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Page 1
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: holmes jl. 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.
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 AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D, Glossop S, Grebe T, Gu C, Hande S, Hawkins J, Hird AW, Holmes J, Horstick J, Jiang Y, Lamb ML, McGuire TM, Moore JE, O'Connell N, Pike A, Pike KG, Proia T, Roberts B, San Martin M, Sarkar U, Shao W, Stead D, Sumner N, Thakur K, Vasbinder MM, Varnes JG, Wang J, Wang L, Wu D, Wu L, Yang B, Yao T. Barlaam B, et al. J Med Chem. 2020 Dec 24;63(24):15564-15590. doi: 10.1021/acs.jmedchem.0c01754. Epub 2020 Dec 11. J Med Chem. 2020. PMID: 33306391
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Barlaam B, De Savi C, Dishington A, Drew L, Ferguson AD, Ferguson D, Gu C, Hande S, Hassall L, Hawkins J, Hird AW, Holmes J, Lamb ML, Lister AS, McGuire TM, Moore JE, O'Connell N, Patel A, Pike KG, Sarkar U, Shao W, Stead D, Varnes JG, Vasbinder MM, Wang L, Wu L, Xue L, Yang B, Yao T. Barlaam B, et al. J Med Chem. 2021 Oct 28;64(20):15189-15213. doi: 10.1021/acs.jmedchem.1c01249. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34647738
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D. McCoull W, et al. Among authors: holmes jl. J Med Chem. 2014 Jul 24;57(14):6128-40. doi: 10.1021/jm500610n. Epub 2014 Jul 8. J Med Chem. 2014. PMID: 24967667
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. Among authors: holmes jl. 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 a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor.
Avgoustou P, Jailani ABA, Zirimwabagabo JO, Tozer MJ, Gibson KR, Glossop PA, Mills JEJ, Porter RA, Blaney P, Bungay PJ, Wang N, Shaw AP, Bigos KJA, Holmes JL, Warrington JI, Skerry TM, Harrity JPA, Richards GO. Avgoustou P, et al. Among authors: holmes jl. ACS Pharmacol Transl Sci. 2020 Jun 25;3(4):706-719. doi: 10.1021/acsptsci.0c00032. eCollection 2020 Aug 14. ACS Pharmacol Transl Sci. 2020. PMID: 32832872 Free PMC article.
105 results