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The Discovery of CCR5 Receptor Antagonists for the Treatment of HIV Infection: Hit‐to‐Lead Studies
Author(s) -
Armour Duncan,
de Groot Marcel J.,
Edwards Martin,
Perros Manos,
Price David A.,
Stammen Blanda L.,
Wood Anthony
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600031
Subject(s) - ccr5 receptor antagonist , drug discovery , human immunodeficiency virus (hiv) , pharmacology , high throughput screening , key (lock) , lead compound , receptor , computational biology , medicine , virology , chemistry , bioinformatics , biology , biochemistry , chemokine , chemokine receptor , in vitro , ecology
The discovery of UK‐374,503 started from a high‐throughput screening hit that was a potent Type II P450 2D6 inhibitor and which displayed no antiviral activity. The optimisation of affinity for the CCR5 receptor while reducing concerns about P450 inhibition and the subsequent introduction of antiviral effects were key milestones for the project.