Compounds > l 682679
Page last updated: 2024-12-11

l 682679

Description

L 682679: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5464378
CHEMBL ID289195
MeSH IDM0192949

Synonyms (16)

Synonym
chembl289195 ,
tert-butyl n-[(2s,3s,5r)-5-benzyl-5-{[(1s)-1-{[(1s)-1-carbamoyl-2-phenylethyl]carbamoyl}-3-methylbutyl]carbamoyl}-3-hydroxy-1-phenylpentan-2-yl]carbamate
bdbm751
126409-24-3
l-682,679
tert-butyl n-[(1s,2s,4r)-5-[[(1s)-1-[[(1s)-2-amino-1-benzyl-2-oxo-ethyl]carbamoyl]-3-methyl-butyl]amino]-1,4-dibenzyl-2-hydroxy-5-oxo-pentyl]carbamate
l-phenylalaninamide, n-(5-(((1,1-dimethylethoxy)carbonyl)amino)-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl)-l-leucyl-, (2r-(2r*,4s*,5s*))-
boc-ch2ph-leu-phe-nh2
l 682679
l-682679
tert-butyl n-[(2s,3s,5r)-6-[[(2s)-1-[[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl]carbamate
4B5 ,
n-{(2r,4s,5s)-2-benzyl-5-[(tert-butoxycarbonyl)amino]-4-hydroxy-6-phenylhexanoyl}-l-leucyl-l-phenylalaninamide
DTXSID70155177
Q27454565
AKOS040746008

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The most potent inhibitor (-)-7 displayed 13% oral bioavailability in dogs."( Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.
Barbosa, J; Cantin, LD; Charnley, AK; Guise-Zawacki, L; Hirschmann, R; Kuo, LC; Munshi, S; Olsen, DB; Pasternak, A; Schleif, WA; Smith, AB; Sprengeler, PA; Yao, W, 2003)		0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (BRU ISOLATE)IC50 (µMol)0.00060.00040.01100.0270AID1795266
Gag-Pol polyproteinHIV-1 M:B_HXB2RIC50 (µMol)0.00060.00060.91418.3200AID1795305
Gag-Pol polyproteinHuman immunodeficiency virus type 1 (NEW YORK-5 ISOLATE)IC50 (µMol)0.00050.00020.10421.7000AID1795268; AID1795289
Protease Human immunodeficiency virus 1IC50 (µMol)0.00060.00010.22487.3200AID161380; AID161728; AID162026; AID162185
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Protease Human immunodeficiency virus 1IC95 (µMol)6.00000.00601.08686.0000AID161883; AID161886
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (2)

Processvia Protein(s)Taxonomy
viral life cycleGag-Pol polyproteinHIV-1 M:B_HXB2R
establishment of integrated proviral latencyGag-Pol polyproteinHIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
peptidase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
integrase activityGag-Pol polyproteinHIV-1 M:B_HXB2R
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1795289Protease Inhibition Assay from Article 10.1021/jm00088a004: \\HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.\\1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
AID1795268Protease Inhibition Assay from Article 10.1021/jm00107a050: \\L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.\\1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
AID1795305Protease Inhibition Assay from Article 10.1021/jm00113a025: \\Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.\\1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
AID1795266Protease Inhibition Assay from Article 10.1021/jm0204587: \\Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.\\2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Design, synthesis, and biological evaluation of monopyrrolinone-based HIV-1 protease inhibitors.
AID199162Concentration required to inhibit 50% activity of plasma renin was determined at pH 7.4; Inactive1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
AID162185In vitro inhibitory concentration against HIV-1 protease1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
AID161380Inhibition of HIV-1 protease1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
AID232360Ratio of CIC95 to IC50 values1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
AID162026Inhibition of HIV-1 protease1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
AID161886Tested for the relative potency against HIV-1 protease in the cellular antiviral assay1994Journal of medicinal chemistry, Jan-21, Volume: 37, Issue:2
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
AID161728Inhibition of HIV-1 protease1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
AID161883Cellular antiviral activity against HIV-1 Protease1997Journal of medicinal chemistry, Aug-01, Volume: 40, Issue:16
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.
AID221809Ex vivo antiviral activity in H9 T-lymphoid cells infected with HIV-1(IIIB).1992Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
AID79273Minimum inhibitory concentration required to prevent HIV infection was determined in H9 human T-lymphoid cell culture1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's5 (83.33)18.2507
2000's1 (16.67)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.24

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

MetricThis Compound (vs All)
Research Demand Index12.24 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
indinavir sulfate
Indinavir: A potent and specific HIV protease inhibitor that appears to have good oral bioavailability.		2.4120dicarboxylic acid diamide;
N-(2-hydroxyethyl)piperazine;
piperazinecarboxamide		HIV protease inhibitor
l 685434
L 685434: structure given in first source; a pseudopeptide with activity against HIV protease		2.6830
ConditionIndicatedRelationship StrengthStudiesTrials
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