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Items: 20


Binding to an Unusual Inactive Kinase Conformation by Highly Selective Inhibitors of Inositol-Requiring Enzyme 1α Kinase-Endoribonuclease.

Colombano G, Caldwell JJ, Matthews TP, Bhatia C, Joshi A, McHardy T, Mok NY, Newbatt Y, Pickard L, Strover J, Hedayat S, Walton MI, Myers SM, Jones AM, Saville H, McAndrew C, Burke R, Eccles SA, Davies FE, Bayliss R, Collins I.

J Med Chem. 2019 Mar 14;62(5):2447-2465. doi: 10.1021/acs.jmedchem.8b01721. Epub 2019 Mar 5.


Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).

Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands M, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, Cheeseman MD, Jones K.

J Med Chem. 2018 Feb 8;61(3):918-933. doi: 10.1021/acs.jmedchem.7b01406. Epub 2018 Jan 5.


Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway.

Collins I, Wang H, Caldwell JJ, Chopra R.

Biochem J. 2017 Mar 15;474(7):1127-1147. doi: 10.1042/BCJ20160762. Review.


Synthesis of a Ribose-Incorporating Medium Ring Scaffold via a Challenging Ring-Closing Metathesis Reaction.

Rankin SS, Caldwell JJ, Cronin NB, van Montfort RL, Collins I.

European J Org Chem. 2016 Sep;2016(26):4496-4507. doi: 10.1002/ejoc.201600756. Epub 2016 Aug 15.


Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library.

Welford AJ, Caldwell JJ, Liu M, Richards M, Brown N, Lomas C, Tizzard GJ, Pitak MB, Coles SJ, Eccles SA, Raynaud FI, Collins I.

Chemistry. 2016 Apr 11;22(16):5657-64. doi: 10.1002/chem.201505093. Epub 2016 Mar 1.


Molecular mechanisms of human IRE1 activation through dimerization and ligand binding.

Joshi A, Newbatt Y, McAndrew PC, Stubbs M, Burke R, Richards MW, Bhatia C, Caldwell JJ, McHardy T, Collins I, Bayliss R.

Oncotarget. 2015 May 30;6(15):13019-35.


Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases.

Allen CE, Chow CL, Caldwell JJ, Westwood IM, van Montfort RL, Collins I.

Bioorg Med Chem. 2013 Sep 15;21(18):5707-24. doi: 10.1016/j.bmc.2013.07.021. Epub 2013 Jul 19.


CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.

Anderson VE, Walton MI, Eve PD, Boxall KJ, Antoni L, Caldwell JJ, Aherne W, Pearl LH, Oliver AW, Collins I, Garrett MD.

Cancer Res. 2011 Jan 15;71(2):463-72. doi: 10.1158/0008-5472.CAN-10-1252.


Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930.

Yap TA, Walton MI, Hunter LJ, Valenti M, de Haven Brandon A, Eve PD, Ruddle R, Heaton SP, Henley A, Pickard L, Vijayaraghavan G, Caldwell JJ, Thompson NT, Aherne W, Raynaud FI, Eccles SA, Workman P, Collins I, Garrett MD.

Mol Cancer Ther. 2011 Feb;10(2):360-71. doi: 10.1158/1535-7163.MCT-10-0760. Epub 2010 Dec 29.


Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2.

Caldwell JJ, Welsh EJ, Matijssen C, Anderson VE, Antoni L, Boxall K, Urban F, Hayes A, Raynaud FI, Rigoreau LJ, Raynham T, Aherne GW, Pearl LH, Oliver AW, Garrett MD, Collins I.

J Med Chem. 2011 Jan 27;54(2):580-90. doi: 10.1021/jm101150b. Epub 2010 Dec 27.


Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).

McHardy T, Caldwell JJ, Cheung KM, Hunter LJ, Taylor K, Rowlands M, Ruddle R, Henley A, de Haven Brandon A, Valenti M, Davies TG, Fazal L, Seavers L, Raynaud FI, Eccles SA, Aherne GW, Garrett MD, Collins I.

J Med Chem. 2010 Mar 11;53(5):2239-49. doi: 10.1021/jm901788j.


Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2.

Hilton S, Naud S, Caldwell JJ, Boxall K, Burns S, Anderson VE, Antoni L, Allen CE, Pearl LH, Oliver AW, Wynne Aherne G, Garrett MD, Collins I.

Bioorg Med Chem. 2010 Jan 15;18(2):707-18. doi: 10.1016/j.bmc.2009.11.058. Epub 2009 Dec 6. Erratum in: Bioorg Med Chem. 2010 Jun 15;18(12):4591.


Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration.

Caldwell JJ, Davies TG, Donald A, McHardy T, Rowlands MG, Aherne GW, Hunter LK, Taylor K, Ruddle R, Raynaud FI, Verdonk M, Workman P, Garrett MD, Collins I.

J Med Chem. 2008 Apr 10;51(7):2147-57. doi: 10.1021/jm701437d. Epub 2008 Mar 18.


Sulfone-mediated total synthesis of (+/-)-lepadiformine.

Caldwell JJ, Craig D.

Angew Chem Int Ed Engl. 2007;46(15):2631-4. No abstract available.


HST spectroscopic observations of Jupiter after the collision of comet Shoemaker-Levy 9.

Noll KS, McGrath MA, Trafton LM, Atreya SK, Caldwell JJ, Weaver HA, Yelle RV, Barnet C, Edgington S.

Science. 1995 Mar 3;267(5202):1307-13.


Alternate gram staining technique using a fluorescent lectin.

Sizemore RK, Caldwell JJ, Kendrick AS.

Appl Environ Microbiol. 1990 Jul;56(7):2245-7.


Paralysis of the Facial Nerve.

Caldwell JJ.

Am J Dent Sci. 1881 Jun;15(2):65-70. No abstract available.


Unity of Force Electricity Its Superlative Velocity.

Caldwell JJ.

Am J Dent Sci. 1877 Dec;11(8):348-353. No abstract available.


The Action of the Nervous System.

Caldwell JJ.

Am J Dent Sci. 1877 Nov;11(7):289-298. No abstract available.

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