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A lower X-gate in TASK channels traps inhibitors within the vestibule.

  • Read more about A lower X-gate in TASK channels traps inhibitors within the vestibule.

Rödström, K., Kiper, A. K., Zhang, W., Rinné, S., Pike, A., Goldstein, M., ... Carpenter, E. P. (2020). A lower X-gate in TASK channels traps inhibitors within the vestibule. Nature, 582(7812), 443–447.

Target 2035: probing the human proteome.

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Carter, A., Kraemer, O., Zwick, M., Mueller-Fahrnow, A., Arrowsmith, C., & Edwards, A. (2019). Target 2035: probing the human proteome. Drug Discovery Today, 24(11), 2111-2115.

The promise and peril of chemical probes.

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Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., … Zuercher, W. J. (2015). The promise and peril of chemical probes. Nature chemical biology, 11(8), 536–541.

Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.

  • Read more about Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design.

Rahm F, Viklund J, Trésaugues L, Ellermann M, Giese A, Ericsson U, ... Andersson M. (2018). Creation of a Novel Class of Potent and Selective MutT Homologue 1 (MTH1) Inhibitors Using Fragment-Based Screening and Structure-Based Drug Design. Journal of Medicinal Chemistry, 61(6), 2533-2551.

Donated Chemical Probes for Open Science

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Müller, S., Ackloo, S., Arrowsmith, C. H., Bauser, M., Baryza, J. L., Blagg, J., … Mueller-Fahrnow, A. (2018). Donated chemical probes for open science. eLife, 7, e34311.

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

  • Read more about Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

Fernández-Montalván, A., Berger, M., Kuropka, B., Koo, S., Badock, V., Weiske, J., ... Gorjánácz, M. (2017). Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. ACS Chemical Biology, 12(11), 2730-2736.

Progress towards a public chemogenomic set for protein kinases and a call for contributions

  • Read more about Progress towards a public chemogenomic set for protein kinases and a call for contributions

Drewry, D. H., Wells, C. I., Andrews, D. M., Angell, R., Al-Ali, H., Axtman, A. D., … Willson, T. M. (2017). Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS ONE, 12(8), e0181585.

Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains

  • Read more about Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains

Bouché, L., Christ, C. D., Siegel, S., Fernández-Montalván, A. E., Holton, S. J., Fedorov, O., … Haendler, B. (2017). Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains. Journal of Medicinal Chemistry, 60(9), 4002–4022.

Structural analysis of human KDM5B guides histone demethylase inhibitor development

  • Read more about Structural analysis of human KDM5B guides histone demethylase inhibitor development

Johansson, C., Velupillai, S., Tumber, A., Szykowska, A., Hookway, E. S., Nowak, R. P., … Oppermann, U. (2016). Structural analysis of human KDM5B guides histone demethylase inhibitor development. Nature Chemical Biology, 12(7), 539-545.

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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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