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Page 1
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L. Pike KG, et al. Among authors: robb gr. J Med Chem. 2024 Feb 22;67(4):3090-3111. doi: 10.1021/acs.jmedchem.3c02277. Epub 2024 Feb 2. J Med Chem. 2024. PMID: 38306388
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J, Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG, Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T. Johannes JW, et al. Among authors: robb gr. ACS Med Chem Lett. 2015 Jan 13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12. ACS Med Chem Lett. 2015. PMID: 25815142 Free PMC article.
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.
McCoull W, Bailey A, Barton P, Birch AM, Brown AJ, Butler HS, Boyd S, Butlin RJ, Chappell B, Clarkson P, Collins S, Davies RM, Ertan A, Hammond CD, Holmes JL, Lenaghan C, Midha A, Morentin-Gutierrez P, Moore JE, Raubo P, Robb G. McCoull W, et al. J Med Chem. 2017 Apr 13;60(7):3187-3197. doi: 10.1021/acs.jmedchem.7b00210. Epub 2017 Apr 4. J Med Chem. 2017. PMID: 28374589
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: robb gr. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: robb gr. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Pike KG, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, Davies NL, de-Almeida C, Degorce SL, Didelot M, Dishington A, Ducray R, Durant ST, Hassall LA, Holmes J, Hughes GD, MacFaul PA, Mulholland KR, McGuire TM, Ouvry G, Pass M, Robb G, Stratton N, Wang Z, Wilson J, Zhai B, Zhao K, Al-Huniti N. Pike KG, et al. J Med Chem. 2018 May 10;61(9):3823-3841. doi: 10.1021/acs.jmedchem.7b01896. Epub 2018 May 2. J Med Chem. 2018. PMID: 29683659
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B. Barlaam B, et al. ACS Med Chem Lett. 2018 Jul 13;9(8):809-814. doi: 10.1021/acsmedchemlett.8b00200. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128072 Free PMC article.
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: robb gr. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
57 results