U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Structurally Diverse
Created
by admin
on Sat Dec 16 11:43:54 UTC 2023
Edited
by admin
on Sat Dec 16 11:43:54 UTC 2023
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
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
HUMAN IMMUNODEFICIENCY VIRUS TYPE 1
Common Name English
HIV-1
Common Name English
Code System Code Type Description
FDA UNII
859A956UY8
Created by admin on Sat Dec 16 11:44:01 UTC 2023 , Edited by admin on Sat Dec 16 11:44:01 UTC 2023
PRIMARY
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infected with HIV-luc/VSV-G (1 ng p24Gag).
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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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DOES NOT ACTIVATE CCR5
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