The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors

(2018) Agustin Casimiro-Garcia et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition

(2016) Jean-Baptiste Telliez et al.   ACS Chemical Biology

Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

(2015) Renato A. Bauer   DRUG DISCOVERY TODAY

Tricyclic Covalent Inhibitors Selectively Target Jak3 through an Active Site Thiol

(2015) Eric R. Goedken et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

ATP-Mediated Kinome Selectivity: The Missing Link in Understanding the Contribution of Individual JAK Kinase Isoforms to Cellular Signaling

(2014) Atli Thorarensen et al.   ACS Chemical Biology

Discovery and Development of Janus Kinase (JAK) Inhibitors for Inflammatory Diseases

(2014) James D. Clark et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drug discovery considerations in the development of covalent inhibitors

(2013) Robert Mah et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bruton’s Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies

(2012) Yan Lou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia

(2012) Amy B. Dounay et al.   ACS Medicinal Chemistry Letters

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain

(2011) Marvin J. Meyers et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Use of Structural Biology in Janus Kinase Targeted Drug Discovery

(2011) Nilda L. Alicea-Velazquez et al.   CURRENT DRUG TARGETS

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

Characterization of Irreversible Kinase Inhibitors by Directly Detecting Covalent Bond Formation: A Tool for Dissecting Kinase Drug Resistance

(2010) Sabine Klüter  et al.   CHEMBIOCHEM