Organic synthesis provides opportunities to transform drug discovery DC Blakemore, L Castro, I Churcher, DC Rees, AW Thomas, DM Wilson, ... Nature chemistry 10 (4), 383-394, 2018 | 1105 | 2018 |
Catalytic in vivo protein knockdown by small-molecule PROTACs DP Bondeson, A Mares, IED Smith, E Ko, S Campos, AH Miah, ... Nature chemical biology 11 (8), 611-617, 2015 | 1070 | 2015 |
Lead‐oriented synthesis: a new opportunity for synthetic chemistry A Nadin, C Hattotuwagama, I Churcher Angewandte Chemie International Edition 51 (5), 1114-1122, 2012 | 432 | 2012 |
Protac-induced protein degradation in drug discovery: breaking the rules or just making new ones? I Churcher Journal of medicinal chemistry 61 (2), 444-452, 2018 | 404 | 2018 |
Selected non-steroidal anti-inflammatory drugs and their derivatives target γ-secretase at a novel site: evidence for an allosteric mechanism D Beher, EE Clarke, JDJ Wrigley, ACL Martin, A Nadin, I Churcher, ... Journal of Biological Chemistry 279 (42), 43419-43426, 2004 | 256 | 2004 |
Tau therapeutic strategies for the treatment of Alzheimer's disease I Churcher Current topics in medicinal chemistry 6 (6), 579-595, 2006 | 199 | 2006 |
Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2 A Mares, AH Miah, IED Smith, M Rackham, AR Thawani, J Cryan, ... Communications biology 3 (1), 140, 2020 | 145 | 2020 |
Modulating PCAF/GCN5 immune cell function through a PROTAC approach ZI Bassi, MC Fillmore, AH Miah, TD Chapman, C Maller, EJ Roberts, ... ACS Chemical Biology 13 (10), 2862-2867, 2018 | 138 | 2018 |
A divergent synthetic approach to diverse molecular scaffolds: assessment of lead-likeness using LLAMA, an open-access computational tool I Colomer, CJ Empson, P Craven, Z Owen, RG Doveston, I Churcher, ... Chemical communications 52 (45), 7209-7212, 2016 | 109 | 2016 |
The novel γ secretase inhibitor N-[cis-4-[(4-chlorophenyl) sulfonyl]-4-(2, 5-difluorophenyl) cyclohexyl]-1, 1, 1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque … JD Best, DW Smith, MA Reilly, R O'Donnell, HD Lewis, S Ellis, N Wilkie, ... Journal of Pharmacology and Experimental Therapeutics 320 (2), 552-558, 2007 | 105 | 2007 |
4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors I Churcher, D Beher, JD Best, JL Castro, EE Clarke, A Gentry, T Harrison, ... Bioorganic & Medicinal Chemistry Letters 16 (2), 280-284, 2006 | 81 | 2006 |
A unified lead-oriented synthesis of over fifty molecular scaffolds RG Doveston, P Tosatti, M Dow, DJ Foley, HY Li, AJ Campbell, D House, ... Organic & biomolecular chemistry 13 (3), 859-865, 2015 | 80 | 2015 |
γ-secretase as a therapeutic target for the treatment of Alzheimer's disease I Churcher, D Beher Current pharmaceutical design 11 (26), 3363-3382, 2005 | 74 | 2005 |
Design and Synthesis of Highly Potent Benzodiazepine γ-Secretase Inhibitors: Preparation of (2S,3R)-3-(3,4- Difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5 … I Churcher, S Williams, S Kerrad, T Harrison, JL Castro, MS Shearman, ... Journal of medicinal chemistry 46 (12), 2275-2278, 2003 | 72 | 2003 |
In vivo characterization of Aβ (40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl) sulfonyl]-4-(2, 5-difluorophenyl … JD Best, MT Jay, F Otu, I Churcher, M Reilly, P Morentin-Gutierrez, ... Journal of Pharmacology and Experimental Therapeutics 317 (2), 786-790, 2006 | 71 | 2006 |
A new series of potent benzodiazepine γ-secretase inhibitors I Churcher, K Ashton, JW Butcher, EE Clarke, T Harrison, HD Lewis, ... Bioorganic & medicinal chemistry letters 13 (2), 179-183, 2003 | 71 | 2003 |
A systematic approach to diverse, lead-like scaffolds from α, α-disubstituted amino acids DJ Foley, RG Doveston, I Churcher, A Nelson, SP Marsden Chemical communications 51 (56), 11174-11177, 2015 | 69 | 2015 |
gamma-Secretase as a target for drug intervention in Alzheimer's disease. T Harrison, I Churcher, D Beher Current opinion in drug discovery & development 7 (5), 709-719, 2004 | 66 | 2004 |
Synthesis and Demonstration of the Biological Relevance of sp3‐rich Scaffolds Distantly Related to Natural Product Frameworks DJ Foley, PGE Craven, PM Collins, RG Doveston, A Aimon, R Talon, ... Chemistry–A European Journal 23 (60), 15227-15232, 2017 | 63 | 2017 |
Leitstruktur‐orientierte Synthese: eine Alternative für die Synthesechemie A Nadin, C Hattotuwagama, I Churcher Angewandte Chemie 124 (5), 1140-1149, 2012 | 60 | 2012 |