Latest publications.
9 April 2026
Using targeted therapy [SRA737] to promote a pro-inflammatory tumour microenvironment and anti-tumour immune response in high grade serous ovarian cancer
View publication >
15 January 2023
A Phase I/II Trial of Oral SRA737 (a Chk1 Inhibitor) Given in Combination with Low-Dose Gemcitabine in Patients with Advanced Cancer.
View publication >
1 December 2019
Combination treatment of the oral CHK1 inhibitor, SRA737 and low dose gemcitabine, enhances the effect of PD-L1 blockade by modulating the immune microenvironment in small cell lung cancer.
View publication >
11 May 2016
Multi-parameter lead optimization to give an oral checkpoint kinase 1 (CHK1) inhibitor clinical candidate: (R)-5-((4-((morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
View publication >
18 April 2013
Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.
View publication >
17 March 2023
Immunotherapeutic effects of the TYK2 inhibitor SAR-20351 in syngeneic tumour models.
Publication:
Science Journal Daily
J Reader, T Mitchell et al
17 March 2023
Inhibition of TYK2 and JAK1 Ameliorates Imiquimod-Induced Psoriasis-like Dermatitis by Inhibiting IL-22 and the IL-23/IL-17 Axis.
Publication:
J Immunol. 2014
Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D’Andrea A
17 March 2023
A New Regulatory Switch in a JAK Protein Kinase.
Publication:
Proteins: Structure, Function & Bioinformatics (2011)
Tsui, V., Gibbons, P., Ultsch, M., Motara, K., Chang, C., Blair, W., Pulk, R., Stanley, M., Starovasnik, M., Willimas, D., Lamers, M., Leonard, P., Magnuson, S., Liang, J. & Eigenbrot, C
17 March 2023
A Phase I/II Trial of Oral SRA737 (a Chk1 Inhibitor) Given in Combination with Low-Dose Gemcitabine in Patients with Advanced Cancer.
Publication:
Clin Cancer Res, 15 November 2022
R Jones R Plummer, V Moreno, L Carter, D Roda, E Garralda, R Kristeleit, D Sarker, T Arkenau, P Roxburgh, HS Walter, S Blagden, A Anthoney, BJ Klencke, MM Kowalski & U Banerji
17 March 2023
A study of combinatorial growth inhibition, cell death and DNA damage repair caused by CHK1 inhibitor SRA737 and WEE1 inhibitor adavosertib in TP53 mutated cell line.
Publication:
AACR Annual Meeting 2021
A Stewart, L Pickard, A Hallsworth, S Sauvaigo, G Muggiolu, F Raynaud, U BANERJI
17 March 2023
CHK1 Inhibition Is Synthetically Lethal with Loss of B-Family DNA Polymerase Function in Human Lung and Colorectal Cancer Cells.
Publication:
Cancer Research (2020)
R Rogers, M Walton, D Cherry, I Collins, P Clarke, M & P Workman
17 March 2023
Combination treatment of the oral CHK1 inhibitor, SRA737 and low dose gemcitabine, enhances the effect of PD-L1 blockade by modulating the immune microenvironment in small cell lung cancer.
Publication:
J Thoracic Oncology 27 Aug 2019
T Sen et. al
17 March 2023
The CHK1 inhibitor SRA737 synergizes with PARP1 inhibitors to kill carcinoma cells
Publication:
Cancer Biology & Therapy 2018
L Booth, J Roberts, A Poklepovic & P Dent
17 March 2023
An orally bioavailable Chk1 inhibitor, CCT244747, sensitizes bladder and head and neck cancer cell lines to radiation.
Publication:
Radiother Oncol (2017)
R Patel, HE Barker, J Kyula, M McLaughlin, MT Dillon, U Schick, H Hafsi, A Thompson, V Khoo, K Harrington & S Zaidi
17 March 2023
DNA replication stress mediates APOBEC3 family mutagenesis in breast cancer.
Publication:
Genome Biology (2016)
N Kanu, MA Cerone, G Goh, L-P Zalmas, J Bartkova, M Dietzen, N McGranahan, R Rogers, EK Law, I Gromova, M Kschischo, MI Walton, OW Rossanese, J Bartek, RS Harris, S Venkatesan and C Swanton
17 March 2023
CHK1 inhibition radiosensitises head and neck cancers to paclitaxel-based chemoradiotherapy.
Publication:
Mol Cancer Therapeutics (2016)
HE Barker, R Patel, M McLaughlin, U Schick, S Zaidi, CM Nutting, KL Newbold, S Bhide, KJ Harrington
17 March 2023
Multi-parameter lead optimization to give an oral checkpoint kinase 1 (CHK1) inhibitor clinical candidate: (R)-5-((4-((morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737).
Publication:
J. Med. Chem. 2016
JD Osborne, TP Matthews, T McHardy, N Proisy, K-M J Cheung, M Lainchbury, N Brown, MI Walton, PD Eve, KJ Boxall, A Hayes, AT Henley, MR Valenti, AK De Haven Brandon, G Box, Y Jamin, SP Robinson, IM Westwood, RLM van Montfort, PM Leonard, MBAC Lamers, JC Reader, GW Aherne, FI Raynaud, SA Eccles, MD Garrett and I Collins
17 March 2023
The clinical development candidate CCT245737 is an orally active CHK1 inhibitor with preclinical activity in RAS mutant NSCLC and Eµ-MYC driven B-cell lymphoma.
Publication:
Oncotarget 2015
MI Walton, PD Eve, A Hayes, AT Henley, MR Valenti, AK De Haven Brandon, G Box, KJ Boxall, M Tall, K Swales, TP Matthews, T McHardy, M Lainchbury, J Osborne, JE Hunter, ND Perkins, GW Aherne, JC Reader, FI Raynaud, SA Eccles, I Collins and MD Garrett
17 March 2023
Targeted radiosensitization by the Chk1 inhibitor SAR-020106.
Publication:
International Journal of Radiation Oncology Biology Physics, 2013
GR Borst, M McLaughlin, JN Kyula, S Neijenhuis, A Khan, J Good … & KJ Harrington
17 March 2023
Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.
Publication:
Expert Opin Drug Discov. 2013
Matthews TP, Jones AM, Collins I
17 March 2023
CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs.
Publication:
Clinical Cancer Research 2012
Walton MI, Eve PD, Hayes A, Valenti MR, Alexis K, Box G, … & Garrett MD
17 March 2023
Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino) pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors.
Publication:
Journal of Medicinal Chemistry 2012
Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, … & Collins
17 March 2023
Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing.
Publication:
J. Med. Chem., 2011
JC Reader, TP Matthews, S Klair, K-MJ Cheung, J Scanlon, N Proisy, G Addison, J Ellard, N Piton, S Taylor, M Cherry, M Fisher, K Boxall, S Burns, MI Walton, IM Westwood, A Hayes, P Eve, M Valenti, A de Haven Brandon, G Box, RLM van Montfort, DH Williams, GW Aherne, FI Raynaud, SA Eccles, MD Garrett and Ian Collins
17 March 2023
CCT244747 is a novel, potent and selective inhibitor of CHK1 with oral efficacy both alone in neuroblastoma and in combination with genotoxic chemotherapeutic agents.
Publication:
AACR NCI EORTC “Molecular Targets and Cancer Therapeutics”, San Francisco, CA, Nov 12-16, 2011
MI. Walton, PE. Eve, A Hayes, MR. Valenti, AK. de Haven Brandon, G Box, A Hallsworth, EL. Smith, KJ. Boxall, M Lainchbury, TP. Matthews, Y Jamin, SP Robinson, GW Aherne, JC. Reader, L Chesler, FI. Raynaud, SE Eccles, I Collins, MD Garrett
17 March 2023
Structure-Guided Evolution of Potent and Selective CHK1 Inhibitors through Scaffold Morphing.
Publication:
AACR NCI EORTC “Molecular Targets and Cancer Therapeutics”, San Francisco, CA, Nov 12-16, 2011
TP Matthews, S Klair, K-MJ Cheung, J Scanlon, M Lainchbury, N Piton, M Fisher, M Cherry, K Boxall, MI. Walton, IM Westwood, A Hayes, P Eve, M Valenti, A de Haven Brandon, G Box, RLM van Montfort, DH. Williams, W Aherne, FI Raynaud, SA Eccles, MD Garrett, JC. Reader, I Collins
17 March 2023
Design and Evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as Inhibitors of Checkpoint and Other Kinases.
Publication:
Bioorg & Med Chem Lett (2010)
Matthews, T.P., McHardy, T., Klair, S., Boxhall, K., Fisher, M., Cherry, M., Allen, C.E., Addison, G.J., Ellard, J., Aherne, G.W., Westwood, I.M, van Montfort, R., Garrett, M.D., Reader, J.C. & Collins
17 March 2023
The Preclinical Pharmacology and Therapeutic Activity of the Novel CHK1 Inhibitor SAR-020106.
Publication:
Mol Cancer Ther (2010)
Walton, M.I., Eve, P.D., Hayes, A., Valenti, M., De Haven Brandon, A., Box, G., Boxall, K.J., Aherne, G.W., Eccles, S.A., Raynauld, F.I., Williams, D.H., Reader, J.C., Collins, I., Garrett, M.D
17 March 2023
Identification of Inhibitors of Checkpoint Kinase 1 through Template Screening.
Publication:
J Medicinal Chemistry (2009)
Matthews, T.P., Klair, S., Burns, S., Boxall, K., Cherry, M., Fisher, M., Westwood, I.M., Walton, M.I., McHardy, T., Kwai-Ming, J.C., Van Montfort, R., Williams, D., Aherne, G.W., Garrett, M.D., Reader, J and Collins, I
17 March 2023
Identification and Structure-guided Optimisation of Novel Inhibitors of Checkpoint Kinase 1 (Chk1) through Combined Biochemical and Crystallographic Screening.
Publication:
AACR Annual Meeting, San Diego, CA, Apr 12-16, 2008
Reader, J., Williams, D., Klair, S., Cherry, M., Fisher, M., Scanlon, J., Piton, N., Addison, G., Lamers, M., et al