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.
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.
ID Source | ID |
---|---|
PubMed CID | 4463 |
CHEMBL ID | 57 |
CHEBI ID | 63613 |
SCHEMBL ID | 3318 |
MeSH ID | M0029429 |
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- |
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.
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.
Nevirapine did not inhibit hydroxylation of tolbutamide (CYP2C9) or S-mephenytoin (Cyp2C19) These CYP isoforms were importantly inhibited by delavirdine and efavirenz.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
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.
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.
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.
Nevirapine (NVP) is used for the management of HIV/AIDS. Bioavailability of lumefantrine, sulfadoxine, pyrimethamine, lopinavir, and efavirenz was decreased in severely malnourished patients.
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.
Role | Description |
---|---|
antiviral drug | A substance used in the prophylaxis or therapy of virus diseases. |
HIV-1 reverse transcriptase inhibitor | An 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] |
Class | Description |
---|---|
dipyridodiazepine | An organic heterotricyclic compound whose skeleton consists of a diazepine ring which is fused to two pyridine rings. |
cyclopropanes | Cyclopropane 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] |
Pathway | Proteins | Compounds |
---|---|---|
Nevirapine Metabolism Pathway | 8 | 21 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 47.3935 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.4507 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
USP1 protein, partial | Homo sapiens (human) | Potency | 0.6310 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
TDP1 protein | Homo sapiens (human) | Potency | 7.3563 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 35.4813 | 0.0112 | 12.4002 | 100.0000 | AID1030 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 31.9093 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 16.2595 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 63.6675 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 63.6675 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 15.9926 | 0.0002 | 29.3054 | 16,493.5996 | AID743080 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 50.1187 | 0.0010 | 19.4141 | 70.9645 | AID588537 |
importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 5.6234 | 5.8048 | 36.1306 | 65.1308 | AID540263 |
DNA polymerase beta | Homo sapiens (human) | Potency | 35.4813 | 0.0224 | 21.0102 | 89.1251 | AID485314 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 6.2303 | 0.0398 | 16.7842 | 39.8107 | AID1454 |
snurportin-1 | Homo sapiens (human) | Potency | 5.6234 | 5.8048 | 36.1306 | 65.1308 | AID540263 |
geminin | Homo sapiens (human) | Potency | 23.7246 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0355 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | EC50 (µMol) | 5.9505 | 0.0004 | 0.6153 | 9.7000 | AID1056583; 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 1 | EC50 (µMol) | 247.8373 | 0.0002 | 1.1683 | 9.0740 | AID1731746; AID1731747; AID1731749; AID1731750; AID1731751; AID1741393; AID1741394; AID1741395; AID1741396; AID1741397 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3 | In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID622057 | Ratio of Ki for HIV1 RT p66/p66 homodimer G190A mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID106053 | Inhibitory activity against 100I strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID82462 | Antiviral activity against K103N/P225H strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID248264 | In vitro inhibitory concentration against HIV Y188L mutant strain | 2005 | Journal 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. |
AID279480 | Antiviral activity against HIV1 isolate with RT 100F mutation relative to wild type | 2007 | Antimicrobial 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. |
AID279463 | Antiviral activity against HIV1 isolate with RT 108I, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1574373 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1637393 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID557045 | Antiviral activity against HIV1 CRF17_BF harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID440071 | Antiviral activity against HIV-1 LAI harboring wild type reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID1574390 | Resistance 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/p51 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID508644 | Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1161105 | Antiviral 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 assay | 2014 | Bioorganic & 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. |
AID226239 | Fold resistance (L100I/ WT) (as per ref 7 in the article) | 2001 | Bioorganic & 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. |
AID1079938 | Chronic 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] | |||
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AID1654213 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID302267 | Resistance index, ratio of Ki for HIV1 reverse transcriptase L100I mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal 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. |
AID248880 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID298079 | Antiviral activity against HIV1 RT 112 mutant in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal 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. |
AID106769 | Cytotoxic dose required to reduce the viability of normal uninfected MT-4 cells by 50% | 2002 | Journal 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. |
AID499278 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV1 3B | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
AID1197831 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID523356 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID279411 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID248846 | Inhibitory concentration against human immunodeficiency virus type 1 (with Y188C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID573475 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5331 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1335201 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID279437 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 225H mutation relative to wild type | 2007 | Antimicrobial 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. |
AID557047 | Antiviral activity against HIV1 clade D harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1750722 | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
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AID1565095 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID361906 | Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1574378 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID82460 | Antiviral activity against K103N/G190A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID198911 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution K103N | 2001 | Journal 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. |
AID1124992 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives. |
AID105716 | Antiviral activity against HIV-1 (strain RF) infected MT-4 cells | 1995 | Journal 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. |
AID1223490 | Apparent permeability across human differentiated Caco2 cells | 2012 | Drug 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. |
AID244633 | Selective index value (ratio of CC50 to IC50 value)against HIV LAI cell line | 2005 | Journal 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. |
AID1729156 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1729152 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV 3B infected in human MT4 cells | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1249715 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & 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. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269798 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & 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. |
AID1485973 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID1773455 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring E138K mutant infected in human MT4 cells | |||
AID297137 | Antiviral activity against wild type HIV1 NL4-3 by cytopathic cell killing assay | 2007 | Journal 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. |
AID666414 | Antiviral 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 ELISA | 2012 | Journal 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. |
AID1163254 | Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID1303216 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and anti-HIV activity of novel quinoxaline derivatives. |
AID198078 | Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
AID725390 | Cytotoxicity against human CEmx174 cells expressing LTR-GFP | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors. |
AID1141978 | Inhibition of HIV1 wild-type reverse transcriptase L1001 mutant using [3H]dTTP by scintillation counting | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID299022 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase | 2007 | Bioorganic & 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. |
AID105693 | Anti-HIV-1 activity against K1001 strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID257917 | Antiviral activity against HIV1 Y181C mutant using HeLa MAGI assay | 2006 | Journal 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. |
AID1357783 | Antiviral activity against wild-type HIV-1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1485974 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
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AID226240 | Fold resistance (L100I/ WT) (as per ref 8 in the article) | 2001 | Bioorganic & 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. |
AID342721 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & 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. |
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AID1761020 | Antiviral activity against HIV-1 harboring reverse transcriptase RES056 mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID198247 | Inhibitory concentration against HIV-1 wild type Reverse transcriptase (RT) | 1995 | Journal 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. |
AID279396 | Antiviral activity against HIV1 isolate with RT 103N, 225H mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1443668 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID297141 | Antiviral activity against HIV1 with RT V108I mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID413566 | Ratio of EC50 for multidrug-resistant HIV1with reverse transcriptase clone 7324-1 to EC50 for wild type HIV1 3B | 2008 | Journal 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). |
AID1200845 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID248841 | Inhibitory concentration against human immunodeficiency virus type 1 (with G190A resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID322392 | Antiviral activity against HIV1 3B assessed as inhibition of virus-induced cytopathogenicity in MT4 cells after 4 days by MTT assay | 2008 | Bioorganic & 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). |
AID1171598 | Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID586904 | Activity at BCRP | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1191403 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID281489 | Selectivity index, CC50 for MT4 cells/IC50 for HIV1 3B | 2007 | Journal 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. |
AID298078 | Antiviral activity against wild type HIV1 3B in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal 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. |
AID1637404 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring F227L/V106A double mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1741400 | Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based fluorescence assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
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AID573480 | Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase to wild-type | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID282738 | Inhibition of HIV1 RT V106A mutant | 2005 | Journal 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. |
AID1171588 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1292366 | Inhibition 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]-dCTP | 2016 | Bioorganic & 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. |
AID1483281 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase K103N mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1565099 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID322394 | Selectivity index, Ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & 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). |
AID508783 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1736356 | Antiviral 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 | |||
AID650693 | Ratio of ID50 for HIV 1 reverse transcriptase Y188L mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1610053 | Antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID1357793 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID361905 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/P225H mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
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AID279430 | Antiviral activity against HIV1 isolate with RT 103N, 106I mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1320864 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID28979 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1290408 | Inhibition 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 counting | 2016 | Journal 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. |
AID1056578 | Antiviral 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 after | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID1636135 | Inhibition of Escherichia coli RNA polymerase | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15 | Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current 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. |
AID1637388 | Antiviral activity against human HIV-1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID607875 | Cytotoxic activity against human MT4 cells assessed as viability of mock-infected cells after 5 days by MTT assay | 2011 | Bioorganic & 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. |
AID1316806 | Selectivity index, ratio of CC50 for human MT-4 cells to IC50 for HIV-1 3B infected in human MT-4 cells | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
AID443757 | Antiviral activity against HIV1 with reverse transcriptase Y181L mutation | 2010 | Journal 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. |
AID247496 | Inhibitory activity against HIV-1 mutant strain 101E | 2004 | Journal 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. |
AID1059146 | Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & 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. |
AID476469 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus replication by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID246153 | Concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C | 2005 | Journal 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. |
AID717257 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant | 2012 | Bioorganic & 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. |
AID1574384 | Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysis | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & 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. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID263153 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & 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. |
AID391991 | Inhibition of HIV1 reverse transcriptase at 100 ug/ml after 1 hr by microtiter plate ELISA | 2008 | European 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. |
AID735329 | Inhibition of HIV-1 reverse transcriptase assessed as decrease in incorporation of [3H]TTP into polyA template | 2013 | Journal 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. |
AID105540 | Inhibitory activity against HIV-1 Wild Type in MT-4 cell culture (human T-cell line with 50% human AB serum) | 1999 | Journal 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. |
AID1558853 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1483269 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID573474 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5269 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID518742 | Selectivity ratio of EC50 for antiviral activity against HIV 1 subtype B harboring reverse transcriptase M230L mutant to EC50 for antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID666413 | Antiviral activity against HIV1 SF33 infected in human MT4 cells assessed as inhibition of viral p24 antigen production after 7 days by ELISA | 2012 | Journal 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. |
AID587747 | Antiviral 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 vi | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID587755 | Antiviral activity against HIV1 NL4-3.Luc in human MDM assessed as infectivity treated for 24 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID246786 | Concentration required to reduce the amount of p24 by 90% in C8166 cells infected with an efavirenz-resistant strain EFVR | 2005 | Journal 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. |
AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current 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. |
AID1077220 | Cytotoxicity against human MT4 cells assessed as growth inhibition after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID508795 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V090I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID197933 | HIV-1 reverse transcriptase inhibitory activity against Ile 100 mutant using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal 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. |
AID1880372 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
AID632804 | Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID1637401 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y181C mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID405582 | Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates. |
AID571978 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID46376 | Antiviral activity against site directed resistant isolate HIV-1 K101E in CEM cells | 2001 | Journal 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. |
AID663306 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal 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. |
AID496616 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39M, K46Q, V60I, S68G, D123E, I135V, S162A, K173A, Q174K,D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1687687 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells reduction in cell viability by MTT assay to EC50 for antiviral activity against wild type HIV-1 strain IIIB infected in human MT4 cells assessed as reduction in virus-induced cytopa | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID734261 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 A17 infected in human MT4 cells | 2013 | Journal 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. |
AID1822273 | Antiviral activity against wild type HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID293562 | Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay | 2007 | European 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. |
AID1565100 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID1877038 | Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability measured after 3 days by XTT assay | 2021 | Journal 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. |
AID508655 | Selectivity index, ratio of CC50 human MT4 cells to EC50 for Human immunodeficiency virus 1 | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID525105 | Antiviral 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 compound | 2008 | Antimicrobial 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. |
AID287003 | Inhibition of drug-resistant reverse transcriptase T181C mutant | 2007 | Journal 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. |
AID82465 | Antiviral activity against L100I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1171590 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1743637 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID395597 | Selectivity index, ratio of CC50 for human CEM cells to EC50 for HIV1 3B | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones. |
AID257918 | Antiviral activity against HIV1 V106A mutant using HeLa MAGI assay | 2006 | Journal 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. |
AID492282 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID279426 | Antiviral activity against HIV1 isolate with RT 227L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID368559 | Antiviral activity against HIV1 reverse transcriptase K103N mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID293563 | Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay | 2007 | European 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. |
AID232981 | Selectivity index; ND = Not determined | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1435517 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase F227L/V106A double mutant | |||
AID1316344 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID481177 | Inhibition of HIV1 reverse transcriptase by ELISA | 2010 | Bioorganic & 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. |
AID197800 | Compound was tested for inhibitory activity against HIV-1 wild type reverse transcriptase | 1998 | Bioorganic & 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. |
AID1460929 | Antiviral 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 assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID571971 | Antiviral activity against HIV-1 subtype CRF01_AE V022820 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID391678 | Antiviral activity against HIV1 infected in human 293T cells assessed as inhibition of pseudovirus infection | 2008 | Journal 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. |
AID650694 | Ratio of ID50 for HIV 1 reverse transcriptase Y181I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1069707 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B | 2014 | Bioorganic & 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. |
AID248316 | In vitro inhibitory concentration against HIV-1 Y181C mutant strain | 2005 | Journal 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. |
AID527562 | Antiviral activity against HIV1 NL4-3 containing reverse transcriptase K103N mutation infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect | 2010 | Bioorganic & 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. |
AID279412 | Antiviral activity against HIV1 isolate with RT 103N, 188L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID279403 | Antiviral activity against HIV1 isolate with RT 108I mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1316336 | Antiviral activity against HIV1 3B harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1565097 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID361917 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106I mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1303215 | Cytotoxicity against human MT4 cells infected with HIV1 3B assessed as cell growth inhibition after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and anti-HIV activity of novel quinoxaline derivatives. |
AID257165 | Inhibition of Y181I mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal 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. |
AID279418 | Antiviral activity against HIV1 isolate with RT 98G, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID619641 | Ratio of EC50 for HIV-1 3B harboring RT K103N mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1483278 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID573470 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID698294 | Antiviral 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 assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID299023 | Antiviral activity against HIV1 assessed as reduction of virus-induced cytopathic effect in MT4 cells | 2007 | Bioorganic & 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. |
AID1880377 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase K103N mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
AID267648 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
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AID269794 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269794 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & 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. |
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AID496618 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, V60I, K122E, D123S, I135V, E138D, S162A, K173T,Q174S, D177E, I178M, V189I, T200A, I202V, Q207E, F214L, V245Q mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
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AID248260 | In vitro inhibitory concentration against HIV K103N mutant strain | 2005 | Journal 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. |
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AID279325 | Inhibition of reverse transcriptase activity in HIV1 NL4-3 infected MT4 cells before dialysis | 2007 | Antimicrobial 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. |
AID584081 | Antiviral 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 to | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
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AID106609 | Cytotoxic concentration that reduces the MT-4 cell viability by 50% | 2004 | Bioorganic & 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. |
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AID1157587 | Antiviral activity against saquinavir-resistant HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID294631 | Cytotoxicity against CEM cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID267862 | Inhibition of HIV1 reverse transcriptase K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
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AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID440638 | Antiviral 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 assay | 2009 | Journal 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. |
AID1822277 | Antiviral activity against HIV-1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1773444 | Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV1 RES056 infected in MT4 cells | |||
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AID106065 | Inhibitory activity against 181C strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID1520037 | Antiviral 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 by | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Preliminary 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. |
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AID1435502 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID650689 | Inhibition of HIV 1 reverse transcriptase K103N mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID523347 | Antiviral activity against HIV1 with RT connection domain N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID82470 | Antiviral activity against V106I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1729149 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
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AID302254 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal 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. |
AID449491 | Cytotoxicity against human MT4 cells as reduction in cell viability after 5 days by MTT assay | 2009 | European 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. |
AID198235 | Inhibitory activity against HIV rRT activity in mutant HIV-1 strain resistant to Nevirapine (Y181C) | 1996 | Journal 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. |
AID1373152 | Inhibition of reverse transcriptase Y181C mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
AID361928 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V108I/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1157582 | Antiviral activity against efavirenz-resistant HIV1 harboring RT 100I, 103R, 179D, 225H mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID660088 | Inhibition of HIV-1 reverse transcriptase at 20 ug after 1 hr by colorimetry | 2012 | Bioorganic & 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. |
AID508785 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1186002 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1565093 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | |||
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AID246359 | Protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity | 2005 | Journal 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. |
AID226250 | Y181C/WTIIIB ratio of the compound | 2001 | Journal 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. |
AID1410488 | Inhibition of HIV1 reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID263522 | Antiviral activity against HIV1 F227L mutant | 2006 | Bioorganic & 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. |
AID698145 | Inhibition of HIV1 reverse transcriptase K103N mutant RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID82474 | Antiviral activity against Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID279472 | Antiviral activity against HIV1 isolate with RT 103S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID302621 | Cytotoxicity against human MT2 cells by MTT assay | 2007 | Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22 | From docking false-positive to active anti-HIV agent. |
AID1743630 | Antiviral activity against HIV1 harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID371907 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID198094 | Inhibitory activity against HIV-1 recombinant reverse transcriptase. | 2001 | Journal 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. |
AID443758 | Antiviral activity against HIV1 with reverse transcriptase G190A mutation | 2010 | Journal 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. |
AID440084 | Antiviral activity against HIV1 HXB2 harboring 100I and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID1572530 | Inhibition of HIV1 reverse transcriptase p66/p51 using poly(rA)/oligo(dT)16 as template/primer measured after 40 mins by pico-green based spectrofluorometric analysis | |||
AID1574387 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 L100I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1175436 | Antiviral activity against wild-type HIV-1 SF33 infected in human TZM-bl cells after 7 days by ELISA | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs. |
AID298074 | Antiviral activity against HIV1 3B in MT4 cells by MTT assay | 2007 | Journal 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. |
AID246274 | Effective concentration against rhuman immunodeficiency virus type 1 L100I mutant strain | 2005 | Journal 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). |
AID508787 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V106M mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID491827 | Antiviral activity against HIV1 with reverse transcriptase 8605MR mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1418464 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID246481 | Effective concentration against human immunodeficiency virus type 1 mutated at 227C; ND:Not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID1483280 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase L100I mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID360706 | Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay | 2007 | The 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. |
AID46377 | Antiviral activity against site directed resistant isolate HIV-1 K103N in CEM cells | 2001 | Journal 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. |
AID1636146 | Antiviral activity against wild type HIV1 NL4-3 | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15 | Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID1304401 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID248843 | Inhibitory concentration against human immunodeficiency virus type 1 (with V106A resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID1591874 | Antiviral activity against HIV1 NL4-3 harboring Y181C mutant infected in human MT2 cells measured 48 hrs post-infection by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase. |
AID105143 | Concentration required to achieve 50% protection of MT-4 cells from HIV-1-induced cytopathogenicity. | 1999 | Journal 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. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID1736154 | Inhibition 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 wi | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal 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). |
AID735082 | Antiviral activity against wild type HIV by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID1443666 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID246779 | Concentration required to reduce the amount of p24 by 90% in wtIIIB-HIV-1-infected C8166 cells | 2005 | Journal 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. |
AID371896 | Antiviral activity against wild type HIV1 NL4-3 in human TZM-b1 cells assessed as beta-galactosidase activity after 48 hrs | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1884541 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1442776 | Inhibition of HIV1 reverse transcriptase by colorimetric assay | 2017 | Journal 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. |
AID248842 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID1888701 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | |||
AID1357785 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1637390 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction of cell viability after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID522373 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I/V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID443754 | Antiviral activity against HIV1 PNL4-3 | 2010 | Journal 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. |
AID1155809 | Antiviral 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 method | 2014 | Journal 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. |
AID346972 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Studies on anti-HIV quinolones: new insights on the C-6 position. |
AID1880376 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase L1001 mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
AID496622 | Antiviral activity against HIV-1 subtype CRF06_cpx ontaining reverse transcriptase V106I/V21I, V35T, V60I, K122T, D123R, I135V, S162A, K173T, Q174K, D177E, I178L, T200A, Q207D, R211K, V245Q, E248D mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & 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. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269801 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & 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. |
AID1056575 | Ratio of EC50 for HIV-1 expressing reverse transcriptase K103N/V108I double mutant to EC50 for wild-type HIV-1 | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID586321 | Inhibition of HIV1 3B reverse transcriptase activity infected in human H9 cells assessed as level of p24 antigen | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
AID1884488 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against NNRTI resistant HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1485967 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID614141 | Antiviral activity against wild type Human immunodeficiency virus 1 3B bearing reverse transcriptase K103N and Y181C double mutation infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17 | Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1418466 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID279417 | Antiviral activity against HIV1 isolate with RT 106A, F227L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID305057 | Antiviral activity against HIV in HEK293T cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | 4-Aminopyrimidines as novel HIV-1 inhibitors. |
AID718368 | Cytotoxicity against HIV2 ROD infected in human MT4 cells by MTT assay | 2012 | Bioorganic & 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. |
AID199997 | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 12 in the article) | 2001 | Bioorganic & 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. |
AID440075 | Antiviral activity against HIV1 HXB2 harboring Y188L mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & 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. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269689 | Antiviral activity against HIV1 NNTRI resistant L100I mutant | 2006 | Bioorganic & 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. |
AID1057037 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in MT4 cells | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID508786 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V108I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1191400 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID199995 | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 8 in the article) | 2001 | Bioorganic & 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. |
AID478386 | Inhibition of HIV1 RT after 1 hr by ELISA relative to control | 2010 | Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9 | Design of potential reverse transcriptase inhibitor containing Isatin nucleus using molecular modeling studies. |
AID1249723 | Antiviral activity against HIV1 expressing reverse transcriptase F227L + V106A mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID361908 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID518735 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by filter-based filtration assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID371897 | Selectivity index, ratio of CC50 for human TZM-b1 cells to EC50 for HIV1 NL4-3 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID361924 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/V108I mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID440074 | Antiviral activity against HIV1 HXB2 harboring Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID508778 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID197779 | Ability to inhibit HIV-1 Reverse Transcriptase (RT) using an rC-dG template/primer | 1994 | Journal 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. |
AID606674 | Inhibition of HIV1 reverse transcriptase V179D mutant | 2011 | Bioorganic & 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. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID496620 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/K30E, I31P, V35Q, T39S, E44G, E53G, A62G, N81H, Q91H,I135V,S162A, K173S, Q174R, D177E, V179I, T200I, Q207N, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID198228 | Inhibitory activity against recombinant HIV-1 reverse transcriptase (rRT) | 1999 | Bioorganic & 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. |
AID279467 | Antiviral activity against HIV1 isolate with RT 106A, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID263517 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & 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. |
AID198411 | Tested for the inhibition of wild type HIV-1 (IIIB) RT | 1996 | Journal 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. |
AID1267612 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-2 ROD | 2015 | Journal 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. |
AID1517761 | Inhibition 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 | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-isoxazol-3-yl-acetamide analogues as heat shock protein 90 (HSP90) inhibitors with significant anti-HIV activity. |
AID1882468 | Antiviral activity against wild type HIV-1 IIIB infected in human MT2 cells assessed as protection against virus-induced cytopathicity by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID248844 | Inhibitory concentration against human immunodeficiency virus type 1 (with V108I resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID267863 | Inhibition of HIV1 reverse transcriptase Y181I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID265467 | Antiviral activity against HIV1 3B in MT4 cell line | 2006 | Journal 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. |
AID366524 | Antiviral activity against HIV1 isolates with reverse transcriptase Y188L mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal 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. |
AID371911 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID738335 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID1483277 | Inhibition of HIV1 3B reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID248493 | In vitro inhibitory concentration value against HIV K103N and Y181C mutant strain | 2005 | Journal 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. |
AID1171585 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID757625 | Antiviral 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 assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID373561 | Half life in plasma of HIV1-infected patient | 2007 | Antimicrobial 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. |
AID508764 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K101E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1773452 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring K103N mutant infected in human MT4 cells | |||
AID198236 | Inhibitory activity against HIV rRT activity in wild type IIIB strain | 1996 | Journal 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. |
AID1304403 | Cytotoxicity against mock-infected human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1373156 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
AID663299 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Journal 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. |
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AID1390712 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
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AID302253 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal 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. |
AID265472 | Activity against HIV-112 assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal 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. |
AID263518 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & 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. |
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AID1811035 | Anti-viral activity against HIV1 harboring RT Y188L mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
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AID88368 | Antiviral activity against K103N/P225H mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
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AID1811034 | Anti-viral activity against HIV1 harboring RT E138K mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
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AID1572554 | Solubility in water at pH 7 | |||
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AID105349 | Tested for the inhibitory activity of HIV-2 infected MT-4 cells | 1994 | Journal 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. |
AID1705195 | Inhibition of RNA-dependent DNA polymerase activity of recombinant HIV-1 p66/p51 reverse transcriptase K103N mutant assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintillation cou | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
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AID305058 | Cytotoxicity against HEK293T cells after 48 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | 4-Aminopyrimidines as novel HIV-1 inhibitors. |
AID430054 | Inhibition of HIV1 recombinant RNA-dependent DNA polymerase activity of reverse transcriptase assessed as incorporation of radioactive dTTP into poly(rA)/oligo(dT) | 2009 | Bioorganic & 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. |
AID1410482 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID1773463 | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into protein incubated for 1 hrs by ELISA | |||
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AID734260 | Antiviral 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 ELISA | 2013 | Journal 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. |
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AID279449 | Antiviral activity against HIV1 isolate with RT 98G, 188L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID299026 | Antiviral activity against HIV1 3B in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
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AID247501 | Inhibitory activity against HIV-1 mutant strain 181C | 2004 | Journal 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. |
AID265473 | Activity against HIV-AB1 assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal 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. |
AID1446815 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
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AID556527 | Antiviral activity against Human immunodeficiency virus 1 clone 14682 harboring 122E, 135V, Q145V, 200A mutation in reverse transcriptase by phenosense assay relative to wild type | 2009 | Antimicrobial 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. |
AID482691 | Antiviral 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 ELISA | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID1884486 | Antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1769793 | Inhibition of recombinant HIV1 reverse transcriptase by colorimetric assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Design of gp120 HIV-1 entry inhibitors by scaffold hopping via isosteric replacements. |
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AID279465 | Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID82467 | Antiviral activity against P236L strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
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AID1884229 | Antiviral activity against HIV-1 RES056 infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID279434 | Antiviral activity against HIV1 isolate with RT 101E, 181C, 190S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1373163 | Inhibition 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 assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
AID1763898 | Antiviral activity against HIV-1 IIIB harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID302271 | Resistance index, ratio of Ki for HIV1 reverse transcriptase Y188L mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal 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. |
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AID1157583 | Antiviral activity against N119-sensitive HIV1 harboring Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID82472 | Antiviral activity against V108I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID82471 | Antiviral activity against V106I/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
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AID443752 | Selectivity index, ratio of IC50 for African green monkey Vero cells to EC50 for HIV1 | 2010 | Journal 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. |
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AID83549 | Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID1558849 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID318126 | Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis at 100 uM | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors. |
AID1743639 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT F227L/V106A mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1763899 | Antiviral activity against HIV-1 IIIB harboring RT K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID606673 | Inhibition of HIV1 reverse transcriptase L100I mutant | 2011 | Bioorganic & 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. |
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AID1773440 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID279416 | Antiviral activity against HIV1 isolate with RT 179A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1457060 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID650687 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV 1 NL4-3 | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID734255 | Antiviral 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 ELISA | 2013 | Journal 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. |
AID279445 | Antiviral activity against HIV1 isolate with RT 101E, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID317733 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
AID1292009 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID1157593 | Antiviral activity against MC1220-resistant HIV1 harboring RT 100I, 179D, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID267851 | Inhibition of wild type HIV1 reverse transcriptase | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID1275547 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1610041 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 N119 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID1654239 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID105341 | Inhibitory activity against resistant HIV-1 strain MC639r was determined. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
AID373565 | Antiviral 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 assay | 2007 | Antimicrobial 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. |
AID1535529 | Inhibition 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 ELISA | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3 | Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs. |
AID1822283 | Inhibition of recombinant wild type p66/p51 HIV1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1056581 | Antiviral 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 after | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID198770 | Binding affinity against HIV reverse transcriptase (Estimated Ki) | 2000 | Bioorganic & 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. |
AID508650 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID573465 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID508791 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101Q mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID287005 | Inhibition of DNA polymerase activity of reverse transcriptase pre-incubated with drug assessed as impairment of primer elongation by DNA polymerase primer-extension assay | 2007 | Journal 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. |
AID622055 | Ratio of Ki for HIV1 RT p66/p66 homodimer Y181C mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID279474 | Antiviral activity against HIV1 isolate with RT 101R, 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID635345 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID1654199 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID198067 | Inhibition of HIV-1 reverse transcriptase at 37 degree Centigrade | 2001 | Journal 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. |
AID298064 | Cytotoxicity against human MT4 cells by MTT assay | 2007 | Journal 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. |
AID1171594 | Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID738334 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID198077 | Inhibitory activity against HIV-1 Mutant Reverse transcriptase P236L | 1998 | Journal 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. |
AID508781 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138R mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1736157 | Selectivity index, ratio of CC50 for human MT2 cells to EC50 for anti-HIV-1 activity against HTLV-3B infected in human MT2 cells | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID508763 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1323001 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
AID1320868 | Solubility of the compound | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1335206 | Ratio 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 glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID106579 | 50% cytotoxic concentration against mock-infected MT-4 cells using MTT method | 2000 | Journal 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. |
AID1304409 | Antiviral activity against HIV-1 3B expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID228281 | Compound was evaluated for the cytotoxic activity by using Microculture Tetrazolium assay (MTA) | 1999 | Bioorganic & 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. |
AID1736366 | Selectivity 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 | |||
AID1267628 | Antiviral activity against nevirapine-resistant SIV mac251 infected in human MT4 cells | 2015 | Journal 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. |
AID1435512 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase L100I mutant | |||
AID267647 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID508647 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, E138G mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID302263 | Inhibition of HIV1 reverse transcriptase V179D mutant | 2007 | Journal 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. |
AID253490 | Dose required to inhibit HIV-1 reverse transcriptase activity (K103N mutant) by 50% | 2005 | Journal 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. |
AID1141962 | Antiviral activity against HIV1 3B infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID82272 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected wild type cells | 2002 | Journal 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. |
AID1773441 | Antiviral activity against wild type HIV2 ROD infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID240140 | Concentration required to inhibit HIV-1 reverse transcriptase activity (wild-type) by 50% | 2005 | Journal 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. |
AID342720 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & 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. |
AID1457053 | Antiviral activity against HIV1 NL4-3 infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID508767 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1275539 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigenin-dUTP/biotin-dUTP/dTTP nucleotides incubated for 1 hr by ELISA | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1418463 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 4 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID232055 | Selectivity index (Ratio of CC50/EC50). | 2004 | Journal 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. |
AID279443 | Antiviral activity against HIV1 isolate with RT 106A, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID199097 | Inhibitory activity against HIV rRT activity in HIV-2 | 1996 | Journal 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. |
AID1141976 | Inhibition of HIV1 wild-type reverse transcriptase K103N mutant using [3H]dTTP by scintillation counting | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1884494 | Inhibition of recombinant wild-type p66/p51 HIV-1 reverse transcriptase incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1410481 | Inhibition of wild-type HIV1 3B reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytotoxicity by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID1877040 | Potency 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 assay | 2021 | Journal 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. |
AID508753 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1155819 | Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase | 2014 | Journal 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. |
AID105325 | Inhibition of Efavirenz resistant HIV-1 (Y181C) induced cytopathicity in MT-4 cells. | 2004 | Journal 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. |
AID197944 | In vitro inhibition of recombinant reverse transcriptase (WT) of HIV-1 IIIB | 1996 | Journal 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. |
AID572180 | Antiviral activity against HIV-1 SM002 harboring NNTRI 181C mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1185995 | Antiviral 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 HIV1 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1636440 | Drug 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 NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1743636 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID572187 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID1077223 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID82271 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain | 2002 | Journal 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. |
AID1687685 | Antiviral activity against HIV-2 ROD strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID1736155 | Anti-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 method | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID279444 | Antiviral activity against HIV1 isolate with RT 101Q, 181C, 190S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID263514 | Antiviral activity against HIV1 V106A mutant | 2006 | Bioorganic & 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. |
AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1574376 | Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID88377 | Antiviral activity against V106A mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1155805 | Cytotoxicity against human MT4 cells assessed as induction of cell death by MTT method | 2014 | Journal 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. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID210590 | In vitro metabolism in human liver microsomes | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
AID518738 | Inhibition of DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant by gel-based primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID1687684 | Antiviral activity against HIV-1 RES056 mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID635302 | Antiviral activity against HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID88371 | Antiviral activity against P236L mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID152641 | Cytotoxic concentration was evaluated against human peripheral blood mononuclear cells (PBMC); ND = Not determined | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID105858 | Compound was tested for potency to achieve protection of MT-4 cells from 100I strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID302248 | Cytotoxicity against MT4 cells after 4 days by MTT method | 2007 | Journal 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. |
AID572172 | Antiviral activity against HIV-1 subtype CRF05_DF V022823 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1173646 | Therapeutic index, ratio of CC50 for human CEmx174 cells expressing GFP to IC50 for HIV-1 LAI infected in human CEMx174-LTR-GFP CG8 cells | 2014 | Bioorganic & 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. |
AID736040 | Inhibition of HIV1 reverse transcriptase p66/p51 Y181C mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID561946 | Antibacterial activity against Streptococcus pneumoniae after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID248494 | In vitro inhibitory concentration against HIV L100I and K103N mutant strain | 2005 | Journal 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. |
AID294634 | Inhibition of HIV1 reverse transcriptase using Poly rA.dT template | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID1228841 | Selectivity index, ratio of CC50 against human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Limonoids with Anti-HIV Activity from Cipadessa cinerascens. |
AID247617 | Inhibitory activity against HIV-1 double mutants strain 100I and 103N | 2004 | Journal 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. |
AID342719 | Antiviral activity against HIV1 3B in human MT4 cells assessed as virus-induced cytopathogenicity after 5 days | 2008 | Bioorganic & 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. |
AID298089 | Inhibition of HIV1 RT Y181I mutant | 2007 | Journal 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. |
AID361923 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/G190A mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID523477 | Antiviral activity against HIV1 with RT connection domain G190A/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID294629 | Antiviral activity against HIV1 3B in CEM cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID1231489 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID106745 | Cytotoxicity against MT-4 cells. | 2001 | Journal 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. |
AID561947 | Antibacterial activity against Haemophilus influenzae after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID1882471 | Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5 | Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID1157592 | Antiviral activity against 6-[(3,5-Dimethylphenyl)fluoromethyl]-5-ethyl-1-{[[4-(3-hydroxyprop-1-ynyl)benzyl]oxy]methyl}pyrimidine-2,4(1H,3H)-dione-resistant HIV1 harboring RT 106I, 181C mutant infected in human MT4 cells assessed as inhibition of virus-in | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1316335 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID246511 | Compound concentration required to achieve 50% protection of infected MT-4 cells from K103N-Y181C strain was determined by the MTT method | 2005 | Journal 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. |
AID566904 | Inhibition of HIV1 reverse transcriptase | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection. |
AID1335218 | Antiviral 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 assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current 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. |
AID1141966 | Antiviral 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 method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID328844 | Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug 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. |
AID366530 | Resistance index, ratio of ID50 for reverse transcriptase Y181I mutant to IC50 for wild-type HIV1 reverse transcriptase | 2008 | Journal 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. |
AID413267 | Antiviral 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 ELISA | 2008 | Journal 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). |
AID1457052 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1558857 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID1610043 | Antiviral activity against HIV1 VB51 infected in human PBMC cells incubated for 5 days by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID232053 | Selectivity index is the ratio of CC50 to EC50 | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
AID1335205 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID389380 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | Bioorganic & 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. |
AID525109 | Antiviral 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 compound | 2008 | Antimicrobial 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. |
AID619630 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID106074 | Inhibitory activity against LAI strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID1152241 | Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay | 2014 | Bioorganic & 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. |
AID247504 | Inhibitory activity against HIV-1 mutant strain 190S | 2004 | Journal 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. |
AID1156485 | Antiviral 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 assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID1773443 | Selectivity ratio of CC50 for human MT4 cells to IC50 for HIV-1 3B infected in MT4 cells | |||
AID1352317 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1561719 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against v | |||
AID736442 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID496621 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase K101E/V35T, E36D, K49R, V60I, K122P, I135R, S162A, E169R, K173T, Q174E,D177E, V189I, T200A, I202V, Q207E, R211K, V245Q mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID279326 | Decrease in reverse transcriptase activity in HIV1 infected HeLa MAGI cells assessed as decrease in number of blue foci after dialysis | 2007 | Antimicrobial 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. |
AID82461 | Antiviral activity against K103N/L100I strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1141963 | Antiviral activity against HIV-2 ROD infected in human CEM cells assessed as protection of cells monitored by giant cell formation by microscopy | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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AID767496 | Solubility of the compound in water by HPLC analysis | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
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AID104800 | Dose required to reduce the viability of mock-infected cells by 50%, determined by MTT method. | 1998 | Journal 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. |
AID1124991 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives. |
AID88382 | Antiviral activity against Y188C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID294632 | Selectivity index, ratio of CC50 for CEM cells to EC50 for HIV1 infected CEM cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID371905 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID246283 | Effective concentration of the compound to inhibit HIV-1 mutant LAI replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
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AID1079935 | Cytolytic 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] | |||
AID88378 | Antiviral activity against V106A/Y181C mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID558393 | Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 200 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial 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. |
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AID1901048 | Inhibition 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 control | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs. |
AID698304 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1077222 | Antiviral activity against HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
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AID1736151 | Inhibition 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 | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
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AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID198915 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution Y181I | 2001 | Journal 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. |
AID1654218 | Drug metabolism in C57BL/6J mouse primary hepatocytes assessed as O-GlucNVP metabolite formation at 10 uM incubated for 24 hrs by uHPLC-MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID1594863 | Inhibition of HIV1 reverse transcriptase derived from HIV patient plasma by LC/MS/MS analysis | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. |
AID247499 | Inhibitory activity against HIV-1 mutant strain 138K | 2004 | Journal 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. |
AID573464 | Inhibition of RNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
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AID523355 | Antiviral activity against HIV1 with RT connection domain Y181C/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID82473 | Antiviral activity against V108I/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1884542 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID527376 | Toxicity in human CEM-SS cells | 2010 | Bioorganic & 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. |
AID650696 | Ratio of ID50 for HIV 1 reverse transcriptase K103N mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1126508 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1185997 | Antiviral 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 r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
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AID496619 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase A98G/V35T, V60I, I135L, S162A, K173A, Q174K, D177E, I178M, T200A,Q207E, R211K, V245Q, D250E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID252950 | Selectivity index of cytotoxic activity (CC50) to inhibitory activity (IC50) relative to LAI cell line | 2004 | Journal 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. |
AID666410 | Inhibition of HIV1 reverse transcriptase using poly(ra)/oligo(dT)15 homopolymer template as substrate after 1 hr | 2012 | Journal 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. |
AID698146 | Inhibition of wild type HIV1 reverse transcriptase RNA-dependent DNA polymerase activity using poly(rA)/oligo(dT)10:1 and [3H]-dTTP substrate | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1059141 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant | 2013 | Bioorganic & 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. |
AID665547 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
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AID263508 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & 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. |
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AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
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AID1171595 | Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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AID1822332 | Antiviral 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 assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
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AID717258 | Cytotoxicity against human MT4 cells by MTT assay | 2012 | Bioorganic & 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. |
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AID1565090 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
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AID648420 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1292367 | Antiviral activity against HIV1 virion infected in human TZM-bl cells after 48 hrs by firefly luciferase assay | 2016 | Bioorganic & 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. |
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AID1435513 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase K103N mutant | |||
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AID395596 | Cytotoxicity against HIV-infected human CEM cells | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones. |
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AID1057038 | Antiviral activity against HIV2 ROD infected in MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID556524 | Antiviral 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 type | 2009 | Antimicrobial 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. |
AID104804 | Tested for the cytotoxic concentration required to reduce the number of viable mock infected MT-4 cells | 1994 | Journal 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. |
AID370729 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V179D mutant expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID298080 | Antiviral activity against HIV1 RT AB1 mutant in lymphocytes assessed as reduction of p24 antigen production | 2007 | Journal 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. |
AID557042 | Antiviral activity against HIV1 isolate R8 harboring wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID608393 | Selectivity index, ratio of CC50 for MAGI-CCR5 cells to IC50 for HIV13B infected in human MAGI-CCR5 cells | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID366526 | Inhibition of RNA dependent DNA polymerase activity of wild-type HIV1 reverse transcriptase | 2008 | Journal 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. |
AID1705194 | Inhibition of RNA-dependent DNA polymerase activity of wild type recombinant HIV-1 His-tagged p66/p51 reverse transcriptase assessed as inhibition of [3H]dTTP incorporation using poly(rA)/oligo(dT) as templates incubated for 15 mins by MicroBeta scintilla | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
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AID1162263 | Selectivity index, ratio of CC50 for human MT2 cells to EC50 for X4 tropic HIV1 3B infected in human MT2 cells | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Semi-synthesis of oxygenated dolabellane diterpenes with highly in vitro anti-HIV-1 activity. |
AID1485968 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
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AID1197832 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID1162262 | Cytotoxicity against human MT2 cells after 4 to 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Semi-synthesis of oxygenated dolabellane diterpenes with highly in vitro anti-HIV-1 activity. |
AID630957 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 subtype C-VB59 | 2011 | Bioorganic & 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. |
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AID269804 | Antiviral activity against HIV1 Y181H mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269804 | Antiviral activity against HIV1 Y181H mutant | 2006 | Bioorganic & 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. |
AID1761018 | Antiviral activity against HIV-1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
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AID248263 | In vitro inhibitory concentration against HIV V179E mutant strain | 2005 | Journal 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. |
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AID1784207 | Antiviral 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 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
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AID155276 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 variant (Y181C,K103N) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & 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. |
AID1888691 | Toxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | |||
AID1435504 | Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID1316345 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1322999 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
AID678717 | Inhibition 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 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1888704 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT F227L + V106A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | |||
AID46381 | Antiviral activity against site directed resistant isolate HIV-1 V179D in CEM cells | 2001 | Journal 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. |
AID508649 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, K103N, V179L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID391687 | Inhibition of RNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity | 2008 | Journal 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. |
AID1155813 | Inhibition of wild type HIV-1 recombinant reverse transcriptase assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal 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. |
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AID198068 | Inhibition of reverse transcriptase activity of HIV-1 in the presence of [alpha35 S] TTP as cosubstrate | 1993 | Journal of medicinal chemistry, Nov-26, Volume: 36, Issue:24 | Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines. |
AID557048 | Antiviral activity against HIV1 clade F1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID717261 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & 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. |
AID508640 | Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1191974 | Selectivity index, ratio of CC50 for mock-infected human HeLa cells to EC50 for HIV2 ROD infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
AID247498 | Inhibitory activity against HIV-1 mutant strain 106A | 2004 | Journal 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. |
AID391690 | Inhibition of DNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181C mutant expressed in Escherichia coli BL21 | 2008 | Journal 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. |
AID1888694 | Antiviral activity against HIV1 with RT L100I mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID106949 | Anti-HIV-1 activity against WTIIIB HIV-1 strain in MT-4 cells | 2001 | Journal 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. |
AID1446819 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID698301 | Antiviral 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 assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1446817 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1446826 | Inhibition of wild-type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using poly(A)/oligo(dT)15 as template/primer after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID299025 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 | 2007 | Bioorganic & 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. |
AID619629 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1249720 | Antiviral activity against HIV1 expressing reverse transcriptase E138K mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID1483273 | Inhibition of HIV1 3B reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1731749 | Inhibition of reverse transcriptase Y188L mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID508641 | Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID253492 | Dose required to inhibit HIV-1 reverse transcriptase activity (V179D mutant) by 50% | 2005 | Journal 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. |
AID1418467 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID1822274 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1485966 | Inhibition 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 Pi | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID246351 | Effective concentration against human immunodeficiency virus type 1 mutated at 188L | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID1056579 | Antiviral 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 after | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID1877036 | Inhibition of recombinant HIV-1 reverse transcriptase incubated for 2 hrs by colorimetric assay | 2021 | Journal 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. |
AID1731744 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | |||
AID1654236 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID635301 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity after 5 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID1473741 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID518740 | Antiviral activity against HIV 1 subtype B harboring wild type reverse transcriptase infected in human TZM-bl cells assessed as inhibition of viral growth by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID523354 | Antiviral activity against HIV1 with RT connection domain Y181C/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID265474 | Selectivity index, TC50 for human lymphocytes/EC50 for HIV1 3B | 2006 | Journal 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. |
AID1316805 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
AID673926 | Antiviral activity against Human immunodeficiency virus 1 infected in human 293T cells assessed as inhibition of viral replication after 48 hrs by luminescence analysis | 2012 | ACS medicinal chemistry letters, Jun-14, Volume: 3, Issue:6 | Novel Cyclopropyl-Indole Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors. |
AID1572527 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID253495 | Dose required to inhibit HIV-1 reverse transcriptase activity ( L100I mutant) by 50% | 2005 | Journal 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. |
AID1561717 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of (E)-4-((4-((4-(4-(2-Cyanovinyl)-2,6-dimethylphenoxy)thieno[2,3- d]pyrimidin-2-yl)amino)piperidin-1-yl)methyl)benzenesulfonamide assessed as protection ag | |||
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AID198259 | Inhibitory concentration against mutant reverse transcriptase of L100I was determined which is in turn resistant TIBO | 1995 | Journal 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. |
AID1565091 | Antiviral activity against drug resistant HIV-1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
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AID46204 | Tested for the inhibitory activity of virus induced giant cell formation in HIV-1 infected CEM cells | 1994 | Journal 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. |
AID1072798 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV2 ROD | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays. |
AID1155806 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 NL4-3 infected in human MT4 cells | 2014 | Journal 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. |
AID1435509 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID1185998 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1784213 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID299029 | Antiviral activity against HIV1 with reverse transcriptase E138K mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
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AID586908 | Induction of MRP1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID665553 | Fold resistance, ratio of EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID248259 | In vitro inhibitory concentration against HIV K101E mutant strain | 2005 | Journal 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. |
AID276232 | Cytotoxicity against MT2 cells | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1244338 | Inhibition of HIV1 reverse transcriptase at 100 ug/ml incubated for 1 hr by ELISA method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition. |
AID279392 | Antiviral activity against HIV1 isolate with RT 100I, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1357795 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1565096 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID473117 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2010 | Bioorganic & 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. |
AID1152245 | Antiviral 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 assay | 2014 | Bioorganic & 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. |
AID449489 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus induced cytotoxicity after 5 days by MTT assay | 2009 | European 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. |
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AID1636149 | Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase K103N/V179F/Y181C mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15 | Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
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AID269803 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269803 | Antiviral activity against HIV1 V179E mutant | 2006 | Bioorganic & 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. |
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AID104802 | In vitro cytotoxicity against mock infected MT-4 cells. | 2004 | Journal 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. |
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AID1572528 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID663307 | Inhibition of HIV1 recombinant reverse transcriptase L100I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal 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. |
AID572185 | Antiviral activity against HIV-1 SM030 harboring NNTRI 100I mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID293557 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 LAI | 2007 | European 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. |
AID1822275 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID222294 | Effect of human plasma protein binding on antiviral efficacy. | 2000 | Journal 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. |
AID1815387 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID297135 | Antiviral activity against HIV1 infected CEM cells | 2007 | Journal 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. |
AID105700 | Anti-HIV-1 activity against K103N+Y181C strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID1446816 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID391683 | Antiviral activity against HIV1 infected in 8186 T cells | 2008 | Journal 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. |
AID1761017 | Antiviral activity against HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1141972 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1443670 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID693584 | Antiviral activity against HIV1 RES056 harbouring RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
AID279433 | Antiviral activity against HIV1 isolate with RT 179T mutation relative to wild type | 2007 | Antimicrobial 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. |
AID449492 | Selective index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | European 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. |
AID19262 | Aqueous solubility | 2000 | Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11 | Prediction of drug solubility from Monte Carlo simulations. |
AID198909 | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y188L | 1999 | Journal 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. |
AID1155817 | Fold resistance, ratio of ID50 for HIV-1 recombinant NNTRI-resistant reverse transcriptase K103N mutant to ID50 for wild type HIV-1 recombinant reverse transcriptase | 2014 | Journal 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. |
AID1591873 | Antiviral activity against wild-type HIV1 NL4-3 infected in human MT2 cells measured 48 hrs post-infection by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16 | Molecular and cellular studies evaluating a potent 2-cyanoindolizine catechol diether NNRTI targeting wildtype and Y181C mutant HIV-1 reverse transcriptase. |
AID299030 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
AID1815400 | Inhibition of HIV1 reverse transcriptase Y188L mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1173644 | Antiviral activity against HIV-1 LAI infected in human CEMx174-LTR-GFP CG8 cells assessed as inhibition of viral replication after 5 days | 2014 | Bioorganic & 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. |
AID557035 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID757623 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1171582 | Antiviral activity against HIV2 ROD infected in human CEM cells assessed as protection against virus-induced cytopathicity by giant cell formation assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID460296 | Inhibition of HIV1 reverse transcriptase by EIA | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1275552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1637398 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID621980 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B expressing reverse transcriptase K103N/Y181C double mutant | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1750717 | Inhibition of HIV-1 p66/p51 reverse transcriptase L100I mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID361914 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190E mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1654201 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID82276 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C+K103N strain | 2002 | Journal 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. |
AID492286 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID767501 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID1379964 | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 assessed as reduction in biotin-dUTP incorporation incubated for 40 mins using poly(rA) template and oligo(dT)16 primer by picogreen dye based spectrofluorometry | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID655387 | Cytotoxicity against human CEmx174 cells | 2012 | Bioorganic & 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. |
AID197780 | Compound was evaluated for its inhibitory activity against recombinant HIV-1 Reverse transcriptase using cell free RT inhibition assay | 2000 | Bioorganic & 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. |
AID1784214 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID1267625 | Antiviral activity against NRTI/NNRTI-resistant HIV1 L6 harboring reverse transcriptase V75I/F77L/K103N/F116Y/Q151M/M184V mutant infected in human MT4 cells | 2015 | Journal 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. |
AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
AID1152246 | Antiviral 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 assay | 2014 | Bioorganic & 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. |
AID1357798 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y188L mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID279323 | Inhibition of reverse transcriptase RTY18C mutant in HIV1 Z6gpt assessed as inhibition of ssDNA synthesis | 2007 | Antimicrobial 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. |
AID267856 | Antiviral activity against HIV1 K103N mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID571968 | Antiviral activity against HIV-1 subtype CRF02_AG V022825 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1352319 | Antiviral activity against HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID82606 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID105859 | Compound was tested for potency to achieve protection of MT-4 cells from 101E strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID1773457 | Resistance factor, ratio of EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | |||
AID1884491 | Antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID572169 | Antiviral activity against HIV-1 subtype D V022832 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID557052 | Antiviral activity against NRTI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID82476 | Antiviral activity against wild-type HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1157595 | Antiviral activity against TMC125-resistant HIV1 harboring RT 109M, 138K, 190E mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID1483272 | Inhibition of HIV1 3B reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID779529 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID1141977 | Inhibition of HIV1 wild-type reverse transcriptase Y181I/Y181C mutant using [3H]dTTP by scintillation counting | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1390711 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID561944 | Antibacterial activity against Shigella sonnei ATCC 111060 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID1565092 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | |||
AID1685255 | Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay | 2021 | ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2 | Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead. |
AID1705193 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID395595 | Antiviral activity against HIV2 ROD infected in human CEM cells assessed as inhibition of virus-induced cytopathicity after 4 days | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones. |
AID1157581 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID571986 | Antiviral activity against HIV-1 subtype C V022829 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID735081 | Antiviral activity against HIV harboring reverse transcriptase Y181C mutant by cell based assay | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID1316337 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID508752 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID619643 | Ratio of EC50 for HIV-1 3B harboring RT L100I mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1729160 | Antiviral activity against HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID317734 | Inhibition of tubulin polymerization after 20 mins | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
AID346970 | Antiviral activity against HIV 3B in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Studies on anti-HIV quinolones: new insights on the C-6 position. |
AID368558 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID198913 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution V106A | 2001 | Journal 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. |
AID1636932 | Aqueous solubility of compound in water at pH 7 by HPLC analysis | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20 | Computer-aided discovery of anti-HIV agents. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID416759 | Antiviral activity against HIV1 with reverse transcriptase Y188L mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal 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. |
AID391996 | Antiviral 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 assay | 2008 | European 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. |
AID105546 | Inhibition of mutant type (Ile100) HIV-1 (IIIB) replication in MT-4 cells | 1996 | Journal 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. |
AID1888703 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | |||
AID1862268 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors. |
AID1186005 | Antiviral 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 r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID226237 | Fold resistance (L100I/ WT) (as per ref 12 in the article) | 2001 | Bioorganic & 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. |
AID689698 | Cytotoxicity against human CEM174 cells assessed as cell viability | 2012 | ACS medicinal chemistry letters, Aug-09, Volume: 3, Issue:8 | Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors. |
AID391677 | Inhibition 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 control | 2008 | Journal 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. |
AID360707 | Inhibition of HIV1 RT K103N mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay | 2007 | The 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. |
AID83554 | Potency evaluated against wild type HIV-1 strain IIIB | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
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AID348906 | Antiviral activity against drug-resistant HIV1 with reverse transcriptase Y181C mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21 | Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
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AID260237 | Antiviral activity against HIV1 3B in MT2 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
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AID266346 | Inhibition of HIV1 reverse transcriptase K103N mutant in 293T cells | 2006 | Bioorganic & 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. |
AID368561 | Antiviral activity against HIV1 reverse transcriptase Y188L mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
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AID391692 | Inhibition of DNA dependent DNA polymerase activity of HIV2 recombinant reverse transcriptase at 140 uM | 2008 | Journal 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. |
AID586902 | Activity at MRP2 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
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AID1059142 | Inhibition of recombinant HIV1 reverse transcriptase using poly rA:dT as template/primer after 1 hr by ELISA | 2013 | Bioorganic & 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. |
AID1877039 | Potency index, ratio of test compound IC50 to NBD-14189 IC50 for inhibition of recombinant HIV-1 reverse transcriptase incubated for 2 hrs by colorimetric assay | 2021 | Journal 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. |
AID1884227 | Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID556525 | Antiviral 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 type | 2009 | Antimicrobial 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. |
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AID460295 | Inhibition of HIV1 reverse transcriptase at 20 ug/mL by EIA | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5 | Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols. |
AID279319 | Inhibition of reverse transcriptase assessed as decrease in ssDNA level in cell free virion HIV1 by NERT-based real-time PCR at 10 uM | 2007 | Antimicrobial 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. |
AID83552 | Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
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AID287004 | Inhibition of drug-resistant reverse transcriptase L100I-K103 mutant | 2007 | Journal 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. |
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AID1316333 | Cytotoxicity against human mock-infected MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
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AID665272 | Antiviral activity against HIV1 RES056 harboring K103N/Y181C RT mutant infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1609103 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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AID586900 | Activity at ABCB1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID263521 | Antiviral activity against HIV1 F227C mutant | 2006 | Bioorganic & 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. |
AID482696 | Antiviral activity against AZT-resistant HIV infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID294630 | Antiviral activity against HIV2 ROD in CEM cells | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID265471 | Activity against HIV1 3B assessed by inhibition of p24 production in human lymphocytes | 2006 | Journal 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. |
AID281485 | Antiviral activity against wild type HIV1 3B in MT4 cells after 4 days by MTT method | 2007 | Journal 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. |
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AID648422 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1373158 | Inhibition of reverse transcriptase L100I mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
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AID1292376 | Cytotoxicity against human U2OS cells assessed as cell viability at 5 uM after 48 hrs relative to control | 2016 | Bioorganic & 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. |
AID1657476 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2020 | Bioorganic & 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. |
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AID366532 | Resistance index, ratio of ID50 for reverse transcriptase L100I mutant to IC50 for wild-type HIV1 reverse transcriptase | 2008 | Journal 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. |
AID282735 | Inhibition of HIV1 RT | 2005 | Journal 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. |
AID608389 | Inhibition of HIV1 reverse transcriptase assessed as residual enzyme activity at 50 uM after 1 hr by ELISA relative to control | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID299028 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
AID557022 | Antiviral activity against HIV1 CRF01_AE harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & 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. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID263152 | Antiviral activity against HIV1 in HEK293T cells | 2006 | Bioorganic & 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. |
AID1335207 | Ratio 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 glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID614142 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17 | Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1596756 | Inhibition 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 ELISA | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Synthesis and biological evaluation of dihydroquinazoline-2-amines as potent non-nucleoside reverse transcriptase inhibitors of wild-type and mutant HIV-1 strains. |
AID366517 | Antiviral activity against HIV1 NL4-3 in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal 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. |
AID413265 | Antiviral 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 ELISA | 2008 | Journal 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). |
AID1077218 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID391691 | Inhibition of DNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I/K103N mutant expressed in Escherichia coli DH5alpha | 2008 | Journal 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. |
AID328845 | Inhibition of human MRP3 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug 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. |
AID263515 | Antiviral activity against HIV1 I135T mutant | 2006 | Bioorganic & 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. |
AID1152247 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 UG070 subtype D | 2014 | Bioorganic & 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. |
AID246275 | Effective concentration against rhuman immunodeficiency virus type 1 Y181C mutant strain | 2005 | Journal 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). |
AID1761015 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1357797 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
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AID1197833 | Resistance index, ratio of EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant to EC50 for wild type HIV1 3B | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID1574386 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1316341 | Antiviral activity against HIV1 3B harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID302252 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT IRLL98 mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal 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. |
AID650540 | Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID586326 | Cytotoxicity against PHA-stimutated human PBMC after 24 hrs by MTS assay | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
AID105539 | Inhibitory activity against HIV-1 Ile 100 mutant in MT-4 cells. | 1999 | Journal 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. |
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AID508643 | Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID197795 | Inhibition of HIV-1 reverse transcriptase using rCdG as template and dGTP as substrate | 1995 | Journal 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. |
AID1161104 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & 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. |
AID1736152 | Selectivity 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 heterodi | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID246799 | Compound 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 P225H | 2005 | Journal 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. |
AID522371 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V179D mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID82275 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected Y181C strain | 2002 | Journal 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. |
AID1175438 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for wild-type HIV-1 SF33 | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs. |
AID299027 | Antiviral activity against HIV1 with reverse transcriptase L100I mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
AID152657 | Inhibitory activity of compound on p24 production in peripheral blood mononuclear cells infected with HIV strain A17 variant. | 1999 | Bioorganic & 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. |
AID391689 | Inhibition of HIV1 BH10 recombinant reverse transcriptase p66/p51 RNase H activity assessed as residual enzyme activity | 2008 | Journal 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. |
AID1884221 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1460940 | Therapeutic 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 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID361910 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase Y188L mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID586905 | Inhibition of ABCB1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID650543 | Cytotoxicity against human MT4 cells assessed as cell viability by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID557051 | Antiviral activity against PI-resistant HIV1 harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1191973 | Cytotoxicity against mock-infected human HeLa cells by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
AID302251 | Antiviral activity against HIV1 with reverse transcriptase IRLL98 mutation in MT4 cells assessed as inhibition of viral induced cytopathic effect by MTT method | 2007 | Journal 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. |
AID366518 | Cytotoxicity against human MT4 cells by MTT assay | 2008 | Journal 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. |
AID1323000 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
AID328885 | Toxicity in human HeLa cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot | 2007 | Proceedings 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. |
AID1126507 | Antiviral activity against HIV1 harboring RT K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of viral cytopathogenicity after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID685333 | Cytotoxicity against mock-infected human MT4 cells by MTT assay | 2012 | Bioorganic & 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. |
AID1736359 | Antiviral 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 | |||
AID1773451 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring L1001 mutant infected in human MT4 cells | |||
AID46375 | Antiviral activity against site directed 4X AZT resistant isolate HIV-1 in CEM cells | 2001 | Journal 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. |
AID106600 | Cytotoxic concentration required to reduce MT-4 cell viability by 50% | 1992 | Journal 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. |
AID718372 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2012 | Bioorganic & 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. |
AID105905 | Effective dose required to achieve protection of MT-4 cells from Y181C HIV-1 induced cytopathogenicity | 2004 | Journal 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 |
AID1352322 | Antiviral activity against HIV1 harboring reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID318120 | Inhibition of HIV1 reverse transcriptase | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors. |
AID523478 | Antiviral activity against HIV1 with RT connection domain G190A/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID665551 | Antiviral 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 assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID571967 | Antiviral activity against HIV-1 subtype CRF02_AG V022808 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID391994 | Selectivity index, ratio of CC50 for human CEM cells to EC50 for HIV1 3B | 2008 | European 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. |
AID571976 | Antiviral activity against HIV-1 subtype B V022807 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID197776 | Compound was evaluated for inhibition of Y181C HIV type I reverse transcriptase. | 1995 | Journal 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. |
AID370726 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID1352312 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID622058 | Ratio of Ki for HIV1 RT p66/p66 homodimer K103N/Y181C double mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID738331 | Cytotoxicity against mock-infected human MT4 cells assessed as cell viability after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID105537 | Inhibitory activity against HIV-1 Cys 181 mutant in MT-4 cells. | 1999 | Journal 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. |
AID1729158 | Antiviral activity against HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1457055 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human ML4 cells assessed as protection against virus-induced cytopathic effect measured on day 5 post infection by MTT assay | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1357786 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID496633 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, K43R, V60I, K101R, K122E, D123S, I135V, S162A, K173T, Q174K, D177E, V179I, G196E, T200A, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID558372 | Drug level in HIV-infected pregnant woman maternal blood plasma at 200 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial 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. |
AID1743626 | Antiviral activity against HIV1 harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID1185996 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1761011 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID522368 | Antiviral activity against wild type HIV1 infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID46380 | Antiviral activity against site directed resistant isolate HIV-1 V106A in CEM cells | 2001 | Journal 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. |
AID1888705 | Resistance index, ratio of EC50 for antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 infected in human MT4 cells | |||
AID734259 | Antiviral 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 ELISA | 2013 | Journal 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. |
AID1357796 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase E138K mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID508652 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101P, K103N, V108I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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AID1729157 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID105891 | Cytotoxicity against uninfected MT-4 cells | 1995 | Journal 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. |
AID153130 | Effective dose for inhibition of viral replication in cell culture of 0.1 uM | 2000 | Journal 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. |
AID1460930 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 Bal infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID318123 | Antiviral activity against HIV2 ROD in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors. |
AID1391087 | Antiviral activity against HIV1 harboring reverse transcriptase RES056 double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1520058 | Antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1057039 | Antiviral 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 assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID263512 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & 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. |
AID619635 | Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID665271 | Antiviral activity against HIV1 3B harboring wild type RT infected in MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID508797 | Ratio of EC50 for HIV1 in presence of 45 mg/ml HSA to EC50 for HIV1 in absence of serum proteins by GFP assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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AID155273 | Ability to inhibit the replication of RT-MDR (V106A) strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & 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. |
AID279464 | Antiviral activity against HIV1 isolate with RT 101Q, 103N, 225H mutation relative to wild type | 2007 | Antimicrobial 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. |
AID366528 | Resistance index, ratio of ID50 for reverse transcriptase K103N mutant to IC50 for wild-type HIV1 sreverse transcriptase | 2008 | Journal 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. |
AID1520057 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID508634 | Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID287000 | Inhibition of RNase H activity of HIV1 reverse transcriptase | 2007 | Journal 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. |
AID198080 | Inhibitory activity against HIV-1 Mutant Reverse transcriptase V106A | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
AID266345 | Inhibition of wild type HIV1 reverse transcriptase in 293T cells | 2006 | Bioorganic & 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. |
AID197934 | HIV-1 reverse transcriptase inhibitory activity against Wild Type Reverse transcriptase using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal 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. |
AID302268 | Resistance index, ratio of Ki for HIV1 reverse transcriptase V106A mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal 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. |
AID1731748 | Inhibition of reverse transcriptase Y183C mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID1171578 | Cytotoxic activity against human MT4 cells by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1483275 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID735080 | Ratio of EC50 for HIV harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID573468 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase DNA-dependent DNA polymerase activity by gel-based primer extension assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1572526 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID457959 | Inhibition of HIV1 reverse transcriptase L100I mutant by RNA-dependent DNA polymerase activity assay | 2010 | Bioorganic & 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. |
AID1072797 | Inhibition of HIV1 reverse transcriptase assessed as inhibition of biotinylated dUTP incorporation after 1 hr by ELISA | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays. |
AID1775803 | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into template | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | 2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies. |
AID1335212 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID1610039 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 92/BR/018 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID1763903 | Antiviral activity against HIV-1 IIIB harboring RT F227L/V106A mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID405412 | Antiviral activity against PERV infected in human 293T cells assessed as inhibition of proximal DNA synthesis after 24 hrs by RT-PCR | 2007 | Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7 | Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates. |
AID586906 | Inhibition of BCRP activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1822276 | Antiviral activity against HIV-1 harboring RT L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
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AID444051 | Total clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
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AID508782 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138Q mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1390715 | Resistance index, ratio of EC50 for HIV1 RES056 harboring K103N/Y181C double mutant infected in human MT4 cells to EC50 for wild-type HIV1 3B infected in human MT4 cells | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1761019 | Antiviral activity against HIV-1 harboring reverse transcriptase F227L/V106A mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID247495 | Inhibitory activity against HIV-1 mutant strain 100I | 2004 | Journal 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. |
AID298061 | Antiviral activity against HIV1 3B in human MT4 cells by XTT assay | 2007 | Journal 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. |
AID632799 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID1743618 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID105523 | Inhibition of HIV-1(IIIB) variants (Ile100/Asn103) in HIV-1 MT-4 cells | 1996 | Journal 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. |
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AID482700 | Cytotoxicity against human Jurkat A72 cells by MTT assay | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID247505 | Inhibitory activity against HIV-1 mutant strain 227C | 2004 | Journal 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. |
AID622049 | Inhibition 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 counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1811036 | Anti-viral activity against HIV1 harboring RT Y181C mutant infected MV4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID281486 | Cytotoxicity against MT4 cells after 4 days by MTT method | 2007 | Journal 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. |
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AID1435514 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase Y181C mutant | |||
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AID1163253 | Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID105866 | Compound was tested for potency to achieve protection of MT-4 cells from LAI strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID1636147 | Antiviral activity against NNRTI resistant HIV1 harboring reverse transcriptase V106I/Y181C/G190A/H221Y mutant assessed as inhibition of viral infection in human TZM-bl cells after 48 hrs by luciferase reporter gene assay | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15 | Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID366531 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase L100I mutant | 2008 | Journal 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. |
AID1335217 | Inhibition 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 hr | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
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AID523480 | Antiviral activity against HIV1 with RT connection domain G190S/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID1763906 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & 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. |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269688 | Antiviral activity against HIV1 NNTRI resistant K103N mutant | 2006 | Bioorganic & 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. |
AID1784209 | Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID1249716 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 4 days by MTT assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID199993 | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 6 in the article) | 2001 | Bioorganic & 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. |
AID1316340 | Antiviral activity against HIV1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
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AID622053 | Ratio of Ki for HIV1 RT p66/p66 homodimer L100I mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID198910 | In vitro inhibitory activity against HIV-1 wild type reverse transcriptase (RT) | 1999 | Journal 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. |
AID586911 | Induction of SLCO1B1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID105326 | Inhibition of HIV-1 (IIIB) induced cytopathicity in MT-4 cells. | 2004 | Journal 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. |
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AID298090 | Inhibition of HIV1 RT L100I mutant | 2007 | Journal 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. |
AID440083 | Antiviral activity against HIV1 HXB2 harboring 227C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID508637 | Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID96296 | Compound was evaluated for antiviral activity against L100I mutant virus; ND is Not Determined. | 2000 | Journal 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. |
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AID726439 | Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID482694 | Antiviral activity against HIV2 ROD infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID235264 | Selectivity index is ratio of CC50 to that of EC50 | 2000 | Bioorganic & 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. |
AID1773454 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y188L mutant infected in human MT4 cells | |||
AID253494 | Dose required to inhibit HIV-1 reverse transcriptase activity (Y188L mutant) by 50% | 2005 | Journal 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. |
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AID1687686 | Cytotoxicity against human MT4 cells assessed as inhibition of cell viability by measuring reduction in absorbance at OD540 by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
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AID583847 | Antiviral 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 HIV | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. |
AID371903 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID1594864 | Oral bioavailability in human | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | The Journey of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) from Lab to Clinic. |
AID302250 | Selectivity index, ratio of CC50 for MT4 cells to EC50 for HIV1 NL43 infected MT4 cells | 2007 | Journal 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. |
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AID1157584 | Antiviral activity against A17-sensitive HIV1 harboring 103N, 181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID252955 | Ratio of CC50 and EC50 against wild type human immunodeficiency virus type 1 LAI strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID717260 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity by MTT assay | 2012 | Bioorganic & 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. |
AID1880379 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y188L mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
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AID525108 | Antiviral 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 compound | 2008 | Antimicrobial 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. |
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AID1537495 | Cytotoxicity against HEK293T cells assessed as reduction in cell viability after 48 hrs by CellTiter 96 aqueous one solution assay | 2019 | ACS medicinal chemistry letters, Feb-14, Volume: 10, Issue:2 | Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. |
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AID198410 | Tested for the inhibition of mutant type (Ile100) HIV-1 (IIIB) RT | 1996 | Journal 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. |
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AID198396 | Inhibitory activity against HIV-1 reverse transcriptase (HIV-RT) | 1993 | Journal 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. |
AID1456306 | Inhibition of HIV-1 3B wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID508776 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179T mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID518739 | Selectivity ratio of IC50 for DNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID293555 | Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay | 2007 | European 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. |
AID586324 | Inhibition of HIV1 3B reverse transcriptase activity | 2011 | Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6 | Antiviral activity of seed extract from Citrus bergamia towards human retroviruses. |
AID1141973 | Ratio of EC50 for HIV1 harboring reverse transcriptase L1001 mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID82604 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1357805 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1446812 | Antiviral activity against HIV-2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization. |
AID1636930 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against viral infection by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20 | Computer-aided discovery of anti-HIV agents. |
AID1736362 | Selectivity 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 | |||
AID1228737 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1-3B | 2015 | Journal of natural products, May-22, Volume: 78, Issue:5 | Antiviral Activity of Flexibilane and Tigliane Diterpenoids from Stillingia lineata. |
AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug 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. |
AID82469 | Antiviral activity against V106A/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID279479 | Antiviral activity against HIV1 isolate with RT 179D, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1784212 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID1171593 | Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID389379 | Cytotoxicity against human MT4 cells | 2008 | Bioorganic & 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. |
AID1435525 | Inhibition of recombinant wild type HIV1 reverse transcriptase using poly (A).oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA | |||
AID44798 | In vitro concentration required to reduce the amount of p24 by 90% in WTIIIB infected C8166 cells | 2004 | Journal 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. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & 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. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269687 | Antiviral activity against HIV1 NNTRI resistant Y181C mutant | 2006 | Bioorganic & 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. |
AID257167 | Antiviral activity against HIV1 IRLL98 mutant strain infected MT4 cells by MTT method | 2005 | Journal 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. |
AID235708 | Selectivity index measured as the ratio of CC50 / EC50. | 1999 | Journal 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. |
AID82464 | Antiviral activity against K103N/Y181C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID757622 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1485965 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID83551 | Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID1391082 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID1705187 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1741396 | Inhibition of reverse transcriptase Y188L mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID242545 | Fold increase in inhibitory concentration against HIV 1 reverse transcriptase mutant type Ile100 over wild type HIV 1 reverse transcriptase | 2004 | Journal 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. |
AID482701 | Selectivity index, ratio of CC50 for human Jurkat A72 cells to EC50 for HIV1 3B | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID767497 | Cytotoxicity against human MT2 cells assessed as growth inhibition | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
AID1186689 | Selectivity 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 cells | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Fused 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. |
AID496627 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K32R, V35E, T39S, S48T, V60I, D121Y, K122E, I135T, S162A, K173A, Q174K, D177E, V179I, T200E, Q207D, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID522577 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V106I mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID482697 | Antiviral activity against HIV S056 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID199994 | Effective concentration required against L100I mutant HIV-1 reverse transcriptase (as per ref 7 in the article) | 2001 | Bioorganic & 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. |
AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1267609 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Journal 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. |
AID79121 | Inhibitory activity against multidrug resistant HIV-1 strain RT-MDR | 2000 | Bioorganic & 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. |
AID105715 | Antiviral activity against HIV-1 resistant to 2-(2-Benzoyl-4-chloro-phenyl)-N-[4-(3-dimethylamino-propoxy)-2-methyl-phenyl]-acetamide in MT-4 cells | 1995 | Journal 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. |
AID105704 | Anti-HIV-1 activity against Y181C strain, in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID297139 | Antiviral activity against HIV1 with RT K101E mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID360710 | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA PPT primed substrate by scintillation proximity assay | 2007 | The 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. |
AID373387 | Antiviral 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 assay | 2007 | Antimicrobial 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. |
AID522376 | Resistance index, ratio of EC50 for recombinant HIV1 harboring reverse transcriptase V179D mutant clone to EC50 for wild type HIV1 | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID1685254 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2 | Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead. |
AID1171592 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574389 | Resistance 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/p51 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID246203 | Concentration required to achieve 50% protection of infected MT-4 cells from Y181C-HIV-1 strain | 2005 | Journal 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. |
AID1741393 | Inhibition of reverse transcriptase L100I mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID1141967 | Antiviral 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 method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID279481 | Antiviral activity against HIV1 isolate with RT 101E mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1741399 | Inhibition of reverse transcriptase RES056 mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID650695 | Ratio of ID50 for HIV 1 reverse transcriptase L100I mutant to ID50 for wild type HIV 1 NL4-3 reverse transcriptase | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID1244340 | Anti-trichomonas activity against MTZ-susceptible Trichomonas vaginalis incubated for 3 to 48 hrs by trypan blue exclusion assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | N-Alkyl/aryl-4-(3-substituted-3-phenylpropyl)piperazine-1-carbothioamide as dual-action vaginal microbicides with reverse transcriptase inhibition. |
AID557021 | Antiviral activity against HIV1 CRF02_AG harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID573482 | Fold resistance, ratio of EC50 for Human immunodeficiency virus 1 isolate 9225 harboring A98S, G190A mutation in reverse transcriptase to wild-type | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID366529 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase Y181I mutant | 2008 | Journal 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. |
AID1275543 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID235859 | CC50/EC50 ratio of the compound | 2001 | Journal 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. |
AID391686 | Antiviral activity against HIV1 infected in human 293T cells | 2008 | Journal 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. |
AID678721 | Metabolic stability in human liver microsomes assessed as GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1231485 | Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID360709 | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using RNA/DNAM duplex primed substrate by scintillation proximity assay | 2007 | The 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. |
AID557050 | Antiviral activity against HIV1 clade H harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID663308 | Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal 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. |
AID630787 | Antiviral 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 assay | 2011 | Bioorganic & 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. |
AID297143 | Antiviral activity against HIV1 with RT Y188C mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID522370 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106I mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1316804 | Antiviral activity against HIV-2 ROD infected in human MT-4 cells assessed as protection against virus induced cytopathic effect after 5 days by MTT assay | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Synthesis of arylated coumarins by Suzuki-Miyaura cross-coupling. Reactions and anti-HIV activity. |
AID619637 | Antiviral activity against HIV-1 3B harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID366522 | Antiviral activity against HIV1 isolates with reverse transcriptase Y181C mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal 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. |
AID1141960 | Antiviral 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 method | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID246519 | Effective concentration against human immunodeficiency virus type 1 mutated at 227L+106A; ND:Not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug 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. |
AID1815382 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID298081 | Selectivity index, ratio of TC50 for lymphocytes to ED50 for HIV1 3B | 2007 | Journal 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. |
AID1731753 | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into wild type RT measured after 1 hr by ELISA | |||
AID235503 | Selectivity index calculated as the ratio between CC50 and EC50 | 1995 | Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17 | Synthesis and anti-HIV-1 activity of thio analogues of dihydroalkoxybenzyloxopyrimidines. |
AID1249707 | Antiviral activity against wild-type HIV-1 infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Discovery of potent HIV-1 non-nucleoside reverse transcriptase inhibitors from arylthioacetanilide structural motif. |
AID1435508 | Antiviral activity against HIV1 expressing reverse transcriptase F227L/V106A double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID1520061 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B harbouring NNRTI K103N mutant infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID82468 | Antiviral activity against V106A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1200844 | Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID279461 | Antiviral activity against HIV1 isolate with RT 179D, 188L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID635346 | Cytotoxicity against human MT4 cells measured by MTT assay | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID1228840 | Antiviral 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 assay | 2015 | Journal of natural products, Jun-26, Volume: 78, Issue:6 | Limonoids with Anti-HIV Activity from Cipadessa cinerascens. |
AID1743621 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID499279 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for HIV2 ROD | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
AID499275 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
AID1157594 | Antiviral activity against TMC120-resistant HIV1 harboring RT 100I, 138G mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID698298 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1435506 | Antiviral activity against HIV1 expressing reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID368569 | Inhibition of HIV1 recombinant reverse transcriptase K103N mutant-DNA-dNTP ternary complex expressed in Escherichia coli BL21 | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID1320866 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B expressing wild type reverse transcriptase | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1171579 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1485971 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID1152248 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 VB59 subtype C | 2014 | Bioorganic & 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. |
AID736443 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID649827 | Cytotoxicity against human CEMx174 cells | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID279460 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID348905 | Antiviral activity against drug-resistant HIV1 with reverse transcriptase K103N mutant infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21 | Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID152788 | Tested for the ability to inhibit the replication of HIV-1 strain HTLV IIIB in human peripheral blood mononuclear cells (PBMC) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1322998 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
AID1377175 | Antiviral activity against NNRTI-resistant HIV1 isolate N119 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6 | Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
AID370727 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y181I mutant expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & 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. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269802 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & 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. |
AID630955 | Antiviral 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 assay | 2011 | Bioorganic & 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. |
AID248492 | In vitro inhibitory concentration against HIV K101E and K103N mutant strain | 2005 | Journal 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. |
AID1572521 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | |||
AID608390 | Inhibition of HIV1 reverse transcriptase assessed as residual enzyme activity at 50 uM after 1 hr by ELISA | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID508751 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, F227C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1884489 | Antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID197792 | Compound was tested for Inhibition of HIV-1 RT activity. | 1996 | Journal 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. |
AID430056 | Cytotoxicity against human MT4 cells after 5 days | 2009 | Bioorganic & 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. |
AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID199999 | Effective concentration required against wild type HIV-1 reverse transcriptase (as per ref 7 in the article) | 2001 | Bioorganic & 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. |
AID106777 | Compound 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 culture | 1992 | Journal 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. |
AID198400 | Tested for inhibitory concentration on HIV-1 Reverse transcriptase in the presence of poly(c)-oligo-(dG) | 2000 | Journal 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. |
AID1460944 | Therapeutic 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 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID299024 | Cytotoxicity against MT4 cells assessed as reduction of cell viability | 2007 | Bioorganic & 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. |
AID1705188 | Antiviral activity against HIV1 harboring RT Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID619632 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID496615 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, K64R, K102Q, D123E, S162A, K173T, Q174K, D177E, G196E,T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID279410 | Antiviral activity against HIV1 isolate with RT 179E mutation relative to wild type | 2007 | Antimicrobial 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. |
AID104785 | Cytotoxic concentration based on the reduction of viability of mock-infected cells | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
AID248256 | In vitro inhibitory concentration against HIV F227C mutant strain | 2005 | Journal 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. |
AID561941 | Antibacterial activity against Haemophilus influenzae ATCC 4927 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID1687681 | Antiviral activity against HIV-1 K103N mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID1460938 | Therapeutic index, ratio of TC50 for human MAGI-CCR5 cells to IC50 for HIV-1 NL4-3 infected in MAGI-CCR5 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID523483 | Antiviral activity against HIV1 with RT connection domain L100I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID1811046 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to IC50 for HIV1 IIIB infected human MT4 cells | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID496617 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, E36D, T39K, I50V, V60I, S68G, I135V, S162A, K173V, Q174K,D177E, T200A, E203Q, Q207D, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1572522 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | |||
AID246517 | Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N; ND:Not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID279321 | Inhibition of reverse transcriptase activity in HIV1 infected HeLa-MAGI cells at 37 deg C after 48 hrs | 2007 | Antimicrobial 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. |
AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19 | Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
AID1357790 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1156487 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID1609110 | Inhibition of recombinant HIV-1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye based spectrofluorometric assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1815381 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1186684 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as protection from viral cytopathicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Fused 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. |
AID267645 | Antiviral activity against wild type HIV1 virus | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID698302 | Antiviral 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 assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1357799 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase F227L/V106A mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1304400 | Antiviral activity against HIV-1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID476468 | Cytotoxicity against human MT2 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID105571 | Antiviral activity was determined against wild type HIV-1 in MT-4 cells infected with HIV-1 IIIB using an XTT assay | 1998 | Bioorganic & 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. |
AID1572525 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID1171580 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1435505 | Antiviral activity against HIV1 expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | |||
AID1736150 | Inhibition 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 incuba | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID1292365 | Inhibition 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 sci | 2016 | Bioorganic & 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. |
AID444053 | Renal clearance in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1141970 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1152371 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1156484 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Design and synthesis of a new series of modified CH-diarylpyrimidines as drug-resistant HIV non-nucleoside reverse transcriptase inhibitors. |
AID1249717 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID287006 | Inhibition of reverse transcriptase binding to DNA assessed as formation of RT-DNA complex by gel mobility shift assay | 2007 | Journal 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. |
AID1460933 | Therapeutic index, ratio of TC50 for human PBMC to IC50 for HIV-1 Bal infected in human PBMC | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID391685 | Antiviral activity against HIV1 infected in human CEM cells | 2008 | Journal 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. |
AID557037 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 50% human serum | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID242248 | Concentration required for 50% inhibition of human immunodeficiency virus type 1 reverse transcriptase mutant type Cys181 | 2004 | Journal 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. |
AID666416 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for NNRTI-resistant HIV1 A17 expressing reverse transcriptase K103N and Y181C mutant | 2012 | Journal 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. |
AID632795 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID586907 | Induction of ABCB1 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID297138 | Antiviral activity against HIV1 with RT L100I mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID508653 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID246300 | Effective concentration of the compound to inhibit HIV-1 mutant Y181C replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID678713 | Inhibition 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 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID105863 | Compound was tested for potency to achieve protection of MT-4 cells from 188L strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID1175435 | Inhibition of HIV-1 recombinant reverse transcriptase after 1 hr by streptavidinalkaline phosphatase reporter system | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs. |
AID282736 | Inhibition of HIV1 RT L100I mutant | 2005 | Journal 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. |
AID1152243 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for R5 tropic Human immunodeficiency virus 1 ADA5 subtype B | 2014 | Bioorganic & 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. |
AID1705191 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID665275 | Selectivity index ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID518734 | Inhibition of RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by filter-based filtration assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID105543 | Inhibition of wild type HIV-1 in MT-4 cell culture (human T cell line) | 1999 | Journal 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. |
AID586903 | Activity at MRP3 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID1069710 | Inhibition 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 analysis | 2014 | Bioorganic & 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. |
AID457956 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed inhibition of viral-induced cytopathic effect after 5 days | 2010 | Bioorganic & 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. |
AID1231488 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13 | Anti-HIV diarylpyrimidine-quinolone hybrids and their mode of action. |
AID440081 | Antiviral activity against HIV1 HXB2 harboring 190A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID717256 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2012 | Bioorganic & 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. |
AID155290 | Inhibit the replication of the HIV-1 strain HTLV111B in human peripheral blood mononuclear cell | 2000 | Bioorganic & 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. |
AID235701 | Selectivity index is the ratio of CC50 and EC50 in MT-4 cells. | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
AID440082 | Antiviral activity against HIV1 HXB2 harboring 190S mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID572181 | Antiviral activity against HIV-1 SM007 harboring NNTRI 103N mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID591001 | Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay | 2011 | Bioorganic & 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. |
AID279409 | Antiviral activity against HIV1 isolate with RT 101P, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1773448 | Antiviral activity against wild type HIV1 harboring Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1079936 | Choleostatic 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] | |||
AID1822279 | Antiviral activity against HIV-1 harboring Y188L mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID491828 | Antiviral activity against HIV1 with reverse transcriptase A17 (K103N, Y181C) mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1736360 | Antiviral 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 | |||
AID351451 | Hydrolytic stability in rat plasma assessed as half life by electrospray ionization mass spectrometry | 2009 | European 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. |
AID1729163 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation into template incubated for 1 hr by ELISA | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID1761016 | Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID561943 | Antibacterial activity against Staphylococcus aureus ATCC 29213 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID1888697 | Antiviral activity against HIV1 with RT Y188L mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID1320869 | Inhibition of recombinant wild type HIV1 p66/p51 using poly(rA) template/oligo(dT)16 primer after 40 mins by PicoGreen-based spectrofluorometric method | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Structural optimization of pyridine-type DAPY derivatives to exploit the tolerant regions of the NNRTI binding pocket. |
AID1884493 | Antiviral activity against drug-resistant HIV-1 E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1565098 | Antiviral activity against drug resistant HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID373571 | Antiviral 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 assay | 2007 | Antimicrobial 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. |
AID496623 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/G18V, Q23P, V35T, E40D, V60I, S68G, D123E, I135V, S162A, K173T, Q174N, T200A, Q207E, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID496626 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K22N, V35T, T39A, K122E, I135V, T139A, S162A, K173T, Q174A, D177E, T200A, Q207E, R211K, F214L mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1456311 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B wild type reverse transcriptase infected in human MT4 cells | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
AID267650 | Antiviral activity against HIV1 K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID482693 | Antiviral activity against HIV1 3B infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID198758 | Percent inhibitory activity against wild type (WT) HIV type I reverse transcriptase at a concentration of 1 uM | 1995 | Journal 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. |
AID371908 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID82475 | Antiviral activity against Y188C strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID525102 | Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay | 2008 | Antimicrobial 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. |
AID81597 | Inhibitory activity against NNI-resistant HIV-1 strain A17 with Y181C,K103N mutation | 2000 | Bioorganic & 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. |
AID88384 | Antiviral activity against wild-type HIV-1 in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID279404 | Antiviral activity against HIV1 isolate with RT 103N, 181C, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1352321 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103 N/Y181C double mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID302270 | Resistance index, ratio of Ki for HIV1 reverse transcriptase Y181I mutant to Ki for wild type HIV1 3B reverse transcriptase | 2007 | Journal 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. |
AID1165078 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID1335210 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID368565 | Inhibition of wild type HIV1 reverse transcriptase-DNA binary complex | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1473740 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID622056 | Ratio of Ki for HIV1 RT p66/p66 homodimer Y188L mutant to Ki for wild-type HIV1 RT p66/p66 homodimer | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1741391 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID492045 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & 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. |
AID1558858 | Inhibition of recombinant wild type HIV1 reverse transcriptase p66/p51 incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID267858 | Antiviral activity against HIV1 Y188L mutant in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID1175437 | Cytotoxicity against human TZM-bl cells after 3 days by XTT assay | 2015 | Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs. |
AID197799 | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (Y181C) | 1998 | Bioorganic & 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. |
AID279446 | Antiviral activity against HIV1 isolate with RT 101Q, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1637387 | Inhibition of HIV-1 reverse transcriptase assessed as reduction in biotin-duTP incorporation using biotin-labeled dUTP and hybrid poly(A)-oligo (dT)15 template primer after 2 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID525104 | Antiviral 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 compound | 2008 | Antimicrobial 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. |
AID491834 | Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID573476 | Antiviral activity of wild-type Human immunodeficiency virus 1 isolate 5512 by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1077219 | Selectivity 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 cells | 2014 | European journal of medicinal chemistry, Apr-09, Volume: 76 | Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach. |
AID572176 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID1380572 | Resistance 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 ag | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents. |
AID1391076 | Inhibition of wild type HIV1 reverse transcriptase using poly (A)/oligo (dT)15 as template/primer assessed as decrease in biotin-dUTP incorporation after 1 hr by ELISA | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID492285 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID1335209 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID259754 | Antiviral activity against wild-type HIV1 in MT2 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1761006 | Antiviral activity against wild type HIV1 NL4-3 infected in human TZM-bl cells assessed as reduction in viral infection measured after 1 day by luciferase reporter gene assay based luminiscence assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID279406 | Antiviral activity against HIV1 isolate with RT 103N, 238T mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1171591 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase L100I mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1884538 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 L100I mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1736348 | Antiviral 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 | |||
AID248491 | In vitro inhibitory concentration against HIV F227L and V106A mutant strain | 2005 | Journal 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. |
AID734266 | Antiviral activity against Human immunodeficiency virus 1 SF33 infected in human TZM-bl cells assessed decrease in p24 level after 7 days by ELISA | 2013 | Journal 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. |
AID82608 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1773456 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells | |||
AID1687680 | Antiviral activity against wild type HIV-1 strain 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID1126510 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to IC50 for HIV1 3B infected in human MT4 cells | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1627029 | Inhibition 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 assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID267854 | Antiviral activity against wild type HIV1 NL4-3 in MT4 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and biological investigation of S-aryl-S-DABO derivatives as HIV-1 inhibitors. |
AID282739 | Inhibition of HIV1 RT Y181I mutant | 2005 | Journal 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. |
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AID230127 | Tested for the ratio between CC50 (MT-4) to EC50 (MT-4) | 1994 | Journal 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. |
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
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AID1155810 | Fold 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 cells | 2014 | Journal 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. |
AID1380574 | Resistance 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 activ | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents. |
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AID1741392 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
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AID1773453 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring Y18IC mutant infected in human MT4 cells | |||
AID779528 | Antiviral 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 assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID508770 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID491833 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13 | Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID508651 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I, V179I, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID525113 | Antiviral 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 assay | 2008 | Antimicrobial 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. |
AID279395 | Antiviral activity against HIV1 isolate with RT 101Q mutation relative to wild type | 2007 | Antimicrobial 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. |
AID368562 | Cytotoxicity against human MT4 cells by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1171596 | Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activity | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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AID279441 | Antiviral activity against HIV1 isolate with RT 101Q, 190S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1249718 | Antiviral activity against HIV1 expressing reverse transcriptase L100I mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID663300 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 NL4-3 | 2012 | Journal 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. |
AID496624 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/A33E, V35T, T39A, D123E, S162A, Q174G, T200E, I202V, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID279425 | Antiviral activity against HIV1 isolate with RT 179G mutation relative to wild type | 2007 | Antimicrobial 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. |
AID81442 | Inhibition of HIV-1 D34 replication in human peripheral blood mononuclear cells. | 1993 | Journal 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 |
AID1079933 | Acute 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 | |||
AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
AID1743619 | Antiviral activity against HIV1 RES056 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID197797 | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (L1001) | 1998 | Bioorganic & 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. |
AID587751 | Antiviral 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 10 | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID619642 | Ratio of EC50 for HIV-1 3B harboring RT E138K mutant infected in human MT4 cells to EC50 for wild type HIV-1 3B infected in human MT4 cells | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID384955 | Intrinsic aqueous solubility at pH 10 by shake-flask method | 2008 | Journal of medicinal chemistry, May-22, Volume: 51, Issue:10 | Molecular characteristics for solid-state limited solubility. |
AID1171583 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID525114 | Antiviral 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 assay | 2008 | Antimicrobial 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. |
AID279420 | Antiviral activity against HIV1 isolate with RT 190S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID508769 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase H221Y mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID368555 | Inhibition of wild type HIV1 reverse transcriptase-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID106950 | Anti-HIV-1 activity against Y181C HIV-1 strain in MT-4 cells | 2001 | Journal 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. |
AID443750 | Antiviral activity against 100 TCID50 HIV1 infected in human TZM-b1 cells assessed as inhibition of viral replication by pseudovirus based assay | 2010 | Journal 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. |
AID1072804 | Antiviral 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 assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6 | Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays. |
AID1731745 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV IIIB | |||
AID46385 | Antiviral activity against site directed wild-type enzyme isolate HIV-1 NL4-3WT in CEM cells | 2001 | Journal 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. |
AID685330 | Antiviral activity against HIV-1 RES056 harboring RT K103N/Y181C mutant gene infected human MT4 cells assessed as inhibition in viral syncytium formation by MTT assay | 2012 | Bioorganic & 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. |
AID1736365 | Selectivity 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 | |||
AID523481 | Antiviral activity against HIV1 with RT connection domain G190S/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID246189 | Effective concentration against human immunodeficiency virus type 1 wild type | 2005 | Journal 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). |
AID1773461 | Resistance factor, ratio of EC50 for HIV1 harboring E138K mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | |||
AID1736344 | Antiviral 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 | |||
AID257169 | Antiviral activity against HIV1 Y188L mutant strain infected MT4 cells by MTT method | 2005 | Journal 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. |
AID1191402 | Cytotoxicity against human MT4 cells after 5 days MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1275554 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV2 ROD infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1654241 | Toxicity 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%) | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID82607 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID734271 | Cytotoxicity against human TZM-bl cells | 2013 | Journal 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. |
AID1335204 | Ratio 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 glycoprotein | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID508758 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1163233 | Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID1520060 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID508771 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase G190A mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID302260 | Inhibition of HIV1 reverse transcriptase K103N mutant | 2007 | Journal 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. |
AID1884224 | Antiviral activity against HIV-1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1249719 | Antiviral activity against HIV1 expressing reverse transcriptase K103N mutant | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID1380571 | 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 assessed as inhibition of viral replication using compound pre-mixed | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents. |
AID82459 | Antiviral activity against K103N strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1636927 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against viral infection by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20 | Computer-aided discovery of anti-HIV agents. |
AID587742 | Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID571987 | Antiviral activity against HIV-1 subtype C V022831 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1880369 | Inhibition of HIV-1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorometric analysis | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
AID1654220 | Drug metabolism in human primary hepatocytes assessed as O-GlucNVP metabolite formation at 10 uM incubated for 24 hrs by uHPLC-MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID302262 | Inhibition of HIV1 reverse transcriptase V106A mutant | 2007 | Journal 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. |
AID444056 | Fraction escaping gut-wall elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1162233 | Antiviral activity against HIV1 | 2014 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 24, Issue:18 | Novel indole based NNRTIs with improved potency against wild type and resistant HIV. |
AID1654208 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1141961 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4.3 infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1373159 | Inhibition of reverse transcriptase K103N mutant in HIV1 infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
AID496632 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I/V35T, T39L, K122E, D123N, S162A, E169T, K173E, Q174E, D177E,T200A, I202V, Q207E mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1815391 | Inhibition of HIV1 reverse transcriptase K103N/Y181C double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID328846 | Inhibition of human MRP1 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay | 2007 | Drug 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. |
AID279408 | Antiviral activity against HIV1 isolate with RT 101Q, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1316343 | Selectivity index, ratio of CC50 for human mock-infected MT4 cells to EC50 for HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID246298 | Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1435516 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 expressing reverse transcriptase E138K mutant | |||
AID246780 | Compound concentration required to reduce the amount of p24 by 90% in wtIIIBinfected C8166 cells | 2005 | Journal 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. |
AID508762 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E, K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID572189 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID1380569 | 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 assessed as inhibition of viral replication using compound pre-mixed | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Design, synthesis and biological evaluation of substituted (+)-SG-1 derivatives as novel anti-HIV agents. |
AID266347 | Inhibition of HIV1 reverse transcriptase Y181C mutant in 293T cells | 2006 | Bioorganic & 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. |
AID630786 | Inhibition of biotin-dNTP labeled HIV-1 reverse transcriptase using ABST as substrate at 100 ug/ml after 1 hr by ELISA | 2011 | Bioorganic & 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. |
AID366519 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2008 | Journal 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. |
AID1773458 | Resistance factor, ratio of EC50 for HIV1 harboring K103N mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | |||
AID571974 | Antiviral activity against HIV-1 subtype CRF01_AE V029521 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID344815 | Antiviral activity against HIV1 NL4-3 infected in HEK293T cells assessed as inhibition of virion-associated p24 antigen production after 24 hrs by ELISA | 2008 | Bioorganic & 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. |
AID346971 | Antiviral activity against HIV ROD in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2 | Studies on anti-HIV quinolones: new insights on the C-6 position. |
AID104772 | Concentration required to reduce the viability of mock-infected MT-4 cells by 50% | 1996 | Journal 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. |
AID457957 | Cytotoxicity in human MT4 cells assessed as reduction in cell viability | 2010 | Bioorganic & 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. |
AID1485969 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID197803 | Inhibitory effect on wild type HIV- 1 reverse transcriptase using rCdG as template and dGTP as substrate. | 1998 | Bioorganic & 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. |
AID1637389 | Antiviral activity against human HIV-1 3B harboring RES056 mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID389378 | Antiviral activity against HIV1 3B in human MT4 cells assessed as protection of cell against virus-induced cytopathogenicity | 2008 | Bioorganic & 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. |
AID766743 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 | 2013 | Bioorganic & 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. |
AID572170 | Antiviral activity against HIV-1 subtype D V022818 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID322393 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2008 | Bioorganic & 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). |
AID492043 | Inhibition of HIV1 reverse transcriptase | 2010 | Bioorganic & 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. |
AID1248226 | Antiviral activity against wild type HIV 2 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID199980 | Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) | 2002 | Journal 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. |
AID518736 | Selectivity ratio of IC50 for RNA-dependent DNA polymerase activity of HIV1 subtype B reverse transcriptase M230L mutant to IC50 for RNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID663313 | Resistance ratio of ID50 for HIV1 reverse transcriptase Y181I mutant to ID50 HIV1 wild type reverse transcriptase | 2012 | Journal 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. |
AID260238 | Cytotoxicity against human MT2 cells by MTT assay | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1705185 | Selectivity ratio of CC50 for human MT4 cells to EC50 for antiviral activity against HIV-1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID1743620 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID317731 | Antiviral activity against HIV2ROD infected in human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
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AID663309 | Inhibition of HIV1 recombinant reverse transcriptase V106A mutant assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal 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. |
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AID1880378 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase Y181C mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
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AID1241792 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase. |
AID1197835 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA after 1 hr using poly(A) x oligo(dT)15 template/primer hybrid, digoxigenin and biotin-labeled nucleotides | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
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AID247503 | Inhibitory activity against HIV-1 mutant strain 190A | 2004 | Journal 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. |
AID279455 | Antiviral activity against HIV1 isolate with RT 103N, 188H mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1655526 | Inhibition 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 incorporat | 2020 | ACS 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. |
AID361912 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190A mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1191399 | Antiviral activity against wild type HIV-1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID276231 | Antiviral activity against HIV1 3B in MT2 cells | 2006 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 16, Issue:21 | Optimization of pyrimidinyl- and triazinyl-amines as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1784208 | Antiviral activity against HIV1 ROD infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID1443669 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1186008 | Antiviral activity against HIV1 infected in 293T cells assessed as time of 50% failure | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
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AID645832 | Cytotoxicity against human MT2 cells by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4 | Discovery of dimeric inhibitors by extension into the entrance channel of HIV-1 reverse transcriptase. |
AID623217 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID298087 | Inhibition of wild type HIV1 RT | 2007 | Journal 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. |
AID1186003 | Antiviral 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 r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID650547 | Resistance 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 cells | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID360705 | Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using RNA PPT primed substrate by scintillation proximity assay | 2007 | The 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. |
AID1754640 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect measured after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID105566 | Antiviral activity was determined against HIV-1 (clone 118) in MT-4 cells infected with HIV-1 IIIB using an XTT assay | 1998 | Bioorganic & 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. |
AID246463 | Compound concentration required to achieve 50% protection of infected MT-4 cells from Y181C strain was determined by the MTT method | 2005 | Journal 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. |
AID508757 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138K, M230L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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AID1884540 | Fold resistance, ratio of EC50 for antiviral activity against drug-resistant HIV-1 Y181C mutant infected in human MT4 cells to EC50 for antiviral activity against NNRTI resistant wild type HIV-1 infected in human MT4 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID767498 | Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility. |
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AID246269 | Effective concentration against human immunodeficiency virus type 1 Y188L mutant strain | 2005 | Journal 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). |
AID1691438 | Selectivity index, ratio of CC50 for cytotoxicity against human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
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AID736441 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1637391 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID650692 | Inhibition of HIV 1 reverse transcriptase Y188L mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID663295 | Antiviral 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 assay | 2012 | Journal 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. |
AID587735 | Antiviral 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 assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID1537494 | Inhibition 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 assay | 2019 | ACS medicinal chemistry letters, Feb-14, Volume: 10, Issue:2 | Aryl Substituted Benzimidazolones as Potent HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. |
AID302257 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y181C mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal 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. |
AID361925 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1418468 | Inhibition of recombinant wild-type HIV1 GST-fused reverse transcriptase p66/p51 RNA-dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in biotin-dUTP incorporation using poly(rA)/oligo(dT)16 as template/primer after 40 | 2018 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 28, Issue:22 | Design and synthesis of a novel series of non-nucleoside HIV-1 inhibitors bearing pyrimidine and N-substituted aromatic piperazine. |
AID246445 | Effective concentration of the compound to inhibit HIV-1 mutant L100I+K103N replication in HIV-infected MT-4 cells; Not determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID557020 | Antiviral activity against HIV1 clade B harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1456308 | Inhibition of HIV1 RES056 reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect measured at 5 days post infection by MTT assay | 2017 | Bioorganic & medicinal chemistry, 04-15, Volume: 25, Issue:8 | Structural modifications of diarylpyrimidines (DAPYs) as HIV-1 NNRTIs: Synthesis, anti-HIV activities and SAR. |
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AID46585 | Inhibitory activity against the HIV-1 in CEM cells | 1996 | Journal 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. |
AID1191401 | Antiviral activity against wild type HIV-2 ROD infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID198908 | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution Y181I | 1999 | Journal 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. |
AID1282050 | Antiretroviral activity against HIV-1 based virus like particles infected in U2OS cells assessed as Gluc activity at highest non-toxic concentration | 2016 | Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8 | Antiretroviral (HIV-1) activity of azulene derivatives. |
AID82603 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID613686 | Induction of human A375 cell differentiation assessed as microtubule reorganization at 20 uM after 96 hrs by immunofluorescence analysis | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors. |
AID1352320 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1410484 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild-type HIV1 3B reverse transcriptase infected in human MT4 cells | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID368560 | Antiviral activity against HIV1 reverse transcriptase Y181C mutant infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
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AID105701 | Anti-HIV-1 activity against LAI strain in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID373389 | Antiviral 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 assay | 2007 | Antimicrobial 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. |
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AID527375 | Antiviral activity against wild type HIV1 NL4-3 infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect | 2010 | Bioorganic & 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. |
AID302258 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT Y188L mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal 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. |
AID1171413 | Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11 | Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID1357794 | Resistance factor, ratio of EC50 for HIV1 harboring reverse transcriptase L100I mutant to EC50 for wild-type HIV-1 3B | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID508759 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1292361 | Cytotoxicity against human TZM-bl cells assessed as reduction of cell viability after 48 hrs | 2016 | Bioorganic & 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. |
AID317732 | Cytotoxicity against human HIV1RF infected CEM-SS cells by MTT assay | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
AID1743628 | Antiviral activity against HIV1 harboring RT Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID608392 | Cytotoxicity against human MAGI-CCR5 cells after 48 hrs by MTS cell viability assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1574374 | Antiviral activity against HIV-1 IRLL98 harboring reverse transcriptase M41L, D67N, Y181C, M184V, R211K, and T215Y mutants infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID1574385 | Inhibition of recombinant HIV-1 His-tagged reverse transcriptase p66/p51 K103N mutant expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer after 20 mins by scintillation counting analysi | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID88366 | Antiviral activity against K103N mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1248222 | Antiviral activity against wild type HIV 1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry, Oct-15, Volume: 23, Issue:20 | A novel family of diarylpyrimidines (DAPYs) featuring a diatomic linker: Design, synthesis and anti-HIV activities. |
AID1637396 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID366521 | Resistance index, ratio of EC50 for drug-resistant HIV1 isolate with reverse transcriptase K103N mutation to EC50 for wild type HIV1 NL4-3 | 2008 | Journal 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. |
AID1610042 | Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID279394 | Antiviral activity against HIV1 isolate with RT 98G mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1275550 | Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1303217 | Cytotoxicity against African green monkey Vero cells assessed as cell growth inhibition after 24 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Jul-19, Volume: 117 | Design, synthesis and anti-HIV activity of novel quinoxaline derivatives. |
AID366520 | Antiviral activity against HIV1 isolates with reverse transcriptase K103N mutation in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by MTT assay | 2008 | Journal 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. |
AID557041 | Antiviral activity against HIV1 isolate R8 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID104760 | Dose required to reduce the viability of mock-infected cells by 50% | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
AID1059144 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2013 | Bioorganic & 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. |
AID1822333 | Antiviral 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 assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID46378 | Antiviral activity against site directed resistant isolate HIV-1 L100I in CEM cells | 2001 | Journal 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. |
AID235444 | Selective index as the ratio of CD50 to that of ED50 against HIV-1 HxB2 strain. | 2002 | Journal 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. |
AID106048 | Inhibitory activity against 100I strain and 103N strain of HIV-I in MT-4 cell was determined; Not determined | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID557019 | Inhibition of HIV1 isolate R8 reverse transcriptase after 90 mins | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1217729 | Intrinsic 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 formation | 2011 | Drug 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. |
AID297144 | Antiviral activity against HIV1 with RT V106A mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID586910 | Induction of BCRP activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID525112 | Antiviral 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 assay | 2008 | Antimicrobial 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. |
AID104963 | Compound was evaluated for the anti-viral activity against cultured MT-4 cells | 1994 | Journal 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. |
AID1460939 | Antiviral 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 assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID44808 | Inhibitory concentration against cell culture of Human T-cell line c8166 infected with HIV-1 IIIB strain was determined | 1995 | Journal 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. |
AID1304406 | Inhibition of wild type HIV-1 BH10 recombinant reverse transcriptase expressed in Escherichia coli assessed as incorporation of [32P]GTP into poly(rA)/oligo(dT) as template primer | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID678714 | Inhibition 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 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1637395 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1410411 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
AID735083 | Inhibition of HIV reverse transcriptase | 2013 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5 | Synthesis and biological evaluation of phosphonate analogues of nevirapine. |
AID473115 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID622052 | Inhibition 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 counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1610044 | Therapeutic index, ratio of CC50 for human PBMC cells to IC50 for antiviral activity against HIV1 VB51 infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & 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. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269797 | Antiviral activity against HIV1 I135V mutant | 2006 | Bioorganic & 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. |
AID648425 | Inhibition of HIV1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rA)-oligo(dT) | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1705184 | Cytotoxicity against human MT-4 cells assessed as reduction in cell viability by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID648424 | Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, May, Volume: 51 | Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID738336 | Inhibition of HIV 1 reverse transcriptase assessed as incorporation of biotin-dUTP into poly rA.dT by ELISA | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7 | Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs. |
AID44797 | In vitro reduction of p24 by 90% in Efavirenz resistant HIV-1 (K103R, V179D, P225H) infected C8166 cells. | 2004 | Journal 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. |
AID1736346 | Selectivity index, ratio of CC50 for human HEK 293T cells to EC50 for VSVG/wild type HIV1 infected in human HEK 293T cells | |||
AID499277 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 4 days by MTT assay | 2010 | Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16 | Anti-HIV and antiplasmodial activity of original flavonoid derivatives. |
AID649826 | Antiviral activity against HIV1 LAI infected in human CEMx174 cells coexpressing GFP preincubated for 1 hr measured after 5 days by fluorimetry | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication. |
AID279428 | Antiviral activity against HIV1 isolate with RT 101E, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID105860 | Compound was tested for potency to achieve protection of MT-4 cells from 103N strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID726438 | Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID46384 | Antiviral activity against site directed resistant isolates in HIV-1 A98G CEM cells | 2001 | Journal 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. |
AID1316339 | Antiviral activity against HIV1 3B harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1609108 | Antiviral activity against HIV-1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID572186 | Antiviral activity against HIV-1 SM034 harboring NNTRI 188L mutant infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1165074 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID523482 | Antiviral activity against HIV1 with RT connection domain G190S/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID1292364 | Inhibition 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 sc | 2016 | Bioorganic & 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. |
AID523351 | Antiviral activity against HIV1 with RT connection domain K103N/T369I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID586909 | Induction of MRP3 activity | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Interaction potential of etravirine with drug transporters assessed in vitro. |
AID416755 | Antiviral activity against HIV1 with reverse transcriptase L100I mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal 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. |
AID698306 | Antiviral 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 assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID561945 | Antibacterial activity against Salmonella group B ATCC 31194 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID1784216 | Antiviral 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 assay | 2021 | European journal of medicinal chemistry, Dec-05, Volume: 225 | Discovery, optimization, and target identification of novel coumarin derivatives as HIV-1 reverse transcriptase-associated ribonuclease H inhibitors. |
AID105695 | Anti-HIV-1 activity against K103N strain in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID246350 | Effective concentration against human immunodeficiency virus type 1 mutated at 181C | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. |
AID1141971 | Ratio of EC50 for HIV1 harboring reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1304402 | Cytotoxicity against mock-infected human CEM-SS cells | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID197931 | HIV-1 reverse transcriptase inhibitory activity against Asn103 mutant using (poly)rC600*(oligo)dGT as template primer. | 1999 | Journal 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. |
AID373562 | Antiviral 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 assay | 2007 | Antimicrobial 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. |
AID1637397 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID561951 | Antibacterial activity against Shigella flexneri group B after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID635347 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2011 | Bioorganic & medicinal chemistry, Dec-01, Volume: 19, Issue:23 | Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs. |
AID1819220 | Inhibition of wild type HIV-1 reverse transcriptase using biotin-labelled dNTPs as substrate incubated for 2 hrs by ELISA | |||
AID351450 | Therapeutic index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | European 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. |
AID246343 | Effective concentration of the compound to inhibit HIV-1 mutant K103N+Y181C replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID457955 | Inhibition of RNA-dependent DNA polymerase activity of HIV1 reverse transcriptase using poly(rA)/pligo(dT) template | 2010 | Bioorganic & 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. |
AID1736347 | Inhibition 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 | |||
AID247497 | Inhibitory activity against HIV-1 mutant strain 103N | 2004 | Journal 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. |
AID444057 | Fraction escaping hepatic elimination in human | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3 | Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. |
AID1561722 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-[4-[2-cyanovinyl]-2,6-dimethylphenoxy]thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonam | |||
AID1729161 | Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect by MTT assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp |
AID613676 | Antiproliferative activity against human A375 cells assessed as cell growth at 350 uM after 96 hrs by trypan blue assay | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors. |
AID525110 | Antiviral 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 compound | 2008 | Antimicrobial 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. |
AID1217727 | Intrinsic 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 assay | 2011 | Drug 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. |
AID650545 | Antiviral activity against HIV 1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID413266 | Antiviral 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 ELISA | 2008 | Journal 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). |
AID1292014 | Inhibition of wild type HIV1 Reverse transcriptase assessed as reduction of biotin deoxyuridine triphosphate incorporation into the wild type HIV1 reverse transcriptase after 1 hr by ELISA | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID1884220 | Antiviral activity against HIV-1 harboring F227L/V106A double mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1685253 | Covalent 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 analysis | 2021 | ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2 | Covalent Inhibition of Wild-Type HIV-1 Reverse Transcriptase Using a Fluorosulfate Warhead. |
AID1443663 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID540212 | Mean residence time in human after iv administration | 2008 | Drug 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. |
AID1773462 | Resistance factor, ratio of EC50 for HIV1 harboring F227L/V106A double mutant infected in human MT4 cells to EC50 for HIV1 3B infected in MT4 cells | |||
AID1056580 | Antiviral 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 after | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID440086 | Antiviral activity against HIV1 HXB2 harboring K103N and Y181C mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID1391085 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID622047 | Inhibition 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 counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID1457065 | Inhibition of HIV1 reverse transcriptase p66 Y181I mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1197829 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID1435518 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase mutant | |||
AID663305 | Inhibition of HIV1 wild type recombinant reverse transcriptase assessed as [3H]dTTP incorporation into poly(rA)/oligo(dT) | 2012 | Journal 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. |
AID1292360 | Cytotoxicity against human U2OS cells assessed as reduction of cell viability after 48 hrs | 2016 | Bioorganic & 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. |
AID351445 | Antiviral activity against HIV1 3B in human MT4 cells assessed as inhibition of virus-induced cytopathicity after 5 days by MTT assay | 2009 | European 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. |
AID370728 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 V106A mutant expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID508796 | Ratio of EC50 for HIV1 in presence of 1 mg/ml alpha-1 acid-glycoprotein to EC50 for HIV1 in absence of serum proteins by GFP assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID82277 | Inhibition of HIV-1 IIIB replication in MT-4-infected wild type cells. | 2002 | Journal 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. |
AID1750721 | Inhibition of HIV-1 p66/p51 reverse transcriptase E138K mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID523346 | Antiviral activity against HIV1 with RT connection domain T369V mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID1572518 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID571975 | Antiviral activity against HIV-1 subtype CRF01_AE V029525 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1750715 | Cytotoxicity against in human MT-4 cells after 5 days by MTT assay | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
AID457958 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2010 | Bioorganic & 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. |
AID1275546 | Antiviral activity against HIV1 3B expressing reverse transcriptase E138K mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID1736156 | Cytotoxicity against human MT2 cells assessed as reduction in cell viability measured after 4 days by Trypan blue assay | 2020 | European journal of medicinal chemistry, Feb-15, Volume: 188 | Design, synthesis and biological evaluation of quinoxaline compounds as anti-HIV agents targeting reverse transcriptase enzyme. |
AID1410405 | Inhibition of recombinant wild type HIV1 reverse transcriptase assessed as decrease in biotin-dUTP incorporation using DIG-labeled dUTP/biotin-labeled dUTP and dTTP as template and viral nucleotides after 1 hr by ELISA | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Discovery of Novel Diarylpyrimidine Derivatives as Potent HIV-1 NNRTIs Targeting the "NNRTI Adjacent" Binding Site. |
AID1691435 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cell death incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | In situ click chemistry-based rapid discovery of novel HIV-1 NNRTIs by exploiting the hydrophobic channel and tolerant regions of NNIBP. |
AID1161108 | Inhibition 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 method | 2014 | Bioorganic & 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. |
AID1657474 | Antiviral activity against HIV1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2020 | Bioorganic & 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. |
AID1199053 | Selectivity index, ratio of CC50 for human MT4 cells to IC50 for Human immunodeficiency virus 1 3b infected in human MT4 cells | 2014 | Journal 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. |
AID105707 | Anti-HIV-1 activity against Y188L strain was determined in MT-4 cells by the MTT method | 2003 | Bioorganic & 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. |
AID1390710 | Antiviral activity against HIV1 3B expressing wild type reverse transcriptase infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID1583030 | Inhibition of recombinant HIV-1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation in to cDNA chain incubated for 1 hr by ELISA | 2020 | Journal of medicinal chemistry, 02-13, Volume: 63, Issue:3 | Discovery and Characterization of Fluorine-Substituted Diarylpyrimidine Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel. |
AID279423 | Antiviral activity against HIV1 isolate with RT 106I, 188L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID200161 | Compound concentration required to inhibit the HIV-1 recombinant Reverse transcriptase (rRT) activity by 50%. | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & 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. |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269799 | Antiviral activity against HIV1 L100I mutant | 2006 | Bioorganic & 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. |
AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Physicochemical determinants of human renal clearance. |
AID1391079 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. |
AID155274 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain A17 (Y181C) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & 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. |
AID508793 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K101E mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID361919 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase E138K mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1124998 | Inhibition of recombinant HIV1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation in to poly [A] x oligo[dT]15 by ELISA | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives. |
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID105861 | Compound was tested for potency to achieve protection of MT-4 cells from 106A strain of HIV-1 virus | 2001 | Bioorganic & 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). |
AID717253 | Inhibition of HIV1 reverse transcriptase assessed as biotin-dUTP incorporation into enzyme using poly(rC)-oligo(dG) as template primer by colorimetric analysis | 2012 | Bioorganic & 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. |
AID619634 | Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID198073 | Inhibitory activity against HIV-1 Mutant Reverse transcriptase G190A | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
AID1292359 | Antiviral activity against HIV1 virus-like particles harboring wild type reverse transcriptase infected in human U2OS cells after 24 hrs by Renilla luciferase assay | 2016 | Bioorganic & 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. |
AID665550 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID197798 | Compound was tested for inhibitory activity against HIV-1 mutant type reverse transcriptase (P236L) | 1998 | Bioorganic & 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. |
AID198907 | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution V106A | 1999 | Journal 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. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1457062 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N/Y1881C double mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID235796 | Selectivity index was measured as the ratio of CC50(HIV-1) to that of EC50(HIV-1); SI Selectivity Index | 1998 | Journal 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. |
AID1241795 | Selectivity index, ratio of IC50 for human CEM-SS cells to EC50 for HIV1 infected in human CEM-SS cells | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase. |
AID104761 | Cytotoxicity against mock-infected MT-4 cells. | 1999 | Journal 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. |
AID391679 | Inhibition 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 control | 2008 | Journal 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. |
AID440076 | Antiviral activity against HIV1 HXB2 harboring 100I mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID440671 | Antiviral 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 assay | 2009 | European 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. |
AID105545 | Inhibition of mutant type (Cys181) HIV-1 (IIIB) replication in MT-4 cells | 1996 | Journal 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. |
AID1187998 | Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 using dsDNA by microplate reader based assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands. |
AID1298246 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID757627 | Inhibition of HIV RT K103N/Y181C mutant by cell based assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1773450 | Antiviral activity against HIV1 harboring F227L/V106A mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug 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. |
AID1636150 | Ratio of IC50 for NNRTI resistant HIV1 harboring reverse transcriptase L100I/K103N/H221Y mutant infected in human TZM-bl cells to IC50 for wild type HIV1 NL4-3 infected in human TZM-bl cells | 2016 | Journal of medicinal chemistry, Aug-11, Volume: 59, Issue:15 | Discovery and Structure-Based Optimization of 2-Ureidothiophene-3-carboxylic Acids as Dual Bacterial RNA Polymerase and Viral Reverse Transcriptase Inhibitors. |
AID1186687 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Fused 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. |
AID1298247 | Inhibition of HIV1 wild type reverse transcriptase p66/p51 using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID1687692 | Antiviral activity against wild type HIV1 infected in human SupT1 cells assessed as inhibitory effect at 100 nM by cell based inhibition assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Rational design and Structure-Activity relationship of coumarin derivatives effective on HIV-1 protease and partially on HIV-1 reverse transcriptase. |
AID1457059 | Ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID666972 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Diverse combinatorial design, synthesis and in vitro evaluation of new HEPT analogues as potential non-nucleoside HIV-1 reverse transcription inhibitors. |
AID473114 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection from virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & 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. |
AID1200848 | Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-labeled dUTP incorporation into DNA using poly(A) x oligo(dT)15 as template/primer after 1 hr by ELISA | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID1267610 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2015 | Journal 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. |
AID153129 | Cytotoxic concentration was determined | 2000 | Journal 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. |
AID263519 | Antiviral activity against HIV1 Y181C mutant | 2006 | Bioorganic & 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. |
AID1822280 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID1057035 | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin dUTP incorporation by primer extension assay | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Design, synthesis and biological evaluation of 3-benzyloxy-linked pyrimidinylphenylamine derivatives as potent HIV-1 NNRTIs. |
AID1161107 | Cytotoxicity against human MT4 cells by MTT assay | 2014 | Bioorganic & 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. |
AID623214 | Antiviral 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 assay | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID370730 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 Y188L mutant expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID1731752 | Inhibition of reverse transcriptase RES056 mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID1377174 | Antiviral activity against NRTI-resistant HIV1 isolate 1617-1 infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6 | Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
AID152777 | Inhibitory activity of compound won p24 production in peripheral blood mononuclear cells infected with HIV strain HTLV IIIB wild type. | 1999 | Bioorganic & 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. |
AID1171587 | Antiviral activity against HIV1 NL4-3 expressing reverse transcriptase K103N-Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cell death by MTT assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID558386 | Drug level in HIV-infected pregnant woman amniotic fluid at 200 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial 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. |
AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID665549 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
AID587737 | Antiviral 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 t | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID242064 | Concentration required for 50% inhibition of wild type human immunodeficiency virus type 1 reverse transcriptase | 2004 | Journal 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. |
AID757621 | Inhibition of recombinant wild type HIV1 RT using poly(rA)/oligo(dT)16 as template after 40 mins by spectrofluorometric analysis | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID298076 | Antiviral activity against HIV1 RT K103N-Y181C mutant in MT4 cells by MTT assay | 2007 | Journal 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. |
AID1357788 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID492283 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID200171 | Inhibition single mutant of HIV-1 RT (Y181C) | 1993 | Journal 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. |
AID368557 | Inhibition of HIV1 recombinant reverse transcriptase Y181I mutant-mediated RNA-dependent DNA polymerase activity assessed as [3H]dTTP incorporation by cell free-based scintillation counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID632801 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID508775 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID572171 | Antiviral activity against HIV-1 subtype D V022819 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID587734 | Antiviral 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 assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID619628 | Inhibition of HIV-1 reverse transcriptase assessed as inhibition of biotin-dUTP incorporation into enzyme by colorimetry | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID106057 | Inhibitory activity against 103N strain and 181C strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID1654198 | Drug metabolism in human assessed as formation of 12-OH-NVP | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
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AID1609105 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 of antiviral activity against HIV-1 IIIB infected in human MT4 cells | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID279398 | Antiviral activity against HIV1 isolate with RT 103N, 108I mutation relative to wild type | 2007 | Antimicrobial 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. |
AID104244 | Cytotoxic concentration against MT-2 cells | 1993 | Journal 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 |
AID558580 | Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 200 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial 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. |
AID1335219 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
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AID440085 | Antiviral activity against HIV1 HXB2 harboring 101E and K103N mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID279405 | Antiviral activity against HIV1 isolate with RT 101E, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1124989 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7 | Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives. |
AID293558 | Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay | 2007 | European 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. |
AID571969 | Antiviral activity against HIV-1 subtype CRF02_AG V022826 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
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AID269685 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269685 | Antiviral activity against HIV1 | 2006 | Bioorganic & 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. |
AID1610054 | Therapeutic index, ratio of CC50 for human TZM-bl cells to IC50 for antiviral activity against HIV1 NARI-DR infected in human TZM-bl cells | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID685335 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B | 2012 | Bioorganic & 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. |
AID1155816 | Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase L100I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal 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. |
AID1572520 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay | |||
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AID1152370 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post viral infection by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID766432 | Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility. |
AID1561718 | Antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide assessed as protection against virus-indu | |||
AID630951 | Cytotoxicity in human TZM-bl cells assessed as cell viability after 48 hrs by MTT assay | 2011 | Bioorganic & 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. |
AID391688 | Inhibition of DNA dependent DNA polymerase activity of HIV1 BH10 recombinant reverse transcriptase p66/p51 assessed as residual enzyme activity | 2008 | Journal 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. |
AID1574382 | Resistance index, ratio of EC50 for HIV-1 harboring reverse transcriptase K103N mutant to EC50 for wild type HIV-1 NL4-3 | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID508639 | Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1877037 | Antiviral 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 assay | 2021 | Journal 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. |
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AID1754638 | Cytotoxicity against mock-infected human MT4 cells incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID1443661 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1316332 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID440078 | Antiviral activity against HIV1 HXB2 harboring 106A mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
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AID1884226 | Antiviral activity against HIV-1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID106775 | Inhibition of cell culture in MT-4 cells | 1993 | Journal 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. |
AID368564 | Inhibition of wild type HIV1 free reverse transcriptase | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID46374 | Antiviral activity against site directed 4X AZT resistant isolate HIV-1 L100I in CEM cells | 2001 | Journal 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. |
AID1335215 | Antiviral 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 gene | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID557049 | Antiviral activity against HIV1 clade G harboring mutant reverse transcriptase relative to HIV1 CNDO with wild type reverse transcriptase | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6 | Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. |
AID1175921 | Cytotoxicity against HEK293 cells infected with VSV-G protein pseudotyped HIV1 | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12 | Diterpenes from a Chinese collection of the brown alga Dictyota plectens. |
AID297142 | Antiviral activity against HIV1 with RT Y181C mutation by cytopathic cell killing assay | 2007 | Journal 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. |
AID279453 | Antiviral activity against HIV1 isolate with RT 98G, 100I, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID781024 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2013 | Bioorganic & 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. |
AID1335211 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID106069 | Inhibitory activity against 188L strain of HIV-I in MT-4 cells | 2001 | Bioorganic & medicinal chemistry letters, Sep-03, Volume: 11, Issue:17 | Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues. |
AID1862265 | Inhibition 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 tem | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors. |
AID396619 | Antiviral activity against HIV1 3B replication in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by tetrazolium-based colorimetric assay | 2008 | European 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. |
AID1763902 | Antiviral activity against HIV-1 IIIB harboring RT E138K mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID1165075 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID1185992 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1736349 | Inhibition of RNase H activity of HIV-1 reverse transcriptase using DNA/RNA hybrid as substrate incubated for 30 mins by fluorescence based analysis | |||
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & 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. |
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269795 | Antiviral activity against HIV1 E138K mutant | 2006 | Bioorganic & 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. |
AID726436 | Cytotoxicity in human MT2 cells assessed as inhibition of cell growth | 2013 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 23, Issue:4 | Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency. |
AID373554 | Antiviral activity against 0.1 MOI HIV1 3B infected in human TZM-b1 cells assessed as inhibition of viral replication after 24 hrs by luciferase assay | 2007 | Antimicrobial 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. |
AID496742 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/V35T, K122E, I135V, T139A, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1483274 | Inhibition of HIV1 3B reverse transcriptase Y188L mutant infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1822334 | Antiviral 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 assay | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3 | Discovery of Novel Pyridine-Dimethyl-Phenyl-DAPY Hybrids by Molecular Fusing of Methyl-Pyrimidine-DAPYs and Difluoro-Pyridinyl-DAPYs: Improving the Druggability toward High Inhibitory Activity, Solubility, Safety, and PK. |
AID508646 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, Y188L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1637394 | Antiviral activity against human HIV-1 3B harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as protection from virus-induced cytopathic effect measured 5 days post infection by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1773445 | Antiviral activity against HIV1 harboring L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1185999 | Antiviral 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 HIV1 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1637399 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring L100I mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID368556 | Inhibition 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 counting | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. |
AID1773447 | Antiviral activity against wild type HIV1 harboring Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1357804 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase Y188L mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID1773446 | Antiviral activity against HIV1 harboring K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1884228 | Antiviral activity against HIV-1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus induced cytotoxicity incubated for 5 to 7 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Chemical space exploration around indolylarylsulfone scaffold led to a novel class of highly active HIV-1 NNRTIs with spiro structural features. |
AID1161103 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2014 | Bioorganic & 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. |
AID523352 | Antiviral activity against HIV1 with RT connection domain K103N/T369I/N348I mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID523479 | Antiviral activity against HIV1 with RT connection domain G190S mutant transfected in HEK293 cells assessed as inhibition of viral replication relative to HIV1 NL4-3 | 2010 | Antimicrobial 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. |
AID79450 | Ability to inhibit HIV-1 multiplication in chronically infected H9/IIIB cells | 1997 | Journal of medicinal chemistry, May-09, Volume: 40, Issue:10 | Dihydro(alkylthio)(naphthylmethyl)oxopyrimidines: novel non-nucleoside reverse transcriptase inhibitors of the S-DABO series. |
AID1473738 | Inhibition 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 assay | 2013 | Toxicological 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. |
AID371906 | Antiviral 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 assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12 | New pyridinone derivatives as potent HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID473116 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2010 | Bioorganic & 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. |
AID1298248 | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant using poly(rA) template and measured after 40 mins by picogreen based spectrofluorometry | 2016 | Bioorganic & medicinal chemistry, 06-01, Volume: 24, Issue:11 | 1,6-Bis[(benzyloxy)methyl]uracil derivatives-Novel antivirals with activity against HIV-1 and influenza H1N1 virus. |
AID248879 | Inhibitory concentration against human immunodeficiency virus type 1 (with K103N/V108I resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID351448 | Cytotoxicity against human MT4 cells by MTT assay | 2009 | European 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. |
AID1157580 | Cytotoxicity against human MT4 cells after 96 hrs by MTT assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Synthesis of novel fluoro analogues of MKC442 as microbicides. |
AID143387 | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 with a Y181C mutation in RT (reverse transcriptase) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1457063 | Inhibition of HIV1 NL4-3 reverse transcriptase His-tagged p66/p51 associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation c | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID1609107 | Antiviral activity against HIV-1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
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AID608391 | Antiviral activity against HIV1 3B infected in human MAGI-CCR5 cells assessed as inhibition of viral replication after 48 hrs by beta-galactosidase reporter assay | 2011 | Bioorganic & medicinal chemistry, Jul-15, Volume: 19, Issue:14 | Imidazo[1,2-a]pyridin-3-amines as potential HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID227244 | The compound was evaluated for antiviral activity using whole cell assay | 2000 | Bioorganic & 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. |
AID1750718 | Inhibition of HIV-1 p66/p51 reverse transcriptase K103N mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
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AID153102 | Cytotoxic concentration against PBMC cells | 1993 | Journal 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 |
AID665552 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 harboring reverse transcriptase K103N/Y181C RT mutant | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors. |
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AID508794 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase L100I mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1815402 | Inhibition of HIV1 reverse transcriptase F227L/V106A double mutant using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1267608 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days by MTT assay | 2015 | Journal 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. |
AID1561721 | Resistance index, ratio of EC50 for antiviral activity against HIV1 3B infected in human MT4 cells grown under 30 passages in presence of 4-[[4-[[4-(4-cyano-2,6-dimethylphenoxy)thieno[3,2-d]pyrimidin-2-yl]amino]-1-piperidyl]methyl]benzenesulfonamide to EC | |||
AID361921 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase P236L mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID1460928 | Cytotoxicity against human MAGI-CCR5 cells assessed as reduction in cell viability after 48 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID1811045 | Cytotoxicity against mock infected human MT4 cells by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID263520 | Antiviral activity against HIV1 Y188L mutant | 2006 | Bioorganic & 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. |
AID198779 | In vitro inhibitory activity against HIV-1 mutant Reverse transcriptase containing the single amino acid substitution K103N | 1999 | Journal 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. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1163232 | Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID248845 | Inhibitory concentration against human immunodeficiency virus type 1 (with Y181C resistant mutation) was determined in HeLa-CD4 MAGI assay | 2004 | Journal 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. |
AID1249714 | Antiviral activity against HIV1 3B expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity incubated for 4 days by MTT method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue. |
AID1335220 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID1637400 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring K103N mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1862269 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Oct-05, Volume: 240 | Design, synthesis, and biological evaluation of novel double-winged galloyl derivatives as HIV-1 RNase H inhibitors. |
AID143385 | Inhibitory activity against non-nucleoside reverse transcriptase inhibitors (NNRTI) -resistant HIV-1 strain A17 variant with Y181C plus K103N mutations in RT (reverse transcriptase) | 2001 | Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4 | Anti-HIV activity of aromatic and heterocyclic thiazolyl thiourea compounds. |
AID1572523 | Antiviral activity against HIV1 harboring reverse transcriptase E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
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AID198912 | Inhibition of HIV-1 Mutant HIV-1 RT enzymes containing the single amino acid substitution L1001 | 2001 | Journal 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. |
AID267652 | Selectivity for wild type HIV1 virus over HIV1 Y181C mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID1485972 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID1743634 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT L100I mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID279400 | Antiviral activity against HIV1 isolate with RT 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID632797 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID279448 | Antiviral activity against HIV1 isolate with RT 101H, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID267654 | Selectivity for wild type HIV1 virus over HIV1 K103N/L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID630950 | Antiviral 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 assay | 2011 | Bioorganic & 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. |
AID302249 | Antiviral activity against HIV1 NL43 in MT4 cells assessed as inhibition of viral induced cytopathic effect after 4 days by MTT method | 2007 | Journal 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. |
AID298062 | Antiviral activity against HIV2 ROD in human MT4 cells by XTT assay | 2007 | Journal 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. |
AID736438 | Inhibition of HIV1 reverse transcriptase p66/p51 K103N mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1888698 | Antiviral activity against HIV1 with RT E138K mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID482699 | Antiviral activity against HIV S07 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID1736361 | Antiviral 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 | |||
AID757624 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2013 | European journal of medicinal chemistry, Jul, Volume: 65 | Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1373153 | Inhibition 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 by | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3 | Structural optimization of N |
AID1173645 | Cytotoxicity against human CEmx174 cells expressing GFP after 5 days by resazurin assay | 2014 | Bioorganic & 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. |
AID267646 | Cytotoxicity against HEK293T cells | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID619640 | Antiviral activity against HIV-1 3B harboring RT K103N and Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1199052 | Antiviral activity against Human immunodeficiency virus 1 3b infected in human MT4 cells assessed as inhibition of virus replication after 5 days by MTT assay | 2014 | Journal 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. |
AID317730 | Antiviral activity against HIV13B infected in human MT4 cells | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
AID508754 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179F, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1763897 | Antiviral activity against HIV-1 IIIB infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 06-15, Volume: 40 | Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs. |
AID104450 | Concentration required to protect the cell against HIV-2 strain ROD viral cytopathogenicity by 50% in MT-4 cells; NA denotes not active | 2004 | Bioorganic & 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. |
AID1335214 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID781025 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2013 | Bioorganic & 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. |
AID279450 | Antiviral activity against HIV1 isolate with RT 98G, 103N, 181C mutation relative to wild type | 2007 | Antimicrobial 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. |
AID440077 | Antiviral activity against HIV1 HXB2 harboring 101E mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & 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. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269805 | Antiviral activity against HIV1 Y181S mutant | 2006 | Bioorganic & 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. |
AID551466 | Selectivity index, ratio of CC50 for human C1866 cells to EC50 for HIV1 3B infected in human C8166 cells | 2011 | Bioorganic & 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. |
AID619639 | Antiviral activity against HIV-1 3B harboring RT F227L and V106A mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1165079 | Inhibition 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 hr | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID1335213 | Antiviral 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 gene | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID1199051 | Cytotoxicity against human MT4 cells assessed as inhibition of overall cell metabolism after 5 days by MTT assay | 2014 | Journal 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. |
AID197943 | In vitro inhibition of mutant Y181C recombinant reverse transcriptase of HIV-1 IIIB | 1996 | Journal 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. |
AID1379959 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity by measuring virus-induced syncytium formation by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID1741390 | Inhibition of reverse transcriptase in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID734263 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 SF33 infected in human MT4 cells | 2013 | Journal 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. |
AID1352318 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1884492 | Antiviral activity against drug-resistant HIV-1 Y188L mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID492281 | Antiviral activity against wild type HIV1 LAI infected in human MT4 cells assessed as protection against virus-induced cytopathogenicity after 4 days by MTT assay | 2010 | Bioorganic & 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. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1335202 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID248262 | In vitro inhibitory concentration against HIV V106A mutant strain | 2005 | Journal 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. |
AID247526 | Inhibitory activity against wild type HIV-1 LAI cell line | 2004 | Journal 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. |
AID265470 | Cytotoxicity against human lymphocytes | 2006 | Journal 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. |
AID496630 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase Y181C/V35T, V60I, I135V, S162A, K173T, Q174K, N175Y, D177E, T200A, Q207E, R211K, H221Y mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID200170 | Inhibition single mutant of HIV-1 RT (K103 N) | 1993 | Journal 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. |
AID279473 | Antiviral activity against HIV1 isolate with RT 230L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID257916 | Antiviral activity against HIV1 K103N mutant using HeLa MAGI assay | 2006 | Journal 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. |
AID248257 | In vitro inhibitory concentration against HIV G190A mutant strain | 2005 | Journal 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. |
AID508772 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y188L mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID246556 | Concentration required for 50% protection of infected MT-4 cells from wtIIIB-HIV-1-induced cytopathogenicity was determined by the MTT method | 2005 | Journal 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. |
AID155280 | Anti-HIV activity by its ability to inhibit the replication of HIV-1 strain RT-MDR(V106A) in peripheral blood mononuclear cells (PBMC) | 1999 | Bioorganic & 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. |
AID1705190 | Resistance index, ratio of EC50 for antiviral activity against HIV1 harboring RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 NL4-3 infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains. |
AID197941 | In vitro inhibition of mutant P236L recombinant reverse transcriptase of HIV-1 IIIB | 1996 | Journal 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. |
AID492047 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID1165077 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | European journal of medicinal chemistry, Nov-24, Volume: 87 | Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization. |
AID561940 | Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID663297 | Antiviral 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 assay | 2012 | Journal 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. |
AID1815396 | Inhibition of wild type HIV1 reverse transcriptase using oligo(dT)16 as primer measured after 40 mins by picogreen-dye based spectrofluorimetric analysis | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug 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. |
AID413565 | Ratio of EC50 for multidrug-resistant HIV1 with reverse transcriptase 41L, 74V, 184V, 210W, 215Y, ins SS, 98G mutation to EC50 for wild type HIV1 3B | 2008 | Journal 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). |
AID508766 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase M230V mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID734270 | Inhibition of HIV1 reverse transcriptase after 1 hr by colorimetric assay | 2013 | Journal 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. |
AID279442 | Antiviral activity against HIV1 isolate with RT 98G, 190A mutation relative to wild type | 2007 | Antimicrobial 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. |
AID698299 | Selectivity index, ratio of EC50 for HIV1 containing reverse transcriptase Y188L mutant to EC50 for wild type HIV1 NL4-3 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID286999 | Inhibition of DNA polymerase activity of HIV1 reverse transcriptase | 2007 | Journal 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. |
AID1316330 | Antiviral activity against wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells assessed as protection against virus induced cytotoxicity after 5 days by MTT assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1609106 | Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 4 days by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Conformational restriction design of thiophene-biphenyl-DAPY HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1435510 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | |||
AID573477 | Antiviral activity of Human immunodeficiency virus 1 isolate 8116 harboring A98S, G190A mutation in reverse transcriptase by cell based assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1815388 | Resistance fold, ratio of EC50 for HIV1 harboring reverse transcriptase K103N mutant infected MV4 cells to EC50 for wild type HIV1 infected MV4 cells | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID1304405 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human MT4 cells to EC50 for antiviral activity against HIV-1 3B | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID1460947 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID279447 | Antiviral activity against HIV1 isolate with RT 236L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID105324 | Inhibition of Efavirenz resistant HIV-1 (K103N-Y181C) induced cytopathicity in MT-4 cells. | 2004 | Journal 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. |
AID1161106 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells | 2014 | Bioorganic & 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. |
AID1815380 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as protection against virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel. |
AID573471 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A-81C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1811044 | Antiviral activity against HIV1 IIIB infected human MT4 cells assessed as protection against virus-induced cytopathic effect by MTT assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID279427 | Antiviral activity against HIV1 isolate with RT 103R, 179D, 188L mutation relative to wild type | 2007 | Antimicrobial 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. |
AID293559 | Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay | 2007 | European 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. |
AID650690 | Inhibition of HIV 1 reverse transcriptase Y181I mutant assessed as inhibition of time-dependent incorporation of [3H]dTTP into poly(rA)n.oligo(dT) | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8 | Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. |
AID370724 | Inhibition of RNA dependent DNA polymerase activity of HIV1 recombinant reverse transcriptase p66/p51 expressed in Escherichia coli JM109 | 2009 | Journal 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. |
AID246265 | Effective concentration against human immunodeficiency virus type 1 G190S mutant strain | 2005 | Journal 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). |
AID1056582 | Antiviral 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 lu | 2013 | Journal of natural products, Dec-27, Volume: 76, Issue:12 | Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73. |
AID198086 | Inhibitory activity against HIV-1 Y181C Reverse transcriptase (RT) | 1995 | Journal 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. |
AID360711 | Inhibition of HIV1 RT Y181C mutant mediated DNA-dependent DNA polymerization using DNA PPT primed substrate by scintillation proximity assay | 2007 | The 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. |
AID1687683 | Antiviral activity against HIV-1 E138K mutant strain infected in human MT4 cells assessed as reduction in virus-induced cytopathogenicity by MTT assay | 2020 | European journal of medicinal chemistry, Jan-15, Volume: 186 | Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities. |
AID510360 | Inhibition of HIV1 reverse transcriptase after 1 hr by ELISA | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents. |
AID1171589 | Resistance index, ratio of EC50 for HIV1 NL4-3 expressing reverse transcriptase Y181C mutant to EC50 for wild type HIV1 NL4-3 | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23 | Indolylarylsulfones carrying a heterocyclic tail as very potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1457061 | Ratio of EC50 for HIV-1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & 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. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269793 | Antiviral activity against HIV1 | 2006 | Bioorganic & 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. |
AID573466 | Inhibition of Human immunodeficiency virus 1 subtype B reverse transcriptase Y181C mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
AID1152373 | Cytotoxicity against human MT4 cells by MTT assay | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID279452 | Antiviral activity against HIV1 isolate with RT 103N, 108I, 238T mutation relative to wild type | 2007 | Antimicrobial 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. |
AID572178 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID734257 | Antiviral 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 ELISA | 2013 | Journal 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. |
AID566900 | Cytotoxicity against human MT4 cells after 5 days by spectrophotometry | 2011 | European journal of medicinal chemistry, Jan, Volume: 46, Issue:1 | Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection. |
AID1163234 | Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay | 2014 | Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19 | From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds. |
AID1186000 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID571981 | Antiviral activity against HIV-1 subtype B V022813 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID1773449 | Antiviral activity against wild type HIV1 harboring E138K mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathogenic effect by MTT assay | |||
AID1636928 | Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method | 2016 | Bioorganic & medicinal chemistry, 10-15, Volume: 24, Issue:20 | Computer-aided discovery of anti-HIV agents. |
AID736439 | Inhibition of HIV1 reverse transcriptase p66/p51 L100I mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID440079 | Antiviral activity against HIV1 HXB2 harboring 138K mutant reverse transcriptase infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal 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. |
AID522369 | Antiviral activity against recombinant HIV1 harboring reverse transcriptase V106A mutant clone infected in MAGIC-5 cells using 5-bromo4-chloro-3-indolyl-beta-D-galactopyranoside staining based light microscopy | 2010 | Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4 | Combination of V106I and V179D polymorphic mutations in human immunodeficiency virus type 1 reverse transcriptase confers resistance to efavirenz and nevirapine but not etravirine. |
AID298065 | Metabolic stability in rat plasma | 2007 | Journal 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. |
AID1292011 | Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
AID1352316 | Antiviral activity against HIV1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 4 days by MTT assay | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. |
AID1637402 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring Y188L mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID392513 | Antiviral activity against HIV1 | 2009 | Bioorganic & 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. |
AID1185994 | Antiviral 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 | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1410486 | Inhibition of wild-type HIV1 reverse transcriptase infected in human MT4 cells assessed as reduction in biotin-dUTP incorporation | 2018 | ACS medicinal chemistry letters, Apr-12, Volume: 9, Issue:4 | Further Exploring Solvent-Exposed Tolerant Regions of Allosteric Binding Pocket for Novel HIV-1 NNRTIs Discovery. |
AID247618 | Inhibitory activity against HIV-1 double mutants strain 101E and 103N | 2004 | Journal 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. |
AID621974 | Inhibition 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 counting | 2011 | Bioorganic & medicinal chemistry, Oct-01, Volume: 19, Issue:19 | 1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents. |
AID257163 | Inhibition of wild type HIV1 reverse transcriptase by [3H]dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal 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. |
AID1750719 | Inhibition of HIV-1 p66/p51 reverse transcriptase Y181C mutant incubated for 40 mins by picogreen dye-based spectrofluorometric analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Hydrophobic Pocket Occupation Design of Difluoro-Biphenyl-Diarylpyrimidines as Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors: from |
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AID479214 | Inhibition of biotin-dUTP labeled HIV-1 reverse transcriptase after 30 mins colorimetric streptavidin alkaline phosphatase reporter system | 2010 | Bioorganic & 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. |
AID496634 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,A98G/V35T, E36D, T39K, S48A, I50V, V60I, S68G, I135V, S162A, K173T, Q174K, D177E, G196E, T200A, E203G, Q207D, R211K, Q222P mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID508755 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179E, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID416757 | Antiviral activity against HIV1 with reverse transcriptase Y181C mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal 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. |
AID1275545 | Antiviral activity against HIV1 3B expressing reverse transcriptase Y181C mutant infected in human MT4 cells assessed as reduction of virus-induced cytopathic effect after 5 days by MTT assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket. |
AID614140 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2011 | Bioorganic & medicinal chemistry, Sep-01, Volume: 19, Issue:17 | Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs. |
AID1741395 | Inhibition of reverse transcriptase Y181C mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID279440 | Antiviral activity against HIV1 isolate with RT 101R, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID82605 | The 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 assay | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID257173 | Cytotoxicity against MT4 cells by MTT method | 2005 | Journal 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. |
AID1197834 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant | 2015 | European journal of medicinal chemistry, Mar-06, Volume: 92 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. |
AID363037 | Cytotoxicity against human MT4 cells after 4 days by MTT assay | 2008 | European 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. |
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AID736041 | Inhibition of HIV1 reverse transcriptase p66/p51 V106A mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1483279 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B harboring reverse transcriptase infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID1520066 | Inhibition of recombinant wild type HIV-1 His-tagged reverse transcriptase p66/p51 expressed in Escherichia coli JM109 using poly(rA)/oligo(dT)16 as template/primer incubated for 40 mins by pico-green based spectrofluorometric analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID83550 | Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
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AID1880373 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
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AID443751 | Toxicity in African green monkey Vero cells | 2010 | Journal 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. |
AID693586 | Cytotoxicity against human MT4 cells assessed as decrease in cell viability after 5 days by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors. |
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AID1185990 | Antiviral 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 assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
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AID1457064 | Inhibition of HIV1 reverse transcriptase p66 K103N mutant associated RNA dependent DNA polymerase activity expressed in Escherichia coli assessed as reduction in [3H]dTTP incorporation using poly(rA)/oligo(dT) as template/primer by scintillation counting | 2017 | Journal of medicinal chemistry, 08-10, Volume: 60, Issue:15 | Chiral Indolylarylsulfone Non-Nucleoside Reverse Transcriptase Inhibitors as New Potent and Broad Spectrum Anti-HIV-1 Agents. |
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AID269686 | Antiviral activity against HIV1 NNTRI resistant Y188L mutant | 2006 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 16, Issue:16 | Synthesis and biological evaluations of sulfanyltriazoles as novel HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID269686 | Antiviral activity against HIV1 NNTRI resistant Y188L mutant | 2006 | Bioorganic & 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. |
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AID1335203 | Ratio 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 glyco | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
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AID46379 | Antiviral activity against site directed resistant isolate HIV-1 L74V in CEM cells | 2001 | Journal 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. |
AID1460945 | Therapeutic 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 cells | 2017 | Bioorganic & medicinal chemistry, 12-01, Volume: 25, Issue:23 | An integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors. |
AID1186688 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV-1 3B infected in human MT4 cells | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Fused 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. |
AID1483284 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for reverse transcriptase E138K mutant in human MT4 cells infected HIV1 3B | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants. |
AID571970 | Antiviral activity against HIV-1 subtype CRF02_AG V022830 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID496631 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase V90I,Y181C/V35T, T39M, P119S, D123E, S162A, E169D, K173T, Q174K, D177E, T200A, Q207E, K219N, V245Q, E248D mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID1754647 | Antiviral activity against HIV1 harboring RT RES056 mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect incubated for 5 days by MTT assay | 2021 | Bioorganic & medicinal chemistry, 07-15, Volume: 42 | Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. |
AID482698 | Antiviral activity against HIV S067 infected in human A72 Jurkat cells assessed as inhibition of GFP expression after 48 hrs by flow cytometry | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | "Viologen" dendrimers as antiviral agents: the effect of charge number and distance. |
AID613681 | Antiproliferative activity against human A375 cells at 350 uM after 96 hrs by trypan blue assay | 2011 | Journal of medicinal chemistry, Aug-25, Volume: 54, Issue:16 | Modulation of cell differentiation, proliferation, and tumor growth by dihydrobenzyloxopyrimidine non-nucleoside reverse transcriptase inhibitors. |
AID246362 | Effective concentration against rhuman immunodeficiency virus type 1 K103N and Y181C mutant strains | 2005 | Journal 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). |
AID1377176 | Antiviral activity against HIV1 isolate LAV infected in PHA-stimulated human PBMC assessed as reduction in p24 level after 7 days by ELISA | 2017 | Journal of natural products, 06-23, Volume: 80, Issue:6 | Potent Inhibitor of Drug-Resistant HIV-1 Strains Identified from the Medicinal Plant Justicia gendarussa. |
AID317728 | Inhibition of HIV1 reverse transcriptase | 2008 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 18, Issue:2 | Inhibition of tubulin polymerization by select alkenyldiarylmethanes. |
AID571982 | Antiviral activity against HIV-1 subtype B V022814 infected in human MT4 cells assessed as inhibition of viral replication relative to HIV-1 3B | 2009 | Antimicrobial 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. |
AID630952 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for X4 tropic Human immunodeficiency virus 1 subtype B-3B | 2011 | Bioorganic & 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. |
AID1811038 | Inhibition of recombinant wild-type HIV1 p66/p51 reverse transcriptase assessed as inhibition of [3H]dGTP incorporation using poly (rA) as templates incubated for 40 mins by spectrofluorometer | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14 | Improving Druggability of Novel Diarylpyrimidine NNRTIs by a Fragment-Based Replacement Strategy: From Biphenyl-DAPYs to Heteroaromatic-Biphenyl-DAPYs. |
AID431619 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as virus-induced cytopathic effect by MTT assay | 2009 | Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16 | Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID440672 | Antiviral 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 assay | 2009 | European 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. |
AID83553 | Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala | 2004 | Journal of medicinal chemistry, May-06, Volume: 47, Issue:10 | Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 varian |
AID279422 | Antiviral activity against HIV1 isolate with RT 190E mutation relative to wild type | 2007 | Antimicrobial 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. |
AID476471 | Cytotoxicity against human MT2 cells infected with HIV1 harboring reverse transcriptase Y181C mutation by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8 | Eastern extension of azoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase; cyano group alternatives. |
AID246299 | Effective concentration of the compound to inhibit HIV-1 mutant L100I replication in HIV-infected MT-4 cells | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID348904 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as virus-induced cell death by MTT method | 2008 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 18, Issue:21 | Towards novel S-DABOC inhibitors: synthesis, biological investigation, and molecular modeling studies. |
AID257164 | Inhibition of K103N mutant HIV1 reverse transcriptase by [3H]-dTTP poly(rA)/oligo(dT) incorporation | 2005 | Journal 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. |
AID391990 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B | 2008 | European 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. |
AID1322997 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytopathic effect after 5 days MTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
AID1485975 | Inhibition 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 analysis | 2017 | Bioorganic & medicinal chemistry, 07-15, Volume: 25, Issue:14 | Searching for novel N |
AID302261 | Inhibition of HIV1 reverse transcriptase L100I mutant | 2007 | Journal 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. |
AID1191972 | Antiviral activity against HIV2 ROD infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 25, Issue:6 | Design, synthesis of new β-carboline derivatives and their selective anti-HIV-2 activity. |
AID1126509 | Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Apr-15, Volume: 22, Issue:8 | Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1610040 | Antiviral activity against HIV1 N119 infected in human TZM-bl cells incubated for 48 hrs by bright Glo-luciferase reporter gene assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis and in-vitro anti-HIV-1 evaluation of novel pyrazolo[4,3-c]pyridin-4-one derivatives. |
AID698305 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathicity measured 5 days post infection by MTT assay | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14 | New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1191670 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | Bioorganic & medicinal chemistry, Mar-01, Volume: 23, Issue:5 | Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs. |
AID734262 | Selectivity index, ratio of CC50 for human TZM-bl cells to EC50 for Human immunodeficiency virus 1 A17 infected in human TZM-bl cells | 2013 | Journal 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. |
AID1558854 | Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24 | Ligand-Based Design of Nondimethylphenyl-Diarylpyrimidines with Improved Metabolic Stability, Safety, and Oral Pharmacokinetic Profiles. |
AID492046 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type HIV1 3B | 2010 | Bioorganic & 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. |
AID1141969 | Ratio of EC50 for HIV1 harboring reverse transcriptase K103N/Y181C double mutant to EC50 for wild type HIV1 NL4.3 | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | New indolylarylsulfones as highly potent and broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID1743635 | Resistance index, ratio of EC50 for antiviral activity against HIV1 expressing RT K103N mutant infected in human MT4 cells to EC50 for antiviral activity against HIV1 3B infected in human MT4 cells | 2020 | European journal of medicinal chemistry, Nov-15, Volume: 206 | Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility. |
AID766431 | Cytotoxicity against human MT2 cells by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18 | Extension into the entrance channel of HIV-1 reverse transcriptase--crystallography and enhanced solubility. |
AID508790 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase K103N mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1190617 | Inhibition 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 control | 2015 | Bioorganic & 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. |
AID587739 | Cytotoxicity against human HeLaT4 cells by WST-1 assay | 2011 | Antimicrobial agents and chemotherapy, Jan, Volume: 55, Issue:1 | Identification and characterization of persistent intracellular human immunodeficiency virus type 1 integrase strand transfer inhibitor activity. |
AID391993 | Cytotoxicity against human CEM cells by MTT assay | 2008 | European 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. |
AID430057 | Selectivity index, CC50 for human MT4 cells to EC50 for HIV1 3B | 2009 | Bioorganic & 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. |
AID106774 | Cell culture inhibitory concentration against spread of HIV-I infection in MT-4 cells was determined | 1993 | Journal 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. |
AID361904 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K103N/L100I mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID416758 | Antiviral activity against HIV1 with reverse transcriptase Y181I mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal 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. |
AID1357800 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 harboring reverse transcriptase L100I mutant | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Targeting the entrance channel of NNIBP: Discovery of diarylnicotinamide 1,4-disubstituted 1,2,3-triazoles as novel HIV-1 NNRTIs with high potency against wild-type and E138K mutant virus. |
AID663296 | Antiviral 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 assay | 2012 | Journal 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. |
AID1520059 | Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Fragment hopping-based discovery of novel sulfinylacetamide-diarylpyrimidines (DAPYs) as HIV-1 nonnucleoside reverse transcriptase inhibitors. |
AID46382 | Antiviral activity against site directed resistant isolate HIV-1 Y181C in CEM cells | 2001 | Journal 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. |
AID1761014 | Antiviral activity against HIV-1 harboring reverse transcriptase L100I mutant infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect measured after 5 days by MTT assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and evaluation of "dual-site"-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase. |
AID1888690 | Antiviral activity against HIV1 3B infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID1741394 | Inhibition of reverse transcriptase K103N mutant in HIV-1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. |
AID263513 | Antiviral activity against HIV1 K103N mutant | 2006 | Bioorganic & 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. |
AID440639 | Antiviral 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 assay | 2009 | Journal 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. |
AID440669 | Cytotoxicity against human MT4 cells assessed as reduction of cell viability after 4 days by MTT assay | 2009 | European 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. |
AID1171412 | Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay | 2014 | ACS medicinal chemistry letters, Nov-13, Volume: 5, Issue:11 | Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. |
AID619631 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10 | Arylazolylthioacetanilide. Part 8: Design, synthesis and biological evaluation of novel 2-(2-(2,4-dichlorophenyl)-2H-1,2,4-triazol-3-ylthio)-N-arylacetamides as potent HIV-1 inhibitors. |
AID1292012 | Selectivity index, ratio of CC50 for mock infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket. |
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AID590348 | Inhibition of Human immunodeficiency virus 1 NL4.3 reverse transcriptase activity at 0.1 ug/ml | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis of 9-substituted derivatives of berberine as anti-HIV agents. |
AID736038 | Inhibition of HIV1 reverse transcriptase p66/p51 K103N/Y181C mutant after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1880380 | Antiviral activity against HIV-1 IIIB harboring reverse transcriptase E138K mutant infected in human MT4 cells by MTT assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12 | Structure-Based Discovery of Novel NH |
AID1654197 | Plasma concentration in human | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
AID299031 | Antiviral activity against HIV1 with reverse transcriptase Y188H mutation in CEM cells assessed as inhibition of virus-induced giant cell formation | 2007 | Bioorganic & 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. |
AID1155807 | Antiviral 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 method | 2014 | Journal 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. |
AID318127 | Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis | 2008 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4 | Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors. |
AID279421 | Antiviral activity against HIV1 isolate with RT 101E, 190S mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1390714 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant | 2018 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 28, Issue:8 | First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. |
AID105000 | Inhibitory concentration which prevents the spread of HIV-1 IIIB infection in MT2 T-lymphoid cells | 1993 | Journal 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. |
AID607876 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for wild type Human immunodeficieny virus 1 3B infected in human MT4 cells | 2011 | Bioorganic & 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. |
AID361918 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase K101E mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID779526 | Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: synthesis, biological investigation and molecular modeling studies. |
AID197948 | In vitro inhibitory concentration against HIV-1 reverse transcriptase using rC-dG template primer | 1993 | Journal 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. |
AID248012 | In vitro inhibitory concentration against HIV LAI cell line | 2005 | Journal 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. |
AID1308895 | Inhibition 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 assay | 2016 | Bioorganic & 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. |
AID1654200 | Drug 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 analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Twelfth-Position Deuteration of Nevirapine Reduces 12-Hydroxy-Nevirapine Formation and Nevirapine-Induced Hepatocyte Death. |
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AID267651 | Selectivity for wild type HIV1 virus over HIV1 K103N mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID391680 | Selectivity 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/p51 | 2008 | Journal 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. |
AID157558 | Cytotoxic concentration was evaluated using microculture tetrazolium assay (MTA) | 1999 | Bioorganic & 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. |
AID1637403 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for human HIV-1 3B harboring E138K mutant infected in human MT4 cells | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. |
AID1888699 | Antiviral activity against HIV1 with RT RES056 mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID279471 | Antiviral activity against HIV1 isolate with RT 103N, 238N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID1155815 | Inhibition of HIV-1 recombinant NNTRI-resistant reverse transcriptase Y181I mutant assessed as incorporation of [3H]dTTP into poly(rA)/oligo(dT)10:1 | 2014 | Journal 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. |
AID1888695 | Antiviral activity against HIV1 with RT K103N mutant infected in human MT4 cells cells assessed as protection against viral-induced cytopathogenecity by MTT assay | |||
AID496629 | Antiviral activity against HIV-1 subtype CRF02_AG containing reverse transcriptase E138A/K20R, V35T, E36D, T39N, V60I, D123N, I135V, S162A, K173T, Q174K, D177E, T200A, Q207E, R211K mutant relative to control | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Resistance-associated mutations to etravirine (TMC-125) in antiretroviral-naïve patients infected with non-B HIV-1 subtypes. |
AID561942 | Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by agar dilution method | 2009 | Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8 | Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens. |
AID361926 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase V106A/Y181C mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
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AID573469 | Inhibition of DNA-dependent DNA polymerase activity of wild-type Human immunodeficiency virus 1 subtype B reverse transcriptase G190A mutant by filter-based filtration assay | 2009 | Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11 | Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine. |
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AID1379962 | Cytotoxicity in mock-infected human MT4 cells assessed as reduction in cell viability by MTT assay | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives as potent HIV-1 NNRTIs. |
AID302265 | Inhibition of HIV1 reverse transcriptase Y188L mutant | 2007 | Journal 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. |
AID1187999 | Antiviral activity against HIV1 3B acutely infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenic effect after 5 days by MTT assay | 2014 | Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17 | Exploiting the anti-HIV 6-desfluoroquinolones to design multiple ligands. |
AID1572519 | Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as inhibition of virus-induced cytotoxicity after 5 days by MTT assay | |||
AID105697 | Anti-HIV-1 activity against K103N+K1001 strain was determined | 2003 | Bioorganic & 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. |
AID1884487 | Cytotoxicity against human MT4 cells assessed as cell growth inhibition incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID1069709 | Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days | 2014 | Bioorganic & 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. |
AID508756 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase V179D, Y181C mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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AID198917 | Inhibition of HIV-1 wild-type RT | 2001 | Journal 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. |
AID294633 | Inhibition of HIV1 reverse transcriptase using Poly rC.dG template | 2007 | European journal of medicinal chemistry, Jul, Volume: 42, Issue:7 | Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones. |
AID328842 | Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence by CMFDA assay | 2007 | Drug 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. |
AID1335208 | Antiviral 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 | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | 2,4,5-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. |
AID293556 | Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay | 2007 | European 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. |
AID492284 | Antiviral 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 assay | 2010 | Bioorganic & 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. |
AID632796 | Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection | 2011 | Journal of medicinal chemistry, Dec-22, Volume: 54, Issue:24 | Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents. |
AID248258 | In vitro inhibitory concentration against HIV G190S mutant strain | 2005 | Journal 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. |
AID1152374 | Selectivity index, ratio CC50 for human MT4 cells to EC50 for HIV 1 3B | 2014 | Bioorganic & medicinal chemistry, Jun-15, Volume: 22, Issue:12 | Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors. |
AID105127 | Compound was evaluated for the inhibition of HIV-1 induced CPE (HTLV-III B strain ) replication in MT-4 cells | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. |
AID725389 | Antiviral activity against HIV1 LAI infected in CEMx174-LTR-GFP cells assessed as inhibition of viral replication after 5 days by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Synthesis and biological evaluation of triazolothienopyrimidine derivatives as novel HIV-1 replication inhibitors. |
AID1316329 | Inhibition of recombinant wild type HIV1 reverse transcriptase using DIG-dUTP/biotin-dUTP/dTTP assessed as suppression of biotin-dUTP incorporation after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17 | Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles. |
AID1884490 | Antiviral activity against drug-resistant HIV-1 K103 N mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
AID267653 | Selectivity for wild type HIV1 virus over HIV1 L100I mutant | 2006 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 16, Issue:13 | Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1. |
AID82141 | Effective concentration required to achieve 50% inhibition of HIV-1 multiplication in MT-4-infected K103N strain | 2002 | Journal 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. |
AID302256 | Resistance index, Ratio of EC50 for drug-resistant HIV1 with RT K103N mutation in MT3 cells to EC50 for HIV1 NL43 in MT3 cells | 2007 | Journal 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. |
AID1627028 | Cytotoxicity against HIV1 infected African green monkey Vero cells assessed as reduction in cell viability after 7 days by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID572173 | Antiviral 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 3B | 2009 | Antimicrobial 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. |
AID1241796 | Selectivity index, ratio of IC50 for human C8166 cells to EC50 for HIV1 3B infected in human C8166 cells | 2015 | Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17 | Pyrroloaryls and pyrroloheteroaryls: Inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase. |
AID1443667 | Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8 | Design and synthesis of hybrids of diarylpyrimidines and diketo acids as HIV-1 inhibitors. |
AID1185991 | Cytotoxicity against HEK293T cells at 10 uM after 48 hrs | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID88369 | Antiviral activity against K103N/V108I mutant virus in the HeLa MAGI assay. | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | 2-Amino-6-arylsulfonylbenzonitriles as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID736440 | Non-competitive inhibition of wild type HIV1 reverse transcriptase p66/p51 after 30 mins by liquid scintillation counting | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5 | N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase. |
AID1152239 | Antiviral 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 assay | 2014 | Bioorganic & 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. |
AID718366 | Inhibition of HIV1 recombinant reverse transcriptase assessed as incorporation of biotin-dUTP into poly(rC)-oligo(dG) by colorimetric analysis | 2012 | Bioorganic & 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. |
AID105203 | Antiviral activity against MT-4 cells infected with wild-type HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID1186001 | Antiviral 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 r | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | 2,4,5-Trisubstituted thiazole derivatives: a novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase. |
AID1736358 | Antiviral 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 | |||
AID518737 | Inhibition of DNA-dependent DNA polymerase activity of wild type HIV1 subtype B reverse transcriptase by gel-based primer extension assay | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity. |
AID366527 | Inhibition of RNA dependent DNA polymerase activity of HIV1 reverse transcriptase K103N mutant | 2008 | Journal 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. |
AID1731746 | Inhibition of reverse transcriptase L100I mutant in HIV-1 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect incubated for 5 days by MTT assay | |||
AID416756 | Antiviral activity against HIV1 with reverse transcriptase K103N mutation in human CEM cells assessed as protection against virus-induced cytopathicity | 2009 | Journal 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. |
AID259755 | Cytotoxicity against MT2 cells | 2006 | Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3 | Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase. |
AID592539 | Selectivity index, CC50 for human CEM cells to IC50 for HIV1 3B | 2011 | Journal 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. |
AID666415 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 SF33 | 2012 | Journal 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. |
AID1200846 | Selectivity index, ratio of CC50 for mock-infected human MT4 cells to EC50 for HIV1 3B infected in human MT4 cells | 2015 | European journal of medicinal chemistry, Mar-26, Volume: 93 | Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 4: design, synthesis and biological evaluation of novel imidazo[1,2-a]pyrazines. |
AID279407 | Antiviral activity against HIV1 isolate with RT 98G, 103N mutation relative to wild type | 2007 | Antimicrobial 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. |
AID155133 | Ability to inhibit the replication of A17 (Y181C) strain of HIV-1 p24 antigen production in PBMC | 1999 | Bioorganic & 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. |
AID82457 | Antiviral activity against G190A strain of HIV-1 | 2004 | Journal of medicinal chemistry, Feb-26, Volume: 47, Issue:5 | Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1. |
AID232779 | Selectivity index was defined as the ratio of CC50 to EC50 | 1992 | Journal 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. |
AID1627030 | Antiviral activity against HIV-1 LAI infected in human PBM cells after 7 days | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1574372 | Antiviral activity against wild type HIV 1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2019 | Journal of medicinal chemistry, 01-24, Volume: 62, Issue:2 | Effect of α-Methoxy Substitution on the Anti-HIV Activity of Dihydropyrimidin-4(3 H)-ones. |
AID606672 | Inhibition of HIV1 reverse transcriptase K103N mutant | 2011 | Bioorganic & 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. |
AID1175920 | Antiviral activity against VSV-G protein pseudotyped HIV1 system in HEK293T cells assessed as reduction in p24 level after 48 hrs by ELISA | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12 | Diterpenes from a Chinese collection of the brown alga Dictyota plectens. |
AID508645 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase Y181C, G190S mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
AID1304404 | Selectivity index, ratio of CC50 for cytotoxicity against mock-infected human CEM-SS cells to EC50 for antiviral activity against HIV-1 RF | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Systematic evaluation of methyl ester bioisosteres in the context of developing alkenyldiarylmethanes (ADAMs) as non-nucleoside reverse transcriptase inhibitors (NNRTIs) for anti-HIV-1 chemotherapy. |
AID508784 | Antiviral activity against Human immunodeficiency virus 1 HXB2 containing reverse transcriptase E138G mutant relative to Human immunodeficiency virus 1 3B | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. |
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AID361913 | Antiviral activity against NNRTI-resistant HIV1 with reverse transcriptase G190S mutant in HeLa cells by MAGI assay | 2008 | Journal 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
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AID1795349 | HIV-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.\\ | 1996 | Journal 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. |
AID1795423 | HIV-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.\\ | 1999 | Journal 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. |
AID1796564 | HIV-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.\\ | 2000 | Journal 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. |
AID1795743 | HIV-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.\\ | 2004 | Bioorganic & medicinal chemistry, Dec-01, Volume: 12, Issue:23 | Studies of nonnucleoside HIV-1 reverse transcriptase inhibitors. Part 1: Design and synthesis of thiazolidenebenzenesulfonamides. |
AID1799587 | In 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.\\ | 2009 | Chemical 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. |
AID1795381 | HIV-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.\\ | 1993 | Journal 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. |
AID1795395 | HIV-1 RT Assay from Article 10.1021/jm0211063: \\Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies.\\ | 2003 | Journal 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. |
AID1795330 | HIV-1 RT Assay from Article 10.1021/jm00111a045: \\Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones.\\ | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones. |
AID1795385 | HIV 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.\\ | 1996 | Journal 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. |
AID1795367 | HIV-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.\\ | 1996 | Journal 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. |
AID1795311 | HIV-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.\\ | 1993 | Journal 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. |
AID1795355 | HIV-1 RT Assay from Article 10.1021/jm9707030: \\Novel Nonnucleoside Inhibitors of HIV-1 Reverse Transcriptase. 8. 8-Aryloxymethyl- and 8-Arylthiomethyldipyridodiazepinones\\ | 1998 | Journal of medicinal chemistry, Jul-30, Volume: 41, Issue:16 | Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 8. 8-Aryloxymethyl- and 8-arylthiomethyldipyridodiazepinones. |
AID1795358 | HIV-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.\\ | 1998 | Journal 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. |
AID1802585 | RT Assay from Article 10.1016/j.bioorg.2017.01.006: \\Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.\\ | 2017 | Bioorganic chemistry, 02, Volume: 70 | Dihydropyrimidinone-isatin hybrids as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. |
AID1801807 | HIV-1 RT Inhibition Assay from Article 10.1111/cbdd.12751: \\Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach.\\ | 2016 | Chemical biology & drug design, 08, Volume: 88, Issue:2 | Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach. |
AID1795433 | HIV-1 RT Assay from Article 10.1021/jm990580e: \\Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.\\ | 2000 | Journal 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. |
AID1795382 | HIV-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)-c | 1993 | Journal 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 |
AID1795384 | HIV-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 inhibit | 2001 | Journal 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. |
AID1795394 | HIV-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.\\ | 1996 | Bioorganic & 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. |
AID1795388 | HIV-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.\\ | 2000 | Journal 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. |
AID1801345 | In vitro Anti-HIV RT Assay from Article 10.1111/cbdd.12497: \\Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents.\\ | 2015 | Chemical biology & drug design, Sep, Volume: 86, Issue:3 | Design, Synthesis, and Biological Evaluation of Novel Benzoyl Diarylamine/ether Derivatives as Potential Anti-HIV-1 Agents. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. 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. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. 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. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. 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. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2006 | The 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. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal 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. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 1995 | Nature structural biology, Apr, Volume: 2, Issue:4 | High resolution structures of HIV-1 RT from four RT-inhibitor complexes. |
AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 357 (11.76) | 18.2507 |
2000's | 1377 (45.37) | 29.6817 |
2010's | 1158 (38.15) | 24.3611 |
2020's | 143 (4.71) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (63.20) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 509 (15.85%) | 5.53% |
Reviews | 202 (6.29%) | 6.00% |
Case Studies | 162 (5.04%) | 4.05% |
Observational | 32 (1.00%) | 0.25% |
Other | 2,307 (71.82%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
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 2 | 452 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
Clinical Trial of CNS Penetrating ART to Prevent NeuroAIDS in China [NCT01340950] | Phase 4 | 250 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
Phase 2 Comparison of Low-Dose Naltrexone vs ARV Effectiveness in HIV+ Progression [NCT01174914] | Phase 2 | 171 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
Optimal Combination Therapy After Nevirapine Exposure [NCT00089505] | Phase 3 | 745 participants (Actual) | Interventional | 2006-11-30 | Completed | ||
NEVIRAPINE Plus LAMIVUDINE (3TC) for HIV Maintenance Therapy - A Single Center Pilot Study [NCT03223402] | 20 participants (Actual) | Interventional | 2016-12-23 | Completed | |||
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) | Interventional | 2016-12-01 | Completed | |||
"Safeguard the Household - A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country" [NCT00255840] | 812 participants (Actual) | Interventional | 2006-07-31 | Completed | |||
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 3 | 576 participants (Actual) | Interventional | 2006-10-31 | Completed | ||
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 2 | 484 participants (Actual) | Interventional | 2006-03-31 | Completed | ||
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 1 | 14 participants (Actual) | Interventional | 1998-04-30 | Completed | ||
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 3 | 2,648 participants (Actual) | Interventional | 1999-04-30 | Completed | ||
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 1 | 92 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
Clinical and Therapeutic Evaluation of the Infection by HIV/AIDS [NCT02191215] | 442 participants (Actual) | Observational | 2003-06-30 | Completed | |||
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) | Observational | 2002-05-31 | Completed | |||
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 1 | 204 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
PI or NNRTI as First-line Treatment of HIV in a West African Population With Low Adherence - the PIONA Trial [NCT01192035] | Phase 4 | 400 participants (Actual) | Interventional | 2011-05-31 | Completed | ||
Intensive Pharmacokinetic Studies of Antiretroviral Drug Combinations in Children [NCT00260078] | Phase 1/Phase 2 | 75 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
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 2 | 175 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
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 3 | 377 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
An Open-label Study in HIV+ Patients to Determine the Effects of Nevirapine (VIRAMUNE®) on the Steady State Pharmacokinetics of Rifabutin (MYCOBUTIN®) [NCT02184078] | Phase 4 | 19 participants (Actual) | Interventional | 1998-10-31 | Completed | ||
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 1 | 96 participants (Actual) | Interventional | 2008-04-30 | Completed | ||
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) | Observational | 1999-12-31 | Completed | |||
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 1 | 48 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (VIRAMUNE®) and Saquinavir-sgc (Fortovase®) in HIV-1 Infected Patients [NCT02184286] | Phase 1 | 5 participants (Actual) | Interventional | 1999-05-31 | Terminated | ||
An Open-label Study in HIV+ Patients to Determine the Effects of Nevirapine (VIRAMUNE®) on the Steady State Pharmacokinetics of Fluconazole (DIFLUCAN®) [NCT02181946] | Phase 4 | 24 participants (Actual) | Interventional | 2001-05-31 | Completed | ||
Phase III Randomized Trial of the Safety and Efficacy of Three Neonatal Antiretroviral Regimens for Prevention of Intrapartum HIV-1 Transmission [NCT00099359] | Phase 3 | 1,735 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
Role of Pharmacogenetics in Efavirenz and Nevirapine Pharmacokinetics, Efficacy and Safety in Mother-infant Pairs During Pregnancy and Lactation [NCT02269462] | 460 participants (Actual) | Observational | 2012-12-31 | Completed | |||
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 2 | 42 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289] | 1,578 participants (Actual) | Observational | 2003-06-09 | Completed | |||
A Randomized Open Label Trial of HIV Protease Inhibitors for the Prevention of Malaria in HIV-Infected Children [NCT00978068] | Phase 3 | 176 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
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 2 | 48 participants (Anticipated) | Interventional | 2009-02-28 | Completed | ||
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 4 | 138 participants (Actual) | Interventional | 1999-04-30 | Completed | ||
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) | Observational | 2002-01-31 | Completed | |||
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 2 | 44 participants (Actual) | Interventional | 2006-12-31 | Completed | ||
Pharmacokinetic Evaluation of Changes in Nevirapine AUC Due to Differences in Weight [NCT01335360] | 21 participants (Actual) | Observational | 2003-05-31 | Completed | |||
An Investigation of the Potential Pharmacokinetic Interaction Between Nevirapine (VIRAMUNE®), Abacavir and Amprenavir in HIV-1 Infected NNRTI Naive Adults [NCT02182765] | Phase 1 | 8 participants (Actual) | Interventional | 1999-04-30 | Terminated | ||
An Open-Label, Single Dose Study to Evaluate the Effects of Underlying Renal or Hepatic Dysfunction on the Pharmacokinetics of Nevirapine (VIRAMUNE®) [NCT02184091] | Phase 1 | 41 participants (Actual) | Interventional | 1999-01-31 | Completed | ||
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 1 | 27 participants (Actual) | Interventional | 2005-05-31 | Completed | ||
Genetic Determinants of the Metabolism of Non-nucleoside Reverse Transcriptase Inhibitors [NCT00730223] | Phase 1 | 33 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
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 3 | 3,526 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
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 3 | 1,068 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
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 1 | 85 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
[NCT00618176] | Phase 4 | 198 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
Pharmacokinetic Interaction Between Coartem® and Either Nevirapine, Efavirenz or Rifampicin in HIV Positive Ugandan Patients [NCT00620438] | Phase 4 | 90 participants (Anticipated) | Interventional | 2008-02-29 | Active, 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 1 | 16 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
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 3 | 722 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
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 1 | 105 participants (Actual) | Interventional | 2009-08-31 | Completed | ||
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 4 | 80 participants (Anticipated) | Interventional | 2006-07-31 | Completed | ||
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 4 | 9 participants (Actual) | Interventional | 2008-02-29 | Terminated(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 3 | 250 participants | Interventional | 2005-04-30 | Recruiting | ||
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 2 | 42 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
[NCT00523458] | Phase 4 | 5 participants (Actual) | Interventional | 2007-07-31 | Terminated(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 1 | 24 participants (Actual) | Interventional | 2010-10-31 | Active, 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 3 | 445 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
Cell Cycle Independent Antiretroviral Therapy: Combination of Nevirapine, FTC, and Tenofovir [NCT00344461] | Phase 4 | 54 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
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 4 | 18 participants (Anticipated) | Interventional | 2008-05-31 | Completed | ||
Randomized Control Trial of Early vs Delayed ART in the Treatment of Cryptococcal Meningitis. [NCT00830856] | 54 participants (Actual) | Interventional | 2006-10-31 | Completed | |||
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 | Interventional | Completed | ||||
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 | Interventional | Completed | ||||
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 2 | 10 participants | Interventional | Completed | |||
Randomized Trial of Protease Inhibitor-Including vs. Protease Inhibitor-Sparing Regimens for Women Who Initiate Therapy of HIV Infection During Pregnancy [NCT00017719] | Phase 3 | 440 participants | Interventional | 2002-05-31 | Completed | ||
Use of Combination Antiviral Therapy to Delineate the Identity and Longevity of Persistent Reservoirs of HIV-1 Infection and Replication [NCT00001644] | Phase 1 | 42 participants (Actual) | Interventional | 1997-03-03 | Completed | ||
HIV Infection and Breastfeeding: Interventions for Maternal and Infant Health [NCT00164736] | Phase 3 | 2,369 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
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 1 | 46 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
Substitution by Nevirapine in HIV-1 Infected Patients on Triple Treatment of Reverse Transcriptase Nucleoside/Nucleotide Inhibitors [NCT00415090] | Phase 4 | 28 participants (Actual) | Interventional | 2004-08-31 | Completed | ||
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 3 | 775 participants (Actual) | Interventional | 2001-02-28 | Completed | ||
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 3 | 120 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
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 1 | 75 participants | Interventional | Completed | |||
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 3 | 1,500 participants | Interventional | Completed | |||
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 2 | 300 participants | Interventional | Completed | |||
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 | Interventional | Completed | ||||
Treatment Outcome of Children With HIV Infection [NCT00476606] | 1,000 participants (Anticipated) | Observational | 2003-03-31 | Active, 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 4 | 140 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
Breastfeeding Version of the PROMISE Study (Promoting Maternal and Infant Survival Everywhere) [NCT01061151] | Phase 3 | 3,747 participants (Actual) | Interventional | 2011-03-01 | Completed | ||
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 4 | 21 participants (Actual) | Interventional | 2007-07-31 | Completed | ||
Open-Label, Multiple-Dose, Drug Interaction Study to Assess the Effect of Nevirapine on the Pharmacokinetics of Atazanavir in HIV-Infected Individuals [NCT00162149] | Phase 1 | 46 participants | Interventional | 2005-10-31 | Completed | ||
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 4 | 80 participants (Actual) | Interventional | 2003-02-28 | Completed | ||
Clinical Relevance of Nevirapine Resistance [NCT00117728] | Phase 3 | 250 participants (Anticipated) | Interventional | 2005-04-30 | Recruiting | ||
ART Pharmacokinetics, Mitochondrial Integrity, and Antioxidant Capacity in Severely Malnourished HIV-infected Malawian Children [NCT01529125] | 42 participants (Actual) | Observational | 2011-07-31 | Completed | |||
The Adult Antiretroviral Treatment and Resistance Study (Tshepo) [NCT00197613] | Phase 3 | 650 participants | Interventional | 2002-12-31 | Completed | ||
A Phase II Randomized, Multicenter Protocol Evaluating Two Antiretroviral Regimens Containing Combinations of Protease Inhibitors, NRTIs, and an NNRTI [NCT00000924] | Phase 2 | 120 participants | Interventional | Completed | |||
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 2 | 25 participants | Interventional | Terminated | |||
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 4 | 18 participants | Interventional | 2007-01-31 | Completed | ||
Efavirenz-based Versus Nevirapine-based Antiretroviral Therapy Among HIV-infected Patients Receiving Rifampin [NCT00483054] | Phase 3 | 142 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
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 3 | 570 participants (Actual) | Interventional | 2007-12-31 | Completed | ||
The Tshilo Dikotla Study: Metabolic Outcomes of Children HIV/ARV-Exposed Uninfected in Botswana (MOCHA) [NCT03088410] | Phase 4 | 495 participants (Actual) | Interventional | 2016-08-22 | Completed | ||
A Pharmacokinetic Evaluation of Levonorgestrel Implant and Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI)-Based Antiretroviral Therapy in HIV-infected Ugandan Women [NCT01789879] | Phase 2 | 60 participants (Actual) | Interventional | 2014-03-04 | Completed | ||
A Phase III Randomized, Double-Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00000942] | Phase 3 | 1,244 participants | Interventional | Completed | |||
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 3 | 0 participants | Interventional | Completed | |||
Comparison Atazanavir/Ritonavir (ATV/r) vs Nevirapine (NVP) Twice a Day (Bid) on Truvada Backbone [NCT00552240] | Phase 4 | 154 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
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 3 | 300 participants (Actual) | Interventional | 2006-04-30 | Completed | ||
[NCT00398684] | Phase 3 | 1,792 participants | Interventional | 2001-01-31 | Completed | ||
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 4 | 10 participants | Interventional | 2002-04-30 | Completed | ||
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) | Observational | 2006-02-28 | Completed | |||
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 2 | 144 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
MEDICLAS Study (Metabolic Effects of Different Classes of AntiretroviralS) [NCT00122226] | Phase 4 | 50 participants | Interventional | 2003-01-31 | Active, 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 2 | 905 participants (Anticipated) | Interventional | 2015-01-23 | Recruiting | ||
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) | Interventional | Withdrawn(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 4 | 67 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
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 3 | 407 participants | Interventional | 2003-01-31 | Completed | ||
[NCT00466180] | Phase 4 | 62 participants (Actual) | Interventional | 2004-06-30 | Completed | ||
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 4 | 15 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
Efavirenz to Nevirapine Switch in HIV-1 Infected Patients With Severe Dyslipidemia: A Randomized Controlled Study [NCT00405171] | Phase 4 | 40 participants | Interventional | 2003-06-30 | Completed | ||
Efficacy and Safety of Concomitant Use of Nevirapine and Rifampicin in Antiretroviral Naive Patients Co-infected With HIV and Tuberculosis in India. [NCT01805258] | Phase 3 | 135 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
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 2 | 240 participants | Interventional | Completed | |||
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 3 | 180 participants (Anticipated) | Interventional | 2006-06-30 | Active, 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 | Interventional | Completed | ||||
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 2 | 1,292 participants | Interventional | Completed | |||
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 2 | 225 participants | Interventional | Completed | |||
Extended Infant Post-exposure Prophylaxis With Antiretrovirals to Reduce Postnatal HIV Transmission [NCT00115648] | Phase 3 | 3,300 participants (Anticipated) | Interventional | 2004-04-30 | Completed | ||
Phase II, Randomized, Open-Label Study of Switching to Protease Inhibitor-Sparing Regimens for Improvement of Metabolic Abnormalities [NCT00021463] | Phase 2 | 342 participants | Interventional | Completed | |||
A Phase III Randomized, Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00000869] | Phase 3 | 2,009 participants | Interventional | Completed | |||
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 1 | 30 participants | Interventional | Completed | |||
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 2 | 25 participants | Interventional | 1998-01-31 | Completed | ||
Prevention of Maternal to Infant HIV Transmission in India [NCT00061321] | Phase 3 | 770 participants (Actual) | Interventional | 2002-08-31 | Completed | ||
A Pilot Study of a Nucleoside Analogue Reverse Transcriptase Inhibitor Sparing Regimen in Antiretroviral-Naïve, HIV-infected Patients [NCT00143689] | Phase 4 | 13 participants (Actual) | Interventional | 2002-04-30 | Completed | ||
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 4 | 53 participants (Actual) | Interventional | 2003-06-30 | Completed | ||
Phase III, Randomized, Double-Blind Comparison of Three Protease Inhibitor-Sparing Regimens for the Initial Treatment of HIV Infection [NCT00013520] | Phase 3 | 1,125 participants | Interventional | Completed | |||
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 | Interventional | 2001-06-30 | Completed | |||
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 | Interventional | 2002-03-31 | Completed | |||
Phase III Trial of Antibiotics to Reduce Chorioamnionitis-Related Perinatal HIV Transmission [NCT00021671] | Phase 3 | 3,720 participants | Interventional | Completed | |||
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 4 | 763 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
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 2 | 520 participants (Anticipated) | Interventional | 2003-07-31 | Active, not recruiting | ||
ARVs to Prevent Breastmilk HIV:Viral and Immune Responses [NCT00167674] | Phase 2 | 58 participants (Actual) | Interventional | 2003-05-31 | Completed | ||
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 3 | 435 participants (Actual) | Interventional | 2008-07-31 | Terminated(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) | Interventional | 2002-08-31 | Completed | |||
Optimizing Pediatric HIV-1 Treatment in Infants With Prophylactic Exposure to Nevirapine, Nairobi, Kenya (6-12 Month RCT) [NCT00427297] | Phase 3 | 34 participants (Actual) | Interventional | 2007-09-30 | Terminated(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) | Interventional | 2011-01-31 | Not 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 4 | 14 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
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 3 | 2,026 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
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 2 | 123 participants | Interventional | 2002-01-31 | Completed | ||
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 4 | 158 participants (Actual) | Interventional | 2001-09-30 | Completed | ||
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 1 | 675 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
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 3 | 379 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
Optimal Dosing of 1st Line Antituberculosis and Antiretroviral Drugs in Children (a Pharmacokinetic Study) [NCT01637558] | Phase 4 | 200 participants (Actual) | Interventional | 2012-11-30 | Completed | ||
Nevirapine vs Ritonavir-boosted Lopinavir in ART HIV-infected Adults in a Resource-limited Setting; a Randomized, Multicenter, Parallel Group Study [NCT01772940] | Phase 4 | 425 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
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 2 | 94 participants | Interventional | Completed | |||
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 2 | 730 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
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 1 | 49 participants | Interventional | Completed | |||
A Comparative Study of Combination Antiretroviral Therapy in Children and Adolescents With Advanced HIV Disease [NCT00000814] | Phase 1 | 390 participants | Interventional | Completed | |||
Multi-Drug Antiretroviral Therapy for Heavily Pretreated Pediatric AIDS Patients: A Phase I Proof of Concept Trial [NCT00001108] | Phase 1 | 6 participants | Interventional | Completed | |||
A Pilot Pharmacokinetic Phase I Evaluation of BI-RG-587 in HIV-Infected Children [NCT00000634] | 6 participants | Interventional | Completed | ||||
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 1 | 36 participants | Interventional | Completed | |||
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 3 | 2,000 participants | Interventional | Completed | |||
Effect of Moringa Oleifera (Moringa, Drumstick/Horseradish Tree) on The Pharmacokinetics of Efavirenz and Nevirapine In-vivo. [NCT01410058] | 19 participants (Actual) | Observational | 2013-01-31 | Completed | |||
A Comparative Study of a Combination of Zidovudine, Didanosine, and Double-Blinded Nevirapine Versus a Combination of Zidovudine and Didanosine [NCT00000770] | Phase 2 | 400 participants | Interventional | Completed | |||
Early Intensive Antiretroviral Combination Therapy in HIV-1 Infected Infants and Children [NCT00000872] | Phase 2 | 55 participants (Anticipated) | Interventional | Completed | |||
RAD-1: A Phase I/II Antiretroviral Management Algorithm for Pediatric Subjects of Four-Drug Combination Therapies Based on Prior Antiretroviral Experience [NCT00000902] | Phase 1 | 217 participants | Interventional | Completed | |||
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 2 | 250 participants | Interventional | Completed | |||
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 1 | 30 participants | Interventional | Completed | |||
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 | Interventional | Completed | ||||
A Phase III Randomized, Double-Blinded Study of Nevirapine for the Prevention of Maternal-Fetal Transmission in Pregnant HIV-Infected Women [NCT00001135] | Phase 3 | 2,009 participants | Interventional | Completed | |||
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 | Interventional | Completed | ||||
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 2 | 52 participants (Actual) | Interventional | 2014-01-10 | Completed | ||
Phase I/II Study of ABT-378/Ritonavir in Protease Inhibitor Experienced HIV-Infected Patients [NCT00004580] | Phase 1 | 0 participants | Interventional | Completed | |||
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 | Interventional | Completed | ||||
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 1 | 200 participants | Interventional | Completed | |||
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 1 | 24 participants | Interventional | Completed | |||
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 3 | 300 participants | Interventional | Completed | |||
A Pharmacokinetic Study to Assess Nevirapine Levels in HIV-infected Patients With Impaired Hepatic Function [NCT00144248] | Phase 4 | 51 participants (Actual) | Interventional | 2004-06-25 | Completed | ||
Neuropsychiatric Adverse Effects of Efavirenz in Children Living With HIV in Kilimanjaro, Tanzania [NCT03227653] | 144 participants (Actual) | Observational | 2017-06-19 | Completed | |||
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 2 | 11 participants (Actual) | Interventional | 2014-09-03 | Terminated(stopped due to This study was terminated early due to poor recruitment.) | ||
Latency and Early Neonatal Provision of Antiretroviral Drugs Clinical Trial [NCT02431975] | Phase 4 | 73 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
Population Pharmacokinetics of Antiretroviral in Children [NCT03194165] | 65 participants (Actual) | Observational | 2017-06-16 | Completed | |||
Steady State Bioequivalence of Generic and Innovator Formulations of Stavudine, Lamivudine, and Nevirapine in HIV-infected Ugandan Adults [NCT01025830] | Phase 4 | 20 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
BHP Early Infant Treatment Study: A Clinical Treatment Trial of HIV+ Infants in Botswana [NCT02369406] | Phase 2/Phase 3 | 67 participants (Actual) | Interventional | 2015-05-04 | Active, not recruiting | ||
Antiretroviral Regime for Viral Eradication in Newborns After Intervention Failure of Mother-to-child Transmission of HIV [NCT02712801] | Phase 4 | 600 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
Randomized Clinical Trial to Evaluate the Interest of a Down-scaled Treatment Strategy Using Dual Therapy (Nucleoside Analogs) in HIV Infected Patients Already Being Treated Using Triple Therapy, Who Present With a Successful Virological Control and for W [NCT02302547] | Phase 3 | 224 participants (Actual) | Interventional | 2014-12-31 | Completed | ||
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 4 | 1,206 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |