William McCoull

chemistry

H指数:24

被引数:2,115

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AZ14289671 is a highly selective and blood-brain barrier penetrant irreversible TKI that targets EGFRExon20 insertions

AZ14289671 是一种高选择性的血脑屏障穿透性不可逆TKI，可靶向EGFRExon20插入突变。

Cell Reports Medicine

IF10.6

2025-08-250

OAAI

The changing landscape of medicinal chemistry optimization

药物化学优化的变化格局

Nature Reviews Drug Discovery

IF101.8

2025-07-070

PRE

Highly Optimized CNS Penetrant Inhibitors of EGFR Exon20 Insertion Mutations

高度优化的中枢神经系统穿透性EGFR外显子20插入突变抑制剂

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2025-01-271

PRE

Mccoull, William; Braybrooke, Erin; Chan, Christina; Colclough, Nicola; Gonzalez, Miguel A. Cortes; Cosulich, Sabina; Davies, Nichola L.; Floc'h, Nicolas; Greenwood, Ryan; Hargreaves, David; Huang, Peng; Hunt, Thomas A.; Johnson, Tony; Johnstrom, Peter; Kettle, Jason G.; Kondrashov, Mikhail; Kostomiris, Demetrios H.; Li, Songlei; Lister, Andrew; Martin, Scott; Mckerrecher, Darren; Mclean, Neville; Nissink, J. Willem M.; Orme, Jonathan P.; Orwig, Paige; Packer, Martin J.; Pearson, Stuart; Qin, Lina; Felisberto-Rodrigues, Catarina; Savoca, Adriana; Schou, Magnus; Stokes, Stephen; Swaih, Aisha M.; Talbot, Sara; Tucker, Michael J.; Ward, Richard A.; Wadforth, Emma; Wang, Chunli; Wilson, Joanne; Yang, Yawen

Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2024-09-280

PRE

Thomson, Clare; Braybrooke, Erin; Colclough, Nicola; Davies, Nichola L.; Floc'h, Nicolas; Greenwood, Ryan; Guerot, Carine; Hargreaves, David; Johnstrom, Peter; Khurana, Puneet; Kostomiris, Demetrios H.; Li, Songlei; Lister, Andrew; Lorthioir, Olivier; Martin, Scott; Mccoull, William; Mclean, Neville J.; Mcwilliams, Lisa; Orme, Jonathan P.; Packer, Martin J.; Pearson, Stuart; Swaih, Aisha M.; Tentarelli, Sharon; Tucker, Michael J.; Ward, Richard A.; Wilkinson, Stephen; Winlow, Poppy; Wood, Isabel L.

Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2024-05-212

PRE

Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment

ARCHIVES OF TOXICOLOGY

IF6.9

2022-01-018

OAAI

Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-09-0319

PRE

McCoull, William; Boyd, Scott; Brown, Martin R.; Coen, Muireann; Collingwood, Olga; Davies, Nichola L.; Doherty, Ann; Fairley, Gary; Goldberg, Kristin; Hardaker, Elizabeth; He, Guang; Hennessy, Edward J.; Hopcroft, Philip; Hodgson, George; Jackson, Anne; Jiang, Xiefeng; Karmokar, Ankur; Laine, Anne-Laure; Lindsay, Nicola; Mao, Yumeng; Markandu, Roshini; McMurray, Lindsay; McLean, Neville; Mooney, Lorraine; Musgrove, Helen; Nissink, J. Willem M.; Pflug, Alexander; Reddy, Venkatesh Pilla; Rawlins, Philip B.; Rivers, Emma; Schimpl, Marianne; Smith, Graham F.; Tentarelli, Sharon; Travers, Jon; Troup, Robert, I; Walton, Josephine; Wang, Cheng; Wilkinson, Stephen; Williamson, Beth; Winter-Holt, Jon; Yang, Dejian; Zheng, Yuting; Zhu, Qianxiu; Smith, Paul D.

Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-03-0818

PREAI

Nissink, J. Willem M.; Bazzaz, Sana; Blackett, Carolyn; Clark, Matthew A.; Collingwood, Olga; Disch, Jeremy S.; Gikunju, Diana; Goldberg, Kristin; Guilinger, John P.; Hardaker, Elizabeth; Hennessy, Edward J.; Jetson, Rachael; Keefe, Anthony D.; McCoull, William; McMurray, Lindsay; Olszewski, Allison; Overman, Ross; Pflug, Alexander; Preston, Marian; Rawlins, Philip B.; Rivers, Emma; Schimpl, Marianne; Smith, Paul; Truman, Caroline; Underwood, Elizabeth; Warwicker, Juli; Winter-Holt, Jon; Woodcock, Simon; Zhang, Ying

Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles (vol 62, pg 9418, 2019)

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-03-010

OAAI

Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy

COMMUNICATIONS BIOLOGY

IF5.1

2021-01-2567

OAAI

Patterson, Claire M.; Balachander, Srividya B.; Grant, Iain; Pop-Damkov, Petar; Kelly, Brian; McCoull, William; Parker, Jeremy; Giannis, Michael; Hill, Kathryn J.; Gibbons, Francis D.; Hennessy, Edward J.; Kemmitt, Paul; Harmer, Alexander R.; Gales, Sonya; Purbrick, Stuart; Redmond, Sean; Skinner, Matthew; Graham, Lorraine; Secrist, J. Paul; Schuller, Alwin G.; Wen, Shenghua; Adam, Ammar; Reimer, Corinne; Cidado, Justin; Wild, Martin; Gangl, Eric; Fawell, Stephen E.; Saeh, Jamal; Davies, Barry R.; Owen, David J.; Ashford, Marianne B.

A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding

BIOCHEMICAL JOURNAL

IF4.3

2020-11-2717

OAAI

Design and optimization of a dendrimer-conjugated dual Bcl-2/Bcl-xL inhibitor, AZD0466, with improved therapeutic index

CANCER RESEARCH

IF16.6

2020-08-152

PRE

Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2019-07-3026

OAAI

Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6

ACS CHEMICAL BIOLOGY

IF3.8

2018-10-17120

OAAI

McCoull, William; Cheung, Tony; Anderson, Erica; Barton, Peter; Burgess, Jonathan; Byth, Kate; Cao, Qing; Castald, M. Paola; Chen, Huawei; Chiarparin, Elisabetta; Carbajo, Rodrigo J.; Code, Erin; Cowan, Suzanna; Davey, Paul R.; Ferguson, Andrew D.; Fillery, Shaun; Fuller, Nathan O.; Gao, Ning; Hargreaves, David; Howard, Martin R.; Hu, Jun; Kawatkar, Aarti; Kemmitt, Paul D.; Leo, Elisabetta; Molina, Daniel M.; O'Conne', Nichole; Petteruti, Philip; Rasmusson, Timothy; Raubo, Piotr; Rawlins, Philip B.; Ricchiuto, Piero; Robb, Graeme R.; Schenone, Monica; Waring, Michael J.; Zinda, Michael; Fawell, Stephen; Wilson, David M.

Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors (vol 60, pg 4386, 2017)

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-07-171

OAAI

McCoull, William; Abrams, Roman D.; Anderson, Erica; Blades, Kevin; Barton, Peter; Box, Matthew; Burgess, Jonathan; Byth, Kate; Cao, Qing; Chuaqui, Claudio; Carbajo, Rodrigo J.; Cheung, Tony; Code, Erin; Ferguson, Andrew D.; Fillery, Shaun; Fuller, Nathan O.; Gangl, Eric; Gao, Ning; Grist, Matthew; Hargreaves, David; Howard, Martin R.; Hu, Jun; Kemmitt, Paul D.; Nelson, Jennifer E.; O'Connell, Nichole; Prince, D. Bryan; Raubo, Piotr; Rawlins, Philip B.; Robb, Graeme R.; Shi, Junjie; Waring, Michael J.; Whittaker, David; Wylot, Marta; Zhu, Xiahui

Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-05-0964

OAAI

Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2017-04-0431

PREAI

Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors

ACS MEDICINAL CHEMISTRY LETTERS