Ho Yin Lo
Affiliation: Boehringer Ingelheim
- 2-Aminobenzimidazoles as potent ITK antagonists: trans-stilbene-like moieties targeting the kinase specificity pocketHo Yin Lo
Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals Inc, 900 Ridgebury Road, P O Box 368, Ridgefield, CT 06877, USA
Bioorg Med Chem Lett 18:6218-21. 2008..Significant improvement on binding affinity and cellular activity were obtained through the trans-stilbene-like antagonists. Several compounds showed inhibitory activity in an IL-2 functional assay...
- Itk inhibitors: a patent reviewHo Yin Lo
Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, CT 06877, USA
Expert Opin Ther Pat 20:459-69. 2010..Rich resources on the structural information for Itk made discovery of novel selective Itk inhibitors blossom in the past decade...
- Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domainHo Yin Lo
Boehringer Ingelheim Pharmaceuticals Inc, Biomolecular Screening, 900 Ridgebury Rd, PO Box 368, Ridgefield, CT 06877, USA
Bioorg Med Chem Lett 20:6379-83. 2010..Lead optimization efforts to replace the aniline core are also described. In particular, 2-pyridine, 3-pyridine and pyridazine analogs are potent sEH inhibitors with favorable CYP3A4 inhibitory and microsomal stability profiles...
- Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) regionHo Yin Lo
Boehringer Ingelheim Pharmaceuticals Inc, Medicinal Chemistry, Ridgefield, CT 06877, USA
Bioorg Med Chem Lett 21:4533-9. 2011..Among the P(1) replacements, benzoisothiazole prevents the formation of GSH conjugate and an in silico analysis of oxidative potentials agreed with the experimental outcome...