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Timothy M Willson - Publications

Affiliations: 
University of North Carolina, Chapel Hill, Chapel Hill, NC 
Area:
Drug Discovery, Chemical Biology
Website:
www.sgc-unc.org
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37 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2024 Gomez SM, Drewry DH, Willson TM, Major MB, Townsend RR, Sorger PK, Johnson GL. Illuminating function of the understudied druggable kinome. Drug Discovery Today. 103881. PMID 38218213 DOI: 10.1016/j.drudis.2024.103881  0.411
2023 Asquith CRM, East MP, Laitinen T, Alamillo-Ferrer C, Hartikainen E, Wells CI, Axtman AD, Drewry DH, Tizzard GJ, Poso A, Willson TM, Johnson GL. Discovery and Optimization of Narrow Spectrum Inhibitors of Tousled Like Kinase 2 (TLK2) Using Quantitative Structure Activity Relationships. Biorxiv : the Preprint Server For Biology. PMID 38234837 DOI: 10.1101/2023.12.28.573261  0.419
2023 Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM. Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3. Biorxiv : the Preprint Server For Biology. PMID 38106118 DOI: 10.1101/2023.12.04.569845  0.333
2023 Nandakumar M, Ollodart A, Fleck N, Kapadia NR, Frando A, Boradia V, Smith JL, Chen J, Zuercher WJ, Willson TM, Grundner C. Dual Inhibition of and the Host TGFBR1 by an Anilinoquinazoline. Journal of Medicinal Chemistry. PMID 37871287 DOI: 10.1021/acs.jmedchem.3c01273  0.333
2023 Fritch EJ, Mordant AL, Gilbert TSK, Wells CI, Yang X, Barker NK, Madden EA, Dinnon KH, Hou YJ, Tse LV, Castillo IN, Sims AC, Moorman NJ, Lakshmanane P, Willson TM, et al. Investigation of the Host Kinome Response to Coronavirus Infection Reveals PI3K/mTOR Inhibitors as Betacoronavirus Antivirals. Journal of Proteome Research. PMID 37634194 DOI: 10.1021/acs.jproteome.3c00182  0.304
2023 Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM. Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines Toward the Development of an In Vivo Chemical Probe for CSNK2A. Biorxiv : the Preprint Server For Biology. PMID 37292607 DOI: 10.1101/2023.05.15.540828  0.677
2023 Yang X, Smith JL, Beck MT, Wilkinson JM, Michaud A, Vasta JD, Robers MB, Willson TM. Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells. Molecules (Basel, Switzerland). 28. PMID 37049713 DOI: 10.3390/molecules28072950  0.388
2023 Yang X, Smith JL, Beck MT, Wilkinson JM, Michaud A, Vasta JD, Robers MB, Willson TM. Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells. Biorxiv : the Preprint Server For Biology. PMID 36865333 DOI: 10.1101/2023.02.25.529946  0.381
2022 Yang X, Dickmander RJ, Bayati A, Taft-Benz SA, Smith JL, Wells CI, Madden EA, Brown JW, Lenarcic EM, Yount BL, Chang E, Axtman AD, Baric RS, Heise MT, McPherson PS, ... ... Willson TM, et al. Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses. Acs Chemical Biology. PMID 35723434 DOI: 10.1021/acschembio.2c00378  0.728
2022 Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, ... ... Willson TM, et al. AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery. Alzheimer's & Dementia (New York, N. Y.). 8: e12246. PMID 35475262 DOI: 10.1002/trc2.12246  0.642
2022 Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH, ... ... Willson TM, et al. Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology. Alzheimer's & Dementia (New York, N. Y.). 8: e12253. PMID 35434254 DOI: 10.1002/trc2.12253  0.652
2022 Yang X, Dickmander RJ, Bayati A, Taft-Benz SA, Smith JL, Brown JW, Lenarcic EM, Yount BL, Chang E, Axtman AD, Baric RS, Heise MT, McPherson PS, Moorman NJ, Willson TM. Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2. Biorxiv : the Preprint Server For Biology. PMID 35018375 DOI: 10.1101/2022.01.03.474779  0.72
2021 Eduful BJ, O'Byrne SN, Temme L, Asquith CRM, Liang Y, Picado A, Pilotte JR, Hossain MA, Wells CI, Zuercher WJ, Catta-Preta CMC, Zonzini Ramos P, Santiago AS, Couñago RM, Langendorf CG, ... ... Willson TM, et al. Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes. Journal of Medicinal Chemistry. PMID 34264658 DOI: 10.1021/acs.jmedchem.0c02274  0.727
2021 Cichońska A, Ravikumar B, Allaway RJ, Wan F, Park S, Isayev O, Li S, Mason M, Lamb A, Tanoli Z, Jeon M, Kim S, Popova M, Capuzzi S, Zeng J, ... ... Willson TM, et al. Crowdsourced mapping of unexplored target space of kinase inhibitors. Nature Communications. 12: 3307. PMID 34083538 DOI: 10.1038/s41467-021-23165-1  0.353
2021 Wells CI, Al-Ali H, Andrews DM, Asquith CRM, Axtman AD, Dikic I, Ebner D, Ettmayer P, Fischer C, Frederiksen M, Futrell RE, Gray NS, Hatch SB, Knapp S, Lücking U, ... ... Willson TM, et al. The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. International Journal of Molecular Sciences. 22. PMID 33429995 DOI: 10.3390/ijms22020566  0.76
2020 Picado A, Chaikuad A, Wells CI, Shrestha S, Zuercher WJ, Pickett JE, Kwarcinski FE, Sinha P, de Silva CS, Zutshi R, Liu S, Kannan N, Knapp S, Drewry DH, Willson TM. A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation. Journal of Medicinal Chemistry. PMID 33215924 DOI: 10.1021/acs.jmedchem.0c01174  0.35
2020 Wells CI, Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Ingold MR, Pickett JE, Drewry DH, Pugh KM, Schwinn MK, Hwang BB, Zegzouti H, Huber KVM, Cong M, Meisenheimer PL, ... Willson TM, et al. Quantifying CDK inhibitor selectivity in live cells. Nature Communications. 11: 2743. PMID 32488087 DOI: 10.1038/s41467-020-16559-0  0.414
2020 Asquith CRM, Tizzard GJ, Bennett JM, Wells CI, Elkins JM, Willson TM, Poso A, Laitinen T. Targeting the water network in cyclin G associated kinase (GAK) with 4-anilino-quin(az)oline inhibitors. Chemmedchem. PMID 32358915 DOI: 10.1002/cmdc.202000150  0.703
2020 Wells C, Couñago RM, Limas JC, Almeida TL, Cook JG, Drewry DH, Elkins JM, Gileadi O, Kapadia NR, Lorente-Macias A, Pickett JE, Riemen A, Ruela-de-Sousa RR, Willson TM, Zhang C, et al. SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K. Acs Medicinal Chemistry Letters. 11: 340-345. PMID 32184967 DOI: 10.1021/Acsmedchemlett.9B00399  0.721
2020 O'Byrne SN, Scott JW, Pilotte JR, Santiago ADS, Langendorf CG, Oakhill JS, Eduful BJ, Couñago RM, Wells CI, Zuercher WJ, Willson TM, Drewry DH. In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds. Molecules (Basel, Switzerland). 25. PMID 31941153 DOI: 10.3390/molecules25020325  0.468
2019 Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ. Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK). Molecules (Basel, Switzerland). 24. PMID 31698822 DOI: 10.3390/molecules24224016  0.699
2019 Drewry DH, Wells CI, Zuercher WJ, Willson TM. A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction. Slas Discovery : Advancing Life Sciences R & D. 2472555219838210. PMID 31034310 DOI: 10.1177/2472555219838210  0.309
2019 Asquith CRM, Berger BT, Wan J, Bennett JM, Capuzzi SJ, Crona DJ, Drewry D, East MP, Elkins JM, Fedorov O, Godoi PH, Hunter DM, Knapp S, Müller S, Torrice CD, ... ... Willson T, et al. SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK). Journal of Medicinal Chemistry. PMID 30768268 DOI: 10.1021/acs.jmedchem.8b01213  0.732
2019 Agajanian MJ, Walker MP, Axtman AD, Ruela-de-Sousa RR, Serafin DS, Rabinowitz AD, Graham DM, Ryan MB, Tamir T, Nakamichi Y, Gammons MV, Bennett JM, Couñago RM, Drewry DH, Elkins JM, ... ... Willson TM, et al. WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop. Cell Reports. 26: 79-93.e8. PMID 30605688 DOI: 10.1016/J.Celrep.2018.12.023  0.681
2018 Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS. 1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors. Molecules (Basel, Switzerland). 23. PMID 29783765 DOI: 10.3390/Molecules23051221  0.726
2018 Krulikas LJ, McDonald IM, Lee B, Okumu DO, East MP, Gilbert TSK, Herring LE, Golitz BT, Wells CI, Axtman AD, Zuercher WJ, Willson TM, Kireev D, Yeh JJ, Johnson GL, et al. Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth. Slas Discovery : Advancing Life Sciences R & D. 2472555218773045. PMID 29742358 DOI: 10.1177/2472555218773045  0.397
2018 Pariollaud M, Gibbs J, Hopwood T, Brown S, Begley N, Vonslow R, Poolman T, Guo B, Saer B, Jones DH, Tellam JP, Bresciani S, Tomkinson NC, Wojno-Picon J, Cooper AW, ... ... Willson TM, et al. Circadian clock component REV-ERBα controls homeostatic regulation of pulmonary inflammation. The Journal of Clinical Investigation. PMID 29533925 DOI: 10.1172/Jci93910  0.478
2017 Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Hartnett JR, Ingold MR, Zimmerman K, Machleidt T, Kirkland TA, Huwiler KG, Ohana RF, Slater M, Otto P, Cong M, Wells CI, ... ... Willson TM, et al. Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. Cell Chemical Biology. PMID 29174542 DOI: 10.1016/j.chembiol.2017.10.010  0.422
2017 Asquith CRM, Laitinen T, Bennett JM, Godoi PH, East MP, Tizzard GJ, Graves LM, Johnson GL, Dornsife RE, Wells CI, Elkins JM, Willson TM, Zuercher W. Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase. Chemmedchem. PMID 29072804 DOI: 10.1002/Cmdc.201700663  0.72
2017 Drewry DH, Wells CI, Andrews DM, Angell R, Al-Ali H, Axtman AD, Capuzzi SJ, Elkins JM, Ettmayer P, Frederiksen M, Gileadi O, Gray N, Hooper A, Knapp S, Laufer S, ... ... Willson TM, et al. Progress towards a public chemogenomic set for protein kinases and a call for contributions. Plos One. 12: e0181585. PMID 28767711 DOI: 10.1371/Journal.Pone.0181585  0.743
2015 Elkins JM, Fedele V, Szklarz M, Abdul Azeez KR, Salah E, Mikolajczyk J, Romanov S, Sepetov N, Huang XP, Roth BL, Al Haj Zen A, Fourches D, Muratov E, Tropsha A, Morris J, ... ... Willson TM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nature Biotechnology. PMID 26501955 DOI: 10.1038/Nbt.3374  0.496
2015 Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, ... ... Willson TM, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. Journal of Medicinal Chemistry. PMID 25799074 DOI: 10.1021/Acs.Jmedchem.5B00209  0.349
2014 Drewry DH, Willson TM, Zuercher WJ. Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS). Current Topics in Medicinal Chemistry. 14: 340-2. PMID 24283969 DOI: 10.2174/1568026613666131127160819  0.417
2013 Trump RP, Bresciani S, Cooper AW, Tellam JP, Wojno J, Blaikley J, Orband-Miller LA, Kashatus JA, Boudjelal M, Dawson HC, Loudon A, Ray D, Grant D, Farrow SN, Willson TM, et al. Optimized chemical probes for REV-ERBα. Journal of Medicinal Chemistry. 56: 4729-37. PMID 23656296 DOI: 10.1021/Jm400458Q  0.557
2013 Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, et al. A public-private partnership to unlock the untargeted kinome. Nature Chemical Biology. 9: 3-6. PMID 23238671 DOI: 10.1038/Nchembio.1113  0.512
2011 Whitby RJ, Stec J, Blind RD, Dixon S, Leesnitzer LM, Orband-Miller LA, Williams SP, Willson TM, Xu R, Zuercher WJ, Cai F, Ingraham HA. Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2). Journal of Medicinal Chemistry. 54: 2266-81. PMID 21391689 DOI: 10.1021/Jm1014296  0.557
2006 Whitby RJ, Dixon S, Maloney PR, Delerive P, Goodwin BJ, Parks DJ, Willson TM. Identification of small molecule agonists of the orphan nuclear receptors liver receptor homolog-1 and steroidogenic factor-1. Journal of Medicinal Chemistry. 49: 6652-5. PMID 17154495 DOI: 10.1021/Jm060990K  0.539
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