Approval Year
Substance Class |
Structurally Diverse
Created
by
admin
on
Edited
Sat Dec 16 11:43:54 GMT 2023
by
admin
on
Sat Dec 16 11:43:54 GMT 2023
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Source Materials Class | ORGANISM |
Source Materials Type | VIRUS |
Organism Family | Retroviridae |
Organism Genus | Lentivirus |
Organism Species | human immunodeficiency virus 1 |
Author | NONE |
Part | WHOLE |
Record UNII |
859A956UY8
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Record Status |
Validated (UNII)
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Record Version |
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-
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Name | Type | Language | ||
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Common Name | English | ||
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Common Name | English |
Code System | Code | Type | Description | ||
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859A956UY8
Created by
admin on Sat Dec 16 11:44:01 GMT 2023 , Edited by admin on Sat Dec 16 11:44:01 GMT 2023
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INHIBITOR->TARGET ORGANISM |
Other
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
HIV maturation inhibitor: Exhibited robust antiviral activity against a panel of HIV-1 clinical isolates, with a mean EC50 of 9 nM
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
The observation of gastrointestinal intolerability and the emergence of resistant virus led to the cessation of development activities in favor of compounds with improved antiviral profiles.
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
Upregulates innate immunity
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
IN-VITRO
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM | |||
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INHIBITOR->TARGET ORGANISM |
infected with HIV-luc/VSV-G (1 ng p24Gag).
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
IC50 values (50% inhibitory
concentration) ranged from 10-100 nM against laboratory and clinical isolates of HIV-1.
IC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
An Fc-aglycosylated, non–T-cell–depleting and CD4-specific humanized IgG1 derived from the parent murine B4, which binds to discontinuous, conformational epitopes on the HIV-receptor complex, including CD4 domain 1, and competitively blocks HIV entry
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
Tipranavir (TPV) is a non-peptidic HIV-1 protease inhibitor that inhibits the virus-specific processing of the viral Gag and Gag-Pol polyproteins in HIV-1 infected cells, thus preventing formation of mature virions.
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
Preclinical assessment of GW678248 indicates that this compound potently inhibits wild-type (WT) and mutant human immunodeficiency virus type 1 (HIV-1) reverse transcriptase in biochemical assays, with 50% inhibitory concentrations (IC50s) between 0.8 and 6.8 nM. In HeLa CD4 MAGI cell culture virus replication assays, GW678248 has an IC50 of 21 nM against HIV-1 isogenic strains with single or double mutations known to be associated with NNRTI resistance, including L100I, K101E, K103N, V106A/I/M, V108I, E138K, Y181C, Y188C, Y188L, G190A/E, P225H, and P236L and various combinations. An IC50 of 86 nM was obtained with a mutant virus having V106I, E138K, and P236L mutations that resulted from serial passage of WT virus in the presence of GW678248.
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM | |||
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
IC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
Upregulates innate immunity
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
DOES NOT ACTIVATE CCR5
IC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
INHIBITS BINDING
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
Inhibits cytopathic effect
EC50
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
The in vitro results showed that the EC50 of BILR 355 was 0.26 ng/ml (0.59 nM) against wild-type HIV-1 and ranged from 1.5 to 13 ng/ml (3.4 –29 nM) against clinically common single and double NNRTI mutations .
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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INHIBITOR->TARGET ORGANISM |
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