Tim Willson

Research Professor (UNC) - Chief Scientist (SGC)

University of North Carolina at Chapel Hill
(919) 491-3177

Tim Willson is chief scientist of the SGC-UNC, an open-discovery network for protein kinases based at the UNC Eshelman School of Pharmacy. He has more than 25 years of experience in pharmaceutical research with a track record in discovery of first-in-class clinical candidates. Throughout his career, Willson has been an advocate for research on pioneer drug targets. He led the Glaxo program on orphan nuclear receptors that uncovered their role in regulation of human metabolism and was co-discoverer of obeticholic acid, a breakthrough medicine for liver diseases targeting FXR. Willson has been a long time supporter of precompetitive chemistry in early drug discovery and was a scientific founder of the SGC Epigenetic Chemical Probes project. He is widely recognized for scientific leadership in chemical biology and was named one of the world’s 400 most influential biomedical researchers. Outside of science, Willson enjoys the challenge of long course triathlons and has completed six Ironman 70.3 distance races.

Research Areas

Willson has been a long-time supporter of precompetitive chemistry as a mechanism to bring innovation to early drug discovery. His team has made potent and selective chemical probes for orphan nuclear receptors widely available in the scientific community. He was a scientific founder of the SGC Epigenetic Chemical Probes project that led to the release into the public domain of more than 30 chemical probes that specifically inhibit enzyme modifiers and protein readers of the histone tails.

Open access chemical and clinical probes to support drug discovery.
Edwards AM, Bountra C, Kerr DJ, Willson TM
Nat. Chem. Biol.. 2009 5(7):436-40. doi: 10.1038/nchembio0709-436
PMID: 19536100

Too many roads not taken.
Edwards AM, Isserlin R, Bader GD, Frye SV, Willson TM, Yu FH
Nature. 2011 470(7333):163-5. doi: 10.1038/470163a
PMID: 21307913

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)
Drewry DH, Willson TM, Zuercher WJ.
Curr Top Med Chem. 2014 14(3):340-2. doi:
PMID: 24283969

Orphan nuclear receptors: shifting endocrinology into reverse.
Kliewer SA, Lehmann JM, Willson TM.
Science. 1999 284(5415):757-60. doi:
PMID: 10221899

Identification of a chemical tool for the orphan nuclear receptor FXR
Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones SA, Willson TM.
J Med Chem.. 2000 43(16):2971-4. doi:
PMID: 10956205

A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.
Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM.
Proc Natl Acad Sci U S A. . 2001 98(9):5306-11.. doi:
PMID: 11309497

6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Maloney PR, Morelli A, Parks DJ, Willson TM.
J Med Chem.. 2002 45(17):3569-72. doi:
PMID: 12166927

A public-private partnership to unlock the untargeted kinome.
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, Zuercher WJ
Nat. Chem. Biol.. 2012 9(1):3-6. doi: 10.1038/nchembio.1113
PMID: 23238671

2024

Identification of 4-(6-((2-methoxyphenyl)amino)pyrazin-2-yl)benzoic acids as CSNK2A inhibitors with antiviral activity and improved selectivity over PIM3.
Galal KA, Krämer A, Strickland BG, Smith JL, Dickmander RJ, Moorman NJ, Willson TM
Bioorg Med Chem Lett. 08.01.2024 99:129617. doi: 10.1016/j.bmcl.2024.129617
PMID: 38199328

2023

Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines toward the Development of an In Vivo Chemical Probe for CSNK2A.
Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM
ACS Omega. 24.10.2023 8(42):39546-39561. doi: 10.1021/acsomega.3c05377
PMID: 37901516

Fused Tetrahydroquinolines Are Interfering with Your Assay.
Bashore FM, Annor-Gyamfi J, Du Y, Katis V, Nwogbo F, Flax RG, Frye SV, Pearce KH, Fu H, Willson TM, Drewry DH, Axtman AD
J Med Chem. 24.10.2023 . doi: 10.1021/acs.jmedchem.3c01277
PMID: 37874947

Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline.
Nandakumar M, Ollodart A, Fleck N, Kapadia NR, Frando A, Boradia V, Smith JL, Chen J, Zuercher WJ, Willson TM, Grundner C
J Med Chem. 23.10.2023 . doi: 10.1021/acs.jmedchem.3c01273
PMID: 37871287

Investigation of the Host Kinome Response to Coronavirus Infection Reveals PI3K/mTOR Inhibitors as Betacoronavirus Antivirals.
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, Herring LE, Graves LM, Baric RS
J Proteome Res. 27.08.2023 . doi: 10.1021/acs.jproteome.3c00182
PMID: 37634194

Target 2035 - an update on private sector contributions.
Ackloo S, Antolin AA, Bartolome JM, Beck H, Bullock A, Betz UAK, Böttcher J, Brown PJ, Chaturvedi M, Crisp A, Daniels D, Dreher J, Edfeldt K, Edwards AM, Egner U, Elkins J, Fischer C, Glendorf T, Goldberg S, Hartung IV, Hillisch A, Homan E, Knapp S, Köster M, Krämer O, Llaveria J, Lessel U, Lindemann S, Linderoth L, Matsui H, Michel M, Montel F, Mueller-Fahrnow A, Müller S, Owen DR, Saikatendu KS, Santhakumar V, Sanderson W, Scholten C, Schapira M, Sharma S, Shireman B, Sundström M, Todd MH, Tredup C, Venable J, Willson TM, Arrowsmith CH
RSC Med Chem. 22.06.2023 14(6):1002-1011. doi: 10.1039/d2md00441k
PMID: 37360399

Development of Cell Permeable NanoBRET Probes for the Measurement of PLK1 Target Engagement in Live Cells.
Yang X, Smith JL, Beck MT, Wilkinson JM, Michaud A, Vasta JD, Robers MB, Willson TM
Molecules. 25.03.2023 28(7):. doi: 10.3390/molecules28072950
PMID: 37049713

2022

A New Chemotype of Chemically Tractable Nonsteroidal Estrogens Based on a Thieno[2,3-d]pyrimidine Core.
Sammeta VR, Norris JD, Artham S, Torrice CD, Byemerwa J, Joiner C, Fanning SW, McDonnell DP, Willson TM
ACS Med Chem Lett. 14.07.2022 13(7):1151-1158. doi: 10.1021/acsmedchemlett.2c00180
PMID: 35859859

CACHE (Critical Assessment of Computational Hit-finding Experiments): A public-private partnership benchmarking initiative to enable the development of computational methods for hit-finding.
Ackloo S, Al-Awar R, Amaro RE, Arrowsmith CH, Azevedo H, Batey RA, Bengio Y, Betz UAK, Bologa CG, Chodera JD, Cornell WD, Dunham I, Ecker GF, Edfeldt K, Edwards AM, Gilson MK, Gordijo CR, Hessler G, Hillisch A, Hogner A, Irwin JJ, Jansen JM, Kuhn D, Leach AR, Lee AA, Lessel U, Morgan MR, Moult J, Muegge I, Oprea TI, Perry BG, Riley P, Rousseaux SAL, Saikatendu KS, Santhakumar V, Schapira M, Scholten C, Todd MH, Vedadi M, Volkamer A, Willson TM
Nat Rev Chem. 06.07.2022 6(4):287-295. doi: 10.1038/s41570-022-00363-z
PMID: 35783295

Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.
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, Moorman NJ, Willson TM
ACS Chem Biol. 19.06.2022 . doi: 10.1021/acschembio.2c00378
PMID: 35723434

AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.
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, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD
Alzheimers Dement (N Y). 28.04.2022 8(1):e12246. doi: 10.1002/trc2.12246
PMID: 35475262

Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology.
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, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD
Alzheimers Dement (N Y). 19.04.2022 8(1):e12253. doi: 10.1002/trc2.12253
PMID: 35434254

Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH
RSC Med Chem. 27.01.2022 13(1):13-21. doi: 10.1039/d1md00228g
PMID: 35211674

2021

Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes.
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, Nay K, Oakhill JS, Pulliam TL, Lin C, Awad D, Willson TM, Frigo DE, Scott JW, Drewry DH
J Med Chem. 15.07.2021 . doi: 10.1021/acs.jmedchem.0c02274
PMID: 34264658

Crowdsourced mapping of unexplored target space of kinase inhibitors.
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, Dang K, Koytiger G, Kang J, Wells CI, Willson TM, Oprea TI, Schlessinger A, Drewry DH, Stolovitzky G, Wennerberg K, Guinney J, Aittokallio T
Nat Commun. 03.06.2021 12(1):3307. doi: 10.1038/s41467-021-23165-1
PMID: 34083538

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.
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, Michaelides M, Mills CE, Müller S, Owen D, Picado A, Saikatendu KS, Schröder M, Stolz A, Tellechea M, Turunen BJ, Vilar S, Wang J, Zuercher WJ, Willson TM, Drewry DH
Int J Mol Sci. 08.01.2021 22(2):. doi: 10.3390/ijms22020566
PMID: 33429995

2020

A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation.
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
J Med Chem. 20.11.2020 . doi: 10.1021/acs.jmedchem.0c01174
PMID: 33215924

Quantifying CDK inhibitor selectivity in live cells
Wells CI, Vasta JD, Corona CR, Wilkinson J, Zimprich CA, Ingold MR, Pickett JE, Drewry DH, Pugh KM, Schwinn MK, Hwang B, Zegzouti H, Huber KVM, Cong M, Meisenheimer PL, Willson TM, Robers MB
Nature Communications. 01.06.2020 11:2743-. doi: 10.1038/s41467-020-16559-0
PMID: 32488087

Quantifying CDK inhibitor selectivity in live cells.
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, Robers MB
Nat Commun. 02.06.2020 11(1):2743. doi: 10.1038/s41467-020-16559-0
PMID: 32488087

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.
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, Zuercher WJ, Zutshi R, Axtman AD
ACS Med Chem Lett. 12.03.2020 11(3):340-345. doi: 10.1021/acsmedchemlett.9b00399
PMID: 32184967

In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds.
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
Molecules. 13.01.2020 25(2):. doi: 10.3390/molecules25020325
PMID: 31941153

2019

Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK)
Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ
Molecules (Basel, Switzerland). 06.11.2019 24:-. doi: 10.3390/molecules24224016
PMID: 31698822

Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK).
Asquith CRM, Bennett JM, Su L, Laitinen T, Elkins JM, Pickett JE, Wells CI, Li Z, Willson TM, Zuercher WJ
Molecules. 06.11.2019 24(22):. doi: 10.3390/molecules24224016
PMID: 31698822

Gram-scale synthesis of FICZ, a photoreactive endogenous ligand of the aryl hydrocarbon receptor.
Zhang C, Creech KL, Zuercher WJ, Willson TM
Sci Rep. 10.07.2019 9(1):9982. doi: 10.1038/s41598-019-46374-7
PMID: 31292477

A Perspective on Extreme Open Science: Companies Sharing Compounds without Restriction.
Drewry DH, Wells CI, Zuercher WJ, Willson TM
SLAS Discov. 29.04.2019 2472555219838210. doi: 10.1177/2472555219838210
PMID: 31034310

WNT Activates the AAK1 Kinase to Promote Clathrin-Mediated Endocytosis of LRP6 and Establish a Negative Feedback Loop.
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, Gileadi C, Gileadi O, Godoi PH, Kapadia N, Müller S, Santiago AS, Sorrell FJ, Wells CI, Fedorov O, Willson TM, Zuercher WJ, Major MB
Cell Rep. 02.01.2019 26(1):79-93.e8. doi: 10.1016/j.celrep.2018.12.023
PMID: 30605688

SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K
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, Zuercher WJ, Zutshi R, Axtman AD
ACS Medicinal Chemistry Letters. 29.10.2019 . doi: 10.1021/acsmedchemlett.9b00399
PMID:

2018

1,2,6-Thiadiazinones as Novel Narrow Spectrum Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CaMKK2) Inhibitors.
Asquith CRM, Godoi PH, Couñago RM, Laitinen T, Scott JW, Langendorf CG, Oakhill JS, Drewry DH, Zuercher WJ, Koutentis PA, Willson TM, Kalogirou AS
Molecules. 19.05.2018 23(5):. doi: 10.3390/molecules23051221
PMID: 29783765

Application of Integrated Drug Screening/Kinome Analysis to Identify Inhibitors of Gemcitabine-Resistant Pancreatic Cancer Cell Growth.
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, Baines AT, Graves LM
SLAS Discov. 01.05.2018 2472555218773045. doi: 10.1177/2472555218773045
PMID: 29742358

Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A
Elife. 20.04.2018 7:. doi: 10.7554/eLife.34311
PMID: 29676732

Circadian clock component REV-ERBα controls homeostatic regulation of pulmonary inflammation.
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, Daniels DA, Trump RP, Grant D, Zuercher W, Willson TM, MacDonald AS, Bolognese B, Podolin PL, Sanchez Y, Loudon AS, Ray DW
J. Clin. Invest.. 13.03.2018 . doi: 10.1172/JCI93910
PMID: 29533925

2017

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.
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, Berger BT, Hanke T, Glas C, Ding K, Drewry DH, Huber KVM, Willson TM, Knapp S, Müller S, Meisenheimer PL, Fan F, Wood KV, Robers MB
Cell Chem Biol. 13.11.2017 . doi: 10.1016/j.chembiol.2017.10.010
PMID: 29174542

Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.
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
ChemMedChem. 26.10.2017 . doi: 10.1002/cmdc.201700663
PMID: 29072804

Progress towards a public chemogenomic set for protein kinases and a call for contributions.
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, Luecking U, Michaelides M, Müller S, Muratov E, Denny RA, Saikatendu KS, Treiber DK, Zuercher WJ, Willson TM
PLoS ONE. 03.08.2017 12(8):e0181585. doi: 10.1371/journal.pone.0181585
PMID: 28767711

2015

Comprehensive characterization of the Published Kinase Inhibitor Set.
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, Teicher BA, Kunkel M, Polley E, Lackey KE, Atkinson FL, Overington JP, Bamborough P, Müller S, Price DJ, Willson TM, Drewry DH, Knapp S, Zuercher WJ
Nat. Biotechnol.. 26.10.2015 . doi: 10.1038/nbt.3374
PMID: 26501955

The promise and peril of chemical probes.
Arrowsmith CH, Audia JE, Austin C, Baell J, Bennett J, Blagg J, Bountra C, Brennan PE, Brown PJ, Bunnage ME, Buser-Doepner C, Campbell RM, Carter AJ, Cohen P, Copeland RA, Cravatt B, Dahlin JL, Dhanak D, Edwards AM, Frye SV, Gray N, Grimshaw CE, Hepworth D, Howe T, Huber KV, Jin J, Knapp S, Kotz JD, Kruger RG, Lowe D, Mader MM, Marsden B, Mueller-Fahrnow A, Müller S, O'Hagan RC, Overington JP, Owen DR, Rosenberg SH, Roth B, Ross R, Schapira M, Schreiber SL, Shoichet B, Sundström M, Superti-Furga G, Taunton J, Toledo-Sherman L, Walpole C, Walters MA, Willson TM, Workman P, Young RN, Zuercher WJ
Nat. Chem. Biol.. 21.07.2015 11(8):536-41. doi: 10.1038/nchembio.1867
PMID: 26196764

Discovery and characterization of GSK2801, a selective chemical probe for the bromodomains BAZ2A and BAZ2B.
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 RK, Rogers CM, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH
J. Med. Chem.. 23.03.2015 . doi: 10.1021/acs.jmedchem.5b00209
PMID: 25799074

2014

Seeding collaborations to advance kinase science with the GSK Published Kinase Inhibitor Set (PKIS)
Drewry DH, Willson TM, Zuercher WJ.
Curr Top Med Chem. 2014 14(3):340-2. doi:
PMID: 24283969

2012

A public-private partnership to unlock the untargeted kinome.
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, Zuercher WJ
Nat. Chem. Biol.. 15.12.2012 9(1):3-6. doi: 10.1038/nchembio.1113
PMID: 23238671

2011

Too many roads not taken.
Edwards AM, Isserlin R, Bader GD, Frye SV, Willson TM, Yu FH
Nature. 10.02.2011 470(7333):163-5. doi: 10.1038/470163a
PMID: 21307913

2009

Open access chemical and clinical probes to support drug discovery.
Edwards AM, Bountra C, Kerr DJ, Willson TM
Nat. Chem. Biol.. 19.06.2009 5(7):436-40. doi: 10.1038/nchembio0709-436
PMID: 19536100

2002

6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
Pellicciari R, Fiorucci S, Camaioni E, Clerici C, Costantino G, Maloney PR, Morelli A, Parks DJ, Willson TM.
J Med Chem.. 08.15.2002 45(17):3569-72. doi:
PMID: 12166927

2001

A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport.
Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM.
Proc Natl Acad Sci U S A. . 04.24.2001 98(9):5306-11.. doi:
PMID: 11309497

2000

Identification of a chemical tool for the orphan nuclear receptor FXR
Maloney PR, Parks DJ, Haffner CD, Fivush AM, Chandra G, Plunket KD, Creech KL, Moore LB, Wilson JG, Lewis MC, Jones SA, Willson TM.
J Med Chem.. 08.10.2000 43(16):2971-4. doi:
PMID: 10956205

1999

Orphan nuclear receptors: shifting endocrinology into reverse.
Kliewer SA, Lehmann JM, Willson TM.
Science. 04.30.1999 284(5415):757-60. doi:
PMID: 10221899

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