Related Experiment Video
Updated: Aug 16, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
Recent developments in the discovery of protein kinase inhibitors from the urea class
Jacques Dumas1, Roger A Smith, Timothy B Lowinger
1Bayer Research Center, Bayer Pharmaceutical Corporation, West Haven, CT 06516, USA. jacques.dumas.b@bayer.com
Abstract:
With two compounds on the market (Gleevec and Iressa), and a number of drug candidates in late-stage clinical trials, small-molecule kinase inhibitors hold great potential as novel therapies for cancer and inflammatory disorders. Inhibitors from the urea class were first reported in 1996 and have emerged as an important compound class for medicinal chemists due to their unique binding mode and kinase inhibition profile. Currently, five members of this class are undergoing clinical trials, BIRB-796 (Boehringer Ingelheim Pharmaceuticals Inc), BAY-43-9006 (Bayer AG/Onyx Pharmaceuticals Inc), CP-547632 (Pfizer Inc), MLN-518 (Millennium Pharmaceuticals Inc) and KRN-951 (Kirin Brewery Co Ltd). This review focuses on the most recent developments in the discovery of urea-based protein kinase inhibitors.
Related Concept Videos
Protein-protein Interfaces
Protein Kinases and Phosphatases
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Inhibition of Cdk Activity
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions
Inhibitors of Viral Protein Synthesis

