Page last updated: 2024-12-08

atazanavir

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Description

atazanavir : A heavily substituted carbohydrazide that is an antiretroviral drug of the protease inhibitor (PI) class used to treat infection of human immunodeficiency virus (HIV). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID148192
CHEMBL ID1163
CHEBI ID37924
SCHEMBL ID41696

Synonyms (92)

Synonym
3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-((4-(2-pyridinyl)phenyl)methyl)-2,5,6,10,13-pentaazatetradecanedioic acid dimethyl ester
AB01274792-03
AB01274792-01
DR7 ,
reyataz
atazanavir (inn)
D07471
(3s,8s,9s,12s)-3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5, 6,10,13-pentaazatetradecanedioic acid dimethyl ester
bms-232632
zrivada
198904-31-3
methyl n-[(1s)-1-[[(1s,2s)-1-benzyl-2-hydroxy-3-[[[(2s)-2-(methoxycarbonylamino)-3,3-dimethyl-butanoyl]amino]-[[4-(2-pyridyl)phenyl]methyl]amino]propyl]carbamoyl]-2,2-dimethyl-propyl]carbamate
reyataz(tm) (*1:1 sulfate*)
cgp-73547
atazanavir
(2s)-n-(3-{[(2s)-2-(methoxycarbonylamino)-3,3-dimethylbutanoylamino][(4-(2-pyridyl)phenyl)methyl]amino}(1s,2s)-2-hydroxy-1-benzylpropyl)-2-(methoxycarbonylamino)-3,3-dimethylbutanamide
ATV ,
latazanavir
methyl n-[(1s)-1-{[(2s,3s)-3-hydroxy-4-[(2s)-2-[(methoxycarbonyl)amino]-3,3-dimethyl-n''-{[4-(pyridin-2-yl)phenyl]methyl}butanehydrazido]-1-phenylbutan-2-yl]carbamoyl}-2,2-dimethylpropyl]carbamate
cgp 73547
DB01072
bdbm13934
methyl n-[(1s)-1-[[(2s,3s)-3-hydroxy-4-[[[(2s)-2-(methoxycarbonylamino)-3,3-dimethyl-butanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenyl-butan-2-yl]carbamoyl]-2,2-dimethyl-propyl]carbamate
chembl1163 ,
2AQU
reyataz (tn)
hsdb 7339
2,5,6,10,13-pentaazatetradecanedioic acid, 3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-((4-(2-pyridinyl)phenyl)methyl)-, dimethyl ester, (3s,8s,9s,12s)-
2,5,6,10,13-pentaazatetradecanedioic acid, 3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-((4-(2-pyridinyl)phenyl)methyl)-, dimethyl ester, (3s-(3r*,8r*,9r*,12r*))-
atazanavir [inn:ban]
dimethyl (3s,8s,9s,12s)-9-benzyl-3,12-di-tert-butyl-8-hydroxy-4,11-dioxo-6-[4-(2-pyridyl)benzyl]-2,5,6,10,13-pentaazatetradecanedioate
CHEBI:37924 ,
atazanavirum
HMS2089P22
methyl n-[(2s)-1-[2-[(2s,3s)-2-hydroxy-3-[[(2s)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
A25022
atazanavir;(2s)-n-(3-{[(2s)-2-(methoxycarbonylamino)-3,3-dimethylbutanoylamino][(4-(2-pyridyl)phenyl)methyl]amino}(1s,2s)-2-hydroxy-1-benzylpropyl)-2-(methoxycarbonylamino)-3,3-dimethylbutanamide
NCGC00182552-01
unii-qzu4h47a3s
qzu4h47a3s ,
tox21_113081
dtxcid5028617
cas-198904-31-3
dtxsid9048691 ,
methyl n-[(1s)-1-{n'-[(2s,3s)-2-hydroxy-3-[(2s)-2-[(methoxycarbonyl)amino]-3,3-dimethylbutanamido]-4-phenylbutyl]-n'-{[4-(pyridin-2-yl)phenyl]methyl}hydrazinecarbonyl}-2,2-dimethylpropyl]carbamate
HY-17367
atv & hsa
NCGC00182552-03
atazanavir & alpha1-acid glycoprotein
atv & aag
atazanavir [who-dd]
dimethyl (3s,8s,9s,12s)-9-benzyl-3,12,di-tert-butyl-8-hydroxy-4,11-dioxo-6-(p-2-pyridylbenzyl)-2,5,6,10,13-pentaazatetradecanedioate
atazanavir [inn]
atazanavir [vandf]
atazanavir [mi]
atazanavir [hsdb]
2,5,6,10,13-pentaazatetradecanedioic acid, 3-12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-((-4-(2-pyridinyl)phenyl)methyl)-, dimethyl ester, (3s,8s,9s,12s)-
CS-0945
3,4-dinitrobenzylalcohol
SCHEMBL41696
NCGC00182552-02
tox21_113081_1
AB01274792-02
AXRYRYVKAWYZBR-GASGPIRDSA-N
atazanavir base
atazanavir, >=98% (hplc)
methyl ((5s,8s,9s,14s)-8-benzyl-5-(tert-butyl)-9-hydroxy-15,15-dimethyl-3,6,13-trioxo-11-(4-(pyridin-2-yl)benzyl)-2-oxa-4,7,11,12-tetraazahexadecan-14-yl)carbamate
methyl n-[(2s)-1-[[(2s,3s)-3-hydroxy-4-[[[(2s)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenylbutan-2-yl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
AB01274792_04
AKOS025396423
J-519602
SR-01000930924-2
sr-01000930924
mfcd08435966
gtpl11138
1,14-dimethyl (3s,8s,9s,12s)-3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,6,10,13-pentaazatetradecanedioate
methyl [(1s,4s,5s,10s)-4-benzyl-1,10-di-tert-butyl-5-hydroxy-2,9,12-trioxo-7-(4-pyridin-2-ylbenzyl)-13-oxa-3,7,8,11-tetraazatetradec-1-yl]carbamate (non-preferred name)
6,10,13-pentaazatetradecanedioic acid dimethyl ester
(3s,8s,9s,12s)-3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-2,5,
S4662
BS-16315
Q423467
atazanavir,bisulfatesalt
methyl n-[(2s)-1-[[(2s,3s)-3-hydroxy-4-[[[(2s)-2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-[(4-pyridin-2-ylphenyl)methyl]amino]-1-phenylbutan-2-yl]ami
AMY31160
CCG-270390
NCGC00182552-14
methyl n-[1-[2-[2-hydroxy-3-[[2-(methoxycarbonylamino)-3,3-dimethylbutanoyl]amino]-4-phenylbutyl]-2-[(4-pyridin-2-ylphenyl)methyl]hydrazinyl]-3,3-dimethyl-1-oxobutan-2-yl]carbamate
EN300-20600002
dimethyl (3s,8s,9s,12s)-9-benzyl-3,12-di-tert-butyl-8-hydroxy-4,11-dioxo-6-(4-(2-pyridyl)benzyl)-2,5,6,10,13-pentaazatetradecanedioate
j05ae08
Z1258932192

Research Excerpts

Overview

Atazanavir (ATV) is an antiretroviral drug of the protease inhibitor class. It has high protein binding in human plasma.

ExcerptReferenceRelevance
"Atazanavir is an HIV-1 protease inhibitor with high protein binding in human plasma. "( Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
Barrail-Tran, A; Chazallon, C; Cosson, C; Gérard, L; Girard, PM; Mentré, F; Piketty, C; Taburet, AM, 2010
)
2.04
"Atazanavir (ATV) is an antiretroviral drug of the protease inhibitor class. "( CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
Li, F; Lu, J; Ma, X; Wang, L, 2011
)
2.06

Toxicity

ExcerptReferenceRelevance
" Although safe and generally well tolerated, 300 mg or 400 mg atazanavir administered every 12 h did not maintain adequate plasma exposure when coadministered with rifampin."( Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
Acosta, EP; Agarwala, S; Alston-Smith, B; Bertz, R; Child, M; Gerber, JG; Haas, DW; Hosey, L; Kendall, MA; Koletar, SL; Zolopa, AR, 2007
)
0.8

Pharmacokinetics

ExcerptReferenceRelevance
" We performed an open-label, single-arm study to assess the safety and pharmacokinetic interactions of the HIV protease inhibitor atazanavir coadministered with rifampin."( Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
Acosta, EP; Agarwala, S; Alston-Smith, B; Bertz, R; Child, M; Gerber, JG; Haas, DW; Hosey, L; Kendall, MA; Koletar, SL; Zolopa, AR, 2007
)
0.77

Compound-Compound Interactions

ExcerptReferenceRelevance
" When brecanavir was tested in combination with nucleoside reverse transcriptase inhibitors, the antiviral activity of brecanavir was synergistic with the effects of stavudine and additive to the effects of zidovudine, tenofovir, dideoxycytidine, didanosine, adefovir, abacavir, lamivudine, and emtricitabine."( 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.
Boone, L; Craig, C; Ferris, R; Furfine, E; Griffin, P; Hale, M; Hanlon, M; Harvey, R; Hazen, R; Kaldor, I; Miller, J; Ray, J; Samano, V; Spaltenstein, A; St Clair, M; Tung, R; Yates, P, 2007
)
0.34
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
" Acylation of the (hydroxethyl)hydrazine dipeptide isostere with the L-tert-leucine derivative 29 increased the oral bioavailability significantly when compared to the corresponding L-valine or L-isoleucine derivatives."( New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
Acemoglu, F; Beck, W; Bold, G; Boss, E; Capraro, HG; Cozens, R; Eschbach, M; Fässler, A; Hürlimann, T; Klimkait, T; Lang, M; Lazdins, J; Masso, E; Mestan, J; Poncioni, B; Rösel, J; Roussel, S; Stover, D; Tintelnot-Blomley, M; Ucci-Stoll, K; Wyss, D, 1998
)
0.3
" Modification of the core regiochemistry and stereochemistry significantly affected the potency, metabolic stability, and oral bioavailability of the inhibitors, as did the variation of a pendent arylmethyl P3 group."( 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.
Chen, HJ; Colletti, L; Degoey, DA; Dekhtyar, T; Flentge, CA; Flosi, WJ; Grampovnik, DJ; Kati, WM; Kempf, DJ; Klein, LL; Mamo, M; Marsh, KC; Mo, H; Molla, A; Morfitt, DC; Nguyen, B; Randolph, JT; Schmidt, JM; Stoll, V; Swanson, SJ; Yeung, CM, 2009
)
0.35
" This afforded a series of potent orally bioavailable inhibitors of which MK-8718 was identified as a compound with a favorable overall profile."( Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
Bahnck-Teets, C; Ballard, JE; Beaulieu, C; Bennett, DJ; Bungard, CJ; Carroll, SS; Chang, RK; Crane, SN; Diamond, TL; Dubost, DC; Fay, JF; Felock, PJ; Gesell, JJ; Greshock, TJ; Hao, L; Holloway, MK; Manikowski, JJ; McCauley, JA; McKay, DJ; Miller, M; Min, X; Molinaro, C; Moradei, OM; Nadeau, C; Nantermet, PG; Sanchez, RI; Satyanarayana, T; Shipe, WD; Singh, SK; Su, HP; Truong, VL; Vacca, JP; Vijayasaradhi, S; Williams, PD; Wiscount, CM, 2016
)
0.43
" However, they are characterized by poor oral bioavailability and a need for boosting with a pharmacokinetic enhancer, which results in additional drug-drug interactions that are sometimes difficult to manage."( Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
Annadurai, M; Arla, R; Bhutani, P; Desai, SD; Jenkins, SM; Kadow, JF; Krystal, MR; Mandlekar, S; Meanwell, NA; Padmanabhan, S; Ramar, T; Sarabu, R; Sinha, S; Sridhar, S; Subbaiah, MAM; Subramani, L; Subramanian, M; Wang, C, 2018
)
0.69
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The subjects had 11 plasma samples drawn over a dosing interval on days 1, 15, and 30."( Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
Cruttenden, K; DiCenzo, R; Gelbard, H; Hochreiter, J; Mariuz, P; Peterson, DR; Rezk, NL; Schifitto, G, 2008
)
0.59
" We investigated a chemo-activated, acyl migration-based prodrug design approach to improve the pharmacokinetic profile of 1 but failed to obtain improved oral bioavailability over dosing the parent drug in rats."( Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
Annadurai, M; Arla, R; Bhutani, P; Desai, SD; Jenkins, SM; Kadow, JF; Krystal, MR; Mandlekar, S; Meanwell, NA; Padmanabhan, S; Ramar, T; Sarabu, R; Sinha, S; Sridhar, S; Subbaiah, MAM; Subramani, L; Subramanian, M; Wang, C, 2018
)
0.69
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
HIV protease inhibitorAn inhibitor of HIV protease, an enzyme required for production of proteins needed for viral assembly.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
carbohydrazideA hydrazide consisting of hydrazine carrying one or more carboacyl groups.
[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 Targets (39)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.29850.006038.004119,952.5996AID1159521
GLI family zinc finger 3Homo sapiens (human)Potency2.98490.000714.592883.7951AID1259369
AR proteinHomo sapiens (human)Potency24.38220.000221.22318,912.5098AID743035; AID743063
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency11.88320.001022.650876.6163AID1224838
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.23020.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency4.68590.001310.157742.8575AID1259253
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency29.84930.001530.607315,848.9004AID1224849
estrogen nuclear receptor alphaHomo sapiens (human)Potency26.60320.000229.305416,493.5996AID743079
GVesicular stomatitis virusPotency10.96400.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency43.64860.00108.379861.1304AID1645840
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.95210.001019.414170.9645AID743094
Histone H2A.xCricetulus griseus (Chinese hamster)Potency27.84740.039147.5451146.8240AID1224845; AID1224896
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.60320.000323.4451159.6830AID743065; AID743067
Interferon betaHomo sapiens (human)Potency10.96400.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.70790.009610.525035.4813AID1479145
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.96400.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HIV-1 ProteaseHuman immunodeficiency virus 1Ki0.00050.00050.00050.0005AID977610
Chain B, HIV-1 ProteaseHuman immunodeficiency virus 1Ki0.00050.00050.00050.0005AID977610
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC50 (µMol)5.20000.55003.70836.1000AID699544
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki5.10000.53004.11578.4800AID699544
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (BRU ISOLATE)Ki0.00060.00000.08283.3000AID1797110
Gag-Pol polyproteinHIV-1 M:B_ARV2/SF2Ki0.00030.00000.01090.0895AID1797666
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (RF/HAT ISOLATE)Ki0.00060.00000.05051.6160AID1797110
ATP-dependent translocase ABCB1Homo sapiens (human)IC50 (µMol)67.80000.00022.318510.0000AID416864
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)67.80000.00021.874210.0000AID416864
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50 (µMol)0.37500.30003.25807.3000AID1593734; AID1886611; AID1886612
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)67.80000.00021.270410.0000AID416864
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (STRAIN UGANDAN / ISOLATE U455)Ki0.00060.00000.05051.6160AID1797110
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)67.80000.00001.819410.0000AID416864
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)30.00000.00091.901410.0000AID1886657
UDP-glucuronosyltransferase 1A1 Rattus norvegicus (Norway rat)IC50 (µMol)4.20004.20004.20004.2000AID1593736
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)0.02600.00011.076810.0000AID198568
Protease Human immunodeficiency virus 1IC50 (µMol)0.00400.00010.22487.3200AID618426
Protease Human immunodeficiency virus 1Ki0.00030.00000.04433.1000AID238682; AID343015; AID343016; AID343017; AID343018; AID343019; AID343020; AID343021
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50 (µMol)0.40000.10472.71957.0795AID699543
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki0.37000.08002.46889.8000AID699543
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)69.10000.00401.966610.0000AID1873200
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50 (µMol)1.40000.05002.37979.7000AID699542
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki1.30000.04401.36305.0000AID699542
Protease Human immunodeficiency virus 1IC50 (µMol)0.00170.00000.81769.8500AID1314231; AID1504971; AID1593754; AID590915; AID664437
Protease Human immunodeficiency virus 1Ki0.00100.00000.02841.1000AID321338; AID321660; AID343014; AID374591; AID443165; AID661001
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protease Human immunodeficiency virus 1Kd0.00040.00010.04120.5770AID238043
Protease Human immunodeficiency virus 1EC50 (µMol)0.00070.00070.69422.7300AID1375430
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminHomo sapiens (human)KD2599.00006.00006.00006.0000AID239810
Protease Human immunodeficiency virus 1ED500.00140.00140.41032.4700AID106906
Protease Human immunodeficiency virus 1ED900.00300.00300.03770.1000AID106913
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (123)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
G2/M transition of mitotic cell cycleATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic metabolic processATP-dependent translocase ABCB1Homo sapiens (human)
response to xenobiotic stimulusATP-dependent translocase ABCB1Homo sapiens (human)
phospholipid translocationATP-dependent translocase ABCB1Homo sapiens (human)
terpenoid transportATP-dependent translocase ABCB1Homo sapiens (human)
regulation of response to osmotic stressATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
transepithelial transportATP-dependent translocase ABCB1Homo sapiens (human)
stem cell proliferationATP-dependent translocase ABCB1Homo sapiens (human)
ceramide translocationATP-dependent translocase ABCB1Homo sapiens (human)
export across plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
positive regulation of anion channel activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transportATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transport across blood-brain barrierATP-dependent translocase ABCB1Homo sapiens (human)
regulation of chloride transportATP-dependent translocase ABCB1Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (65)

Processvia Protein(s)Taxonomy
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
protein bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATP bindingATP-dependent translocase ABCB1Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
efflux transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ATP hydrolysis activityATP-dependent translocase ABCB1Homo sapiens (human)
transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
ubiquitin protein ligase bindingATP-dependent translocase ABCB1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
carboxylic acid transmembrane transporter activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylcholine floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
phosphatidylethanolamine flippase activityATP-dependent translocase ABCB1Homo sapiens (human)
ceramide floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
floppase activityATP-dependent translocase ABCB1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (40)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
cytoplasmATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
cell surfaceATP-dependent translocase ABCB1Homo sapiens (human)
membraneATP-dependent translocase ABCB1Homo sapiens (human)
apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
extracellular exosomeATP-dependent translocase ABCB1Homo sapiens (human)
external side of apical plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
plasma membraneATP-dependent translocase ABCB1Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (776)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1797110Protease 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.\\2006Biochemistry, 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.
AID1797666Enzyme Inhibition Assay from Article 10.1021/jm070284z: \\Design and Synthesis of HIV-1 Protease Inhibitors Incorporating Oxazolidinones as P2/P2' Ligands in Pseudosymmetric Dipeptide Isosteres.\\2007Journal 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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID572561AUC in HIV-1 infected patient at 300 mg, po qd coadministered with 100 mg of ritonavir, po qd and NRTI2008Antimicrobial 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.
AID519548Antiviral 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 asse2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID279176Ratio of intracellular drug level to extracellular drug level in CEM CCL19 cells at 20 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID519786Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID321685Antiviral activity against wild type HIV12008Bioorganic & 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.
AID81431Antiviral activity against HIV-1 protease inhibitor-resistant strain(indinavir resistant) of the HI virus(L10R,M46I,L63P,V82T,I84V)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID246965Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID546991Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position M46I, I50L, N88S mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assa2010Antimicrobial 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.
AID1886651Cmax in Sprague-Dawley rat at 1 mg/kg,iv measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID321664Cmax in Beagle dog at 15 mg/kg, po2008Bioorganic & 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.
AID372189Resistance 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 assay2007Antimicrobial 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.
AID519556Antiviral 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 fr2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID668816Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID564043Antiviral 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 assay2010Antimicrobial 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.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1380929Resistance 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 cells2018Journal 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.
AID519554Antiviral 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, 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID521549Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID322097Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1216284Drug excretion in wildtype mouse feces assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2-hydroxymethyl-2-methyl-propyl)-carbamic acid me2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID1216289Drug metabolism in human liver microsomes assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazino]-propylcarbamoyl}-2,2-dimethyl-propyl)-carbamic acid methyl ester formation at 50 mg/kg, po by LC-MS2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID279178Ratio of intracellular drug level to extracellular drug level in human PBMC at 2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID374604Resistance 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 assay2007Antimicrobial 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.
AID726412Selectivity 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 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID519542Antiviral 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 infectio2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID278955Antiviral activity against HIV1 A3 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID374639Resistance 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 assay2007Antimicrobial 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.
AID1593673Tmax in cannulated Sprague-Dawley rat at 3 mg/kg administered orally by UPLC/MS/MS analysis2019Journal 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.
AID368660Toxicity in HIV-negative human assessed as hemoglobin level at 300 mg, po administered every 12 hrs administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1216282Drug excretion in wildtype mouse feces assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2,2-dimethyl-propyl)-carbamic acid methyl ester f2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID586621Ratio of EC50 for HIV1 harboring HIV1 harboring wild type 8.9NSX with gag T81A and Y76K mutant to EC50 for wild type HIV12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID1593666Aqueous solubility of the compound in pH 7.4 phosphate buffer by RP-UPLC analysis2019Journal 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.
AID1706647Solubility of compound in phosphate buffer at pH 6.52020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID1886561Aqueous solubility of compound at pH 6.5 by UPLC analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID322116Antiviral activity against HIV1 MDR/B X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1504971Inhibition of HIV1 protease expressed in Escherichia coli using Val-Ser-Gln-Asn-(beta-naphtyl)Ala-Pro-Ile-Val as substrate preincubated for 30 mins followed by substrate addition measured after 1 hr by mass spectrometric method2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
AID586623Antiviral 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 assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID368459Cmax in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID297668Inhibition of HIV1 Protease M1 variant by FRET based assay2007Journal 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.
AID415247Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID279171Increase in accumulation of the drug in CEM CCL19 cells in presence of 50 uM Verapamil relative to control2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID519541Antiviral 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 meas2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID263208Antiviral activity against HIV1 EP13 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID278962Antiviral activity against HIV1 A10 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID321338Inhibition of HIV1 protease expressed in Escherichia coli2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
AID572564Apparent oral clearance in HIV-1 infected patient at 300 mg, po qd coadministered with 400 mg, po bid and 100 mg, po bid of Lopinavir and ritonavir respectively2008Antimicrobial 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.
AID557291Antiviral 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 ELISA2009Antimicrobial 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.
AID1607529Antiviral activity against lopinavir resistant HIV1 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as inhibition of p24 Gag production2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID369944Ratio of EC50 for HIV2 MS to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID1593759Oral bioavailability in dog2019Journal 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.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID374617Resistance 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 assay2007Antimicrobial 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.
AID124202Drug concentration in blood sample was analyzed by reversed phase HPLC 30 min (c30) after oral application of 120 mg/kg in a standardized formulation1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID368667Toxicity in gilbert's genotype lacking human assessed as bilirubin level at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID372188Resistance 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 assay2007Antimicrobial 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.
AID566849Antiviral activity against HIV-1 MDR/G infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID249499Toxicity value against wild type HIV-1 IIIB was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID322120Antiviral activity against HIV1 92UG037 subtype A R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID321687Antiviral activity against HIV1 mutant strain 22008Bioorganic & 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.
AID322099Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID242866Dissociation rate constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID1706654AUClast in Sprague-Dawley rat at 3 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID279168Intracellular drug level in human PBMC at 0.2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID519553Antiviral 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 vir2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID242933Dissociation rate constant for the interaction between the compound and serum albumin2005Journal 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.
AID519783Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID374626Resistance 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 assay2007Antimicrobial 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.
AID322102Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1886559Aqueous solubility of compound at pH 1 by UPLC analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID547238Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease polymorphism at M36 position and I50FILV, A71V mutant gene to EC50 for wild type HIV1 subtype CRF02_AG2010Antimicrobial 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.
AID519543Antiviral 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 in2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1375411Cmax in Sprague-Dawley rat at 3 mg/kg, po after 0.25 to 24 hrs by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID343017Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID519544Antiviral 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 mutation2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID368462Drug level in HIV-negative human serum at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs measured at 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1380924Antiviral 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 immunoassay2018Journal 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.
AID417047Inhibition of esterase mediated-hydrolysis of tenofovir disoproxil fumarate in human intestinal sub cellular fraction S9 at 2 uM after 30 mins2007Antimicrobial 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.
AID278970Antiviral activity against HIV1 C3 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID1216275Drug level assessed as human CYP3A4-mediated (S)-methyl 3,3-dimethyl-1-oxo-1-(2-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ylcarbamate formation treated with 50 uM atazanavir by UPLC-TOFMS system2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID1706660Trough plasma concentration in Sprague-Dawley rat at 30 mg/kg, po measured after 24 hrs2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID566850Antiviral activity against HIV-1 MDR/TM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID368672Cmin in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID81430Antiviral activity against HIV-1 protease inhibitor-resistant strain(Wild type) of the HI virus1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID368657Toxicity in HIV-negative human assessed as creatinine levels at 300 mg, po administered every 12 hrs administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID369946Ratio of EC50 for HIV2 CDC310319 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID278971Antiviral activity against HIV1 C4 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID1409310Antiviral 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 immunoassay2018Journal 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.
AID459083Ratio of IC50 for multi drug-resistant HIV1 isolate of subtype TM to IC50 for wild type HIV1 isolate ERS104pre2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID372183Resistance 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 assay2007Antimicrobial 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.
AID661004Apparent permeability from apical to basolateral side in human Caco2 cells after 60 mins2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.
AID372186Resistance 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 assay2007Antimicrobial 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.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1593657Half life in pH 6.5 30%CH3CN/phosphate buffer at 50 mM by RP-UPLC analysis2019Journal 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.
AID496579Absorption rate constant in human by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID1593736Inhibition of recombinant rat UGT1A1 using beta-estradiol as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis2019Journal 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.
AID543386Half life in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID496583Half life in patient with elevated alpha-1- glycoprotein acid level by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID1593730Prodrug conversion in mesenteric vein plasma of closed loop rat intestinal model assessed as atazanavir recovery at 1 mg/kg administered as cassette dose by LC/MS analysis2019Journal 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.
AID374609Resistance 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 assay2007Antimicrobial 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.
AID321663AUC in Beagle dog at 15 mg/kg, po2008Bioorganic & 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.
AID343023Ratio of Ki for HIV1 recombinant protease M46I/A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID459079Antiviral activity against wild type HIV1 isolate ERS104pre in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID532463Antiviral 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,2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID519787Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID532655Antiviral 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 infecte2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1725418Antiviral activity against HIV1 NL4-3 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID396260Antiviral activity against HIV1 NL4-32007Antimicrobial 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.
AID1375435Half life in rat whole blood at 1 uM after 5 to 90 mins by UPLC-MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID1593738Inhibition of UGT1A1 in rat liver microsomes using beta-estradiol as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis2019Journal 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.
AID368675Cmax in HIV-negative human at 400 mg administered every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID519577Antiviral 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 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID532454Antiviral 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 mutant2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID525171Antimicrobial 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 inocu2008Antimicrobial 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.
AID1482909Antiviral 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 immunoassay2017Journal 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.
AID519792Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID278958Antiviral activity against HIV1 A6 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID519784Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID699542Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting2012Journal 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.
AID372182Resistance 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 assay2007Antimicrobial 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.
AID417036Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated healthy human assessed as change in plasma Cmin of tenofovir at 300 mg, po, QD co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial 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.
AID532455Antiviral 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 r2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1216296Drug excretion in wildtype mouse urine assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2-hydroxymethyl-2-methyl-propyl)-carbamic acid me2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID28083Cmax value at the period of 0-24 h after dosing.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID1593675AUClast in cannulated Sprague-Dawley rat at 3 mg/kg administered orally by UPLC/MS/MS analysis2019Journal 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.
AID368466AUC (24 hrs) in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID279174Ratio of intracellular drug level to extracellular drug level in CEM CCL19 cells at 0.2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID519791Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID368456Tmax in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID532459Antiviral 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-assa2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1886653Cmin in Sprague-Dawley rat at 1 mg/kg,iv measured after 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID321665Tmax in Beagle dog at 15 mg/kg, po2008Bioorganic & 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.
AID564037Antiviral 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 assay2010Antimicrobial 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.
AID322104Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID519782Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID557296Ratio of EC50 for HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID564063Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay2010Antimicrobial 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.
AID1593708Aqueous solubility of the compound in pH 4 citrate buffer by RP-UPLC analysis2019Journal 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.
AID557297Ratio of EC50 for HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID532461Antiviral 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 I92010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID519788Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID459078Antiviral activity against multi drug-resistant HIV1 isolate of subtype JSL in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID1375438AUC (0 to 24 hrs) in pentagastrin treated Sprague-Dawley rat at 10 mg/kg, po by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID374625Resistance 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 assay2007Antimicrobial 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.
AID1482926Ratio 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 cells2017Journal 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.
AID322110Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1886650Ratio of Cmax/Cmin in Sprague-Dawley rat at 1 mg/kg,iv measured after 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID278973Antiviral activity against HIV1 C6 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID343026Ratio of Ki for HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID668811Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID1706639Dissociation constant, pKa of compound2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID369951Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID1380928Resistance 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 2018Journal 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.
AID1375409Solubility of the compound in acetate buffer at pH 4 at 25 degC by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID726413Selectivity 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 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1380927Antiviral 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 immunoassay2018Journal 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.
AID575064Antiviral activity against Human immunodeficiency virus 1 harboring M46I and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial 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.
AID1593748Prodrug conversion in pH 6.5 30%CH3CN/phosphate buffer assessed as atazanavir formation at 50 mM measured after 60 mins by RP-UPLC analysis2019Journal 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.
AID543379Cmax in HIV-infected patient at 300 mg, qd2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID668810Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID322105Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID586627Antiviral 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 assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID1593659Aqueous solubility of the compound in pH 4 acetate buffer by RP-UPLC analysis2019Journal 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.
AID532457Antiviral 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,2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374631Resistance 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 assay2007Antimicrobial 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.
AID532456Antiviral 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-2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374612Resistance 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 assay2007Antimicrobial 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.
AID557286Antiviral 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 ELISA2009Antimicrobial 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.
AID1216285Drug excretion in wild type mouse feces assessed as methyl (S)-1-(2-((2S,3S)-3-((S)-2-amino-3,3-dimethylbutanamido)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/MS 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID374623Resistance 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 assay2007Antimicrobial 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.
AID1593732Prodrug conversion in intestinal content of closed loop rat intestinal model assessed as atazanavir recovery at 1 mg/kg administered as cassette dose by LC/MS analysis2019Journal 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.
AID575062Antiviral 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 type2010Antimicrobial 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.
AID368654Toxicity in HIV-negative human assessed as alanine aminotransferase levels at 300 mg, po administered every 12 hrs administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID368658Toxicity in HIV-negative human assessed as creatinine levels at 400 mg, po administered every 12 hrs coadministered with 400 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID532460Antiviral 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, I2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374635Resistance 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 assay2007Antimicrobial 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.
AID1706652Cmax in Sprague-Dawley rat at 3 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID20788Orally bioavailability in rats2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID322114Antiviral activity against HIV1 MDR/MM R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID532468Antiviral 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, I2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1593757Drug recovery in feces of po dosed human2019Journal 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.
AID519578Antiviral 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 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID532473Antiviral 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 M2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID566851Antiviral activity against HIV-1 MDR/MM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID1593658Aqueous solubility of the compound in pH 1 HCl buffer by RP-UPLC analysis2019Journal 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.
AID525166Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy2008Antimicrobial 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.
AID1593747Prodrug conversion in pH 6.5 30%CH3CN/phosphate buffer assessed as atazanavir formation at 50 mM measured after 30 mins by RP-UPLC analysis2019Journal 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.
AID278974Antiviral activity against HIV1 C7 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID321688Antiviral activity against HIV1 mutant strain 32008Bioorganic & 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.
AID279177Ratio of intracellular drug level to extracellular drug level in human PBMC at 0.2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID1593655Half life in pH 1 30%CH3CN/HCl buffer at 50 mM by RP-UPLC analysis2019Journal 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.
AID279181Increase in accumulation of the drug in CEM CCL19 cells in presence of 24 uM Efavirenz relative to control2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID322103Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID532467Antiviral 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 I92010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID564047Antiviral 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 assay2010Antimicrobial 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.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1886582Ratio of Cmax/Cmin in Sprague-Dawley rat at 3 mg/kg,po measured after 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID278965Antiviral activity against HIV1 A13 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID1725421Antiviral activity against DRV resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID368464AUC (12 hrs) in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1216267Drug metabolism in human liver microsomes assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2,2-dimethyl-propyl)-carbamic acid methyl este2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID374603Resistance 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 assay2007Antimicrobial 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.
AID496587Half life in patient with => 40 IU/liter ALAT level by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID547012Selectivity ratio of EC50 for HIV1 subtype B harboring protease D30N, M46I, A71T and V77I and polymorphism at M36 position mutant gene to EC50 for wild type HIV1 subtype B2010Antimicrobial 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.
AID368471Terminal apparent distribution volume in HIV-negative human serum at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID374611Resistance 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 assay2007Antimicrobial 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.
AID278977Antiviral activity against HIV1 C10 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID673377Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M5 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID246319Protease inhibitory activity against HIV-1 r13034 mutant strain was determined; (not determined)2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID1380930Resistance 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 cells2018Journal 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.
AID443165Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay2010Journal 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.
AID572567Cmax in HIV-1 infected patient at 300 mg, po qd coadministered with 400 mg, po bid and 100 mg, po bid of Lopinavir and ritonavir respectively2008Antimicrobial 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.
AID279173Decrease in accumulation of the drug in CEM CCL19 cells in presence of 28 uM Nevirapine relative to control2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID1482907Ratio 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 cells2017Journal 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.
AID374607Resistance 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 assay2007Antimicrobial 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.
AID322111Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID374629Resistance 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 assay2007Antimicrobial 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.
AID1593707Aqueous solubility of the compound in pH 3 buffer by RP-UPLC analysis2019Journal 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.
AID668815Cytotoxicity against human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID673367Inhibition of wild type Human immunodeficiency virus protease expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.52012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID1886575AUClast in Sprague-Dawley rat at 30 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID519790Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID278963Antiviral activity against HIV1 A11 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID278966Antiviral activity against HIV1 A14 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID372191Resistance 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 assay2007Antimicrobial 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.
AID496575Apparent oral clearance in human by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID374637Resistance 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 assay2007Antimicrobial 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.
AID321666Volume of distribution at steady state in Beagle dog at 15 mg/kg, iv2008Bioorganic & 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.
AID322101Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay2007Antimicrobial 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.
AID564046Antiviral 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 assay2010Antimicrobial 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.
AID547016Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and I50FILV, A71V mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter g2010Antimicrobial 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.
AID658567Resistance factor, ratio of EC50 for multidrug-resistant HIV1 106-PR infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells2012Journal 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.
AID543374Cmin in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID668817Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID416864Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells2007Antimicrobial 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.
AID369953Antiviral 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 assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID368676AUC (24hrs) in HIV-negative human at 400 mg administered every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID368670Cmax in HIV-negative human at 300 mg coadministered with 100 mg of ritonavir every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID374624Resistance 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 assay2007Antimicrobial 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.
AID1216280Drug excretion in wild type mouse urine assessed as (S)-methyl 3,3-dimethyl-1-oxo-1-(2-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/MS analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID547233Selectivity ratio of EC50 for HIV1 subtype C harboring protease L23I, M46I/M, L89T mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype C2010Antimicrobial 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.
AID1593753Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells2019Journal 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.
AID1607527Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID532474Antiviral 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 re2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID322112Antiviral activity against wild type HIV1 ERS104prc X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID532478Antiviral 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 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID322098Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID368661Toxicity in HIV-negative human assessed as hemoglobin level at 400 mg, po administered every 12 hrs coadministered with 400 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID572563Cmin in HIV-1 infected patient at 300 mg, po qd coadministered with 100 mg of ritonavir, po qd and NRTI2008Antimicrobial 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.
AID416865Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated healthy human assessed as change in plasma AUC of tenofovir at 300 mg, po, QD co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial 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.
AID519780Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID557292Antiviral 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 E2009Antimicrobial 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.
AID239819Association rate constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID1593755Antiviral activity against HIV1 NL4-3 infected in human MT2 cells assessed as reduction in viral yield measured after 4 days by EnduRen live cell substrate based luciferase reporter gene assay2019Journal 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.
AID459085Ratio of IC50 for multi drug-resistant HIV1 isolate of subtype JSL to IC50 for wild type HIV1 isolate ERS104pre2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID198568The percent reduction of the reverse transcriptase (RT) activity in HIV-1/MN-infected MT-2 cells.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID496585AUC in patient with elevated alpha-1- glycoprotein acid level by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID564042Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay2010Antimicrobial 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.
AID1593735Inhibition of recombinant cynomolgus monkey UGT1A1 using bilirubin as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis2019Journal 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.
AID368655Toxicity in HIV-negative human assessed as alanine aminotransferase levels at 400 mg, po administered every 12 hrs coadministered with 400 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1375430Inhibition of HIV1 NL4-3 protease assessed as decrease in viral replication in human MT2 cells after 4 days by luciferase reporter gene assay2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID726416Antiviral 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 replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID343027Ratio 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 coli2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID673368Inhibition of Human immunodeficiency virus protease M8 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.52012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID496582Half life in patient with elevated alpha-1- glycoprotein acid level by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID368460Drug level in HIV-negative human serum at 300 mg, po administered every 12 hrs measured at 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID519795Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID374615Resistance 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 assay2007Antimicrobial 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.
AID1593762Dissociation constant, pKa of the compound2019Journal 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.
AID1216268Drug metabolism in human liver microsomes assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2-hydroxymethyl-2-methyl-propyl)-carbamic acid2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID1216287Drug excretion in wild type mouse assessed as (S)-methyl 3,3-dimethyl-1-oxo-1-(2-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/MS analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID1482921Antiviral 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 2017Journal 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.
AID699541Inhibition 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 counting2012Journal 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.
AID321669Plasma concentration in Beagle dog at 15 mg/kg, po after 12 hrs2008Bioorganic & 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.
AID372184Resistance 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 assay2007Antimicrobial 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.
AID1593711Aqueous solubility of the compound in FeSSIF by RP-HPLC analysis2019Journal 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.
AID297671Antiviral activity against HIV1 infected MT4 cells by MTT method2007Journal 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.
AID543375Cmin in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline and 250 mg valporic acid, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID519547Antiviral 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 redu2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID586625Antiviral 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 assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID368673Cmin in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID278972Antiviral activity against HIV1 C5 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID368669Cmin in HIV-negative human at 300 mg coadministered with 100 mg of ritonavir every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID374605Resistance 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 assay2007Antimicrobial 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.
AID396238Antiviral activity against HIV1 BaL in human PBMC assessed as blockade of reverse transcriptase activity2007Antimicrobial 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.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID321662Antiviral activity against HIV1 3B in presence of 50% human serum2008Bioorganic & 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.
AID368662Toxicity in HIV-negative human assessed as bilirubin level at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID557285Antiviral 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 ELISA2009Antimicrobial 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.
AID368463AUC (12 hrs) in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID557298Ratio of EC50 for HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID519793Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID372192Resistance 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 assay2007Antimicrobial 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.
AID279175Ratio of intracellular drug level to extracellular drug level in CEM CCL19 cells at 2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID1482922Ratio 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 cells2017Journal 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.
AID1706658Tmax in Sprague-Dawley rat at 30 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID368474Apparent oral clearance in HIV-negative human serum at 300 mg, po administered every 12 hrs coadministered with 400 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID328878Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 48 hrs by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID576054Cmin in HIV infected patient at 400 mg qd measured after 13.06 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID668813Selectivity 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 protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID459075Antiviral activity against multi drug-resistant HIV1 isolate of subtype G in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID519555Antiviral 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 fr2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID572568Cmin in HIV-1 infected patient at 300 mg, po qd coadministered with 400 mg, po bid and 100 mg, po bid of Lopinavir and ritonavir respectively2008Antimicrobial 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.
AID1607532Selectivity ratio of IC50 for antiviral activity against lopinavir resistant HIV1 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells to IC50 for antiviral activity against wild-type HIV1 NL4-32020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID278960Antiviral activity against HIV1 A8 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID321668Oral bioavailability in Beagle dog at 15 mg/kg2008Bioorganic & 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.
AID532476Antiviral 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, 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID246193Protease inhibitory activity against HIV-1 r13025 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID343021Inhibition 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 assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID459076Antiviral activity against multi drug-resistant HIV1 isolate of subtype TM in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID519794Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID1216272Drug level assessed as human CYP3A4-mediated ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazino]-propylcarbamoyl}-2,2-dimethyl-propyl)-carbamic acid methyl ester formation treated with 50 uM atazanavir by 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID321699Ratio of EC50 for HIV1 mutant strain 7 to EC50 for wild type HIV12008Bioorganic & 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.
AID557287Antiviral 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 ELISA2009Antimicrobial 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.
AID248600Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line2005Bioorganic & 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.
AID1504972Antiviral activity against HIV1 infected in GFP expressing human MT4 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% normal human serum2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors.
AID368472Apparent oral clearance in HIV-negative human serum at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1482923Ratio 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 cells2017Journal 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.
AID1593754Inhibition of HIV1 protease activity2019Journal 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.
AID321690Antiviral activity against HIV1 mutant strain 52008Bioorganic & 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.
AID328890Inhibition of farnesyl transferase2007Proceedings 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.
AID374633Resistance 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 assay2007Antimicrobial 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.
AID557288Antiviral 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 ELISA2009Antimicrobial 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.
AID726415Antiviral 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 replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID532657Antiviral 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 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1482927Ratio 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 cells2017Journal 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.
AID246160Protease inhibitory activity against wild type HIV-1 IIIB was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID557289Antiviral 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 ELISA2009Antimicrobial 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.
AID1314231Inhibition of wild-type HIV1 protease expressed in Escherichia coli assessed as reduction in product formation preincubated for 30 mins followed by addition of Val-Ser-Gln-Asn-(beta-naphtyl)Ala-Pro-Ile-Val as substrate measured after 1 hr2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
AID1886611Inhibition of human recombinant UGT1A1 using bilirubin as substrate incubated for 40 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID374600Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay2007Antimicrobial 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.
AID575063Antiviral activity against Human immunodeficiency virus 1 harboring M46I mutation in viral protease assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial 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.
AID1375408Solubility of the compound in 0.1 N aqueous HCl at pH 1 at 25 degC by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID673372Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M8 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID368458Cmax in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID322123Antiviral activity against HIV1 92TH019 R5 subtype E in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496574Binding affinity to human alpha-1-glycoprotein acid2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID673369Inhibition of Human immunodeficiency virus protease M9 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.52012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID297670Inhibition of HIV1 Protease M3 variant by FRET based assay2007Journal 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.
AID726417Cytotoxicity against human MT4 cells2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID278953Antiviral activity against HIV1 A1 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID1314232Antiviral activity against HIV-1 infected in human MT4 cells assessed as inhibition of viral infection measured after 72 hrs2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
AID546997Antiviral activity against HIV1 subtype C harboring protease L23I, M46I/M, L89T 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 gen2010Antimicrobial 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.
AID343028Ratio 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 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID368668AUC (24 hrs) in HIV-negative human at 300 mg coadministered with 100 mg of ritonavir every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1482915Antiviral 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 immunoassay2017Journal 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.
AID263209Antiviral activity against HIV D545701 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID521548Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID374606Resistance 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 assay2007Antimicrobial 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.
AID321692Antiviral activity against HIV1 mutant strain 72008Bioorganic & 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.
AID673378Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M6 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID246195Protease inhibitory activity against HIV-1 r13363 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID321697Ratio of EC50 for HIV1 mutant strain 5 to EC50 for wild type HIV12008Bioorganic & 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.
AID369955Ratio of EC50 for HIV2 ROD with protease G17N mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID564038Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay2010Antimicrobial 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.
AID1706656Oral bioavailability in Sprague-Dawley rat at 3 mg/kg2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal 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.
AID564044Antiviral 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 assay2010Antimicrobial 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.
AID1886612Inhibition of UGT1A1 in human liver microsomes using beta-estradiol as substrate incubated for 40 mins by LC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID322119Antiviral activity against HIV1 92UG029 X4 subtype A in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID564060Antiviral 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 assay2010Antimicrobial 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.
AID322100Selectivity index, ratio of CC50 for MT2 cells to EC50 for HIV1 LAI2007Antimicrobial 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.
AID1216281Drug excretion in wildtype mouse feces assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazino propylcarbamoyl}-2,2-dimethyl-propyl)-carbamic acid methyl ester formation at 50 mg/kg, po by LC-MS/MS 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID519580Antiviral 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 RF2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1607530Antiviral activity against darunavir resistant HIV1 harboring protease P30 L10I/I15V/K20R/L24I/V32I/M36I/ M46L/L63P/K70Q/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag production2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID532452Antiviral 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 X2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID321667Plasma clearance in Beagle dog at 15 mg/kg, iv2008Bioorganic & 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.
AID699544Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting2012Journal 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.
AID1409313Antiviral 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 immunoassay2018Journal 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.
AID519573Antiviral 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 days2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID459077Antiviral activity against multi drug-resistant HIV1 isolate of subtype MM in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID239809Equilibrium dissociation constant for the interaction between the compound and serum albumin2005Journal 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.
AID673371Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing wild type protease infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID459082Ratio of IC50 for multi drug-resistant HIV1 isolate of subtype G to IC50 for wild type HIV1 isolate ERS104pre2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID1375432Apparent permeability across basolateral to apical side in human Caco2 cells2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID532475Antiviral 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-ass2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID525167Antimicrobial activity against chloroquine-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy2008Antimicrobial 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.
AID572560Half life in HIV-1 infected patient at 300 mg, po qd coadministered with 100 mg of ritonavir, po qd and NRTI2008Antimicrobial 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.
AID248546Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line2005Bioorganic & 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.
AID374618Resistance 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 assay2007Antimicrobial 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.
AID738148Inhibition of transferrin receptor-fused wild type HIV1 protease autoprocessing expressed in Escherichia coli by SDS-PAGE analysis2013Journal of medicinal chemistry, May-23, Volume: 56, Issue:10
Extreme multidrug resistant HIV-1 protease with 20 mutations is resistant to novel protease inhibitors with P1'-pyrrolidinone or P2-tris-tetrahydrofuran.
AID1593737Inhibition of UGT1A1 in human liver microsomes using beta-estradiol as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis2019Journal 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.
AID368468AUC (24 hrs) in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID368656Toxicity in HIV-negative human assessed as creatinine levels at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID566852Antiviral activity against HIV-1 MDR/JSL infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID519572Antiviral 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 infectio2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID321659Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of UDPGA by RP-HPLC2008Bioorganic & 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.
AID1216269Drug metabolism in human liver microsomes assessed as methyl (S)-1-(2-((2S,3S)-3-((S)-2-amino-3,3-dimethylbutanamido)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/M2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID519538Antiviral 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 assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID415282Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID519539Antiviral 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 assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID343025Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID1706646Solubility of compound in acetate buffer at pH 42020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID106906Concentration required to inhibit 50% of RT production in HIV-1/MN-infected MT-2 cells.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID278954Antiviral activity against HIV1 A2 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID557290Antiviral 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 ELISA2009Antimicrobial 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.
AID543367AUC (0 to 24 hrs) in HIV-infected patient at 300 mg, qd2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID278976Antiviral activity against HIV1 C9 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID557295Ratio 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 NL4-32009Antimicrobial 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.
AID321675Metabolic stability in dog liver microsomes assessed as compound remaining in presence of UDPGA by RP-HPLC2008Bioorganic & 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.
AID368467AUC (24 hrs) in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1375406Half life of the compound in phosphate buffer at pH 6.5 at 37 degC after 24 hrs by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID1216279Drug excretion in wild type mouse urine assessed as methyl (S)-1-((2S,3S)-4-(2-((S)-2-amino-3,3-dimethylbutanoyl)-1-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3-hydroxy-1-phenylbutan-2-ylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by L2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID532458Antiviral 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 and2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374593Cytotoxicity against human MT4 cells after 6 days by MTT assay2007Antimicrobial 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.
AID343024Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID547019Selectivity ratio of EC50 for HIV1 subtype B harboring protease polymorphism at I36 position and M46I, I50L, N88S mutant gene to EC50 for wild type HIV1 subtype B2010Antimicrobial 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.
AID1886565Cmax in Sprague-Dawley rat at 3 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID519785Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID1593656Half life in pH 4 30%CH3CN/acetate buffer at 50 mM by RP-UPLC analysis2019Journal 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.
AID1593752Apparent permeability across basolateral to apical side in human Caco2 cells at 2 uM2019Journal 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.
AID369943Antiviral activity against HIV2 CDC310319 isolate infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID372187Resistance 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 assay2007Antimicrobial 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.
AID328885Toxicity in human HeLa cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot2007Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells.
AID459081Ratio of IC50 for multi drug-resistant HIV1 isolate of subtype C to IC50 for wild type HIV1 isolate ERS104pre2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID372185Resistance 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 assay2007Antimicrobial 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.
AID369957Ratio of EC50 for HIV2 ROD with protease G17N/V47A mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID322113Antiviral activity against HIV1 MDR/TM X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID368671Cmin in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID278961Antiviral activity against HIV1 A9 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID374627Resistance 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 assay2007Antimicrobial 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.
AID1216290Drug metabolism in human liver microsomes assessed as (S)-methyl 3,3-dimethyl-1-oxo-1-(2-(4-(pyridin-2-yl)benzyl)hydrazinyl)butan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/MS analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID322117Antiviral activity against HIV1 MDR/C X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID519579Antiviral 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 pN2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID343016Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID374591Inhibition of HIV1 protease2007Antimicrobial 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.
AID321339Antiviral activity against HIV1 in MT4 cells by XTT assay2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
AID1706659AUClast in Sprague-Dawley rat at 30 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID124203Drug concentration in blood sample was analyzed by reversed phase HPLC 30 min (c90) after oral application of 120 mg/kg in a standardized formulation1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID1725419Antiviral activity against LPV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID1593680Oral bioavailability in cannulated Sprague-Dawley rat plasma at 3 mg/kg by UPLC/MS/MS analysis2019Journal 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.
AID521547Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID543387Half life in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline and 250 mg valporic acid, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID557293Ratio of EC50 for HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1482919Antiviral 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 immunoassa2017Journal 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.
AID279179Ratio of intracellular drug level to extracellular drug level in human PBMC at 20 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID1593731Prodrug conversion in intestinal homogenates of closed loop rat intestinal model assessed as atazanavir recovery at 1 mg/kg administered as cassette dose by LC/MS analysis2019Journal 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.
AID81433Antiviral activity against HIV-1 protease inhibitor-resistant strain(saquinavir resistant) of the HI virus.(Mutant: G48V,L90M)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID532464Antiviral 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-type2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID81427Antiviral activity against HIV-1 protease inhibitor-resistant strain(CGP 61755 resistant) of the HI virusMutant: K45I,A71Tmix,L76F,I84Vmix)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID1482911Antiviral 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 immunoassay2017Journal 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.
AID532471Antiviral 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 human2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374610Resistance 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 assay2007Antimicrobial 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.
AID557294Ratio of EC50 for HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID343020Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID1706655Trough plasma concentration in Sprague-Dawley rat at 3 mg/kg, po measured after 24 hrs2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID572559Oral clearance in HIV-1 infected patient at 300 mg, po qd coadministered with 100 mg of ritonavir, po qd and NRTI2008Antimicrobial 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.
AID1706657Cmax in Sprague-Dawley rat at 30 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID668812Selectivity 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 protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID1886560Aqueous solubility of compound at pH 4 by UPLC analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID81615Inhibitory activity against indinavir-resistant resistant strain of HIV-1.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID519575Antiviral 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 p2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1886571AUClast in Sprague-Dawley rat at 3 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID278969Antiviral activity against HIV1 C2 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID278967Antiviral activity against HIV1 A15 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID1593761Drug recovery in feces of po dosed dog2019Journal 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.
AID416859Increase in P-glycoprotein-mediated tenofovir disoproxil fumarate permeation from apical to basolateral side of human Caco-2 cells at 20 uM2007Antimicrobial 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.
AID496588AUC in patient with => 40 IU/liter ALAT level by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID724346Inhibition 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-NH22013European journal of medicinal chemistry, Feb, Volume: 60Linear and cyclic glycopeptide as HIV protease inhibitors.
AID1482920Antiviral 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 immunoassay2017Journal 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.
AID242869Association rate constant for the interaction between the compound and serum albumin2005Journal 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.
AID368469Terminal apparent distribution volume in HIV-negative human serum at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID673379Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M7 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID322107Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID519551Antiviral 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 mutati2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID673376Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M4 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID1216294Drug excretion in wildtype mouse urine assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-N-(4-pyridin-2-yl-benzyl)-hydrazino]-propylcarbamoyl}-3-hydroxy-2,2-dimethyl-propyl)-carbamic acid methyl ester f2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1409312Antiviral 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 immunoassay2018Journal 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.
AID557284Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA2009Antimicrobial 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.
AID532465Antiviral 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, I52010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID547235Selectivity ratio of EC50 for HIV1 subtype C harboring protease E35G mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype C2010Antimicrobial 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.
AID564062Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay2010Antimicrobial 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.
AID369956Ratio of EC50 for HIV2 ROD with protease V47A mutation to EC50 for wild type HIV2 ROD2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID519537Antiviral 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 assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1482905Antiviral 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 immunoassay2017Journal 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.
AID321686Antiviral activity against HIV1 mutant strain 12008Bioorganic & 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.
AID263207Antiviral activity against HIV1 HXB2 in MT4 cells2006Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385.
AID368665Toxicity in human with two gilbert's genotype homozygotes assessed as bilirubin level at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID415245Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID459084Ratio of IC50 for multi drug-resistant HIV1 isolate of subtype MM to IC50 for wild type HIV1 isolate ERS104pre2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID496584AUC in patient with elevated alpha-1- glycoprotein acid level by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID374628Resistance 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 assay2007Antimicrobial 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.
AID368653Toxicity in HIV-negative human assessed as alanine aminotransferase levels at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID543368AUC (0 to 24 hrs) in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID661002Antiviral activity against HIV1 infected in human MT4 cells2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID543373Cmin in HIV-infected patient at 300 mg, qd2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID322096Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID532472Antiviral 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/2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1380925Antiviral 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 immunoassay2018Journal 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.
AID368465AUC (12 hrs) in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID321689Antiviral activity against HIV1 mutant strain 42008Bioorganic & 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.
AID368452Half life in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1593671Cmax in cannulated Sprague-Dawley rat at 3 mg/kg administered orally by UPLC/MS/MS analysis2019Journal 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.
AID279165Intracellular drug level in CEM CCL19 cells at 0.2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID668814Selectivity 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 protease2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID496576Apparent oral clearance in human by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID547015Antiviral activity against HIV1 subtype B harboring protease polymorphism at I36 position and M46I, I50L, N88S mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene 2010Antimicrobial 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.
AID1886576Cmin in Sprague-Dawley rat at 30 mg/kg,po measured after 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID238682Inhibition constant for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID369952Antiviral 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 assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID532462Antiviral 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 gen2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1886652AUClast in Sprague-Dawley rat at 1 mg/kg,iv measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID1593734Inhibition of recombinant human UGT1A1 using bilirubin as substrate preincubated for 5 mins followed by substrate addition and measured after 40 mins by LC-MS/MS analysis2019Journal 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.
AID576053Plasma concentration in HIV infected patient at 400 mg qd measured after 13.06 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID374616Resistance 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 assay2007Antimicrobial 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.
AID1375415Oral bioavailability in Sprague-Dawley rat at 3 mg/kg after 0.25 to 24 hrs by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID496580Absorption rate constant in human by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID374602Resistance 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 assay2007Antimicrobial 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.
AID374592Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay2007Antimicrobial 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.
AID575061Antiviral 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 type2010Antimicrobial 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.
AID1409307Antiviral 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 immunoassay2018Journal 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.
AID343015Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID661001Inhibition of HIV1 protease expressed in Escherichia coli using DABCYL-Abu-Ser-Gln-ASN-Tyr-Pro-Ile-Val-Gln-EDANS as substrate preincubated for 20 mins measured for 45 mins by fluorometry2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.
AID699543Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting2012Journal 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.
AID519576Antiviral 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 pNL4-32008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID673374Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M10 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID1886654Clearance in Sprague-Dawley rat at 1 mg/kg,iv measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID658565Antiviral 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 assay2012Journal 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.
AID242932Dissociation rate constant for the interaction between the compound and serum albumin2005Journal 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.
AID368453Half life in HIV-negative human at 400 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID668809Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID699540Inhibition 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 counting2012Journal 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.
AID279167Intracellular drug level in CEM CCL19 cells at 20 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID532658Antiviral 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 gene2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1725420Antiviral activity against ATV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID1482924Ratio 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 cells2017Journal 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.
AID417026Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated healthy human assessed as change in plasma Cmax of tenofovir at 300 mg, po, QD co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate2007Antimicrobial 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.
AID576055Cmin in HIV infected patient at 300 mg qd measured after 16.60 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID564061Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay2010Antimicrobial 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.
AID673370Inhibition of Human immunodeficiency virus protease M10 mutant expressed in Escherichia coli using ArgGlu(EDANS)SerGlnAsnTyrProIleValGlnLys(DABCYL)Arg as substrate preincubated with compound for 0.5 to 1 min measured by fluorometric analysis at pH 6.52012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID321658Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of NADPH by RP-HPLC2008Bioorganic & 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.
AID321695Ratio of EC50 for HIV1 mutant strain 3 to EC50 for wild type HIV12008Bioorganic & 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.
AID1409309Antiviral 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 immunoassay2018Journal 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.
AID1593710Aqueous solubility of the compound in FaSSIF by RP-HPLC analysis2019Journal 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.
AID1886574Tmax in Sprague-Dawley rat at 30 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID519789Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID1375433Efflux ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID532466Antiviral 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/2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID374608Resistance 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 assay2007Antimicrobial 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.
AID396261Ratio of EC50 for HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient to EC50 for drug sensitive HIV1 NL4-32007Antimicrobial 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.
AID297669Inhibition of HIV1 Protease M2 variant by FRET based assay2007Journal 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.
AID1375403Trough concentration in Sprague-Dawley rat at 3 mg/kg, po at 24 hrs by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID369941Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID368470Terminal apparent distribution volume in HIV-negative human serum at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID374636Resistance 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 assay2007Antimicrobial 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.
AID278959Antiviral activity against HIV1 A7 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID242868Association rate constant for the interaction between the compound and serum albumin2005Journal 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.
AID673373Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M9 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID374630Resistance 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 assay2007Antimicrobial 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.
AID519546Antiviral 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 Lopinavi2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID343019Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID368473Apparent oral clearance in HIV-negative human serum at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID343018Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID496577Apparent volume of distribution with respect to the bioavailability in human by one-comparment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID519550Antiviral 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 Lopina2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1375431Apparent permeability across apical to basolateral side in human Caco2 cells2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID726414Antiviral 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 replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID279172Increase in accumulation of the drug in CEM CCL19 cells in presence of 50 uM Probenecid relative to control2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID532453Antiviral 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-as2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID572566AUC in HIV-1 infected patient at 300 mg, po qd coadministered with 400 mg, po bid and 100 mg, po bid of Lopinavir and ritonavir respectively2008Antimicrobial 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.
AID576052Plasma concentration in HIV infected patient at 300 mg qd measured after 16.60 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID586620Antiviral activity against HIV1 harboring wild type 8.9NSX with gag T81A mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID519545Antiviral 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 fro2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID496586Half life in patient with => 40 IU/liter ALAT level by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID321661Antiviral activity against HIV1 3B2008Bioorganic & 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.
AID1725422Antiviral activity against HIV1 DRVR P30 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID374614Resistance 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 assay2007Antimicrobial 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.
AID321691Antiviral activity against HIV1 mutant strain 62008Bioorganic & 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.
AID576056Cmax in HIV infected patient at 400 mg qd measured after 13.06 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID279170Intracellular drug level in human PBMC at 20 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID321693Ratio of EC50 for HIV1 mutant strain 1 to EC50 for wild type HIV12008Bioorganic & 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.
AID322106Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1216274Drug level assessed as human CYP2D6-mediated ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazino]-propylcarbamoyl}-2,2-dimethyl-propyl)-carbamic acid methyl ester formation treated with 50 uM atazanavir by 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID278975Antiviral activity against HIV1 C8 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID322121Antiviral activity against HIV1 BaL R5 subtype B in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID586626Antiviral 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 assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID1375436AUC (0 to 24 hrs) in famotidine treated Sprague-Dawley rat at 10 mg/kg, po by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID547005Antiviral activity against HIV1 subtype CRF02_AG harboring protease polymorphism at M36 position and I50FILV, A71V mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter g2010Antimicrobial 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.
AID668808Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
AID1706653Tmax in Sprague-Dawley rat at 3 mg/kg, po2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID278964Antiviral activity against HIV1 A12 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID575059Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations assessed as fold change in drug susceptibility relative to wild type2010Antimicrobial 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.
AID543381Cmax in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline and 250 mg valporic acid, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID1380926Antiviral 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 immunoassay2018Journal 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.
AID543369AUC (0 to 24 hrs) in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline and 250 mg valporic acid, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID1593746Prodrug conversion in pH 6.5 30%CH3CN/phosphate buffer assessed as atazanavir formation at 50 mM measured after 2 mins by RP-UPLC analysis2019Journal 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.
AID1886657Inhibition of human ERG by patch-clamp assay2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID1593697Cmin in cannulated Sprague-Dawley rat at 3 mg/kg administered orally measured after 24 hrs by UPLC/MS/MS analysis2019Journal 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.
AID673375Antiviral activity against Human immunodeficiency virus 1 HXB2 expressing protease M3 mutant infected in human MT4 cells after 5 days by MTT assay2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Enamino-oxindole HIV protease inhibitors.
AID519644Antiviral 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 Lopinavi2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID368457Cmax in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID726411Selectivity 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 3B2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID372190Resistance 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 assay2007Antimicrobial 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.
AID106913concentration of compound required to inhibit 90% of RT production in HIV-1/MN-infected MT-2 cells.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID81426Antiviral activity against HIV-1 protease inhibitor-resistant strain(CGP 61755 resistant) of the HI virus(Mutant: V32I,M46I,L63P,I84A)1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
AID590915Inhibition 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 analysis2011Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease.
AID1375404Half life of the compound in 0.1 N aqueous HCl at pH 1 at 37 degC after 24 hrs by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID369838Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID564041Antiviral 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 assay2010Antimicrobial 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.
AID278968Antiviral activity against HIV1 C1 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID278978Antiviral activity against HIV1 C11 isolate with protease I84C mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID576059Plasma concentration in HIV infected patient with HIV RNA of >50 copies/ml by dried blood spot assay using reversed-phase ultrahigh-performance liquid chromatography2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID368666Toxicity in human with six gilbert's genotype heterozygotes assessed as bilirubin level at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID321696Ratio of EC50 for HIV1 mutant strain 4 to EC50 for wild type HIV12008Bioorganic & 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.
AID1216293Drug excretion in wildtype mouse urine assessed as ((S)-1-{(1S,2S)-1-Benzyl-2-hydroxy-3-[N'-((S)-2-methoxycarbonylamino-3,3-dimethyl-butyryl)-hydrazino propylcarbamoyl}-2,2-dimethyl-propyl)-carbamic acid methyl ester formation at 50 mg/kg, po by LC-MS/MS 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID519781Antiviral 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 months2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
AID368455Tmax in HIV-negative human at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID374601Resistance 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 assay2007Antimicrobial 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.
AID1375442Ratio of AUC in pentagastrin treated Sprague-Dawley rat at 10 mg/kg, po to AUC in famotidine treated Sprague-Dawley rat at 10 mg/kg, po2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID1216270Drug metabolism in human liver microsomes assessed as methyl (S)-1-((2S,3S)-4-(2-((S)-2-amino-3,3-dimethylbutanoyl)-1-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3-hydroxy-1-phenylbutan-2-ylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID564040Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay2010Antimicrobial 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.
AID496573Binding affinity to human serum albumin2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID1375405Half life of the compound in acetate buffer at pH 4 at 37 degC after 24 hrs by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID566848Antiviral activity against HIV-1 MDR/C infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID1593660Aqueous solubility of the compound in pH 6.5 phosphate buffer by RP-UPLC analysis2019Journal 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.
AID661005Intrinsic clearance in human liver microsomes at 1 uM after 30 mins by LC-MS/MS analysis2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Synthesis, X-ray analysis, and biological evaluation of a new class of stereopure lactam-based HIV-1 protease inhibitors.
AID519540Antiviral 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 assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1706645Solubility of compound in 0.1 N aqueous HCl buffer at pH 12020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID566847Antiviral activity against HIV-1 MDR/B infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID1216283Drug excretion in wildtype mouse feces assessed as {(S)-3-Hydroxy-1-[N'-[(2S,3S)-2-hydroxy-3-((S)-4-hydroxy-2-methoxycarbonylamino-3,3-dimethyl-butyrylamino)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl}-carbamic acid 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID1375440AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID374632Resistance 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 assay2007Antimicrobial 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.
AID368454Tmax in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID532656Antiviral 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 L2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1886655Half life in Sprague-Dawley rat at 1 mg/kg,iv measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID374594Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-32007Antimicrobial 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.
AID1725423Antiviral activity against HIV1 DRVR P51 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay2020ACS 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.
AID532477Antiviral 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, M42010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID322118Antiviral activity against HIV1 MDR/G X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID322109Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID368451Half life in HIV-negative human at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID322108Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1886656Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg,iv measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID368674Cmin in HIV-negative human at 400 mg administered every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1886573Cmax in Sprague-Dawley rat at 30 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID368461Drug level in HIV-negative human serum at 300 mg, po administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs measured at 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID396259Antiviral activity against HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient2007Antimicrobial 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.
AID81616Inhibitory activity against saquinavir-resistant resistant strain of HIV-1.2000Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
Protease inhibitors: current status and future prospects.
AID415283Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay2009Journal 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.
AID374613Resistance 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 assay2007Antimicrobial 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.
AID564045Antiviral 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 assay2010Antimicrobial 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.
AID519574Antiviral 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 infecti2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID1593709Aqueous solubility of the compound in pH 5 buffer by RP-UPLC analysis2019Journal 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.
AID496578Apparent volume of distribution with respect to the bioavailability in human by covariate model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID374619Resistance 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 assay2007Antimicrobial 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.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID321698Ratio of EC50 for HIV1 mutant strain 6 to EC50 for wild type HIV12008Bioorganic & 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.
AID557300Ratio 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 NL4-32009Antimicrobial 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.
AID1593758Oral bioavailability in rat2019Journal 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.
AID566846Antiviral activity against wild type HIV-1 ERS104 pre infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production2011Journal 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.
AID443166Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay2010Journal 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.
AID586624Antiviral 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 assay2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity.
AID496589AUC in patient with => 40 IU/liter ALAT level by one-compartment model2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID1482906Antiviral 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 chemilumi2017Journal 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.
AID278957Antiviral activity against HIV1 A5 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID368677Toxicity in HIV-negative human assessed as grade 3 fatigue2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1607531Selectivity ratio of IC50 for antiviral activity against atazanavir resitant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to IC50 for antiviral activity against wild-type HIV1 NL4-32020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID576057Cmax in HIV infected patient at 300 mg qd measured after 16.60 hrs by plasma based assay using HPLC2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID1593760Drug recovery in feces of po dosed rat2019Journal 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.
AID368663Toxicity in HIV-negative human assessed as bilirubin level at 300 mg, po administered every 12 hrs administered every 12 hrs coadministered with 600 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1482925Ratio 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 cells2017Journal 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.
AID1375420AUClast in Sprague-Dawley rat at 3 mg/kg, po after 0.25 to 24 hrs by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID519552Antiviral 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 2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
AID726419Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID248545Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line2005Bioorganic & 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.
AID343014Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID1409308Antiviral 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 immunoassay2018Journal 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.
AID368659Toxicity in HIV-negative human assessed as hemoglobin level at 300 mg, po administered every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID547241Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease polymorphism at I36 position and I50FILV, A71V mutant gene to EC50 for wild type HIV1 subtype CRF02_AG2010Antimicrobial 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.
AID369945Ratio of EC50 for HIV2 CBL-23 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID322115Antiviral activity against HIV1 MDR/JSL R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID1375434Half life in rat hepatocytes at 1 uM after 5 to 120 mins by UPLC-MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID1375410Solubility of the compound in phosphate buffer at pH 6.5 at 25 degC by UPLC method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID1375416Tmax in Sprague-Dawley rat at 3 mg/kg, po after 0.25 to 24 hrs by UPLC/MS/MS method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
AID572565Half life in HIV-1 infected patient at 300 mg, po qd coadministered with 400 mg, po bid and 100 mg, po bid of Lopinavir and ritonavir respectively2008Antimicrobial 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.
AID322122Antiviral activity against HIV1 97ZA003 R5 subtype C in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay2007Antimicrobial 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.
AID576058Plasma concentration in HIV infected patient with HIV RNA of <50 copies/ml by dried blood spot assay using reversed-phase ultrahigh-performance liquid chromatography2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Clinical evaluation of a dried blood spot assay for atazanavir.
AID321674Metabolic stability in dog liver microsomes assessed as compound remaining in presence of NADPH by RP-HPLC2008Bioorganic & 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.
AID564039Antiviral 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 assay2010Antimicrobial 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.
AID618426Inhibition 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 spectrophotometry2011European 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.
AID1409311Antiviral 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 immunoassay2018Journal 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.
AID372181Resistance 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 assay2007Antimicrobial 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.
AID1886570Tmax in Sprague-Dawley rat at 3 mg/kg,po measured upto 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID572562Cmax in HIV-1 infected patient at 300 mg, po qd coadministered with 100 mg of ritonavir, po qd and NRTI2008Antimicrobial 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.
AID1593719Elimination half life in rat hepatocytes at 1 uM in absence of esterase inhibitor PMSF/CYP450 inhibitor ABT2019Journal 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.
AID1873200Inhibition 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 cytometry2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID726418Antiviral 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 plasma2013Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
AID369942Antiviral activity against HIV2 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID279180Increase in accumulation of the drug in CEM CCL19 cells in presence of 50 uM Dipyridamole relative to control2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID532469Antiviral 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 2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1706640Oral bioavailability in rat2020European journal of medicinal chemistry, Dec-01, Volume: 207(Carbonyl)oxyalkyl linker-based amino acid prodrugs of the HIV-1 protease inhibitor atazanavir that enhance oral bioavailability and plasma trough concentration.
AID557299Ratio of EC50 for HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-32009Antimicrobial 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.
AID1216286Drug excretion in wild type mouse feces assessed as methyl (S)-1-((2S,3S)-4-(2-((S)-2-amino-3,3-dimethylbutanoyl)-1-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3-hydroxy-1-phenylbutan-2-ylamino)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by L2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID278956Antiviral activity against HIV1 A4 isolate with protease I84A mutation in HEK 293 cells relative to wild type2007Antimicrobial 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.
AID564036Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay2010Antimicrobial 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.
AID343022Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease2008Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
AID547000Antiviral activity against HIV1 subtype C harboring protease E35G 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 gene assay2010Antimicrobial 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.
AID279166Intracellular drug level in CEM CCL19 cells at 2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID374620Resistance 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 assay2007Antimicrobial 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.
AID543380Cmax in HIV-infected patient at 300 mg, qd co-administered with 100 mg minocycline, bid for 15 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID564048Antiviral 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 assay2010Antimicrobial 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.
AID1607533Selectivity ratio of IC50 for antiviral activity against darunavir resistant HIV1 P30 harboring protease L10I/I15V/K20R/L24I/V32I/M36I/ M46L/L63P/K70Q/V82A/I84V/L89M mutant infected in human MT4 cells to IC50 for antiviral activity against wild-type HIV1 2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID239810Equilibrium dissociation constant for the interaction between the compound and serum albumin2005Journal 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.
AID1886572Cmin of Atazanavir in Sprague-Dawley rat at 3 mg/kg,po measured after 24 hrs by UPLC-MS/MS analysis2022Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
Improving Drug Delivery While Tailoring Prodrug Activation to Modulate
AID543385Half life in HIV-infected patient at 300 mg, qd2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Effects of minocycline and valproic acid coadministration on atazanavir plasma concentrations in human immunodeficiency virus-infected adults receiving atazanavir-ritonavir.
AID374622Resistance 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 assay2007Antimicrobial 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.
AID1593751Apparent permeability across apical to basolateral side in human Caco2 cells at 2 uM2019Journal 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.
AID532470Antiviral 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, V822010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat.
AID1216295Drug excretion in wildtype mouse urine assessed as {(S)-3-Hydroxy-1-[N'-[(2S,3S)-2-hydroxy-3-((S)-4-hydroxy-2-methoxycarbonylamino-3,3-dimethyl-butyrylamino)-4-phenyl-butyl]-N'-(4-pyridin-2-yl-benzyl)-hydrazinocarbonyl]-2,2-dimethyl-propyl}-carbamic acid 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID321660Inhibition of HIV1 protease2008Bioorganic & 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.
AID1607528Antiviral activity against atazanavir 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 production2020Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9
Structure-Based Design of Highly Potent HIV-1 Protease Inhibitors Containing New Tricyclic Ring P2-Ligands: Design, Synthesis, Biological, and X-ray Structural Studies.
AID664437Inhibition 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 spectrophotometry2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease.
AID369954Antiviral 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 assay2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
AID496581Plasma protein binding in human assessed as unbound fraction at 15000 ng/ml total serum concentration2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Influence of alpha-1 glycoprotein acid concentrations and variants on atazanavir pharmacokinetics in HIV-infected patients included in the ANRS 107 trial.
AID321694Ratio of EC50 for HIV1 mutant strain 2 to EC50 for wild type HIV12008Bioorganic & 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.
AID374638Resistance 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 assay2007Antimicrobial 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.
AID374621Resistance 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 assay2007Antimicrobial 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.
AID368664Toxicity in HIV-negative human assessed as bilirubin level at 400 mg, po administered every 12 hrs coadministered with 400 mg of rifampin every 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID459074Antiviral activity against multi drug-resistant HIV1 isolate of subtype C in PHA-stimulated human PBMC assessed as inhibition of p24 antigen production2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
AID246225Protease inhibitory activity against HIV-1 GSS004421 mutant strain was determined2005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
AID1216278Drug excretion in wild type mouse urine assessed as methyl (S)-1-(2-((2S,3S)-3-((S)-2-amino-3,3-dimethylbutanamido)-2-hydroxy-4-phenylbutyl)-2-(4-(pyridin-2-yl)benzyl)hydrazinyl)-3,3-dimethyl-1-oxobutan-2-ylcarbamate formation at 50 mg/kg, po by LC-MS/MS 2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
AID374634Resistance 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 assay2007Antimicrobial 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.
AID238043Binding affinity for human immunodeficiency virus type 1 protease2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data.
AID575060Antiviral 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 type2010Antimicrobial 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.
AID279169Intracellular drug level in human PBMC at 2 ug/ml after 24 hrs2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Quantitative immunoassay to measure plasma and intracellular atazanavir levels: analysis of drug accumulation in cultured T cells.
AID1745854NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1745855NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay2023Disease models & mechanisms, 03-01, Volume: 16, Issue:3
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2006Biochemistry, 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.
AID1811Experimentally measured binding affinity data derived from PDB2006Biochemistry, 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (75)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (1.33)18.2507
2000's27 (36.00)29.6817
2010's35 (46.67)24.3611
2020's12 (16.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 65.55

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

MetricThis Compound (vs All)
Research Demand Index65.55 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index5.85 (4.65)
Search Engine Demand Index106.56 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (65.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.33%)5.53%
Reviews3 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other71 (94.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]