| Assay ID | Title | Year | Journal | Article |
|---|
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2008 | Journal of virology, Jun, Volume: 82, Issue:12
| Ninety-nine is not enough: molecular characterization of inhibitor-resistant human immunodeficiency virus type 1 protease mutants with insertions in the flap region. |
| AID1797110 | Protease Inhibition Assay from Article 10.1021/bi051886s: \\Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir.\\ | 2006 | Biochemistry, May-02, Volume: 45, Issue:17
| Analysis of HIV-1 CRF_01 A/E protease inhibitor resistance: structural determinants for maintaining sensitivity and developing resistance to atazanavir. |
| AID1796953 | Enzyme Inhibition Assay from Article 10.1021/jm060666p: \\Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands.\\ | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
| AID1799570 | Inhibition Assay from Article 10.1111/j.1747-0285.2007.00514.x: \\Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis.\\ | 2007 | Chemical biology & drug design, May, Volume: 69, Issue:5
| Design of mutation-resistant HIV protease inhibitors with the substrate envelope hypothesis. |
| AID1796876 | Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2005.03.008: \\Oximinoarylsulfonamides as potent HIV protease inhibitors.\\ | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
| Oximinoarylsulfonamides as potent HIV protease inhibitors. |
| AID328893 | Inhibition of mouse ZMPSTE24 expressed n delta ste24 delta rce1 yeast | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID369953 | Antiviral activity against HIV2 ROD with protease V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID374591 | Inhibition of HIV1 protease | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID557231 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured before administering last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID328891 | Inhibition of human ICMT expressed in yeast assessed as methylation of N-acetyl-farnesylcysteine | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID557282 | Ratio of EC50 for HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID369954 | Antiviral activity against HIV2 ROD with protease G17N/V47A mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID519783 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-60K/N-65E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID668809 | Antiviral activity against Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID297669 | Inhibition of HIV1 Protease M2 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID564038 | Antiviral activity against HIV1 expressing protease L10F/D30N/K45I/A71V/T74S mutant infected in human MT4 cells selected at 5 uM of nelfinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID558383 | Drug level in HIV-infected pregnant woman amniotic fluid at 400 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID238682 | Inhibition constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
| AID1482906 | Antiviral activity against tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemilumi | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID415245 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID374626 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/53L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | | | |
| AID369941 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID372182 | Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1482921 | Antiviral activity against atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID321695 | Ratio of EC50 for HIV1 mutant strain 3 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID558397 | Ratio of drug level in HIV-infected pregnant woman amniotic fluid to maternal blood plasma at 400 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID622660 | Antiviral activity against HIV1 harboring protease L10I, I13V, G16A, Q18H, L33F, N37D, M46I, I54V, G57R, Q61H,I62V, L63P, A71L, I72T, L76V, V77I, V82A, N88G, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID519552 | Antiviral activity against HIV1 isolate 9 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15I/V, K20R, L33F, E35D, M36I, N37D, R41K, K43I, M46I, I54V, I62V, L63P, A71T, I72T, V82A, I84V, L90M, I93L | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID564031 | Antiviral activity against HIV2 ROD infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1219738 | Maximum plasma concentration in healthy human at 400 mg co-administered with 50 mg ritonavir | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID328878 | Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 48 hrs by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID278976 | Antiviral activity against HIV1 C9 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID374593 | Cytotoxicity against human MT4 cells after 6 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID519545 | Antiviral activity against HIV1 isolate 2 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, G16E, K20R, E35D, M36I, R41K, I54A, R57K, Q61D, A71V, I72R, V82A, L89I, L90M, Q92K mutation derived fro | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID519789 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10V/I-40D-43I-56V-70K-82F-84V-89V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID557273 | Antiviral activity against HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID519780 | Antiviral activity against HIV 2 subtype H expressing 10I-34E-40P-41Y-60H-63N-70T-73G-82F-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID396260 | Antiviral activity against HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
| AID622658 | Antiviral activity against HIV1 B26 harboring protease L33F, K45I, M46I, I50V, A71V and V82F mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID105346 | Tested for cytopathic effect of HIVIIIB in MT-4 cells in presence of 50% human serum | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships. |
| AID372186 | Resistance index, ratio of EC50 for HIV1 with protease 54V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1350503 | Ratio of EC50 for inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells to EC50 for wild-type HIV-1 pNL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
| AID13678 | Cmax value in the period of 8 hr after dosing. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID279336 | Antiviral activity against wild type HIV2 in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID322122 | Antiviral activity against HIV1 97ZA003 R5 subtype C in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID343025 | Ratio of Ki for HIV1 recombinant protease V32I/I47A mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID1669456 | Inhibition of HIV1 NL4-3 protease I50V/A71V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 6 | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
| AID532460 | Antiviral activity against Human immunodeficiency virus 1 isolate 20 harboring Gag-capsid I138L, V215L, V218P, H219Q, M228I, E230D, G248T, T280A, E312D, A340G and G357S mutant gene and protease L10F, A22V, D30N, S37N, K45R, I54L, I62V, L63P, A71V, V77I, I | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1717746 | Selectivity index, ratio of CC50 for African green monkey Vero E6 cells to EC50 for SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID375204 | Ratio of EC50 for multidrug-resistant HIV1 isolate TM to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID519577 | Antiviral activity against HIV1 clone2 infected in HEK293 cells harboring A-790742-selected protease V82L mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1482925 | Ratio of IC50 for nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID519554 | Antiviral activity against HIV1 isolate 11 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I15V, K20R, E21Q, E35D, M36I, N37D, R41K, M46L, I54V, I62V, L63P, A71V, T74D, P79A, V82T, I84V, I85V, L90M, | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID446195 | Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID278958 | Antiviral activity against HIV1 A6 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID547020 | Selectivity ratio of EC50 for HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype C | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID279344 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L99F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID1219734 | Drug metabolism in human liver microsomes assessed as CYP2D6-mediated lopinavir-GSH adduct formation at 2 uM after after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID416859 | Increase in P-glycoprotein-mediated tenofovir disoproxil fumarate permeation from apical to basolateral side of human Caco-2 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID374623 | Resistance index, ratio of EC50 for HIV1 with protease 32I/46L/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID353726 | Aqueous solubility in water by shake flask method | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
| AID557290 | Antiviral activity against HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of Lopinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID374628 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/53L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1474091 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID21894 | The partition coefficient was reported | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
| AID519580 | Antiviral activity against HIV1 clone5 infected in HEK293 cells harboring A-790742-selected protease L63P, A71V, and V82G mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 RF | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID572579 | Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID541175 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S and Q148H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID248098 | Inhibitory concentration against resistant (A17) human immunodeficiency virus | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
| Oximinoarylsulfonamides as potent HIV protease inhibitors. |
| AID278969 | Antiviral activity against HIV1 C2 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID374613 | Resistance index, ratio of EC50 for non-B type HIV1 with protease 32I/47A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID162683 | Inhibition of HIV protease at 0.5 nM | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
| AID297668 | Inhibition of HIV1 Protease M1 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID558390 | Ratio of drug level in HIV-infected pregnant woman cord blood plasma to maternal blood plasma at 400 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | | | |
| AID369958 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 1 passage | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID532473 | Antiviral activity against Human immunodeficiency virus 1 isolate 34 harboring Gag-capsid I138L, I147L, V159I, V215L, T280V, A309C, S310T, E312D and G357S mutant gene and protease L10I, I13V, E35D, S37N, I62V, L63P and I64M mutant gene infected in human M | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369956 | Ratio of EC50 for HIV2 ROD with protease V47A mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID242933 | Dissociation rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID572577 | Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir with NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID374592 | Antiviral activity against wild type HIV1 NL4-3 infected in MT4 cells after 6 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID369957 | Ratio of EC50 for HIV2 ROD with protease G17N/V47A mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID353765 | AUC in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
| AID668815 | Cytotoxicity against human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID1669457 | Antiviral activity against wild-type HIV1 NL4-3 infected in human TZM-bl cells infected with supernatants from virus-infected human 293T cells treated with compound for 18 hrs assessed as reduction in viral replication by luciferase assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
| AID582282 | Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI measured 12 hrs after last dose | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID521547 | Antiviral activity against Human immunodeficiency virus type 2 (ISOLATE ROD) after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID519550 | Antiviral activity against HIV1 isolate 7 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, M46M/L, G48V, I54V, L63P, A71V, I72M, V77I, V82A, L90M, I93L mutation derived from viral passages with Lopina | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID679931 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in Caco-2 cells | 2003 | AIDS (London, England), May-02, Volume: 17, Issue:7
| Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. |
| AID446202 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate G to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID532453 | Antiviral activity against Human immunodeficiency virus 1 isolate 32 harboring Gag-capsid, I138L, A146P, I147L, V159I, V215L, I223A, N252S/N, T280V and S310T and protease R41K/R, I62V, L63P, V77I and I93L mutant gene infected in human MT-2 cells by XTT-as | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID564048 | Antiviral activity against multidrug-resistant HIV1 isolate JSL containing L10I, L24I, I33F, E35D, M36I, N37S, M46L, I54V, R57K, I62V, L63P, A71V, G73S, and V82A mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1219720 | Drug metabolism in human liver microsomes assessed as GSH-conjugated monohydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID321698 | Ratio of EC50 for HIV1 mutant strain 6 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID242868 | Association rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID557286 | Antiviral activity against HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of amprenavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID541164 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID557297 | Ratio of EC50 for HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID278975 | Antiviral activity against HIV1 C8 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID321660 | Inhibition of HIV1 protease | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID417048 | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID446205 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate JSL to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID572581 | Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID369946 | Ratio of EC50 for HIV2 CDC310319 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID658567 | Resistance factor, ratio of EC50 for multidrug-resistant HIV1 106-PR infected in HEK293T cells to wildtype HIV1 infected in HEK293T cells | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID557232 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID322105 | Antiviral activity against nelfinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID278974 | Antiviral activity against HIV1 C7 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID537771 | Antiviral activity against multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID1482914 | Antiviral activity against darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production af | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID519793 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 12T-14Y-19P-40N-41D-61N-62I-96S-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID278956 | Antiviral activity against HIV1 A4 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID374622 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
| Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID278966 | Antiviral activity against HIV1 A14 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID541163 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92Q mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID572582 | Apparent oral clearance in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID369951 | Antiviral activity against wild type HIV2 ROD infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID374627 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID557277 | Ratio of EC50 for HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1482926 | Ratio of IC50 for atazanavir-resistant HIV1 NL4-3 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID541130 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTM184V mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID519546 | Antiviral activity against HIV1 isolate 3 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, E35D, N37D, M461, I54V, L63P, A71V, T74P, I84V, L90M, I93L mutation derived from viral passages with Lopinavi | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID519575 | Antiviral activity against HIV1 P13 infected in human MT4 cells derived from viral passages with A-790742 harboring protease M46I, L63P, A71V, and V82G mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days p | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID525488 | Antigametocyte activity against Plasmodium falciparum harboring GFP-tagged Pfs16 protein assessed as reduction in number of gametocytes after 40 hrs by [3H]hypoxanthine incorporation assay | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID557278 | Ratio of EC50 for HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1725421 | Antiviral activity against DRV resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID374630 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID575063 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I mutation in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID321681 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID1295706 | Aqueous solubility of the compound by shake flask method | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends. |
| AID278973 | Antiviral activity against HIV1 C6 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID519786 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-45K/R-46V-54M-64I/V-69K/R-71V/I-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID566850 | Antiviral activity against HIV-1 MDR/TM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | | | |
| AID343028 | Ratio of Ki for HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID537768 | Antiviral activity against Human immunodeficiency virus 1 clade A isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID1725420 | Antiviral activity against ATV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID532469 | Antiviral activity against Human immunodeficiency virus 1 isolate 6 harboring Gag-capsid I138L and V215L mutant gene and protease L10I, S37N, M46L, G48V, R57K, L63P, I66F, A71V, V82T and I84V mutant gene infected in human MT-2 cells by XTT-assay relative | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID557295 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1380930 | Resistance index, ratio of EC50 for antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID586625 | Antiviral activity against HIV1 harboring mutant protease with matrix K76R mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID586618 | Ratio of EC50 for HIV1 harboring mutant protease with matrix Y79F mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID558369 | Drug level in HIV-infected pregnant woman maternal blood plasma at 400 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID532463 | Antiviral activity against Human immunodeficiency virus 1 isolate 9 harboring Gag-capsid I138L, A146S, I147L, V215L, N252H, T280A, A340G and E345D mutant gene and protease L10I, I13V, K20M, L33V, M36I, S37N, I54V, R57K, I62V, L63P, I66L, A71V, G73S, P79A, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID726411 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID343026 | Ratio of Ki for HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID322112 | Antiviral activity against wild type HIV1 ERS104prc X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID105589 | Cytotoxicity against MT-4 cells | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
| AID519553 | Antiviral activity against HIV1 isolate 10 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20R, L33F, E35D, M36I, N37D, I54L, Q58E, I62V, L63P, A71V, V82A, I84V, L90M mutation derived from vir | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID532466 | Antiviral activity against Human immunodeficiency virus 1 isolate 27 harboring Gag-capsid I138L, S173T/S, V215L, L268M, R275K/R, T280V, S310T, E319D and G357S and protease L10I, I15V, L19V, V32I, L33F, M46I, I54V, K55R, R57K, L63P, C67F, H69Q, A71V, G73C/ | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID589156 | Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone hydroxylation | 2005 | Current drug metabolism, Oct, Volume: 6, Issue:5
| Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity. |
| AID321662 | Antiviral activity against HIV1 3B in presence of 50% human serum | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID1057015 | Inhibition of HIV-1 multidrug-resistant protease 769 preincubated for 20 mins by FRET analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | | | |
| AID162704 | Compound was tested for its inhibitory potency against HIV protease at 0.5 nM | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
| AID278982 | Resistance to HIV1 with protease 46I, 54I and I84A mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID279341 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID297670 | Inhibition of HIV1 Protease M3 variant by FRET based assay | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID1482913 | Antiviral activity against darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID278961 | Antiviral activity against HIV1 A9 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID1057014 | Ratio of IC50 for HIV-1 multidrug-resistant protease 769 to IC50 for HIV-1 NL4-3 wild type protease | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | | | |
| AID446198 | Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID415251 | Metabolic stability in human liver microsomes assessed as inhibition of metabolism at 2 uM by LC/MS/MS analysis in presence of ritonavir | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID446201 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate C to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID369962 | Ratio of EC50 for HIV2 MS infected in human MT4 cells after 18 passages to EC50 for HIV2 MS infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID546990 | Antiviral activity against HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gene assay | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID278984 | Resistance to HIV1 with protease 46I, 54V and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID525477 | Antigametocyte activity against ring stage Plasmodium falciparum D10 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1482923 | Ratio of IC50 for lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID622656 | Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay in presence of 50% human serum | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID537774 | Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 MDRC4 to EC50 for wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID446200 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate B to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID321696 | Ratio of EC50 for HIV1 mutant strain 4 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID443166 | Antiviral activity against HIV1 infected in human MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 6 days by XTT assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
| HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells. |
| AID532478 | Antiviral activity against Human immunodeficiency virus 1 isolate 12 harboring Gag-capsid I138L E207D, V215L, V218P, H219Q, M228I, G248T, T280S, E312D, A340G, G357S and V362I mutant gene and protease S37N, I62V/I, L63P, I64L and V82I mutant gene infected | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID724346 | Inhibition of C-south african HIV-1 protease assessed as hydrolysis of the chromogenic peptide substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 | 2013 | European journal of medicinal chemistry, Feb, Volume: 60 | Linear and cyclic glycopeptide as HIV protease inhibitors. |
| AID1482918 | Ratio of IC50 for darunavir-resistant HIV1 derived from 51 passages harboring protease L10I/I15V/K20R/L24I/V32I/L33F/M36I/M46L/I54M/L63P/K70Q/V82I/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID1422658 | Inhibition of ZMPSTE24 in human KP4 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID1725423 | Antiviral activity against HIV1 DRVR P51 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID369952 | Antiviral activity against HIV2 ROD with protease G17N mutation infected in human CEM cells assessed as inhibition of virus production after 7 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID446196 | Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | | | |
| AID1409312 | Antiviral activity against darunavir-resistant HIV1 at passage 30 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID442713 | Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
| AID279347 | Antiviral activity against HIV1 isolate 5512 with D30N, M461 and V771 mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID328892 | Inhibition of mouse RCE1 expressed in delta ste24 delta rce1 yeast | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID547007 | Antiviral activity against HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID246194 | Protease inhibitory activity against HIV-1 r13034 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID532655 | Antiviral activity against Human immunodeficiency virus 1 isolate 39 harboring Gag-capsid A146P, I147L, V215L, M228I, G248A, R286K, A326S, G357S and V362I mutant gene and protease K14R, E35D, M36I, S37N, R41K, K45R, D60E, I62V and I64V mutant gene infecte | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID417028 | Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmax of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID586617 | Ratio of EC50 for HIV1 harboring mutant protease with matrix A81T mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID416864 | Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID432028 | Antimalarial activity against Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
| Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2. |
| AID322102 | Antiviral activity against saquinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID322100 | Selectivity index, ratio of CC50 for MT2 cells to EC50 for HIV1 LAI | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID519782 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 5L/F-14Y/H-17G/D-43T-54I/M-62V/A-70R/K-71I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID1845236 | Inhibition of SARS-CoV-2 MPro | 2021 | Bioorganic & medicinal chemistry, 01-01, Volume: 29 | Protease targeted COVID-19 drug discovery and its challenges: Insight into viral main protease (Mpro) and papain-like protease (PLpro) inhibitors. |
| AID525279 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1422656 | Inhibition of ZMPSTE24 in human U2OS cells assessed as increase in intracellular accumulation of prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID564063 | Antiviral activity against HIV1 expressing protease L10F/M46M,I/Q61Q mutant infected in human MT4 cells selected at 1 uM of GRL-396 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID564032 | Cytotoxicity against human MT2 cells after 7 days by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID442704 | Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
| AID279346 | Antiviral activity against HIV1 isolate 5512 with V321 and M46L mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID521549 | Antiviral activity against HIV 2 subtype H expressing 10I-40P-41Y-60H-63N-70T-73G-89L-92E protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID446204 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate MM to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID162693 | Inhibitory activity (0.5 nM) against Protease | 2004 | Bioorganic & medicinal chemistry letters, May-17, Volume: 14, Issue:10
| Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships. |
| AID322101 | Antiviral activity against HIV1 NL4-3 in MT4 cells by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID541132 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTK103N mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID343017 | Inhibition of HIV1 recombinant protease A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID519784 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 54M-65E-71I-74N-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID575060 | Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations and protease L76V mutation in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID532457 | Antiviral activity against Human immunodeficiency virus 1 isolate 26 harboring Gag-capsid I138L, A146S, I147L, E312D, A326S, L337M, and A340G mutant gene and protease T4S, L10F, V11L, I13V, I15V, K20A, V32I, L33F, M36I, S37D, K43T, M46I, I54L, I62V, L63P, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID557239 | Ratio of drug level in 2 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID541131 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RT-6TAMs mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID374603 | Resistance index, ratio of EC50 for HIV1 with protease 54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1323585 | Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide at 5 to 50 uM preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies. |
| AID278959 | Antiviral activity against HIV1 A7 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID163477 | Binding affinity against ritonavir-resistant strains. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID564042 | Antiviral activity against wild type HIV1 ERS104 containing protease L36P mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1057016 | Inhibition of HIV-1 NL4-3 wild type protease expressed in Escherichia coli preincubated for 20 mins by FRET analysis | 2013 | Bioorganic & medicinal chemistry, Dec-01, Volume: 21, Issue:23
| Ligand modifications to reduce the relative resistance of multi-drug resistant HIV-1 protease. |
| AID541109 | Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID328888 | Effect on HDJ2 farnesylation in mouse fibroblast cells at 20 uM after 24 hrs by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID1219735 | Drug metabolism in human liver microsomes assessed as CYP1A2-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID546996 | Antiviral activity against HIV1 subtype C harboring protease L10R, M46I, I54V, V82S mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID683726 | Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 100 mg/kg, po co-administered with 50 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculation | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Targeting the liver stage of malaria parasites: a yet unmet goal. |
| AID519792 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-61N-64V-71I-90M-95I protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T2 during compound treatment measured after 3 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID532455 | Antiviral activity against Human immunodeficiency virus 1 isolate 8 harboring Gag-capsid V215T mutant gene and protease L10I, L24I, L33F, S37N, R41K, I54V, D60E, I62V, L63P, A71V, V77I, V82A and I84V mutant gene infected in human MT-2 cells by XTT-assay r | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID374639 | Resistance index, ratio of EC50 for HIV1 with protease 46L/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID547004 | Antiviral activity against HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporte | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID557221 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID274380 | Inhibition of HIV1 protease L10I/G48V/I54V/L63P/V82A mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
| AID343018 | Inhibition of HIV1 recombinant protease V32I/I47A mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID105401 | Antiviral activity against the cytopathic effects of HIV IIIB in MT-4 cells was assayed in the presence of 50% human serum | 2002 | Bioorganic & medicinal chemistry letters, Nov-04, Volume: 12, Issue:21
| Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships. |
| AID247984 | Inhibitory concentration against wild type human immunodeficiency virus | 2005 | Bioorganic & medicinal chemistry letters, May-02, Volume: 15, Issue:9
| Oximinoarylsulfonamides as potent HIV protease inhibitors. |
| AID532471 | Antiviral activity against Human immunodeficiency virus 1 isolate 31 harboring Gag-capsid I138L, S173T, V215L, I223N, M228L, G248Q, N252H, T280V and E312D mutant gene and protease I13V, K14R/K, M36I, S37N, I64V, H69K and I72V mutant gene infected in human | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID566851 | Antiviral activity against HIV-1 MDR/MM infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID586622 | Ratio of EC50 for HIV1 harboring HIV1 harboring wild type 8.9NSX with gag RF79F and T81A mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID547018 | Selectivity ratio of EC50 for HIV1 subtype B harboring protease polymorphism at M36 position and L10F, V82A mutant gene to EC50 for wild type HIV1 subtype B | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID557279 | Ratio of EC50 for HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1482905 | Antiviral activity against amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID274379 | Inhibition of wild type HIV1 protease Q7K mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
| AID582276 | Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID278985 | Resistance to HIV1 with protease 46I, 54M/V and I84A mutation in HEK 293 relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID417038 | Effect on tenofovir disoproxil fumarate metabolism in HIV infected patient assessed as change in plasma Cmin of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID279345 | Antiviral activity against wild type HIV1 in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID532462 | Antiviral activity against Human immunodeficiency virus 1 isolate 37 harboring Gag-capsid V135I, I138P, V143I, Q182H, V215L/V, V218P/A, H219Q, I223V, E230D, N252S, T280A, R286K, K302R and G357S mutant gene and protease S37D, R41K, L63P and I93L mutant gen | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID369959 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 11 passages | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID274381 | Inhibition of HIV1 protease D30N/L63P/N88D mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
| AID532467 | Antiviral activity against Human immunodeficiency virus 1 isolate 1 harboring Gag-capsid I138L, V159I, E203D, V215L, I223V, T280V, E312D and V323I mutant gene and protease L10I, K20R, M36I, S37N, G48V, I54M, I62V, L63P, A71V, I72V, V82A, I84V, L90M and I9 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID698059 | Selectivity index, ratio of Ki for HIV protease V82A mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Rational approaches to improving selectivity in drug design. |
| AID352084 | Antimalarial activity after 24 hrs against chloroquine-resistant Plasmodium falciparum W2 by [3H]hypoxanthine uptake | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
| Synthesis and antimalarial activity of hydroxyethylpiperazine derivatives. |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | | | |
| AID1380926 | Antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID321679 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID322117 | Antiviral activity against HIV1 MDR/C X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID321677 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID279340 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 150V mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID668816 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for Human immunodeficiency virus 1 3B | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID541172 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID1717754 | Antiviral activity against SARS-CoV isolate Frankfurt-1 infected in African green monkey Vero E6 cells incubated for 3 days | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | | | |
| AID1409308 | Antiviral activity against Atazanavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID446193 | Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID1193134 | Antimalarial activity against Plasmodium knowlesi infected Chinese rhesus macaques assessed as parasitemia level in blood smears at 40 mg/kg, intragastric treated 5 days before infection measured between day 0 to 7 by Giemsa-staining in presence of ritona | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
| Ritonavir-boosted indinavir but not lopinavir inhibits erythrocytic stage Plasmodium knowlesi malaria in rhesus macaques. |
| AID532657 | Antiviral activity against Human immunodeficiency virus 1 isolate 4 harboring Gag-capsid A146P, V159I, K162R, Q182S, T186I, V215L, I223G/V, N252G, P255A, E260D, E312D and G357S mutant gene and protease L10R, S37N, M46L, I62V, L63P, A71V, T74S, V82T, L90M | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID372181 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50L/54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID572574 | Cmax in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID557244 | Toxicity in HIV-infected Thai pregnant women assessed as adverse effect at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID374625 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID519544 | Antiviral activity against HIV1 isolate 1 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10V, I15V, G16E, K20R, E35D, M36I, R41K, M46I, I54V, R57K, Q61N, I64L, A71V, I72R, V82A, L89I, L90M, Q92K mutation | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID374638 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID532458 | Antiviral activity against Human immunodeficiency virus 1 isolate 28 harboring Gag-capsid I138M mutant gene and protease L10I, I13V, L23I, L33F, S37N, M46I, I54V, K55R, R57K, Q58E, D60E, I62V, L63P, A71I, I72V, L76V, V77I, V82A, I84V, I85V, L89M, L90M and | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID683725 | Antimalarial activity against liver stages of Plasmodium yoelii 17XNL infected in Swiss Webster mouse assessed as reduction in liver parasite load at 25 mg/kg, po co-administered with 12.5 mg/kg ritonavir incubated for 6 hrs prior to sporozoite inoculatio | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Targeting the liver stage of malaria parasites: a yet unmet goal. |
| AID322110 | Antiviral activity against HIV1 GRL98065p30 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID321680 | Metabolic stability in dog liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID322111 | Antiviral activity against HIV1 GRL98065p40 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID537766 | Inhibition of multidrug resistant HIV1 protease L101I, L36P, A71V, G73S, I84V, L90M mutant by FRET | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID668810 | Antiviral activity against Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID328894 | Effect on change in ZMPSTE24 mRNA expression level in mouse fibroblasts at 20 uM after 10 days by PCR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID369943 | Antiviral activity against HIV2 CDC310319 isolate infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID321694 | Ratio of EC50 for HIV1 mutant strain 2 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID239810 | Equilibrium dissociation constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID375205 | Ratio of EC50 for multidrug-resistant HIV1 isolate MM to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID553577 | Antiviral activity against HIV1 MM harboring L10I/K43T/M46L/I54V/L63P/A71V/V82A/L90M/Q92K in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID519785 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-17D-40D-43I-46V-66V/A-70R/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID374609 | Resistance index, ratio of EC50 for HIV1 with protease 84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID557299 | Ratio of EC50 for HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID322097 | Antiviral activity against HIV2 EHO in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID372184 | Resistance index, ratio of EC50 for HIV1 with protease 37T/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID519579 | Antiviral activity against HIV1 clone4 infected in HEK293 cells harboring A-790742-selected protease L33F, A71V, G73S, V77I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pN | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID374601 | Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID279338 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID278967 | Antiviral activity against HIV1 A15 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID321685 | Antiviral activity against wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID668808 | Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID1380929 | Resistance index, ratio of EC50 for antiviral activity against LPV resistant HIV1 harboring protease L10F/M46/I54V/V82A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID297671 | Antiviral activity against HIV1 infected MT4 cells by MTT method | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID541173 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K and Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID375199 | Antiviral activity against wild type HIV1 isolate ERS104pre infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID532465 | Antiviral activity against Human immunodeficiency virus 1 isolate 25 harboring Gag-capsid I138M, S173A, V215L, N252S, I256T, S310T/S, A340G and E345D mutant gene and protease L10F, V11I, I13V, K20I, V32I, L33F, E34Q, E35D, M36I, S37N, K43T, M46I, F53Y, I5 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID586628 | Ratio of EC50 for HIV1 harboring 8gpNS with K76R, F79Y, and A81T mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID343027 | Ratio of Ki for HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant to Ki for wild-type HIV1 BH10 protease expressed in Escherichia coli | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID369960 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as p27 antigen level after 18 passages | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID369947 | Antiviral activity against HIV2 MS infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID553576 | Antiviral activity against HIV1 TM harboring L10I/K14R/R41K/M46L/I54V/L63P/A71V/V82A/L90M/I93L in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID553571 | Antiviral activity against HIV1 LAI infected in human MT2 cells after 7 days by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID321690 | Antiviral activity against HIV1 mutant strain 5 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID519573 | Antiviral activity against HIV1 P15 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L33L/F, K45I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID668817 | Antiviral activity against Human immunodeficiency virus 1 3B expressing wild-type protease infected in human MT4 cells in presence of 50% human serum | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID519538 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in presence of 50% human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID343022 | Ratio of Ki for HIV1 recombinant protease D30N/N88D mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID374612 | Resistance index, ratio of EC50 for HIV1 with protease 30N/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID532475 | Antiviral activity against Human immunodeficiency virus 1 isolate 38 harboring Gag-capsid I138L, I147L, V215L, H219Q/H, I223V, N252H, P292S, A336S/A and A340G mutant gene and protease E35D, S37A and L63P mutant gene infected in human MT-2 cells by XTT-ass | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID564040 | Antiviral activity against HIV1 expressing protease L10F/M46I/I54V/V82A mutant infected in human MT4 cells selected at 5 uM of Lopinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID557298 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/M46I/I54V/V82A amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1482915 | Antiviral activity against nelfinavir-resistant HIV1 NL4-3 harboring protease L10F/K20T/D30N/K45I/A71V/V77I mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID369944 | Ratio of EC50 for HIV2 MS to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID588986 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1A2 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
| AID374604 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/73S/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID257271 | Antiviral activity against HIV1 in the presence of 50% human serum | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
| Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
| AID586624 | Antiviral activity against HIV1 harboring wild type 8.9NSX with mutant amino acid 116 insertion infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID1219721 | Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID1219719 | Drug metabolism in human liver microsomes assessed as compound-GSH adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID557276 | Antiviral activity against HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID322098 | Antiviral activity against HIV2 ROD in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID582278 | Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID1725418 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID622659 | Antiviral activity against HIV1 isolate 1 harboring protease L10I, E35D, N37D, M46I, I54V, G57R, L63P, A71V, T74P, I84V, L90M, I93L mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID328886 | Toxicity in HEK293 cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID374610 | Resistance index, ratio of EC50 for HIV1 with protease 33F/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID322115 | Antiviral activity against HIV1 MDR/JSL R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID557287 | Antiviral activity against HIV1 NL4-3 harboring L10F/L24I/M46I/L63P/A71V/G73S/V82T amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of indinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1482919 | Antiviral activity against saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassa | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID557293 | Ratio of EC50 for HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID532454 | Antiviral activity against Human immunodeficiency virus 1 isolate 7 harboring Gag-capsid I138L, I147L, S173A, V215L, I223V, T242N, G248A, N252A, I126T, T280V and E312D mutant gene and protease K20R, M36I, R41K, M46I, L63Q, I64V, P79S, V82F and L90M mutant | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID521548 | Antiviral activity against Human immunodeficiency virus type 1 (BRU ISOLATE) after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID564037 | Antiviral activity against HIV1 expressing protease L10I/G48V/I54V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of saquinavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID321697 | Ratio of EC50 for HIV1 mutant strain 5 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID664437 | Inhibition of South African HIV1 subtype C protease expressed in Escherichia coli BL21S4 (DE3)pLysS cells using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | Synthesis and molecular modelling studies of novel carbapeptide analogs for inhibition of HIV-1 protease. |
| AID519787 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-40D-70K-72R/K-91T/S protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID566847 | Antiviral activity against HIV-1 MDR/B infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID278971 | Antiviral activity against HIV1 C4 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID248600 | Inhibitory concentration against wild type Human immuno deficiency virus (D545701) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
| Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
| AID328883 | Toxicity in mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID525281 | Antimicrobial activity against Plasmodium falciparum harboring HFP-tagged Pfs16 protein after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID726413 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID519572 | Antiviral activity against HIV1 P9 infected in human MT4 cells derived from viral passages with A-790742 harboring protease V82V/L and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infectio | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID343019 | Inhibition of HIV1 recombinant protease L10I/I15V/E35D/N37S/R41K/I62V/L63P/A71V/G73S/L90M mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID525484 | Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
| AID278964 | Antiviral activity against HIV1 A12 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID343015 | Inhibition of HIV1 recombinant protease D30N/N88D mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID238043 | Binding affinity for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
| AID369942 | Antiviral activity against HIV2 CBL-23 infected in human PBMC assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID1409313 | Antiviral activity against darunavir-resistant HIV1 at passage 51 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID353764 | Cmax in Sprague-Dawley rat plasma at 5 mg/kg, po coadministered with RTV | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
| AID374620 | Resistance index, ratio of EC50 for HIV1 with protease 32I/46I/47V/50L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID519790 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-61N-99L protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID519556 | Antiviral activity against HIV1 isolate 13 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, K14R, L33F, E34Q, R41K, K45R, M46I, I50V, K55R, L63P, A71V, G73T, V77I, V82A, L90M, I93L mutation derived fr | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID374629 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54M/82L/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID525166 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
| Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | | | |
| AID547237 | Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease L76V, M46I, I84V mutant gene and polymorphism at M36 position to EC50 for wild type HIV1 subtype CRF02_AG | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID353740 | AUC in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
| AID537773 | Resistance index, ratio of EC50 for multidrug resistant Human immunodeficiency virus 1 harboring protease M46I, I54V, V82A and L90M mutant to EC50 for wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID572578 | Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID415249 | Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID557280 | Ratio of EC50 for HIV1 A harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID698061 | Selectivity index, ratio of Ki for HIV protease L10I mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Rational approaches to improving selectivity in drug design. |
| AID557294 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/V32I/M46I/I54M//A71V/I84V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID532464 | Antiviral activity against Human immunodeficiency virus 1 isolate 30 harboring Gag-capsid I138L, V215L, R286K and Q311A mutant gene and protease I13V, E35D, S37N and L63P mutant gene infected in human MT-2 cells by XTT-assay relative to wild-type | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID541167 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring Q148K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID1219737 | Maximum plasma concentration in healthy human at 400 mg | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID519548 | Antiviral activity against HIV1 isolate 5 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10F, I15V, M46I, L63P, A71V, I72L, V82T, I84V, I85V, L90M mutation derived from viral passages with Lopinavir asse | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1482927 | Ratio of IC50 for tipranavir-resistant HIV1 NL4-3 harboring protease L10I/L33I/M36I/M46I/I54V/K55R/I62V/L63P/A71V/G73S/V82T/L90M/I93L mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID374611 | Resistance index, ratio of EC50 for HIV1 with protease 48V/54V/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | | | |
| AID519794 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 12Q-14R-17G/D-19P-61N-62I-92A protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID588982 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B3 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
| AID564029 | Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID343016 | Inhibition of HIV1 recombinant protease M46I/A71V/V82T/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID374624 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1350495 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days in absence of human serum by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
| AID328877 | Toxicity in human AG07095 cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID375202 | Antiviral activity against multidrug-resistant HIV1 isolate C infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID242866 | Dissociation rate constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | | | |
| AID322116 | Antiviral activity against HIV1 MDR/B X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID343020 | Inhibition of HIV1 recombinant protease L10I/L24I/L33F/M46L/154V/L63P/A71V/V82A/I84V mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID1409310 | Antiviral activity against amprenavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID586626 | Antiviral activity against HIV1 harboring mutant protease with matrix Y79F mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID279343 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and 184V mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID322096 | Antiviral activity against HIV1 LAI in MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID321693 | Ratio of EC50 for HIV1 mutant strain 1 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID564061 | Antiviral activity against HIV1 expressing protease L10F/M46I/T91S mutant infected in human MT4 cells selected at 1 uM of GRL-246 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID321699 | Ratio of EC50 for HIV1 mutant strain 7 to EC50 for wild type HIV1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID582283 | Tmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID321676 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID519542 | Antiviral activity against HIV1 B26 infected in human MT4 cells harboring protease L33F, K45I, M46I, I50V, I54V, A71V, and V82F mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infectio | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID278965 | Antiviral activity against HIV1 A13 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID257270 | Antiviral activity against HIV1 in the absence of human serum | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
| Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
| AID104835 | Effective concentration against ritonavir -resistant strains in MT-4 cells. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID557218 | AUC (0 to 12 hrs) in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID322103 | Antiviral activity against ritonavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID532461 | Antiviral activity against Human immunodeficiency virus 1 isolate 5 harboring Gag-capsid I138M, V159I, T280V and S310T mutant gene and protease I13V, D30N, L33I, E35D, M36I, S37N, M46I/L, I54V, I62V, L63P, I66M/I, A71N/T, I72T/I, V82L/V, N88D, L90M and I9 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID519781 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 14H-17D-43T-68N/D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID726416 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/M46I/I64V/I84V/L90M/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID248546 | Inhibitory concentration against wild type Human immuno deficiency virus (HXB2) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
| Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
| AID1307691 | Binding affinity to HIV1 protease I47A mutant | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands. |
| AID1873200 | Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells mediated pheophorbide A efflux preincubated with PhA followed by compound addition and measured after 60 mins by flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
| AID1323586 | Binding affinity to mouse anti-dsDNA monoclonal antibody R4A assessed as inhibition of RA4 binding to DWEYS peptide preincubated for 1 hr followed by DWEYS peptide addition measured after 1 hr by ELISA | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Amending HIV Drugs: A Novel Small-Molecule Approach To Target Lupus Anti-DNA Antibodies. |
| AID279342 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 154M and L90M mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID1482909 | Antiviral activity against lopinavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/M46I/I47A/A71V/I84V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID1725419 | Antiviral activity against LPV-resistant HIV1 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID343014 | Inhibition of wild-type HIV1 BH10 protease expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID372190 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/54V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID374607 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID415248 | Fold resistance, ratio of EC50 for HIV1 bearing protease gene with A17 mutation to EC50 for wild-type HIV1 pNL4-3 | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID1422660 | Inhibition of ZMPSTE24 in human HCT116 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID1593661 | Prodrug conversion in cannulated Sprague-Dawley rat plasma assessed as atazanavir formation at 3 mg/kg equiv of atazanavir administered orally by UPLC/MS/MS analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. |
| AID374634 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1350502 | Inhibition of protease L10F/V32I/M46I/I47V/Q58E/I84V mutant in HIV1 A17 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
| AID1219724 | Drug metabolism in human liver microsomes assessed as GSH-conjugated hydroxylated DMP adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID541168 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID586619 | Ratio of EC50 for HIV1 harboring mutant protease with matrix K76R mutant to EC50 for wild type HIV1 | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID519791 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 14Y-19P-33I-61N-71I-75M-84V-90M protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID375200 | Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1
| Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
| AID28092 | Cmax value in the period of 8 hr after dosing, when administered with ritonavir. | 2000 | Journal of medicinal chemistry, Feb-10, Volume: 43, Issue:3
| Protease inhibitors: current status and future prospects. |
| AID519541 | Antiviral activity against HIV1 A17 infected in human MT4 cells harboring protease L10F, V32I, M46I, I47V, Q58E, and I84V mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post infection meas | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID278953 | Antiviral activity against HIV1 A1 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID372188 | Resistance index, ratio of EC50 for HIV1 with protease 46L mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID372185 | Resistance index, ratio of EC50 for HIV1 with protease 46I/53L/82T/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID575062 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, V82A and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID537769 | Antiviral activity against Human immunodeficiency virus 1 clade B isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID572575 | AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID374605 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46L/54V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID375207 | Ratio of EC50 for multidrug-resistant HIV1 isolate G to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID279348 | Antiviral activity against HIV1 isolate 5512 with M36I/M and V82T mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID416860 | Increase in P-glycoprotein-mediated forward permeation of tenofovir disoproxil fumarate in human Caco-2 cells at 2 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID415250 | Metabolic stability in human liver microsomes assessed as compound disappearance at 2 uM by LC/MS/MS analysis in presence of ritonavir | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID541166 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring G140S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID257273 | Antiviral activity against Lopinavir resistant HIV A17 mutant strain | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
| Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
| AID278980 | Resistance to HIV1 with protease 46M, 54I and I84C mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID374615 | Resistance index, ratio of EC50 for HIV1 with protease 46I/47A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID328889 | Effect on Rap1A isoprenylation in mouse fibroblast cells at 20 uM after 24 hrs by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID321682 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID557292 | Antiviral activity against HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of GRL-02031 by E | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1717745 | Antiviral activity against HCoV-229E harboring GFP infected in human Huh-7 cells treated 1 hr prior to viral infection by fluorometric analysis | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID557284 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of p24 gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID566849 | Antiviral activity against HIV-1 MDR/G infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID328880 | Toxicity in ICMT deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID278963 | Antiviral activity against HIV1 A11 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID446197 | Antiviral activity against multidrug-resistant HIV1 isolate TM infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID322114 | Antiviral activity against HIV1 MDR/MM R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID321691 | Antiviral activity against HIV1 mutant strain 6 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID658565 | Antiviral activity against multidrug-resistant HIV1 106-PR infected in HEK293T cells assessed as inhibition of viral replication after 4 days by beta-galactosidase reporter gene assay | 2012 | Journal of natural products, Mar-23, Volume: 75, Issue:3
| Library-based discovery and characterization of daphnane diterpenes as potent and selective HIV inhibitors in Daphne gnidium. |
| AID372183 | Resistance index, ratio of EC50 for HIV1 with protease 37S/41K/70E mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1669454 | Inhibition of HIV1 NL4-3 protease expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 mins by FRET as | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
| AID726415 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID1219736 | Drug metabolism in human liver microsomes assessed as CYP2D6-mediated GSH-conjugated hydroxylated DMP adduct formation adduct formation at 2 uM after after 30 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID374600 | Antiviral activity against wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID372191 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID525290 | Antigametocyte activity against Plasmodium falciparum D10 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID668814 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID586623 | Antiviral activity against 8gpNS with amino acid 116 insertion removed HIV1 infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID369950 | Antiviral activity against HIV1 NL4-3 infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID553574 | Antiviral activity against HIV1 ERS104pre infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID278972 | Antiviral activity against HIV1 C5 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID557274 | Antiviral activity against HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID519576 | Antiviral activity against HIV1 clone1 infected in HEK293 cells harboring A-790742-selected protease I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID415246 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells after 5 days by MTT assay in presence of 50% human serum | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID106958 | Compound was tested for antiviral activity against HIV-IIIB in MT-4 cells in presence of 50% human serum | 2002 | Bioorganic & medicinal chemistry letters, Apr-22, Volume: 12, Issue:8
| Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir). |
| AID564043 | Antiviral activity against multidrug-resistant HIV1 isolate B containing protease L10I, K14R, L33I, M36I,M46I, F53I, K55R, I62V, L63P, A71V, G73S, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID322118 | Antiviral activity against HIV1 MDR/G X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID564046 | Antiviral activity against multidrug-resistant HIV1 isolate TM containing L10I, K14R, R41K, M46L, I54V, L63P, A71V, V82A, L90M, and I93L mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID564039 | Antiviral activity against HIV1 expressing protease L10F/M46I/I50V/A71V/I84V/L90M mutant infected in human MT4 cells selected at 5 uM of amprenavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1409309 | Antiviral activity against lopinavir-resistant HIV1 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID374633 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID668811 | Antiviral activity against Human immunodeficiency virus 1 isolate M3 expressing protease L10I, K20R, M36I, G48V, I62V, A71V, V82A, I93L mutant infected in human MT4 cells | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID321686 | Antiviral activity against HIV1 mutant strain 1 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID1474092 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID396259 | Antiviral activity against HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
| AID537767 | Antiviral activity against wild type Human immunodeficiency virus 1 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID1678482 | Antiviral activity against SARS-CoV-2 infected in Vero E6 cells preincubated for 1 hr followed by viral infection at MOI of 0.02 and measured after 48 hrs by qRT-PCR method | 2020 | ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
| Identification of 14 Known Drugs as Inhibitors of the Main Protease of SARS-CoV-2. |
| AID374619 | Resistance index, ratio of EC50 for HIV1 with protease 30N/33F/46L/54L/84V/88D mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID257272 | Antiviral activity against indinavir resistant HIV IND-R mutant strain | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
| Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
| AID278970 | Antiviral activity against HIV1 C3 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID519555 | Antiviral activity against HIV1 isolate 12 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, K20I, E35D, M36I, M46I, I50V, I54V, R57K, I62V, L63P, A71V, V82A, L89V, L90M, Q92K mutation derived fr | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID278979 | Resistance to HIV1 with protease 46M, 54I and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID443165 | Inhibition of HIV1 protease expressed in Escherichia coli by fluorometric assay | 2010 | Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
| HIV-1 protease inhibitors with a transition-state mimic comprising a tertiary alcohol: improved antiviral activity in cells. |
| AID566848 | Antiviral activity against HIV-1 MDR/C infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID575059 | Antiviral activity against Human immunodeficiency virus 1 harboring protease inhibitor resistance-associated mutations assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID278977 | Antiviral activity against HIV1 C10 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID625397 | Antimalarial activity against chloroquine resistant, mefloquine sensitive Plasmodium falciparum W2 infected in human erythrocytes by [3H]-hypoxanthine incorporation assay | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
| Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3. |
| AID1065160 | Inhibition of Plasmodium falciparum DC6 plasmepsin-5 using DABCYL-GNKRTLAQKQG-EDANS as substrate measured every 15 mins of 75 mins by fluorescence assay | 2014 | ACS medicinal chemistry letters, Jan-09, Volume: 5, Issue:1
| Evaluation of aminohydantoins as a novel class of antimalarial agents. |
| AID541133 | Selectivity ratio of EC50 for antiviral activity against NNRTI-resistant HIV1 harboring RTY181C mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID582280 | Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID415282 | Antiviral activity against HIV1 bearing protease gene with B26 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID557283 | Ratio of EC50 for HIV1 G harboring L10I/V11I/T12E/I15V/L19I/R41K/M46L/L63P/A71T/V82A/L90M in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID1380927 | Antiviral activity against APV resistant HIV1 harboring protease L10F/M46I/I50V/I85V mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID532452 | Antiviral activity against Human immunodeficiency virus 1 isolate 22 harboring Gag-capsid V215L, H219Q, I223V, N252S, P255A, L268M and A340G mutant gene and Protease L19I, E35D, M36I, S37N, L63P, V77I and I93L mutant gene infected in human MT-2 cells by X | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID160461 | Inhibitory activity against HIV protease | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). |
| AID442705 | Antiviral activity against HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
| AID278960 | Antiviral activity against HIV1 A8 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID557237 | Ratio of drug level before intrapartum initiation to 30 days pre-last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID246193 | Protease inhibitory activity against HIV-1 r13025 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID1717747 | Cytotoxicity against African green monkey Vero E6 cells incubated for 3 days by the MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID557241 | Ratio of drug level in 4 hrs to 30 days post last dose of HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID698060 | Selectivity index, ratio of Ki for HIV protease G48V mutant to Ki for HIV1 wild type protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Rational approaches to improving selectivity in drug design. |
| AID278968 | Antiviral activity against HIV1 C1 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID726412 | Selectivity ratio of EC50 for Human immunodeficiency virus 1 3B clinical isolate harboring L10I/I13V/M46I/I50V/L63P/L76V protease mutant to EC50 for wild type Human immunodeficiency virus 1 3B | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID532474 | Antiviral activity against Human immunodeficiency virus 1 isolate 35 harboring Gag-capsid V159I, I223T, N252S, A326S/A, A340G and G357S mutant gene and protease I15V, G16E, E35D, S37N, L63H and I72V mutant gene infected in human MT-2 cells by XTT-assay re | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID1669455 | Inhibition of HIV1 NL4-3 protease I84V mutant expressed in Escherichia coli TAP-106 cells using EDANS/DABCYL-labelled 10-amino acid containing protease cleavage site as substrate preincubated for 1 hr followed by substrate addition and measured for 60 min | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Structural Analysis of Potent Hybrid HIV-1 Protease Inhibitors Containing Bis-tetrahydrofuran in a Pseudosymmetric Dipeptide Isostere. |
| AID415247 | Antiviral activity against HIV1 bearing protease gene with A17 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID564033 | Selectivity ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI infected human MT2 cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID396261 | Ratio of EC50 for HIV1 drug resistant mutant isolates from protease inhibitor treated HIV patient to EC50 for drug sensitive HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV. |
| AID1482922 | Ratio of IC50 for amprenavir-resistant HIV1 NL4-3 harboring protease L10F/V32I/L33F/M46L/I54M/A71V mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID532470 | Antiviral activity against Human immunodeficiency virus 1 isolate 10 harboring Gag-capsid I138L, I147L, V159I, V215L, G248A, I256V, T280V, R286K and N315H mutant gene and protease L10I, K20R, E35D, M36I, S37N, R41K, K45R, F53L, I54V, L63P, I64V, A71T, V82 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID374618 | Resistance index, ratio of EC50 for HIV1 with protease 33F/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID572573 | Cmin in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID353733 | Cmax in po dosed Beagle dog at dose molar equivalent to 5 mg/kg LPV, po coadministered with RTV dosed as 5% dextrose containing solution | 2009 | Journal of medicinal chemistry, May-14, Volume: 52, Issue:9
| Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir. |
| AID575064 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I and L76V mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID1422659 | Inhibition of ZMPSTE24 in human SW1990 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID525289 | Antigametocyte activity against Plasmodium falciparum D10 trophozoites assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID519551 | Antiviral activity against HIV1 isolate 8 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, I13V, L33F, E34Q, R41K, M46I, I54V, K55R, R57K, Q58E, I62V, L63P, A71V, I72I/T, G73S, V82A, I84V, L90M mutati | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | | | |
| AID1725422 | Antiviral activity against HIV1 DRVR P30 infected in human MT4 cells incubated for 7 days by fully automated chemiluminescent enzyme immunoassay | 2020 | ACS medicinal chemistry letters, Oct-08, Volume: 11, Issue:10
| Design, Synthesis, and X-ray Studies of Potent HIV-1 Protease Inhibitors with P2-Carboxamide Functionalities. |
| AID557229 | Drug level in HIV-infected Thai pregnant women serum before intrapartum initiation of 400 mg, po bid in combination with 100 mg, po bid ritonavir | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID249499 | Toxicity value against wild type HIV-1 IIIB was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
| AID1482917 | Ratio of IC50 for darunavir-resistant HIV1 derived from 30 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/K70R/V82A/I84V/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID590915 | Inhibition of HIV1 subtype C protease expressed in Escherichia coli BL21 assessed as hydrolysis of substrate using chromogenic substrate Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 by spectrophotometric analysis | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8
| Pentacycloundecane-based inhibitors of wild-type C-South African HIV-protease. |
| AID525167 | Antimicrobial activity against chloroquine-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as potentiation of choloroquine-mediated antimalarial activity by light microscopy | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
| Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
| AID525171 | Antimicrobial activity against chloroquine-resistant Plasmodium chabaudi ASCQ infected in NIH mice (Mus musculus) assessed as potentiation of 2.5 mg/kg chloroquine-mediated antimalarial activity at 100 mg/kg, perorally administered after 72 hrs post inocu | 2008 | Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
| Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo. |
| AID374635 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID586627 | Antiviral activity against HIV1 harboring mutant protease with matrix A81T mutant infected in HEK293T cells assessed as inhibition of viral replication after 48 hrs by luciferase assay | 2011 | Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
| Three residues in HIV-1 matrix contribute to protease inhibitor susceptibility and replication capacity. |
| AID321687 | Antiviral activity against HIV1 mutant strain 2 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID519574 | Antiviral activity against HIV1 P21 infected in human MT4 cells derived from viral passages with A-790742 harboring protease L23I, L33F, K45I, A71A/V, V77I, V82L, and I84V mutation assessed as reduction in viral cytopathogenicity treated 1 hr post infecti | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID322099 | Cytotoxicity against human MT2 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID372189 | Resistance index, ratio of EC50 for HIV1 with protease 46I mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID564030 | Antiviral activity against HIV2 EHO infected in human MT2 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID519537 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID557220 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 2 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | | | |
| AID322121 | Antiviral activity against HIV1 BaL R5 subtype B in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID321689 | Antiviral activity against HIV1 mutant strain 4 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID242869 | Association rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID532459 | Antiviral activity against Human immunodeficiency virus 1 isolate 36 harboring Gag-capsid I138L, A146P, S165N/S, E207D, V215L and E312D mutant gene and protease K14R/K, I15V, E35D, S37D, R57K/R and L63P mutant gene infected in human MT-2 cells by XTT-assa | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID618427 | Cytotoxicity against human MT4 cells after 5 days by XTT assay | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach. |
| AID374602 | Resistance index, ratio of EC50 for HIV1 with protease 24I/33F/46I/54L/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID1474090 | Ratio of drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID446203 | Selectivity ratio of IC50 for multidrug-resistant HIV1 isolate TM to IC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID374616 | Resistance index, ratio of EC50 for HIV1 with protease 46I/88S mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID705597 | Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
| AID1482912 | Antiviral activity against darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemil | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID278981 | Resistance to HIV1 with protease 46I, 54I and I84V mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID1422662 | Antimigratory activity against human KP4 cells at 10 uM after 10 days by crystal violet staining-based assay | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID547234 | Selectivity ratio of EC50 for HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype C | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID683727 | Antimalarial activity against liver stages of Plasmodium berghei 17XNL infected in human Hepa1-6 cells assessed as reduction in liver parasite load at 10 uM/L incubated for 1 hr prior to sporozoite inoculation measured after 46 to 48 hrs by fluorescence m | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Targeting the liver stage of malaria parasites: a yet unmet goal. |
| AID726417 | Cytotoxicity against human MT4 cells | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID622657 | Antiviral activity against HIV1 A17 harboring protease L10F, V32I, M46I, I47V, Q58E and I84V mutant infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay relative to wild type HIV1 pNL4-3 | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID321692 | Antiviral activity against HIV1 mutant strain 7 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID572576 | Half life in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and NRTI | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID519795 | Antiviral activity against HIV 2 subtype B clinical isolate expressing 41D protease gene sequence from HIV2 infected patient plasma and PBMC obtained before compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID343024 | Ratio of Ki for HIV1 recombinant protease A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID541165 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E138K mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | | | |
| AID1482920 | Antiviral activity against indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID1219722 | Drug metabolism in human liver microsomes assessed as GSH-conjugated dihydroxylated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID375206 | Ratio of EC50 for multidrug-resistant HIV1 isolate C to EC50 for wild type HIV1 isolate ERS104pre | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID369838 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID582279 | AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID557291 | Antiviral activity against HIV1 NL4-3 harboring L23I/K43I/M46I/I50L/G51A/A71V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 1 uM of atazanavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID519788 | Antiviral activity against HIV 2 subtype A clinical isolate expressing 10I-40D-43I-70K-82F-84V-85L-89V-90M-91T/L-98N/K protease gene sequence from HIV2 infected patient plasma and PBMC obtained at T1 during compound treatment measured after 13 months | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | | | |
| AID509270 | Inhibition of HIV1 protease assessed as substrate cleavage by cell free assay | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
| Antiviral efficacy of the novel compound BIT225 against HIV-1 release from human macrophages. |
| AID532476 | Antiviral activity against Human immunodeficiency virus 1 isolate 23 harboring Gag-capsid I138L, V215L, E319D, A340G, G357S and V362I mutant gene and protease L10V, V11L, V32I, L33F, E34Q, E35D, M36L, S37T, M46I, I47V, G48V, I54M, I62V, L63P, I64V, I72V, | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID321688 | Antiviral activity against HIV1 mutant strain 3 | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID618426 | Inhibition of HIV1 subtype C protease Q7K mutant expressed in Escherichia coli BL21 (DE3) pLysS using Lys-Ala-Arg-Val-Nle-p-nitro-Phe-Glu-Ala-Nle-NH2 as substrate by spectrophotometry | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Synthesis and structural studies of pentacycloundecane-based HIV-1 PR inhibitors: a hybrid 2D NMR and docking/QM/MM/MD approach. |
| AID1474089 | Drug concentration at steady state in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1219723 | Drug metabolism in human liver microsomes assessed as GSH-conjugated trihydroxylated/dehydrogenated lopinavir adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID374621 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/82A/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID557285 | Antiviral activity against HIV1 NL4-3 harboring L10I/G48V/I54V/L90M amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of saquinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID519539 | Antiviral activity against wild-type HIV1 RF infected in human MT4 cells assessed as reduction in viral cytopathogenicity treated 1 hr post infection measured 5 days post infection in absence of human serum by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1380928 | Resistance index, ratio of EC50 for antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells to EC50 for antiviral activity against wild type HIV1 NL4-3 infected | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID532656 | Antiviral activity against Human immunodeficiency virus 1 isolate 2 harboring Gag-capsid A146P, S173A, V215L, H219P, E230D, N252S, R264K, L268M and A340G mutant gene and protease L10I, I15V, K20R, M36I, S37N, M46I, L63P, T80A, V82A, N83H, I84V, I85T and L | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID248545 | Inhibitory concentration against wild type Human immuno deficiency virus (EP13) was determined in an MT-4 cell line | 2005 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15
| Novel P1 chain-extended HIV protease inhibitors possessing potent anti-HIV activity and remarkable inverse antiviral resistance profiles. |
| AID553578 | Antiviral activity against HIV1 JSL harboring L10I/L24I/L33F/E35D/M36I/N37S/M46L/I54V/R57K/I62V/L63P/A71V/G73S/82A in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID263208 | Antiviral activity against HIV1 EP13 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
| AID537772 | Antiviral activity against multidrug resistant Human immunodeficiency virus 1 MDRC4 | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID392513 | Antiviral activity against HIV1 | 2009 | Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
| Unified QSAR approach to antimicrobials. 4. Multi-target QSAR modeling and comparative multi-distance study of the giant components of antiviral drug-drug complex networks. |
| AID372187 | Resistance index, ratio of EC50 for HIV1 with protease 54V/82A mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID278955 | Antiviral activity against HIV1 A3 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID726414 | Antiviral activity against Human immunodeficiency virus 1 3B clinical isolate harboring L10I/K20R/M36I/G48V/ I62V/A71V/V82A/I93L protease mutant infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID557300 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/L33F/M46I/I47V/Q58E/V82I/I84V/I85V amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID564041 | Antiviral activity against HIV1 expressing protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells selected at 5 uM of atazanavir by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID541135 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTG48V, V82A and L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID106953 | Antiviral activity against HIV in presence of 50% human serum in MT-4 cell was determined | 2001 | Bioorganic & medicinal chemistry letters, Jun-04, Volume: 11, Issue:11
| Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir). |
| AID564060 | Antiviral activity against HIV1 expressing protease L10I/L24I/M46I/V82I/I84V mutant infected in human MT4 cells selected after 50 passages of GRL-216 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1409307 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID322106 | Antiviral activity against atazanavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID566852 | Antiviral activity against HIV-1 MDR/JSL infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID1717811 | Toxicity in human infected with SARS-CoV2 assessed as adverse events at at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID321684 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID278962 | Antiviral activity against HIV1 A10 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID446194 | Antiviral activity against multidrug-resistant HIV1 isolate B infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID415283 | Antiviral activity against HIV1 bearing protease gene with P25 mutation infected in human MT4 cells after 5 days by MTT assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| 2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
| AID1717742 | Antiviral actvity against SARS-CoV2 infected in human assessed as improvement rate of chest at 400 mg, po administered twice daily cotreated with 100 mg ritonavir and measured after 14 days by computed tomography | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID1717743 | Selectivity index, ratio of CC50 for human Huh-7 cells to EC50 for HCoV-229E harboring GFP infected in human Huh-7 cells | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID575061 | Antiviral activity against Human immunodeficiency virus 1 harboring M46I, M46L, I54V, and V82A mutations in viral protease assessed as fold change in drug susceptibility relative to wild type | 2010 | Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
| Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease. |
| AID572580 | AUC in HIV-1 infected patient at 400 mg, po bid coadministered with 100 mg, po bid of ritonavir and 300 mg, po qd of atazanavir | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
| Decrease of atazanavir and lopinavir plasma concentrations in a boosted double human immunodeficiency virus protease inhibitor salvage regimen. |
| AID328890 | Inhibition of farnesyl transferase | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID328885 | Toxicity in human HeLa cells transfected with GFP-prelamin A construct assessed as accumulation of uncleaved protein at 20 uM by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID557288 | Antiviral activity against HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of nelfinavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID541170 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155S mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID566846 | Antiviral activity against wild type HIV-1 ERS104 pre infected in human PHA-PBM cells assessed as inhibition of p24 Gag protein production | 2011 | Journal of medicinal chemistry, Jan-27, Volume: 54, Issue:2
| Design and synthesis of potent HIV-1 protease inhibitors incorporating hexahydrofuropyranol-derived high affinity P(2) ligands: structure-activity studies and biological evaluation. |
| AID705596 | Inhibition of CYP3A4-mediated testosterone 6 beta hydroxylation in human liver microsome by Dixon plot analysis | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
| AID374636 | Resistance index, ratio of EC50 for HIV1 with protease 48V/82A/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID374608 | Resistance index, ratio of EC50 for HIV1 with protease 33I/46I/84V/88D/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID375201 | Antiviral activity against multidrug-resistant HIV1 isolate MM infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID446199 | Antiviral activity against multidrug-resistant HIV1 isolate JSL infected in PHA-stimulated human PBMC assessed as inhibition of p24 gap protein production | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease inhibitors to combat drug resistance. |
| AID582281 | Clearance in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with ritonavir and NNRTI | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID321678 | Metabolic stability in rat liver microsomes assessed as compound remaining at 5 uM in presence of 2.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID279339 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with V62A and L99F mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID537765 | Inhibition of wild type HIV1 protease by FRET | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID564044 | Antiviral activity against multidrug-resistant HIV1 isolate C containing protease L10I, I15V, K20R, L24I, M36I, M46L, I54V, I62V, L63P, K70Q, V82A, and L89M mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1380924 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID582275 | Cmax in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID322123 | Antiviral activity against HIV1 92TH019 R5 subtype E in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID668812 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M1 expressing protease L10I, M46I, I64V, I84V, L90M, I93L mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID622578 | Antiviral activity against wild type HIV1 pNL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cell death after 5 days by MTT assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses. |
| AID1593667 | Prodrug conversion assessed as calf intestinal alkaline phosphatase-mediated compound dephosphorylation by measuring half life by UPLC-MS/MS analysis | 2019 | Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
| Design, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir. |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | | | |
| AID519540 | Antiviral activity against wild-type HIV1 pNL4-3 infected in human MT4 cells assessed as reduction in viral cytopathogenicity after 5 days post dose by MTT assay | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID257269 | Inhibitory activity against HIV1 protease at 0.5 uM | 2005 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 15, Issue:24
| Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains. |
| AID239809 | Equilibrium dissociation constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID1482916 | Ratio of IC50 for darunavir-resistant HIV1 derived from 20 passages harboring protease L10I/I15V/K20R/L24I/V32I/M36I/M46L/L63P/V82A/L89M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID369955 | Ratio of EC50 for HIV2 ROD with protease G17N mutation to EC50 for wild type HIV2 ROD | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID558376 | Drug level in HIV-infected pregnant woman cord blood plasma at 400 mg, po BID by HPLC/UV analysis | 2009 | Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
| Genital tract, cord blood, and amniotic fluid exposures of seven antiretroviral drugs during and after pregnancy in human immunodeficiency virus type 1-infected women. |
| AID343023 | Ratio of Ki for HIV1 recombinant protease M46I/A71V/V82T/I84V mutant to Ki for wild-type HIV1 BH10 protease | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID532468 | Antiviral activity against Human immunodeficiency virus 1 isolate 3 harboring Gag-capsid I138L, A146P, I147L, V159I, S176A, V215L, H219Q/H, T242N, G248A, T280V, A340G and G357S mutant gene and protease L10I, T31S/T, V32I, M36I/M, S37C, R41K, M46I, F53L, I | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID537770 | Antiviral activity against Human immunodeficiency virus 1 clade C isolated from HIV-AIDS patient | 2010 | Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
| Structure-based design, synthesis, and structure-activity relationship studies of HIV-1 protease inhibitors incorporating phenyloxazolidinones. |
| AID541174 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring E92V, G140S and V151A mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID525485 | Antigametocyte activity against drug-resistant Plasmodium falciparum Dd2 schizonts assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID519547 | Antiviral activity against HIV1 isolate 4 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease N37T, M46I, Q58E, I64V, T74K, V77I, V82F, L90M mutation derived from viral passages with Lopinavir assessed as redu | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID1380925 | Antiviral activity against ATV resistant HIV1 harboring protease L23I/E34Q/K43I/M46I/I50L/G51A/L63P/A71V/V82A/T91A mutant infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
| Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis. |
| AID374606 | Resistance index, ratio of EC50 for HIV1 with protease 46I/82T/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID322104 | Antiviral activity against idinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID532472 | Antiviral activity against Human immunodeficiency virus 1 isolate 33 harboring Gag-capsid I138L, V215L, V218P, H219Q, I223V, M228I, G248T, N252S, N253T, I256M, E312D and A326S mutant gene and protease T12S/T, I13V/I, I15V, L19I, S37T, L63V/A/P/L and I72V/ | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID557233 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum administered for 30 days in combination with 100 mg, po bid ritonavir measured 4 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID557281 | Ratio of EC50 for HIV1 B harboring L10I/I15V/E35D/N37E/K45R/I54V/L63P/A71V/V82T/L90M/I93L/C95F in protease encoding region to EC50 for HIV1 ERS104pre | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID278957 | Antiviral activity against HIV1 A5 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID369961 | Ratio of EC50 for HIV2 MS infected in human MT4 cells after 1 passage to EC50 for HIV2 MS infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID328879 | Toxicity in RCE1 deficient mouse fibroblast cells assessed as accumulation of prelamin A at 20 uM after 24 hrs by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID369945 | Ratio of EC50 for HIV2 CBL-23 infected in human PBMC to EC50 for HIV1 NL4-3 infected in human MT4 cells | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID417047 | Inhibition of esterase mediated-hydrolysis of tenofovir disoproxil fumarate in human intestinal sub cellular fraction S9 at 2 uM after 30 mins | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID274382 | Inhibition of HIV1 protease L10I/L63P/A71V/G73S/I84V/L90M mutant | 2006 | Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
| Discovery of HIV-1 protease inhibitors with picomolar affinities incorporating N-aryl-oxazolidinone-5-carboxamides as novel P2 ligands. |
| AID321683 | Metabolic stability in human liver microsomes assessed as compound remaining at 5 uM in presence of 0.5 uM ritonavir by RP-HPLC | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID541169 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring N155H mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID557296 | Ratio of EC50 for HIV1 NL4-3 harboring L10F/D30N/K45I/A71V/T74S amino acid substitution in protease encoding region to EC50 for HIV1 NL4-3 | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID374632 | Resistance index, ratio of EC50 for HIV1 with protease 46L/54V/73C/84V/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID278983 | Resistance to HIV1 with protease 46I/L, 54I and I84C mutation in HEK 293 cells relative to similar background | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID322113 | Antiviral activity against HIV1 MDR/TM X4 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID442714 | Fold resistance, ratio of EC50 for indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells to EC50 for HIV1 pNL4-3 infected in human MT4 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket. |
| AID1482924 | Ratio of IC50 for indinavir-resistant HIV1 NL4-3 harboring protease L10F/L24I/M46I/I54V/L63P/A71V/G73S/V82T mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID375203 | Antiviral activity against multidrug-resistant HIV1 isolate G infected in PHA-stimulated PBMC assessed as inhibition of p24 gap protein | 2009 | Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13
| Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies. |
| AID557222 | Drug level in HIV-infected Thai pregnant women serum at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured 12 hrs post last dose | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID698062 | Binding affinity to wild type HIV1 protease | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Rational approaches to improving selectivity in drug design. |
| AID322107 | Antiviral activity against lopinavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID374614 | Resistance index, ratio of EC50 for non-B type HIV1 with protease 46I/47V/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID532477 | Antiviral activity against Human immunodeficiency virus 1 isolate 24 harboring Gag-capsid I138L, V159I, V215L, I223A, T239S, N252S, T280V, R286K, S310T and V362I mutant gene and protease L10V, I13V, I15V, K20R, D30N, V32I, L33F, E35D, M36I, S37N, K43T, M4 | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID263207 | Antiviral activity against HIV1 HXB2 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
| AID1409311 | Antiviral activity against darunavir-resistant HIV1 at passage 21 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by automated chemiluminescent enzyme immunoassay | 2018 | Journal of medicinal chemistry, 11-08, Volume: 61, Issue:21
| Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies. |
| AID374594 | Selectivity index, ratio of CC50 for human MT4 cells to EC50 for HIV1 NL4-3 | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID557217 | Cmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID726419 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID242932 | Dissociation rate constant for the interaction between the compound and serum albumin | 2005 | Journal of medicinal chemistry, May-19, Volume: 48, Issue:10
| Early absorption and distribution analysis of antitumor and anti-AIDS drugs: lipid membrane and plasma protein interactions. |
| AID369948 | Antiviral activity against HIV2 MS infected in human PBMC cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID541129 | Selectivity ratio of EC50 for antiviral activity against NRTI-resistant HIV1 harboring RTK65R mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID541161 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring T66I mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID328895 | Effect on change in ZMPSTE24 protein level in mouse fibroblasts at 20 uM after 10 days by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID1219725 | Drug metabolism in human liver microsomes assessed as lopinavir semicarbazide adduct formation at 30 uM preincubated for 5 mins prior NADPH addition measured after 50 mins by UPLC-TOFMS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
| CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. |
| AID582274 | AUC in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID519644 | Antiviral activity against HIV1 isolate 6 infected in human MT4 cells obtained from protease inhibitor-resistant patient harboring protease L10I, L24I, M46I, I54V, K55R, Q58E, L63P, I64V, A71V, V82A, T91A mutation derived from viral passages with Lopinavi | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID278978 | Antiviral activity against HIV1 C11 isolate with protease I84C mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID1482911 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction in p24 Gag protein production after 7 days by chemiluminescent enzyme immunoassay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID246965 | Effective dose of compound required to inhibit replication of human immunodeficiency virus type 1 in MT-4 cells | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
| AID553570 | Cytotoxicity against human MT2 cells by MTT assay | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID541171 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M and E92V mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID321661 | Antiviral activity against HIV1 3B | 2008 | Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3
| Structure-activity relationships of novel HIV-1 protease inhibitors containing the 3-amino-2-chlorobenzoyl-allophenylnorstatine structure. |
| AID1307690 | Binding affinity to HIV1 protease | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| OpenGrowth: An Automated and Rational Algorithm for Finding New Protein Ligands. |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | | | |
| AID279337 | Antiviral activity against HIV2 isolate CBL20, CBL23, MVP15132 with 182L mutation in CBMCs | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. |
| AID322120 | Antiviral activity against HIV1 92UG037 subtype A R5 in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID322109 | Antiviral activity against HIV1 GRL98065p20 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID557289 | Antiviral activity against HIV1 NL4-3 harboring M46I/V82F/I84V amino acid substitution in protease encoding region infected in human MT4 cells assessed as inhibition of p24 Gag protein production selected at 5 uM of ritonavir by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID369949 | Antiviral activity against HIV1 NL4-3 infected in human MT4 cells assessed as inhibition of virus production after 5 days by Lenti-RT activity assay | 2007 | Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
| In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir. |
| AID263209 | Antiviral activity against HIV D545701 in MT4 cells | 2006 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 16, Issue:7
| Ultra-potent P1 modified arylsulfonamide HIV protease inhibitors: the discovery of GW0385. |
| AID564036 | Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID582277 | Plasma concentration in HIV-infected patient at 400 mg/m2, po administered every 12 hrs for 2 weeks co-administered with 120 mg/m2 of ritonavir measured 12 hrs after last dose | 2008 | Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
| Pharmacokinetics of high-dose lopinavir-ritonavir with and without saquinavir or nonnucleoside reverse transcriptase inhibitors in human immunodeficiency virus-infected pediatric and adolescent patients previously treated with protease inhibitors. |
| AID1482907 | Ratio of IC50 for saquinavir-resistant HIV1 NL4-3 harboring protease L10I/N37D/G48V/I54V/L63P/G73C/I84V/L90M mutant infected in human MT4 cells to IC50 for wild type HIV1 NL4.3 infected in human MT4 cells | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Design and Development of Highly Potent HIV-1 Protease Inhibitors with a Crown-Like Oxotricyclic Core as the P2-Ligand To Combat Multidrug-Resistant HIV Variants. |
| AID374617 | Resistance index, ratio of EC50 for HIV1 with protease 33F/54L/88S/90M mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID374637 | Resistance index, ratio of EC50 for HIV1 with protease 46L/48V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID246225 | Protease inhibitory activity against HIV-1 GSS004421 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID525486 | Antigametocyte activity against drug-resistant ring stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth at 20 uM after 1 to 8 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID726418 | Antiviral activity against wild type Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication in presence of 50% human plasma | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application. |
| AID372192 | Resistance index, ratio of EC50 for HIV1 with protease 46I/50V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID278954 | Antiviral activity against HIV1 A2 isolate with protease I84A mutation in HEK 293 cells relative to wild type | 2007 | Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
| Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication. |
| AID343021 | Inhibition of HIV1 recombinant protease L10F/L19I/K20R/L33F/E35D/M36I/R41K/F53L/I54V/L63P/H69K/A71V/T74P/I84V/L89M/L90M/I93L mutant expressed in Escherichia coli by spectrophotometric assay | 2008 | Journal of medicinal chemistry, Aug-14, Volume: 51, Issue:15
| Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance. |
| AID239819 | Association rate constant for human immunodeficiency virus type 1 protease | 2004 | Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
| Improved structure-activity relationship analysis of HIV-1 protease inhibitors using interaction kinetic data. |
| AID519543 | Antiviral activity against HIV1 P25 infected in human MT4 cells harboring protease L10F, G16E, V32I, M46I, I47A, H69Y, I84V, and T91S mutation derived from viral passages with Lopinavir assessed as reduction in viral cytopathogenicity treated 1 hr post in | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID416867 | Effect on tenofovir disoproxil fumarate metabolism in ritonavir booster drug treated HIV infected patient assessed as change in plasma AUC of tenofovir at 400 mg, po, BID co-administered with 300 mg once daily dose of tenofovir disoproxil fumarate | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID532456 | Antiviral activity against Human immunodeficiency virus 1 isolate 21 harboring Gag-capsid I138L, A146P, I147L/I, V159I/V, E211D, V215L, N252H/N, R286K/R and K331R/K mutant gene and protease E35D, M36I, S37N, I62V and L63C mutant gene infected in human MT- | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID532658 | Antiviral activity against Human immunodeficiency virus 1 isolate 29 harboring Gag-capsid I138M, A146P, R286K, T303V and A326S mutant gene and protease L10F, I13V, V32I, M36L, S37N, L38W, P39Q, M46I, I47V, I50V, I62V, L63P, A71I, I72V and V82A mutant gene | 2010 | Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
| Phenotypic susceptibility to bevirimat in isolates from HIV-1-infected patients without prior exposure to bevirimat. |
| AID541162 | Selectivity ratio of EC50 for antiviral activity against HIV1 harboring L74M mutation in catalytic core domain of integrase to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID564045 | Antiviral activity against multidrug-resistant HIV1 isolate G containing L10I, V11I, T12E, I15V, L19I,R41K, M46L, L63P, A71T, V82A, and L90M mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
| Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
| AID557219 | Tmax in HIV-infected Thai pregnant women at 400 mg, po bid initiated intrapartum in combination with 100 mg, po bid ritonavir measured within 72 hrs postpartum | 2009 | Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
| Early postpartum pharmacokinetics of lopinavir initiated intrapartum in Thai women. |
| AID588981 | Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B1 | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
| AID322108 | Antiviral activity against amprenavir-resistant HIV1 in MT4 cells assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID246195 | Protease inhibitory activity against HIV-1 r13363 mutant strain was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | | | |
| AID1474088 | AUC in human at 400 to 800 mg, po QD used as formulation with ritonavir measured after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID553575 | Antiviral activity against HIV1 MOKW infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID668813 | Selectivity index, ratio of EC50 for Human immunodeficiency virus 1 isolate M2 expressing protease L10I, I13V, M46I, I50V, L63P, L76V mutant to EC50 for Human immunodeficiency virus 1 3B expressing wild-type protease | 2011 | ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
| Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors. |
| AID553568 | Selectivity index, ratio of CC50 for human MT2 cells to EC50 for HIV1 LAI | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID541134 | Selectivity ratio of EC50 for antiviral activity against PI-resistant HIV1 harboring RTI84V, L90M mutant gene to EC50 for antiviral activity against wild-type HIV1 3B | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| Preclinical evaluation of GS-9160, a novel inhibitor of human immunodeficiency virus type 1 integrase. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | | | |
| AID564062 | Antiviral activity against HIV1 expressing protease L10F/M46L/I50V/A71Vmutant infected in human MT4 cells selected at 1 uM of GRL-286 by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID1350504 | Cytotoxicity against human MT4 cells after 5 days by MTT assay | 2018 | Journal of medicinal chemistry, 06-28, Volume: 61, Issue:12
| Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine. |
| AID525280 | Antimicrobial activity against chloroquine-sensitive Plasmodium falciparum D10 after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
| Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors. |
| AID1717744 | Cytotoxicity against human Huh-7 cells incubated for 1 hr by MTS assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
| Chinese Therapeutic Strategy for Fighting COVID-19 and Potential Small-Molecule Inhibitors against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). |
| AID374631 | Resistance index, ratio of EC50 for HIV1 with protease 46I/54V/82A/84V mutation to EC50 for wild type HIV1 NL4-3 in HEK293 cells after 48 hrs by replication-deffective luciferase reporter gene-based phenotypic assay | 2007 | Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
| In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
| AID246160 | Protease inhibitory activity against wild type HIV-1 IIIB was determined | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Design of HIV-1 protease inhibitors active on multidrug-resistant virus. |
| AID1422657 | Inhibition of ZMPSTE24 in human HPAF2 cells assessed as increase in intracellular accumulation of prenylated prelamin A at 10 uM after 24 hrs by Western blot analysis relative to control | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration. |
| AID547240 | Selectivity ratio of EC50 for HIV1 subtype CRF02_AG harboring protease M46, I47A, I84V mutant gene and polymorphism at I36 position to EC50 for wild type HIV1 subtype CRF02_AG | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID519578 | Antiviral activity against HIV1 clone3 infected in HEK293 cells harboring A-790742-selected protease L33F, K45I, V82L, and I84V mutation assessed as reduction in viral replication by luciferase reporter gene assay relative to wild type HIV1 pNL4-3 | 2008 | Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
| Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742. |
| AID546999 | Antiviral activity against HIV1 subtype C harboring protease L32I, M46I/M, L76V mutant gene and polymorphism at I36 position infected in human cord blood mononuclear cells assessed as inhibition of viral replication after 48 hrs by luciferase reporter gen | 2010 | Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
| HIV-1 protease codon 36 polymorphisms and differential development of resistance to nelfinavir, lopinavir, and atazanavir in different HIV-1 subtypes. |
| AID416857 | Decrease in P-glycoprotein-mediated tenofovir disoproxil fumarate efflux in MDCK2 expressing human MDR1 cells at 20 uM | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
| Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro. |
| AID557275 | Antiviral activity against HIV1 C harboring L10I/I15V/K20R/L24I/M36I/M46L/I54V/I62V/L63P/K70Q/V82A/L89M in protease encoding region infected in human PHA-PBC assessed as inhibition of p24 Gag protein production by ELISA | 2009 | Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
| GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro. |
| AID328876 | Toxicity in human AG08470 cells assessed as accumulation of prelamin A at 20 uM after 10 days by Western blot | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| HIV protease inhibitors block the zinc metalloproteinase ZMPSTE24 and lead to an accumulation of prelamin A in cells. |
| AID564047 | Antiviral activity against multidrug-resistant HIV1 isolate MM containing L10I, K43T, M46L, I54V, L63P, A71V, V82A, L90M, and Q92K mutant infected in human PHA-PBMC cells by MTT assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro. |
| AID322119 | Antiviral activity against HIV1 92UG029 X4 subtype A in phytohemagglutininin-activated PBMCs assessed as inhibition of p24 Gag protein expression by MTT assay | 2007 | Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
| A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508629 | Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1508628 | Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| AID1508627 | Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4
| A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2013 | Biochemical and biophysical research communications, Jul-26, Volume: 437, Issue:2
| Crystallographic study of multi-drug resistant HIV-1 protease lopinavir complex: mechanism of drug recognition and resistance. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1
| The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
| AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7
| Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
| AID1805801 | Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\ | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Perspectives on SARS-CoV-2 Main Protease Inhibitors. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2002 | Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8
| X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2002 | Bioorganic & medicinal chemistry, Aug, Volume: 10, Issue:8
| X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2007 | Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
| Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2007 | Journal of virology, May, Volume: 81, Issue:10
| Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2007 | Journal of virology, May, Volume: 81, Issue:10
| Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations. |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2008 | Protein science : a publication of the Protein Society, Sep, Volume: 17, Issue:9
| Enzymatic and structural analysis of the I47A mutation contributing to the reduced susceptibility to HIV protease inhibitor lopinavir. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |