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Gag-Pol polyprotein
A lentivirus-type gag-pol polyprotein that is encoded in the genome of Human immunodeficiency virus type 1 group M subtype B (isolate NY5). [PRO:DAN, UniProtKB:P12497]
Synonyms
Pr160Gag-Pol
Research
Bioassay Publications (34)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 22 (64.71) | 18.2507 |
| 2000's | 9 (26.47) | 29.6817 |
| 2010's | 3 (8.82) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (30)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nevirapine | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.6900 | 1 | 1 |
| flavaspidic acid | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 26.0000 | 1 | 1 |
| kynostatin 272 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0004 | 2 | 2 |
| efavirenz | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0200 | 1 | 1 |
| kni 102 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0575 | 1 | 1 |
| kynostatin 227 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0000 | 2 | 2 |
| amprenavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0558 | 2 | 2 |
| amprenavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0163 | 1 | 4 |
| bms 186318 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.1000 | 1 | 1 |
| a 74704 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0045 | 1 | 1 |
| dmp 323 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0010 | 1 | 1 |
| palinavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0001 | 1 | 2 |
| lopinavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0350 | 1 | 1 |
| etravirine | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.3700 | 1 | 1 |
| sc 52151 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0060 | 1 | 1 |
| ritonavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0670 | 1 | 1 |
| saquinavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0066 | 3 | 3 |
| saquinavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0009 | 2 | 2 |
| skf 107457 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0180 | 1 | 1 |
| je 2147 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0003 | 1 | 1 |
| kni-727 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0014 | 1 | 1 |
| l 739594 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0018 | 1 | 1 |
| indinavir sulfate | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0261 | 6 | 12 |
| indinavir sulfate | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0020 | 1 | 10 |
| l 685434 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0003 | 4 | 4 |
| l 689502 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0004 | 1 | 1 |
| l 682679 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 0.0005 | 2 | 2 |
| pepstatin | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 3.1000 | 1 | 1 |
| brecanavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0000 | 1 | 4 |
| phenprocoumon | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 1.0000 | 1 | 1 |
| tipranavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | Ki | 0.0000 | 1 | 1 |
| nsc 158393 | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | IC50 | 1.7000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| amprenavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | EC50 | 0.0074 | 1 | 6 |
| darunavir | Human immunodeficiency virus type 1 (NEW YORK-5 ISOLATE) | EC50 | 0.0003 | 1 | 6 |
Testing the substrate-envelope hypothesis with designed pairs of compounds.ACS chemical biology, , Nov-15, Volume: 8, Issue:11, 2013
Oximinoarylsulfonamides as potent HIV protease inhibitors.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Inhibition of wild-type and mutant human immunodeficiency virus type 1 proteases by GW0385 and other arylsulfonamides.Biochemistry, , Nov-16, Volume: 43, Issue:45, 2004
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
2',6'-Dimethylphenoxyacetyl: a new achiral high affinity P(3)-P(2) ligand for peptidomimetic-based HIV protease inhibitors.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Bis tertiary amide inhibitors of the HIV-1 protease generated via protein structure-based iterative design.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Protein structure-based design of potent orally bioavailable, nonpeptide inhibitors of human immunodeficiency virus protease.Proceedings of the National Academy of Sciences of the United States of America, , Apr-11, Volume: 92, Issue:8, 1995
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.Journal of medicinal chemistry, , Oct-15, Volume: 36, Issue:21, 1993
Potent HIV protease inhibitors: the development of tetrahydrofuranylglycines as novel P2-ligands and pyrazine amides as P3-ligands.Journal of medicinal chemistry, , Aug-06, Volume: 36, Issue:16, 1993
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors possessing augmented P2' side chains.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.Bioorganic & medicinal chemistry letters, , Sep-20, Volume: 14, Issue:18, 2004
Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 13, Issue:22, 2003
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.Proceedings of the National Academy of Sciences of the United States of America, , Apr-26, Volume: 91, Issue:9, 1994
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 36, Issue:2, 1993
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
Benzocycloalkyl amines as novel C-termini for HIV protease inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991