID571982Antiviral activity against HIV-1 subtype B V022814 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID630952Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 subtype B-3B2011Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22
Lead optimization at C-2 and N-3 positions of thiazolidin-4-ones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1811038Inhibition 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 spectrofluorometer2021Journal 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.
AID431619Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID440672Antiviral activity against HIV1 EFV with reverse transcriptase K103R, V179D, P225H mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID83553Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala2004Journal 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
AID279422Antiviral activity against HIV1 isolate with RT 190E mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID476471Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase Y181C mutation by MTT assay2010Bioorganic & 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.
AID246299Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells2005Journal 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.
AID348904Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as virus-induced cell death by MTT method2008Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21
Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies.
AID257164Inhibition of K103N mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation2005Journal of medicinal chemistry, Dec-15, Volume: 48, Issue:25
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
AID391990Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID1322997Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells.
AID1485975Inhibition of HIV-1 reverse transcriptase G190A mutant assessed as reduction in dTTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 mins by PicoGreen dye based spectrofluorometric analysis2017Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14
Searching for novel N
AID302261Inhibition of HIV1 reverse transcriptase L100I mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1191972Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay2015Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6
Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity.
AID1126509Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8
Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1610040Antiviral activity against HIV1 N119 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay2019European journal of medicinal chemistry, Dec-01, Volume: 183Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives.
AID698305Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay2012Journal 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.
AID1191670Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
AID734262Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for Human immunodeficiency virus 1 A17 infected in human TZM-bl cells2013Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
Novel pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
AID1558854Antiviral 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 assay2019Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles.
AID492046Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
AID1141969Ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV1 NL4.32014European journal of medicinal chemistry, Jun-10, Volume: 80New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID1743635Resistance 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 cells2020European journal of medicinal chemistry, Nov-15, Volume: 206Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
AID766431Cytotoxicity against human MT2 cells by MTT assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility.
AID508790Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1190617Inhibition of HIV-1 reverse transcriptase using digoxigenin/biotin-labeled dUTP as substrate at 100 ug/ml incubated for 1 hr followed by compound washout measured after 1 hr by non-radioactive ELISA relative to control2015Bioorganic & medicinal chemistry letters, Feb-15, Volume: 25, Issue:4
Dithiocarbamate-thiourea hybrids useful as vaginal microbicides also show reverse transcriptase inhibition: design, synthesis, docking and pharmacokinetic studies.
AID587739Cytotoxicity against human HeLaT4 cells by WST-1 assay2011Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1
Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity.
AID391993Cytotoxicity against human CEM cells by MTT assay2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
AID430057Selectivity index, CC50 for human MT4 cells to EC50 for HIV1 3B2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
AID106774Cell culture inhibitory concentration against spread of HIV-I infection in MT-4 cells was determined1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
AID361904Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/L100I mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID416758Antiviral activity against HIV1 with reverse transcriptase Y181I mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID1357800Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant2018European journal of medicinal chemistry, May-10, Volume: 151Targeting 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.
AID663296Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay2012Journal of medicinal chemistry, Apr-12, Volume: 55, Issue:7
2-(Alkyl/aryl)amino-6-benzylpyrimidin-4(3H)-ones as inhibitors of wild-type and mutant HIV-1: enantioselectivity studies.
AID1520059Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay2020European journal of medicinal chemistry, Jan-01, Volume: 185Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors.
AID46382Antiviral activity against site directed resistant isolate HIV-1 Y181C in CEM cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
AID1761014Antiviral 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 assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase.
AID1888690Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID1741394Inhibition 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 assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
AID263513Antiviral activity against HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Apr-15, Volume: 16, Issue:8
Design, synthesis, and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part 2.
AID440639Antiviral activity against NNRTI-resistant HIV1 NL4-3 with reverse transcriptase Y181C mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
AID440669Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Activity and molecular modeling of a new small molecule active against NNRTI-resistant HIV-1 mutants.
AID1171412Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay2014ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11
Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers.
AID619631Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2011European 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.
AID1292012Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2016European journal of medicinal chemistry, Jun-10, Volume: 115Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
AID571979Antiviral activity against HIV-1 subtype B V022811 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID590348Inhibition of Human immunodeficiency virus 1 NL4.3 reverse transcriptase activity at 0.1 ug/ml2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Synthesis of 9-substituted derivatives of berberine as anti-HIV agents.
AID736038Inhibition of HIV1 reverse transcriptase p66/p51 K103N/Y181C mutant after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1880380Antiviral activity against HIV-1 IIIB harboring reverse transcriptase E138K mutant infected in human MT4 cells by MTT assay2022Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
Structure-Based Discovery of Novel NH
AID1654197Plasma concentration in human2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID299031Antiviral activity against HIV1 with reverse transcriptase Y188H mutation in CEM cells assessed as inhibition of virus-induced giant cell formation2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
AID1155807Antiviral activity against HIV-1 harboring NNTRI-resistant reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID318127Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis2008Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
AID279421Antiviral activity against HIV1 isolate with RT 101E, 190S mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1390714Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant2018Bioorganic & 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.
AID105000Inhibitory concentration which prevents the spread of HIV-1 IIIB infection in MT2 T-lymphoid cells1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID607876Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type Human immunodeficieny virus 1 3B infected in human MT4 cells2011Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID361918Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K101E mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID779526Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay2013Bioorganic & 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.
AID197948In vitro inhibitory concentration against HIV-1 reverse transcriptase using rC-dG template primer1993Journal of medicinal chemistry, Jan-22, Volume: 36, Issue:2
Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.
AID248012In vitro inhibitory concentration against HIV LAI cell line2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1308895Inhibition of HIV reverse transcriptase transfected in HEK293T cells assessed as reduction in viral replication measured at 48 hrs postinfection by luciferase reporter based single-cycle non replicative phenotypic assay2016Bioorganic & medicinal chemistry letters, Aug-01, Volume: 26, Issue:15
Application of the Huisgen cycloaddition and 'click' reaction toward various 1,2,3-triazoles as HIV non-nucleoside reverse transcriptase inhibitors.
AID1654200Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as Cytochrome P450-mediated formation of 3-OHNVP at 10 uM incubated for 24 hrs by uHPLC-MS analysis2020Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12
Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death.
AID508633Cytotoxicity against human MT4 cells by cell based assay2010Antimicrobial 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.
AID241996Concentration required for 50% inhibition of human immunodeficiency virus type 1 reverse transcriptase Ile1002004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID267651Selectivity for wild type HIV1 virus over HIV1 K103N mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID391680Selectivity index, ratio of inhibition of DNA dependent DNA polymerase activity of Escherichia coli DNA polymerase 1 Klenow fragment to inhibition of DNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p512008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Virtual screening, identification, and biochemical characterization of novel inhibitors of the reverse transcriptase of human immunodeficiency virus type-1.
AID157558Cytotoxic concentration was evaluated using microculture tetrazolium assay (MTA)1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID1637403Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring E138K mutant infected in human MT4 cells2016Bioorganic & 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.
AID1888699Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID279471Antiviral activity against HIV1 isolate with RT 103N, 238N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1155815Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:12014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Exploring the role of 2-chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes.
AID1888695Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay
AID496629Antiviral 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 control2010Antimicrobial 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.
AID561942Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
AID361926Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A/Y181C mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID573469Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay2009Antimicrobial 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.
AID279399Antiviral activity against HIV1 isolate with RT 179D mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID1335216Antiviral activity against HIV-1 NL4-3 harboring RT-K103N mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase reporter gene2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID1784215Antiviral 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 assay2021European journal of medicinal chemistry, Dec-05, Volume: 225Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors.
AID247500Inhibitory activity against HIV-1 mutant strain 179E2004Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
AID1379962Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay2017European journal of medicinal chemistry, Nov-10, Volume: 140Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs.
AID302265Inhibition of HIV1 reverse transcriptase Y188L mutant2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1187999Antiviral activity against HIV1 3B acutely infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect after 5 days by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands.
AID1572519Antiviral 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
AID105697Anti-HIV-1 activity against K103N+K1001 strain was determined2003Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24
3-iodo-4-phenoxypyridinones (IOPY's), a new family of highly potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1884487Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID1069709Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days2014Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4
Design and synthesis of N₁-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID508756Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1320863Antiviral 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 assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket.
AID1487264Inhibition 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 control2017Bioorganic & 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.
AID1882470Antiviral activity against HIV-1 harboring K103N/Y181C mutant infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay2022Journal 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.
AID198917Inhibition of HIV-1 wild-type RT2001Journal of medicinal chemistry, Feb-01, Volume: 44, Issue:3
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent.
AID294633Inhibition of HIV1 reverse transcriptase using Poly rC.dG template2007European journal of medicinal chemistry, Jul, Volume: 42, Issue:7
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
AID328842Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Inhibition of MRP1/ABCC1, MRP2/ABCC2, and MRP3/ABCC3 by nucleoside, nucleotide, and non-nucleoside reverse transcriptase inhibitors.
AID1335208Antiviral activity against HIV-1 NL4-3 harboring RT-K103N/Y181C double mutant infected in HEK293T cells coexpressing vesicular stomatitis virus glycoprotein pretreated with cells for 15 mins followed by viral infection measured after 48 hrs by luciferase 2016European journal of medicinal chemistry, Nov-10, Volume: 1232,4,5-Trisubstituted thiazole derivatives as HIV-1 NNRTIs effective on both wild-type and mutant HIV-1 reverse transcriptase: Optimization of the substitution of positions 4 and 5.
AID293556Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay2007European journal of medicinal chemistry, May, Volume: 42, Issue:5
Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
AID492284Antiviral activity against HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay2010Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
AID632796Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection2011Journal 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.
AID248258In vitro inhibitory concentration against HIV G190S mutant strain2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains.
AID1152374Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
AID105127Compound was evaluated for the inhibition of HIV-1 induced CPE (HTLV-III B strain ) replication in MT-4 cells1995Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
AID725389Antiviral activity against HIV1 LAI infected in CEMx174-LTR-GFP cells assessed as inhibition of viral replication after 5 days by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors.
AID1316329Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA2016Journal 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.
AID1884490Antiviral 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 assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase.
AID267653Selectivity for wild type HIV1 virus over HIV1 L100I mutant2006Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
AID82141Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected K103N strain2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
AID302256Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT K103N mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
AID1627028Cytotoxicity against HIV1 infected African green monkey Vero cells assessed as reduction in cell viability after 7 days by MTT assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID572173Antiviral activity against HIV-1 subtype CRF05_DF V022824 harboring NNRTI V106I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Inhibition of human immunodeficiency virus type 1 infection by the candidate microbicide dapivirine, a nonnucleoside reverse transcriptase inhibitor.
AID1241796Selectivity index, ratio of IC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase.
AID1443667Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors.
AID1185991Cytotoxicity against HEK293T cells at 10 uM after 48 hrs2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID88369Antiviral activity against K103N/V108I mutant virus in the HeLa MAGI assay.2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID736440Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting2013Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
AID1152239Antiviral activity against X4 tropic Human immunodeficiency virus 1 3B subtype B infected in human TZM-bl cells assessed as reduction in virus-induced cytopathic effect after 48 hrs by luminescence assay2014Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12
Rational design and synthesis of novel thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID718366Inhibition of HIV1 recombinant reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rC)-oligo(dG) by colorimetric analysis2012Bioorganic & medicinal chemistry, Dec-01, Volume: 20, Issue:23
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
AID105203Antiviral activity against MT-4 cells infected with wild-type HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID1186001Antiviral activity against HIV1 harboring reverse transcriptase K103N/P225H double mutant infected in HEK293T cells transfected with plasmid VSV-G/pNL4-3.luc.R-E- assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay r2014European journal of medicinal chemistry, Oct-06, Volume: 852,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase.
AID1736358Antiviral activity against VSVG/HIV-1 harboring reverse transcriptase L100I/K103N double mutant infected in human HEK 293T cells assessed as inhibition of virus replication preincubated with cells for 15 mins prior to viral infection and measured at 48 hr
AID518737Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay2010Antimicrobial 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.
AID366527Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile.
AID1731746Inhibition 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
AID416756Antiviral activity against HIV1 with reverse transcriptase K103N mutation in human CEM cells assessed as protection against virus-induced cytopathicity2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
AID259755Cytotoxicity against MT2 cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID592539Selectivity index, CC50 for human CEM cells to IC50 for HIV1 3B2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
AID666415Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 SF332012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Design, synthesis, and biological evaluation of 1-[(2-benzyloxyl/alkoxyl)methyl]-5-halo-6-aryluracils as potent HIV-1 non-nucleoside reverse transcriptase inhibitors with an improved drug resistance profile.
AID1200846Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells2015European journal of medicinal chemistry, Mar-26, Volume: 93Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines.
AID279407Antiviral activity against HIV1 isolate with RT 98G, 103N mutation relative to wild type2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
A novel nonnucleoside analogue that inhibits human immunodeficiency virus type 1 isolates resistant to current nonnucleoside reverse transcriptase inhibitors.
AID155133Ability to inhibit the replication of A17 (Y181C) strain of HIV-1 p24 antigen production in PBMC1999Bioorganic & medicinal chemistry letters, Dec-20, Volume: 9, Issue:24
N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1.
AID82457Antiviral activity against G190A strain of HIV-12004Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
AID232779Selectivity index was defined as the ratio of CC50 to EC501992Journal of medicinal chemistry, Aug-07, Volume: 35, Issue:16
TSAO analogues. Stereospecific synthesis and anti-HIV-1 activity of 1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro -5''- (4''-amino-1'',2''-oxathiole 2'',2''-dioxide) pyrimidine and pyrimidine-modified nucleosides.
AID1627030Antiviral activity against HIV-1 LAI infected in human PBM cells after 7 days2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1574372Antiviral 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 assay2019Journal 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.
AID606672Inhibition of HIV1 reverse transcriptase K103N mutant2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants.
AID1175920Antiviral activity against VSV-G protein pseudotyped HIV1 system in HEK293T cells assessed as reduction in p24 level after 48 hrs by ELISA2014Journal of natural products, Dec-26, Volume: 77, Issue:12
Diterpenes from a Chinese collection of the brown alga Dictyota plectens.
AID508645Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID1304404Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human CEM-SS cells to EC50 for antiviral activity against HIV-1 RF2016Bioorganic & 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.
AID508784Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B2010Antimicrobial 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.
AID518741Antiviral 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 assay2010Antimicrobial 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.
AID361913Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190S mutant in HeLa cells by MAGI assay2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Structural basis for the improved drug resistance profile of new generation benzophenone non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1795346HIV-1 RT Assay from Article 10.1021/jm00025a010: \\Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.\\1995Journal of medicinal chemistry, Dec-08, Volume: 38, Issue:25
Phenethylthiazolethiourea (PETT) compounds, a new class of HIV-1 reverse transcriptase inhibitors. 1. Synthesis and basic structure-activity relationship studies of PETT analogs.
AID1803151HIV-1 RT Activity Assay from Article 10.3109/14756366.2011.636362: \\Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.\\2013Journal of enzyme inhibition and medicinal chemistry, Feb, Volume: 28, Issue:1
Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.
AID1802330HIV-1 RT Inhibitory Assay from Article 10.1021/acs.biochem.6b00943: \\Physiological Mg(2+) Conditions Significantly Alter the Inhibition of HIV-1 and HIV-2 Reverse Transcriptases by Nucleoside and Non-Nucleoside Inhibitors in Vitro.\\
AID1795390HIV-1 RT Assay from Article 10.1021/jm960802y: \\Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.\\1997Journal of medicinal chemistry, May-09, Volume: 40, Issue:10
Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series.
AID1796846HIV-1 RT Assay. from Article 10.1021/jm040071z: \\Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.\\2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved drug resistance properties. 1.
AID1795386HIV-1 RT Assay from Article 10.1021/jm980260f: \\5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.\\1999Journal of medicinal chemistry, Feb-25, Volume: 42, Issue:4
5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3, 4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives.
AID1797479HIV-1 RT Assay from Article 10.1021/jm0613121: \\De Novo Parallel Design, Synthesis and Evaluation of Inhibitors against the Reverse Transcriptase of Human Immunodeficiency Virus Type-1 and Drug-Resi\\2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
De novo parallel design, synthesis and evaluation of inhibitors against the reverse transcriptase of human immunodeficiency virus type-1 and drug-resistant variants.
AID1795327HIV-1 RT Assay from Article 10.1021/jm00024a011: \\Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.\\1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 5. 4-Substituted and 2,4-disubstituted analogs of nevirapine.
AID1798816Reverse Transcriptase Assay from Article 10.1021/jm801395v: \\Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations.\\2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations.
AID1795322HIV-1 RT Assay from Article 10.1021/jm00024a010: \\Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 rev1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. 4. 2-Substituted dipyridodiazepinones as potent inhibitors of both wild-type and cysteine-181 HIV-1 reverse transcriptase enzymes.
AID1795349HIV-1 RT Assay from Article 10.1021/jm960158n: \\Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.\\1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Targeting delavirdine/atevirdine resistant HIV-1: identification of (alkylamino)piperidine-containing bis(heteroaryl)piperazines as broad spectrum HIV-1 reverse transcriptase inhibitors.
AID1795423HIV-1 RT Assay from Article 10.1021/jm990095j: \\Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.\\1999Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
AID1796564HIV-1 RT Assay from Article 10.1021/jm0009437: \\Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.\\2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
Synthesis and antiviral activity of 4-benzyl pyridinone derivatives as potent and selective non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
AID1795743HIV-1 RT Assay from Article 10.1016/j.bmc.2004.08.050: \\Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.\\2004Bioorganic & medicinal chemistry, Dec-01, Volume: 12, Issue:23
Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides.
AID1799587In Vitro Enzyme Assay from Article 10.1111/j.1747-0285.2009.00852.x: \\In silico screening for non-nucleoside HIV-1 reverse transcriptase inhibitors using physicochemical filters and high-throughput docking followed by in vitro evaluation.\\2009Chemical biology & drug design, Sep, Volume: 74, Issue:3
In silico screening for non-nucleoside HIV-1 reverse transcriptase inhibitors using physicochemical filters and high-throughput docking followed by in vitro evaluation.
AID1795381HIV-1 RT Assay from Article 10.1021/jm00061a022: \\5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.\\1993Journal of medicinal chemistry, Apr-30, Volume: 36, Issue:9
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.
AID1795395HIV-1 RT Assay from Article 10.1021/jm0211063: \\Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.\\2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.
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Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.
AID1795385HIV RT Assay from Article 10.1021/jm950568w: \\2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.\\1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
2-Sulfonyl-4-chloroanilino moiety: a potent pharmacophore for the anti-human immunodeficiency virus type 1 activity of pyrrolyl aryl sulfones.
AID1795367HIV-1 RT Assay from Article 10.1021/jm950639r: \\Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.\\1996Journal of medicinal chemistry, Oct-11, Volume: 39, Issue:21
Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs.
AID1795311HIV-1 RT Assay from Article 10.1021/jm00069a011: \\Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.\\1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Selective non-nucleoside HIV-1 reverse transcriptase inhibitors. New 2,3-dihydrothiazolo[2,3-a]isoindol-5(9bH)-ones and related compounds with anti-HIV-1 activity.
AID1795355HIV-1 RT Assay from Article 10.1021/jm9707030: \\Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones\\1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones.
AID1795358HIV-1 RT Assay from Article 10.1021/jm9707028: \\Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.\\1998Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
AID1802585RT Assay from Article 10.1016/j.bioorg.2017.01.006: \\Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.\\2017Bioorganic chemistry, 02, Volume: 70Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
AID1801807HIV-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.\\2016Chemical 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.
AID1795433HIV-1 RT Assay from Article 10.1021/jm990580e: \\Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.\\2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
AID1795382HIV-1 RT Assay from Article 10.1021/jm00062a027: \\Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-c1993Journal of medicinal chemistry, May-14, Volume: 36, Issue:10
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]pi
AID1795384HIV-1 RT Assay from Article 10.1021/jm010853h: \\Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibit2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
Structure-based design, synthesis, and biological evaluation of conformationally restricted novel 2-alkylthio-6-[1-(2,6-difluorophenyl)alkyl]-3,4-dihydro-5-alkylpyrimidin-4(3H)-ones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID1795394HIV-1 RT Assay from Article 10.1016/0968-0896(96)00075-2: \\5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors.\\1996Bioorganic & medicinal chemistry, Jun, Volume: 4, Issue:6
5H-pyrrolo[1,2-b] [1,2,5]benzothiadiazepines (PBTDs): a novel class of non-nucleoside reverse transcriptase inhibitors.
AID1795388HIV-1 RT Assay from Article 10.1021/jm9901125: \\Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.\\2000Journal of medicinal chemistry, May-04, Volume: 43, Issue:9
Structure-based design, synthesis, and biological evaluation of novel pyrrolyl aryl sulfones: HIV-1 non-nucleoside reverse transcriptase inhibitors active at nanomolar concentrations.
AID1801345In 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.\\2015Chemical 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.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2006The FEBS journal, Aug, Volume: 273, Issue:16
Structural insights into mechanisms of non-nucleoside drug resistance for HIV-1 reverse transcriptases mutated at codons 101 or 138.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB1995Nature structural biology, Apr, Volume: 2, Issue:4
High resolution structures of HIV-1 RT from four RT-inhibitor complexes.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,035)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's357 (11.76)18.2507
2000's1377 (45.37)29.6817
2010's1158 (38.15)24.3611
2020's143 (4.71)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 63.20

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index63.20 (24.57)
Research Supply Index8.22 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index111.80 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (63.20)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials509 (15.85%)5.53%
Reviews202 (6.29%)6.00%
Case Studies162 (5.04%)4.05%
Observational32 (1.00%)0.25%
Other2,307 (71.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (169)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase II, Parallel, Randomized, Clinical Trials Comparing the Responses to Initiation of NNRTI-Based Versus PI-Based Antiretroviral Therapy in HIV Infected Infants Who Have and Have Not Previously Received Single Dose Nevirapine for Prevention of Mother-t [NCT00307151]Phase 2452 participants (Actual)Interventional2005-12-31Completed
Clinical Trial of CNS Penetrating ART to Prevent NeuroAIDS in China [NCT01340950]Phase 4250 participants (Actual)Interventional2010-07-31Completed
Phase 2 Comparison of Low-Dose Naltrexone vs ARV Effectiveness in HIV+ Progression [NCT01174914]Phase 2171 participants (Actual)Interventional2008-03-31Completed
Optimal Combination Therapy After Nevirapine Exposure [NCT00089505]Phase 3745 participants (Actual)Interventional2006-11-30Completed
NEVIRAPINE Plus LAMIVUDINE (3TC) for HIV Maintenance Therapy - A Single Center Pilot Study [NCT03223402]20 participants (Actual)Interventional2016-12-23Completed
Efficacy of Rilpivirine-based Regimens as Switch Therapy From Nevirapine-based Regimens in HIV-infected Patients With Complete Virological Suppression: A Randomized Controlled Trial [NCT03664440]106 participants (Actual)Interventional2016-12-01Completed
"Safeguard the Household - A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country" [NCT00255840]812 participants (Actual)Interventional2006-07-31Completed
Randomized, Open Label Study Evaluating the Lipid Profile Difference and Efficacy of a Combined Therapy Including Tenofovir, Emtricitabine + Atazanavir / r or NVP in Naive HIV - 1 Infected Patients. [NCT00389207]Phase 3576 participants (Actual)Interventional2006-10-31Completed
Maintaining Options for Mothers Study (MOMS): A Phase II Randomized Comparison of Three Antiretroviral Strategies Administered for 7 or 21 Days to Reduce the Emergence of Nevirapine Resistant HIV-1 Following a Single Intrapartum Dose of Nevirapine [NCT00099632]Phase 2484 participants (Actual)Interventional2006-03-31Completed
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (VIRAMUNE® ) and Ethinyl Estradiol/Norethindrone [ORTHO-NOVUM® 1/35 (21 Pack)] in HIV-1 Infected Women [NCT02182791]Phase 114 participants (Actual)Interventional1998-04-30Completed
A Prospective Randomised Open Label Clinical Trial to Determine the Efficacy of Nevirapine, Compared With a Combination of ZDV + 3TC, in Decreasing the Peripartum Mother to Child Transmission of HIV. Women, Who Present After 38 Weeks Gestation or in Labou [NCT02181933]Phase 32,648 participants (Actual)Interventional1999-04-30Completed
Steady State Bioavailability of 2 Different Nevirapine Extended Release Formulations Compared to Steady State 400 mg of Viramune® (200 mg BID), in HIV-1 Infected Subjects, an Open Label, Non Randomised, Multidose and Multistage Parallel Group Study. (ERVI [NCT02194179]Phase 192 participants (Actual)Interventional2006-12-31Completed
Clinical and Therapeutic Evaluation of the Infection by HIV/AIDS [NCT02191215]442 participants (Actual)Observational2003-06-30Completed
Long-term Observational Study in Patients Under Anti-retroviral Combination Therapy Who Were Switched From Protease Inhibitors or Other NNRTI to Viramune® Plus Two Nucleoside Reverse Transcriptase Inhibitors (NRTI) for Reasons of Therapy. (Long-Term Switc [NCT02191293]228 participants (Actual)Observational2002-05-31Completed
Relative Bioavailability of Different Oral Viramune Extended Release Formulations Containing 300 mg or 400 mg Compared to 200 mg or 400 mg as One or Two 200 mg IR Tablets Following Administration in Healthy Male Volunteers - an Openlabel, Non-randomized, [NCT02192463]Phase 1204 participants (Actual)Interventional2006-04-30Completed
PI or NNRTI as First-line Treatment of HIV in a West African Population With Low Adherence - the PIONA Trial [NCT01192035]Phase 4400 participants (Actual)Interventional2011-05-31Completed
Intensive Pharmacokinetic Studies of Antiretroviral Drug Combinations in Children [NCT00260078]Phase 1/Phase 275 participants (Actual)Interventional2006-02-28Completed
Phase II Study of the Pharmacokinetics of Nevirapine and the Incidence of Nevirapine Resistance Mutations in HIV-Infected Women Receiving a Single Intrapartum Dose of Nevirapine With the Concomitant Administration of Zidovudine/Didanosine or Zidovudine/Di [NCT00109590]Phase 2175 participants (Actual)Interventional2006-06-30Completed
A Phase III, Randomized, Open-Label Trial to Evaluate Strategies for Providing Antiretroviral Therapy to Infants Shortly After Primary Infection in a Resource Poor Setting [NCT00102960]Phase 3377 participants (Actual)Interventional2005-07-31Completed
An Open-label Study in HIV+ Patients to Determine the Effects of Nevirapine (VIRAMUNE®) on the Steady State Pharmacokinetics of Rifabutin (MYCOBUTIN®) [NCT02184078]Phase 419 participants (Actual)Interventional1998-10-31Completed
An Open-label, Non-randomised, Single-dose, Parallel-group Study of Pharmacokinetic Properties of 200 mg (2 x 100 mg Tablets Once Daily) and 300 mg (3 x 100 mg Tablets Once Daily) Nevirapine Extended Release Formulations Compared to 200 mg VIRAMUNE® Table [NCT02184312]Phase 196 participants (Actual)Interventional2008-04-30Completed
Collecting Data in Patients With HIV Infection Type 1 After Switching From a Protease Inhibitor-containing Therapy Regimen and a Viral Load Below Detection Level to a Viramune®-Containing Therapy Regimen [NCT02191332]147 participants (Actual)Observational1999-12-31Completed
An Open-label, Randomised, Single Dose, Parallel-group Phase I Study to Investigate the Pharmacokinetic Properties of 200 mg Nevirapine Extended Release Tablets When Administered Orally as 2x100 mg Tablets or as 4x50 mg Tablets in Healthy Male Volunteers [NCT02194218]Phase 148 participants (Actual)Interventional2009-09-30Completed
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (VIRAMUNE®) and Saquinavir-sgc (Fortovase®) in HIV-1 Infected Patients [NCT02184286]Phase 15 participants (Actual)Interventional1999-05-31Terminated
An Open-label Study in HIV+ Patients to Determine the Effects of Nevirapine (VIRAMUNE®) on the Steady State Pharmacokinetics of Fluconazole (DIFLUCAN®) [NCT02181946]Phase 424 participants (Actual)Interventional2001-05-31Completed
Phase III Randomized Trial of the Safety and Efficacy of Three Neonatal Antiretroviral Regimens for Prevention of Intrapartum HIV-1 Transmission [NCT00099359]Phase 31,735 participants (Actual)Interventional2004-02-29Completed
Role of Pharmacogenetics in Efavirenz and Nevirapine Pharmacokinetics, Efficacy and Safety in Mother-infant Pairs During Pregnancy and Lactation [NCT02269462]460 participants (Actual)Observational2012-12-31Completed
A Phase I/II Comparative Pharmacokinetic Study of the Fixed-Dose Combination (FDC) of Zidovudine (ZDV), Lamivudine (3TC), and Nevirapine (NVP) as GPO-Vir Z30 Pediatric Tablets Versus the Individual Liquid Formulations in HIV-Infected Children Greater Than [NCT00672412]Phase 1/Phase 242 participants (Actual)Interventional2008-10-31Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
A Randomized Open Label Trial of HIV Protease Inhibitors for the Prevention of Malaria in HIV-Infected Children [NCT00978068]Phase 3176 participants (Actual)Interventional2009-09-30Completed
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in South Africa: A Phase II Trial [NCT00640887]Phase 248 participants (Anticipated)Interventional2009-02-28Completed
A Multicenter, Randomized, Open-label, Controlled Study of Nevirapine (VIRAMUNE®) and a Short Course of Prednisone to Determine the Safety and Effectiveness of This Strategy in Preventing Nevirapine (VIRAMUNE®) Associated Rash. [NCT02184299]Phase 4138 participants (Actual)Interventional1999-04-30Completed
Observational Study With Antiretroviral Treated Patients Switching Therapy Because of Therapeutic Reasons From Protease Inhibitor- or NNRTI-containing Regimens to Nevirapine Plus Two Nucleoside Reverse Transcriptase Inhibitor (NRTI) Regimens [NCT02191319]55 participants (Actual)Observational2002-01-31Completed
A Phase I/II Comparative Pharmacokinetic Study of the Fixed-Dose Combination (FDC) of Stavudine (d4T), Lamivudine (3TC), and Nevirapine (NVP) as GPO-VIR Pediatric Chewable Tablets Versus the Individual Liquid Formulations in HIV Infected Children 6 Months [NCT00312091]Phase 1/Phase 244 participants (Actual)Interventional2006-12-31Completed
Pharmacokinetic Evaluation of Changes in Nevirapine AUC Due to Differences in Weight [NCT01335360]21 participants (Actual)Observational2003-05-31Completed
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (VIRAMUNE®), Abacavir and Amprenavir in HIV-1 Infected NNRTI Naive Adults [NCT02182765]Phase 18 participants (Actual)Interventional1999-04-30Terminated
An Open-Label, Single Dose Study to Evaluate the Effects of Underlying Renal or Hepatic Dysfunction on the Pharmacokinetics of Nevirapine (VIRAMUNE®) [NCT02184091]Phase 141 participants (Actual)Interventional1999-01-31Completed
A Single-dose, 2-part, Open-label, Randomised, Pharmacoscintigraphic Investigation Into the Absorption of Nevirapine When Released Into Different Parts of the Gastro-intestinal Tract [NCT02191189]Phase 127 participants (Actual)Interventional2005-05-31Completed
Genetic Determinants of the Metabolism of Non-nucleoside Reverse Transcriptase Inhibitors [NCT00730223]Phase 133 participants (Actual)Interventional2004-03-31Completed
A Randomized Trial to Evaluate the Effectiveness of Antiretroviral Therapy Plus HIV Primary Care Versus HIV Primary Care Alone to Prevent the Sexual Transmission of HIV-1 in Serodiscordant Couples [NCT00074581]Phase 33,526 participants (Actual)Interventional2005-02-28Completed
A Randomised, Double Blind, Double Dummy, Parallel Group, Active Controlled Trial to Evaluate the Antiviral Efficacy of 400 mg QD neVirapine Extended Release Formulation in Comparison to 200 mg BID neVirapinE Immediate Release in Combination With Truvada® [NCT00561925]Phase 31,068 participants (Actual)Interventional2007-11-30Completed
An Open-label, Multiple Dose, Cross-over Study to Evaluate the Steady-state Pharmacokinetic Parameters of Nevirapine Extended Release Tablets in HIV-1 Infected Children, With an Optional Extension Phase [NCT00905489]Phase 185 participants (Actual)Interventional2009-06-30Completed
[NCT00618176]Phase 4198 participants (Actual)Interventional2005-01-31Completed
Pharmacokinetic Interaction Between Coartem® and Either Nevirapine, Efavirenz or Rifampicin in HIV Positive Ugandan Patients [NCT00620438]Phase 490 participants (Anticipated)Interventional2008-02-29Active, not recruiting
A Phase I, Open-label, Single-sequence Drug-drug Interaction Trial to Investigate the Pharmacokinetic Interaction Between Steady-state Nevirapine and Single-dose TMC207 in HIV-1 Infected Subjects. [NCT00910806]Phase 116 participants (Actual)Interventional2009-06-30Completed
A Phase III Randomized Clinical Trial of the Standard Two Dose Nevirapine (NVP) Regimen With the Addition of HIV Immune Globulin(HIVIGLOB) or Extended Infant NVP Dosing Compared With the Standard NVP Regimen Alone for the Prevention of Maternal-Infant HIV [NCT00639938]Phase 3722 participants (Actual)Interventional2004-07-31Completed
P1060 Substudy Comparing Differences in Malaria Parasitemia by Real Time Quantitative PCR in HIV-Infected Infants and Children on PI-Based HAART Versus NNRTI-Based HAART [NCT00719602]Early Phase 1105 participants (Actual)Interventional2009-08-31Completed
Randomized Multicenter Study to Compare Starting Nevirapine at the Full Dose With Dose Escalation in Patients Who Require Efavirenz to be Withdrawn Due to Adverse Reactions [NCT00704249]Phase 480 participants (Anticipated)Interventional2006-07-31Completed
Prospective, Open Label and Randomized Clinical Trial About Hepatic Security of Antiretroviral Treatment Based on Kaletra Versus Nevirapine in Co-infected HIV/HCV Patients [NCT00661349]Phase 49 participants (Actual)Interventional2008-02-29Terminated(stopped due to It has been impossible to achieve the number of patients defined by protocol)
Multicenter, Randomized, Open-Label Trial, Assessing the Efficacy of Zidovudine, Lamivudine and Nevirapine Combination Administered Twice Daily, Versus the Association of Tenofovir, Lamivudine and Nevirapine, Once Daily, in Antiretroviral Naive HIV-1 Infe [NCT00199979]Phase 3250 participants Interventional2005-04-30Recruiting
A 48 Week, Randomized, Open-label, 2 Arm Study to Compare the Efficacy, Safety and Tolerability of HAART Containing Nevirapine 400mg/Day Versus Nevirapine 600 mg/Day in HIV-1 Infected Patients Started at 2-6 Weeks After Initiating Rifampin Containing Anti [NCT00476853]Phase 242 participants (Actual)Interventional2005-10-31Completed
[NCT00523458]Phase 45 participants (Actual)Interventional2007-07-31Terminated(stopped due to A delay in protocol approval and approval of laboratory sites in Salvador, Brazil left too little time for completion of enrollment into the study.)
Phase I Three-way Crossover Bioequivalence Study of Pediatric Formulations of Lamivudine/Zidovudine/Nevirapine Using Healthy Adult Volunteers [NCT01469520]Phase 124 participants (Actual)Interventional2010-10-31Active, not recruiting
An Open Label, Phase IIIb, Randomised Parallel Group Study to Assess the Efficacy and Safety of Switching HIV-1 Infected Patients Successfully Treated With a Nevirapine IR Based Regiment to Nevirapine XR 400 mg QD or Remaining on Nevirapine IR 200 mg BID [NCT00819052]Phase 3445 participants (Actual)Interventional2008-12-31Completed
Cell Cycle Independent Antiretroviral Therapy: Combination of Nevirapine, FTC, and Tenofovir [NCT00344461]Phase 454 participants (Actual)Interventional2004-03-31Completed
Comparison of Nevirapine Levels With and Without Dose Escalation in HIV-infected Patients Commencing Antiretroviral Therapy Who Are Also Receiving Rifampicin Based Anti-tuberculous Therapy [NCT00617643]Phase 418 participants (Anticipated)Interventional2008-05-31Completed
Randomized Control Trial of Early vs Delayed ART in the Treatment of Cryptococcal Meningitis. [NCT00830856]54 participants (Actual)Interventional2006-10-31Completed
Pathogenesis of MAC Disease in Advanced HIV-1-Infected Subjects and the Impact of Highly-Active Antiretroviral Treatment (HAART) on Immune Functions Relevant for MAC and Other Opportunistic Infections [NCT00000895]85 participants InterventionalCompleted
A Randomized, Open-Label Study of the Long-Term Effectiveness of Three Initial Highly Active Antiretroviral Therapy (HAART) Strategies in HAART-Niave, HIV-Infected Persons [NCT00000922]1,710 participants InterventionalCompleted
An Open-Label, Pilot Study to Evaluate the Development of Resistance to Nevirapine (BI-RG-587) in HIV-Infected Patients With CD4 Cell Count >= 500/mm3 [NCT00000747]Phase 210 participants InterventionalCompleted
Randomized Trial of Protease Inhibitor-Including vs. Protease Inhibitor-Sparing Regimens for Women Who Initiate Therapy of HIV Infection During Pregnancy [NCT00017719]Phase 3440 participants Interventional2002-05-31Completed
Use of Combination Antiviral Therapy to Delineate the Identity and Longevity of Persistent Reservoirs of HIV-1 Infection and Replication [NCT00001644]Phase 142 participants (Actual)Interventional1997-03-03Completed
HIV Infection and Breastfeeding: Interventions for Maternal and Infant Health [NCT00164736]Phase 32,369 participants (Actual)Interventional2004-03-31Completed
A Multiple Dose, Open Label, Pivotal, 4 Period, 2 Treatment, Sequence Full Replicative Crossover Study to Assess the Bioequivalence (BE) of TEVA's Generic Once Daily Nevirapine 400 mg Prolonged Release (PR) Formulation Compared With the Approved Reference [NCT02202005]Phase 146 participants (Actual)Interventional2014-08-31Completed
Substitution by Nevirapine in HIV-1 Infected Patients on Triple Treatment of Reverse Transcriptase Nucleoside/Nucleotide Inhibitors [NCT00415090]Phase 428 participants (Actual)Interventional2004-08-31Completed
Nevirapine (NVP) Use to Prevent Maternal-Infant HIV Transmission: A Randomized Clinical Trial of Two Doses of NVP Compared to Six Weeks of NVP for the Prevention of Maternal-Infant HIV Transmission in the Breastfeeding Infant [NCT00074399]Phase 3775 participants (Actual)Interventional2001-02-28Completed
Phase 3 Randomized Trial Evaluating the Virological Efficacy and the Tolerance of 4 New Simplified Antiretroviral Treatments in Naive HIV-1 Infected Patients in Dakar and Yaounde [NCT00573001]Phase 3120 participants (Actual)Interventional2008-07-31Completed
Phase I/II Study to Assess the Safety and Plasma Concentrations of Nevirapine Given Daily, Twice a Week or Weekly as Prophylaxis in Breastfeeding Infants From Birth to 6 Months [NCT00006279]Phase 175 participants InterventionalCompleted
A Phase III Placebo-Controlled Trial to Determine the Efficacy of Oral AZT and the Efficacy of Oral Nevirapine for the Prevention of Vertical Transmission of HIV-1 Infection in Pregnant Ugandan Women and Their Neonates [NCT00006396]Phase 31,500 participants InterventionalCompleted
A Double-Blinded, Randomized Trial Comparing Zidovudine (AZT) Versus AZT Plus Didanosine (ddI) Versus AZT Plus ddI Plus Nevirapine in Asymptomatic Patients on AZT Monotherapy Who Develop a Mutation at Codon 215 of HIV Reverse Transcriptase in Serum/Plasma [NCT00001045]Phase 2300 participants InterventionalCompleted
Pharmacokinetics, Safety, Tolerance, and Activity of Nevirapine (BI-RG-587) Alone and in Combination With AZT in Mildly to Moderately Symptomatic HIV-1 Infected Children [NCT00001111]35 participants InterventionalCompleted
Treatment Outcome of Children With HIV Infection [NCT00476606]1,000 participants (Anticipated)Observational2003-03-31Active, not recruiting
Durability of Stavudine, Lamivudine and Nevirapine Among Advanced HIV-1 Infected Patients With/Without Prior Co-Administration of Rifampicin: A 144-Week Prospective Study [NCT00703898]Phase 4140 participants (Actual)Interventional2004-11-30Completed
Breastfeeding Version of the PROMISE Study (Promoting Maternal and Infant Survival Everywhere) [NCT01061151]Phase 33,747 participants (Actual)Interventional2011-03-01Completed
A Randomised Prospective Study Assessing Changes in Neurocognitive Function, Using a Computerised Test Battery, in Treatment Naïve HIV-1 Positive Subjects Commencing Two Different Antiretroviral Regimens [NCT00540137]Phase 421 participants (Actual)Interventional2007-07-31Completed
Open-Label, Multiple-Dose, Drug Interaction Study to Assess the Effect of Nevirapine on the Pharmacokinetics of Atazanavir in HIV-Infected Individuals [NCT00162149]Phase 146 participants Interventional2005-10-31Completed
Analysis of Lipodystrophy in HIV-Infected Individuals A Prospective, Non-randomised, 48 Week Study of the Effect of PI Containing and Non-PI Containing Antiretroviral Regimens on the Expression of Adipocyte Specific Genes, Protein Levels and Cellular Stru [NCT00192660]Phase 480 participants (Actual)Interventional2003-02-28Completed
Clinical Relevance of Nevirapine Resistance [NCT00117728]Phase 3250 participants (Anticipated)Interventional2005-04-30Recruiting
ART Pharmacokinetics, Mitochondrial Integrity, and Antioxidant Capacity in Severely Malnourished HIV-infected Malawian Children [NCT01529125]42 participants (Actual)Observational2011-07-31Completed
The Adult Antiretroviral Treatment and Resistance Study (Tshepo) [NCT00197613]Phase 3650 participants Interventional2002-12-31Completed
A Phase II Randomized, Multicenter Protocol Evaluating Two Antiretroviral Regimens Containing Combinations of Protease Inhibitors, NRTIs, and an NNRTI [NCT00000924]Phase 2120 participants InterventionalCompleted
A Phase II, 24-Week, Open-Label Study Designed to Evaluate the Pharmacokinetics, Safety, Tolerability, and Efficacy of Novel Combination Therapy With Videx (Didanosine), Zerit (Stavudine), Viramune (Nevirapine), and MKC-442 (With or Without Hydroxyurea) f [NCT00002418]Phase 225 participants InterventionalTerminated
Comparison of the Steady State Pharmacokinetics of Nevirapine, Stavudine Plus Lamivudine in HIV Positive Ugandan Patients Taking Triomune 40 With the Pharmacokinetics of the Originator Products. [NCT00455585]Phase 418 participants Interventional2007-01-31Completed
Efavirenz-based Versus Nevirapine-based Antiretroviral Therapy Among HIV-infected Patients Receiving Rifampin [NCT00483054]Phase 3142 participants (Actual)Interventional2007-01-31Completed
Randomized Non-inferiority Trial Comparing the Nevirapine-based Antiretroviral Therapy Versus the Standard Efavirenz-based ART for the Treatment of HIV-TB Co-infected Patients on Rifampicin-based Therapy (ANRS 12146 CARINEMO) [NCT00495326]Phase 2/Phase 3570 participants (Actual)Interventional2007-12-31Completed
The Tshilo Dikotla Study: Metabolic Outcomes of Children HIV/ARV-Exposed Uninfected in Botswana (MOCHA) [NCT03088410]Phase 4495 participants (Actual)Interventional2016-08-22Completed
A Pharmacokinetic Evaluation of Levonorgestrel Implant and Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI)-Based Antiretroviral Therapy in HIV-infected Ugandan Women [NCT01789879]Phase 260 participants (Actual)Interventional2014-03-04Completed
A Phase III Randomized, Double-Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00000942]Phase 31,244 participants InterventionalCompleted
An Open-Label, Non-Randomized Trial to Evaluate the Tolerability and Safety of Viramune (Nevirapine) in Adult and Pediatric Patients With Progressive HIV Disease [NCT00002166]Phase 30 participants InterventionalCompleted
Comparison Atazanavir/Ritonavir (ATV/r) vs Nevirapine (NVP) Twice a Day (Bid) on Truvada Backbone [NCT00552240]Phase 4154 participants (Actual)Interventional2007-09-30Completed
An Open Label, Randomized Study to Compare Antiretroviral Therapy (ART) Initiation When CD4 is Between 15% to 24% to ART Initiation When CD4 Falls Below 15% in Children With HIV Infection and Moderate Immune Suppression [NCT00234091]Phase 3300 participants (Actual)Interventional2006-04-30Completed
[NCT00398684]Phase 31,792 participants Interventional2001-01-31Completed
A Pharmacokinetic Study to Evaluate the Interaction Between Nevirapine (Viramune®) and Methadone in HIV-1 Infected, Opioid-dependent Adults on Stable Methadone Maintenance Therapy [NCT00273988]Phase 410 participants Interventional2002-04-30Completed
A Case-Control Toxicogenomics Study to Identify Unique Genetic Polymorphisms in Patients Who Have Experienced Symptomatic Hepatotoxicity or Severe Cutaneous Toxicity Within the First 8 Weeks of Nevirapine Therapy [NCT00310843]889 participants (Actual)Observational2006-02-28Completed
The Effect of Single Dose Carbamazepine on the Pharmacokinetics of Single Dose Nevirapine (Viramune, NVP) and Development of NVP Resistance, PMTCT Program of Moshi, Tanzania (VITA1) [NCT00294892]Phase 2144 participants (Actual)Interventional2006-02-28Completed
MEDICLAS Study (Metabolic Effects of Different Classes of AntiretroviralS) [NCT00122226]Phase 450 participants Interventional2003-01-31Active, not recruiting
Very Early Intensive Treatment of HIV-Infected Infants to Achieve HIV Remission: A Phase I/II Proof of Concept Study [NCT02140255]Phase 1/Phase 2905 participants (Anticipated)Interventional2015-01-23Recruiting
Tenofovir, Emtricitabine, and Nevirapine for Recently HIV-Infected Subjects: Can Short-Course, Once Daily Therapy Reduce the Viral Load at 12 Months From Estimated Date of Infection? [NCT00087464]0 participants (Actual)InterventionalWithdrawn(stopped due to study was withdrawn before any participants were recruited and enrolled)
Randomised, Prospective Multicentre Clinical Study on the Effect of the Combination of Lopinavir/Rtv + Nevirapine as Maintenance Bitherapy (Without Nucleoside Analogues) in Comparison With a Triple Therapy Including Lopinavir/Rtv + Nucleoside Analogues in [NCT00335686]Phase 467 participants (Actual)Interventional2003-10-31Completed
An Open-label Study Evaluating the Resistance Profile of Single Dose Nevirapine(NVP) When Combined With a 4 or 7 Day Course of Combivir® (ZDV/3TC) Compared to Single Dose Nevirapine for the Prevention of Mother to Child Transmission (pMTCT) of HIV - Treat [NCT00144183]Phase 3407 participants Interventional2003-01-31Completed
[NCT00466180]Phase 462 participants (Actual)Interventional2004-06-30Completed
An Open-label, Non-randomized, Single-arm Study, to Investigate the Mechanism(s) by Which Nevirapine Increases Plasma High Density Lipoproteins Concentration in HIV+ Subjects Treated With VIRAMUNE® Tablets [NCT00144261]Phase 415 participants (Actual)Interventional2003-11-30Completed
Efavirenz to Nevirapine Switch in HIV-1 Infected Patients With Severe Dyslipidemia: A Randomized Controlled Study [NCT00405171]Phase 440 participants Interventional2003-06-30Completed
Efficacy and Safety of Concomitant Use of Nevirapine and Rifampicin in Antiretroviral Naive Patients Co-infected With HIV and Tuberculosis in India. [NCT01805258]Phase 3135 participants (Actual)Interventional2007-06-30Completed
A Phase II Rolling Arm Master Protocol (PRAM) of Novel Antiretroviral Therapy in Stable Experienced HIV- Infected Children; PRAM-1: ZDV+3TC vs. d4T+Ritonavir vs. ZDV+3TC+Ritonavir; PRAM-1, Step 2: d4T+Nevirapine+Ritonavir; PRAM-1, Step 3: d4T+Indinavir vs [NCT00001083]Phase 2240 participants InterventionalCompleted
Evaluation of Safety and Efficacy of Two Different Once Daily Anti Retroviral Treatment Regimens Along With Anti-tuberculosis Treatment in Patients With HIV-1 and Tuberculosis [NCT00332306]Phase 3180 participants (Anticipated)Interventional2006-06-30Active, not recruiting
A Randomized Controlled Trial to Compare the Efficacy of a Four Drug Antiretroviral Regimen Alone or in Combination With GM-CSF or IL-12 Administered to HIV-1 Infected Subjects as Measured by the Characteristics of Viral Decay [NCT00000896]24 participants InterventionalCompleted
A Randomized, Double-Blind, Four-Arm Study Comparing Combination Nucleoside, Alternating Nucleoside, and Triple-Drug Therapy for the Treatment of Advanced HIV Disease (CD4 <= 50/mm3) [NCT00000781]Phase 21,292 participants InterventionalCompleted
A Master Protocol to Evaluate the Safety and Efficacy of Multi-Drug Combination Antiretroviral Therapy for the Treatment of HIV Infection: Retrovir/HIVID/Nevirapine and Retrovir/HIVID/Invirase [NCT00002347]Phase 2225 participants InterventionalCompleted
Extended Infant Post-exposure Prophylaxis With Antiretrovirals to Reduce Postnatal HIV Transmission [NCT00115648]Phase 33,300 participants (Anticipated)Interventional2004-04-30Completed
Phase II, Randomized, Open-Label Study of Switching to Protease Inhibitor-Sparing Regimens for Improvement of Metabolic Abnormalities [NCT00021463]Phase 2342 participants InterventionalCompleted
A Phase III Randomized, Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00000869]Phase 32,009 participants InterventionalCompleted
An Open Label, Staggered Rising Dose Cohort Study Assessing Safety, Tolerance, and Activity of BI-RG-587 in Patients With HIV Infection (CD4+ Cell Count < 400 Cells/mm3) [NCT00000962]Phase 130 participants InterventionalCompleted
A Pilot Study of the Immunologic Reconstitution in HIV-1 Infected Children Receiving Highly Active Antiretroviral Therapy With Combination Ritonavir, Nevirapine and Stavudine [NCT00001688]Phase 225 participants Interventional1998-01-31Completed
Prevention of Maternal to Infant HIV Transmission in India [NCT00061321]Phase 3770 participants (Actual)Interventional2002-08-31Completed
A Pilot Study of a Nucleoside Analogue Reverse Transcriptase Inhibitor Sparing Regimen in Antiretroviral-Naïve, HIV-infected Patients [NCT00143689]Phase 413 participants (Actual)Interventional2002-04-30Completed
An Open-Label Study of Nevirapine Plus Combivir® (ZDV+3TC) Treatment in Women Who Have Previously Received a Nevirapine Regimen for the Prevention of Mother to Child Transmission (pMTCT) of HIV-1. [NCT00144157]Phase 453 participants (Actual)Interventional2003-06-30Completed
Phase III, Randomized, Double-Blind Comparison of Three Protease Inhibitor-Sparing Regimens for the Initial Treatment of HIV Infection [NCT00013520]Phase 31,125 participants InterventionalCompleted
An Open-Label, Non-Randomized Study of Pharmacokinetic Interactions Between Depo-Medroxyprogesterone Acetate (DMPA, Depo-Provera) and Selected Protease Inhibitor (PI) and Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI) Therapies Among HIV-Infected W [NCT00016601]76 participants Interventional2001-06-30Completed
A Restrictively Randomized, Open-Label, Controlled, Pilot Study of the Effect of a Thymidine Analogue Substitution or Change to a Nucleoside-Sparing Regimen on Peripheral Fat Wasting [NCT00028314]150 participants Interventional2002-03-31Completed
Phase III Trial of Antibiotics to Reduce Chorioamnionitis-Related Perinatal HIV Transmission [NCT00021671]Phase 33,720 participants InterventionalCompleted
A Retrospective Study to Compare the 3-Year Antiviral Efficacy of Nevirapine and Efavirenz in Combination With D4t and 3tc in 2NN Patients and of Trizivir Versus Trizivir Plus Nevirapine in CHARM Patients [NCT00127972]Phase 4763 participants (Actual)Interventional2004-02-29Completed
A Phase II Open Label Clinical Trial of Maternal Zidovudine/Lamivudine and Either Nevirapine or Nelfinavir for Maximal Reduction of Mother-to-child HIV Transmission in Resource-limited Settings Among Breastfeeding Populations [NCT00146380]Phase 2520 participants (Anticipated)Interventional2003-07-31Active, not recruiting
ARVs to Prevent Breastmilk HIV:Viral and Immune Responses [NCT00167674]Phase 258 participants (Actual)Interventional2003-05-31Completed
Maternal and Infant Peripartum Nevirapine, Versus Infant Only Peripartum Nevirapine, or Maternal Lopinavir/Ritonavir in Addition to Standard Zidovudine Prophylaxis for the Prevention of Perinatal HIV in Thailand. [NCT00409591]Phase 3435 participants (Actual)Interventional2008-07-31Terminated(stopped due to Change in National PMTCT guidelines in Thailand)
"Prevention of Milk-Borne Transmission of HIV-1C in Botswana (Mashi)" [NCT00197587]1,200 participants (Actual)Interventional2002-08-31Completed
Optimizing Pediatric HIV-1 Treatment in Infants With Prophylactic Exposure to Nevirapine, Nairobi, Kenya (6-12 Month RCT) [NCT00427297]Phase 334 participants (Actual)Interventional2007-09-30Terminated(stopped due to There is no longer equipoise. DSMB recommended termination.)
Influence of Nevirapine on HCV Viral Load Among HIV/HCV-coinfected Patients [NCT01277627]60 participants (Anticipated)Interventional2011-01-31Not yet recruiting
Clinical Pilot Trial to Evaluate the Influence of Nevirapine in Exposure to Atazanavir in Steady State Equilibrium in HIV-infected Adult Patients. [NCT00355719]Phase 414 participants (Actual)Interventional2007-01-31Completed
A Phase III Trial to Determine the Efficacy and Safety of an Extended Regimen of Nevirapine in Infants Born to HIV-Infected Women to Prevent Vertical HIV Transmission During Breastfeeding [NCT00074412]Phase 32,026 participants (Actual)Interventional2007-01-31Completed
A Randomised Open Label Multi-centre Trial to Evaluate the Pharmacokinetic, Efficacy and Safety Parameters of Nevirapine 150mg/m2 and Nevirapine 4 or 7 mg/kg When Administered in Combination With AZT and 3TC for 48 Weeks in Antiretroviral naïve Paediatric [NCT00273975]Phase 2123 participants Interventional2002-01-31Completed
An Open, Randomised, Multicentre, Comparative Trial, to Evaluate the Benefit of Switching From a PI-based Regimen to a Nevirapine-based Regimen on the Quality of Life, Patient Adherence, Patient's Perception of Fat Redistribution and Metabolic Changes, in [NCT00274001]Phase 4158 participants (Actual)Interventional2001-09-30Completed
Cross-sectional Study for the Characterisation of the Pharmacokinetic Parameters of Protease Inhibitors and Non-nucleoside Analog Reverse Transcriptase Inhibitors in the Spanish Population of HIV-infected Subjects [NCT00307502]Phase 1675 participants (Actual)Interventional2005-01-31Completed
PHPT-5 Second Phase: Perinatal Antiretroviral Intensification for the Prevention of Mother-to-child Transmission of HIV in Thai Women Having Received Less Than 8 Weeks of HAART During Pregnancy [NCT01511237]Phase 3379 participants (Actual)Interventional2011-12-31Completed
Optimal Dosing of 1st Line Antituberculosis and Antiretroviral Drugs in Children (a Pharmacokinetic Study) [NCT01637558]Phase 4200 participants (Actual)Interventional2012-11-30Completed
Nevirapine vs Ritonavir-boosted Lopinavir in ART HIV-infected Adults in a Resource-limited Setting; a Randomized, Multicenter, Parallel Group Study [NCT01772940]Phase 4425 participants (Actual)Interventional2008-12-31Completed
A Phase II Study of 1) Amprenavir (141W94/VX478) Plus 3TC Plus ZDV (or d4T) or 2) IDV Plus NVP Plus 3TC Plus d4T in Subjects Previously Treated With Amprenavir and 3) Other Treatment Regimens (Observational ARM) in Subjects Previously Treated With Amprena [NCT00001095]Phase 294 participants InterventionalCompleted
Lopinavir/Ritonavir/Combivir vs. Abacavir/Zidovudine/Lamivudine for Virologic Efficacy and the Prevention of Mother-to-Child HIV Transmission Among Breastfeeding Women With CD4 Counts Greater Than or Equal to 200 Cells/mm3 in Botswana [NCT00270296]Phase 2730 participants (Actual)Interventional2006-06-30Completed
A Phase I Study of Safety and Pharmacokinetics of Nevirapine in HIV-1 Infected Pregnant Women and Neonates Born to HIV-1 Infected Mothers [NCT00000808]Phase 149 participants InterventionalCompleted
A Comparative Study of Combination Antiretroviral Therapy in Children and Adolescents With Advanced HIV Disease [NCT00000814]Phase 1390 participants InterventionalCompleted
Multi-Drug Antiretroviral Therapy for Heavily Pretreated Pediatric AIDS Patients: A Phase I Proof of Concept Trial [NCT00001108]Phase 16 participants InterventionalCompleted
A Pilot Pharmacokinetic Phase I Evaluation of BI-RG-587 in HIV-Infected Children [NCT00000634]6 participants InterventionalCompleted
An Open-Label Study in HIV+ Patients to Determine the Effects of Nevirapine (Viramune) on the Pharmacokinetics of Clarithromycin and Activity of Cytochrome 3A4. [NCT00002194]Phase 136 participants InterventionalCompleted
An International, Double Blind, Randomized, Phase III Study to Evaluate the Tolerance, Safety, and Effectiveness of Viramune (Nevirapine) in Preventing Clinical AIDS Progression Events or Death When Used in Combination With Lamivudine (3TC) and Stable (>= [NCT00002368]Phase 32,000 participants InterventionalCompleted
Effect of Moringa Oleifera (Moringa, Drumstick/Horseradish Tree) on The Pharmacokinetics of Efavirenz and Nevirapine In-vivo. [NCT01410058]19 participants (Actual)Observational2013-01-31Completed
A Comparative Study of a Combination of Zidovudine, Didanosine, and Double-Blinded Nevirapine Versus a Combination of Zidovudine and Didanosine [NCT00000770]Phase 2400 participants InterventionalCompleted
Early Intensive Antiretroviral Combination Therapy in HIV-1 Infected Infants and Children [NCT00000872]Phase 255 participants (Anticipated)InterventionalCompleted
RAD-1: A Phase I/II Antiretroviral Management Algorithm for Pediatric Subjects of Four-Drug Combination Therapies Based on Prior Antiretroviral Experience [NCT00000902]Phase 1217 participants InterventionalCompleted
A Multi-Center, Placebo-Controlled, Double-Blind, Randomized Trial Comparing the Activity, Safety, and Tolerance of 1) 400 Mg Nevirapine in Combination With 500-600 Mg Zidovudine Versus Zidovudine Alone in Asymptomatic HIV-1 Infected Patients With 3-24 Mo [NCT00002324]Phase 2250 participants InterventionalCompleted
An Open-Label, Staggered Rising Dose Cohort Study Assessing the Pharmacokinetics, Safety, and Tolerance of BI-RG-587 in Combination With Zidovudine in Patients With HIV Infection (CD4+ Cell Count < 400/mm3) [NCT00000649]Phase 130 participants InterventionalCompleted
A Multi-Center, Placebo-Controlled, Double-Blind, Randomized Trial Comparing the Virologic and Immunologic Activities of 400 Mg Nevirapine in Combination With Zidovudine Versus Zidovudine Alone in Asymptomatic HIV-1 Infected Patients With 4-12 Months of P [NCT00002323]60 participants InterventionalCompleted
A Phase III Randomized, Double-Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00001135]Phase 32,009 participants InterventionalCompleted
A Randomized Open-Label Strategic Study to Evaluate the Safety and Efficacy of 3 Different Convergent and Divergent Drug Combination Therapies in Anti-Retroviral Naive HIV-1 Infected Patients With CD4+ Counts Above 200/mm3 [NCT00002407]0 participants InterventionalCompleted
An Open-Label, Proof of Concept, Randomized Trial Comparing a LPV/r-Based to an nNRTI-Based Antiretroviral Therapy Regimen for Clearance of Plasmodium Falciparum Subclinical Parasitemia in HIV-infected Adults With CD4+ Counts >200 and <500 Cells/mm^3 [NCT01632891]Phase 1/Phase 252 participants (Actual)Interventional2014-01-10Completed
Phase I/II Study of ABT-378/Ritonavir in Protease Inhibitor Experienced HIV-Infected Patients [NCT00004580]Phase 10 participants InterventionalCompleted
A Randomized, Open-Label, Pilot Treatment Trial Evaluating Cellular Dynamics and Immune Restoration in Treatment-Naive HIV-Infected Subjects Receiving Either the Protease Inhibitor LPV/r or the Nucleoside Analogue Reverse Transcriptase Inhibitors d4T/3TC/ [NCT00004855]55 participants InterventionalCompleted
A Phase II Rolling Arm Master Protocol (PRAM) of Novel Antiretroviral Therapy in Stable Experienced HIV-Infected Children. PRAM-2: A Phase I/II Randomized, Multicenter Protocol Comparing Four Antiretroviral Regimens Containing Combinations of Protease Inh [NCT00001091]Phase 1200 participants InterventionalCompleted
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (Viramune) and Nelfinavir (Viracept) and the Efficacy of This Combination Therapy in HIV-1 Infected Adults Treated With Stavudine [d4T] (Zerit) [NCT00002381]Phase 124 participants InterventionalCompleted
A Randomized, Open-Label, Phase III Study of ABT-378/Ritonavir in Combination With Nevirapine and Two Nucleoside Reverse Transcriptase Inhibitors (NRTIs) vs. Investigator Selected Protease Inhibitor(s) in Combination With Nevirapine and Two NRTIs in Antir [NCT00004581]Phase 3300 participants InterventionalCompleted
A Pharmacokinetic Study to Assess Nevirapine Levels in HIV-infected Patients With Impaired Hepatic Function [NCT00144248]Phase 451 participants (Actual)Interventional2004-06-25Completed
Neuropsychiatric Adverse Effects of Efavirenz in Children Living With HIV in Kilimanjaro, Tanzania [NCT03227653]144 participants (Actual)Observational2017-06-19Completed
Switching From Regimens Consisting of a RTV-Boosted Protease Inhibitor Plus TDF/FTC to a Combination of Raltegravir Plus Nevirapine and Lamivudine in HIV Patients With Suppressed Viremia and Impaired Renal Function (RANIA Study) (Pilot Study) Protocol MK- [NCT02116660]Phase 211 participants (Actual)Interventional2014-09-03Terminated(stopped due to This study was terminated early due to poor recruitment.)
Latency and Early Neonatal Provision of Antiretroviral Drugs Clinical Trial [NCT02431975]Phase 473 participants (Actual)Interventional2015-08-31Completed
Population Pharmacokinetics of Antiretroviral in Children [NCT03194165]65 participants (Actual)Observational2017-06-16Completed
Steady State Bioequivalence of Generic and Innovator Formulations of Stavudine, Lamivudine, and Nevirapine in HIV-infected Ugandan Adults [NCT01025830]Phase 420 participants (Actual)Interventional2006-02-28Completed
BHP Early Infant Treatment Study: A Clinical Treatment Trial of HIV+ Infants in Botswana [NCT02369406]Phase 2/Phase 367 participants (Actual)Interventional2015-05-04Active, not recruiting
Antiretroviral Regime for Viral Eradication in Newborns After Intervention Failure of Mother-to-child Transmission of HIV [NCT02712801]Phase 4600 participants (Actual)Interventional2016-04-30Completed
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 3224 participants (Actual)Interventional2014-12-31Completed
A Randomised Trial of Monitoring Practice and Induction Maintenance Drug Regimens in the Management of Antiretroviral Therapy in Children With HIV Infection in Africa [NCT02028676]Phase 41,206 participants (Actual)Interventional2007-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
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 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: 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 12 Hours (AUC12) With Median (Range) 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]Plasma Concentration for Contraceptives
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: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
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 Half-life (T1/2) of 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]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 (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]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]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
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]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
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: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00074412 (5) [back to overview]Frequency and Severity of Adverse Reactions Among Participating Infants
NCT00074412 (5) [back to overview]HIV Infection in Infants Determined to be HIV Uninfected at 6 Weeks Enrolled in Each Arm of the Study
NCT00074412 (5) [back to overview]Infant Survival Rates (Mortality Regardless of HIV Infection) in the Two Arms
NCT00074412 (5) [back to overview]Proportion of Infants Who Are Alive and HIV-uninfected in the Two Arms
NCT00074412 (5) [back to overview]Relative Rates of HIV Infection in the Two Arms
NCT00074581 (2) [back to overview]All Partner HIV Infection Rates in Early-ART and Delayed-ART Arms
NCT00074581 (2) [back to overview]Linked Partner HIV Infection Rates in Early-ART and Delayed-ART Arms
NCT00089505 (9) [back to overview]Number of Participants Who Experienced HIV-related Disease Progression or Death
NCT00089505 (9) [back to overview]Number of Participants Who Experienced Treatment-related Toxicity That Led to Discontinuation of Randomized Regimen.
NCT00089505 (9) [back to overview]Number of Participants Who Experienced Virologic Failure or Died.
NCT00089505 (9) [back to overview]Number of Participants Who Received NVP-containing Regimens at Randomization and Experienced NVP-associated Rash or Grade 2+ Liver Lab Abnormality
NCT00089505 (9) [back to overview]CD4 Count Change From Randomization
NCT00089505 (9) [back to overview]Percent of Participants Who Experienced Virologic Failure or Died
NCT00089505 (9) [back to overview]Percent of Participants Who Reported to Never Missed Any of the Study Drug Regimen in the Past Month
NCT00089505 (9) [back to overview]Time From Randomization to Virologic Failure or Death for Participants Who Had SD NVP Exposure Prior to Study Entry
NCT00089505 (9) [back to overview]Time From Randomization to Virologic Failure or Death for Participants Without SD NVP Exposure Prior to Study Entry
NCT00099359 (7) [back to overview]NVP Pharmacokinetics
NCT00099359 (7) [back to overview]Infant HIV Infection Status
NCT00099359 (7) [back to overview]Participant Deaths
NCT00099359 (7) [back to overview]Infant HIV-1 Infection Status
NCT00099359 (7) [back to overview]Risk Factors for Perinatal HIV-1 Transmission
NCT00099359 (7) [back to overview]Participants With Serious Adverse Events
NCT00099359 (7) [back to overview]3TC and NFV Pharmacokinetics
NCT00099632 (5) [back to overview]Severe (Grade 3) and Higher Adverse Events and Any Grade Adverse Event That Leads to a Treatment Change From First Day of Study Treatment to Week 12
NCT00099632 (5) [back to overview]Number of Participants With New PI-resistant Variants as Detected by Standard Composite (Bulk) Genotyping.
NCT00099632 (5) [back to overview]Number of Participants With New Circulating NRTI-resistant Variants Detected by Standard Composite (Bulk) Genotyping.
NCT00099632 (5) [back to overview]Number of Participants With New Circulating Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI)-Resistant Variants as Detected by Standard Composite (Bulk) Genotyping
NCT00099632 (5) [back to overview]Number of Participants Who Discontinued Study Treatment Prematurely
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Virological Failure Defined as Confirmed HIV-1 RNA Value of at Least 10,000 Copies Per/ml Recorded on Two Consecutive Separate Occasions After 24 Weeks of Treatment (Initial Therapy or Restart)
NCT00102960 (13) [back to overview]Time From Randomization to Starting or Needing to Start Continuous Therapy
NCT00102960 (13) [back to overview]Time to Death Alone or Death Plus Life Threatening Stage C Events or HIV Events Associated With Permanent End-organ Damage.
NCT00102960 (13) [back to overview]Time to Failure of First Line Therapy or Death
NCT00102960 (13) [back to overview]Time to First Hospitalization
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Laboratory Events
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Immunological Failure Defined as Failure of CD4% to Reach 20% or CD4% Falls Below 20% on Two Occasions, Within 4 Weeks, at Any Time After the First 24 Weeks of Therapy (Initial Therapy or Restart)
NCT00102960 (13) [back to overview]Total Occurrence of Grade 3 or 4 Clinical Events
NCT00102960 (13) [back to overview]Duration of Hospitalisation
NCT00102960 (13) [back to overview]Hospitalization Rates
NCT00102960 (13) [back to overview]Number of Children Experiencing Severe CDC Stage B or Stage C Disease or Death (Cumulative After 3.5 Years)
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Clinical Failure (Defined as Development of Severe CDC Stage B or Stage C Disease.) on Therapy.
NCT00102960 (13) [back to overview]Number of Participants Who Experienced Regimen-limiting ART Drug Toxicity
NCT00109590 (12) [back to overview]The Proportion of Women With Any New ZDV, ddI, or LPV/r Resistance Mutations.
NCT00109590 (12) [back to overview]Proportion of Women With New NVP Resistance Mutation Within 8 Weeks Postpartum Who Had a NVP Resistance Mutation Detected at 72 Weeks Postpartum.
NCT00109590 (12) [back to overview]The Proportion of Women Who Develop One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay in Plasma (Sampling Was Done at Days 10,21,30, and Weeks 5,6, and 8 Postpartum).
NCT00109590 (12) [back to overview]The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations for the Subgroup of Women With Plasma HIV RNA >= 500 Copies/ml At Entry
NCT00109590 (12) [back to overview]The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay (OLA) in Plasma
NCT00109590 (12) [back to overview]Area Under the Curve Pharmacokinetic Outcome for LPV/r. (AUC ug*hr/mL)
NCT00109590 (12) [back to overview]Four (4) Hour Concentration Pharmacokinetic Outcome for LPV/r (C4hour ug/mL).
NCT00109590 (12) [back to overview]Maximum Concentration Pharmacokinetic Outcome for LPV/r (Cmax ug/mL) .
NCT00109590 (12) [back to overview]Median HIV-1 Viral Load at 24 Weeks Postpartum in Women
NCT00109590 (12) [back to overview]Number of Women With Grade >=3 Events After Start of Study Treatment
NCT00109590 (12) [back to overview]Pre-dose Concentration Pharmacokinetic Outcome for LPV/r (Cpredose ug/mL).
NCT00109590 (12) [back to overview]Resistance Mutations in HIV Infected Infants
NCT00255840 (1) [back to overview]Cumulative Treatment Failure Rate of Participants on First Line Antiretroviral Therapy Monitored by Primary Health Care Nurses (Investigative Arm)is Not Inferior to the Cumulative Treatment Failure Rate of Participants Monitored by Doctors (Control Arm).
NCT00270296 (2) [back to overview]Number of Participants With Virologic Suppression
NCT00270296 (2) [back to overview]Number of HIV+ Infants
NCT00307151 (9) [back to overview]Time From Randomization to Death
NCT00307151 (9) [back to overview]Percent of Participants With Treatment Failure, Defined as a Confirmed Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment
NCT00307151 (9) [back to overview]Percent of Participants Experiencing Virologic Failure
NCT00307151 (9) [back to overview]Number of Participants Developing New NRTI, NNRTI or PI-resistant Virus
NCT00307151 (9) [back to overview]Change in CD4 Percent From Entry to Week 48
NCT00307151 (9) [back to overview]Time From Start of Study Treatment to First New Grade >=3 Lab Abnormality, Sign or Symptom Occurring on Study Treatment
NCT00307151 (9) [back to overview]Time From Randomization to Virologic Failure
NCT00307151 (9) [back to overview]Time From Randomization to Treatment Failure, Defined as Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment
NCT00307151 (9) [back to overview]Time From Randomization to HIV-related Disease Progression or Death
NCT00344461 (6) [back to overview]Patients With Plasma HIV RNA < 50 Copies/mL
NCT00344461 (6) [back to overview]Patients With Plasma HIV RNA < 400 Copies/mL
NCT00344461 (6) [back to overview]Patients With Grade 2, 3 and 4 Adverse Events and Laboratory Toxicities
NCT00344461 (6) [back to overview]Number of Participants With Sustained Virologic Response
NCT00344461 (6) [back to overview]Changes in CD4 Cell Count From Baseline and Week 96
NCT00344461 (6) [back to overview]Change in Plasma HIV RNA From Baseline to Week 96
NCT00389207 (34) [back to overview]Proportion of Patients With VL < 400 Copies/ml
NCT00389207 (34) [back to overview]Time to Treatment Response (First Confirmed VL<50 Copies/mL)
NCT00389207 (34) [back to overview]Proportion of Patients Reporting CNS (Central Nervous System) Side Effects of Any Severity
NCT00389207 (34) [back to overview]Proportion of Patients Reporting Hepatic Events of Any Severity
NCT00389207 (34) [back to overview]Proportion of Patients Reporting Rash of Any Severity
NCT00389207 (34) [back to overview]Time to Loss of Virologic Response (Rebound)
NCT00389207 (34) [back to overview]Time to Treatment Failure
NCT00389207 (34) [back to overview]Change in CD4+ Count From Baseline
NCT00389207 (34) [back to overview]Change in Framingham Score From Baseline
NCT00389207 (34) [back to overview]Change in Mental Health Summary (MHS) Score From Baseline
NCT00389207 (34) [back to overview]Change in Physical Health Summary (PHS) Score From Baseline
NCT00389207 (34) [back to overview]Change in the Calculated Glomerular Filtration Rate (GFR) at Week 48, 96 and 144
NCT00389207 (34) [back to overview]Change of Cholesterol Values From Baseline to Week 48, 96, 144
NCT00389207 (34) [back to overview]Change of hsCRP From Baseline to Week 48, 96, 144
NCT00389207 (34) [back to overview]Change of Total Cholesterol to HDL-cholesterol Ratio From Baseline to Week 48, 96, 144
NCT00389207 (34) [back to overview]Change of Total Triglycerides From Baseline to Week 48, 96, 144
NCT00389207 (34) [back to overview]Changes of Apolipoprotein Values From Baseline to Week 48, 96, 144
NCT00389207 (34) [back to overview]Genotypic Resistance Associated With Virologic Failure
NCT00389207 (34) [back to overview]Glycaemic Abnormalities
NCT00389207 (34) [back to overview]Lipodystrophy
NCT00389207 (34) [back to overview]Non-scheduled Physician Visits
NCT00389207 (34) [back to overview]Number of Patients Hospitalized
NCT00389207 (34) [back to overview]Proportion of Patients With >= DAIDS Grade 2 Laboratory Abnormalities
NCT00389207 (34) [back to overview]Proportion of Patients With Virologic Failure at Week 48, 96, 144
NCT00389207 (34) [back to overview]Proportion of Patients With Virological Rebound With VL >=400 Copies/mL After CVR at Week 24, 48, 96, 144
NCT00389207 (34) [back to overview]Proportion of Patients With Virological Rebound With VL >=50 Copies/mL After CVR (Confirmed Virological Response) at Week 24, 48, 96, 144
NCT00389207 (34) [back to overview]Proportion of Patients With VL < 50 Copies/ml
NCT00389207 (34) [back to overview]Serum Lipid Abnormalities
NCT00389207 (34) [back to overview]Treatment Response at Week 144
NCT00389207 (34) [back to overview]Treatment Response at Week 48
NCT00389207 (34) [back to overview]Treatment Response at Week 48 (TLOVR Algorithm)
NCT00389207 (34) [back to overview]Treatment Response at Week 96
NCT00389207 (34) [back to overview]Treatment-emergent AIDS-defining Illness
NCT00389207 (34) [back to overview]Treatment-emergent AIDS-defining Illness Leading to Death
NCT00427297 (4) [back to overview]Immunologic Failure
NCT00427297 (4) [back to overview]Incidence of Severe Adverse Events (Excluding Mortality)
NCT00427297 (4) [back to overview]Viral Failure
NCT00427297 (4) [back to overview]Incidence of Mortality
NCT00552240 (46) [back to overview]Change in Fasting High Density Lipoprotein (HDL) Cholesterol Level
NCT00552240 (46) [back to overview]Number of Participants With Virologic Success (FDA Definition)
NCT00552240 (46) [back to overview]Number of Patients With Virologic Rebound to >400 Copies/ml
NCT00552240 (46) [back to overview]Proportion of Patients With DAIDS Grade >= 2 Laboratory Abnormalities
NCT00552240 (46) [back to overview]Number of Participants With Loss of Virologic Response Following Confirmed Virologic Response
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 2 of Treatment
NCT00552240 (46) [back to overview]Change in Fasting Total Cholesterol to High Density Lipoprotein (HDL) Ratio
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 8.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 6.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 48.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 4.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 36.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 24.
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 2.
NCT00552240 (46) [back to overview]AIDS Progression and Death: Number of Patients With a Treatment-emergent AIDS Defining Illness or an AIDS-defining Illness Leading to Death
NCT00552240 (46) [back to overview]Change in Fasting Plasma Triglycerides Level
NCT00552240 (46) [back to overview]Change in Fasting Plasma Total Cholesterol Level
NCT00552240 (46) [back to overview]Change in Fasting Low Density Lipoprotein (LDL)Cholesterol Level
NCT00552240 (46) [back to overview]Change in Glomerular Filtration Rate (GFR) From Baseline to Week 48
NCT00552240 (46) [back to overview]Change in Framingham Score
NCT00552240 (46) [back to overview]Percentage Adherence by Pill Count
NCT00552240 (46) [back to overview]Proportion of Patients Reporting CNS Side Effects of Any Severity
NCT00552240 (46) [back to overview]Proportion of Patients Reporting Hepatic Events of Any Severity
NCT00552240 (46) [back to overview]Proportion of Patients Reporting Rash of Any Severity
NCT00552240 (46) [back to overview]Time to Virologic Response (First Confirmed Viral Load < 50 Copies/ml), All Participants
NCT00552240 (46) [back to overview]Time to Virologic Response (First Confirmed Viral Load < 50 Copies/ml), Only Participants With Confirmed Viral Load < 50 Copies/ml
NCT00552240 (46) [back to overview]Incidence of Patients With AIDS Progression at Each Visit
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 12 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 2 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 24 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 36 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 4 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 48 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 6 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 400 Copies/ml at Week 8 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 12 of Treatment
NCT00552240 (46) [back to overview]Change in CD4+ Cell Count From Baseline to Week 12.
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 24 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 36 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 4 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 48
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 48 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 6 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With HIV Viral Load < 50 Copies/ml at Week 8 of Treatment
NCT00552240 (46) [back to overview]Number of Participants With Virologic Response (VR)
NCT00552240 (46) [back to overview]Number of Participants With Virologic Response According to the Time to Loss of Virologic Response (TLOVR) Algorithm
NCT00561925 (15) [back to overview]Kaplan -Meier Estimate of Cumulative Probability of Group III or IV Drug-related Rash
NCT00561925 (15) [back to overview]Kaplan -Meier Estimate of Cumulative Probability of Permanent Discontinuation of Study Medication
NCT00561925 (15) [back to overview]Kaplan-Meier Estimates for Time to New AIDS or AIDS-related Progression Event or Death, Full Analysis Set Population
NCT00561925 (15) [back to overview]Kaplan-Meier Estimates of the Proportions of Patients Without Loss of Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00561925 (15) [back to overview]Occurrence of Elevations in Laboratory Measurement by DAIDS Grade
NCT00561925 (15) [back to overview]Proportion of Sustained Virologic Response at Week 144 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00561925 (15) [back to overview]Comparison of CD4+ Cell Count (Cells/Cubic Millimeter) Change From Baseline at Week 144, Full Analysis Set Population
NCT00561925 (15) [back to overview]Occurrence of Rashes
NCT00561925 (15) [back to overview]Comparison of HIV-1 Viral Load (log10 Copies/mL) Change From Baseline at Week 144, Full Analysis Set Population
NCT00561925 (15) [back to overview]Occurrence of Hepatic Events
NCT00561925 (15) [back to overview]Relative Bioavailability Trough C_pre,ss,1
NCT00561925 (15) [back to overview]Comparison of Proportion of Virologic Response at Week 48 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00561925 (15) [back to overview]Kaplan -Meier Estimate of Cumulative Probability of Clinical Hepatic Events
NCT00561925 (15) [back to overview]Kaplan -Meier Estimate of Cumulative Probability of Grade 3 or 4 ALT/AST Abnormalities
NCT00561925 (15) [back to overview]Kaplan -Meier Estimate of Cumulative Probability of Grade 3 or 4 Asymptotic Transaminases Abnormalities
NCT00819052 (42) [back to overview]Trough Plasma Concentration
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Last Available Visit, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 108, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 12, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 120, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 132, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 144, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 2, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 24, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 4, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 48, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 60, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 72, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 8, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 84, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 96, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Comparison of CD4 Count (Cells/Cubic Millimeter) Change From Baseline at Week 24, Observed Cases, Full Analysis Set Population
NCT00819052 (42) [back to overview]Occurence of Hepatic Events
NCT00819052 (42) [back to overview]Summary of CD4 Count (Cells/Cubic Millimeter) at Baseline, Full Analysis Set Population
NCT00819052 (42) [back to overview]Time to Loss of Virologic Response
NCT00819052 (42) [back to overview]Change From Baseline in VL (HIV-1 Viral Load) at Each Visit
NCT00819052 (42) [back to overview]Changes in Safety Parameters Related to Treatment
NCT00819052 (42) [back to overview]Comparison of Virologic Response at Week 24 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Kaplan-Meier Estimates of the Proportions of Patients Without Loss of Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]New AIDS or AIDS-related Progression Event or Death
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population
NCT00819052 (42) [back to overview]Occurence of Rashes
NCT00819052 (42) [back to overview]Proportion of Virologic Response (Viral Load <400 Copies/mL) Trough Week 144
NCT00905489 (16) [back to overview]Efficacy: Patients Maintaining a VL < 50 Copies/mL
NCT00905489 (16) [back to overview]Efficacy: Patients Maintaining a VL < 400 Copies/mL in Optional Extension Phase
NCT00905489 (16) [back to overview]Efficacy: Patients Maintaining a VL < 400 Copies/mL
NCT00905489 (16) [back to overview]CL/F,ss
NCT00905489 (16) [back to overview]Tmax,ss
NCT00905489 (16) [back to overview]Ratio Cmax,ss/Cmin,ss
NCT00905489 (16) [back to overview]Percentage Change From Baseline in Mean CD4+ Count
NCT00905489 (16) [back to overview]Cmin,ss (for IR and XR Formulations by Nevirapine XR Dose Group)
NCT00905489 (16) [back to overview]Cmax,ss (for IR and XR Formulations by Nevirapine XR Dose Group)
NCT00905489 (16) [back to overview]Cavg
NCT00905489 (16) [back to overview]Change From Baseline in Mean CD4+ Count (Absolute)
NCT00905489 (16) [back to overview]Efficacy: Patients Maintaining a VL < 50 Copies/mL at Last Available Visit
NCT00905489 (16) [back to overview]Efficacy: Patients Maintaining a VL < 50 Copies/mL at Week 24 of Optional Extension Phase
NCT00905489 (16) [back to overview]Trough Cpre,N.
NCT00905489 (16) [back to overview]%PTF
NCT00905489 (16) [back to overview]AUCt,ss
NCT00978068 (6) [back to overview]Percentage of Uncomplicated Malaria Episodes With Accompanying Adverse Events That Occurred in the 28 Days Following Antimalarial Therapy
NCT00978068 (6) [back to overview]Incidence-density of Malaria Defined as the Number of Incident Episodes of Malaria Per Time at Risk.
NCT00978068 (6) [back to overview]Incidence-density of Malaria Defined as the Number of Incident Episodes of Complicated Malaria Per Time at Risk.
NCT00978068 (6) [back to overview]Estimates of the 6-month Risk of a First Episode of Malaria
NCT00978068 (6) [back to overview]28-day Risk of Recurrent Parasitemia
NCT00978068 (6) [back to overview]63-day Risk of Recurrent Malaria
NCT01025830 (2) [back to overview]Area Under the Concentration-Time Curve(AUC)
NCT01025830 (2) [back to overview]Maximum Plasma Concentration of Drug
NCT01061151 (28) [back to overview]Antepartum Component: Number of Confirmed Infant HIV Infections
NCT01061151 (28) [back to overview]Antepartum Component: Number of Infant HIV Infections
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of AIDS-defining Illness
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Death
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Event or Death
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Event or World Health Organization (WHO) Clinical Stage 2 or 3 Events
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of HIV/AIDS-related Events
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Progression to AIDS-defining Illness or Death
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence of Tuberculosis
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Obstetrical Complications
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Obstetrical Complications
NCT01061151 (28) [back to overview]Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)
NCT01061151 (28) [back to overview]Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)
NCT01061151 (28) [back to overview]Postpartum Component: Proportion of Infants Alive Through 12 and 24 Months Post-delivery
NCT01061151 (28) [back to overview]Antepartum Component: Maternal HIV RNA Less Than 400 Copies/mL at Delivery
NCT01061151 (28) [back to overview]Postpartum Component: Adherence to the Maternal and/or Infant ARV Regimens, as Measured by Maternal Report and Hair Measures
NCT01061151 (28) [back to overview]Postpartum Component: Incidence of Grade 3 or Higher Adverse Events and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events
NCT01061151 (28) [back to overview]Postpartum Component: Incidence of Confirmed Infant HIV Infection
NCT01061151 (28) [back to overview]Maternal Health Component: Toxicity: Incidence of Grade 3 or Greater Laboratory Results or Signs and Symptoms and Selected Grade 2 Hematologic, Renal, and Hepatic Laboratory Results
NCT01061151 (28) [back to overview]Maternal Health Component: Other Targeted Medical Conditions
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Progression to AIDS-defining Illness, Death, or a Serious Non-AIDS Cardiovascular, Hepatic, or Renal Event
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Death or Any Condition of Particular Concern
NCT01061151 (28) [back to overview]Maternal Health Component: Incidence Rate of Cardiovascular or Other Metabolic Events
NCT01061151 (28) [back to overview]Postpartum Component: Proportion of Mother-Infant Pairs With no Death or HIV Diagnosis Through 24 Months Post-delivery
NCT01061151 (28) [back to overview]Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)
NCT01410058 (3) [back to overview]Cmax
NCT01410058 (3) [back to overview]AUC
NCT01410058 (3) [back to overview]C12h
NCT01632891 (7) [back to overview]Change in log10(Pf Gametocyte Density) From Entry to Day 30
NCT01632891 (7) [back to overview]Number of Participants With Uncomplicated Clinical Malaria
NCT01632891 (7) [back to overview]Time to First Pf SCP Clearance
NCT01632891 (7) [back to overview]Log10(Pf Parasite Density)
NCT01632891 (7) [back to overview]Number of Participants With Detectable Pf Gametocyte Density
NCT01632891 (7) [back to overview]Proportion of Participants With Plasmodium Falciparum (Pf) Subclinical Parasitemia (SCP) Clearance
NCT01632891 (7) [back to overview]Change in log10(Pf Parasite Density) From Entry to Day 30
NCT02028676 (58) [back to overview]Cotrimoxazole: New Severe Pneumonia
NCT02028676 (58) [back to overview]CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 144 Weeks After Baseline
NCT02028676 (58) [back to overview]CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 72 Weeks After Baseline
NCT02028676 (58) [back to overview]Cotrimoxazole: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]Cotrimoxazole: All-cause Mortality
NCT02028676 (58) [back to overview]Cotrimoxazole: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]Cotrimoxazole: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]Cotrimoxazole: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]Cotrimoxazole: Height-for-age Z-score
NCT02028676 (58) [back to overview]Cotrimoxazole: New Clinical and Diagnostic Positive Malaria
NCT02028676 (58) [back to overview]Cotrimoxazole: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Cotrimoxazole: New Hospitalisation or Death
NCT02028676 (58) [back to overview]Cotrimoxazole: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 3 Severe Recurrent Pneumonia or Diarrhoea
NCT02028676 (58) [back to overview]Cotrimoxazole: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]Cotrimoxazole: Weight-for-age Z-score
NCT02028676 (58) [back to overview]Induction ART: Change From Baseline in CD4% 72 Weeks After ART Initiation
NCT02028676 (58) [back to overview]Induction ART: Change From Baseline in CD4% to 144 Weeks From ART Initiation
NCT02028676 (58) [back to overview]Induction ART: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Induction ART: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: All-cause Mortality
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Cessation of First-line Regimen for Clinical/Immunological Failure
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 144
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Height-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New ART-modifying Adverse Event
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New Grade 3 or 4 Adverse Event Definitely/Probably or Uncertainly Related to ART
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New or Recurrent WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM, Induction ART: Weight-for-age Z-score
NCT02028676 (58) [back to overview]LCM vs CDM: Change From Baseline in CD4% to Week 144
NCT02028676 (58) [back to overview]LCM vs CDM: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]LCM vs CDM: Disease Progression to a New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]LCM vs CDM: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 48 Weeks
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 96 Weeks
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: All-cause Mortality
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Body Mass Index-for-age Z-score
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 48
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 72
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 96
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 48
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 72
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 96
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Height-for-age Z-score
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Grade 3 or 4 Adverse Event (AE), Not Solely Related to HIV, Judged Definitely/Probably or Uncertain Whether Related to Lamivudine or Abacavir
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New Serious Adverse Events Not Solely Related to HIV
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 3 or 4 Event or Death
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 4 Event or Death
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Suppressed HIV RNA Viral Load 48 Weeks After Randomisation
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Suppression of HIV RNA Viral Load 96 Weeks After Randomisation
NCT02028676 (58) [back to overview]Once Versus Twice Daily Abacavir+Lamivudine: Weight-for-age Z-score
NCT02116660 (1) [back to overview]Change From Baseline in Estimated Glomerular Filtration Rate (eGFR)

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

Measured in 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, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 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, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (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.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (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.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (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.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 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, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 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, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
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.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed 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. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed 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. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (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.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
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.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (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

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

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
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

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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.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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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.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
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.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) 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.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) 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.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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PK Parameter: Maximum Concentration (Cmax) in ng/mL 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.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed 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. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
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.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (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.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (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. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (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

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Frequency and Severity of Adverse Reactions Among Participating Infants

For those infants who were randomized at 6 weeks and who initiated study drug we looked at the frequency and severity of adverse reactions through 18 months of study. The severity of all AEs was graded according to the DAIDS Table for Grading the Severity of Adult and Pediatric Adverse Events. The term severity is described as the intensity grade or level for specific event (i.e. mild, moderate, severe, or life-threatening). Severity is not the same as seriousness. (NCT00074412)
Timeframe: 6 weeks through 18 months

,
InterventionNumber of Adverse Events (Number)
DeathLife-ThreateningSevereModerateMild
Nevirapine2687375694832
Placebo3087332677838

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HIV Infection in Infants Determined to be HIV Uninfected at 6 Weeks Enrolled in Each Arm of the Study

(NCT00074412)
Timeframe: At Month 6

,
Interventionparticipants (Number)
# of HIV infections at 6 months# of Infants at risk for HIV infection at 6 months
Nevirapine8700
Placebo18699

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Infant Survival Rates (Mortality Regardless of HIV Infection) in the Two Arms

(NCT00074412)
Timeframe: At Month 18

,
Interventionparticipants (Number)
# Infant Deaths at 18 months# Infants at risk of death at 18 months
Nevirapine26678
Placebo30684

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Proportion of Infants Who Are Alive and HIV-uninfected in the Two Arms

(NCT00074412)
Timeframe: At Months 6 and 18

,
Interventionparticipants (Number)
Number of Infants Alive and HIV-free at 6 monthsNumber of Infants Alive and HIV-free at 18 months
Nevirapine689629
Placebo683616

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Relative Rates of HIV Infection in the Two Arms

(NCT00074412)
Timeframe: At Month 18

,
Interventionparticipants (Number)
# of infants with HIV infection at 18 months# of infants @ risk for HIV infection at 18 months
Nevirapine16664
Placebo23663

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All Partner HIV Infection Rates in Early-ART and Delayed-ART Arms

All Incident HIV infections occurring in the partners (HIV-negative at enrollment) of randomized HIV-infected index (HIV-positive at enrollment) cases are assessed, by arm. (NCT00074581)
Timeframe: Throughout study

Interventionevent rate per 100 person-yr (Number)
Early-ART0.44
Delayed-ART1.41

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Linked Partner HIV Infection Rates in Early-ART and Delayed-ART Arms

incident HIV infections occurring in the partners (HIV-negative at enrollment) of randomized HIV-infected index (HIV-positive at enrollment) cases are assessed, by arm. Only acquisition from the index partner were included in the primary analysis, therefore, each endpoint was required to be confirmed (by genotyping) such that the viral envelop sequence in the index case matched that of the partner. (NCT00074581)
Timeframe: Throughout study

Interventionevent rate per 100 person-yr (Number)
Early-ART0.07
Delayed-ART1.03

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Number of Participants Who Experienced Virologic Failure or Died.

Virologic failure (VF) is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r. Throughout study for NoNVP/NVP and NoNVP/LPV_r.

Interventionparticipants (Number)
NVP/NVP32
NVP/LPV_r10
NoNVP/NVP42
NoNVP/LPV_r50

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Number of Participants Who Received NVP-containing Regimens at Randomization and Experienced NVP-associated Rash or Grade 2+ Liver Lab Abnormality

Any grade of rash or grade 2+ liver lab abnormality events that were claimed to be NVP associated (definitely, probably, or possibly) by site investigators were evaluated. Grade 2+ liver lab abnormality is defined as aspartate aminotransferase (AST)>=2.6 x ULN or alanine aminotransferase (ALT)>=2.6 x ULN. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP arm. Throughout study for NoNVP/NVP arm.

Interventionparticipants (Number)
NVP/NVP20
NoNVP/NVP51

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CD4 Count Change From Randomization

Change was calculated as the CD4 count at Week 48 (or at Week 96) minus the baseline CD4 count (last CD4 before/on treatment start date). For NVP/NVP and NVP/LPV_r arms, data through DSMB review cutoff (October 6, 2008) were used to report the outcome. For NoNVP/NVP and NoNVP/LPV_r arms, since the follow-up continued as planned, data through overall study were used. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r. Throughout study for NoNVP/NVP and NoNVP/LPV_r. Week 48 and 96.

,,,
Interventioncells/mm^3 (Median)
Week 48 CD4 count change from randomizationWeek 96 CD4 count change from randomization
NoNVP/LPV_r172256
NoNVP/NVP172223
NVP/LPV_r201278
NVP/NVP191291

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Percent of Participants Who Experienced Virologic Failure or Died

Results report cumulative percent of participants reaching virologic failure (VF) or death by week 48 and week 96 calculated using the Kaplan-Meier method. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r arms. Throughout study for NoNVP/NVP and NoNVP/LPV_r arms.

,,,
InterventionPercent of participants (Number)
week 48 percent of virologic failure or deathweek 96 percent of virologic failure or death
NoNVP/LPV_r1420
NoNVP/NVP1417
NVP/LPV_r412
NVP/NVP2331

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Percent of Participants Who Reported to Never Missed Any of the Study Drug Regimen in the Past Month

Self-reported adherence at week 48 and 96 while participants remained on randomized regimen. Adherence interviews for each antiretroviral drug drug the participant is taking was performed by site personnel every 24 weeks. For NVP/NVP and NVP/LPV_r arms, data through DSMB review cutoff (October 6, 2008) were used to report the outcome. For NoNVP/NVP and NoNVP/LPV_r arms, since the follow-up continued as planned, data through overall study were used. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) for NVP/NVP and NVP/LPV_r arms. Throughout study for NoNVP/NVP and NoNVP/LPV_r arms.

,,,
Interventionpercent of participants (Number)
week 48 percent of full adherence in past monthweek 96 percent of full adherence in past month
NoNVP/LPV_r8687
NoNVP/NVP9093
NVP/LPV_r8895
NVP/NVP8994

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Time From Randomization to Virologic Failure or Death for Participants Who Had SD NVP Exposure Prior to Study Entry

5th and 10th Percentiles in weeks from randomization to virologic failure (VF) or death. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Through database cutoff for DSMB review (by October 6, 2008) with median follow-up 72 weeks and range from 0 to 144 weeks.

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
NVP/LPV_r6084NA
NVP/NVP121260

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Time From Randomization to Virologic Failure or Death for Participants Without SD NVP Exposure Prior to Study Entry

5th and 10th Percentiles in weeks from randomization to virologic failure (VF) or death. VF is defined as a plasma HIV-1 RNA level that is 1 log10 below baseline 12 weeks after treatment is initiated or as a plasma HIV-1 RNA level that is >=400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized treatment was being taken at the time of VF. (NCT00089505)
Timeframe: Throughout study with median follow-up 72 weeks and range from 0 to 180 weeks.

,
Interventionweeks (Number)
5th percentile10th percentile25th percentile
NoNVP/LPV_r1236132
NoNVP/NVP2436NA

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NVP Pharmacokinetics

Descriptive study of NVP pharmacokinetics during first two weeks of life using weight band dosing in a subset of enrolled infants. (NCT00099359)
Timeframe: 14 days

Interventionng/mL (Median)
NVP conc prior to 3rd doseNVP peak conc (Cmax) post 3rd doseNVP conc 3-5 day post 3rd doseNVP conc 7 day post 3rd dose
ARM B (ZDV + NVP)362228645976

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Infant HIV Infection Status

Intrapartum HIV infection at 3 Months (NCT00099359)
Timeframe: 3 months

Interventionparticipants (Number)
ARM A (ZDV - Standard of Care)24
ARM B (ZDV + NVP)11
ARM C (ZDV +3TC+NFV)12

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Participant Deaths

(NCT00099359)
Timeframe: through age 6 months

Interventionparticipants (Number)
Arm A (ZDV Only)11
ARM B (ZDV + NVP)15
ARM C (ZDV + 3TC + NFV)17

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Infant HIV-1 Infection Status

In utero HIV-1 infection rate (NCT00099359)
Timeframe: birth

Interventionparticipants (Number)
Arm A (ZDV Only)37
ARM B (ZDV + NVP)28
ARM C (ZDV + 3TC + NFV)28

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Risk Factors for Perinatal HIV-1 Transmission

Risk factors to be assessed include maternal HIV-1 RNA levels at delivery, maternal syphilis and other infections, obstetrical factors such as duration of membrane rupture, and adherence to neonatal medication. (NCT00099359)
Timeframe: through age 3 months

,
Interventionparticipants (Number)
Treatment Arm C (ZDV+3TC/NFV)Treatment Arm B (ZDV+NFV)Treatment Arm A (ZDV only)Illegal Substance Abuse during pregnancy
Infected1211247
Uninfected516523505130

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Participants With Serious Adverse Events

Serious Adverse Events by System Organ Class=Blood and lymphatic system disorders (NCT00099359)
Timeframe: through age 6 months.

Interventionparticipants (Number)
ARM A (ZDV Only)86
ARM B (ZDV + NVP)59
ARM C (ZDV + 3TC/NFV)110

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3TC and NFV Pharmacokinetics

Descriptive study of 3TC and NFV pharmacokinetics during first two weeks of life using weight band dosing regimen in a subset of enrolled infants. (NCT00099359)
Timeframe: through age 14 days

Interventionug*h/mL (Median)
(NFV-AUC-12h) 4-7 day(NFV-AUC-12h) 10-14 day(3TC-AUC-12 h) 4-7 day(3TC-AUC-12h) 10-14 day
ARM C (ZDV + 3TC/NFV)20.725.54.07.9

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Severe (Grade 3) and Higher Adverse Events and Any Grade Adverse Event That Leads to a Treatment Change From First Day of Study Treatment to Week 12

"Grade 3 or higher signs and symptoms, laboratory abnormalities, events that are reported through the EAE system, and any grade event that leads to a treatment change from first day of study treatment to week 12.~Grade 3 = Severe Grade 4 = Life threatening Grade 5 = Death" (NCT00099632)
Timeframe: From first day of study treatment to week 12

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)5
21-day Lamivudine/Zidovudine (3TC/ZDV)1
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)2
21-day Lopinavir/Ritonavir (LPV/r)2

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Number of Participants With New PI-resistant Variants as Detected by Standard Composite (Bulk) Genotyping.

For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed. (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)0
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)0
21-day Lopinavir/Ritonavir (LPV/r)0

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Number of Participants With New Circulating NRTI-resistant Variants Detected by Standard Composite (Bulk) Genotyping.

For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed. (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)1
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)1
7-day Lopinavir/Ritonavir (LPV/r)1
21-day Lopinavir/Ritonavir (LPV/r)0

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Number of Participants With New Circulating Nonnucleoside Reverse Transcriptase Inhibitor (NNRTI)-Resistant Variants as Detected by Standard Composite (Bulk) Genotyping

"For the 7-day treatment duration group, only the genotype results from weeks 3 and 7 contributed to the primary endpoint; For the 21-day treatment duration groups, only the genotype results from weeks 5 and 9 contributed to primary endpoint.~10 participants who did not have resistance samples available were excluded from the primary endpoint analysis." (NCT00099632)
Timeframe: 2 and 6 weeks after completion of treatment

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)1
21-day Lamivudine/Zidovudine (3TC/ZDV)0
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)3
21-day Lopinavir/Ritonavir (LPV/r)1

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Number of Participants Who Discontinued Study Treatment Prematurely

participants assigned to 7-day treatment arm and 21-day treatment arm were supposed to stay in study treatment for 7 days and 21 days respectively. (NCT00099632)
Timeframe: From first day of study treatment to last day of study treatment (up to 21 days)

Interventionparticipants (Number)
7-day Lamivudine/Zidovudine (3TC/ZDV)0
21-day Lamivudine/Zidovudine (3TC/ZDV)2
7-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
21-day Emtricitabine/Tenofovir Disoproxil Fumarate (FTC/TDF)0
7-day Lopinavir/Ritonavir (LPV/r)0
21-day Lopinavir/Ritonavir (LPV/r)5

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Number of Participants Who Experienced Virological Failure Defined as Confirmed HIV-1 RNA Value of at Least 10,000 Copies Per/ml Recorded on Two Consecutive Separate Occasions After 24 Weeks of Treatment (Initial Therapy or Restart)

This was part of the primary outcome measure that was a composite endpoint that included confirmed HIV-1 RNA value of at least 10,000 copies per/ml recorded on two consecutive separate occasions after 24 weeks of treatment (initial therapy or restart). (NCT00102960)
Timeframe: Virological failure was assessed from randomization through the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy10
Early Therapy 40 Weeks1
Early Therapy 96 Weeks1

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Time From Randomization to Starting or Needing to Start Continuous Therapy

Time from randomization to starting (deferred therapy Arm) or needing to start continuous therapy (early therapy 40 or 96 weeks) (NCT00102960)
Timeframe: 4.8 years

InterventionWeeks (Median)
Deferred Therapy20
Early Therapy 40 Weeks33
Early Therapy 96 Weeks70

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Time to Death Alone or Death Plus Life Threatening Stage C Events or HIV Events Associated With Permanent End-organ Damage.

This was a composite endpoint in which the number of children experiencing the events is reported. The number of participants experiencing the events did not reach the 50% survival and thus median time-to-event is not be presented. Therefore, we report the number of participants experiencing the events per Arm. (NCT00102960)
Timeframe: 4.8 years

InterventionParticipants (Count of Participants)
Deferred Therapy34
Early Therapy 40 Weeks18
Early Therapy 96 Weeks13

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Time to Failure of First Line Therapy or Death

To compare time to failure of first line ART (due to clinical, virological or immunological disease progression, or regimen-limiting ART toxicities) or death among three randomized arms (infants who receive early ART in Arms 2 and 3 and infants in whom ART is deferred until clinical or immunological disease progression in Arm 1) during the study (up to 4.8 years). The number of participants experiencing the events did not reach the 50% survival and thus median time-to-event is not be presented. Therefore we report the number of participants experiencing the events per Arm. (NCT00102960)
Timeframe: From date of randomization up to failure of first-line therapy or death from any cause, whichever came first, assessed up to 4.8 years

InterventionParticipants (Count of Participants)
Deferred Therapy48
Early Therapy up to 40 Weeks32
Early Therapy up to 96 Weeks26

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Time to First Hospitalization

To compare time to first hospitalization in the three randomized arms (infants who received early ART in Arms 2 and 3 and those who received deferred ART in Arm 1). Not all participants were hospitalized and thus the upper limits could not be evaluated. (NCT00102960)
Timeframe: From randomization up to 4.8 years

InterventionWeeks (Median)
Deferred Therapy73.1
Early Therapy 40 WeeksNA
Early Therapy 96 WeeksNA

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Total Occurrence of Grade 3 or 4 Laboratory Events

(NCT00102960)
Timeframe: From randomization up to 4.8 years

InterventionCount of events (Number)
Deferred Therapy35
Early Therapy 40 Weeks44
Early Therapy 96 Weeks33

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Number of Participants Who Experienced Immunological Failure Defined as Failure of CD4% to Reach 20% or CD4% Falls Below 20% on Two Occasions, Within 4 Weeks, at Any Time After the First 24 Weeks of Therapy (Initial Therapy or Restart)

This was part of the primary outcome measure above. The primary outcome was a composite endpoint. The primary outcome analysis only considered the initially enrolled children that were 377 in total (ART-Deferred n=125, Early therapy 40 weeks n=126 and Early therapy 96 weeks n=126). This was part of the primary outcome measure that was a composite endpoint. (NCT00102960)
Timeframe: This outcome was assessed from the date of randomization to immunological failure. Immunological failure was assessed in the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy9
Early ART for 40 Weeks14
Early Therapy for 96 Weeks11

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Total Occurrence of Grade 3 or 4 Clinical Events

This was a secondary outcome measure that assessed the total count of Grade 3 or 4 (clinical or laboratory) adverse events. (NCT00102960)
Timeframe: 4.8 years

InterventionCount of events (Number)
Deferred Therapy170
Early Therapy 40 Weeks118
Early Therapy 96 Weeks88

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Duration of Hospitalisation

This is the total number of days spent in hospital by the participants and is reported per arm (NCT00102960)
Timeframe: 4.8 years, the study duration

InterventionDays (Number)
Deferred Therapy1018
Early Therapy 40 Weeks533
Early Therapy 96 Weeks414

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Hospitalization Rates

Hospitalisation rates in the three arms enrolled in the CHER study (NCT00102960)
Timeframe: 4.8 years

InterventionEvents per 100 person years (Number)
Deferred Therapy27.6
Early Therapy 40 Weeks16.4
Early Therapy 96 Weeks14.2

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Number of Children Experiencing Severe CDC Stage B or Stage C Disease or Death (Cumulative After 3.5 Years)

The outcome measure is defined as a number because it represents the number of children that experienced severe CDC Stage B or Stage C disease or death as defined in the outcome measure title above (NCT00102960)
Timeframe: Occurrence of severe CDC Stage B or Stage C disease or death (cumulative after 3.5 years), whichever came first, was assessed from randomization up to at least 3.5 years.

InterventionParticipants (Count of Participants)
Deferred Therapy41
Early Therapy 40 Weeks28
Early Therapy 96 Weeks21

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Number of Participants Who Experienced Clinical Failure (Defined as Development of Severe CDC Stage B or Stage C Disease.) on Therapy.

This included development of severe CDC Stage B or Stage C disease.This was part of the primary outcome measure that was a composite endpoint (NCT00102960)
Timeframe: Clinical failure on therapy was assessed at each visit for the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy8
Early Therapy 40 Weeks6
Early Therapy 96 Weeks5

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Number of Participants Who Experienced Regimen-limiting ART Drug Toxicity

Development of toxicity requiring more than one drug substitution within the same class or a switch to a new class of drugs (regimen-limiting toxicity failure) or requiring a permanent treatment discontinuation. This was part of the primary outcome measure that was a composite endpoint. (NCT00102960)
Timeframe: Regimen limiting drug toxicity was monitored from randomization up to the entire study duration of 4.8 years.

InterventionParticipants (Count of Participants)
Deferred Therapy0
Early Therapy 40 Weeks0
Early Therapy 96 Weeks0

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The Proportion of Women With Any New ZDV, ddI, or LPV/r Resistance Mutations.

(NCT00109590)
Timeframe: At Week 5 postpartum (ZDV) and at the first timepoint with viral load >=500 copies/ml after treatment discontinuation (ddI and LPV/r).

,,
Interventionpercent of participants (Number)
The proportion of women with new ZDV resistanceThe proportion of women with new ddI resistanceThe proportion of women with new LPV/r resistance
Arm A : LPV/r x 7d000
Arm B : no LPV/r1.7800
Arm C: LPV/r x 30d000

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Proportion of Women With New NVP Resistance Mutation Within 8 Weeks Postpartum Who Had a NVP Resistance Mutation Detected at 72 Weeks Postpartum.

Resistance mutations as identified by OLA in plasma samples or PBMC at 72 weeks postpartum amongst women who had new NVP resistance mutations within 8 weeks postpatrum. These results were based on the 13 women who developed a new NVP resistance mutation in the first 8 weeks postpartum. For the primary outcome measure 1, one particpant in arm A was unavailable for follow-up after week 5 and was conservatively imputed to have developed resistance mutation. (NCT00109590)
Timeframe: within 72 weeks postpartum

,,
Interventionparticipants (Number)
OLA in plasma samplesOLA in PBMC
Arm A : LPV/r x 7d00
Arm B : no LPV/r00
Arm C: LPV/r x 30d01

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The Proportion of Women Who Develop One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay in Plasma (Sampling Was Done at Days 10,21,30, and Weeks 5,6, and 8 Postpartum).

The incidence of new NVP resistance mutation in plasma HIV within 8 weeks postpartum in each randomized arm was estimated using an exact binomial confidence interval. If a resistance mutation was detected at any of the timepoints then an endpoint was met. Samples with VL <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml (e.g.missed visit), it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: within 8 weeks postpartum.

Interventionpercent of participants (Number)
Arm A : LPV/r x 7d7.1
Arm B : no LPV/r12.5
Arm C: LPV/r x 30d5.3

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The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations for the Subgroup of Women With Plasma HIV RNA >= 500 Copies/ml At Entry

The incidence of new NVP resistance mutations at day 10 or week 6 postpartum in each randomized arm. Samples with viral load <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: at Day 10 or Week 6 postpartum.

Interventionpercent of participants (Number)
Arm A: LPV/r x 7d4.9
Arm B: no LPV/r9.5
Arm C : LPV/r x 30d7.0

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The Proportion of Women in Each Randomized Arm Who Have One or More New NVP Resistance Mutations as Identified by Consensus Sequencing or Oligonucleotide Ligation Assay (OLA) in Plasma

The incidence of new NVP resistance mutations at day 10 or week 6 postpartum in each randomized arm. Samples with viral load <500 copies/mL were considered free of mutations. If a resistance result was missing for reasons other than VL <500 copies/ml it was conservatively imputed as resistant in the primary analysis. (NCT00109590)
Timeframe: at Day 10 or Week 6 postpartum.

Interventionpercent of participants (Number)
Arm A : LPV/r x 7d3.6
Arm B : no LPV/r7.1
Arm C : LPV/r x 30d5.3

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Area Under the Curve Pharmacokinetic Outcome for LPV/r. (AUC ug*hr/mL)

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug*hr/mL (Median)
Within 72 Hrs Ppm99.7
At Day 30 PpmNA

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Four (4) Hour Concentration Pharmacokinetic Outcome for LPV/r (C4hour ug/mL).

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm10.78
At Day 30 Ppm12.96

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Maximum Concentration Pharmacokinetic Outcome for LPV/r (Cmax ug/mL) .

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm11.2
At Day 30 PpmNA

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Median HIV-1 Viral Load at 24 Weeks Postpartum in Women

(NCT00109590)
Timeframe: at 24 weeks postpartum

Interventionlog10 copies/mL (Median)
Arm A : LPV/r x 7d4.3
Arm B : no LPV/r3.9
Arm C: LPV/r x 30d4.0

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Number of Women With Grade >=3 Events After Start of Study Treatment

Adverse events were graded using the Division of AIDS (DAIDS) Table for Grading > the Severity of Adult and Pediatric Adverse Events (December 2004). All grade 3 and higher signs, symptoms, and laboratory toxicities (and events of any grade that led to a change in study treatment) were included. (NCT00109590)
Timeframe: After start of study Treatment (postpartum)

Interventionparticipants (Number)
Arm A : LPV/r x 7d2
Arm B : no LPV/r0
Arm C: LPV/r x 30d2

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Pre-dose Concentration Pharmacokinetic Outcome for LPV/r (Cpredose ug/mL).

Data was analyzed with WinNonLin (Version 5.2, Pharsight, USA) using non-compartmental methods. The pharmacokinetic parameters were calculated using the linear-trapezoidal rule. Cpredose and C4hour at the two measurement times were compared within-subject using the Wilcoxon signed-rank test. (NCT00109590)
Timeframe: Within 72 hours postpartum and during the first 30 days postpartum

Interventionug/mL (Median)
Within 72 Hrs Ppm6.08
At Day 30 Ppm9.17

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Resistance Mutations in HIV Infected Infants

Resistance mutations as identified by consensus sequencing or OLA (NCT00109590)
Timeframe: 24 weeks postpartum

Interventionparticipants (Number)
Arm B : no LPV/r0
Arm C: LPV/r x 30d0

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Cumulative Treatment Failure Rate of Participants on First Line Antiretroviral Therapy Monitored by Primary Health Care Nurses (Investigative Arm)is Not Inferior to the Cumulative Treatment Failure Rate of Participants Monitored by Doctors (Control Arm).

Cumulative treatment failure is a composite endpoint made up of death, virological failure, toxicity failure and protocol-defined loss to follow-up failure. (NCT00255840)
Timeframe: 96 weeks

InterventionPercentage of participants (Number)
Antiretroviral Therapy Monitored by Medical Officer44
Antiretroviral Therapy Managed by Primary Health Care Nurse48

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Number of Participants With Virologic Suppression

Suppression of the plasma HIV-1 RNA level to less than 400 copies per milliliter (NCT00270296)
Timeframe: Throughout study, including breastfeeding, assessed up to 24 months

InterventionParticipants (Count of Participants)
TZV Arm274
Kaletra Arm256
NVP Arm160

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Number of HIV+ Infants

Number of infants with HIV-positive status (NCT00270296)
Timeframe: Throughout study, including breastfeeding, assessed up to 24 months

InterventionInfants (Number)
TZV Arm6
Kaletra Arm1
NVP Arm1

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Time From Randomization to Death

Results report 2nd percentile of time from randomization to death (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

InterventionWeeks (Number)
Coh I: NVP11
Coh I: LPV/r3
Coh II: NVP2
Coh II: LPV/r83

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Percent of Participants With Treatment Failure, Defined as a Confirmed Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment

Treatment failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR permanent discontinuation of the randomized NNRTI or PI component of study treatment at or prior to 24 weeks of treatment for any reason including death. Results report percent of participants reaching a treatment failure endpoint by week 24 calculated using the Kaplan-Meier method. (NCT00307151)
Timeframe: Earlier of 24 weeks or date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of participants (Number)
Coh I: NVP39.6
Coh I: LPV/r21.7
Coh II: NVP40.8
Coh II: LPV/r19.3

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Percent of Participants Experiencing Virologic Failure

Virologic failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR death on or before 24 weeks. Results report percent of participants reaching a virologic failure endpoint by week 24 calculated using the Kaplan-Meier method. (NCT00307151)
Timeframe: Earlier of 24 weeks or date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of participants (Number)
Coh I: NVP27.4
Coh I: LPV/r10.4
Coh II: NVP28.6
Coh II: LPV/r12.9

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Number of Participants Developing New NRTI, NNRTI or PI-resistant Virus

Numbers of participants developing new NRTI, NNRTI or PI-resistant virus after reaching a virologic failure endpoint (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

Interventionparticipants (Number)
Coh I: NVP16
Coh I: LPV/r1
Coh II: NVP10
Coh II: LPV/r4

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Change in CD4 Percent From Entry to Week 48

Change was calculated as CD4 percent at week 48 minus entry CD4 percent (last CD4 percent before randomization date). Only subjects who reached 48 weeks of follow-up before DSMB decisions to unblind each Cohort were included in summary. (NCT00307151)
Timeframe: 48 weeks if before date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

InterventionPercent of CD4 (Mean)
Coh I: NVP13.9
Coh I: LPV/r12.0
Coh II: NVP15.2
Coh II: LPV/r14.3

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Time From Start of Study Treatment to First New Grade >=3 Lab Abnormality, Sign or Symptom Occurring on Study Treatment

Safety events include lab abnormalities, signs or symptoms of grade 3 or higher. Events were graded according to the Division of AIDS Table for Grading Severity of Adult and Pediatric Adverse Events, Version 1.0. Events defined as new if first occurrence was after initiation of study treatment or if severity increased from entry and while on the NNRTI or PI component of study treatment. (NCT00307151)
Timeframe: On randomized NNRTI or PI component of study treatment and until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009; Coh II: October 27, 2010)

,,,
InterventionWeeks (Number)
10th percentile25th percentile
Coh I: LPV/r836
Coh I: NVP424
Coh II: LPV/r412
Coh II: NVP34

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Time From Randomization to Virologic Failure

Virologic failure is defined as the earlier of a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR a confirmed viral rebound >4000 copies/mL after week 24 OR death. (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

,,,
InterventionWeeks (Number)
5th percentile10th percentile
Coh I: LPV/r1624
Coh I: NVP1212
Coh II: LPV/r1624
Coh II: NVP1216

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Time From Randomization to Treatment Failure, Defined as Virologic Failure or Permanent Discontinuation of the Randomized NNRTI or PI Component of Study Treatment

Treatment failure is defined as a confirmed plasma HIV-1 RNA level that is <1 log10 copies/mL below the study entry value at 12 to 24 weeks after treatment is initiated OR a confirmed plasma HIV-1 RNA level >400 copies/mL at 24 weeks OR a confirmed viral rebound >4000 copies/mL after week 24 OR permanent discontinuation of the randomized NNRTI or PI component of study treatment for any reason including death. (NCT00307151)
Timeframe: Until date of DSMB decision to unblind Cohort results (Coh I: April 20, 2009 - median follow-up 48 weeks and range 0 - 125 weeks; Coh II: October 27, 2010 - median follow-up 72 weeks and range from 0 to 204 weeks)

,,,
InterventionWeeks (Number)
10th percentile25th percentile
Coh I: LPV/r436
Coh I: NVP1216
Coh II: LPV/r1436
Coh II: NVP416

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Patients With Plasma HIV RNA < 50 Copies/mL

The number of participants with plasma HIV RNA < 50 copies/mL (NCT00344461)
Timeframe: 96 weeks.

InterventionParticipants (Count of Participants)
Single Group (TDF/FTC & NVP)32

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Patients With Plasma HIV RNA < 400 Copies/mL

The number of participants with plasma HIV RNA < 400 copies/mL (NCT00344461)
Timeframe: 96 weeks

InterventionParticipants (Count of Participants)
Nevirapine, FTC, Tenofovir32

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Patients With Grade 2, 3 and 4 Adverse Events and Laboratory Toxicities

The number of participants with grades 2,3 and 4 adverse events and laboratory toxicities. (NCT00344461)
Timeframe: Protocol length is 96 weeks

InterventionParticipants (Count of Participants)
Nevirapine, FTC, Tenofovir13

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Number of Participants With Sustained Virologic Response

The primary outcome is sustained Virologic response, defined as HIV-1 RNA <500 copies/mL until trial completion at 96 weeks. (NCT00344461)
Timeframe: 96 Weeks

InterventionParticipants (Count of Participants)
Single Group (TDF/FTC & NVP)33

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Changes in CD4 Cell Count From Baseline and Week 96

To determine the mean change from Baseline in CD4 cell count to week 96. (NCT00344461)
Timeframe: Baseline to week 96

Interventionpercentage of CD4 Increase (Mean)
Nevirapine, FTC, Tenofovir252

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Change in Plasma HIV RNA From Baseline to Week 96

Percent Change From Baseline in Plasma HIV RNA at 96 weeks (NCT00344461)
Timeframe: Baseline to week 96

Interventionpercentage of change (Mean)
Nevirapine, FTC, Tenofovir3.32

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Proportion of Patients With VL < 400 Copies/ml

VL <400 copies/mL among observed patients on treatment at each visit, with the final visit at Week 144 or end of trial (EOT) (NCT00389207)
Timeframe: From baseline to Weeks 4, 8, 12, 24, 36, 48, 60, 72, 84, 96, 108, 120, 132 and 144/EOT

,
InterventionProportion of patients (Number)
Proportion with VL<400 copies /mL at Week 4Proportion with VL<400 copies /mL at Week 8Proportion with VL<400 copies /mL at Week 12Proportion with VL<400 copies /mL at Week 24Proportion with VL<400 copies /mL at Week 36Proportion with VL<400 copies /mL at Week 48Proportion with VL<400 copies /mL at Week 60Proportion with VL<400 copies /mL at Week 72Proportion with VL<400 copies /mL at Week 84Proportion with VL<400 copies /mL at Week 96Proportion with VL<400 copies /mL at Week 108Proportion with VL<400 copies /mL at Week 120Proportion with VL<400 copies /mL at Week 132Proportion with VL<400 copies /mL at Week 144/EOT
Atazanvir/Ritonavir0.2870.6790.8340.9560.9660.9770.9880.9880.9940.9871.0000.9940.9930.986
Nevirapine QD+BID0.3650.7140.8560.9240.9680.9850.9930.9960.9881.0000.9961.0000.9960.991

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Time to Treatment Response (First Confirmed VL<50 Copies/mL)

Time to treatment response was defined as the time from start of treatment until the first measurement of the first confirmed virological response (NCT00389207)
Timeframe: baseline to week 144

Interventionweeks (Median)
Nevirapine QD12.00
Nevirapine BID12.14
Nevirapine QD+BID12.00
Atazanvir/Ritonavir23.71

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Proportion of Patients Reporting CNS (Central Nervous System) Side Effects of Any Severity

Proportion of Patients reporting CNS (central nervous system) side effects of any severity (NCT00389207)
Timeframe: week 148

Interventionparticipants (Number)
Nevirapine QD41
Nevirapine BID41
Atazanvir/Ritonavir37

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Proportion of Patients Reporting Hepatic Events of Any Severity

Proportion of Patients reporting hepatic events of any severity (NCT00389207)
Timeframe: week 148

Interventionparticipants (Number)
Nevirapine QD26
Nevirapine BID24
Atazanvir/Ritonavir92

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Proportion of Patients Reporting Rash of Any Severity

Proportion of Patients reporting rash of any severity (NCT00389207)
Timeframe: week 148

Interventionparticipants (Number)
Nevirapine QD75
Nevirapine BID64
Atazanvir/Ritonavir74

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Time to Loss of Virologic Response (Rebound)

Time to loss of virologic response (TLOVR) was defined as the time from start of treatment to the first measurement showing VL ≥ 50 copies/mL in the first virologic rebound, after having a confirmed virological response. (NCT00389207)
Timeframe: Baseline to week 144

Interventionweeks (Median)
Nevirapine QD143.86
Nevirapine BID143.21
Nevirapine QD+BID143.71
Atazanvir/Ritonavir143.00

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Time to Treatment Failure

Treatment failure is defined as the occurrence of the first of at least one of the following events: early discontinuation of trial drug, change in ARV therapy, failure to achieve an HIV RNA count < 50 copies/mL up to Visit 10 (week 48) or loss of virologic response (NCT00389207)
Timeframe: baseline to week 144

Interventionweeks (Median)
Nevirapine QD143.86
Nevirapine BID143.21
Nevirapine QD+BID143.71
Atazanvir/Ritonavir143.00

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Change in CD4+ Count From Baseline

Change in CD4+ cell count from baseline among patients on treatment at each visit, with the final visit at Week 144 or EOT (NCT00389207)
Timeframe: From baseline to Weeks 4, 8, 12, 24, 36, 48, 60, 72, 84, 96, 108, 120, 132 and 144/EOT

,
Interventioncells/mm^3 (Mean)
Change in CD4+ count to Week 4Change in CD4+ count to Week 8Change in CD4+ count to Week 12Change in CD4+ count to Week 24Change in CD4+ count to Week 36Change in CD4+ count to Week 48Change in CD4+ count to Week 60Change in CD4+ count to Week 72Change in CD4+ count to Week 84Change in CD4+ count to Week 96Change in CD4+ count to Week 108Change in CD4+ count to Week 120Change in CD4+ count to Week 132Change in CD4+ count to Week 144/EOT
Atazanvir/Ritonavir86.198.0110.9133.8163.4183.6208.2231.9246.4251.6267.2269.2281.3285.8
Nevirapine QD+BID77.2105.6120.3134.4160.1168.2184.8213.7223.0217.7231.2231.3243.4251.0

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Change in Framingham Score From Baseline

Change in the estimated risk of cardiovascular disease using the Framingham algorithm from baseline to after 48, 96 and 144 weeks, last observation carried forward (LOCF). The score is based on age, gender, systolic blood pressure, total cholesterol, high density lipoprotein cholesterol and smoking status. Scores range from 0 to 21 with higher scores indicating a greater risk. (NCT00389207)
Timeframe: From baseline to Weeks 48, 96 and 144/EOT

,
InterventionUnits on a scale (Mean)
Change in Framingham score to Week 48Change in Framingham score to Week 96Change in Framingham score to Week 144/EOT
Atazanvir/Ritonavir0.661.190.82
Nevirapine QD+BID0.500.931.14

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Change in Mental Health Summary (MHS) Score From Baseline

Quality of life (QoL) assessment by change in MHS score from baseline to after 48, 96 and 144 weeks (observed cases), from the Medical Outcomes Study HIV Health Survey (MOS-HIV), a 35-item self-administered questionnaire including 10 scales covering: health perceptions, pain, physical functioning, role functioning, social and cognitive functioning, mental health, energy/fatigue, health distress, and QoL. The MHS is a weighted average of the 10 scales and ranges from 0 to 100 with higher scores indicating better QoL. (NCT00389207)
Timeframe: From baseline to Weeks 48, 96 and 144/EOT

,
InterventionUnits on a scale (Mean)
Change in MHS score to Week 48Change in MHS score to Week 96Change in MHS score to Week 144/EOT
Atazanvir/Ritonavir4.524.894.70
Nevirapine QD+BID6.096.104.76

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Change in Physical Health Summary (PHS) Score From Baseline

QoL assessment by change in PHS score from baseline to after 48, 96 and 144 weeks (observed cases), from the MOS-HIV, a 35-item self-administered questionnaire including 10 scales covering: health perceptions, pain, physical functioning, role functioning, social and cognitive functioning, mental health, energy/fatigue, health distress, and QoL. The PHS is a weighted average of the 10 scales and ranges from 0 to 100 with higher scores indicating better QoL. (NCT00389207)
Timeframe: From baseline to Weeks 48, 96 and 144/EOT

,
InterventionUnits on a scale (Mean)
Change in PHS score to Week 48Change in PHS score to Week 96Change in PHS score to Week 144/EOT
Atazanvir/Ritonavir3.353.003.35
Nevirapine QD+BID3.343.192.22

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Change in the Calculated Glomerular Filtration Rate (GFR) at Week 48, 96 and 144

Calculations based on the MDRD algorithm. (NCT00389207)
Timeframe: From baseline to Week 48, 96, 144

,,,
InterventionmL/min/1.73 m^2 (Mean)
change baseline to week 48 (N=143, 128, 271, 173)change baseline to week 96 (N=130, 122, 252, 157)change baseline to week 144 (N=163, 168, 331, 174)
Atazanvir/Ritonavir-7.18-11.53-9.56
Nevirapine BID-5.92-10.02-6.33
Nevirapine QD-3.91-6.93-3.27
Nevirapine QD+BID-4.86-8.42-4.82

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Change of Cholesterol Values From Baseline to Week 48, 96, 144

Changes frombaseline in total cholesterol, LDL-cholesterol(LDL-c) and HDL (NCT00389207)
Timeframe: baseline to week 48, 96, 144

,,
Interventionmg/dL (Mean)
total cholesterol, week 48 (N=138,122,164)total cholesterol, week 96 (N=124,114,147)total cholesterol, week 144 (N=154,155,160)LDL-c, week 48 (N=136,117,159)LDL-c, week 96 (N=119,110,145)LDL-c, week 144 (N=151,150,157)HDL, week 48(N=138,122,164)HDL, week 96 (N=124,114,147)HDL, week 144(N=154,155,160)
Atazanvir/Ritonavir20.8429.9928.1310.5819.1917.613.494.745.73
Nevirapine BID29.5436.8730.6617.7021.6617.9511.5913.3310.47
Nevirapine QD29.2839.1733.1216.5421.9321.4212.0613.8612.61

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Change of hsCRP From Baseline to Week 48, 96, 144

Change of hsCRP from baseline to week 48, 96, 144 (NCT00389207)
Timeframe: baseline to week 48, 96, 144

,,
Interventionmg/L (Mean)
hsCRP, week 48 (N=142,126,173)hsCRP, week 96 (N=128,120,157)hsCRP, week 144 (N=160,164,174)
Atazanvir/Ritonavir-0.700.350.04
Nevirapine BID-0.67-0.79-0.02
Nevirapine QD-1.01-1.54-0.09

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Change of Total Cholesterol to HDL-cholesterol Ratio From Baseline to Week 48, 96, 144

Change of Total cholesterol to HDL-cholesterol ratio from baseline to week 48, 96, 144 (NCT00389207)
Timeframe: baseline to week 48, 96, 144

,,
Interventionratio (Mean)
total triglycerides, week 48 (N=138,122,164)total triglycerides, week 96 (N=124,114,147)total triglycerides, week 144 (N=154,155,160)
Atazanvir/Ritonavir0.200.280.17
Nevirapine BID-0.33-0.25-0.07
Nevirapine QD-0.37-0.22-0.24

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Change of Total Triglycerides From Baseline to Week 48, 96, 144

Change of total triglycerides from baseline to week 48, 96, 144 (NCT00389207)
Timeframe: baseline to week 48, 96, 144

,,
Interventionmg/dL (Mean)
total triglycerides, week 48 (N=138,120,164)total triglycerides, week 96 (N=124,113,147)total triglycerides, week 144 (N=153,153,159)
Atazanvir/Ritonavir36.2830.4527.11
Nevirapine BID1.675.356.11
Nevirapine QD0.089.34-3.46

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Changes of Apolipoprotein Values From Baseline to Week 48, 96, 144

Changes frombaseline apolipoprotein A1 & B (NCT00389207)
Timeframe: baseline to week 48, 96, 144

,,
Interventiong/L (Mean)
apolipoprotein A1, week 48 (N=134,121,156)apolipoprotein A1, week 96 (N=115,106,141)apolipoprotein A1, week 144 (N=144,140,148)apolipoprotein B, week 48 (N=134,120,156)apolipoprotein B, week 96 (N=115,106,141)apolipoprotein B, week 144 (N=144,139,148)
Atazanvir/Ritonavir0.080.070.060.030.030.03
Nevirapine BID0.230.230.140.03-0.000.05
Nevirapine QD0.230.230.160.000.000.01

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Genotypic Resistance Associated With Virologic Failure

Number of treatment-emergent drug-associated substitutions in patients with virological failure up to Week 48. The total number of genotypic mutations in those patients who were virologic failures is given, not the number of patients with mutations. (NCT00389207)
Timeframe: From baseline to Week 48

,
InterventionNumber of substitutions (Number)
Emtricitabine-associated substitutions at Week 48Tenofovir-associated substitutions at Week 48Nevirapine-associated substitutions at Week 48
Atazanvir/Ritonavir000
Nevirapine QD+BID211134

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Glycaemic Abnormalities

Number of patients with AE elevated serum glucose (NCT00389207)
Timeframe: From baseline to Week 144

,
InterventionPatients (Number)
Number with glycaemic abnormalitiesNumber without glycaemic abnormalities
Atazanvir/Ritonavir3190
Nevirapine QD+BID0376

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Lipodystrophy

Number of patients with AE lipodystrophy (NCT00389207)
Timeframe: From baseline to Week 144

,
InterventionPatients (Number)
Number with lipodystrophyNumber without lipodystrophy
Atazanvir/Ritonavir1192
Nevirapine QD+BID1375

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Non-scheduled Physician Visits

Cost effectiveness assessment by number of patients with non-scheduled physician visits (NCT00389207)
Timeframe: From baseline to Week 24, Week 24 to 48, Week 48 to 96, and Week 96 to 144/EOT

,
Interventionpatients (Number)
Number between baseline and Week 24Number between Week 24 and Week 48Number between Week 48 and Week 96Number between Week 96 and Wk 144/EOT
Atazanvir/Ritonavir35352835
Nevirapine QD+BID74455858

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Number of Patients Hospitalized

Cost effectiveness assessment by number of patients hospitalized (NCT00389207)
Timeframe: From baseline to Week 24, Week 24 to 48, Week 48 to 96, and Week 96 to 144/EOT

,
InterventionPatients (Number)
Number hospitalized between baseline and Week 24Number hospitalized between Week 24 and Week 48Number hospitalized between Week 48 and Week 96Number hospitalized between Week 96 and Wk 144/EOT
Atazanvir/Ritonavir2551
Nevirapine QD+BID8659

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Proportion of Patients With >= DAIDS Grade 2 Laboratory Abnormalities

(NCT00389207)
Timeframe: week 148

,,
Interventionparticipants (Number)
DAIDS 2 moderateDAIDS 3 severeDAIDS 4 potential lifethreatening
Atazanvir/Ritonavir72399
Nevirapine BID842815
Nevirapine QD74309

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Proportion of Patients With Virologic Failure at Week 48, 96, 144

(NCT00389207)
Timeframe: at Week 48, 96, 144

,,,
Interventionparticipants (Number)
virologic failure at Week 48virologic failure at Week 96virologic failure at Week 144
Atazanvir/Ritonavir251317
Nevirapine BID252528
Nevirapine QD201519
Nevirapine QD+BID454047

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Proportion of Patients With Virological Rebound With VL >=400 Copies/mL After CVR at Week 24, 48, 96, 144

The analyses of virologic rebound were performed on the original values at each visit(ORGV) rather than calculated results within time windows (CAL) (NCT00389207)
Timeframe: at Week 24, 48, 96, 144

,,,
Interventionparticipants (Number)
virologic rebound after CVR at Week 24virologic rebound after CVR at Week 48virologic rebound after CVR at Week 96virologic rebound after CVR at Week 144
Atazanvir/Ritonavir2225
Nevirapine BID2366
Nevirapine QD2334
Nevirapine QD+BID46910

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Proportion of Patients With Virological Rebound With VL >=50 Copies/mL After CVR (Confirmed Virological Response) at Week 24, 48, 96, 144

The analyses of virologic rebound were performed on the original values at each visit(ORGV) rather than calculated results within time windows (CAL) (NCT00389207)
Timeframe: at Week 24, 48, 96, 144

,,,
Interventionparticipants (Number)
virologic rebound after CVR at Week 24virologic rebound after CVR at Week 48virologic rebound after CVR at Week 96virologic rebound after CVR at Week 144
Atazanvir/Ritonavir5121015
Nevirapine BID2569
Nevirapine QD3448
Nevirapine QD+BID591017

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Proportion of Patients With VL < 50 Copies/ml

VL <50 copies/mL among observed patients on treatment at each visit, with the final visit at Week 144 or end of trial (EOT) for the patient (NCT00389207)
Timeframe: From baseline to Weeks 4, 8, 12, 24, 36, 48, 60, 72, 84, 96, 108, 120, 132 and 144/EOT

,
InterventionProportion of patients (Number)
Proportion with VL<50 copies /mL at Week 4Proportion with VL<50 copies /mL at Week 8Proportion with VL<50 copies /mL at Week 12Proportion with VL<50 copies /mL at Week 24Proportion with VL<50 copies /mL at Week 36Proportion with VL<50 copies /mL at Week 48Proportion with VL<50 copies /mL at Week 60Proportion with VL<50 copies /mL at Week 72Proportion with VL<50 copies /mL at Week 84Proportion with VL<50 copies /mL at Week 96Proportion with VL<50 copies /mL at Week 108Proportion with VL<50 copies /mL at Week 120Proportion with VL<50 copies /mL at Week 132Proportion with VL<50 copies /mL at Week 144/EOT
Atazanvir/Ritonavir0.090.250.4120.7790.830.8860.9010.9150.8960.9240.9680.9550.9470.929
Nevirapine QD+BID0.1070.3040.5150.8420.9070.9310.9590.9650.9720.980.9640.9760.9710.952

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Serum Lipid Abnormalities

Number of patients with AE elevated serum lipids (i.e. hypercholesterolaemia) (NCT00389207)
Timeframe: From baseline to Week 144

,
Interventionpatients (Number)
Number with serum lipid abnormalitiesNumber without serum lipid abnormalities
Atazanvir/Ritonavir4189
Nevirapine QD+BID9367

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Treatment Response at Week 144

Treatment response is defined as a viral load (VL) <50 copies/mL measured at two consecutive visits prior to Week 144 and without subsequent rebound or change of antiretroviral (ARV) therapy prior to Week 144. (NCT00389207)
Timeframe: From baseline to Week 144

,,,
Interventionparticipants (Number)
Number of respondersNumber of non-responders
Atazanvir/Ritonavir14350
Nevirapine BID11375
Nevirapine QD12167
Nevirapine QD+BID234142

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Treatment Response at Week 48

Treatment response is defined as a viral load (VL) <50 copies/mL measured at two consecutive visits prior to Week 48 and without subsequent rebound or change of antiretroviral (ARV) therapy prior to Week 48. (NCT00389207)
Timeframe: From baseline to Week 48

,,,
InterventionPatients (Number)
Number of respondersNumber of non-responders
Atazanvir/Ritonavir12667
Nevirapine BID12464
Nevirapine QD12662
Nevirapine QD+BID250126

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Treatment Response at Week 48 (TLOVR Algorithm)

Treatment response is defined as a VL <50 copies/mL measured at two consecutive visits up to Week 48 and without subsequent rebound or change of ARV therapy up to Week 48, based on time to loss of virologic response (TLOVR) algorithm, as a sensitivity analysis for the primary analysis. (NCT00389207)
Timeframe: From baseline to Week 48

,
InterventionPatients (Number)
Number of respondersNumber of non-responders
Atazanvir/Ritonavir14251
Nevirapine QD+BID261115

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Treatment Response at Week 96

Treatment response is defined as a viral load (VL) <50 copies/mL measured at two consecutive visits prior to Week 96 and without subsequent rebound or change of antiretroviral (ARV) therapy prior to Week 96. (NCT00389207)
Timeframe: From baseline to Week 96

,,,
Interventionparticipants (Number)
Number of respondersNumber of non-responders
Atazanvir/Ritonavir14944
Nevirapine BID12266
Nevirapine QD13157
Nevirapine QD+BID253123

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Treatment-emergent AIDS-defining Illness

Treatment-emergent AIDS-defining illness (tr.-emerg. AIDS-def.illness) including worsening during treatment (NCT00389207)
Timeframe: From baseline to Week 144

,
InterventionPatients (Number)
Number with tr.-emerg. AIDS-def.illnessNumber without tr.-emerg. AIDS-def.illness
Atazanvir/Ritonavir7186
Nevirapine QD+BID26350

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Treatment-emergent AIDS-defining Illness Leading to Death

Patients with an AIDS-defining illness leading to death broken out by treatment. Statistical analysis shows time to death from AIDS-defining illness. (NCT00389207)
Timeframe: From baseline to Week 144

,
InterventionPatients (Number)
Number with AIDS-def. illness leading to deathNumber without AIDS-def. illness leading to death
Atazanvir/Ritonavir0193
Nevirapine QD+BID3373

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Immunologic Failure

Immunologic treatment failure was defined as CD4% dropping below 15%, after a previous result greater than or equal to 15% (following along WHO Guidelines). (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing2
NVP-sparing1

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Incidence of Severe Adverse Events (Excluding Mortality)

(NCT00427297)
Timeframe: 2 years

Interventionevent (Number)
NVP-containing21
NVP-sparing6

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Viral Failure

Virologic treatment failure was defined as follow-up (at least 24 weeks after enrollment date) viral load > 400 copies. (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing2
NVP-sparing2

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Incidence of Mortality

Death during follow-up (NCT00427297)
Timeframe: 2 years

InterventionParticipants (Count of Participants)
NVP-containing4
NVP-sparing5

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Change in Fasting High Density Lipoprotein (HDL) Cholesterol Level

(NCT00552240)
Timeframe: baseline to week 48

Interventionmg/dl (Mean)
Nevirapine (NVP) Plus Truvada9.6
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada3.5

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Number of Participants With Virologic Success (FDA Definition)

HIV viral load <50 copies/ml measured in the Week 48 window whereby patients withdrawing early and patients without a Week 48 assessment are considered failures. Includes all participants in full analysis set (FAS). (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
RespondersNonresponders
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada4829
Nevirapine (NVP) Plus Truvada4233

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Number of Patients With Virologic Rebound to >400 Copies/ml

HIV viral load >400 copies/ml on two consecutive measurements separated by at least 2 weeks, after confirmed virologic response (2 consecutive HIV viral load values < 50 copies/ml) (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
Rebound following responseNo rebound following response
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada663
Nevirapine (NVP) Plus Truvada255

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Proportion of Patients With DAIDS Grade >= 2 Laboratory Abnormalities

(NCT00552240)
Timeframe: baseline to week 52

,
Interventionparticipants (Number)
Grade 2 moderateGrade 3 severeGrade 4 potential lifethreatening
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada3173
Nevirapine (NVP) Plus Truvada2587

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Number of Participants With Loss of Virologic Response Following Confirmed Virologic Response

HIV viral load > 50 copies/ml on two consecutive measurements separated by at least 2 weeks, after confirmed virologic response (2 consecutive HIV viral load values < 50 copies/ml) (NCT00552240)
Timeframe: baseline to week 24 and week 48

,
InterventionParticipants (Number)
At week 24At week 48
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada49
Nevirapine (NVP) Plus Truvada12

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 2 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 2

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada5639
Nevirapine (NVP) Plus Truvada6627

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Change in Fasting Total Cholesterol to High Density Lipoprotein (HDL) Ratio

(NCT00552240)
Timeframe: baseline to week 48

Interventionratio (Mean)
Nevirapine (NVP) Plus Truvada-0.38
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada-0.02

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Change in CD4+ Cell Count From Baseline to Week 8.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 8

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada111.9
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada90.5

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Change in CD4+ Cell Count From Baseline to Week 6.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 6

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada87.2
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada78.4

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Change in CD4+ Cell Count From Baseline to Week 48.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 48

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada155.1
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada160.4

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Change in CD4+ Cell Count From Baseline to Week 4.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 4

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada76.4
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada63.0

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Change in CD4+ Cell Count From Baseline to Week 36.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 36

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada147.6
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada120.5

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Change in CD4+ Cell Count From Baseline to Week 24.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 24

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada131.8
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada132.5

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Change in CD4+ Cell Count From Baseline to Week 2.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 2

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada62.6
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada61.0

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AIDS Progression and Death: Number of Patients With a Treatment-emergent AIDS Defining Illness or an AIDS-defining Illness Leading to Death

"AIDS defining illnesses include: Aspergillosis, Bartonellosis, Candidiasis, Cervical cancer, Chagas disease, Coccidiodomycosis, Cryptococcosis, Cytomegalovirus retinus, encephalopathy, Herpes Simplex Virus, Histoplasmosis, Isosporiasis, Kaposi's sarcoma, Leishmaniasis, Microsporidiosis, Mycobacterium avium complex, mycobacterium (non-tuberculous), Nocardiosis, Pneumocystis carinii pneumonia, Pneumonia, Progressive Multifocal Leukoencephalopathy, Rhodococcus equi, Salmonella, Toxoplasmosis, Wasting.~Number of cases (no time-to analysis was performed due to small numbers)." (NCT00552240)
Timeframe: baseline to week 48

InterventionParticipants (Number)
Nevirapine (NVP) Plus Truvada1
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada3

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Change in Fasting Plasma Triglycerides Level

(NCT00552240)
Timeframe: baseline to week 48

Interventionmg/dl (Mean)
Nevirapine (NVP) Plus Truvada-4.7
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada8.4

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Change in Fasting Plasma Total Cholesterol Level

(NCT00552240)
Timeframe: baseline to week 48

Interventionmg/dl (Mean)
Nevirapine (NVP) Plus Truvada18.2
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada13.8

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Change in Fasting Low Density Lipoprotein (LDL)Cholesterol Level

(NCT00552240)
Timeframe: baseline to week 48

Interventionmg/dl (Mean)
Nevirapine (NVP) Plus Truvada8.7
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada6.9

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Change in Glomerular Filtration Rate (GFR) From Baseline to Week 48

using 4-variable Modification of Diet in Renal Disease (MDRD) formula (NCT00552240)
Timeframe: baseline to week 48

Interventionml/min/1.73m^2 (Mean)
Nevirapine (NVP) Plus Truvada-0.06
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada-12.81

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Change in Framingham Score

Framingham prediction of 10-year risk of Coronary Heart Disease (CHD) outcomes (myocardial infarction [MI] or CHD death) based on the patient's gender, age, systolic blood pressure, total cholesterol, HDL-c and smoking status. The scale for the estimated risk ranges from 0 to 30%. (NCT00552240)
Timeframe: baseline to week 48

Interventionpercent 10-year risk (Mean)
Nevirapine (NVP) Plus Truvada-0.09
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada0.14

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Percentage Adherence by Pill Count

Number of pills not returned / number of treatment days in percent (%) (NCT00552240)
Timeframe: baseline to week 48

Interventionpercentage adherence (Mean)
Nevirapine (NVP) Plus Truvada94.3
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada97.0

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Proportion of Patients Reporting CNS Side Effects of Any Severity

(NCT00552240)
Timeframe: baseline to week 52

Interventionparticipants (Number)
Nevirapine (NVP) Plus Truvada25
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada23

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Proportion of Patients Reporting Hepatic Events of Any Severity

(NCT00552240)
Timeframe: baseline to week 52

Interventionparticipants (Number)
Nevirapine (NVP) Plus Truvada5
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada24

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Proportion of Patients Reporting Rash of Any Severity

(NCT00552240)
Timeframe: baseline to week 52

Interventionparticipants (Number)
Nevirapine (NVP) Plus Truvada21
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada19

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Time to Virologic Response (First Confirmed Viral Load < 50 Copies/ml), All Participants

Time to response whereby patients withdrawing early were censored after their withdrawal (NCT00552240)
Timeframe: baseline to week 48

Interventiondays (Median)
Nevirapine (NVP) Plus Truvada57
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada84

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Time to Virologic Response (First Confirmed Viral Load < 50 Copies/ml), Only Participants With Confirmed Viral Load < 50 Copies/ml

(NCT00552240)
Timeframe: baseline to week 48

Interventiondays (Median)
Nevirapine (NVP) Plus Truvada55
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada84

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Incidence of Patients With AIDS Progression at Each Visit

Cumulative incidence of patients with AIDS progression are shown (NCT00552240)
Timeframe: baseline to week 52

,
Interventionparticipants (Number)
week 0week 2week 4week 6week 8week 12week 24week 36week 48week 50End of Study Visit
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada00011233333
Nevirapine (NVP) Plus Truvada00000000112

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 12 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 12

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada6377
Nevirapine (NVP) Plus Truvada56613

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 2 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 2

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada17519
Nevirapine (NVP) Plus Truvada24447

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 24 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 24

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada63311
Nevirapine (NVP) Plus Truvada51618

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 36 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 36

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada59117
Nevirapine (NVP) Plus Truvada54318

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 4 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 4

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada31415
Nevirapine (NVP) Plus Truvada382710

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 48 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada54221
Nevirapine (NVP) Plus Truvada43131

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 6 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 6

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada442310
Nevirapine (NVP) Plus Truvada402114

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Number of Participants With HIV Viral Load < 400 Copies/ml at Week 8 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 8

,
InterventionParticipants (Number)
HIV viral load < 400 copies/mlHIV viral load ≥ 400 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada58154
Nevirapine (NVP) Plus Truvada481116

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 12 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 12

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada43277
Nevirapine (NVP) Plus Truvada422013

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Change in CD4+ Cell Count From Baseline to Week 12.

Patients on-treatment, data within time windows (NCT00552240)
Timeframe: baseline to week 12

Interventioncells/mm^3 (Mean)
Nevirapine (NVP) Plus Truvada123.1
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada102.2

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 24 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 24

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada61511
Nevirapine (NVP) Plus Truvada48918

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 36 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 36

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada55517
Nevirapine (NVP) Plus Truvada53418

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 4 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 4

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada10625
Nevirapine (NVP) Plus Truvada125310

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 48

HIV viral load <50 copies/ml measured at Week 48 among observed cases on-treatment. (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
RespondersNonresponders
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada488
Nevirapine (NVP) Plus Truvada422

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 48 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada48821
Nevirapine (NVP) Plus Truvada42231

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 6 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 6

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada145310
Nevirapine (NVP) Plus Truvada233814

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Number of Participants With HIV Viral Load < 50 Copies/ml at Week 8 of Treatment

Results within time windows, patients on-treatment (NCT00552240)
Timeframe: baseline to week 8

,
InterventionParticipants (Number)
HIV viral load < 50 copies/mlHIV viral load ≥ 50 copies/mlMissing data
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada23504
Nevirapine (NVP) Plus Truvada342516

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Number of Participants With Virologic Response (VR)

VR is defined as HIV viral load of <50 copies/ml measured at two consecutive visits PRIOR TO Week 48 and without subsequent rebound or change of ARV therapy prior to Week 48. (NCT00552240)
Timeframe: baseline to week 48

,
Interventionparticipants (Number)
RespondersNonresponders
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada5027
Nevirapine (NVP) Plus Truvada4629

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Number of Participants With Virologic Response According to the Time to Loss of Virologic Response (TLOVR) Algorithm

HIV viral load <50 copies/ml measured at two consecutive visits UP TO Week 48 and without subsequent rebound or change of ARV therapy up to Week 48. (NCT00552240)
Timeframe: baseline to week 48

,
InterventionParticipants (Number)
RespondersNonresponders
Atazanavir Plus Ritonavir (ATV/r) Plus Truvada5126
Nevirapine (NVP) Plus Truvada4827

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Kaplan -Meier Estimate of Cumulative Probability of Permanent Discontinuation of Study Medication

(NCT00561925)
Timeframe: week 0 to 144

,
Interventioncumulative probability (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <6Interval Week 6 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <24Interval Week 24 to <32Interval Week 32 to <40Interval Week 40 to <48Interval Week 48 to <60Interval Week 60 to <72Interval Week 72 to <84Interval Week 84 to <96Interval Week 96 to <108Interval Week 108 to <120Interval Week 120 to <132Interval Week 132 to <144
NVP IR0.0000.0000.0340.0670.0810.0930.1130.1300.1560.1720.1920.2020.2130.2290.2430.2670.2750.289
NVP XR0.0000.0000.0260.0460.0590.0670.0830.1150.1390.1560.1620.1760.1880.2060.2180.2320.2360.244

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Kaplan-Meier Estimates of the Proportions of Patients Without Loss of Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

(NCT00561925)
Timeframe: week 0 to 144

,
Interventionproportion of participants (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <6Interval Week 6 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <24Interval Week 24 to <32Interval Week 32 to <40Interval Week 40 to <48Interval Week 48 to <60Interval Week 60 to <72Interval Week 72 to <84Interval Week 84 to <96Interval Week 96 to <108Interval Week 108 to <120Interval Week 120 to <132Interval Week 132 to <144Interval Week 144 to <168
NVP IR 200mg BID10.840.8380.8340.8340.8320.830.8220.8060.7920.7770.7590.7330.7130.6860.6620.650.630.61
NVP XR 400mg QD10.8650.8650.8650.8630.8610.8590.8480.8320.8160.8080.7880.7660.7450.7190.6970.6810.6710.66

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Occurrence of Elevations in Laboratory Measurement by DAIDS Grade

(NCT00561925)
Timeframe: until last patient completed 144 weeks (up to 193 weeks)

,,,
Interventionparticipants (Number)
DAIDS grade 3 or 4 AEsDAIDS grade 4 AEs
IR-IR/XR7111
NVP IR5317
NVP XR11125
XR-IR/XR83

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Proportion of Sustained Virologic Response at Week 144 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 144 using LLOQ = 50 copies/mL (NCT00561925)
Timeframe: week 144

,
Interventionparticipants (Number)
ResponderNon responder
NVP IR 200mg BID296210
NVP XR 400mg QD321184

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Comparison of CD4+ Cell Count (Cells/Cubic Millimeter) Change From Baseline at Week 144, Full Analysis Set Population

(NCT00561925)
Timeframe: baseline, week 144

Interventioncells/cubic millimeter (Mean)
NVP IR 200mg BID239.3
NVP XR 400mg QD270.7

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Occurrence of Rashes

Frequency of patients with drug related rash events by functional grouping (NCT00561925)
Timeframe: until last patient completed 144 weeks (up to 193 weeks)

,,,
Interventionparticipants (Number)
rash group Irash group IIrash group IIArash group IIIrash group IV
IR-IR/XR63100
NVP IR96430
NVP XR1113550
XR-IR/XR00000

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Comparison of HIV-1 Viral Load (log10 Copies/mL) Change From Baseline at Week 144, Full Analysis Set Population

(NCT00561925)
Timeframe: baseline, week 144

Interventionlog10 copies/mL (Mean)
NVP IR 200mg BID-2.7
NVP XR 400mg QD-2.8

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Occurrence of Hepatic Events

Frequency of patients with hepatitis symptoms (NCT00561925)
Timeframe: until last patient completed 144 weeks (up to 193 weeks)

Interventionparticipants (Number)
NVP IR10
NVP XR8
IR-IR/XR2
XR-IR/XR0

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Relative Bioavailability Trough C_pre,ss,1

Relative bioavailability measured of trough concentrations. Analysis based on adjusted by-treatment geometric means, the adjusted geometric mean ratio of NVP XR : NVP IR and it's 90% confidence interval with p-value and the inter-individual geometric coefficient of variation. (NCT00561925)
Timeframe: week 132

Interventionng/mL (Geometric Mean)
NVP IR4567.03
NVP XR3634.26

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Comparison of Proportion of Virologic Response at Week 48 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Primary endpoint was the number of patients with a sustained virologic response through week 48 using LLOQ = 50 copies/mL (NCT00561925)
Timeframe: week 48

,
Interventionparticipants (Number)
ResponderNon responder
NVP IR 200mg BID384122
NVP XR 400mg QD40996

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Kaplan -Meier Estimate of Cumulative Probability of Clinical Hepatic Events

(NCT00561925)
Timeframe: week 0 to 72

,
Interventioncumulative probability (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <6Interval Week 6 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <24Interval Week 24 to <32Interval Week 32 to <40Interval Week 40 to <48Interval Week 48 to <60Interval Week 60 to <72Interval Week >=72
NVP IR0.0000.0000.0120.0220.0240.0260.0260.0260.0260.0290.0290.0320.038
NVP XR0.0000.0020.0100.0160.0180.0180.0180.0200.0220.0220.0220.0220.026

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Kaplan -Meier Estimate of Cumulative Probability of Grade 3 or 4 ALT/AST Abnormalities

(NCT00561925)
Timeframe: week 0 to 72

,
Interventioncumulative probability (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <6Interval Week 6 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <24Interval Week 24 to <32Interval Week 32 to <40Interval Week 40 to <48Interval Week 48 to <60Interval Week 60 to <72Interval Week >=72
NVP IR0.0000.0000.0120.0490.0590.0630.0630.0670.0700.0760.0760.0760.076
NVP XR0.0000.0020.0140.0260.0340.0360.0360.0430.0490.0560.0580.0580.070

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Kaplan -Meier Estimate of Cumulative Probability of Grade 3 or 4 Asymptotic Transaminases Abnormalities

(NCT00561925)
Timeframe: week 0 to 72

,
Interventioncumulative probability (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <6Interval Week 6 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <24Interval Week 24 to <32Interval Week 32 to <40Interval Week 40 to <48Interval Week 48 to <60Interval Week 60 to <72Interval Week >=72
NVP IR0.0000.0000.0060.0270.0330.0390.0390.0420.0440.0530.0530.0530.053
NVP XR0.0000.0000.0020.0060.0080.0080.0080.0150.0190.0280.0310.0330.033

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Trough Plasma Concentration

Trough plasma concentrations of Nevirapine at steady state after multiple oral administrations of Nevirapine treatments from day 1 (visit 2) to week 48 (visit 9). (NCT00819052)
Timeframe: Day 1 to week 48

,
Interventionng/mL (Geometric Mean)
Day 1 (N=146, 0)Week 2 (N=107, 229)Week 4 (N=103, 234)Week 8 (N=110, 225)Week 12 (N=103, 223)Week 24 (N=103, 212)Week 36 (N=103, 215)Week 48 (N=101, 213)
Nevirapine Extended Release (NVP XR)NA3270323036503590375039303650
Nevirapine Immediate Release (NVP IR)37203650372040804170408043703960

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Last Available Visit, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, last available visit (up to 144 weeks)

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR71.9
Nevirapine IR After Week 48165.9
Nevirapine XR After Week 4880.9

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 108, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 108

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR72.4
Nevirapine IR After Week 48117.4
Nevirapine XR After Week 4873.5

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 12, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 12

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)22.3
Nevirapine Extended Release (NVP XR)-10.2

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 120, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 120

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR79.5
Nevirapine IR After Week 4890.0
Nevirapine XR After Week 4866.6

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 132, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 132

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR58.8
Nevirapine IR After Week 48124.8
Nevirapine XR After Week 4870.8

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 144, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 144

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR85.3
Nevirapine IR After Week 48205.6
Nevirapine XR After Week 4882.7

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 2, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 2

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)3.7
Nevirapine Extended Release (NVP XR)-4.7

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 24, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 24

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)50.4
Nevirapine Extended Release (NVP XR)45.7

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 4, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 4

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)0.8
Nevirapine Extended Release (NVP XR)-15.4

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 48, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 48

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR77.8
Nevirapine IR After Week 48139.8
Nevirapine XR After Week 4852.7

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 60, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 60

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR51.1
Nevirapine IR After Week 4811.5
Nevirapine XR After Week 4855.1

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 72, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 72

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR61.3
Nevirapine IR After Week 4877.9
Nevirapine XR After Week 4867.4

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 8, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 8

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)-18.6
Nevirapine Extended Release (NVP XR)-24.4

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 84, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 84

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR80.3
Nevirapine IR After Week 48134.6
Nevirapine XR After Week 4855.0

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Change From Baseline in CD4 Count (Cells/Cubic Millimeter) at Week 96, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 96

Interventioncells/cubic millimeter (Mean)
Nevirapine (NVP) IR / NVP XR55.1
Nevirapine IR After Week 4855.4
Nevirapine XR After Week 4860.2

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Comparison of CD4 Count (Cells/Cubic Millimeter) Change From Baseline at Week 24, Observed Cases, Full Analysis Set Population

(NCT00819052)
Timeframe: baseline, week 24

Interventioncells/cubic millimeter (Least Squares Mean)
Nevirapine Immediate Release (NVP IR)50.74
Nevirapine Extended Release (NVP XR)46.10

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Occurence of Hepatic Events

(NCT00819052)
Timeframe: 144 weeks

Interventionparticipants (Number)
Nevirapine Immediate Release (NVP IR)0
Nevirapine Extended Release (NVP XR)1

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Summary of CD4 Count (Cells/Cubic Millimeter) at Baseline, Full Analysis Set Population

(NCT00819052)
Timeframe: week 0

Interventioncells/cubic millimeter (Mean)
Nevirapine Immediate Release (NVP IR)569.7
Nevirapine Extended Release (NVP XR)557.7

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Time to Loss of Virologic Response

Kaplan-Meier Estimates of time to loss of virologic response defined as the time between the start of treatment and the time of treatment failure, up to and including the time when the last patient was on treatment for 48 weeks. (NCT00819052)
Timeframe: 48 weeks

Interventiondays (Median)
Nevirapine Immediate Release (NVP IR)393
Nevirapine Extended Release (NVP XR)391

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Change From Baseline in VL (HIV-1 Viral Load) at Each Visit

(NCT00819052)
Timeframe: week 48, 60, 72, 84, 96, 108, 120, 132, 144, last available visit

,,
Interventioncopies/mL (Mean)
week 48 (N=130, 12, 275)week 60 (N=130, 12, 274)week 72 (N=129, 9, 271)week 84 (N=125, 8, 268)week 96 (N=124, 9, 263)week 108 (N=125, 8, 260)week 120 (N=121, 8, 257)week 132 (121, 7, 252)week 144 (N=121, 7, 250)last available visit(N=130,13,276)
Nevirapine (NVP) IR / NVP XR48.411004.41747.02798.80.253.13.510.21.04472.6
Nevirapine IR After Week 4858.494.10.04.10.00.00.44.00.086.4
Nevirapine XR After Week 48-4.3-1.8-4.94140.1168.4-3.5-2.3-1.8-4.64103.2

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Comparison of Virologic Response at Week 24 Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Primary endpoint was the number of patients with a sustained virologic response through week 24 (NCT00819052)
Timeframe: week 24

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)27619
Nevirapine Immediate Release (NVP IR)13711

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Kaplan-Meier Estimates of the Proportions of Patients Without Loss of Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

(NCT00819052)
Timeframe: week 0 to 24

,
Interventionproportion of participants (Number)
Interval Week 0 to <2Interval Week 2 to <4Interval Week 4 to <8Interval Week 8 to <12Interval Week 12 to <16Interval Week 16 to <20Interval Week 20 to <24Interval Week 24 to <28
Nevirapine Extended Release (NVP XR)10.9860.980.9730.9660.9530.9460.942
Nevirapine Immediate Release (NVP IR)110.9930.9730.9590.9460.9460.946

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 12 (NCT00819052)
Timeframe: week 12

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)2896
Nevirapine Immediate Release (NVP IR)1435

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 2 (NCT00819052)
Timeframe: week 2

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)2923
Nevirapine Immediate Release (NVP IR)1480

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 24 (NCT00819052)
Timeframe: week 24

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)28510
Nevirapine Immediate Release (NVP IR)1408

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 4 (NCT00819052)
Timeframe: week 4

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)2914
Nevirapine Immediate Release (NVP IR)1462

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 400 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 8 (NCT00819052)
Timeframe: week 8

,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine Extended Release (NVP XR)2905
Nevirapine Immediate Release (NVP IR)1462

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response at their last available visit (NCT00819052)
Timeframe: last available visit, up to 144 weeks

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1219
Nevirapine IR After Week 48112
Nevirapine XR After Week 4826115

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 108 (NCT00819052)
Timeframe: week 108

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1196
Nevirapine IR After Week 4881
Nevirapine XR After Week 4824713

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 120 (NCT00819052)
Timeframe: week 120

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1129
Nevirapine IR After Week 4871
Nevirapine XR After Week 4823523

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 132 (NCT00819052)
Timeframe: week 132

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1156
Nevirapine IR After Week 4861
Nevirapine XR After Week 4823814

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 144 (NCT00819052)
Timeframe: week 144

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1156
Nevirapine IR After Week 4870
Nevirapine XR After Week 4823812

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 48 (NCT00819052)
Timeframe: week 48

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1255
Nevirapine IR After Week 48111
Nevirapine XR After Week 482688

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 60 (NCT00819052)
Timeframe: week 60

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1228
Nevirapine IR After Week 4893
Nevirapine XR After Week 4825321

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 72 (NCT00819052)
Timeframe: week 72

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1246
Nevirapine IR After Week 4890
Nevirapine XR After Week 482656

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 84 (NCT00819052)
Timeframe: week 84

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1187
Nevirapine IR After Week 4871
Nevirapine XR After Week 4824424

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Number of Participants With Virologic Response Using Lower Limit of Quantification (LLOQ) = 50 Copies/mL, Full Analysis Set Population

Endpoint was the number of patients with a sustained virologic response through week 96 (NCT00819052)
Timeframe: week 96

,,
Interventionparticipants (Number)
ResponderNon responder
Nevirapine (NVP) IR / NVP XR1177
Nevirapine IR After Week 4890
Nevirapine XR After Week 4824221

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Occurence of Rashes

drug-related rashes by severity (NCT00819052)
Timeframe: 144 weeks

,
Interventionparticipants (Number)
rash Grade 1 mildrash Grade 2 moderaterash Grade 3 severerash Grade 4 potential life-threatening
Nevirapine Extended Release (NVP XR)1100
Nevirapine Immediate Release (NVP IR)0000

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Proportion of Virologic Response (Viral Load <400 Copies/mL) Trough Week 144

Endpoint was the number of patients with a sustained virologic response through week 144 (NCT00819052)
Timeframe: week 144

,,
Interventionparticipants (Number)
ResponderNo Responder
Nevirapine (NVP) IR / NVP XR1210
Nevirapine IR After Week 4870
Nevirapine XR After Week 482500

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Efficacy: Patients Maintaining a VL < 50 Copies/mL

Patients maintaining a viral load < 50 copies/mL at Day 22. (NCT00905489)
Timeframe: Day 22

Interventionpercentage of patients (Number)
3-<6 yr96.0
6-<12 yr100.0
12-<18 yr100.0
Total.98.7

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Efficacy: Patients Maintaining a VL < 400 Copies/mL in Optional Extension Phase

Patients maintaining a viral load < 400 copies/mL at week 24 of the Optional Extension Phase (OEP) (NCT00905489)
Timeframe: week 24

Interventionpercentage of patients (Number)
3-<6 yr100.0
6-<12 yr100.0
12-<18 yr100.0
Total.100.0

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Efficacy: Patients Maintaining a VL < 400 Copies/mL

Patients maintaining a viral load < 400 copies/mL at Day 22 (NCT00905489)
Timeframe: Day 22

Interventionpercentage of patients (Number)
3-<6 yr100.0
6-<12 yr100.0
12-<18 yr100.0
Total.100.0

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CL/F,ss

Apparent clearance of the Nevirapine in the plasma after extravascular administration at steady-state Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
InterventionmL/h (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR178022402640
NVP XR201020803700

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Tmax,ss

"Time from dosing to the maximum concentration of the Nevirapine in plasma at steady state over the time dosing interval τ Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22.~The standard deviation is actually the coefficient of variation." (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionhours (Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR2.462.494.41
NVP XR6.347.285.73

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Ratio Cmax,ss/Cmin,ss

Ratio of (maximum measured concentration of the Nevirapine in plasma at steady state over the time dosing interval τ)/(minimum measured concentration of the analyte in plasma at steady state over the time dosing interval τ) Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
InterventionRatio (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR2.091.821.57
NVP XR1.731.911.73

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Percentage Change From Baseline in Mean CD4+ Count

((Day 22 value-Baseline value)/Baseline value)*100. ((Week 24 value-Baseline value)/Baseline value)*100. (NCT00905489)
Timeframe: Baseline to day 22 and baseline to week 24

,,
Interventionpercentage change (Mean)
Day 22Week 24 (n=8, 10, 9)
12-<18 yr0.5-1.0
3-<6 yr-2.1-2.1
6-<12 yr-0.0-2.1

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Cmin,ss (for IR and XR Formulations by Nevirapine XR Dose Group)

Minimum measured concentration of the Nevirapine in plasma at steady state over the time dosing interval τ by nevirapine XR dose group Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 21. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionng/mL (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR328036204960
NVP XR309041603410

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Cmax,ss (for IR and XR Formulations by Nevirapine XR Dose Group)

Maximum measured concentration of the Nevirapine in plasma at steady state over the time dosing interval τ Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionng/mL (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR685065807790
NVP XR535079705890

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Cavg

Average measured concentration of the Nevirapine in plasma at steady state Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionng/mL (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR482048406120
NVP XR414060104510

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Change From Baseline in Mean CD4+ Count (Absolute)

Change in mean CD4+ count (absolute) from baseline to Day 22 and from baseline to Week 24. (NCT00905489)
Timeframe: Baseline, Day 22 and week 24

,,
Interventioncells/mm^3 (Mean)
Day 22Week 24 (n=8;10;9)
12-<18 yr60.331.1
3-<6 yr-115.6-214.5
6-<12 yr24.2-51.2

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Efficacy: Patients Maintaining a VL < 50 Copies/mL at Last Available Visit

Patients maintaining a viral load < 50 copies/mL at the last available visit (NCT00905489)
Timeframe: Last available visit, up to 155 weeks

Interventionpercentage of patients (Number)
3-<6 yr100.0
6-<12 yr100.0
12-<18 yr100.0
Total.100.0

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Efficacy: Patients Maintaining a VL < 50 Copies/mL at Week 24 of Optional Extension Phase

Patients maintaining a viral load < 50 copies/mL at week 24 (approximately 168 days) of Optional Extension Phase (OEP). (NCT00905489)
Timeframe: week 24

Interventionpercentage of patients (Number)
3-<6 yr100.0
6-<12 yr100.0
12-<18 yr100.0
Total.100.0

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Trough Cpre,N.

"Trough Nevirapine concentration immediately prior to the next scheduled dose. Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22.~The measure of dispersion presented is the coefficient of variation (%) rather than the geometric coefficient of variation." (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

Intervention(ng/mL/mg) (Geometric Mean)
NVP XR15.47
NVP IR16.66

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%PTF

Percentage peak-trough Nevirapine fluctuation, % fluctuation (degree of peak to trough fluctuation) Patients took Nevirapine (NVP) Immediate Release (IR) up to day 10 and had PK measurements taken on Day 11. This was followed by 9 days (from day 12 to day 20) taking NVP Extended Release (XR) with PK measurements taken on Day 22. (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionpercentage fluctuation (Geometric Mean)
200 mg XR QD (175-249 mg IR/day), n=23,22300 mg XR QD (250-349 mg IR/day), n=11,12400 mg XR QD (≥350 mg IR/day), n=11,15
NVP IR67.959.141.5
NVP XR49.754.651.0

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AUCt,ss

"Area under the concentration-time curve of the Nevirapine (NVP) in plasma at steady state over the time dosing interval τ.~All patients received nevirapine IR for 10 days prior to collection of 12-hour Area Under the Curve (AUC) data. Then, all patients were switched to nevirapine XR for 9 days prior to collection of 24-hour AUC data. The treatments of IR and XR are summarized separately using geometric means and geometric coefficients of variation.~For NVP IR AUC measured over hours: 0,1,2,3,4,8 and 12, For NVP XR AUC measured over hours: 0,1,2,3,4,8,10,12 and 24." (NCT00905489)
Timeframe: Day 11 prior to the next scheduled dose of Nevirapine IR and day 22 prior to the next scheduled dose of Nevirapine XR

,
Interventionng*h/ml (Geometric Mean)
200mg NVP XR QD (175-249 mg IR/day), n=23/22300mg NVP XR QD (250-349 mg IR/day), n=11/12400mg NVP XR QD (≥350 mg IR/day), n=11/15
NVP IR579005810073400
NVP XR99300144000108000

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Percentage of Uncomplicated Malaria Episodes With Accompanying Adverse Events That Occurred in the 28 Days Following Antimalarial Therapy

The rates of adverse events, defined as severity grade 2 or higher that are possibly, probably or definitely related to study drugs over the course of the 28-day period after antimalarial therapy with artemether-lumefantrine (AL). (NCT00978068)
Timeframe: 28 days after antimalarial therapy

Intervention% uncomplicated malaria episodes w/ AEs (Number)
LPV/r + 2 NRTIs71.0
NVP or EFV + 2 NRTIs79.3

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Incidence-density of Malaria Defined as the Number of Incident Episodes of Malaria Per Time at Risk.

(NCT00978068)
Timeframe: Time from randomization to at least 24 months of follow up or until end of the study

InterventionEpisodes/ Person-Yr at Risk (Number)
Group 1: LPV/r + 2 NRTIs1.32
Group 2: Nevirapine (NVP) or Efavirenz (EFV) + 2 NRTIs2.25

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Incidence-density of Malaria Defined as the Number of Incident Episodes of Complicated Malaria Per Time at Risk.

(NCT00978068)
Timeframe: Time from randomization to at least 24 months of follow up or until end of the study

InterventionEpisodes/ Person-Yr at Risk (Number)
Group 10.024
Group 20.026

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Estimates of the 6-month Risk of a First Episode of Malaria

To assess the effect of ART independently of potential interactions with antimalarial therapy after treatment for malaria, we compared the two groups with respect to the time to the first episode of malaria. Cumulative risk was estimated using the Kaplan-Meier product-limit formula. (NCT00978068)
Timeframe: Enrollment to 6 months follow up

InterventionCumulative Risk Percentage (Number)
LPV/r + 2 NRTIs40.7
NVP or EFV + 2 NRTIs52.5

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28-day Risk of Recurrent Parasitemia

To assess the effect of potential interactions between ART and artemether-lumefantrine, the risks of recurrent parasitemia at 28 days were compared between the two groups. (NCT00978068)
Timeframe: 28 days after antimalarial therapy

InterventionCummulative Risk Percentage (Number)
LPV/r + 2 NRTIs14.0
NVP or EFV + 2 NRTIs40.8

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63-day Risk of Recurrent Malaria

To assess the effect of potential interactions between ART and artemether-lumefantrine, the risks of recurrent malaria at 63 days were compared between the two groups. (NCT00978068)
Timeframe: 28 days after antimalarial therapy

InterventionCumulative Risk Percentage (Number)
LPV/r + 2 NRTIs28.1
NVP or EFV + 2 NRTIs54.2

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Area Under the Concentration-Time Curve(AUC)

Mean Area Under the Plasma Concentration-Time Curve for each drug, log transformed (NCT01025830)
Timeframe: Assessed at 0, 0.5, 1, 1.5, 2, 3, 4, 6, 10 and 12 hr post-dosing

Interventionhour*milligram/liter (Geometric Mean)
Generic Stavudine3.6
Brand Stavudine3.4
Generic Nevirapine85.8
Brand Nevirapine79.2
Generic Lamivudine5.2
Brand Lamivudine6.4

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Maximum Plasma Concentration of Drug

Maximum concentration of drug in plasma that was attained post dosing (NCT01025830)
Timeframe: Assessed at 0, 0.5, 1, 1.5, 2, 3, 4, 6, 10 and 12 hr post-dosing

Interventionmilligram/liter (Geometric Mean)
Generic Stavudine1.6
Brand Stavudine1.3
Generic Nevirapine8.8
Brand Nevirapine8.4
Generic Lamivudine1.0
Brand Lamivudine1.3

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Antepartum Component: Number of Confirmed Infant HIV Infections

Defined as HIV nucleic acid test (NAT) positivity of the specimen drawn at either the birth (Day 0-5) or Week 1 (Day 6-14) visit, confirmed by HIV NAT positivity of a second specimen collected at a different time point (NCT01061151)
Timeframe: Measured at birth or Week 1 study visit

InterventionParticipants (Count of Participants)
Antepartum Arm A25
Antepartum Arm B7
Antepartum Arm C2

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Antepartum Component: Number of Infant HIV Infections

Detected by HIV NAT positivity (NCT01061151)
Timeframe: Measured at the birth (<= 3 days postpartum) visit

InterventionParticipants (Count of Participants)
Antepartum Arm A22
Antepartum Arm B4
Antepartum Arm C2

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Maternal Health Component: Incidence of AIDS-defining Illness

"AIDS-defining illness refers to the WHO Clinical Stage 4 illnesses listed in Appendix IV. Stage 4 illnesses were reviewed and confirmed by an Endpoint review group." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.08
Maternal Health Arm B (Discontinue Triple ARVs)0.25

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Maternal Health Component: Incidence of Death

Number of women who died during the maternal health component; that is, who had been randomized to either continue or discontinue ART after risk of HIV vertical transmission through breastfeeding was over. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.24
Maternal Health Arm B (Discontinue Triple ARVs)0.43

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Maternal Health Component: Incidence of Progression to AIDS-defining Illness or Death

AIDS-defining illness refers to the WHO Clinical Stage 4 illnesses in Appendix IV of the protocol. These events were reviewed and confirmed by an Endpoint review group. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.24
Maternal Health Arm B (Discontinue Triple ARVs)0.49

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Maternal Health Component: Incidence of Tuberculosis

Incidence of tuberculosis. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.40
Maternal Health Arm B (Discontinue Triple ARVs)0.31

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Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)

Composite outcome (NCT01061151)
Timeframe: Measured at birth

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A38991
Antepartum Arm B563123

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Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C60

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Antepartum Component: Number of Mothers With Grade 3 or Higher Toxicities and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A26159
Antepartum Arm B31861

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Antepartum Component: Number of Mothers With Obstetrical Complications

"Complications included deaths, diagnoses, signs/symptoms, chemistry lab tests, or hematological lab tests, with grades of 3 (Severe) or worse. Obstetrical complications were those classified by the MedDra coding system as Pregnancy, puerperium and perinatal conditions, except if the condition was the death of the fetus: Abortions not specified as induced or spontaneous, Abortions spontaneous, or Stillbirth and foetal death." (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C23

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Antepartum Component: Number of Mothers With Obstetrical Complications

"Complications included deaths, diagnoses, signs/symptoms, chemistry lab tests, or hematological lab tests, with grades of 3 (Severe) or worse. Obstetrical complications were those classified by the MedDra coding system as Pregnancy, puerperium and perinatal conditions, except if the condition was the death of the fetus: Abortions not specified as induced or spontaneous, Abortions spontaneous, or Stillbirth and foetal death." (NCT01061151)
Timeframe: Measured through the Week 1 postpartum study visit

,
InterventionParticipants (Count of Participants)
Periods 1 and 2Period 2
Antepartum Arm A8920
Antepartum Arm B7512

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Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)

For overall survival, failure was defined to be death. For HIV-free survival, failure was defined to be either death or developing HIV. The probability of living, or living without HIV infection, at 104 weeks was calculated by Kaplan-Meier estimation of the survival function. (NCT01061151)
Timeframe: Measured from birth through 104 weeks of age

InterventionProportional probability (Number)
Overall survival, period 2 groupHIV-free survival, period 2 group
Antepartum Arm C0.9420.921

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Antepartum Component: Probability of Overall and HIV-free Infant Survival Until 104 Weeks of Age, by Antepartum Arm (in Conjunction With Infants in the Postpartum Component)

For overall survival, failure was defined to be death. For HIV-free survival, failure was defined to be either death or developing HIV. The probability of living, or living without HIV infection, at 104 weeks was calculated by Kaplan-Meier estimation of the survival function. (NCT01061151)
Timeframe: Measured from birth through 104 weeks of age

,
InterventionProportional probability (Number)
Overall survival, Periods 1 & 2 group (arms A & B only)Overall survival, period 2 groupHIV-free survival, Periods 1&2 group (arms A&B only)HIV-free survival, period 2 group
Antepartum Arm A0.9590.9510.9370.936
Antepartum Arm B0.9670.9820.9470.940

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Postpartum Component: Proportion of Infants Alive Through 12 and 24 Months Post-delivery

Analyses (Kaplan-Meier probabilities) conducted for all individual infants (rather than M-I pair) (NCT01061151)
Timeframe: Measured at 12 and 24 months post-delivery

,
InterventionProbability (Number)
12 months post delivery24 months post delivery
Postpartum Arm A (Maternal Prophylaxis)0.9880.978
Postpartum Arm B (Infant Prophylaxis)0.9890.987

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Antepartum Component: Maternal HIV RNA Less Than 400 Copies/mL at Delivery

Analysis used the principle of intent to treat. (NCT01061151)
Timeframe: Measured at the time of delivery

InterventionParticipants (Count of Participants)Participants (Count of Participants)
Periods 1 and 272329519Periods 1 and 272329520Period 272329520Period 272329519Period 272329521
HIV RNA < 400 copies/mLHIV RNA >= 400 copies/mL
Antepartum Arm A415
Antepartum Arm B1092
Antepartum Arm A929
Antepartum Arm B275
Antepartum Arm A102
Antepartum Arm B259
Antepartum Arm C225
Antepartum Arm A210
Antepartum Arm B62
Antepartum Arm C79

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Postpartum Component: Adherence to the Maternal and/or Infant ARV Regimens, as Measured by Maternal Report and Hair Measures

"Adherence is by maternal report; adherence through hair analysis is not included here.~The protocol did not distinguish between outcomes essential to the primary publication and outcomes for subsequent publications of lesser priority. This outcome measure was listed as secondary in the protocol but the intention was as an exploratory outcome since adherence was not a focus of the study." (NCT01061151)
Timeframe: Week 6 visit (14 days - 9 weeks postpartum); Week 14 visit (10-19 weeks postpartum); Week 26 visit (20 to 31 weeks postpartum); Week 50 visit (44 to 55 weeks postpartum); and Week 74 visit (68 to 80 weeks postpartum).

InterventionParticipants (Count of Participants)
Week 6 visit72329524Week 6 visit72329525Week 14 visit72329524Week 14 visit72329525Week 26 visit72329524Week 26 visit72329525Week 50 visit72329524Week 50 visit72329525Week 74 visit72329524Week 74 visit72329525
Missed dose over 1 month agoNever missed a doseMissed dose 2-4 weeks agoMissed dose within last 2 weeks
Postpartum Arm A (Maternal Prophylaxis)1003
Postpartum Arm B (Infant Prophylaxis)1104
Postpartum Arm A (Maternal Prophylaxis)12
Postpartum Arm A (Maternal Prophylaxis)17
Postpartum Arm B (Infant Prophylaxis)4
Postpartum Arm A (Maternal Prophylaxis)140
Postpartum Arm B (Infant Prophylaxis)74
Postpartum Arm A (Maternal Prophylaxis)956
Postpartum Arm B (Infant Prophylaxis)1081
Postpartum Arm A (Maternal Prophylaxis)20
Postpartum Arm B (Infant Prophylaxis)0
Postpartum Arm A (Maternal Prophylaxis)35
Postpartum Arm A (Maternal Prophylaxis)112
Postpartum Arm B (Infant Prophylaxis)50
Postpartum Arm A (Maternal Prophylaxis)888
Postpartum Arm B (Infant Prophylaxis)1035
Postpartum Arm A (Maternal Prophylaxis)48
Postpartum Arm A (Maternal Prophylaxis)31
Postpartum Arm B (Infant Prophylaxis)8
Postpartum Arm A (Maternal Prophylaxis)103
Postpartum Arm B (Infant Prophylaxis)47
Postpartum Arm A (Maternal Prophylaxis)716
Postpartum Arm B (Infant Prophylaxis)841
Postpartum Arm A (Maternal Prophylaxis)37
Postpartum Arm A (Maternal Prophylaxis)34
Postpartum Arm B (Infant Prophylaxis)7
Postpartum Arm A (Maternal Prophylaxis)64
Postpartum Arm B (Infant Prophylaxis)30
Postpartum Arm A (Maternal Prophylaxis)311
Postpartum Arm B (Infant Prophylaxis)377
Postpartum Arm A (Maternal Prophylaxis)15
Postpartum Arm B (Infant Prophylaxis)2
Postpartum Arm B (Infant Prophylaxis)1
Postpartum Arm B (Infant Prophylaxis)9

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Postpartum Component: Incidence of Grade 3 or Higher Adverse Events and Selected Grade 2 Hematologic, Renal, and Hepatic Adverse Events

These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: Measured through site recommended duration of breastfeeding, complete cessation of breastfeeding or 18 months of age, whichever comes first

InterventionNew cases per 100 person-years (Number)
Postpartum Arm A (Maternal Prophylaxis)14.4
Postpartum Arm B (Infant Prophylaxis)14.1

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Postpartum Component: Incidence of Confirmed Infant HIV Infection

Defined as infant HIV NAT positivity of a specimen drawn at any post-randomization visit (i.e., any visit after the Week 1 [Day 6-14] visit), confirmed by HIV NAT positivity of a second specimen drawn at a different time point. Analyses were conducted at the Mother-Infant (M-I) pair level, hence the worst outcome for multiple births was counted as a single event. (NCT01061151)
Timeframe: Measured through site recommended duration of breastfeeding, complete cessation of breastfeeding or 18 months of age, whichever comes first

InterventionNew cases per 100 person-years (Number)
Postpartum Arm A (Maternal Prophylaxis)0.56
Postpartum Arm B (Infant Prophylaxis)0.55

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Maternal Health Component: Toxicity: Incidence of Grade 3 or Greater Laboratory Results or Signs and Symptoms and Selected Grade 2 Hematologic, Renal, and Hepatic Laboratory Results

The maternal safety endpoints summarized include grade 2, 3 or 4 hematologies (hemoglobin (Hb), White Blood Cells (WBC), Absolute Neutrophil Count (ANC), platelet count), chemistries (Alanine Aminotransferase (ALT or SGPT), serum creatinine), and grade 3 or 4 signs and symptoms that occurred post-randomization. These events were graded using the Division of AIDS (DAIDS) AE Grading Table, Version 1.0, December 2004, Clarification August 2009, which is available on the RSC website (http://rsc.tech-res.com). (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

InterventionNew cases per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)15.3
Maternal Health Arm B (Discontinue Triple ARVs)13.9

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Maternal Health Component: Other Targeted Medical Conditions

Other (non-cardiologic) medical conditions of particular concern were included in this outcome. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. Events included were metabolic events, hepatic events, renal events, infections such as pulmonary tuberculosis, malaria, or other serious bacterial infections, and others. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)4.0
Maternal Health Arm B (Discontinue Triple ARVs)4.6

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Maternal Health Component: Incidence Rate of Progression to AIDS-defining Illness, Death, or a Serious Non-AIDS Cardiovascular, Hepatic, or Renal Event

"This outcome included AIDS-defining illnesses or cardiovascular, hepatic, or renal adverse events of particular concern which were evaluated as serious. Serious outcomes were both those defined as serious according to the International Conference on Harmonization (ICH) definition, or outcomes with grades equal to or worse than 3 (Severe). A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. Cardiovascular events considered were hypertension, congestive heart failure, stroke, Transient Ischemia Event (TIA), pulmonary embolism, myocardial infarction (whether acute symptomatic or silent), coronary artery disease, deep vein thrombosis, peripheral vascular disease, or symptomatic HIV-associated cardiomyopathy. Hepatic events considered were cirrhosis and idiopathic sclerosing cholangitis. Renal events considered were renal insufficiency, acute or chronic." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)0.5
Maternal Health Arm B (Discontinue Triple ARVs)0.9

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Maternal Health Component: Incidence Rate of Death or Any Condition of Particular Concern

Particular events were targeted as those of particular concern. This outcome considered all such events: death, events defining WHO stages II, III, or IV, targeted cardiovascular adverse events, other targeted adverse events, or cancers which were not AIDS-defining. A complete list can be found in Appendix IV of the Protocol. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates. (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)9.0
Maternal Health Arm B (Discontinue Triple ARVs)14.0

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Maternal Health Component: Incidence Rate of Cardiovascular or Other Metabolic Events

"Cardiovascular or metabolic events of particular concern were included in this analysis. A Poisson model with time to first event as an offset and an over-dispersion parameter was used to estimate incidence rates.~Metabolic events considered were diabetes mellitus, lipodystrophy, or dyslipidemia. Cardiovascular events considered were hypertension, congestive heart failure, stroke, Transient Ischemia Event (TIA), pulmonary embolism, myocardial infarction (whether acute symptomatic or silent), coronary artery disease, deep vein thrombosis, peripheral vascular disease, or symptomatic HIV-associated cardiomyopathy." (NCT01061151)
Timeframe: From study entry until July 7, 2015, an average of 94 weeks of follow-up.

Interventionevents per 100 person-years (Number)
Maternal Health Arm A (Continue Triple ARVs)2.9
Maternal Health Arm B (Discontinue Triple ARVs)5.7

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Postpartum Component: Proportion of Mother-Infant Pairs With no Death or HIV Diagnosis Through 24 Months Post-delivery

Defined as infant HIV NAT positivity of a specimen drawn at any post-randomization visit, confirmed by HIV NAT positivity of a second specimen drawn at a different time point, or infant death. Analyses (Kaplan-Meier probabilities) were conducted at the Mother-Infant (M-I) pair level, hence the worst outcome for multiple births was counted as a single event. (NCT01061151)
Timeframe: Measured through 24 months post-delivery

InterventionProbability (Number)
Postpartum Arm A (Maternal Prophylaxis)0.971
Postpartum Arm B (Infant Prophylaxis)0.977

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Antepartum Component: Number of Mothers With Adverse Pregnancy Outcomes (e.g.,Stillbirth, Preterm Delivery (< 37 Weeks), Low Birth Weight (< 2,500 Grams), and Congenital Anomalies)

Composite outcome (NCT01061151)
Timeframe: Measured at birth

InterventionParticipants (Count of Participants)
Period 2
Antepartum Arm C111

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Cmax

Maximum plasma concentration post does, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (day 22), Post-moringa (day 35)

,
Interventionmicrogram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz5.085.51
Nevirapine9.9210.57

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AUC

Area under the plasma concentration time curve, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (day 22), Post-moringa (day 35)

,
Interventionh*microgram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz34.6732.58
Nevirapine94.17100.44

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C12h

plasma concentration 12h post dose, determined using a non-compartmental approach by means of the Phoenix WinNonlin software application. Time points for sample collection were 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h (NCT01410058)
Timeframe: Baseline (Day 22); Post-moringa (Day 35)

,
Interventionmicrogram/mL (Geometric Mean)
Baseline (Day 22)Post-moringa (Day 35)
Efavirenz2.962.53
Nevirapine7.307.55

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Change in log10(Pf Gametocyte Density) From Entry to Day 30

"Change in log10(Pf gametocyte density) as evaluated using a Hodges-Lehmann estimate from entry to day 30 is evaluated in two groups:~Randomized to nNRTI-based ART with continued Pf SCP at day 15~Randomized to LPV/r-based ART with continued Pf SCP at day 15~Analysis was not conducted in either group with clearance at day 15 due to the small sample size and high number of undetectable samples in both clearance groups at entry and day 30." (NCT01632891)
Timeframe: Entry, Day 30

Interventionlog10(gametocyte/µL) (Number)
nNRTI-based ART, Not Cleared-0.46
LPV/R-based ART, Not Cleared0.17

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Number of Participants With Uncomplicated Clinical Malaria

Uncomplicated clinical malaria is defined as the presence of non-severe fever/symptoms and parasitemia without organ complication. (NCT01632891)
Timeframe: From study entry to day 30

InterventionParticipants (Count of Participants)
LPV/R-based ART2
nNRTI-based ART1

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Time to First Pf SCP Clearance

Time to clearance is defined by time to first measurement with PCR < 10 parasites/µL, and is evaluated as the point estimate and 95% CI for the day when 50% of participants cleared parasite. (NCT01632891)
Timeframe: From study entry up to day 30

InterventionDays (Median)
LPV/R-based ART12
nNRTI-based ART14

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Log10(Pf Parasite Density)

Pf parasite density was determined by PCR. If parasite density equals 0, the value is set to 0.01 before log10 transformation. The value 0.01 was chosen based on the smallest observed parasite density value of 0.017. (NCT01632891)
Timeframe: Entry, days 3, 6, 9, 12, 15, 20, 25, 30

,
Interventionlog10(parasites/µL) (Mean)
EntryDay 3Day 6Day 9Day 12Day 15Day 20Day 25Day 30
LPV/R-based ART2.481.921.771.651.591.590.650.280.14
nNRTI-based ART2.091.571.491.631.561.430.670.490.30

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Number of Participants With Detectable Pf Gametocyte Density

Number of participants with detectable Pf gametocyte density as determined by PCR. Due to the large number of undetectable results, this outcome was measured as dichotomous. (NCT01632891)
Timeframe: Entry, days 3, 6, 9, 12, 15, 20, 25, 30

,
InterventionParticipants (Count of Participants)
EntryDay 3Day 6Day 9Day 12Day 15Day 20Day 25Day 30
LPV/R-based ART1110911610111211
nNRTI-based ART121512131114141613

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Proportion of Participants With Plasmodium Falciparum (Pf) Subclinical Parasitemia (SCP) Clearance

"Pf SCP clearance defined by polymerase chain reaction (PCR) < 10 parasites/µL on three consecutive occasions within a 24-hour period.~If a participant had missing data on day 15, they were considered as not having clearance." (NCT01632891)
Timeframe: Day 15 (3 samples collected, separated by at least 5 hours and all three collected within 24-hours)

,
InterventionProportion of participants (Number)
Proportion ClearedProportion Not Cleared
LPV/R-based ART0.230.77
nNRTI-based ART0.270.73

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Change in log10(Pf Parasite Density) From Entry to Day 30

"Change is evaluated as log10(Pf parasite density) at day 30 minus log10(Pf parasite density) at entry.~Change is evaluated in four groups:~Randomized to nNRTI-based ART with continued Pf SCP at day 15~Randomized to nNRTI-based ART with clearance of Pf SCP at day 15~Randomized to LPV/r-based ART with continued Pf SCP at day 15~Randomized to LPV/r-based ART with clearance of Pf SCP at day 15" (NCT01632891)
Timeframe: Entry, Day 30

Interventionlog10(parasites/µL) (Median)
nNRTI-based ART, Not Cleared-2.26
nNRTI-based ART, Cleared-1.65
LPV/R-based ART, Not Cleared-1.82
LPV/R-based ART, Cleared-3.61

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Cotrimoxazole: New Severe Pneumonia

Number of participants with a new severe pneumonia, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis7
Stopped Cotrimoxazole Prophylaxis10

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CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 144 Weeks After Baseline

Number of participants with HIV RNA viral load <80 copies/ml 144 weeks after baseline. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 144 weeks

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)192
Laboratory Plus Clinical Monitoring (LCM)193
Arm A: ABC+3TC+NNRTI127
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance135
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance124

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CDM vs LCM, Induction ART: Suppression of HIV RNA Viral Load 72 Weeks After Baseline

Number of participants with HIV RNA viral load <80 copies/ml 72 weeks after baseline. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 72 weeks

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)76
Laboratory Plus Clinical Monitoring (LCM)78
Arm A: ABC+3TC+NNRTI56
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance72
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance26

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Cotrimoxazole: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Mean over median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Intervention% of visits reporting missed pills (Mean)
Continued Cotrimoxazole Prophylaxis9
Stopped Cotrimoxazole Prophylaxis8

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Cotrimoxazole: All-cause Mortality

Number of participants who died, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis3
Stopped Cotrimoxazole Prophylaxis2

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Cotrimoxazole: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis-0.24
Stopped Cotrimoxazole Prophylaxis-0.28

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Cotrimoxazole: Change From Baseline in Absolute CD4 to Week 72

Estimated in those >5 years at randomization to stop vs continue, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 72

Interventioncells per mm3 (Mean)
Continued Cotrimoxazole Prophylaxis7
Stopped Cotrimoxazole Prophylaxis-2

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Cotrimoxazole: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Continued Cotrimoxazole Prophylaxis1.7
Stopped Cotrimoxazole Prophylaxis1.1

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Cotrimoxazole: Height-for-age Z-score

Age-adjusted change in height-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis0.22
Stopped Cotrimoxazole Prophylaxis0.19

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Cotrimoxazole: New Clinical and Diagnostic Positive Malaria

Number of participants with a new clinical and diagnostic positive malaria, to be analysed using time-to-event methods. Diagnostic positive by either microscopy (thick film) or rapid diagnostic test (RDT) (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis39
Stopped Cotrimoxazole Prophylaxis77

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Cotrimoxazole: New Hospitalisation or Death

Number of participants with a new hospitalisation or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis48
Stopped Cotrimoxazole Prophylaxis72

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Cotrimoxazole: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis8
Stopped Cotrimoxazole Prophylaxis19

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Cotrimoxazole: New WHO Stage 3 Severe Recurrent Pneumonia or Diarrhoea

Number of participants with a new WHO stage 3 severe recurrent pneumonia or diarrhoea, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis1
Stopped Cotrimoxazole Prophylaxis4

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Cotrimoxazole: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.5 years)

Interventionparticipants (Number)
Continued Cotrimoxazole Prophylaxis4
Stopped Cotrimoxazole Prophylaxis7

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Cotrimoxazole: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from cotrimoxazole randomization to 16 March 2012; maximum 2.5 years)

Interventionage-adjusted z-score (Mean)
Continued Cotrimoxazole Prophylaxis-0.01
Stopped Cotrimoxazole Prophylaxis-0.05

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Induction ART: Change From Baseline in CD4% 72 Weeks After ART Initiation

(NCT02028676)
Timeframe: Baseline, 72 weeks

Interventionpercentage of total lymphocytes (Mean)
Arm A: ABC+3TC+NNRTI16.4
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance17.1
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance17.3

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Induction ART: Change From Baseline in CD4% to 144 Weeks From ART Initiation

(NCT02028676)
Timeframe: Baseline, 144 weeks

Interventionpercentage of total lymphocytes (Mean)
Arm A: ABC+3TC+NNRTI19.8
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance19.6
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance19.2

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Induction ART: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Arm A: ABC+3TC+NNRTI30
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance28
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance28

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LCM vs CDM, Induction ART: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Intervention% of visits reporting missed pills (Mean)
Clinically Driven Monitoring (CDM)8.5
Laboratory Plus Clinical Monitoring (LCM)9.4
Arm A: ABC+3TC+NNRTI8.3
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance9.5
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance9.1

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LCM vs CDM, Induction ART: All-cause Mortality

Number of participants who died from any cause, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)25
Laboratory Plus Clinical Monitoring (LCM)29
Arm A: ABC+3TC+NNRTI20
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance14
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance20

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LCM vs CDM, Induction ART: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.65
Laboratory Plus Clinical Monitoring (LCM)0.61
Arm A: ABC+3TC+NNRTI0.56
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.64
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.69

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LCM vs CDM, Induction ART: Cessation of First-line Regimen for Clinical/Immunological Failure

Number of participants stopping their first-line regimen for clinical/immunological failure, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)28
Laboratory Plus Clinical Monitoring (LCM)35

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LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 144

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 144

Interventionabsolute cells per mm3 (Mean)
Clinically Driven Monitoring (CDM)418
Laboratory Plus Clinical Monitoring (LCM)420
Arm A: ABC+3TC+NNRTI446
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance450
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance360

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LCM vs CDM, Induction ART: Change From Baseline in Absolute CD4 to Week 72

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Baseline, week 72

Interventionabsolute cells per mm3 (Mean)
Clinically Driven Monitoring (CDM)408
Laboratory Plus Clinical Monitoring (LCM)385
Arm A: ABC+3TC+NNRTI402
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance447
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance336

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LCM vs CDM, Induction ART: Height-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.36
Laboratory Plus Clinical Monitoring (LCM)0.43
Arm A: ABC+3TC+NNRTI0.40
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.40
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.38

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LCM vs CDM, Induction ART: New ART-modifying Adverse Event

Number of participants with a new ART-modifying adverse event, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)31
Laboratory Plus Clinical Monitoring (LCM)32
Arm A: ABC+3TC+NNRTI8
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance30
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance25

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LCM vs CDM, Induction ART: New or Recurrent WHO Stage 3 or 4 Event or Death

Number of participants with a new or recurrent WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)91
Laboratory Plus Clinical Monitoring (LCM)79
Arm A: ABC+3TC+NNRTI64
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance53
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance53

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LCM vs CDM, Induction ART: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)77
Laboratory Plus Clinical Monitoring (LCM)73
Arm A: ABC+3TC+NNRTI73
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance61
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance54

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LCM vs CDM, Induction ART: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 4 years (maximum 5 years)

Interventionage-adjusted z-score (Mean)
Clinically Driven Monitoring (CDM)0.76
Laboratory Plus Clinical Monitoring (LCM)0.78
Arm A: ABC+3TC+NNRTI0.72
Arm B: ZDV+ABC+3TC+NNRTI->ABC+3TC+NNRTI Maintenance0.79
Arm C: ZDV+ABC+3TC+NNRTI->ZDV+ABC+3TC Maintenance0.80

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LCM vs CDM: Change From Baseline in CD4% to Week 144

(NCT02028676)
Timeframe: Baseline, week 144

Interventionpercentage of total lymphocytes (Mean)
Clinically Driven Monitoring (CDM)19.7
Laboratory Plus Clinical Monitoring (LCM)19.4

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LCM vs CDM: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Clinically Driven Monitoring (CDM)17.2
Laboratory Plus Clinical Monitoring (LCM)16.7

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LCM vs CDM: Disease Progression to a New WHO Stage 4 Event or Death

Number of participants with disease progression to a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 4 years (from randomization to 16 March 2012; maximum 5 years)

Interventionparticipants (Number)
Clinically Driven Monitoring (CDM)47
Laboratory Plus Clinical Monitoring (LCM)39

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks)

Binary outcome measure: missed any doses of ART in the last 4 weeks by self-report. Mean calculated across all 12-weekly visits attended over the whole follow-up (no specific timepoint prespecified), giving the percentage of visits attended where the carer/participant reported missing any pills in the last 4 weeks. (NCT02028676)
Timeframe: Mean over median 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Intervention% of visits reporting missed pills (Mean)
Once-daily ABC+3TC8
Twice-daily ABC+3TC8

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 48 Weeks

Number of participants reporting missing any doses of ART in the last 4 weeks by self-report at 48 weeks. (NCT02028676)
Timeframe: 48 weeks after randomization to once- versus twice-daily

Interventionparticipants (Number)
Once-daily ABC+3TC32
Twice-daily ABC+3TC29

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Once Versus Twice Daily Abacavir+Lamivudine: Adherence to ART as Measured by Self-reported Questionnaire (Missing Any Pills in the Last 4 Weeks) at 96 Weeks

Number of participants reporting missing any doses of ART in the last 4 weeks by self-report at 96 weeks. (NCT02028676)
Timeframe: 96 weeks after randomization to once- versus twice-daily

Interventionparticipants (Number)
Once-daily ABC+3TC26
Twice-daily ABC+3TC25

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Once Versus Twice Daily Abacavir+Lamivudine: All-cause Mortality

Number of participants who died, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC1
Twice-daily ABC+3TC4

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Once Versus Twice Daily Abacavir+Lamivudine: Body Mass Index-for-age Z-score

Age-adjusted change in body mass index-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC-0.29
Twice-daily ABC+3TC-0.35

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 48

Estimated in those >5 years at enrolment, in whom absolute CD4 is meaningful. (In uninfected children, CD4 decreases with age during early childhood.) (NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 48

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC3
Twice-daily ABC+3TC-3

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 72

All participants aged >5 years at randomization to once versus twice daily alive in follow-up with CD4 measured (NCT02028676)
Timeframe: Baseline, week 72

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC-6
Twice-daily ABC+3TC27

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in Absolute CD4 to Week 96

All participants aged >5 years at randomization to once versus twice daily alive in follow-up with CD4 measured (NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 96

Interventioncells per mm3 (Mean)
Once-daily ABC+3TC-26
Twice-daily ABC+3TC60

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 48

(NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 48

Interventionpercentage of total lymphocytes (Mean)
Once-daily ABC+3TC0.9
Twice-daily ABC+3TC1.3

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 72

(NCT02028676)
Timeframe: Baseline, week 72

Interventionpercentage of total lymphocytes (Mean)
Once-daily ABC+3TC1.9
Twice-daily ABC+3TC1.9

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Once Versus Twice Daily Abacavir+Lamivudine: Change From Baseline in CD4% to Week 96

(NCT02028676)
Timeframe: Randomisation to once vs twice daily, week 96

Interventionpercentage of lymphocytes (Mean)
Once-daily ABC+3TC1.6
Twice-daily ABC+3TC2.5

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Once Versus Twice Daily Abacavir+Lamivudine: Height-for-age Z-score

Age-adjusted change in height-for-age Z-score over all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC0.28
Twice-daily ABC+3TC0.32

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Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 3 or 4 Event or Death

Number of participants with a new WHO stage 3 or 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC9
Twice-daily ABC+3TC12

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Once Versus Twice Daily Abacavir+Lamivudine: New WHO Stage 4 Event or Death

Number of participants with a new WHO stage 4 event or death, to be analysed using time-to-event methods (NCT02028676)
Timeframe: Median 2 years (from randomization to 16 March 2012; maximum 2.6 years)

Interventionparticipants (Number)
Once-daily ABC+3TC3
Twice-daily ABC+3TC7

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Once Versus Twice Daily Abacavir+Lamivudine: Suppressed HIV RNA Viral Load 48 Weeks After Randomisation

Number of participants with HIV RNA viral load <80 copies/ml at 48 weeks. Measured retrospectively on stored plasma specimens: due to low stored volumes from some children, samples had to be diluted and therefore a threshold of <80 copies/ml was used to indicate suppression. (NCT02028676)
Timeframe: 48 weeks

Interventionparticipants (Number)
Once-daily ABC+3TC236
Twice-daily ABC+3TC242

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Once Versus Twice Daily Abacavir+Lamivudine: Suppression of HIV RNA Viral Load 96 Weeks After Randomisation

Number of participants with HIV RNA viral load <80 copies/ml at 96 weeks. Threshold for suppression <80 copies/ml as samples had to be diluted due to low volumes. (NCT02028676)
Timeframe: 96 weeks

Interventionparticipants (Number)
Once-daily ABC+3TC230
Twice-daily ABC+3TC234

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Once Versus Twice Daily Abacavir+Lamivudine: Weight-for-age Z-score

Age-adjusted change in weight-for-age Z-score at all 12-weekly visits attended over the whole follow-up, no specific timepoint prespecified. Mean and SD are time-averaged area under the change curve calculated using the trapezoidal rule. Z-scores calculated using UK norms which cover the full age range of children (Cole, T. J., J. V. Freeman, and M. A. Preece. 1998. British 1990 growth reference centiles for weight, height, body mass index and head circumference fitted by maximum penalized likelihood. Statistics in Medicine 17(4): 407-29). (NCT02028676)
Timeframe: Baseline and a median of 2 years (from once vs twice daily randomization to 16 March 2012; maximum 2.6 years)

Interventionage-adjusted z-score (Mean)
Once-daily ABC+3TC0.01
Twice-daily ABC+3TC-0.00

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Change From Baseline in Estimated Glomerular Filtration Rate (eGFR)

Glomerular Filtration Rate (eGFR) was estimated from the Modification of Diet in Renal Disease (MDRD)-6 equation. The MDRD-6 equation = 198 × [serum creatinine(mg/dL)]^-0.858 × [age]-0.167 × [0.822 if patient is female] × [1.178 if patient is black] × [serum urea nitrogen concentration (mg/dL)]^-0.293 × [urine urea nitrogen excretion (g/d)]^0.249. (NCT02116660)
Timeframe: Baseline and Week 48

InterventionmL/min (Mean)
Raltegravir Plus Nevirapine Plus Lamivudine-1.1
Protease Inhibitor/Ritonavir Plus Tenofovir/Emtricitabine-5.5

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