Kinase inhibitors represent a very hot topic in drug discovery: 48 protein kinase inhibitors are approved drugs, with several hundred undergoing clinical trials. Moreover, over the past 10 years the number of kinase inhibitor chemotypes has dramatically expanded.
To provide good quality hits for drug discovery projects Life Chemicals, a leading developer and supplier of novel screening compounds and targeted libraries, has released its proprietary Kinase Screening Library (KSL) built by the front-end industry standards.
KSL is a high quality library of protein kinase inhibitors, created as a part of the Focused Subset Screening initiative at Life Chemicals, following the “screen less, identify more good quality hits” paradigm. KSL was designed based on about 1,000 Markush structures of kinase inhibitors derived from literature and consists of 2,090 inhibitors and activator targeted key kinases in cancer and inflammation.
KSL is recommended for screening to identify good quality hits for drug discovery projects related to kinases and other ATP-binding proteins.
Coverage of Kinase & Inhibitor Types:
- Protein kinases heavily pursued by industry: ABL, AKT, ALK, AMPK, Aur, Bcr-ABL, Braf, BTK, CDK, cFMS, CHK, CK2, cKIT, cMET, EGFR, FLT3, Fyn, GSK3, HER, JAK, IGFR, IKK, ITK, KDR, LCK, LRRK, MEK, mTOR, p38α, PI3K, PIM, PKA, PKC, PKM2, ROCK, Src, Syk, Tie2, Trk, VEGFR
- ATP-competitive inhibitors
- DGF-out & αC-helix out non-ATP competitive inhibitors
- MEK non-ATP competitive inhibitors
- Covalent kinase inhibitors
- Allosteric kinase inhibitors
- Kinase activators: AMPK, ABL, DPK1, PKM2
- Generic hinge binders
Examples of structures from thr Kinase-Targeted Screening Library: