Success examples
Development and Characterization of Selective FAK Inhibitors and PROTACs with In Vivo Activity

Koide E., Mohardt M. L., Doctor Z. M., Yang A., Hao M., Donovan K. A., Kuismi C. C., Nelson A. J., Abell K., Aguiar M., Che J., Stokes M. P., Zhang T., Aguirre A. J., Fischer E. S., Gray N. S., Jiang B., Nabet B.

Chembiochem. 2023, 24(19):e202300141.

PTK2 PROTAC PTK2 PROTAC
DOI
PubMed
Success examples
Hydroxyproline metabolism enhances IFN-γ-induced PD-L1 expression and inhibits autophagic flux

Spangenberg S. H., Palermo A., Gazaniga N. R., Martínez-Peña F., Guijas C., Chin E. N., Rinschen M. M., Sander P. N., Webb B., Pereira L. E., Jia Y., Meitz L., Siuzdak G., Lairson L. L.

Cell Chem Biol. 2023, 30(9):1115-1134.e10.

IKKβ inhibitor
DOI
PubMed
Success examples
Chamelogk: A Chromatographic Chameleonicity Quantifier to Design Orally Bioavailable Beyond-Rule-of-5 Drugs

Jimenez D. G., Vallaro M., Rossi Sebastiano M., Apprato G., D'Agostini G., Rossetti P., Ermondi G., Caron G.

J Med Chem. 2023, 66(15):10681-10693.

BET PROTAC
DOI
PubMed
Success examples
Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes

Hartung I. V., Rudolph J., Mader M. M., Mulder M. P. C., Workman P.

J Med Chem. 2023, 66(14):9297-9312.

SMARCA2 PROTAC
DOI
PubMed
Success examples
Development of BromoTag: A "Bump-and-Hole"-PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins

Bond A. G., Craigon C., Chan K., Testa A., Karapetsas A., Fasimoye R., Macartney T., Blow J. J., Alessi D. R., Ciulli A.

J Med Chem. 2021, 64(20):15477-15502.

BET PROTAC
DOI
PubMed
Success examples
Development of cellular metabolite-based MALDI mass spectrometry assays for drug discovery

Weight D.

heiDOK 2019.

FAS inhibitor
DOI