Concepedia

Optimization of a series of potent, selective and orally bioavailable SYK inhibitors

Neil P. Grimster, Lakshmaiah Gingipalli, Bernard Barlaam, Qibin Su, Xiaolan Zheng, David Watson, Haixia Wang, Iain Simpson, Andy Pike, Amber Balazs,

Bioorganic & Medicinal Chemistry Letters · 2020 · 11 citations · 17 references

Concepts

PharmacyMedicinal ChemistryPharmacologyBioavailabilityDrug DiscoveryLead OptimizationEnzyme InhibitionLigand-based DesignPotency OptimizationSolubility OptimizationStereochemical OptimizationTyrosine Kinase InhibitorsKinase InhibitorsProtein Kinase InhibitorsSelective Tyrosine Kinase Inhibitors

References

17

A small molecule–kinase interaction map for clinical kinase inhibitors

Miles A. Fabian, William Biggs, Daniel K. Treiber et al. · Nature Biotechnology · 2005 · 1.9K citations · Full text

Pharmacy, Medicinal Chemistry, Molecular Biology +12

Fundamental Properties of the CH···O Interaction: Is It a True Hydrogen Bond?

Yanliang Gu, Tapas Kar, Steve Scheiner · Journal of the American Chemical Society · 1999 · 1K citations

Natural Sciences, Chemistry, Computational Chemistry +16

Oxadiazoles in Medicinal Chemistry

Jonas Boström, Anders Hogner, Antonio Llinàs et al. · Journal of Medicinal Chemistry · 2011 · 595 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +15

Oxadiazoles as Ester Bioisosteric Replacements in Compounds Related to Disoxaril. Antirhinovirus Activity

Guy D. Diana, Deborah L. Volkots, Theodore J. Nitz et al. · Journal of Medicinal Chemistry · 1994 · 182 citations

Pharmacy, Medicinal Chemistry, Pharmacology +16

Discovery of GS-9973, a Selective and Orally Efficacious Inhibitor of Spleen Tyrosine Kinase

Kevin Currie, Jeffrey E. Kropf, Tony Lee et al. · Journal of Medicinal Chemistry · 2014 · 171 citations · Full text

Medicine, Oncology, Pharmacology +13