Assay ID | Title | Year | Journal | Article |
AID311575 | Antiviral activity against HIV1 in CEM cells | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV. |
AID236641 | Maximum plasma concentration in dog after 80 mg/kg oral administration | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID415238 | Antiviral activity against protease inhibitor resistant HIV1 isolates | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease. |
AID415236 | Inhibition of HIV1 protease | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease. |
AID446190 | Inhibition of HIV1 protease | 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. |
AID311574 | Inhibition of HIV1 protease | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
| Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV. |
AID160442 | Inhibitory activity against HIV-1 protease | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
| Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere. |
AID237955 | Percentage of remaining compound after 30 min incubation in rat liver microsomes was determined as metabolic stability | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID236937 | Half-life in dog after 80 mg/kg oral administration | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID236972 | Time to reach maximum concentration in dog after 80 mg/kg oral administration | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID237954 | Percentage of remaining compound after 30 min incubation in dog liver microsomes was determined as metabolic stability | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID1465009 | Antiviral activity against HIV-1 harboring protease I50V mutant | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands. |
AID391264 | Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of virus-induced cytopathic effect | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID391263 | Inhibition of HIV1 protease | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
| Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies. |
AID237560 | Area under concentration time curve value in dog after 80 mg/kg oral administration | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID1465008 | Inhibition of wild-type HIV-1 protease | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands. |
AID249504 | Effective concentration against PI-Resistant HIV strain (M2) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID328063 | Antiviral activity against HIV1 LAI in MT2 cells | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. |
AID1482910 | Antiviral activity against HIV1 Lai infected in human MT2 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. |
AID249505 | Effective concentration against PI-Resistant HIV strain (M3) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID249503 | Effective concentration against PI-Resistant HIV strain (M1) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID328062 | Inhibition of HIV1 protease dimerization in MT2 cells | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. |
AID446191 | Antiviral activity against HIV1 LAI infected in human MT2 cells by MTT assay | 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. |
AID249507 | Effective concentration against PI-Resistant HIV strain (M5) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID328067 | Inhibition of HIV1 protease dimerization in MT2 cells at 1 uM | 2007 | The Journal of biological chemistry, Sep-28, Volume: 282, Issue:39
| Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization. |
AID105016 | Compound was tested for the inhibition of HIV-1 in MT-4 human T-lymphoid cells infected with IIIB isolate | 1998 | Bioorganic & medicinal chemistry letters, Mar-17, Volume: 8, Issue:6
| Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere. |
AID246282 | Effective concentration against human immunodeficiency virus type 1 strains; (0.3-0.5 nM) | 2005 | Journal of medicinal chemistry, Mar-10, Volume: 48, Issue:5
| New approaches toward anti-HIV chemotherapy. |
AID237956 | Percentage of remaining compound after 30 min incubation in human liver microsomes was determined as metabolic stability | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID1482908 | Inhibition of HIV1 protease expressed in Escherichia coli using 2-aminobenzoyl-Thr-Ile-Nle-Phe(p-N02)-Gln-Arg-NH as substrate preincubated for 5 to 10 mins followed by substrate addition measured after 1 hr by fluorescence assay | 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. |
AID249509 | Effective concentration as average activity on mutant HIV panel (AVMUT) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID249506 | Effective concentration against PI-Resistant HIV strain (M4) | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID249508 | Effective concentration of against HIV Wild Type (IIIB) strain | 2005 | Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
| Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. |
AID1796306 | Protease Inhibition Assay from Article 10.1016/s0960-894x(02)00300-1: \\Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy.\\ | 2002 | Bioorganic & medicinal chemistry letters, Aug-05, Volume: 12, Issue:15
| Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy. |
AID1799362 | Enzyme Inhibition Assay (Ki) and Antiviral Activity Assay (EC50/IC50) from Article 10.1021/jm900695w: \\Design, synthesis, protein-ligand X-ray structure, and biological evaluation of a series of novel macrocyclic human immunodeficiency virus-1 protease in | 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2006 | Journal of molecular biology, Oct-27, Volume: 363, Issue:3
| Suppression of HIV-1 protease inhibitor resistance by phosphonate-mediated solvent anchoring. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2006 | Journal of molecular biology, Oct-27, Volume: 363, Issue:3
| Suppression of HIV-1 protease inhibitor resistance by phosphonate-mediated solvent anchoring. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 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. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |