Identification of novel azaindazole CCR1 antagonist clinical candidates
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
•Scaffold hopping approach led to identification of novel indazole CCR1 antagonists.•Multi parameter optimization led to three clinical candidate compounds.•Sub-micromolar CCR1 antagonists with attractive drug-like properties.•Candidates show >1000-fold improved CCR1 potency compared to initial hit.
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关键词
Chemokine receptors,CCR1,Indazole,Scaffold hopping,Clinical compound
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