The Identification of Potent, Selective, and Brain Penetrant PI5P4Kγ Inhibitors as In Vivo-Ready Tool Molecules
Rooney, Timothy P. C., Aldred, Gregory G., Boffey, Helen K., Willems, Henriëtte M. G., Edwards, Simon, Chawner, Stephen J., Scott, Duncan E., Green, Christopher, Winpenny, David, Skidmore, John, Clarke, Jonathan H., Andrews, Stephen P.
Published in Journal of medicinal chemistry (12.01.2023)
Published in Journal of medicinal chemistry (12.01.2023)
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Journal Article
Systematic Investigation of the Permeability of Androgen Receptor PROTACs
Scott, Duncan E, Rooney, Timothy P. C, Bayle, Elliott D, Mirza, Tashfina, Willems, Henriette M. G, Clarke, Jonathan H, Andrews, Stephen P, Skidmore, John
Published in ACS medicinal chemistry letters (13.08.2020)
Published in ACS medicinal chemistry letters (13.08.2020)
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Journal Article
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1:NRF2) Protein–Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery
Davies, Thomas G, Wixted, William E, Coyle, Joseph E, Griffiths-Jones, Charlotte, Hearn, Keisha, McMenamin, Rachel, Norton, David, Rich, Sharna J, Richardson, Caroline, Saxty, Gordon, Willems, Henriëtte M. G, Woolford, Alison J.-A, Cottom, Joshua E, Kou, Jen-Pyng, Yonchuk, John G, Feldser, Heidi G, Sanchez, Yolanda, Foley, Joseph P, Bolognese, Brian J, Logan, Gregory, Podolin, Patricia L, Yan, Hongxing, Callahan, James F, Heightman, Tom D, Kerns, Jeffrey K
Published in Journal of medicinal chemistry (28.04.2016)
Published in Journal of medicinal chemistry (28.04.2016)
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Journal Article
The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)
Aldred, Gregory G, Rooney, Timothy P. C, Willems, Henriette M. G, Boffey, Helen K, Green, Christopher, Winpenny, David, Skidmore, John, Clarke, Jonathan H, Andrews, Stephen P
Published in MedChemComm (18.10.2023)
Published in MedChemComm (18.10.2023)
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Journal Article
Structure–Activity and Structure–Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2‑Related Factor 2 (KEAP1/NRF2) Protein–Protein Interaction
Heightman, Tom D, Callahan, James F, Chiarparin, Elisabetta, Coyle, Joseph E, Griffiths-Jones, Charlotte, Lakdawala, Ami S, McMenamin, Rachel, Mortenson, Paul N, Norton, David, Peakman, Torren M, Rich, Sharna J, Richardson, Caroline, Rumsey, William L, Sanchez, Yolanda, Saxty, Gordon, Willems, Henriëtte M. G, Wolfe, Lawrence, Woolford, Alison J.-A, Wu, Zining, Yan, Hongxing, Kerns, Jeffrey K, Davies, Thomas G
Published in Journal of medicinal chemistry (09.05.2019)
Published in Journal of medicinal chemistry (09.05.2019)
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Journal Article
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein−Protein Interaction
Norton, David, Bonnette, William G, Callahan, James F, Carr, Maria G, Griffiths-Jones, Charlotte M, Heightman, Tom D, Kerns, Jeffrey K, Nie, Hong, Rich, Sharna J, Richardson, Caroline, Rumsey, William, Sanchez, Yolanda, Verdonk, Marcel L, Willems, Henriëtte M. G, Wixted, William E, Woolford, Alison J.-A, Wu, Zining, Davies, Thomas G
Published in Journal of medicinal chemistry (11.11.2021)
Published in Journal of medicinal chemistry (11.11.2021)
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Journal Article
Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor
Willems, Henriëtte M. G, Edwards, Simon, Boffey, Helen K, Chawner, Stephen J, Green, Christopher, Romero, Tamara, Winpenny, David, Skidmore, John, Clarke, Jonathan H, Andrews, Stephen P
Published in MedChemComm (25.05.2023)
Published in MedChemComm (25.05.2023)
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Journal Article
Small-Molecule Inhibitors of the MDM2-p53 Protein−Protein Interaction Based on an Isoindolinone Scaffold
Hardcastle, Ian R, Ahmed, Shafiq U, Atkins, Helen, Farnie, Gillian, Golding, Bernard T, Griffin, Roger J, Guyenne, Sabrina, Hutton, Claire, Källblad, Per, Kemp, Stuart J, Kitching, Martin S, Newell, David R, Norbedo, Stefano, Northen, Julian S, Reid, Rebecca J, Saravanan, K, Willems, Henriëtte M. G, Lunec, John
Published in Journal of medicinal chemistry (19.10.2006)
Published in Journal of medicinal chemistry (19.10.2006)
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Journal Article
Development of Selective Phosphatidylinositol 5‑Phosphate 4‑Kinase γ Inhibitors with a Non-ATP-competitive, Allosteric Binding Mode
Boffey, Helen K., Rooney, Timothy P. C., Willems, Henriette M. G., Edwards, Simon, Green, Christopher, Howard, Tina, Ogg, Derek, Romero, Tamara, Scott, Duncan E., Winpenny, David, Duce, James, Skidmore, John, Clarke, Jonathan H., Andrews, Stephen P.
Published in Journal of medicinal chemistry (24.02.2022)
Published in Journal of medicinal chemistry (24.02.2022)
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Journal Article
Disease phenotypic screening in neuron-glia cocultures identifies blockers of inflammatory neurodegeneration
Birkle, Timothy J.Y., Willems, Henriette M.G., Skidmore, John, Brown, Guy C.
Published in iScience (19.04.2024)
Published in iScience (19.04.2024)
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Journal Article
De Novo Ligand Design to Partially Flexible Active Sites: Application of the ReFlex Algorithm to Carboxypeptidase A, Acetylcholinesterase, and the Estrogen Receptor
Firth-Clark, Stuart, Kirton, Stewart B, Willems, Henriëtte M. G, Williams, Anthony
Published in Journal of chemical information and modeling (01.02.2008)
Published in Journal of chemical information and modeling (01.02.2008)
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Journal Article
Isoindolinone-based inhibitors of the MDM2–p53 protein–protein interaction
Hardcastle, Ian R., Ahmed, Shafiq U., Atkins, Helen, Calvert, A. Hilary, Curtin, Nicola J., Farnie, Gillian, Golding, Bernard T., Griffin, Roger J., Guyenne, Sabrina, Hutton, Claire, Källblad, Per, Kemp, Stuart J., Kitching, Martin S., Newell, David R., Norbedo, Stefano, Northen, Julian S., Reid, Rebecca J., Saravanan, K., Willems, Henriëtte M.G., Lunec, John
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
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Journal Article
ChemInform Abstract: De Novo Ligand Design to Partially Flexible Active Sites: Application of the ReFlex Algorithm to Carboxypeptidase A, Acetylcholinesterase, and the Estrogen Receptor
Firth-Clark, Stuart, Kirton, Stewart B., Willems, Henriette M. G., Williams, Anthony
Published in ChemInform (20.05.2008)
Published in ChemInform (20.05.2008)
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Journal Article