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Targeting the Water Network in Cyclin G-Associated Kinase (GAK) with 4-Anilino-quin(az)oline Inhibitors.

  • Read more about Targeting the Water Network in Cyclin G-Associated Kinase (GAK) with 4-Anilino-quin(az)oline Inhibitors.

Asquith, C., Tizzard, G. J., Bennett, J. M., Wells, C. I., Elkins, J. M., Willson, T. M., ... Laitinen, T. (2020). Targeting the Water Network in Cyclin G-Associated Kinase (GAK) with 4-Anilino-quin(az)oline Inhibitors. ChemMedChem, 15(13), 1200–1215.

Discovery of a First-in-class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.

  • Read more about Discovery of a First-in-class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.

Shen, Y., Li, F., Szewczyk, M. M., Halabelian, L., Park, K. S., Chau, I., Dong, A., ... Jin, J. (2020). Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. Journal of medicinal chemistry, 63(10), 5477–5487.

Quantifying CDK inhibitor selectivity in live cells.

  • Read more about Quantifying CDK inhibitor selectivity in live cells.

Wells, C. I., Vasta, J. D., Corona, C. R., Wilkinson, J., Zimprich, C. A., Ingold, M. R., ... Robers, M. B. (2020). Quantifying CDK inhibitor selectivity in live cells. Nature communications, 11(1), 2743.

Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12.

  • Read more about Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12.

Chen, Z., Wasney, G. A., Picaud, S., Filippakopoulos, P., Vedadi, M., D'Angiolella, V., & Bullock, A. N. (2020). Identification of a PGXPP degron motif in dishevelled and structural basis for its binding to the E3 ligase KLHL12. Open biology, 10(6), 200041.

Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.

  • Read more about Mining Public Domain Data to Develop Selective DYRK1A Inhibitors.

Henderson, S. H., Sorrell, F., Bennett, J., Hanley, M. T., Robinson, S., Hopkins Navratilova, I., ... Ward, S. E. (2020). Mining Public Domain Data to Develop Selective DYRK1A Inhibitors. ACS medicinal chemistry letters, 11(8), 1620–1626.

Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.

  • Read more about Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma.

Smil, D., Wong, J. F., Williams, E. P., Adamson, R. J., Howarth, A., McLeod, D. A., ... Isaac, M. B. (2020). Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma. Journal of medicinal chemistry, 63(17), 10061–10085.

Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.

  • Read more about Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family.

Quevedo, C. E., Bataille, C., Byrne, S., Durbin, M., Elkins, J., Guillermo, A., ... Russell, A. J. (2020). Aminothiazolones as potent, selective and cell active inhibitors of the PIM kinase family. Bioorganic & medicinal chemistry, 28(22), 115724.

Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death.

  • Read more about Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death.

Cottone, L., Cribbs, A., Khandelwal, G., Wells, G., Ligammari, L., Philpott, M., ... Flanagan, A. (2020). Inhibition of Histone H3K27 Demethylases Inactivates Brachyury (TBXT) and Promotes Chordoma Cell Death. Cancer Research, 80(20), 4540-4551.

Discovery of allosteric binding sites by crystallographic fragment screening.

  • Read more about Discovery of allosteric binding sites by crystallographic fragment screening.

Krojer, T., Fraser, J. S., & von Delft, F. (2020). Discovery of allosteric binding sites by crystallographic fragment screening. Current opinion in structural biology, 65, 209–216.

Identifying novel B-cell targets for chronic inflammatory autoimmune disease by screening of chemical probes in a patient-derived cell assay

  • Read more about Identifying novel B-cell targets for chronic inflammatory autoimmune disease by screening of chemical probes in a patient-derived cell assay

Sundström, Y., Shang, M. M., Panda, S. K., Grönwall, C., Wermeling, F., Gunnarsson, I., ... Berg, L. (2020). Identifying novel B-cell targets for chronic inflammatory autoimmune disease by screening of chemical probes in a patient-derived cell assay. Transl Res. S1931-5244(20)30225-5.

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The ULTRA-DD project is supported by the Innovative Medicines Initiative Joint Undertaking (IMI JU) under grant agreement n° [115766], resources of which are composed of financial contribution from the European Union's Seventh Framework Programme (FP7/2007-2013) and EFPIA companies’ in kind contribution. This website reflects only the author’s views and neither IMI nor the European Commission is liable for any use that may be made of the information contained therein.
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