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Graeme Robb
Graeme Robb
Director, AstraZeneca
Verifierad e-postadress på astrazeneca.com
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Matched molecular pairs as a medicinal chemistry tool: miniperspective
E Griffen, AG Leach, GR Robb, DJ Warner
Journal of medicinal chemistry 54 (22), 7739-7750, 2011
2822011
Potent and selective bivalent inhibitors of BET bromodomains
MJ Waring, H Chen, AA Rabow, G Walker, R Bobby, S Boiko, ...
Nature chemical biology 12 (12), 1097-1104, 2016
1372016
Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6
W McCoull, T Cheung, E Anderson, P Barton, J Burgess, K Byth, Q Cao, ...
ACS Chemical Biology 13 (11), 3131-3141, 2018
1302018
The identification of potent, selective, and orally available inhibitors of ataxia telangiectasia mutated (ATM) kinase: the discovery of AZD0156 (8-{6-[3-(Dimethylamino …
KG Pike, B Barlaam, E Cadogan, A Campbell, Y Chen, N Colclough, ...
Journal of medicinal chemistry 61 (9), 3823-3841, 2018
1042018
Hypothesis driven drug design: improving quality and effectiveness of the design-make-test-analyse cycle
AT Plowright, C Johnstone, J Kihlberg, J Pettersson, G Robb, ...
Drug discovery today 17 (1-2), 56-62, 2012
892012
Learning medicinal chemistry absorption, distribution, metabolism, excretion, and toxicity (ADMET) rules from cross-company matched molecular pairs analysis (MMPA) miniperspective
C Kramer, A Ting, H Zheng, J Hert, T Schindler, M Stahl, G Robb, ...
Journal of medicinal chemistry 61 (8), 3277-3292, 2017
762017
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors
W McCoull, RD Abrams, E Anderson, K Blades, P Barton, M Box, ...
Journal of Medicinal Chemistry 60 (10), 4386-4402, 2017
672017
Residues within the transmembrane domain of the glucagon-like peptide-1 receptor involved in ligand binding and receptor activation: modelling the ligand-bound receptor
K Coopman, R Wallis, G Robb, AJH Brown, GF Wilkinson, D Timms, ...
Molecular endocrinology 25 (10), 1804-1818, 2011
662011
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C
JG Kettle, SK Bagal, S Bickerton, MS Bodnarchuk, J Breed, RJ Carbajo, ...
Journal of medicinal chemistry 63 (9), 4468-4483, 2020
592020
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology
JW Johannes, L Almeida, B Barlaam, PA Boriack-Sjodin, R Casella, ...
ACS medicinal chemistry letters 6 (3), 254-259, 2015
572015
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse …
JS Scott, SL Degorce, R Anjum, J Culshaw, RDM Davies, NL Davies, ...
Journal of medicinal chemistry 60 (24), 10071-10091, 2017
532017
Temperature-resolved, in-situ powder X-ray diffraction of silver iodide under microwave irradiation
GR Robb, A Harrison, AG Whittaker
PhysChemComm 5 (19), 135-137, 2002
522002
In situ neutron diffraction studies of single crystals and powders during microwave irradiation
A Harrison, R Ibberson, G Robb, G Whittaker, C Wilson, D Youngson
Faraday discussions 122, 363-379, 2003
382003
Property based optimisation of glucokinase activators–discovery of the phase IIb clinical candidate AZD1656
MJ Waring, DS Clarke, MD Fenwick, L Godfrey, SD Groombridge, ...
MedChemComm 3 (9), 1077-1081, 2012
362012
Potent, selective small molecule inhibitors of type III phosphatidylinositol-4-kinase α-but not β-inhibit the phosphatidylinositol signaling cascade and cancer cell proliferation
MJ Waring, DM Andrews, PF Faulder, V Flemington, JC McKelvie, ...
Chemical communications 50 (40), 5388-5390, 2014
332014
Indazole-6-phenylcyclopropylcarboxylic acids as selective GPR120 agonists with in vivo efficacy
W McCoull, A Bailey, P Barton, AM Birch, AJH Brown, HS Butler, S Boyd, ...
Journal of medicinal chemistry 60 (7), 3187-3197, 2017
322017
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C
JG Kettle, SK Bagal, S Bickerton, MS Bodnarchuk, S Boyd, J Breed, ...
Journal of Medicinal Chemistry 65 (9), 6940-6952, 2022
312022
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists
W McCoull, P Barton, AJH Brown, SS Bowker, J Cameron, DS Clarke, ...
Journal of medicinal chemistry 57 (14), 6128-6140, 2014
312014
Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092
MJ Waring, C Johnstone, D McKerrecher, KG Pike, G Robb
MedChemComm 2 (8), 775-779, 2011
312011
Free ligand 1D NMR conformational signatures to enhance structure based drug design of a Mcl-1 inhibitor (AZD5991) and other synthetic macrocycles
AYS Balazs, RJ Carbajo, NL Davies, Y Dong, AW Hird, JW Johannes, ...
Journal of Medicinal Chemistry 62 (21), 9418-9437, 2019
292019
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Artiklar 1–20