Today kinase modulators remain a prominent area in drug discovery. As of 1 January 2024, the FDA approved 80 small-molecule therapeutic protein kinase inhibitors, and several hundred were reported to be in clinical trials [1]. Noteworthy, over the past decade the diversity of kinase inhibitor chemotypes significantly expanded [2].
To meet the growing demand for high-quality kinase modulators, Life Chemicals has developed its proprietary Kinase Screening Library (KSL) featuring over 3,200 drug-like screening compounds, designed and selected following industry-leading standards [3,4].
The compound selection can be customized based on your requirements, cherry picking is available.
Please, contact us at orders@lifechemicals.com for any additional information and price quotations.
Key Features of the Kinase Screening Library:
- Built using approximately 1,000 Markush structures and pharmacophore models of known kinase inhibitors sourced from the ChEMBL and PubChem databases.
- A 2D fingerprint similarity search applied to our proprietary HTS Compound Collection resulted in nearly 3,000 screening compounds selected to target key kinases involved in cancer and inflammation.
- Each compound entry includes information on its closest homolog and highest activity, derived from the ChEMBL and PubChem databases (examples provided in Fig. 1).
Kinase Modulators Included in the Library
The KSL is specifically designed to provide high-quality hits for drug discovery projects focused on kinases and other ATP-binding proteins, including:
- ATP-competitive inhibitors
- DGF-out and 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
- Inhibitors of protein kinases heavily pursued by industry: ACVRL, ABL, ADK, AKT, ALK, AMPK, Aurora, ATM, AXL, Bcr-ABL, βARK1, Braf, BMX, BRK, BTK, CAMK, CDK, CDC7, CqsS, cFMS, CHK, CK, CNKSR1, cKIT, cMET, CLK, CPK, DAPK, DNA-PK, DYRK, EEFK, EGFR, EPH, erbB, FAK, FLT3, Fyn, GRK, GSK, HK, HPK, HER, JAK, JNK, IGFR, IKK, ILK, IRE, IRAK, ITK, KDR, LCK, luxN, LIMK, LRRK, MAPK, MEK, MELK, MLCK, mTOR, p38α, PAK, PASK, PDPK, PDGF, PIK, PIM, PIP, PGK, PKA, PKC, PFK, PFMRK, PKM2, PLK, PknB, PRKACA, PRMT, RAF, RET, RIPK, ROCK, RTK, SH2, SAPK, SRC, S6K, SKSphK, SPHK, SYK, SGK, TAO, Tie2, TGFB, TK2, TRPM, Trk, TTSP, VEGFR, ZAP-70
Representative screening compounds from the Kinase Screening Library (KSL)
Reference:
- Roskoski R Jr. Properties of FDA-approved small molecule protein kinase inhibitors: A 2020 update. Pharmacol Res. 2020;152:104609.
- Bhullar KS, Lagarón NO, McGowan EM, et al. Kinase-targeted cancer therapies: progress, challenges and future directions. Mol Cancer. 2018;17(1):48.
- Gagic Z, Ruzic D, Djokovic N, Djikic T, Nikolic K. In silico Methods for Design of Kinase Inhibitors as Anticancer Drugs. Front Chem. 2020;7:873.
- Fabbro D, Cowan-Jacob SW, Moebitz H. Ten things you should know about protein kinases: IUPHAR Review 14. Br J Pharmacol. 2015;172(11):2675-2700.