Lopinavir is a protease inhibitor medication used to treat HIV infection. It works by blocking the activity of the HIV protease enzyme, which is necessary for the virus to replicate. Lopinavir is typically taken in combination with ritonavir, another protease inhibitor, which helps to increase the levels of lopinavir in the blood. Lopinavir is available as both oral and intravenous formulations. It was developed by Abbott Laboratories and approved by the Food and Drug Administration (FDA) in 1999. Lopinavir is a synthetic compound, and its chemical name is (2S)-N-[(2R)-2-hydroxy-1-(phenylmethyl)-2-(2-[[(2S)-2-(2-quinolyl)acetyl]amino]phenyl)ethyl]-3,3-dimethylbutanamide. Lopinavir is effective in treating HIV infection, and it has been shown to reduce the risk of death and AIDS-related illnesses in people living with HIV. However, lopinavir can have side effects, such as diarrhea, nausea, and vomiting. It is important to note that lopinavir is not a cure for HIV, and it is not effective in preventing HIV transmission. It is also important to note that lopinavir should only be taken under the supervision of a healthcare provider. Lopinavir has been extensively studied for its antiviral activity against HIV, and it is one of the most commonly used antiretroviral medications. Research on lopinavir has focused on its mechanism of action, pharmacokinetics, efficacy, safety, and potential resistance development. Lopinavir is an important medication for people living with HIV, and it has significantly improved the quality of life for many individuals.'
ID Source | ID |
---|---|
PubMed CID | 92727 |
CHEMBL ID | 729 |
CHEBI ID | 31781 |
SCHEMBL ID | 21775 |
MeSH ID | M0558541 |
Synonym |
---|
a-157378.0 |
1(2h)-pyrimidineacetamide, n-((1s,3s,4s)-4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahyrdo-alpha-1-methylethyl)-2-oxo-, (alphas)- |
(1s-(1r*(r*),3r*,4r*))-n-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide |
c37h48n4o5 |
lopinavir , |
n-{1-benzyl-4-[2-(2,6-dimethyl-phenoxy)-acetylamino]-3-hydroxy-5-phenyl-pentyl}-3-methyl-2-(2-oxo-tetrahydro-pyrimidin-1-yl)-butyramide |
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, (alphas)- (9ci) |
1(2h)-pyrimidineacetamide, n-[4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, [1s-[1r*(r*),3r*,4r*]]- |
(alphas)-tetrahydro-n-((alphas)-alpha-((2s,3s)-2-hydroxy-4-phenyl-3-(2-(2,6-xylyloxy)acetamido)butyl)phenethyl)-alpha-isopropyl-2-oxo-1(2h)-pyrimidineacetamide |
aids032937 |
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-, (alphas)- |
koletra |
abt 378 |
aluviran |
a 157378 |
a 157378.0 |
abt-378 |
lpv , |
(2s)-n-[(1s,3s,4s)-1-benzyl-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-pentyl]-3-methyl-2-(2-oxohexahydropyrimidin-1-yl)butanamide |
rs-346 |
1(2h)-pyrimidineacetamide, n-[(1s,3s,4s)-4-[[(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-.alpha.-(1-methylethyl)-2-oxo-, (as)- |
1MUI |
DB01601 |
D01425 |
lopinavir (jan/usp/inn) |
NCGC00164576-01 |
NCGC00164576-02 |
2Q5K |
2O4S |
2RKF |
2RKG |
lopinavir, (s-(2s,4s,5s))- |
lopinavir- |
lopinavirum |
CHEMBL729 |
a-157378-0 |
chebi:31781 , |
NCGC00164576-03 |
dtxcid6026456 |
dtxsid8046456 , |
tox21_112204 |
cas-192725-17-0 |
(2s)-n-[(2r,4s,5s)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenyl-hexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide |
A813594 |
abt378 |
MLS004774152 |
lopinavir [usan:usp:inn:ban] |
unii-2494g1jf75 |
2494g1jf75 , |
hsdb 8138 |
BCP9000857 |
lpv & aag |
lopinavir & alpha1-acid glycoprotein |
BCPP000184 |
smr002529581 |
MLS003915624 |
lopinavir [ema epar] |
(1s-(1r*(r*),3r*,4r*))-n-(4-(((2,6-dimethylphenoxy)acetyl)amino)-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl)tetrahydro-.alpha.-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide |
lopinavir [usp monograph] |
lopinavir [who-ip] |
lopinavir [vandf] |
lopinavir [mart.] |
lopinavirum [who-ip latin] |
lopinavir [mi] |
kaletra component lopinavir |
lopinavir [usan] |
lopinavir [ep monograph] |
lopinavir [usp-rs] |
lopinavir component of kaletra |
(s)-n-((2s,4s,5s)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-diphenylhexan-2-yl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide |
(alphas)-tetrahydro-n-[(alphas)-alpha-[(2s,3s)-2-hydroxy-4-phenyl-3-[2-(2,6-xylyloxy)acetamido]butyl]phenethyl]-alpha-isopropyl-2-oxo-1(2h)-pyrimidineacetamide |
lopinavir [jan] |
lopinavir [inn] |
lopinavir [orange book] |
lopinavir [who-dd] |
S1380 |
AB01274785-01 |
HY-14588 |
CS-2077 |
lopinavir & plga |
MLS006011206 |
SCHEMBL21775 |
2QHC |
tox21_112204_1 |
NCGC00164576-04 |
3OGQ |
(2s)-n-((1s,3s,4s)-1-benzyl-4-{[(2,6-dimethylphenoxy)acetyl]amino}-3-hydroxy-5-phenylpentyl)-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide |
KJHKTHWMRKYKJE-SUGCFTRWSA-N |
AKOS025243115 |
(2s)-n-[(2s,4s,5s)-5-{[(2,6-dimethylphenoxy)acetyl]amino}-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide |
KS-1436 |
AB01274785_02 |
4L1A |
lopinavir (abt-378) |
(2s)-n-[(2s,4s,5s)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide |
J-521653 |
SR-01000931910-2 |
sr-01000931910 |
(alphas)-n-[(1s,3s,4s)-4-[[2-(2,6-dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-alpha-(1-methylethyl)-2-oxo-1(2h)-pyrimidineacetamide |
bdbm50180655 |
SW219767-1 |
abt-378; lopinavir |
(2s)-n-[(1s,3s,4s)-1-benzyl-4-{[(2,6-dimethylphenoxy)acetyl]amino}-3-hydroxy-5-phenylpentyl]-3-methyl-2-(2-oxotetrahydropyrimidin-1(2h)-yl)butanamide |
Q422585 |
EX-A4008 |
BRD-K99451608-001-02-4 |
CCG-270285 |
kaletra (lpv+rtv) |
a-1573780 |
gtpl11504 |
lopinavir 100 microg/ml in acetonitrile |
BL164636 |
lopinavir, bio-x |
HB7108 |
EN300-7402887 |
L0377 |
Z2235801862 |
lopinavir (mart.) |
lopinavir (ep monograph) |
lopinavir (usp monograph) |
abt-378/r |
lopinavir (usp-rs) |
j05ae06 |
Lopinavir (LPV) is a second-generation HIV protease inhibitor (PI) designed to overcome resistance development in patients undergoing long-term antiviral therapy. The drug has low aqueous solubility leading to poor oral bioavailability and thus frequent dosing.
Lopinavir/ritonavir has been approved for once-daily dosing in antiretroviral-naive patients. The drug has shown no improvement in time to clinical improvement which is seen in our meta-analyses (P=0.1). Lopinavirs and Ritonavir have been reported to be able to induce intracellular oxidative stress in diverse cellular models.
Lopinavir induced an increase in the fluorescence of pZsProSensor-1 transfected SiHa cells, indicative of proteasomal inhibition.
Excerpt | Reference | Relevance |
---|---|---|
"Lopinavir/ritonavir may increase the risk of diarrhoea and nausea and/or vomiting." | ( Adverse effects of remdesivir, hydroxychloroquine and lopinavir/ritonavir when used for COVID-19: systematic review and meta-analysis of randomised trials. Agoritsas, T; Bartoszko, JJ; Brignardello-Petersen, R; Chu, DK; Ge, L; Izcovich, A; Khamis, AM; Kum, E; McLeod, SL; Mustafa, RA; Qasim, A; Rochwerg, B; Siemieniuk, RA; Vandvik, P; Zeraatkar, D, 2022) | 1.69 |
"Lopinavir induced an increase in the fluorescence of pZsProSensor-1 transfected SiHa cells, indicative of proteasomal inhibition. " | ( Lopinavir up-regulates expression of the antiviral protein ribonuclease L in human papillomavirus-positive cervical carcinoma cells. Batman, G; Hampson, IN; Hampson, L; Oliver, AW; Richard, C; Zehbe, I, 2011) | 3.25 |
Treatment with lopinavir-ritonavir (adjusted hazard ratio [aHR], 2.28; 95% confidence interval [CI], 1.24 to 4.21) and younger age was associated with negative conversion of viral RNA. LopinavIR-rit onavir treatment was stopped early in 13 patients (13.8%) because of adverse events.
Study showed a high incidence of adverse events when a higher than standard dose of the new lopinavir/ritonavir tablets was combined with rifampicin. Grade 1 or 2 gastrointestinal adverse events were higher amon. It remains unclear whether a safe and effective rifabutin dose exists for treatment of TB.
Lopinavir Cmax and AUC12 were increased 20% to 30% when combined with ritonavir. 32 HIV-infected children received treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 1.
The KLEAN study extension assessed the long-term efficacy and safety of fosamprenavir-ritonavir (FPV/r) and lopinavirs (LPV) Both are administered with abacavir/lamivudine (ABC/3TC) fix.
Lopinavir (LPV), a newer HIV protease inhibitor, has poor bioavailability being a substrate of both cytochrome P450 3A enzyme system (CYP3A) and permeability-glycoprotein (P-gp) In HIV+ children on lopinavIR/ritonavir, bioavailability was reduced by 32% [median (IQR) steady-state Cmax = 0.0].
Lopinavir-ritonavir (LPV/r) recently became the preferred protease inhibitor (PI) for use in Nigeria since it is dosed once daily, which may improve treatment adherence. Further efficacy studies are necessary before routinely recommending this dosing strategy.
Role | Description |
---|---|
antiviral drug | A substance used in the prophylaxis or therapy of virus diseases. |
HIV protease inhibitor | An inhibitor of HIV protease, an enzyme required for production of proteins needed for viral assembly. |
anticoronaviral agent | Any antiviral agent which inhibits the activity of coronaviruses. |
[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 |
---|---|
amphetamines | Amines that constitute a class of central nervous system stimulants based on the structure of the parent amphetamine 1-phenylpropan-2-amine. |
dicarboxylic acid diamide | |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 29.8493 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521; AID1159523 |
SMAD family member 2 | Homo sapiens (human) | Potency | 23.9145 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 44.6684 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
SMAD family member 3 | Homo sapiens (human) | Potency | 23.9145 | 0.1737 | 34.3047 | 61.8120 | AID1346859 |
TDP1 protein | Homo sapiens (human) | Potency | 13.9650 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 29.8493 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 25.8544 | 0.0002 | 21.2231 | 8,912.5098 | AID1259243; AID1259247; AID743035; AID743036; AID743042; AID743054; AID743063 |
Smad3 | Homo sapiens (human) | Potency | 12.5893 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 24.2258 | 0.0006 | 57.9133 | 22,387.1992 | AID1259377; AID1259378 |
nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 33.4915 | 0.0010 | 22.6508 | 76.6163 | AID1224838; AID1224893 |
progesterone receptor | Homo sapiens (human) | Potency | 33.4915 | 0.0004 | 17.9460 | 75.1148 | AID1346784; AID1346795 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.4640 | 0.0123 | 7.9835 | 43.2770 | AID1346984; AID1645841 |
EWS/FLI fusion protein | Homo sapiens (human) | Potency | 26.9969 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 20.4223 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 3.7827 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 21.4552 | 0.0008 | 17.5051 | 59.3239 | AID1159527; AID1159531 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 20.5062 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403 |
farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 29.8470 | 0.3758 | 27.4851 | 61.6524 | AID743217; AID743220 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 16.9152 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 27.4759 | 0.0002 | 29.3054 | 16,493.5996 | AID1259244; AID1259248; AID743069; AID743075; AID743078; AID743079 |
G | Vesicular stomatitis virus | Potency | 17.3768 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 13.8029 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
67.9K protein | Vaccinia virus | Potency | 7.9433 | 0.0001 | 8.4406 | 100.0000 | AID720580 |
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 8.4120 | 0.0010 | 24.5048 | 61.6448 | AID743212 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 13.4184 | 0.0010 | 19.4141 | 70.9645 | AID743094; AID743140; AID743191 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 33.4915 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 11.2202 | 0.1000 | 9.1916 | 31.6228 | AID1346983 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 22.3872 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 29.0145 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 23.8128 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 12.5893 | 0.0079 | 8.2332 | 1,122.0200 | AID2551 |
geminin | Homo sapiens (human) | Potency | 35.5420 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 20.3148 | 0.0056 | 12.3677 | 36.1254 | AID624032 |
Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 33.4915 | 0.0015 | 57.7890 | 15,848.9004 | AID1259244 |
Interferon beta | Homo sapiens (human) | Potency | 17.3768 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 17.3768 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.2985 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 33.4915 | 0.0015 | 51.7393 | 15,848.9004 | AID1259244 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 17.3768 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
ATPase family AAA domain-containing protein 5 | Homo sapiens (human) | Potency | 23.7101 | 0.0119 | 17.9420 | 71.5630 | AID651632 |
Ataxin-2 | Homo sapiens (human) | Potency | 23.7101 | 0.0119 | 12.2221 | 68.7989 | AID651632 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 17.3768 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain B, protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain A, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain B, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain A, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain B, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain A, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain B, Protease | Human immunodeficiency virus 1 | Ki | 0.0000 | 0.0000 | 0.0000 | 0.0000 | AID977610 |
Chain A, PROTEASE RETROPEPSIN | Human immunodeficiency virus 1 | Ki | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977610 |
Chain B, PROTEASE RETROPEPSIN | Human immunodeficiency virus 1 | Ki | 0.0011 | 0.0011 | 0.0011 | 0.0011 | AID977610 |
Chain A, Protease Retropepsin | Human immunodeficiency virus 1 | Ki | 0.0045 | 0.0008 | 0.0045 | 0.0082 | AID977610 |
Chain B, Protease Retropepsin | Human immunodeficiency virus 1 | Ki | 0.0045 | 0.0008 | 0.0045 | 0.0082 | AID977610 |
Chain A, Protease Retropepsin | Human immunodeficiency virus 1 | Ki | 0.0045 | 0.0008 | 0.0045 | 0.0082 | AID977610 |
Chain B, Protease Retropepsin | Human immunodeficiency virus 1 | Ki | 0.0045 | 0.0008 | 0.0045 | 0.0082 | AID977610 |
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 21.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 47.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 17.3000 | 0.1100 | 7.1903 | 10.0000 | AID1443980; AID1473738 |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 (BRU ISOLATE) | Ki | 0.0017 | 0.0000 | 0.0828 | 3.3000 | AID1797110 |
Gag-Pol polyprotein | HIV-1 M:B_ARV2/SF2 | Ki | 0.0018 | 0.0000 | 0.0109 | 0.0895 | AID1796953 |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 (RF/HAT ISOLATE) | Ki | 0.0017 | 0.0000 | 0.0505 | 1.6160 | AID1797110 |
ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 0.0002 | 2.3185 | 10.0000 | AID416864; AID679931 |
Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.7050 | 0.0001 | 1.4162 | 9.9000 | AID589156 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | Ki | 15.0000 | 0.0075 | 3.0083 | 9.1100 | AID1805801 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 (µMol) | 14.9150 | 0.0002 | 2.4585 | 9.9600 | AID1804171; AID1845236 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | Ki | 15.0000 | 0.0000 | 1.6307 | 9.0000 | AID1805801 |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 (µMol) | 0.0350 | 0.0002 | 0.1042 | 1.7000 | AID1796876 |
Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.3000 | 0.0002 | 1.8742 | 10.0000 | AID416864 |
Alpha-1D adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.3000 | 0.0002 | 1.2704 | 10.0000 | AID416864 |
Gag-Pol polyprotein | Human immunodeficiency virus type 1 (STRAIN UGANDAN / ISOLATE U455) | Ki | 0.0017 | 0.0000 | 0.0505 | 1.6160 | AID1797110 |
Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 10.3000 | 0.0000 | 1.8194 | 10.0000 | AID416864 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 8.5114 | 0.0009 | 1.9014 | 10.0000 | AID576612 |
Protease | Human immunodeficiency virus 1 | IC50 (µMol) | 0.0250 | 0.0001 | 0.2248 | 7.3200 | AID618426 |
Protease | Human immunodeficiency virus 1 | Ki | 0.0007 | 0.0000 | 0.0443 | 3.1000 | AID160461; AID163477; AID1669454; AID238682; AID274379; AID274380; AID274381; AID274382; AID343015; AID343016; AID343017; AID343018; AID343019; AID343020; AID343021 |
CAAX prenyl protease 1 homolog | Mus musculus (house mouse) | IC50 (µMol) | 18.4000 | 1.2000 | 1.2000 | 1.2000 | AID328893 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 7.6000 | 0.0040 | 1.9666 | 10.0000 | AID1873200 |
Protease | Human immunodeficiency virus 1 | IC50 (µMol) | 0.0175 | 0.0000 | 0.8176 | 9.8500 | AID1057016; AID590915; AID664437 |
Protease | Human immunodeficiency virus 1 | Ki | 0.0002 | 0.0000 | 0.0284 | 1.1000 | AID1669455; AID1669456; AID321660; AID343014; AID374591; AID443165; AID537765; AID698062 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain B, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain A, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain B, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain A, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain B, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain A, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain B, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain A, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Chain B, protease | Human immunodeficiency virus 1 | Kd | 0.0000 | 0.0000 | 0.0039 | 0.0150 | AID977611 |
Spike glycoprotein | Betacoronavirus England 1 | EC50 (µMol) | 12.8200 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 (µMol) | 12.8200 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
Transmembrane protease serine 2 | Homo sapiens (human) | EC50 (µMol) | 12.8200 | 0.0030 | 4.5168 | 9.8200 | AID1804127 |
Procathepsin L | Homo sapiens (human) | EC50 (µMol) | 12.8200 | 0.0030 | 4.4874 | 9.8200 | AID1804127 |
Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 12.8200 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Human coronavirus 229E | EC50 (µMol) | 12.8200 | 0.0030 | 4.6136 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 12.8200 | 0.0030 | 4.4554 | 9.8200 | AID1804127 |
Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 (µMol) | 12.8200 | 0.0030 | 4.1105 | 9.8200 | AID1804127 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 (µMol) | 12.8200 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
Protease | Human immunodeficiency virus 1 | Kd | 0.0001 | 0.0001 | 0.0412 | 0.5770 | AID238043 |
Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 (µMol) | 12.8200 | 0.0030 | 4.5755 | 9.8200 | AID1804127 |
Protease | Human immunodeficiency virus 1 | EC50 (µMol) | 1.1600 | 0.0007 | 0.6942 | 2.7300 | AID1350502 |
Protease | Human immunodeficiency virus 1 | Kd | 0.0006 | 0.0000 | 0.6117 | 8.1500 | AID1307690; AID1307691 |
[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) |
---|---|---|---|---|---|---|---|
Albumin | Homo sapiens (human) | KD2 | 6.0000 | 6.0000 | 6.0000 | 6.0000 | AID239810 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2008 | Journal of virology, Jun, Volume: 82, Issue:12 | Ninety-nine is not enough: molecular characterization of inhibitor-resistant human immunodeficiency virus type 1 protease mutants with insertions in the flap region. |
AID1797110 | Protease Inhibition Assay from Article 10.1021/bi051886s: \\Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.\\ | 2006 | Biochemistry, May-02, Volume: 45, Issue:17 | Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir. |
AID1796953 | Enzyme Inhibition Assay from Article 10.1021/jm060666p: \\Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.\\ | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
AID1799570 | Inhibition Assay from Article 10.1111/j.1747-0285.2007.00514.x: \\Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.\\ | 2007 | Chemical biology & drug design, May, Volume: 69, Issue:5 | Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis. |
AID1796876 | Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2005.03.008: \\Oximinoarylsulfonamides as potent HIV protease inhibitors.\\ | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Oximinoarylsulfonamides as potent HIV protease inhibitors. |
AID328893 | Inhibition of mouse ZMPSTE24 expressed n delta ste24 delta rce1 yeast | 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. |
AID369953 | Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID374591 | Inhibition of HIV1 protease | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID557231 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured before administering last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID328891 | Inhibition of human ICMT expressed in yeast assessed as methylation of N-acetyl-farnesylcysteine | 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. |
AID557282 | Ratio of EC50 for HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID369954 | Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID519783 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-60K/N-65E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID668809 | Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID297669 | Inhibition of HIV1 Protease M2 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID564038 | Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID558383 | Drug level in HIV-infected pregnant woman amniotic fluid at 400 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. |
AID238682 | Inhibition constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
AID1482906 | Antiviral activity against tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemilumi | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID415245 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID374626 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/53L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID369941 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID372182 | Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1482921 | Antiviral activity against atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID321695 | Ratio of EC50 for HIV1 mutant strain 3 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID558397 | Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 400 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. |
AID622660 | Antiviral activity against HIV1 harboring protease L10I, I13V, G16A, Q18H, L33F, N37D, M46I, I54V, G57R, Q61H,I62V, L63P, A71L, I72T, L76V, V77I, V82A, N88G, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
AID519552 | Antiviral activity against HIV1 isolate 9 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15I/V, K20R, L33F, E35D, M36I, N37D, R41K, K43I, M46I, I54V, I62V, L63P, A71T, I72T, V82A, I84V, L90M, I93L | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID564031 | Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1219738 | Maximum plasma concentration in healthy human at 400 mg co-administered with 50 mg ritonavir | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID328878 | Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 48 hrs 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. |
AID278976 | Antiviral activity against HIV1 C9 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID374593 | Cytotoxicity against human MT4 cells after 6 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID519545 | Antiviral activity against HIV1 isolate 2 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, G16E, K20R, E35D, M36I, R41K, I54A, R57K, Q61D, A71V, I72R, V82A, L89I, L90M, Q92K mutation derived fro | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID519789 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10V/I-40D-43I-56V-70K-82F-84V-89V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID557273 | Antiviral activity against HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID519780 | Antiviral activity against HIV 2 subtype H expressing 10I-34E-40P-41Y-60H-63N-70T-73G-82F-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID396260 | Antiviral activity against HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
AID622658 | Antiviral activity against HIV1 B26 harboring protease L33F, K45I, M46I, I50V, A71V and V82F mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
AID105346 | Tested for cytopathic effect of HIVIIIB in MT-4 cells in presence of 50% human serum | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10 | Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships. |
AID372186 | Resistance index, ratio of EC50 for HIV1 with protease 54V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1350503 | Ratio of EC50 for inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells to EC50 for wild-type HIV-1 pNL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
AID13678 | Cmax value in the period of 8 hr after dosing. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Protease inhibitors: current status and future prospects. |
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. |
AID279336 | Antiviral activity against wild type HIV2 in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID322122 | Antiviral activity against HIV1 97ZA003 R5 subtype C in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID343025 | Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID1669456 | Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 6 | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
AID532460 | Antiviral activity against Human immunodeficiency virus 1 isolate 20 harboring Gag-capsid I138L, V215L, V218P, H219Q, M228I, E230D, G248T, T280A, E312D, A340G and G357S mutant gene and protease L10F, A22V, D30N, S37N, K45R, I54L, I62V, L63P, A71V, V77I, I | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID1717746 | Selectivity index, ratio of CC50 for African green monkey Vero E6 cells to EC50 for SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID375204 | Ratio of EC50 for multidrug-resistant HIV1 isolate TM to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID519577 | Antiviral activity against HIV1 clone2 infected in HEK293 cells harboring A-790742-selected protease V82L mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID1482925 | Ratio of IC50 for nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID519554 | Antiviral activity against HIV1 isolate 11 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, K20R, E21Q, E35D, M36I, N37D, R41K, M46L, I54V, I62V, L63P, A71V, T74D, P79A, V82T, I84V, I85V, L90M, | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID446195 | Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID278958 | Antiviral activity against HIV1 A6 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID547020 | Selectivity ratio of EC50 for HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype C | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID279344 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L99F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID1219734 | Drug metabolism in human liver microsomes assessed as CYP2D6-mediated lopinavir-GSH adduct formation at 2 uM after after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID416859 | Increase in P-glycoprotein-mediated tenofovir disoproxil fumarate permeation from apical to basolateral side of human Caco-2 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID374623 | Resistance index, ratio of EC50 for HIV1 with protease 32I/46L/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID353726 | Aqueous solubility in water by shake flask method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
AID557290 | Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID374628 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/53L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1474091 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells | 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. |
AID21894 | The partition coefficient was reported | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8 | Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
AID519580 | Antiviral activity against HIV1 clone5 infected in HEK293 cells harboring A-790742-selected protease L63P, A71V, and V82G mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 RF | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID572579 | Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID541175 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S and Q148H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID248098 | Inhibitory concentration against resistant (A17) human immunodeficiency virus | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Oximinoarylsulfonamides as potent HIV protease inhibitors. |
AID278969 | Antiviral activity against HIV1 C2 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID374613 | Resistance index, ratio of EC50 for non-B type HIV1 with protease 32I/47A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID162683 | Inhibition of HIV protease at 0.5 nM | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8 | Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
AID297668 | Inhibition of HIV1 Protease M1 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID558390 | Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 400 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. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID369958 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 1 passage | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID532473 | Antiviral activity against Human immunodeficiency virus 1 isolate 34 harboring Gag-capsid I138L, I147L, V159I, V215L, T280V, A309C, S310T, E312D and G357S mutant gene and protease L10I, I13V, E35D, S37N, I62V, L63P and I64M mutant gene infected in human M | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID369956 | Ratio of EC50 for HIV2 ROD with protease V47A mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID242933 | Dissociation rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID572577 | Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir with NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID374592 | Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID369957 | Ratio of EC50 for HIV2 ROD with protease G17N/V47A mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID353765 | AUC in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
AID668815 | Cytotoxicity against human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID1669457 | Antiviral activity against wild-type HIV1 NL4-3 infected in human TZM-bl cells infected with supernatants from virus-infected human 293T cells treated with compound for 18 hrs assessed as reduction in viral replication by luciferase assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
AID582282 | Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI measured 12 hrs after last dose | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID521547 | Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID519550 | Antiviral activity against HIV1 isolate 7 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, M46M/L, G48V, I54V, L63P, A71V, I72M, V77I, V82A, L90M, I93L mutation derived from viral passages with Lopina | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID679931 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells | 2003 | AIDS (London, England), May-02, Volume: 17, Issue:7 | Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. |
AID446202 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate G to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID532453 | Antiviral activity against Human immunodeficiency virus 1 isolate 32 harboring Gag-capsid, I138L, A146P, I147L, V159I, V215L, I223A, N252S/N, T280V and S310T and protease R41K/R, I62V, L63P, V77I and I93L mutant gene infected in human MT-2 cells by XTT-as | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID564048 | Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1219720 | Drug metabolism in human liver microsomes assessed as GSH-conjugated monohydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID321698 | Ratio of EC50 for HIV1 mutant strain 6 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID242868 | Association rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID557286 | Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID541164 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID557297 | Ratio of EC50 for HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport 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. |
AID278975 | Antiviral activity against HIV1 C8 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID321660 | Inhibition of HIV1 protease | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID417048 | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID446205 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate JSL to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID572581 | Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID369946 | Ratio of EC50 for HIV2 CDC310319 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID658567 | Resistance factor, ratio of EC50 for multidrug-resistant HIV1 106-PR infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3 | Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID557232 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID322105 | Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID278974 | Antiviral activity against HIV1 C7 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID537771 | Antiviral activity against multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID1482914 | Antiviral activity against darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production af | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID519793 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 12T-14Y-19P-40N-41D-61N-62I-96S-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID278956 | Antiviral activity against HIV1 A4 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID374622 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2 | Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
AID278966 | Antiviral activity against HIV1 A14 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID541163 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92Q mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID572582 | Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID369951 | Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID374627 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID557277 | Ratio of EC50 for HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1482926 | Ratio of IC50 for atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID541130 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTM184V mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID519546 | Antiviral activity against HIV1 isolate 3 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, E35D, N37D, M461, I54V, L63P, A71V, T74P, I84V, L90M, I93L mutation derived from viral passages with Lopinavi | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in 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. |
AID519575 | Antiviral activity against HIV1 P13 infected in human MT4 cells derived from viral passages with A-790742 harboring protease M46I, L63P, A71V, and V82G mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days p | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
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. |
AID525488 | Antigametocyte activity against Plasmodium falciparum harboring GFP-tagged Pfs16 protein assessed as reduction in number of gametocytes after 40 hrs by [3H]hypoxanthine incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID557278 | Ratio of EC50 for HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1725421 | Antiviral activity against DRV resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID374630 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID575063 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I mutation in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID321681 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID1295706 | Aqueous solubility of the compound by shake flask method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7 | Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends. |
AID278973 | Antiviral activity against HIV1 C6 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID519786 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-45K/R-46V-54M-64I/V-69K/R-71V/I-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID566850 | Antiviral activity against HIV-1 MDR/TM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID343028 | Ratio of Ki for HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID537768 | Antiviral activity against Human immunodeficiency virus 1 clade A isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID1725420 | Antiviral activity against ATV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID532469 | Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-capsid I138L and V215L mutant gene and protease L10I, S37N, M46L, G48V, R57K, L63P, I66F, A71V, V82T and I84V mutant gene infected in human MT-2 cells by XTT-assay relative | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID557295 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1380930 | Resistance index, ratio of EC50 for antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID586625 | Antiviral activity against HIV1 harboring mutant protease with matrix K76R mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID586618 | Ratio of EC50 for HIV1 harboring mutant protease with matrix Y79F mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID558369 | Drug level in HIV-infected pregnant woman maternal blood plasma at 400 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. |
AID532463 | Antiviral activity against Human immunodeficiency virus 1 isolate 9 harboring Gag-capsid I138L, A146S, I147L, V215L, N252H, T280A, A340G and E345D mutant gene and protease L10I, I13V, K20M, L33V, M36I, S37N, I54V, R57K, I62V, L63P, I66L, A71V, G73S, P79A, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID726411 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID343026 | Ratio of Ki for HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID322112 | Antiviral activity against wild type HIV1 ERS104prc X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID105589 | Cytotoxicity against MT-4 cells | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
AID519553 | Antiviral activity against HIV1 isolate 10 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20R, L33F, E35D, M36I, N37D, I54L, Q58E, I62V, L63P, A71V, V82A, I84V, L90M mutation derived from vir | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID532466 | Antiviral activity against Human immunodeficiency virus 1 isolate 27 harboring Gag-capsid I138L, S173T/S, V215L, L268M, R275K/R, T280V, S310T, E319D and G357S and protease L10I, I15V, L19V, V32I, L33F, M46I, I54V, K55R, R57K, L63P, C67F, H69Q, A71V, G73C/ | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID589156 | Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone hydroxylation | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5 | Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
AID321662 | Antiviral activity against HIV1 3B in presence of 50% human serum | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID1057015 | Inhibition of HIV-1 multidrug-resistant protease 769 preincubated for 20 mins by FRET analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID162704 | Compound was tested for its inhibitory potency against HIV protease at 0.5 nM | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
AID278982 | Resistance to HIV1 with protease 46I, 54I and I84A mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID279341 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID297670 | Inhibition of HIV1 Protease M3 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID1482913 | Antiviral activity against darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID278961 | Antiviral activity against HIV1 A9 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID1057014 | Ratio of IC50 for HIV-1 multidrug-resistant protease 769 to IC50 for HIV-1 NL4-3 wild type protease | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID446198 | Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID415251 | Metabolic stability in human liver microsomes assessed as inhibition of metabolism at 2 uM by LC/MS/MS analysis in presence of ritonavir | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID446201 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate C to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID369962 | Ratio of EC50 for HIV2 MS infected in human MT4 cells after 18 passages to EC50 for HIV2 MS infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID546990 | Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID278984 | Resistance to HIV1 with protease 46I, 54V and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID525477 | Antigametocyte activity against ring stage Plasmodium falciparum D10 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID1482923 | Ratio of IC50 for lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID622656 | Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay in presence of 50% human serum | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
AID537774 | Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 MDRC4 to EC50 for wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID446200 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate B to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID321696 | Ratio of EC50 for HIV1 mutant strain 4 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID443166 | Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells. |
AID532478 | Antiviral activity against Human immunodeficiency virus 1 isolate 12 harboring Gag-capsid I138L E207D, V215L, V218P, H219Q, M228I, G248T, T280S, E312D, A340G, G357S and V362I mutant gene and protease S37N, I62V/I, L63P, I64L and V82I mutant gene infected | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID724346 | Inhibition of C-south african HIV-1 protease assessed as hydrolysis of the chromogenic peptide substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Linear and cyclic glycopeptide as HIV protease inhibitors. |
AID1482918 | Ratio of IC50 for darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID1422658 | Inhibition of ZMPSTE24 in human KP4 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID1725423 | Antiviral activity against HIV1 DRVR P51 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID369952 | Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID446196 | Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
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] | |||
AID1409312 | Antiviral activity against darunavir-resistant HIV1 at passage 30 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID442713 | Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
AID279347 | Antiviral activity against HIV1 isolate 5512 with D30N, M461 and V771 mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID328892 | Inhibition of mouse RCE1 expressed in delta ste24 delta rce1 yeast | 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. |
AID547007 | Antiviral activity against HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID246194 | Protease inhibitory activity against HIV-1 r13034 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
AID532655 | Antiviral activity against Human immunodeficiency virus 1 isolate 39 harboring Gag-capsid A146P, I147L, V215L, M228I, G248A, R286K, A326S, G357S and V362I mutant gene and protease K14R, E35D, M36I, S37N, R41K, K45R, D60E, I62V and I64V mutant gene infecte | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID417028 | Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmax of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID586617 | Ratio of EC50 for HIV1 harboring mutant protease with matrix A81T mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID416864 | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID432028 | Antimalarial activity against Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2. |
AID322102 | Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID322100 | Selectivity index, ratio of CC50 for MT2 cells to EC50 for HIV1 LAI | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID519782 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 5L/F-14Y/H-17G/D-43T-54I/M-62V/A-70R/K-71I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID1845236 | Inhibition of SARS-CoV-2 MPro | 2021 | Bioorganic & medicinal chemistry, 01-01, Volume: 29 | Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors. |
AID525279 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID1422656 | Inhibition of ZMPSTE24 in human U2OS cells assessed as increase in intracellular accumulation of prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID564063 | Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID564032 | Cytotoxicity against human MT2 cells after 7 days by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID442704 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
AID279346 | Antiviral activity against HIV1 isolate 5512 with V321 and M46L mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID521549 | Antiviral activity against HIV 2 subtype H expressing 10I-40P-41Y-60H-63N-70T-73G-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID446204 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate MM to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID162693 | Inhibitory activity (0.5 nM) against Protease | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10 | Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships. |
AID322101 | Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID541132 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTK103N mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID343017 | Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID519784 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 54M-65E-71I-74N-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID575060 | Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations and protease L76V mutation in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID532457 | Antiviral activity against Human immunodeficiency virus 1 isolate 26 harboring Gag-capsid I138L, A146S, I147L, E312D, A326S, L337M, and A340G mutant gene and protease T4S, L10F, V11L, I13V, I15V, K20A, V32I, L33F, M36I, S37D, K43T, M46I, I54L, I62V, L63P, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID557239 | Ratio of drug level in 2 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID541131 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RT-6TAMs mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID374603 | Resistance index, ratio of EC50 for HIV1 with protease 54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1323585 | Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide at 5 to 50 uM preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies. |
AID278959 | Antiviral activity against HIV1 A7 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID163477 | Binding affinity against ritonavir-resistant strains. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Protease inhibitors: current status and future prospects. |
AID564042 | Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1057016 | Inhibition of HIV-1 NL4-3 wild type protease expressed in Escherichia coli preincubated for 20 mins by FRET analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23 | Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
AID541109 | Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID328888 | Effect on HDJ2 farnesylation in mouse fibroblast cells at 20 uM after 24 hrs 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. |
AID1219735 | Drug metabolism in human liver microsomes assessed as CYP1A2-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID546996 | Antiviral activity against HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID683726 | Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 100 mg/kg, po co-administered with 50 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculation | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Targeting the liver stage of malaria parasites: a yet unmet goal. |
AID519792 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-61N-64V-71I-90M-95I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID532455 | Antiviral activity against Human immunodeficiency virus 1 isolate 8 harboring Gag-capsid V215T mutant gene and protease L10I, L24I, L33F, S37N, R41K, I54V, D60E, I62V, L63P, A71V, V77I, V82A and I84V mutant gene infected in human MT-2 cells by XTT-assay r | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID374639 | Resistance index, ratio of EC50 for HIV1 with protease 46L/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID547004 | Antiviral activity against HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID557221 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID274380 | Inhibition of HIV1 protease L10I/G48V/I54V/L63P/V82A mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
AID343018 | Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID105401 | Antiviral activity against the cytopathic effects of HIV IIIB in MT-4 cells was assayed in the presence of 50% human serum | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21 | Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
AID247984 | Inhibitory concentration against wild type human immunodeficiency virus | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9 | Oximinoarylsulfonamides as potent HIV protease inhibitors. |
AID532471 | Antiviral activity against Human immunodeficiency virus 1 isolate 31 harboring Gag-capsid I138L, S173T, V215L, I223N, M228L, G248Q, N252H, T280V and E312D mutant gene and protease I13V, K14R/K, M36I, S37N, I64V, H69K and I72V mutant gene infected in human | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID566851 | Antiviral activity against HIV-1 MDR/MM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID586622 | Ratio of EC50 for HIV1 harboring HIV1 harboring wild type 8.9NSX with gag RF79F and T81A mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID547018 | Selectivity ratio of EC50 for HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene to EC50 for wild type HIV1 subtype B | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID557279 | Ratio of EC50 for HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1482905 | Antiviral activity against amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID274379 | Inhibition of wild type HIV1 protease Q7K mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
AID582276 | Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID278985 | Resistance to HIV1 with protease 46I, 54M/V and I84A mutation in HEK 293 relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID417038 | Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmin of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID279345 | Antiviral activity against wild type HIV1 in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID532462 | Antiviral activity against Human immunodeficiency virus 1 isolate 37 harboring Gag-capsid V135I, I138P, V143I, Q182H, V215L/V, V218P/A, H219Q, I223V, E230D, N252S, T280A, R286K, K302R and G357S mutant gene and protease S37D, R41K, L63P and I93L mutant gen | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID369959 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 11 passages | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID274381 | Inhibition of HIV1 protease D30N/L63P/N88D mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
AID532467 | Antiviral activity against Human immunodeficiency virus 1 isolate 1 harboring Gag-capsid I138L, V159I, E203D, V215L, I223V, T280V, E312D and V323I mutant gene and protease L10I, K20R, M36I, S37N, G48V, I54M, I62V, L63P, A71V, I72V, V82A, I84V, L90M and I9 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID698059 | Selectivity index, ratio of Ki for HIV protease V82A mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Rational approaches to improving selectivity in drug design. |
AID352084 | Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID1380926 | Antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID321679 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID322117 | Antiviral activity against HIV1 MDR/C X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID321677 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID279340 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 150V mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID668816 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID541172 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1717754 | Antiviral activity against SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells incubated for 3 days | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID1409308 | Antiviral activity against Atazanavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID446193 | Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID1193134 | Antimalarial activity against Plasmodium knowlesi infected Chinese rhesus macaques assessed as parasitemia level in blood smears at 40 mg/kg, intragastric treated 5 days before infection measured between day 0 to 7 by Giemsa-staining in presence of ritona | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Ritonavir-boosted indinavir but not lopinavir inhibits erythrocytic stage Plasmodium knowlesi malaria in rhesus macaques. |
AID532657 | Antiviral activity against Human immunodeficiency virus 1 isolate 4 harboring Gag-capsid A146P, V159I, K162R, Q182S, T186I, V215L, I223G/V, N252G, P255A, E260D, E312D and G357S mutant gene and protease L10R, S37N, M46L, I62V, L63P, A71V, T74S, V82T, L90M | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID372181 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID572574 | Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID557244 | Toxicity in HIV-infected Thai pregnant women assessed as adverse effect at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID374625 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID519544 | Antiviral activity against HIV1 isolate 1 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10V, I15V, G16E, K20R, E35D, M36I, R41K, M46I, I54V, R57K, Q61N, I64L, A71V, I72R, V82A, L89I, L90M, Q92K mutation | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID374638 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID532458 | Antiviral activity against Human immunodeficiency virus 1 isolate 28 harboring Gag-capsid I138M mutant gene and protease L10I, I13V, L23I, L33F, S37N, M46I, I54V, K55R, R57K, Q58E, D60E, I62V, L63P, A71I, I72V, L76V, V77I, V82A, I84V, I85V, L89M, L90M and | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID683725 | Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 25 mg/kg, po co-administered with 12.5 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculatio | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Targeting the liver stage of malaria parasites: a yet unmet goal. |
AID322110 | Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID321680 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID322111 | Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID537766 | Inhibition of multidrug resistant HIV1 protease L101I, L36P, A71V, G73S, I84V, L90M mutant by FRET | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID668810 | Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID328894 | Effect on change in ZMPSTE24 mRNA expression level in mouse fibroblasts at 20 uM after 10 days by PCR | 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. |
AID369943 | Antiviral activity against HIV2 CDC310319 isolate infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID321694 | Ratio of EC50 for HIV1 mutant strain 2 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID239810 | Equilibrium dissociation constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID375205 | Ratio of EC50 for multidrug-resistant HIV1 isolate MM to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID553577 | Antiviral activity against HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID519785 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-46V-66V/A-70R/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID374609 | Resistance index, ratio of EC50 for HIV1 with protease 84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID557299 | Ratio of EC50 for HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID322097 | Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID372184 | Resistance index, ratio of EC50 for HIV1 with protease 37T/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID519579 | Antiviral activity against HIV1 clone4 infected in HEK293 cells harboring A-790742-selected protease L33F, A71V, G73S, V77I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pN | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID374601 | Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID279338 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID278967 | Antiviral activity against HIV1 A15 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID321685 | Antiviral activity against wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID668808 | Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID1380929 | Resistance index, ratio of EC50 for antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID297671 | Antiviral activity against HIV1 infected MT4 cells by MTT method | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID541173 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K and Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID375199 | Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID532465 | Antiviral activity against Human immunodeficiency virus 1 isolate 25 harboring Gag-capsid I138M, S173A, V215L, N252S, I256T, S310T/S, A340G and E345D mutant gene and protease L10F, V11I, I13V, K20I, V32I, L33F, E34Q, E35D, M36I, S37N, K43T, M46I, F53Y, I5 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID586628 | Ratio of EC50 for HIV1 harboring 8gpNS with K76R, F79Y, and A81T mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID343027 | Ratio of Ki for HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant to Ki for wild-type HIV1 BH10 protease expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID369960 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 18 passages | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID369947 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID553576 | Antiviral activity against HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID553571 | Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID321690 | Antiviral activity against HIV1 mutant strain 5 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID519573 | Antiviral activity against HIV1 P15 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L33L/F, K45I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID668817 | Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID519538 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID343022 | Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID374612 | Resistance index, ratio of EC50 for HIV1 with protease 30N/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID532475 | Antiviral activity against Human immunodeficiency virus 1 isolate 38 harboring Gag-capsid I138L, I147L, V215L, H219Q/H, I223V, N252H, P292S, A336S/A and A340G mutant gene and protease E35D, S37A and L63P mutant gene infected in human MT-2 cells by XTT-ass | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID564040 | Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID557298 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1482915 | Antiviral activity against nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID369944 | Ratio of EC50 for HIV2 MS to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID588986 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1A2 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3 | Membrane transporters in drug development. |
AID374604 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID257271 | Antiviral activity against HIV1 in the presence of 50% human serum | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
AID586624 | Antiviral activity against HIV1 harboring wild type 8.9NSX with mutant amino acid 116 insertion infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID1219721 | Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID1219719 | Drug metabolism in human liver microsomes assessed as compound-GSH adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID557276 | Antiviral activity against HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID322098 | Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID582278 | Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID1725418 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID622659 | Antiviral activity against HIV1 isolate 1 harboring protease L10I, E35D, N37D, M46I, I54V, G57R, L63P, A71V, T74P, I84V, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
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. |
AID328886 | Toxicity in HEK293 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. |
AID374610 | Resistance index, ratio of EC50 for HIV1 with protease 33F/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID322115 | Antiviral activity against HIV1 MDR/JSL R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID557287 | Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1482919 | Antiviral activity against saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassa | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID557293 | Ratio of EC50 for HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID532454 | Antiviral activity against Human immunodeficiency virus 1 isolate 7 harboring Gag-capsid I138L, I147L, S173A, V215L, I223V, T242N, G248A, N252A, I126T, T280V and E312D mutant gene and protease K20R, M36I, R41K, M46I, L63Q, I64V, P79S, V82F and L90M mutant | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID521548 | Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID564037 | Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID321697 | Ratio of EC50 for HIV1 mutant strain 5 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID664437 | Inhibition of South African HIV1 subtype C protease expressed in Escherichia coli BL21S4 (DE3)pLysS cells using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease. |
AID519787 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-40D-70K-72R/K-91T/S protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID566847 | Antiviral activity against HIV-1 MDR/B infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID278971 | Antiviral activity against HIV1 C4 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID248600 | Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
AID328883 | Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 10 days 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. |
AID525281 | Antimicrobial activity against Plasmodium falciparum harboring HFP-tagged Pfs16 protein after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID726413 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID519572 | Antiviral activity against HIV1 P9 infected in human MT4 cells derived from viral passages with A-790742 harboring protease V82V/L and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infectio | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID343019 | Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID525484 | Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
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). |
AID278964 | Antiviral activity against HIV1 A12 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID343015 | Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID238043 | Binding affinity for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
AID369942 | Antiviral activity against HIV2 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID1409313 | Antiviral activity against darunavir-resistant HIV1 at passage 51 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID353764 | Cmax in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
AID374620 | Resistance index, ratio of EC50 for HIV1 with protease 32I/46I/47V/50L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID519790 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-61N-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID519556 | Antiviral activity against HIV1 isolate 13 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, K14R, L33F, E34Q, R41K, K45R, M46I, I50V, K55R, L63P, A71V, G73T, V77I, V82A, L90M, I93L mutation derived fr | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID374629 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54M/82L/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID525166 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID547237 | Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype CRF02_AG | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID353740 | AUC in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
AID537773 | Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant to EC50 for wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID572578 | Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID415249 | Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID557280 | Ratio of EC50 for HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID698061 | Selectivity index, ratio of Ki for HIV protease L10I mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Rational approaches to improving selectivity in drug design. |
AID557294 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID532464 | Antiviral activity against Human immunodeficiency virus 1 isolate 30 harboring Gag-capsid I138L, V215L, R286K and Q311A mutant gene and protease I13V, E35D, S37N and L63P mutant gene infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID541167 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1219737 | Maximum plasma concentration in healthy human at 400 mg | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID519548 | Antiviral activity against HIV1 isolate 5 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10F, I15V, M46I, L63P, A71V, I72L, V82T, I84V, I85V, L90M mutation derived from viral passages with Lopinavir asse | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID1482927 | Ratio of IC50 for tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID374611 | Resistance index, ratio of EC50 for HIV1 with protease 48V/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
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] | |||
AID519794 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 12Q-14R-17G/D-19P-61N-62I-92A protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID588982 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B3 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3 | Membrane transporters in drug development. |
AID564029 | Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID343016 | Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID374624 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1350495 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days in absence of human serum by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
AID328877 | Toxicity in human AG07095 cells assessed as accumulation of prelamin A at 20 uM after 10 days 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. |
AID375202 | Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID242866 | Dissociation rate constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID322116 | Antiviral activity against HIV1 MDR/B X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID343020 | Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID1409310 | Antiviral activity against amprenavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID586626 | Antiviral activity against HIV1 harboring mutant protease with matrix Y79F mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID279343 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and 184V mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID322096 | Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID321693 | Ratio of EC50 for HIV1 mutant strain 1 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID564061 | Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID321699 | Ratio of EC50 for HIV1 mutant strain 7 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID582283 | Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID321676 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID519542 | Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID278965 | Antiviral activity against HIV1 A13 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID257270 | Antiviral activity against HIV1 in the absence of human serum | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
AID104835 | Effective concentration against ritonavir -resistant strains in MT-4 cells. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Protease inhibitors: current status and future prospects. |
AID557218 | AUC (0 to 12 hrs) in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID322103 | Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID532461 | Antiviral activity against Human immunodeficiency virus 1 isolate 5 harboring Gag-capsid I138M, V159I, T280V and S310T mutant gene and protease I13V, D30N, L33I, E35D, M36I, S37N, M46I/L, I54V, I62V, L63P, I66M/I, A71N/T, I72T/I, V82L/V, N88D, L90M and I9 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID519781 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-17D-43T-68N/D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID726416 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID248546 | Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
AID1307691 | Binding affinity to HIV1 protease I47A mutant | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9 | OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands. |
AID1873200 | Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux preincubated with PhA followed by compound addition and measured after 60 mins by flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
AID1323586 | Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies. |
AID279342 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L90M mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID1482909 | Antiviral activity against lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID1725419 | Antiviral activity against LPV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID343014 | Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID372190 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/54V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID374607 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID415248 | Fold resistance, ratio of EC50 for HIV1 bearing protease gene with A17 mutation to EC50 for wild-type HIV1 pNL4-3 | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID1422660 | Inhibition of ZMPSTE24 in human HCT116 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID1593661 | Prodrug conversion in cannulated Sprague-Dawley rat plasma assessed as atazanavir formation at 3 mg/kg equiv of atazanavir administered orally by UPLC/MS/MS analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. |
AID374634 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1350502 | Inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
AID1219724 | Drug metabolism in human liver microsomes assessed as GSH-conjugated hydroxylated DMP adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID541168 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID586619 | Ratio of EC50 for HIV1 harboring mutant protease with matrix K76R mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID519791 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-33I-61N-71I-75M-84V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID375200 | Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 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. |
AID28092 | Cmax value in the period of 8 hr after dosing, when administered with ritonavir. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3 | Protease inhibitors: current status and future prospects. |
AID519541 | Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID278953 | Antiviral activity against HIV1 A1 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID372188 | Resistance index, ratio of EC50 for HIV1 with protease 46L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID372185 | Resistance index, ratio of EC50 for HIV1 with protease 46I/53L/82T/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID575062 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, V82A and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID537769 | Antiviral activity against Human immunodeficiency virus 1 clade B isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID572575 | AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID374605 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID375207 | Ratio of EC50 for multidrug-resistant HIV1 isolate G to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID279348 | Antiviral activity against HIV1 isolate 5512 with M36I/M and V82T mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID416860 | Increase in P-glycoprotein-mediated forward permeation of tenofovir disoproxil fumarate in human Caco-2 cells at 2 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID415250 | Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis in presence of ritonavir | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID541166 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID257273 | Antiviral activity against Lopinavir resistant HIV A17 mutant strain | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
AID278980 | Resistance to HIV1 with protease 46M, 54I and I84C mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID374615 | Resistance index, ratio of EC50 for HIV1 with protease 46I/47A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID328889 | Effect on Rap1A isoprenylation in mouse fibroblast cells at 20 uM after 24 hrs 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. |
AID321682 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID557292 | Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1717745 | Antiviral activity against HCoV-229E harboring GFP infected in human Huh-7 cells treated 1 hr prior to viral infection by fluorometric analysis | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID557284 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID566849 | Antiviral activity against HIV-1 MDR/G infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID328880 | Toxicity in ICMT deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs 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. |
AID278963 | Antiviral activity against HIV1 A11 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID446197 | Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID322114 | Antiviral activity against HIV1 MDR/MM R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID321691 | Antiviral activity against HIV1 mutant strain 6 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID658565 | Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3 | Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
AID372183 | Resistance index, ratio of EC50 for HIV1 with protease 37S/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1669454 | Inhibition of HIV1 NL4-3 protease expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET as | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
AID726415 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID1219736 | Drug metabolism in human liver microsomes assessed as CYP2D6-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID374600 | Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID372191 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID525290 | Antigametocyte activity against Plasmodium falciparum D10 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID668814 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID586623 | Antiviral activity against 8gpNS with amino acid 116 insertion removed HIV1 infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID369950 | Antiviral activity against HIV1 NL4-3 infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID553574 | Antiviral activity against HIV1 ERS104pre infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID278972 | Antiviral activity against HIV1 C5 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID557274 | Antiviral activity against HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID519576 | Antiviral activity against HIV1 clone1 infected in HEK293 cells harboring A-790742-selected protease I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID415246 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay in presence of 50% human serum | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID106958 | Compound was tested for antiviral activity against HIV-IIIB in MT-4 cells in presence of 50% human serum | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8 | Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
AID564043 | Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID322118 | Antiviral activity against HIV1 MDR/G X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID564046 | Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID564039 | Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1409309 | Antiviral activity against lopinavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID374633 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID668811 | Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID321686 | Antiviral activity against HIV1 mutant strain 1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID1474092 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells | 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. |
AID396259 | Antiviral activity against HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
AID537767 | Antiviral activity against wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID1678482 | Antiviral activity against SARS-CoV-2 infected in Vero E6 cells preincubated for 1 hr followed by viral infection at MOI of 0.02 and measured after 48 hrs by qRT-PCR method | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12 | Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2. |
AID374619 | Resistance index, ratio of EC50 for HIV1 with protease 30N/33F/46L/54L/84V/88D mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID257272 | Antiviral activity against indinavir resistant HIV IND-R mutant strain | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
AID278970 | Antiviral activity against HIV1 C3 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID519555 | Antiviral activity against HIV1 isolate 12 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20I, E35D, M36I, M46I, I50V, I54V, R57K, I62V, L63P, A71V, V82A, L89V, L90M, Q92K mutation derived fr | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID278979 | Resistance to HIV1 with protease 46M, 54I and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID443165 | Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2 | HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells. |
AID566848 | Antiviral activity against HIV-1 MDR/C infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID575059 | Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID278977 | Antiviral activity against HIV1 C10 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID625397 | Antimalarial activity against chloroquine resistant, mefloquine sensitive Plasmodium falciparum W2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11 | Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3. |
AID1065160 | Inhibition of Plasmodium falciparum DC6 plasmepsin-5 using DABCYL-GNKRTLAQKQG-EDANS as substrate measured every 15 mins of 75 mins by fluorescence assay | 2014 | ACS medicinal chemistry letters, Jan-09, Volume: 5, Issue:1 | Evaluation of aminohydantoins as a novel class of antimalarial agents. |
AID541133 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTY181C mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID582280 | Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID415282 | Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID557283 | Ratio of EC50 for HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID1380927 | Antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID532452 | Antiviral activity against Human immunodeficiency virus 1 isolate 22 harboring Gag-capsid V215L, H219Q, I223V, N252S, P255A, L268M and A340G mutant gene and Protease L19I, E35D, M36I, S37N, L63P, V77I and I93L mutant gene infected in human MT-2 cells by X | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID160461 | Inhibitory activity against HIV protease | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). |
AID442705 | Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
AID278960 | Antiviral activity against HIV1 A8 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID557237 | Ratio of drug level before intrapartum initiation to 30 days pre-last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID246193 | Protease inhibitory activity against HIV-1 r13025 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
AID1717747 | Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by the MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID557241 | Ratio of drug level in 4 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID698060 | Selectivity index, ratio of Ki for HIV protease G48V mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Rational approaches to improving selectivity in drug design. |
AID278968 | Antiviral activity against HIV1 C1 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID726412 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID532474 | Antiviral activity against Human immunodeficiency virus 1 isolate 35 harboring Gag-capsid V159I, I223T, N252S, A326S/A, A340G and G357S mutant gene and protease I15V, G16E, E35D, S37N, L63H and I72V mutant gene infected in human MT-2 cells by XTT-assay re | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID1669455 | Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 min | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
AID415247 | Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID564033 | Selectivity ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI infected human MT2 cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID396261 | Ratio of EC50 for HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient to EC50 for drug sensitive HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
AID1482922 | Ratio of IC50 for amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID532470 | Antiviral activity against Human immunodeficiency virus 1 isolate 10 harboring Gag-capsid I138L, I147L, V159I, V215L, G248A, I256V, T280V, R286K and N315H mutant gene and protease L10I, K20R, E35D, M36I, S37N, R41K, K45R, F53L, I54V, L63P, I64V, A71T, V82 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID374618 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID572573 | Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID353733 | Cmax in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9 | Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
AID575064 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID1422659 | Inhibition of ZMPSTE24 in human SW1990 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID525289 | Antigametocyte activity against Plasmodium falciparum D10 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID519551 | Antiviral activity against HIV1 isolate 8 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, L33F, E34Q, R41K, M46I, I54V, K55R, R57K, Q58E, I62V, L63P, A71V, I72I/T, G73S, V82A, I84V, L90M mutati | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
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 | |||
AID1725422 | Antiviral activity against HIV1 DRVR P30 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10 | Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
AID557229 | Drug level in HIV-infected Thai pregnant women serum before intrapartum initiation of 400 mg, po bid in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID249499 | Toxicity value against wild type HIV-1 IIIB was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID1482917 | Ratio of IC50 for darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID590915 | Inhibition of HIV1 subtype C protease expressed in Escherichia coli BL21 assessed as hydrolysis of substrate using chromogenic substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 by spectrophotometric analysis | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease. |
AID525167 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
AID525171 | Antimicrobial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mice (Mus musculus) assessed as potentiation of 2.5 mg/kg chloroquine-mediated antimalarial activity at 100 mg/kg, perorally administered after 72 hrs post inocu | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7 | Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
AID374635 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID586627 | Antiviral activity against HIV1 harboring mutant protease with matrix A81T mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3 | Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
AID321687 | Antiviral activity against HIV1 mutant strain 2 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID519574 | Antiviral activity against HIV1 P21 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L23I, L33F, K45I, A71A/V, V77I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infecti | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID322099 | Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID372189 | Resistance index, ratio of EC50 for HIV1 with protease 46I mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID564030 | Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID519537 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID557220 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
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] | |||
AID322121 | Antiviral activity against HIV1 BaL R5 subtype B in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID321689 | Antiviral activity against HIV1 mutant strain 4 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID242869 | Association rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID532459 | Antiviral activity against Human immunodeficiency virus 1 isolate 36 harboring Gag-capsid I138L, A146P, S165N/S, E207D, V215L and E312D mutant gene and protease K14R/K, I15V, E35D, S37D, R57K/R and L63P mutant gene infected in human MT-2 cells by XTT-assa | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID618427 | Cytotoxicity against human MT4 cells after 5 days by XTT assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach. |
AID374602 | Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/46I/54L/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID1474090 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 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. |
AID446203 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate TM to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID374616 | Resistance index, ratio of EC50 for HIV1 with protease 46I/88S mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID705597 | Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
AID1482912 | Antiviral activity against darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemil | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID278981 | Resistance to HIV1 with protease 46I, 54I and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID1422662 | Antimigratory activity against human KP4 cells at 10 uM after 10 days by crystal violet staining-based assay | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID547234 | Selectivity ratio of EC50 for HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype C | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID683727 | Antimalarial activity against liver stages of Plasmodium berghei 17XNL infected in human Hepa1-6 cells assessed as reduction in liver parasite load at 10 uM/L incubated for 1 hr prior to sporozoite inoculation measured after 46 to 48 hrs by fluorescence m | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | Targeting the liver stage of malaria parasites: a yet unmet goal. |
AID726417 | Cytotoxicity against human MT4 cells | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID622657 | Antiviral activity against HIV1 A17 harboring protease L10F, V32I, M46I, I47V, Q58E and I84V mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
AID321692 | Antiviral activity against HIV1 mutant strain 7 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
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. |
AID572576 | Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID519795 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 41D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID343024 | Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID541165 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID1482920 | Antiviral activity against indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID1219722 | Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID375206 | Ratio of EC50 for multidrug-resistant HIV1 isolate C to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID369838 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID582279 | AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID557291 | Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID519788 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-40D-43I-70K-82F-84V-85L-89V-90M-91T/L-98N/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID509270 | Inhibition of HIV1 protease assessed as substrate cleavage by cell free assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. |
AID532476 | Antiviral activity against Human immunodeficiency virus 1 isolate 23 harboring Gag-capsid I138L, V215L, E319D, A340G, G357S and V362I mutant gene and protease L10V, V11L, V32I, L33F, E34Q, E35D, M36L, S37T, M46I, I47V, G48V, I54M, I62V, L63P, I64V, I72V, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID321688 | Antiviral activity against HIV1 mutant strain 3 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID618426 | Inhibition of HIV1 subtype C protease Q7K mutant expressed in Escherichia coli BL21 (DE3) pLysS using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach. |
AID1474089 | Drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs | 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. |
AID1219723 | Drug metabolism in human liver microsomes assessed as GSH-conjugated trihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID374621 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID557285 | Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID519539 | Antiviral activity against wild-type HIV1 RF infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID1380928 | Resistance index, ratio of EC50 for antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID532656 | Antiviral activity against Human immunodeficiency virus 1 isolate 2 harboring Gag-capsid A146P, S173A, V215L, H219P, E230D, N252S, R264K, L268M and A340G mutant gene and protease L10I, I15V, K20R, M36I, S37N, M46I, L63P, T80A, V82A, N83H, I84V, I85T and L | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID248545 | Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15 | Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
AID553578 | Antiviral activity against HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID263208 | Antiviral activity against HIV1 EP13 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
AID537772 | Antiviral activity against multidrug resistant Human immunodeficiency virus 1 MDRC4 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
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. |
AID372187 | Resistance index, ratio of EC50 for HIV1 with protease 54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID278955 | Antiviral activity against HIV1 A3 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID726414 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID557300 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID564041 | Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID541135 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTG48V, V82A and L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID106953 | Antiviral activity against HIV in presence of 50% human serum in MT-4 cell was determined | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11 | Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). |
AID564060 | Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1409307 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID322106 | Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID566852 | Antiviral activity against HIV-1 MDR/JSL infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID1717811 | Toxicity in human infected with SARS-CoV2 assessed as adverse events at at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID321684 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID278962 | Antiviral activity against HIV1 A10 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID446194 | Antiviral activity against multidrug-resistant HIV1 isolate B infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID415283 | Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8 | 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
AID1717742 | Antiviral actvity against SARS-CoV2 infected in human assessed as improvement rate of chest at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days by computed tomography | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID1717743 | Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for HCoV-229E harboring GFP infected in human Huh-7 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID575061 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, and V82A mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11 | Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
AID572580 | AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
AID328890 | Inhibition of farnesyl transferase | 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. |
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. |
AID557288 | Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID541170 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID566846 | Antiviral activity against wild type HIV-1 ERS104 pre infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2 | Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
AID705596 | Inhibition of CYP3A4-mediated testosterone 6 beta hydroxylation in human liver microsome by Dixon plot analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11 | Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
AID374636 | Resistance index, ratio of EC50 for HIV1 with protease 48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID374608 | Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID375201 | Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID446199 | Antiviral activity against multidrug-resistant HIV1 isolate JSL infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
AID582281 | Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID321678 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID279339 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with V62A and L99F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID537765 | Inhibition of wild type HIV1 protease by FRET | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID564044 | Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1380924 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID582275 | Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID322123 | Antiviral activity against HIV1 92TH019 R5 subtype E in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID668812 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID622578 | Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20 | P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
AID1593667 | Prodrug conversion assessed as calf intestinal alkaline phosphatase-mediated compound dephosphorylation by measuring half life by UPLC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7 | Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID519540 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID257269 | Inhibitory activity against HIV1 protease at 0.5 uM | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24 | Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
AID239809 | Equilibrium dissociation constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID1482916 | Ratio of IC50 for darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID369955 | Ratio of EC50 for HIV2 ROD with protease G17N mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID558376 | Drug level in HIV-infected pregnant woman cord blood plasma at 400 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. |
AID343023 | Ratio of Ki for HIV1 recombinant protease M46I/A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID532468 | Antiviral activity against Human immunodeficiency virus 1 isolate 3 harboring Gag-capsid I138L, A146P, I147L, V159I, S176A, V215L, H219Q/H, T242N, G248A, T280V, A340G and G357S mutant gene and protease L10I, T31S/T, V32I, M36I/M, S37C, R41K, M46I, F53L, I | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID537770 | Antiviral activity against Human immunodeficiency virus 1 clade C isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21 | Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
AID541174 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V, G140S and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID525485 | Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID519547 | Antiviral activity against HIV1 isolate 4 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease N37T, M46I, Q58E, I64V, T74K, V77I, V82F, L90M mutation derived from viral passages with Lopinavir assessed as redu | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID1380925 | Antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
AID374606 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID322104 | Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID532472 | Antiviral activity against Human immunodeficiency virus 1 isolate 33 harboring Gag-capsid I138L, V215L, V218P, H219Q, I223V, M228I, G248T, N252S, N253T, I256M, E312D and A326S mutant gene and protease T12S/T, I13V/I, I15V, L19I, S37T, L63V/A/P/L and I72V/ | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID557233 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID557281 | Ratio of EC50 for HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID278957 | Antiviral activity against HIV1 A5 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID369961 | Ratio of EC50 for HIV2 MS infected in human MT4 cells after 1 passage to EC50 for HIV2 MS infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID328879 | Toxicity in RCE1 deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs 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. |
AID369945 | Ratio of EC50 for HIV2 CBL-23 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID417047 | Inhibition of esterase mediated-hydrolysis of tenofovir disoproxil fumarate in human intestinal sub cellular fraction S9 at 2 uM after 30 mins | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID274382 | Inhibition of HIV1 protease L10I/L63P/A71V/G73S/I84V/L90M mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25 | Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
AID321683 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID541169 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID557296 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID374632 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/73C/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID278983 | Resistance to HIV1 with protease 46I/L, 54I and I84C mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID322113 | Antiviral activity against HIV1 MDR/TM X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID442714 | Fold resistance, ratio of EC50 for indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells to EC50 for HIV1 pNL4-3 infected in human MT4 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
AID1482924 | Ratio of IC50 for indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID375203 | Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13 | Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID557222 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 12 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID698062 | Binding affinity to wild type HIV1 protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4 | Rational approaches to improving selectivity in drug design. |
AID322107 | Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID374614 | Resistance index, ratio of EC50 for non-B type HIV1 with protease 46I/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID532477 | Antiviral activity against Human immunodeficiency virus 1 isolate 24 harboring Gag-capsid I138L, V159I, V215L, I223A, T239S, N252S, T280V, R286K, S310T and V362I mutant gene and protease L10V, I13V, I15V, K20R, D30N, V32I, L33F, E35D, M36I, S37N, K43T, M4 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID263207 | Antiviral activity against HIV1 HXB2 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
AID1409311 | Antiviral activity against darunavir-resistant HIV1 at passage 21 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21 | Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
AID374594 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID557217 | Cmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID726419 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID242932 | Dissociation rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10 | Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
AID369948 | Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID541129 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTK65R mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID541161 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring T66I mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID328895 | Effect on change in ZMPSTE24 protein level in mouse fibroblasts at 20 uM after 10 days 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. |
AID1219725 | Drug metabolism in human liver microsomes assessed as lopinavir semicarbazide adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
AID582274 | AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID519644 | Antiviral activity against HIV1 isolate 6 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, L24I, M46I, I54V, K55R, Q58E, L63P, I64V, A71V, V82A, T91A mutation derived from viral passages with Lopinavi | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID278978 | Antiviral activity against HIV1 C11 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID1482911 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID246965 | Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
AID553570 | Cytotoxicity against human MT2 cells by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID541171 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M and E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID321661 | Antiviral activity against HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3 | Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
AID1307690 | Binding affinity to HIV1 protease | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9 | OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID279337 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182L mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
AID322120 | Antiviral activity against HIV1 92UG037 subtype A R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID322109 | Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID557289 | Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID369949 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9 | In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
AID263209 | Antiviral activity against HIV D545701 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7 | Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
AID564036 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID582277 | Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir measured 12 hrs after last dose | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9 | Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
AID1482907 | Ratio of IC50 for saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10 | Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
AID374617 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/88S/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID374637 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID246225 | Protease inhibitory activity against HIV-1 GSS004421 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
AID525486 | Antigametocyte activity against drug-resistant ring stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID726418 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1 | Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
AID372192 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID278954 | Antiviral activity against HIV1 A2 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2 | Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
AID343021 | Inhibition of HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15 | Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
AID239819 | Association rate constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24 | Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
AID519543 | Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID416867 | Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated HIV infected patient assessed as change in plasma AUC of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID532456 | Antiviral activity against Human immunodeficiency virus 1 isolate 21 harboring Gag-capsid I138L, A146P, I147L/I, V159I/V, E211D, V215L, N252H/N, R286K/R and K331R/K mutant gene and protease E35D, M36I, S37N, I62V and L63C mutant gene infected in human MT- | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID532658 | Antiviral activity against Human immunodeficiency virus 1 isolate 29 harboring Gag-capsid I138M, A146P, R286K, T303V and A326S mutant gene and protease L10F, I13V, V32I, M36L, S37N, L38W, P39Q, M46I, I47V, I50V, I62V, L63P, A71I, I72V and V82A mutant gene | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6 | Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
AID541162 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID564045 | Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
AID557219 | Tmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5 | Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
AID588981 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B1 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3 | Membrane transporters in drug development. |
AID322108 | Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
AID246195 | Protease inhibitory activity against HIV-1 r13363 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
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] | |||
AID1474088 | AUC in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs | 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. |
AID553575 | Antiviral activity against HIV1 MOKW infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID668813 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6 | Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
AID553568 | Selectivity index, ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID541134 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTI84V, L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID564062 | Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID1350504 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12 | Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
AID525280 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3 | Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
AID1717744 | Cytotoxicity against human Huh-7 cells incubated for 1 hr by MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
AID374631 | Resistance index, ratio of EC50 for HIV1 with protease 46I/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11 | In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
AID246160 | Protease inhibitory activity against wild type HIV-1 IIIB was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6 | Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
AID1422657 | Inhibition of ZMPSTE24 in human HPAF2 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20 | Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
AID547240 | Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype CRF02_AG | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID519578 | Antiviral activity against HIV1 clone3 infected in HEK293 cells harboring A-790742-selected protease L33F, K45I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4 | Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
AID546999 | Antiviral activity against HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gen | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7 | HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
AID416857 | Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
AID557275 | Antiviral activity against HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3 | GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
AID328876 | Toxicity in human AG08470 cells assessed as accumulation of prelamin A at 20 uM after 10 days 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. |
AID564047 | Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8 | Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
AID322119 | Antiviral activity against HIV1 92UG029 X4 subtype A in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6 | A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
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. |
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. |
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. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
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. |
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. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1508628 | Confirmatory 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. |
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. |
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. |
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. |
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. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
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. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | Biochemical and biophysical research communications, Jul-26, Volume: 437, Issue:2 | Crystallographic study of multi-drug resistant HIV-1 protease lopinavir complex: mechanism of drug recognition and resistance. |
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. |
AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1 | The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7 | Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
AID1805801 | Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\ | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23 | Perspectives on SARS-CoV-2 Main Protease Inhibitors. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2002 | Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8 | X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2002 | Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8 | X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18 | Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2007 | Journal of virology, May, Volume: 81, Issue:10 | Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2007 | Journal of virology, May, Volume: 81, Issue:10 | Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2008 | Protein science : a publication of the Protein Society, Sep, Volume: 17, Issue:9 | Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir. |
[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 | 19 (0.84) | 18.2507 |
2000's | 771 (34.08) | 29.6817 |
2010's | 840 (37.14) | 24.3611 |
2020's | 632 (27.94) | 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 (59.80) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 499 (20.94%) | 5.53% |
Reviews | 213 (8.94%) | 6.00% |
Case Studies | 198 (8.31%) | 4.05% |
Observational | 62 (2.60%) | 0.25% |
Other | 1,411 (59.21%) | 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 | ||
---|---|---|---|---|---|---|---|
Pharmacokinetics of Pediatric Aluvia® (Lopinavir /Ritonavir 100/25 mg) and Generic Lopinavir/Ritonavir Tablet Formulation (200/50 mg) in Clinically and Virologically Stable HIV-1 Infected Thai Adults [NCT01159275] | Phase 1/Phase 2 | 20 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Pharmacokinetic Interactions Between an Herbal Medicine (African Potato) and Antiretroviral Agents (Lopinavir/Ritonavir) [NCT01227590] | Phase 1 | 18 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
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 | ||
Maternal Tenofovir-containing Combination Drug Regimen During the Second and Third Trimesters of Pregnancy for Prevention of Mother-to-child Transmission of HIV and HBV in HIV-HBV Co-infected Mothers [NCT01125696] | Phase 2 | 45 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
The Influence of Ritonavir, Alone and in Combination With Lopinavir, on Fenofibric Acid Pharmacokinetics in Healthy Volunteers [NCT01148004] | Phase 1 | 25 participants (Actual) | Interventional | 2010-05-13 | 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 | ||
A Multicenter Phase III Trial of Second-line Antiretroviral Treatment Strategies in African Adults (Tanzania Ans South Africa) Using Atazanavir or Lopinavir/Ritonavir [NCT01255371] | Phase 3 | 0 participants (Actual) | Interventional | 2012-03-31 | Withdrawn(stopped due to drug procurement issues) | ||
A Randomized Controlled Study Compares the 48 Weeks Results of HIV-1 RNA Between Ritonavir-boosted Lopinavir Monotherapy and Ritonavir-boosted Lopinavir + Optimized Background Regimens in HIV-1 Infected Patients Who Have HIV-1 RNA <50 Copies/ml More Than [NCT01189695] | Phase 4 | 63 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
Comparative LUSZ Therapeutic Study of Antiviral, Antiretroviral, and Immunosuppressive Treatments in Hospitalized COVID-19 Patients With High-Risk Factors, Biomarkers, and Disease Progression. [NCT05925140] | Phase 1 | 1,000 participants (Anticipated) | Interventional | 2020-03-28 | Recruiting | ||
Randomised Evaluation of COVID-19 Therapy [NCT04381936] | Phase 2/Phase 3 | 50,000 participants (Anticipated) | Interventional | 2020-03-19 | Recruiting | ||
The Effect of Kaletra on CD4 Immune Reconstitution in HIV-infected Patients With Long-term Virologic Suppression on a Non-Kaletra Containing ART Regimen, But With a Blunted Immune Response [NCT00344487] | 3 participants (Actual) | Interventional | 2005-12-31 | Terminated(stopped due to Inability to enroll subjects.) | |||
Randomized Trial of a Switch to a Kaletra + Current Dual Nucleoside Reverse Transcriptase Inhibitor (NRTI) Backbone Versus Continuation of the Current Regimen in Patients With Poor Immune Responses to Highly Active Antiretroviral Therapy (HAART) in Patien [NCT00145795] | Phase 4 | 20 participants (Actual) | Interventional | 2004-04-30 | 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 | |||
Metabolic Effects of Switching Kaletra to Boosted Reyataz [NCT00413153] | 15 participants (Actual) | Interventional | 2006-05-31 | 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 | ||
Use of an Aluvia Based Highly Active Antiretroviral Therapy (HAART) Regimen in the Prevention of Mother to Child HIV Transmission (PMTCT) Antepartum, Intrapartum and Postpartum in Africa [NCT01088516] | Phase 4 | 280 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
An Evaluation of the Uptake and Safety of, and Adherence to Antiretroviral Treatment Among Individuals With CD4 ≥ 250 Cells/mm3 and HIV Virus Load ≥ 50,000 cp/mL [NCT01583439] | 11 participants (Actual) | Interventional | 2012-09-30 | Terminated(stopped due to Low Accrual.) | |||
Changes in Insulin Resistance in Healthy Volunteers on STRIBILD® Medication - A Controlled, Mono Center, Three-arm, Randomized Phase I Study. [NCT02203461] | Phase 1 | 30 participants (Actual) | Interventional | 2014-07-31 | 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 | ||
Multicenter Study of Options for Second-Line Effective Combination Therapy (SELECT) [NCT01352715] | Phase 3 | 515 participants (Actual) | Interventional | 2012-03-13 | Completed | ||
Combination Therapies to Reduce the Nasopharyngeal Carriage of SARS-CoV-2 and Improve the Outcome of COVID-19 Infection in Ivory Coast (INTENSE-COV): a Phase IIb Randomized Clinical Trial [NCT04466241] | Phase 2/Phase 3 | 294 participants (Anticipated) | Interventional | 2020-11-27 | Recruiting | ||
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 | ||
Efficacy and Safety of Darunavir/Cobicistat vs. Lopinavir/Ritonavir in the Management of Patients With COVID-19 Pneumonia in Qatar [NCT04425382] | 400 participants (Actual) | Observational | 2020-03-01 | Completed | |||
Multi-centre, Adaptive, Randomized Trial of the Safety and Efficacy of Treatments of COVID-19 in Hospitalized Adults [NCT04315948] | Phase 3 | 1,552 participants (Actual) | Interventional | 2020-03-22 | Completed | ||
HIV Infection and Gut Mucosal Immune Function: Longitudinal Analyses of Intestinal CD4+ and Th17 T Cells in HIV-infected Individuals on Short-term Antiretroviral Therapy [NCT02097381] | 10 participants (Actual) | Interventional | 2010-04-30 | Active, not recruiting | |||
Implementation and Evaluation of an HIV-2 Viral Load and ARV Resistance Informed Algorithm for 2nd-line ART in HIV-2 Infected Patients in the Initiative Sénégalaise d'Accès Aux Antirétroviraux (ISAARV) Program [NCT03394196] | 152 participants (Actual) | Interventional | 2018-07-04 | Terminated(stopped due to COVID-19 and Funding) | |||
A Phase 3, Randomized, Open Label, Controlled Study of Lopinavir/Ritonavir and Lamivudine Versus Standard Therapy in Naïve HIV-1 Infected Subjects. [NCT01237444] | Phase 3 | 417 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
The SETPOINT Study - A Randomized Study of the Effect of Immediate Treatment With Potent Antiretroviral Therapy Versus Observation With Treatment as Indicated in Newly Infected HIV-1 Infected Subjects: Does Early Therapy After the Virologic Setpoint? [NCT00090779] | Phase 2 | 130 participants (Actual) | Interventional | 2005-01-31 | Terminated(stopped due to The DSMB concluded that the findings regarding the primary analysis would persist and that no additional study goals would be achieved by continuing the study.) | ||
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289] | 1,578 participants (Actual) | Observational | 2003-06-09 | Completed | |||
Exploratory, Cross-sectional Study to Compare the Virologic Efficacy in Cerebrospinal Fluid (CSF) and Neurocognitive State in Patients Infected by HIV-1 Long-term Treatment (> 3 Years) With Lopinavir / Ritonavir Monotherapy [NCT01116817] | Phase 4 | 35 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
Pharmacokinetics of Low- Dose Lopinavir/Ritonavir Tablet Formulation HIV-1 Infected Children [NCT01139905] | Phase 2 | 24 participants (Actual) | Interventional | 2010-04-30 | Completed | ||
A Phase IIa Randomized, Controlled Study of Combination Therapies to Treat COVID-19 Infection [NCT04459702] | Phase 2 | 0 participants (Actual) | Interventional | 2020-07-31 | Withdrawn(stopped due to Was never started) | ||
COVID-19 Ring-based Prevention Trial With Lopinavir/Ritonavir [NCT04321174] | Phase 3 | 123 participants (Actual) | Interventional | 2020-04-17 | Active, not recruiting | ||
A Randomized Prospective Open Label Study of Switching to Raltegravir Based ART Compared to Maintaining Ritonavir Boosted PI-based ART on Liver Fibrosis Progression in HIV-HCV Coinfected Patients [NCT01231685] | Phase 2 | 9 participants (Actual) | Interventional | 2011-12-31 | Completed | ||
A Double-Blind, Randomized, Placebo-Controlled Phase II Study of Lopinavir/Ritonavir Versus Placebo in COVID-19 Positive Patients With Cancer and Immune Suppression in the Last Year [NCT04455958] | Phase 2 | 0 participants (Actual) | Interventional | 2021-05-01 | Withdrawn(stopped due to limited resources) | ||
Ensayo clínico, Abierto, Aleatorizado Para Comparar la Calidad de Vida de Los Pacientes VIH+ Que Inician Monoterapia Con Comprimidos de LPV/r vs Triple Terapia Que Contenga un IP Potenciado [NCT01166477] | Phase 4 | 228 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
the Investigation Into Beneficial Effects of High-dose Interferon Beta 1-a, Compared to Low-dose Interferon Beta 1-a in Moderate to Severe Covid-19 [NCT04521400] | Phase 2 | 100 participants (Anticipated) | Interventional | 2020-08-20 | Not yet recruiting | ||
Phase II Trial of Ritonavir/Lopinavir in Patients With Progressive of Recurrent High-Grade Gliomas [NCT01095094] | Phase 2 | 19 participants (Actual) | Interventional | 2009-01-31 | Terminated(stopped due to Study did not meet its primary objective) | ||
Multicenter Clinical Study on the Efficacy and Safety of Xiyanping Injection in the Treatment of New Coronavirus Infection Pneumonia (General and Severe) [NCT04295551] | 80 participants (Anticipated) | Interventional | 2020-03-14 | Not yet recruiting | |||
Protease Inhibitors to Reduce Malaria Morbidity in HIV-Infected Pregnant Women [NCT00993031] | Phase 3 | 389 participants (Actual) | Interventional | 2009-12-15 | Completed | ||
Atazanavir (BMS-232632) for HIV Infected Individuals Completing Atazanavir Clinical Trials: An Extended Access Study [NCT01003990] | Phase 3 | 710 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Randomised Controlled Trial Comparing the Efficacy of Infant Peri-exposure Prophylaxis With Lopinavir/Ritonavir (LPV/r) Versus Lamivudine to Prevent HIV-1 Transmission by Breastfeeding [NCT00640263] | Phase 3 | 1,500 participants (Anticipated) | Interventional | 2009-12-31 | 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 Randomised, Open Label Switch Study Comparing Darunavir/Ritonavir 400mg/100mg Daily With Lopinavir/Ritonavir 800mg/200mg Daily, in HIV-positive Participants [NCT02671383] | Phase 3 | 300 participants (Actual) | Interventional | 2016-06-30 | Completed | ||
Phase IV, Non Randomized Study in ARV Experienced Patients Under Switch Therapy With Kaletra [NCT00648999] | Phase 4 | 207 participants (Actual) | Interventional | 2003-11-30 | Completed | ||
A Pilot Study Of the Effects of Highly Active Antiretroviral Therapy on Kaposi's Sarcoma in Zimbabwe [NCT00834457] | Phase 2/Phase 3 | 49 participants (Actual) | Interventional | 2007-06-30 | Completed | ||
A Randomized, Open-label Trial to Compare the Efficacy and Safety of Early Initiation of cART With or Without Autologous HIV-1 Specific Cytotoxic T Lymphocyte (CTL) Infusion in Treatment-Naïve Acute HIV-1 Infected Adults [NCT02231281] | Phase 3 | 65 participants (Anticipated) | Interventional | 2014-08-31 | Active, not recruiting | ||
A Randomized, Non-comparative, Phase IIb, Unblinded Trial, Evaluating the Efficacy and Safety of Tenofovir-emtricitabine or Lamivudine Plus Zidovudine, Lopinavir/Ritonavir, or Raltegravir, Among ARV-naïve HIV-2 Infected Adult Patients, in West Africa [NCT02150993] | Phase 2/Phase 3 | 210 participants (Actual) | Interventional | 2016-01-26 | Completed | ||
Trial of Early Therapies During Non-hospitalized Outpatient Window (TREAT NOW) for COVID-19 [NCT04372628] | Phase 2 | 452 participants (Actual) | Interventional | 2020-06-01 | Completed | ||
Evaluation of the Capacity of a Weekly Strategy of 4 Consecutive Days on Treatment Followed by 3 Days Off Treatment, in HIV-1 Infected Patients With Undetectable Viral Load for at Least 12 Months, to Maintain a Virological Success With This Intermittent M [NCT02157311] | Phase 3 | 100 participants (Actual) | Interventional | 2014-07-31 | Completed | ||
Lopinavir/Ritonavir as an Immunomodulator to Enhance Vaccine Responsiveness [NCT01165645] | 0 participants (Actual) | Interventional | 2010-11-30 | Withdrawn(stopped due to no patients enrolled) | |||
An Adaptive, Multicenter, Randomized, Open-label, Comparative Clinical Study to Assess Efficacy and Safety of Favipiravir in Hospitalized Patients With COVID-19 [NCT04434248] | Phase 2/Phase 3 | 330 participants (Actual) | Interventional | 2020-04-23 | Active, not recruiting | ||
A 48-week, Randomized, Open-label, 2-arm Study to Compare the Efficacy of Saquinavir/Ritonavir Twice Daily (BID) Plus Emtricitabine/Tenofovir Once Daily (QD) Versus Lopinavir/Ritonavir BID Plus Emtricitabine/Tenofovir QD in Treatment-naïve Human Immunodef [NCT00105079] | Phase 3 | 337 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
ProSpective, MultI-Center, Observational PrograM to Assess the Effectiveness of Dual TheraPy (Lopinavir/Ritonavir + LamivudinE) in Treatment-Experienced HIV Infected Patients in the Routine Clinical Settings of the Russian Federation (SIMPLE) [NCT02581202] | 216 participants (Actual) | Observational | 2015-12-21 | Completed | |||
Prophylaxis for HIV-1: Tenofovir/Emtricitabine (Truvada ®) + Lopinavir/Ritonavir (Kaletra ®) vs Tenofovir/Emtricitabine/Cobicistat/Elvitegravir (Stribild ®). Prospective, Randomized, Open. [NCT02198443] | Phase 4 | 160 participants (Actual) | Interventional | 2015-06-06 | Completed | ||
A Pilot Study to Assess the Safety, Efficacy, and PK Profile of a Switch in Antiretroviral Therapy to a RTI Sparing Combination of LPV/r and RAL in Virologically Suppressed HIV-infected Patients [NCT00700115] | Phase 4 | 60 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
Pilot Assessment of Lopinavir/Ritonavir and Maraviroc in Experienced Patients [NCT00981318] | Phase 4 | 3 participants (Actual) | Interventional | 2009-12-31 | Terminated(stopped due to unable to enroll expected number of subjects) | ||
IMPAACT P1058A: Intensive Pharmacokinetic Studies of New Classes of Antiretroviral Drug Combinations in Children, Adolescents and Young Adults [NCT00977756] | 168 participants (Actual) | Observational | 2002-08-31 | Completed | |||
A Phase I, Open-label, Randomized Cross-over, 2-period, 2-way Interaction Trial to Investigate the Pharmacokinetic Interaction Between Lopinavir/Ritonavir and TMC125 Both at Steady-state in Healthy Subjects. [NCT00767117] | Phase 1 | 16 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
A 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 Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Antiretroviral Activity of MK0518 Versus KALETRA in HIV-Infected Patients Switched From a Stable KALETRA-Based Regimen - Study A [NCT00443703] | Phase 3 | 352 participants (Actual) | Interventional | 2007-05-31 | Terminated(stopped due to primary efficacy analysis at Week 24 did not demonstrate non-inferiority of raltegravir versus lopinavir (+) ritonavir) | ||
Randomised and Prospective Clinical Study to Evaluate the Efficacy and Safety of Lopinavir/Ritonavir Monotherapy Versus Darunavir/Ritonavir Monotherapies as Simplification Switching Strategies of PI/NNRTI-Triple Therapy Based-Regimens [NCT00994344] | Phase 4 | 73 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia [NCT02735707] | Phase 3 | 10,000 participants (Anticipated) | Interventional | 2016-04-11 | Recruiting | ||
Phase III Open Label Atazanavir (BMS-232632) in Combination With Ritonavir or Saquinavir, and Lopinavir/Ritonavir, Each With Tenofovir and a Nucleoside in Subjects With HIV [NCT00035932] | Phase 3 | 571 participants (Actual) | Interventional | 2001-11-30 | Completed | ||
A Multicenter, Double-Blind, Randomized, Active-Controlled Study to Evaluate the Safety and Antiretroviral Activity of MK0518 Versus KALETRA in HIV-Infected Patients Switched From a Stable KALETRA-Based Regimen - Study B [NCT00443729] | Phase 3 | 355 participants (Actual) | Interventional | 2007-05-31 | Terminated(stopped due to Primary efficacy analysis at Week 24 did not demonstrate non-inferiority of raltegravir versus lopinavir (+) ritonavir) | ||
International Trial of Modified Directly Observed Therapy Versus Self-Administered Therapy for Participants With First Virologic Failure on a Non-Nucleoside Reverse Transcriptase Inhibitor-Containing Antiretroviral Regimen [NCT00608569] | 529 participants (Actual) | Interventional | 2009-03-31 | Completed | |||
A Randomized, Open-label, Multi-centre Clinical Trial Evaluating and Comparing the Safety and Efficiency of ASC09/Ritonavir and Lopinavir/Ritonavir for Confirmed Cases of Pneumonia Caused by Novel Coronavirus Infection [NCT04261907] | 6 participants (Actual) | Interventional | 2020-02-11 | Terminated(stopped due to There were no more subjects enrolled.) | |||
A Randomised Open-label Study Comparing the Safety and Efficacy of Ritonavir Boosted Lopinavir and 2-3N(t)RTI Backbone Versus Ritonavir Boosted Lopinavir and Raltegravir in Participants Virologically Failing First-line NNRTI/2N(t)RTI Therapy [NCT00931463] | Phase 4 | 558 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
Multicentric, Non-inferiority, Randomized, Non-blinded Phase 3 Trial Comparing Virological Response at 48 Weeks of 3 Antiretroviral Treatment Regimens in HIV-1-infected Patients With Treatment Failure After 1st Line Antiretroviral Therapy (Cameroon, Burki [NCT00928187] | Phase 3 | 454 participants (Actual) | Interventional | 2009-11-30 | Completed | ||
An International Randomized Trial of Additional Treatments for COVID-19 in Hospitalized Patients Who Are All Receiving the Local Standard of Care Philippines [NCT05024006] | 1,314 participants (Actual) | Interventional | 2020-04-23 | Completed | |||
A Prospective Longitudinal Pilot Study to Measure the Effect of Intensification With Raltegravir +/- a Protease Inhibitor (PI) or Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) on HIV-1 Levels in the Gut [NCT00884793] | 8 participants (Actual) | Interventional | 2008-09-30 | Completed | |||
Lumefantrine Pharmacokinetics When Administered as a Fixed Dose Combination With Artemether in HIV Positive Patients on Lopinavir/Ritonavir [NCT00619944] | Phase 4 | 32 participants (Anticipated) | Interventional | 2008-02-29 | Completed | ||
Pharmacokinetics of Rifabutin Combined With Antiretroviral Therapy in the Treatment of Tuberculosis Patient With HIV Infection in Vietnam : A Phase II Trial [NCT00651066] | Phase 2 | 47 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
A Randomised Controlled Trial to Evaluate Options for Second-line Therapy in Patients Failing a First-line 2NRTI + NNRTI Regimen in Africa [NCT00988039] | Phase 3 | 1,277 participants (Actual) | Interventional | 2010-03-31 | 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 | ||
A Multicenter, Randomized, Open Label, Pilot Study to Assess the Possibility of Concomitant Treatment of HCV/HIV co Infection With Peg-interferon + Ribavirin, and Lopinavir/r as a Single Antiretroviral Agent. [NCT00866021] | Phase 4 | 68 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
A Phase IV-III Comparative, Randomized, Open-label Study to Evaluate the Efficacy for the Recovery of Peripheral Fat (or of the Extremities) of Lopinavir/Ritonavir in Monotherapy Versus Abacavir/Lamivudine and Lopinavir/Ritonavir [NCT00865007] | Phase 4 | 88 participants (Actual) | Interventional | 2008-12-31 | Completed | ||
Effects of Traditional Chinese Medicines (TCMs) on Patients With COVID-19 Infection: A Perspective, Open-labeled, Randomized, Controlled Trial [NCT04251871] | 150 participants (Anticipated) | Interventional | 2020-01-22 | Recruiting | |||
Pharmacokinetics, Pharmacodynamics, and Safety Profile of Understudied Drugs [NCT04278404] | 5,000 participants (Anticipated) | Observational | 2020-03-05 | Recruiting | |||
A Study Comparing Efficacy and Tolerance of Two Maintenance Strategies : a Monotherapy With Lopinavir/Ritonavir or a Single-tablet Triple Therapy by Efavirenz/Emtricitabin/Tenofovir in HIV-1 Infected Patients With HIV RNA Below 50 cp/mL [NCT00946595] | Phase 2/Phase 3 | 420 participants (Anticipated) | Interventional | 2009-11-30 | Completed | ||
A Phase 3, Randomized, Open-Label Study of Lopinavir/Ritonavir (LPV/r) Tablets 800/200 Milligram (mg) Once-Daily (QD) Versus 400/100 mg Twice-Daily (BID) When Coadministered With Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) in Antiretrov [NCT00358917] | Phase 3 | 599 participants (Actual) | Interventional | 2006-08-31 | Completed | ||
A Comparison of the Bioavailability of Rifabutin With and Without Lopinavir/Ritonavir in Healthy Adult Subjects [NCT00743470] | Phase 1 | 15 participants (Actual) | Interventional | 2008-08-31 | Terminated | ||
Pharmacokinetics and Pharmacodynamics of Lopinavir an Anti-HIV Drug in Israeli Ethiopian and Non-Ethiopian Populations [NCT00347750] | 0 participants (Actual) | Observational | 2006-09-30 | Withdrawn(stopped due to lack of participants) | |||
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combinations, Artesunate/Amodiaquine and Artemether/Lumefantrine. [NCT00697892] | Phase 1 | 38 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
Nucleoside-Sparing Combination Therapy With Lopinavir/Ritonavir (LPV/r) + Raltegravir (RAL) vs. Efavirenz (EFV) + Tenofovir Disoproxil Fumarate + Emtricitabine (TDF/FTC) in Antiretroviral-Naïve Patients [NCT00752856] | Phase 2 | 51 participants (Actual) | Interventional | 2008-08-26 | Completed | ||
Pilot Study Of Novel Combination Of Maraviroc + Atazanavir/Ritonavir vs. Atazanavir/Ritonavir + Emtricitabine/Tenofovir For The Treatment Of Naïve HIV-Infected Patients With R5 HIV-1 [NCT00827112] | Phase 2 | 129 participants (Actual) | Interventional | 2009-03-31 | 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) | ||
The Pharmacokinetics of Two Generic Co-formulations of Lopinavir/Ritonavir for HIV Infected Children: a Pilot Study of Lopimune vs. the Branded Product (SURF Study). [NCT00665951] | Phase 1 | 12 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
Pharmacokinetics of Efavirenz and Lopinavir Nano-formulations in HIV Negative Healthy Volunteers: an Adaptive Design Study [NCT02631473] | Phase 1 | 50 participants (Anticipated) | Interventional | 2015-11-30 | Suspended(stopped due to Study is on hold whilst a grant application for further funding is put together) | ||
Effects of 2 Initial Standard Antiretroviral Combinations Therapies on Lipid Metabolism in ARV-naive HIV-infected Subjects [NCT00759070] | Phase 4 | 50 participants (Anticipated) | Interventional | 2008-09-30 | Active, not recruiting | ||
Pharmacokinetics of Lopinavir Crushed Versus Whole Tablets in Pediatric Patients [NCT00810108] | Phase 4 | 12 participants (Actual) | Interventional | 2006-06-30 | Completed | ||
A Phase I Study to Evaluate the Effect of Darunavir/Ritonavir and Lopinavir/Ritonavir on GSK2248761 Pharmacokinetics and to Assess the Effect of GSK2248761 on CYP450 Probe Drugs in Healthy Adult Subjects [NCT00920088] | Phase 1 | 24 participants (Actual) | Interventional | 2009-06-30 | Completed | ||
A Randomized, Open-label Study of Lopinavir/Ritonavir 400/100 mg Tablet Twice Daily + Co-formulated Emtricitabine/Tenofovir Disoproxil Fumarate 200/300 mg Once Daily Versus Lopinavir/Ritonavir 400/100 mg Tablet Twice Daily + Raltegravir 400 mg Twice Daily [NCT00711009] | Phase 3 | 206 participants (Actual) | Interventional | 2008-07-31 | Completed | ||
Safety and Efficacy of Lopinavir/Ritonavir in Combination With Raltegravir in HIV-infected Patients [NCT00752037] | Phase 4 | 30 participants (Actual) | Interventional | 2008-09-30 | Completed | ||
Adjusting Antiretroviral Therapy Dosage Using Therapeutic Drug Monitoring [NCT00836212] | Phase 4 | 12 participants (Anticipated) | Interventional | 2008-03-31 | Recruiting | ||
CID 0708 - Sex, Aging and Antiretroviral Pharmacokinetics [NCT00666055] | 11 participants (Actual) | Observational | 2008-03-31 | Completed | |||
Randomized Controlled Clinical Trials of Lopinavir/Ritonavir or Hydroxychloroquine in Patients With Mild Coronavirus Disease (COVID-19) [NCT04307693] | Phase 2 | 65 participants (Actual) | Interventional | 2020-03-11 | Terminated(stopped due to Terminated early because no patients were further enrolled since mid-Apr 2020.) | ||
An Open, Prospective/Retrospective, Randomized Controlled Cohort Study to Compare the Efficacy of Three Antiviral Drugs(Abidol Hydrochloride, Oseltamivir and Lopinavir/Ritonavir) in the Treatment of 2019-nCoV Pneumonia. [NCT04255017] | Phase 4 | 400 participants (Anticipated) | Interventional | 2020-02-01 | Recruiting | ||
Kaletra and Maraviroc in Antiretroviral Therapy-Naïve Patients - KALMAR Study -Version 1.0 Amendment 2 [NCT01068873] | Phase 4 | 1 participants (Actual) | Interventional | 2010-04-30 | Terminated(stopped due to Poor enrollment) | ||
Phase 3, Single Center, Controlled, Investigator-blinded, Randomized Matched Pair Design Study of CD4 Cell Recovery in HIV-1 Patients With Sustained Virologic Response Comparing Protease Inhibitor and Non-nucleoside Reverse Transcriptase Inhibitor Based T [NCT00966160] | Phase 3 | 215 participants (Actual) | Interventional | 1999-01-31 | Completed | ||
The Effect of Pregnancy on the Pharmacokinetics of the Kaletra Tablet: A Longitudinal Investigation in the Second and Third Trimesters Including Empiric Dosage Adjustment [NCT00766818] | Phase 1 | 12 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
A Phase I, Open Label, Randomized, Three Period, One-way, Two Cohort, Adaptive Crossover Study to Evaluate the Effect of Darunavir/Ritonavir Plus Etravirine and Lopinavir/Ritonavir Plus Etravirine on GSK1349572 Pharmacokinetics in Healthy Adult Subjects ( [NCT00867152] | Phase 1 | 17 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
An Evaluation of the Pharmacological Interaction of Lopinavir 800mg - Ritonavir 200mg Combination and Rifampin in Subjects Presenting Tuberculosis, With Contraindication for Antiretroviral Regimens Including Efavirenz [NCT00771498] | Phase 4 | 30 participants (Actual) | Interventional | 2008-11-30 | Completed | ||
Pharmacokinetics and Efficacy of Low- or Standard-dose of Lopinavir/Ritonavir (Kaletra®) in PI-naïve HIV-1 Infected Children [NCT00887120] | Phase 2 | 24 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
Low Doses of Lung Radiation Therapy in Cases of COVID-19 Pneumonia: Prospective Multicentric Study in Radiation Oncology Centers [NCT04394182] | 15 participants (Anticipated) | Interventional | 2020-04-21 | Suspended(stopped due to lack of recruitment) | |||
A Phase I Study of Intra-anally Administered Lopinavir/Ritonavir in People Living With HIV (PLWH) With High-Grade Anal Intraepithelial Neoplasia (AIN 2/3) [NCT05334004] | Phase 1 | 21 participants (Anticipated) | Interventional | 2024-01-31 | Recruiting | ||
Treatment Outcomes and Plasma Level of Ritonavir-boosted Lopinavir Monotherapy Among HIV-infected Patients Who Had Non-nucleoside Reverse Transcriptase Inhibitor (NRTI) and NNRTI Failure: A Pilot Study [NCT01002898] | Phase 3 | 40 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
A Phase 4 Study of the Effect on Immune Reconstitution of a Lopinavir/Ritonavir-Based Versus an Efavirenz-based HAART (Highly Active Antiretroviral Therapy) Regimen in Antiretroviral-Naïve Subjects With Advanced HIV Disease [NCT00775606] | Phase 4 | 15 participants (Actual) | Interventional | 2008-10-31 | Terminated(stopped due to Study stopped 12/2010 due to poor enrollment. Only 15 of 60 needed enrolled.) | ||
Multicenter, International, Prospective, Phase III, Randomized, Superiority Trial Comparing Two Maintenance Strategies With Mono or Bi-therapy of Protease Inhibitors With or Without Lamivudine in Virologically Suppressed HIV Patients on Second Line Antire [NCT01905059] | Phase 3 | 265 participants (Actual) | Interventional | 2014-02-28 | Completed | ||
A Phase II Exploratory Study Examining Immunologic and Virologic Indices in Two Age-Differentiated Cohorts of HIV-Infected Subjects to Explore the Basis of Accelerated HIV-Disease Progression Associated With Aging [NCT00006144] | Phase 2 | 90 participants | Interventional | 2000-10-31 | Completed | ||
An Open-Label Study of a Once Daily Dose of Emtricitabine in Combination With Other Antiretroviral Agents in HIV-Infected Pediatric Patients [NCT00017992] | Phase 2 | 100 participants | Interventional | Recruiting | |||
A Phase III, Randomized, Controlled, Open-Label, Multicentre, Three Arm Study to Compare the Efficacy and Safety of a Dual-Boosted HIV-1 Protease Inhibitor Regimen of Fosamprenavir/Lopinavir/Ritonavir 1400mg/533mg/133mg Twice Daily and an Increased Dosage [NCT00144833] | Phase 3 | 150 participants (Anticipated) | Interventional | 2005-03-31 | Terminated(stopped due to Incomplete data) | ||
Pilot Simplification Study to Lopinavir/Ritonavir 800/200 mg Monotherapy Regimen Once Daily [NCT01581853] | Phase 4 | 21 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Once-daily Antiretroviral Therapy in HIV-1 Infected Patients With CD4+ Cell Counts Below 100 Cells/Mcl. A Prospective, Randomized, Multicentre, Open Clinical Study. [NCT00532168] | Phase 4 | 108 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
A Phase 3, Randomized, Open-label, Study of Lopinavir/Ritonavir Tablets Versus Soft Gel Capsules and Once Daily Versus Twice Daily Administration, When Coadministered With NRTIs in Antiretroviral Naive HIV-1 Infected Subjects [NCT00262522] | Phase 3 | 664 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
A Pilot Study of Lopinavir/Ritonavir in Participants Experiencing Virologic Relapse on NNRTI-Containing Regimens [NCT00357552] | 123 participants (Actual) | Interventional | 2008-01-31 | Completed | |||
Optimizing Antiretroviral Therapy in HIV-Infected Children and Adolescents [NCT00207948] | 4 participants (Actual) | Observational | 2004-11-30 | Terminated(stopped due to no measurable response was detected at the 50% increase threshold.) | |||
Lopinavir/r Plus Saquinavir Salvage Therapy in HIV-infected Children With NRTI and/or NNRTI Failure: PK and Two-year Treatment Follow up [NCT00476359] | Phase 4 | 50 participants (Actual) | Interventional | 2003-10-31 | Completed | ||
An Open-Label, Sequential, 3-Period Study to Evaluate Pharmacokinetics of Coadministered Raltegravir (Isentress) and Lopinavir-Ritonavir (Kaletra) in Healthy Adults [NCT00564772] | Phase 4 | 15 participants (Actual) | Interventional | 2007-11-30 | 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 | ||
Evaluation of Clinical Response and Safety in HIV Positive Subjects Co-infected With Hepatitis C Treated With a Kaletra Containing HAART Regimen [NCT00234975] | Phase 4 | 86 participants (Actual) | Interventional | 2002-10-31 | Completed | ||
A Phase II/III Trial of Lopinavir/Ritonavir Dosed According to the WHO Pediatric Weight Band Dosing Guidelines [NCT01172535] | Phase 2/Phase 3 | 97 participants (Actual) | Interventional | 2010-11-30 | Completed | ||
Randomized, Double-blinded, Controlled Trial of Intensive HAART Including Raltegravir, and Maraviroc, on HIV-1 Pro-viral DNA and Reservoir Decay in HIV-1-infected Individuals During the Acute/Early Infection [NCT01154673] | Phase 2/Phase 3 | 32 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
Long-term Effectiveness and Safety in Hepatitis-co-infected Patients [NCT01153269] | 33 participants (Actual) | Observational | 2001-05-31 | Completed | |||
Treatment Options for Protease Inhibitor-exposed Children [NCT01146873] | Phase 3 | 300 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
A Randomized, Pilot Study on the Antiviral Activity and Immunological Effects of Lopinavir/Ritonavir vs. Efavirenz in Treatment-naïve HIV-Infected Patients With CD4 Cell Counts Below 100 Cells/mm3 [NCT00386659] | Phase 4 | 60 participants | Interventional | Terminated | |||
Evaluation of Kaletra Therapy Over the Long-term [NCT01083810] | 284 participants (Actual) | Observational | 2001-06-30 | Completed | |||
A Multi-centre, Double-blinded, Randomized, Placebo-controlled Trial on the Efficacy and Safety of Lopinavir / Ritonavir Plus Ribavirin in the Treatment of Severe Acute Respiratory Syndrome [NCT00578825] | 340 participants (Anticipated) | Interventional | Not yet recruiting | ||||
Study on the Impact of Triptolide Woldifiion on HIV-1 Reservoir of Chinese HIV/AIDS Patients In Acute HIV-1 Infection [NCT02219672] | Phase 3 | 18 participants (Anticipated) | Interventional | 2014-07-31 | Recruiting | ||
Clinical, Virological and Safety Outcomes of a Lopinavir/Ritonavir-Based Regimen in HIV-1 Infected Patients in Routine Clinical Use in China: A Multicenter Post-Marketing Observational Study [NCT01074931] | 98 participants (Actual) | Observational | 2008-04-30 | Completed | |||
Effect of HIV-1 Protease Inhibitors on Endothelial Function and Glucose Metabolism in Normal, HIV-Uninfected Subjects: Atazanavir or Lopinavir/Ritonavir or Placebo [NCT00720590] | 30 participants (Actual) | Interventional | 2003-11-30 | Completed | |||
Safety and Efficacy of the Universal Use of EFV-TDF-FTC and AZT-3TC-LPV/r Combinations in Pregnant and Breastfeeding Women to Prevent mother-to Child Transmission of HIV-1 o, Resource-limited Settings: A Multicentre Randomized Phase 3 Clinical Trial [NCT00936195] | Phase 3 | 0 participants (Actual) | Interventional | 2010-01-31 | Withdrawn(stopped due to faillure to obtain insurance because of refusal from insurance companies) | ||
Therapeutic Drug Monitoring of the Generic Lopinavir/Ritonavir Tablets 200/50 mg in the Thai HIV-infected Patient [NCT00802334] | Phase 2 | 70 participants (Actual) | Interventional | 2008-01-31 | Completed | ||
A Phase I, Open-label, Single Sequence, Crossover Study Evaluating the Safety and the Pharmacokinetics of Lopinavir/Ritonavir and Eltrombopag Given Alone and When Co-administered in Healthy Adult Subjects. [NCT00833378] | Phase 1 | 40 participants (Actual) | Interventional | 2009-01-19 | Completed | ||
Pharmacokinetics of the Tablet Formulation of Lopinavir/r as Standard and Increased Dosage During Pregnancy in HIV-infected Women [NCT00605098] | Phase 4 | 60 participants (Actual) | Interventional | 2008-02-29 | Completed | ||
The Pharmacokinetics and Safety of Generic Lopinavir/Ritonavir (200/50 mg Tablets) 400/100 mg q12h in Thai HIV-infected Pregnant Women [NCT00621166] | Phase 2 | 20 participants (Actual) | Interventional | 2008-06-30 | Completed | ||
Special Investigation of Kaletra in Pregnant Women [NCT01076985] | 24 participants (Actual) | Observational | 2000-12-31 | Completed | |||
MERS-CoV Infection tReated With A Combination of Lopinavir /Ritonavir and Interferon Beta-1b: a Multicenter, Placebo-controlled, Double-blind Randomized Trial [NCT02845843] | Phase 2/Phase 3 | 95 participants (Actual) | Interventional | 2016-07-31 | 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 Phase IV Study of Antiretroviral Therapy for HIV Infected Adults Presenting With Acute Opportunistic Infections: Immediate Versus Deferred Initiation of Antiretroviral Therapy [NCT00055120] | Phase 4 | 283 participants (Actual) | Interventional | 2003-03-31 | Completed | ||
A 3 Arm, Prospective Study to Compare the Effect of 6 Weeks Exposure to the Combination of Lopinavir (LPVr)/Combivir® (AZT/3TC) Versus Lopinavir Alone or Combivir® Alone in HIV-negative Healthy Subjects on the Development of Abnormalities of Lipid and Glu [NCT00192621] | Phase 4 | 50 participants (Actual) | Interventional | 2004-11-30 | Completed | ||
A Phase I/II Safety, Tolerability, and Pharmacokinetic Study of High Dose Lopinavir/Ritonavir With or Without Saquinavir in HIV-Infected Pediatric Subjects Previously Treated With Protease Inhibitors [NCT00084058] | Phase 1/Phase 2 | 26 participants (Actual) | Interventional | Completed | |||
A Phase III Randomized Trial of the Safety and Antiretroviral Effects of Zidovudine/Lamivudine/Abacavir Versus Zidovudine/Lamivudine/Lopinavir/Ritonavir in the Prevention of Perinatal Transmission of HIV [NCT00086359] | Phase 3 | 19 participants (Actual) | Interventional | 2004-07-31 | Completed | ||
Evaluation of the Use of Antiretroviral Regimens Containing Raltegravir for Prophylaxis of Mother-to-child-transmission of HIV Infection in Pregnant Women Presenting With Detectable Viral Load After 32 Weeks of Gestation: a Pilot Study [NCT01854762] | Phase 2/Phase 3 | 40 participants (Anticipated) | Interventional | 2015-03-31 | Recruiting | ||
Drug-Drug Interaction Study to Assess the Effects of Steady-State Lopinavir/Ritonavir on Pitavastatin in Healthy Adult Volunteers [NCT01057433] | Phase 4 | 24 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
A 24-week, Randomized, Open-label, 2-arm Study to Compare the Safety, Efficacy and Tolerability of Invirase® Tablets With Ritonavir Versus Kaletra® Tablets in HIV 1 Infected Adults on a Kaletra® Based Regimen With 2 Nucleosides/Nucleotides [NCT00438152] | Phase 4 | 53 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
[NCT00525239] | 60 participants (Anticipated) | Interventional | 2004-03-31 | Recruiting | |||
HIV- Monotherapy in Switzerland (MOST- ch) [NCT00531986] | Phase 4 | 60 participants (Actual) | Interventional | 2007-01-31 | Terminated(stopped due to Unexpectedely high rates of treatment-failure) | ||
Baricitinib Combined With Antiviral Therapy in Symptomatic Patients Infected by COVID-19: an Open-label, Pilot Study [NCT04320277] | Phase 2/Phase 3 | 200 participants (Anticipated) | Interventional | 2020-05-16 | Not yet recruiting | ||
Monotherapy in Africa: Evaluation of New Therapy [NCT02155101] | Phase 3 | 120 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
Comprehensive in Vitro Proarrhythmia Assay (CiPA) Clinical Phase 1 ECG Biomarker Validation Study (CiPA Phase 1 ECG Biomarker Study) [NCT03070470] | Phase 1 | 60 participants (Actual) | Interventional | 2017-03-14 | Completed | ||
Phase I/II Study of ABT-378/Ritonavir in Combination With Reverse Transcriptase Inhibitors in Antiretroviral Naive HIV-Infected Patients [NCT00004578] | Phase 1/Phase 2 | 100 participants (Actual) | Interventional | 1997-11-30 | 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 | ||
A Phase III, Open Label, Randomized, Comparative Study of the Antiviral Efficacy of ARV Therapy With Lopinavir/Ritonavir (LPV/r-Kaletra) in Combination With Tenofovir (TDF) Versus Standard of Care (Kaletra in Combination With 2 Nucleoside RTIs) in naïve-H [NCT00234910] | Phase 3 | 152 participants (Actual) | Interventional | 2005-01-31 | Completed | ||
An Open-Label, Randomized Study to Determine the Impact of Antiretroviral Treatment in HCV/HIV-Coinfected Subjects With High CD4+ Cell Count on the Efficacy of Hepatitis C Treatment With Pegylated Interferon Alfa-2A and Ribavirin [NCT00100581] | 2 participants (Actual) | Interventional | Completed | ||||
Safeguard the Household: A Study of HIV Antiretroviral Therapy Treatment Strategies Appropriate for a Resource Poor Country [NCT00080522] | 813 participants | Interventional | 2005-02-28 | Completed | |||
A Randomized, Open-Label Study Assessing Safety, Tolerability and Efficacy of an Induction-Maintenance Treatment Strategy Including Lopinavir/Ritonavir Plus Tenofovir Disoproxil Fumarate and Emtricitabine Versus Efavirenz Plus Tenofovir Disoproxil Fumarat [NCT00121017] | Phase 2 | 200 participants | Interventional | Withdrawn | |||
MEDICLAS Study (Metabolic Effects of Different Classes of AntiretroviralS) [NCT00122226] | Phase 4 | 50 participants | Interventional | 2003-01-31 | Active, not recruiting | ||
A Pharmacokinetic Study of Super-boosted Lopinavir/Ritonavir in Combination With Rifampin in HIV-1-infected Patients With Tuberculosis. [NCT01700790] | Phase 4 | 9 participants (Actual) | Interventional | 2016-02-29 | Terminated(stopped due to No Further Funding) | ||
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 | ||
The Pharmacokinetics of Lopinavir/Ritonavir in Combination With Atazanavir in HIV-Infected Subjects [NCT00420355] | Phase 4 | 19 participants (Actual) | Interventional | 2007-04-30 | Terminated(stopped due to Unexpected adverse event) | ||
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 | ||
A Randomized Clinical Trial Assessing Continuous HAART Versus Interrupted HAART in a Resource Poor Clinic [NCT00100646] | 30 participants (Actual) | Interventional | 2007-03-31 | Completed | |||
A Phase II, Randomized, Open-Label Study to Evaluate the Safety and Effectiveness of Two Antiretroviral Therapeutic Strategies: A Dual PI-Based HAART Regimen Versus a Multi-NRTI ART Regimen, in ART-Experienced Children and Youth Who Have Experienced Virol [NCT00102206] | Phase 2 | 6 participants (Actual) | Interventional | Completed | |||
Sex Differences in Lopinavir/Ritonavir Pharmacokinetics Among HIV-1-Infected Men and Women [NCT00102986] | 116 participants (Actual) | Interventional | 2005-10-31 | Completed | |||
Phase III-IV, Comparative, Randomized, Open-Label, Study to Evaluate Safety and Efficacy of Suspending Nucleosides From a Triple-Drug Therapy Based on Lopinavir/Ritonavir Versus Continuing Triple-Drug Therapy in HIV-Infected Subjects With Undetectable Pla [NCT00114933] | Phase 4 | 200 participants | Interventional | 2005-01-31 | Completed | ||
A Randomized Comparison of Protease Inhibitor-based Versus Non-nucleoside Reverse Transcriptase Inhibitor-based Antiretroviral Therapy for Initial Treatment of Individuals With AIDS-related Kaposi's Sarcoma in Sub-Saharan Africa [NCT00444379] | Phase 4 | 224 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
A 48-Weeks National Multicenter Randomized Open Clinical Trial Evaluating Tolerance and Efficacy of a Treatment Simplification by Lopinavir/Ritonavir Versus Continuation of Current Treatment in HIV-Infected Patients With a Viral Load Inferior to 50 Copies [NCT00140751] | Phase 3 | 186 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Evaluation of Efficacy of Pharmacotherapy Treatment of COVID- 19 Infection Using Oral Levamisole and Formoterol+Budesonide Inhaler and Comparison of This Treatment Protocol With Standard National Treatment of the Disease [NCT04331470] | Phase 2/Phase 3 | 30 participants (Anticipated) | Interventional | 2020-04-04 | Recruiting | ||
Effect of HIV Protease Inhibitor Drugs on Glucose and Insulin Metabolism [NCT00135434] | Phase 1 | 25 participants | Interventional | 2004-09-30 | Completed | ||
Randomized, Single Oral Dose,Two Treatment,Four-period,Full-replicated,Cross-over Trial to Assess the BE of Orvical 200 mg/50 mg FT in Comparison With Kaletra 200 mg/50 mg FT in Healthy Male Subjects Under Fasting Conditions [NCT04386876] | Phase 1 | 30 participants (Actual) | Interventional | 2020-04-30 | Completed | ||
The Regimen of Favipiravir Plus Hydroxychloroquine Can Accelerate Recovery of the COVID-19 Patients With Moderate Severity in Comparison to Lopinavir/Ritonavir Plus Hydroxychloroquine Regimen: an Open-label, Non-randomized Clinical Trial Study [NCT04376814] | 40 participants (Actual) | Interventional | 2020-03-29 | Completed | |||
A Randomized Trial of Efficacy and Safety of an Early OUTpatient Treatment of COVID-19 in Patients With Risk Factor for Poor Outcome: a Strategy to Prevent Hospitalization [NCT04365582] | Phase 3 | 0 participants (Actual) | Interventional | 2020-05-07 | Withdrawn(stopped due to The PI decided.) | ||
Efficacy of Pragmatic Same-day Ring COVID-19 Prophylaxis for Adult Individuals Exposed to SARS-CoV-2 in Switzerland: an Open-label Cluster Randomized Trial [NCT04364022] | Phase 3 | 326 participants (Actual) | Interventional | 2020-04-23 | Completed | ||
Efficacy and Safety of Umifenovir as an Adjuvant Therapy Compared to the Control Therapeutic Regiment of Interferon Beta 1a, Lopinavir / Ritonavir and a Single Dose of Hydroxychloroquine in Moderate to Severe COVID-19: A Randomized, Double-Blind, Placebo- [NCT04350684] | Phase 4 | 40 participants (Anticipated) | Interventional | 2020-04-15 | Enrolling by invitation | ||
A Multi-Center Comparison of Raltegravir to Lopinavir/Ritonavir, Both in Combination With Truvada, in HIV-Infected Individuals Naive to Antiretroviral Therapy [NCT00632970] | Phase 4 | 6 participants (Actual) | Interventional | 2008-02-29 | Terminated(stopped due to no patients completed) | ||
A Proof of Concept Study for GSK2248761 (An Extension of NV-05A-002: A Phase I/IIa Double-Blind Study to Evaluate the Safety and Tolerability, Antiretroviral Activity, Pharmacokinetics and Pharmacodynamics of IDX12899 in Antiretroviral Treatment-Naive HIV [NCT00945282] | Phase 2 | 8 participants (Actual) | Interventional | 2009-10-20 | Completed | ||
Bone and Body Comp: A Sub Study of the SECOND-LINE Study [NCT01513122] | Phase 4 | 210 participants (Actual) | Interventional | 2010-02-28 | Completed | ||
HIV Infection and Breastfeeding: Interventions for Maternal and Infant Health [NCT00164736] | Phase 3 | 2,369 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
"Study ACA-ARGE-04-001 A Pilot, Open-Label Study Assessing Safety, Tolerability, Efficacy of a Simplified Lopinavir/Ritonavir Induction/Maintenance Therapy in HIV-Infected Subjects on Their First Protease Inhibitor-Based Regimen." [NCT00159224] | Phase 4 | 100 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
The Efficacy and Safety of Carrimycin Treatment in Patients With Novel Coronavirus Infectious Disease (COVID-19) : A Multicenter, Randomized, Open-controlled Study [NCT04286503] | Phase 4 | 520 participants (Anticipated) | Interventional | 2020-02-23 | Not yet recruiting | ||
A Randomized, Open-label, Controlled Study of the Efficacy of Lopinavir Plus Ritonavir and Arbidol for Treating With Patients With Novel Coronavirus Infection [NCT04252885] | Phase 4 | 86 participants (Actual) | Interventional | 2020-01-28 | Completed | ||
An Open Label Study of the Impact on Insulin Sensitivity, Lipid Profile and Vascular Inflammation by Treatment With Lopinavir / Ritonavir (400 / 100 mg Twice Daily) or Raltegravir 400 mg Twice Daily in HIV Negative Male Volunteers. [NCT00531999] | Phase 1 | 18 participants (Actual) | Interventional | 2007-10-31 | Completed | ||
Open Randomized Study Comparing Two Alternatives of Antiretroviral Therapy as Post-exposure Prophylaxis to HIV-1: TENOFOVIR+EMTRICITABINA + LOPINAVIR/RITONAVIR VS TENOFOVIR+EMTRICITABINA + MARAVIROC [NCT01533272] | Phase 4 | 240 participants (Actual) | Interventional | 2012-02-29 | Completed | ||
Pharmacokinetics of and Rate of HIV-1 RNA Decline in ARV-naive HIV-1 Infected Patients Treated With Low- or Standard-dose Saquinavir HGC (Invirase®) and Lopinavir/Ritonavir (Kaletra® [NCT00400738] | Phase 2 | 48 participants (Actual) | Interventional | 2004-03-31 | Completed | ||
A Phase IIb, 96 Week, Randomized, Open-label Multicenter, Parallel Group, Repeat Dose Study to Evaluate the Safety, Tolerability, PK and Antiviral Effect of Different Doses and Regimens of GW873140 in Combination With Kaletra (Lopinavir and Ritonavir) in [NCT00102778] | Phase 2 | 175 participants | Interventional | 2004-12-31 | Terminated | ||
Prospective Trial to Evaluate How Therapeutic Drug Monitoring of Protease Inhibitors Increases Virologic Success and Tolerance of HAART (ANRS 111 COPHAR2) [NCT00122590] | 115 participants | Interventional | 2002-07-31 | Terminated | |||
Effect of Change to a Nucleoside Reverse Transcriptase Inhibitor (NRTI)-Sparing Regimen of Efavirenz (EFV) and Lopinavir/Ritonavir (LPV/r) on Liver Histology in HIV-1-Infected Individuals With Lactic Acidemia and Persistent Alanine Aminotransferase (ALT) [NCT00023218] | 0 participants (Actual) | Interventional | Withdrawn | ||||
A Randomized, Comparative Study of Lopinavir/Ritonavir Versus GW433908 and Ritonavir Versus Lopinavir/Ritonavir and GW433908 (In Combination With Tenofovir Disoproxil Fumarate and One or Two Nucleoside Reverse Transcriptase Inhibitors) in HIV-1-Infected S [NCT00028366] | 56 participants | Interventional | Completed | ||||
A Randomized, Controlled Trial of Two Potent, Simplified Regimens Utilizing A Protease Inhibitor-Sparing Regimen Versus A Nucleoside-Sparing Regimen for HIV-Infected Subjects Who Participated in ACTG 388 or Who Responded to A First Potent Combination Regi [NCT00014937] | 240 participants | Interventional | Completed | ||||
A Randomized, Open-Label Study of 800 Mg Lopinavir/200 Mg Ritonavir QD in Combination With Tenofovir and Emtricitabine Vs. 400 Mg Lopinavir /100 Mg Ritonavir BID in Combination With Tenofovir and Emtricitabine in HIV-Infected Antiretroviral Naïve Subjects [NCT00043966] | Phase 3 | 200 participants | Interventional | 2002-07-31 | Completed | ||
A Phase II, Randomized, Open-Label Study Comparing Fixed-Dose Versus Concentration-Adjusted Lopinavir/Ritonavir Therapy in HIV-Infected Subjects on Salvage Therapy [NCT00046033] | Phase 2 | 118 participants | Interventional | Completed | |||
A Comparative Trial of Protease-Containing and Protease-Sparing HAART Regimens in HIV-Infected Adolescents With an Evaluation of Therapeutic Drug Monitoring [NCT00075907] | Phase 3 | 240 participants | Interventional | 2004-07-31 | 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 | ||
A Phase II Study of the Predictive Value of Pharmacokinetic-Adjusted Phenotypic Susceptibility (C12h/IC50) on Antiretroviral Response to Ritonavir-Enhanced Protease Inhibitors in Subjects With Failure of Previous Protease Inhibitor-Based Regimens [NCT00027339] | Phase 2 | 53 participants (Actual) | Interventional | 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 | |||
Immunologic Consequences of Antiretroviral Therapy Intensification in Subjects With Moderately Advanced HIV-1 Disease: A Follow-Up Study to ACTG 315/375 [NCT00034086] | 22 participants | Interventional | Completed | ||||
A Phase I/II, Open Label Study to Evaluate the Ability of Combination Therapy With ABT-378/Ritonavir (Kaletra), Lamivudine (Epivir), Efavirenz (Sustiva)and Tenofovir DF to Completely Suppress Viral Replication in Subjects Infected With HIV-1 [NCT00038220] | Phase 2 | 40 participants | Interventional | 2000-07-31 | Completed | ||
A Phase III, Randomized, Open-Label Comparison of Lopinavir/Ritonavir Plus Efavirenz Versus Lopinavir/Ritonavir Plus 2 NRTIs Versus Efavirenz Plus 2 NRTIs as Initial Therapy for HIV-1 Infection [NCT00050895] | Phase 3 | 775 participants | Interventional | Completed | |||
A Phase III, Randomized, Multicenter, Parallel Group, Open-Label, Three Arm Study to Compare the Efficacy and Safety of Two Dosing Regimens of GW433908/Ritonavir (700mg/100mg Twice Daily or 1400mg/200mg Once Daily) Versus Lopinavir/Ritonavir (400mg/100mg [NCT00025727] | Phase 3 | 330 participants | Interventional | 2001-05-31 | Active, not recruiting | ||
A Randomized, Phase II, Open Label Study to Compare Twice Daily and Once Daily Potent Antiretroviral Therapy and to Compare Self-Administered Therapy and Therapy Administered Under Direct Observation [NCT00036452] | Phase 2 | 402 participants (Actual) | 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 Phase I/II Study of Lopinavir/Ritonavir in HIV-1 Infected Infants Less Than 6 Months of Age [NCT00038480] | Phase 1 | 31 participants (Actual) | Interventional | Completed | |||
A Study of Two Different Doses of ABT-378/Ritonavir in HIV-Infected Patients Who Have Taken Protease Inhibitors and Non-Nucleoside Reverse Transcriptase Inhibitors [NCT00038636] | Phase 3 | 36 participants | Interventional | 2000-09-30 | Completed | ||
A Phase II Pharmacokinetic Study of the Transdermal Contraceptive System and Oral Contraceptive in HIV-1 Infected Women on Lopinavir/Ritonavir [NCT00125983] | Phase 2 | 32 participants (Actual) | Interventional | Completed | |||
A Randomized, Open-Label Study Exploring a Simplified Kaletra® (Lopinavir/Ritonavir)-Based Therapy Versus a Sustiva® (Efavirenz)-Based Standard of Care in Previously Non-Treated HIV-Infected Subjects [NCT00075231] | Phase 2 | 150 participants | Interventional | 2003-12-31 | Completed | ||
A Phase II Study of Lopinavir/Ritonavir in Combination With Saquinavir Mesylate or Lamivudine/Zidovudine to Explore Metabolic Toxicities in Antiretroviral HIV-Infected Subjects [NCT00043953] | Phase 2 | 30 participants (Actual) | Interventional | 2002-08-31 | Completed | ||
Study on the Feasibility of Antiretroviral Therapy With a Single Agent - Lopinavir/r - in Patients Treated With HAART and With Viral Load Below 80 Copies/Ml [NCT00160849] | Phase 4 | 60 participants | Interventional | 2004-08-31 | Completed | ||
Boosted PI VS. NNRTI Based Therapy as Initial Treatment for HIV-1 Infected Patients With Advanced Disease [NCT00162643] | Phase 4 | 300 participants | Interventional | 2004-12-31 | Recruiting | ||
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) | ||
Latency and Early Neonatal Provision of Antiretroviral Drugs Clinical Trial [NCT02431975] | Phase 4 | 73 participants (Actual) | Interventional | 2015-08-31 | Completed | ||
Randomized, Open-Label 2x2 Factorial Study to Compare the Safety and Efficacy of Different Combination Antiretroviral Therapy Regimens in Treatment Naive Patients With Advanced HIV Disease and/or CD4+ Cell Counts Less Than 200 Cells/MicroL [NCT00342355] | Phase 4 | 1,771 participants (Actual) | Interventional | 2004-01-31 | 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.) | ||
Pharmacokinetic Interactions Between Buprenorphine and Kaletra (Lopinavir/Ritonavir) [NCT00571961] | 12 participants (Actual) | Interventional | 2007-01-31 | Completed | |||
An Open-label Randomized Controlled Trial on Lopinavir/ Ritonavir, Ribavirin and Interferon Beta 1b Combination Versus Lopinavir/ Ritonavir Alone, as Treatment for 2019 Novel Coronavirus Infection [NCT04276688] | Phase 2 | 127 participants (Actual) | Interventional | 2020-02-10 | Completed | ||
Pharmacokinetic Properties of Antiretroviral and Anti-Tuberculosis Drugs During Pregnancy and Postpartum [NCT04518228] | 325 participants (Anticipated) | Observational | 2021-06-08 | Recruiting | |||
Pharmacokinetic Interactions Between Antiretroviral Agents, Lopinavir/Ritonavir and Efavirenz and Antimalarial Drug Combination, Artemether/Lumefantrine [NCT00266058] | Phase 1 | 33 participants (Actual) | Interventional | 2005-12-31 | Completed | ||
A Pilot, Open-Label, Randomized, Comparative Study of the Antiviral Efficacy of Lopinavir/Ritonavir Single-Drug Regimen Versus Lopinavir/Ritonavir in Combination With Lamivudine/Zidovudine in Antiretroviral Naïve Patients [NCT00234923] | Phase 3 | 138 participants (Actual) | Interventional | 2003-08-31 | Completed | ||
Factors Associated With Adherence in a Cohort of HIV Positive Subjects on a First Time PI Containing HAART Regimen: Observational Study of the Impact of Adherence on Viral Load for a HAART Regimen Containing Kaletra vs Other Selected PI Containing HAART. [NCT00234962] | Phase 4 | 200 participants | Interventional | 2002-08-31 | Terminated | ||
Prevention of HIV1 Mother to Child Transmission Without Nucleoside Analogue Reverse Transcriptase Inhibitors in the Pre-partum Phase. A Multicenter Randomised Phase II/III Open Label Study With a Group of 100 Pregnant Women Receiving Lopinavir/Ritonavir a [NCT00424814] | Phase 2/Phase 3 | 105 participants (Actual) | Interventional | 2007-03-31 | Completed | ||
A Phase IV, Randomized, Open-label Study of the Tolerability of Once Daily Lopinavir/Ritonavir (LPV/r) Liquid Versus Capsules [NCT00281606] | Phase 4 | 65 participants (Actual) | Interventional | 2006-02-14 | Completed | ||
Enfuvirtide for the Initial Phase of Antiretroviral Therapy in HIV-infected Patients With High Risk of Clinical Progression : ANRS 130 APOLLO [NCT00302822] | Phase 3 | 195 participants (Actual) | Interventional | 2006-04-30 | 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 | ||
Low Dose Anti-inflammatory Radiotherapy for the Treatment of Pneumonia by COVID-19: Multi-central Prospective Study [NCT04380818] | 106 participants (Anticipated) | Interventional | 2020-06-05 | Recruiting | |||
Maraviroc Switch Central Nervous System (CNS) Substudy: a Substudy of MARCH, a Randomised, Open-label Study to Evaluate the Efficacy and Safety of Maraviroc (MVC) as a Switch for Either Nucleoside or Nucleotide Analogue Reverse Transcriptase Inhibitors (N [NCT01637233] | 28 participants (Actual) | Observational | 2012-06-30 | Completed | |||
Maraviroc Switch Collaborative Study Renal Substudy [NCT01637259] | Phase 4 | 76 participants (Actual) | Interventional | 2012-06-30 | 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 | ||
A Phase 1, Open-Label, Parallel Study to Evaluate the Effect of Multiple Doses of Isavuconazole on the Pharmacokinetics of Multiple Doses of Lopinavir/Ritonavir and the Effects of Lopinavir/Ritonavir on the Pharmacokinetics of Multiple Doses of Isavuconaz [NCT01660477] | Phase 1 | 68 participants (Actual) | Interventional | 2012-06-30 | 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 Multicenter, Randomized, Active Controlled, Open Label, Platform Trial on the Efficacy and Safety of Experimental Therapeutics for Patients With COVID-19 (Caused by Infection With Severe Acute Respiratory Syndrome Coronavirus-2) [NCT04351724] | Phase 2/Phase 3 | 500 participants (Anticipated) | Interventional | 2020-04-16 | Recruiting | ||
An Investigation Into Beneficial Effects of Interferon Beta 1a, Compared to The Base Therapeutic Regiment in Moderate to Severe COVID-19: A Randomized, Double-Blind, Placebo-Controlled, Clinical Trial [NCT04350671] | Phase 4 | 40 participants (Anticipated) | Interventional | 2020-04-15 | Enrolling by invitation | ||
A Pilot Study of the Pharmacokinetics and Safety of Rifabutin 150 mg Once Daily Versus Rifabutin 300 mg Thrice Weekly With Lopinavir/Ritonavir Based HAART in HIV/TB Co-infected Patients [NCT02415985] | Phase 2 | 40 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
A Study on ART Naïve Patients On Different Regimens to Treat Hiv (a Phase 4 Study) [NCT01445223] | Phase 4 | 242 participants (Actual) | Interventional | 2004-04-30 | Completed | ||
Pharmacokinetics of Plasma Lopinavir/Ritonavir Over a 12 Hour Dosing Interval Following Administration of 400/100, 200/150, and 200/50 mg Twice Daily to HIV-negative Healthy Volunteers [NCT00985543] | Phase 1 | 22 participants (Actual) | Interventional | 2009-10-31 | Completed | ||
Real-Life Effectiveness of the Kaletra Adherence Support Assistance (KASA) Program: A Prospective Observational Cohort Study (KASA PMOS) [NCT01662336] | 173 participants (Actual) | Observational | 2012-06-30 | Completed | |||
A Phase II Study of ABT-378/Ritonavir and Efavirenz in Multiple Protease Inhibitor-Experienced Subjects [NCT00004582] | Phase 2 | 0 participants | Interventional | Completed | |||
Comparative Therapeutic Efficacy and Safety of Remdesivir Plus Lopinavir/ Ritonavir and Tocilizumab Versus Hydroxychloroquine Plus Ivermectin and Tocilizumab in COVID-19 Patients. [NCT04779047] | Phase 4 | 150 participants (Anticipated) | Interventional | 2020-10-01 | Recruiting | ||
Efficacy of Novel Agents for Treatment of SARS-CoV-2 Infection Among High-Risk Outpatient Adults: An Adaptive Randomized Platform Trial [NCT04354428] | Phase 2/Phase 3 | 289 participants (Actual) | Interventional | 2020-04-16 | Terminated(stopped due to Low number of events contributing to primary outcome) | ||
A Randomized Phase II Study of the Safety, Immunologic, and Virologic Effects of Cyclosporine A in Conjunction With Trizivir(R) and Kaletra(R) Versus Trizivir(R) and Kaletra(R) Alone During Primary HIV-1 Infection [NCT00084149] | Phase 2 | 54 participants (Actual) | Interventional | 2004-02-29 | Completed | ||
A Phase I, Three-Arm Safety, Tolerability, and Pharmacokinetic Interaction Study of PA-824, an Investigational Nitroimidazole for the Treatment of Tuberculosis, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin [NCT01571414] | Phase 1 | 52 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Open Randomized Study Comparing Two Alternatives of Antiretroviral Therapy as Post-exposure Prophylaxis to HIV-1: Tenofovir + Emtricitabine + Lopinavir/Ritonavir Versus Tenofovir + Emtricitabine + Raltegravir [NCT01576731] | Phase 4 | 240 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
Randomized Controlled Pilot Study of Highly Active Anti-Retroviral Therapy for Patients With Primary Biliary Cirrhosis [NCT01614405] | 13 participants (Actual) | Interventional | 2012-06-30 | Completed | |||
Safety and Efficacy of Intravenous Infusion of Wharton's Jelly Derived Mesenchymal Stem Cell Plus Standard Therapy for the Treatment of Patients With Acute Respiratory Distress Syndrome Diagnosis Due to COVID 19: A Randomized Controlled Trial [NCT04390152] | Phase 1/Phase 2 | 40 participants (Anticipated) | Interventional | 2020-01-13 | Recruiting | ||
An Open Label, Randomized, Parallel-group Pharmacokinetics Trial of Tipranavir / Ritonavir (TPV/RTV), Alone or in Combination With RTV-boosted Saquinavir (SQV), Amprenavir (APV), or Lopinavir (LPV), Plus an Optimized Background Regimen, in Multiple Antire [NCT00056641] | Phase 2 | 328 participants | Interventional | 2003-02-18 | 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 | ||||
Chemoprophylaxis of SARS-CoV-2 Infection (COVID-19) in Exposed Healthcare Workers : A Randomized Double-blind Placebo-controlled Clinical Trial [NCT04328285] | Phase 3 | 118 participants (Actual) | Interventional | 2020-04-14 | Terminated(stopped due to French authority's decision) | ||
An Investigation Into Beneficial Effects of Interferon Beta 1a, Compared to Interferon Beta 1b And The Base Therapeutic Regiment in Moderate to Severe COVID-19: A Randomized Clinical Trial [NCT04343768] | Phase 2 | 60 participants (Actual) | Interventional | 2020-04-09 | Completed | ||
Comparative Therapeutic Efficacy and Safety of Remdesivir Versus Lopinavir/ Ritonavir and Remdesivir Combination in COVID-19 Patients [NCT04738045] | Phase 4 | 90 participants (Anticipated) | Interventional | 2020-11-01 | Recruiting | ||
A Phase 1 Clinical Study to Assess the Effect of Darunavir/Ritonavir or Lopinavir/Ritonavir on the Pharmacokinetics of Daclatasvir in Healthy Subjects [NCT02159352] | Phase 1 | 49 participants (Actual) | Interventional | 2014-06-30 | Completed | ||
Evaluation of Additional Treatments for COVID-19: a Randomized Trial in Niger [NCT04409483] | Phase 3 | 0 participants (Actual) | Interventional | 2020-06-01 | Withdrawn(stopped due to Epidemic dynamics) | ||
The Influence of Lopinavir/Ritonavir on Gemfibrozil Pharmacokinetics in Healthy Volunteers [NCT00474201] | 15 participants (Actual) | Interventional | 2007-05-31 | 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.) | ||
Pharmacokinetics Study of Tenofovir in HIV-infected Thai Children Using Tenofovir-based Regimen [NCT02404259] | 32 participants (Actual) | Interventional | 2010-06-30 | Completed | |||
A Pharmacokinetics Study Comparing Lopinavir Plasma Exposure When Given as Lopinavir/Ritonavir (1:1) in the Presence of Rifampicin and Lopinavir/Ritonavir (4:1) Without Rifampicin in HIV and TB Co-infected Children in South Africa. [NCT02348177] | Phase 4 | 96 participants (Actual) | Interventional | 2013-01-31 | Completed | ||
Efficacy and Safety of Albuvirtide for Injection Combined With LPV/r for Treatment of HIV-1-Infected Patients Failed First-line Antiretroviral Therapy [NCT02369965] | Phase 3 | 418 participants (Actual) | Interventional | 2014-02-19 | Completed | ||
HIV Postexposure Prophylaxis With Darunavir/r (PEPDar) [NCT01516970] | Phase 3 | 312 participants (Actual) | Interventional | 2011-11-25 | Completed | ||
A Pilot Study to Assess Virologic Suppression and Immune Recovery With Raltegravir and Lopinavir/Ritonavir and Raltegravir and Emtricitabine/Tenofovir in HIV-1 Infected Treatment-naïve Subjects [NCT00654147] | Phase 2 | 44 participants (Actual) | Interventional | 2008-04-30 | 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 | ||
Drug Use Investigation of Kaletra [NCT01076972] | 1,184 participants (Actual) | Observational | 2000-12-31 | Completed | |||
Retrospective Cohort to Evaluate the Effectiveness and Safety of Xiyanping Injection Combined With Conventional Treatment for New Coronavirus Infection Pneumonia (Common Type) [NCT04275388] | 426 participants (Anticipated) | Observational | 2020-05-15 | Not yet recruiting | |||
Immune Reconstitution as a Determinant of Adverse Effects to New Antiretroviral Therapy in Persons With Advanced HIV Infection [NCT00885664] | Phase 4 | 60 participants (Actual) | Interventional | 2005-10-31 | Completed | ||
Baricitinib Therapy in COVID-19: A Pilot Study on Safety and Clinical Impact [NCT04358614] | Phase 2/Phase 3 | 12 participants (Actual) | Interventional | 2020-03-16 | Completed | ||
A Pilot Project to Operationalize the Prevention Strategy of Post Exposure Prophylaxis Following Sexual Exposure to HIV in Combination With Educational Programming and Behavioral Risk Reduction Strategies in Los Angeles County [NCT00949234] | Phase 2 | 267 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
"Hydroxychloroquine and Lopinavir/ Ritonavir for Hospitalization and Mortality Reduction in Patients With COVID-19 and Mild Disease Symptoms: The Hope Coalition" [NCT04403100] | Phase 3 | 1,968 participants (Anticipated) | Interventional | 2020-06-03 | Recruiting | ||
A Randomized, Double-Blind, Phase III Study of ABT-378/Ritonavir Plus Stavudine and Lamivudine vs Nelfinavir Plus Stavudine and Lamivudine in Antiretroviral Naive HIV-Infected Subjects [NCT00004583] | Phase 3 | 660 participants | Interventional | 1999-03-31 | Completed | ||
An Open-Label Randomized Clinical Trial to Evaluate the Efficacy and Safety of Short Course Antiretroviral Therapy for Acute or Recent HIV-1 Infection in Zimbabwe and the United States [NCT00414518] | 16 participants (Actual) | Interventional | 2007-01-31 | Completed | |||
Comparison of Liquid Kaletra and Low Dose Kaletra Tablets in HIV-Positive Children [NCT00762320] | 8 participants (Actual) | Interventional | 2008-10-31 | Completed | |||
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 | ||
IMPAACT 1092: Phase IV Evaluation Of The Steady State Pharmacokinetics Of Zidovudine, Lamivudine, and Lopinavir/Ritonavir in Severely Malnourished HIV-1-Infected Children [NCT01818258] | Phase 4 | 52 participants (Actual) | Interventional | 2015-10-26 | Completed | ||
A Randomized, Phase 2b Study of a Double-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifampin-Based Tuberculosis Treatment Versus a Standard-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifabutin-Based Tuberculosis Treatment W [NCT01601626] | Phase 2 | 71 participants (Actual) | Interventional | 2013-07-13 | Terminated(stopped due to The study was stopped early due to feasibility concerns.) | ||
A Phase IIIb, Open -Label, Randomized Multi-center Study Comparing the Antiviral Efficacy, Safety, and Effect on Serum Lipids of Atazanavir/Ritonavir Versus Lopinavir/Ritonavir, in Combination With Two Nucleoside or Nucleotide Reverse Transcriptase Inhibi [NCT00135395] | Phase 3 | 200 participants (Anticipated) | Interventional | 2004-05-31 | Completed | ||
A Randomized Open-label Study of the Antiviral Efficacy and Safety of Atazanavir Versus Lopinavir/Ritonavir(LPV/RTV), Each in Combination With Two Nucleosides in Subjects Who Have Experienced Virologic Failure With Prior Protease Inhibitor-Containing HAAR [NCT00028301] | Phase 3 | 0 participants | Interventional | 2001-02-28 | 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 | ||
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 | ||
HIV Reservoir Dynamics After Switching to Dolutegravir in Patients With Two NRTI and a Protease Inhibitor Based Regimen. A Phase IV Open Randomized Trial [NCT02513147] | Phase 4 | 44 participants (Actual) | Interventional | 2015-06-30 | Completed | ||
Favipiravir, Lopinavir/Ritonavir or Combination Therapy: a Randomised, Double Blind, 2x2 Factorial Placebo-controlled Trial of Early Antiviral Therapy in COVID-19 [NCT04499677] | Phase 2 | 240 participants (Actual) | Interventional | 2020-09-24 | Completed | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |