| Year |
Citation |
Score |
| 2023 |
Saint-Dizier F, Matthews TP, Gregson AM, Prevet H, McHardy T, Colombano G, Saville H, Rowlands M, Ewens C, McAndrew PC, Tomlin K, Guillotin D, Mak GW, Drosopoulos K, Poursaitidis I, ... ... Collins I, et al. Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes. Journal of Medicinal Chemistry. PMID 36749938 DOI: 10.1021/acs.jmedchem.2c01591 |
0.312 |
|
| 2022 |
Miller DSJ, Voell SA, Sosič I, Proj M, Rossanese OW, Schnakenburg G, Gütschow M, Collins I, Steinebach C. Encoding BRAF inhibitor functions in protein degraders. Rsc Medicinal Chemistry. 13: 731-736. PMID 35814929 DOI: 10.1039/d2md00064d |
0.31 |
|
| 2020 |
Pal A, Asad Y, Ruddle R, Henley AT, Swales K, Decordova S, Eccles SA, Collins I, Garrett MD, De Bono J, Banerji U, Raynaud FI. Metabolomic changes of the multi (-AGC-) kinase inhibitor AT13148 in cells, mice and patients are associated with NOS regulation. Metabolomics : Official Journal of the Metabolomic Society. 16: 50. PMID 32285223 DOI: 10.1007/S11306-020-01676-0 |
0.408 |
|
| 2020 |
Rogers RF, Walton MI, Cherry DL, Collins I, Clarke PA, Garrett MD, Workman P. CHK1 inhibition is synthetically lethal with loss of B-family DNA polymerase function in human lung and colorectal cancer cells. Cancer Research. PMID 32161100 DOI: 10.1158/0008-5472.Can-19-1372 |
0.362 |
|
| 2019 |
Pollock K, Liu M, Zaleska M, Meniconi M, Pfuhl M, Collins I, Guettler S. Fragment-based screening identifies molecules targeting the substrate-binding ankyrin repeat domains of tankyrase. Scientific Reports. 9: 19130. PMID 31836723 DOI: 10.1038/S41598-019-55240-5 |
0.37 |
|
| 2019 |
Prevet H, Collins I. Labelled chemical probes for demonstrating direct target engagement in living systems. Future Medicinal Chemistry. 11: 1195-1224. PMID 31280668 DOI: 10.4155/Fmc-2018-0370 |
0.311 |
|
| 2019 |
Chopra R, Sadok A, Collins I. A critical evaluation of the approaches to targeted protein degradation for drug discovery. Drug Discovery Today. Technologies. 31: 5-13. PMID 31200859 DOI: 10.1016/J.Ddtec.2019.02.002 |
0.333 |
|
| 2019 |
Zaleska M, Pollock K, Collins I, Guettler S, Pfuhl M. Solution NMR assignment of the ARC4 domain of human tankyrase 2. Biomolecular Nmr Assignments. PMID 30847846 DOI: 10.1007/S12104-019-09887-W |
0.306 |
|
| 2019 |
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 S, Jones AM, Saville H, ... ... Collins I, et al. Binding to an unusual inactive kinase conformation by highly selective inhibitors of inositol-requiring enzyme 1α kinase-endoribonuclease. Journal of Medicinal Chemistry. PMID 30779566 DOI: 10.1021/Acs.Jmedchem.8B01721 |
0.451 |
|
| 2018 |
Sharp SY, Chessum NE, Caldwell JJ, Powers MV, Pasqua AE, Wilding B, Collins I, Ozer B, Rowlands M, Stubbs M, Burke R, Montfort RLv, Cheeseman MD, Clarke PA, Workman P, et al. Abstract 2976: Confirmation of in-cell target engagement using the proteolysis targeting chimeras (PROTACs) against pirin Cancer Research. 78: 2976-2976. DOI: 10.1158/1538-7445.Am2018-2976 |
0.395 |
|
| 2017 |
Chessum NEA, Sharp SY, Caldwell JJ, Pasqua AE, Wilding B, Colombano G, Collins I, Ozer B, Richards M, Rowlands MG, Stubbs M, Burke R, McAndrew PC, Clarke PA, Workman P, et al. Demonstrating In-Cell Target Engagement using a Pirin Protein Degradation Probe (CCT367766). Journal of Medicinal Chemistry. PMID 29240418 DOI: 10.1021/Acs.Jmedchem.7B01406 |
0.329 |
|
| 2017 |
Collins I, Wang H, Caldwell JJ, Chopra R. Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway. The Biochemical Journal. 474: 1127-1147. PMID 28298557 DOI: 10.1042/Bcj20160762 |
0.367 |
|
| 2017 |
Rogers R, Walton MI, Clarke P, Collins I, Garrett MD, Workman P. Abstract 293: Screening the druggable genome for synthetic lethal interactions with the CHK1 inhibitor PNT737 Cancer Research. 77: 293-293. DOI: 10.1158/1538-7445.Am2017-293 |
0.383 |
|
| 2016 |
Rankin SS, Caldwell JJ, Cronin NB, van Montfort RL, Collins I. Synthesis of a Ribose-Incorporating Medium Ring Scaffold via a Challenging Ring-Closing Metathesis Reaction. European Journal of Organic Chemistry. 2016: 4496-4507. PMID 28042283 DOI: 10.1002/Ejoc.201600756 |
0.301 |
|
| 2016 |
Jones AM, Westwood IM, Osborne JD, Matthews TP, Cheeseman MD, Rowlands MG, Jeganathan F, Burke R, Lee D, Kadi N, Liu M, Richards M, McAndrew C, Yahya N, Dobson SE, ... ... Collins I, et al. A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms. Scientific Reports. 6: 34701. PMID 27708405 DOI: 10.1038/Srep34701 |
0.365 |
|
| 2016 |
Osborne JD, Matthews TP, McHardy T, Proisy N, Cheung KJ, Lainchbury M, Brown N, Walton MI, Eve PD, Boxall KJ, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, ... ... Collins I, et al. 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). Journal of Medicinal Chemistry. PMID 27167172 DOI: 10.1021/Acs.Jmedchem.5B01938 |
0.427 |
|
| 2016 |
Cheeseman MD, Westwood IM, Barbeau O, Rowlands MG, Dobson S, Jones AM, Jeganathan F, Burke R, Kadi N, Workman P, Collins I, van Montfort RL, Jones K. Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70. Journal of Medicinal Chemistry. PMID 27119979 DOI: 10.1021/Acs.Jmedchem.5B02001 |
0.375 |
|
| 2016 |
Myers SM, Collins I. Recent findings and future directions for interpolar mitotic kinesin inhibitors in cancer therapy. Future Medicinal Chemistry. PMID 26976726 DOI: 10.4155/Fmc.16.5 |
0.396 |
|
| 2016 |
Welford AJ, Caldwell JJ, Liu M, Richards M, Brown N, Lomas C, Tizzard GJ, Pitak MB, Coles SJ, Eccles SA, Raynaud FI, Collins I. Synthesis and Evaluation of a 2,11-Cembranoid-Inspired Library. Chemistry (Weinheim An Der Bergstrasse, Germany). PMID 26929153 DOI: 10.1002/Chem.201505093 |
0.347 |
|
| 2015 |
Walton MI, Eve PD, Hayes A, Henley AT, Valenti MR, De Haven Brandon AK, Box G, Boxall KJ, Tall M, Swales K, Matthews TP, McHardy T, Lainchbury M, Osborne J, Hunter JE, ... ... Collins I, et al. 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. Oncotarget. PMID 26295308 DOI: 10.18632/Oncotarget.4919 |
0.378 |
|
| 2015 |
Joshi A, Newbatt Y, McAndrew PC, Stubbs M, Burke R, Richards MW, Bhatia C, Caldwell JJ, McHardy T, Collins I, Bayliss R. Molecular mechanisms of human IRE1 activation through dimerization and ligand binding. Oncotarget. 6: 13019-35. PMID 25968568 DOI: 10.18632/Oncotarget.3864 |
0.378 |
|
| 2015 |
Sadok A, McCarthy A, Caldwell J, Collins I, Garrett MD, Yeo M, Hooper S, Sahai E, Kuemper S, Mardakheh FK, Marshall CJ. Rho kinase inhibitors block melanoma cell migration and inhibit metastasis. Cancer Research. 75: 2272-84. PMID 25840982 DOI: 10.1158/0008-5472.Can-14-2156 |
0.388 |
|
| 2015 |
Smith E, Collins I. Photoaffinity labeling in target- and binding-site identification. Future Medicinal Chemistry. 7: 159-83. PMID 25686004 DOI: 10.4155/Fmc.14.152 |
0.324 |
|
| 2015 |
Hensbergen AW, Mills VR, Collins I, Jones AM. An expedient synthesis of oxazepino and oxazocino quinazolines Tetrahedron Letters. 56: 6478-6483. DOI: 10.1016/J.Tetlet.2015.10.008 |
0.313 |
|
| 2014 |
Collins I, Jones AM. Diversity-oriented synthetic strategies applied to cancer chemical biology and drug discovery. Molecules (Basel, Switzerland). 19: 17221-55. PMID 25350364 DOI: 10.3390/Molecules191117221 |
0.34 |
|
| 2014 |
Palmer JT, Axford LC, Barker S, Bennett JM, Blair M, Collins I, Davies DT, Ford L, Gannon CT, Lancett P, Logan A, Lunniss CJ, Morton CJ, Offermann DA, Pitt GR, et al. Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors. Bioorganic & Medicinal Chemistry Letters. 24: 4215-22. PMID 25086682 DOI: 10.1016/J.Bmcl.2014.07.037 |
0.344 |
|
| 2014 |
Itzhak D, Bright M, McAndrew P, Mirza A, Newbatt Y, Strover J, Widya M, Thompson A, Morgan G, Collins I, Davies F. Multiple autophosphorylations significantly enhance the endoribonuclease activity of human inositol requiring enzyme 1α. Bmc Biochemistry. 15: 3. PMID 24524643 DOI: 10.1186/1471-2091-15-3 |
0.344 |
|
| 2014 |
Stokes NR, Baker N, Bennett JM, Chauhan PK, Collins I, Davies DT, Gavade M, Kumar D, Lancett P, Macdonald R, Macleod L, Mahajan A, Mitchell JP, Nayal N, Nayal YN, et al. Design, synthesis and structure-activity relationships of substituted oxazole-benzamide antibacterial inhibitors of FtsZ. Bioorganic & Medicinal Chemistry Letters. 24: 353-9. PMID 24287381 DOI: 10.1016/J.Bmcl.2013.11.002 |
0.445 |
|
| 2014 |
Allen CE, Welford AJ, Matthews TP, Caldwell JJ, Collins I. Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments Medchemcomm. 5: 180-185. DOI: 10.1039/C3Md00308F |
0.339 |
|
| 2013 |
Axford LC, Agarwal PK, Anderson KH, Andrau LN, Atherall J, Barker S, Bennett JM, Blair M, Collins I, Czaplewski LG, Davies DT, Gannon CT, Kumar D, Lancett P, Logan A, et al. Design, synthesis and biological evaluation of α-substituted isonipecotic acid benzothiazole analogues as potent bacterial type II topoisomerase inhibitors. Bioorganic & Medicinal Chemistry Letters. 23: 6598-603. PMID 24239017 DOI: 10.1016/J.Bmcl.2013.10.058 |
0.37 |
|
| 2013 |
Stokes NR, Thomaides-Brears HB, Barker S, Bennett JM, Berry J, Collins I, Czaplewski LG, Gamble V, Lancett P, Logan A, Lunniss CJ, Peasley H, Pommier S, Price D, Smee C, et al. Biological evaluation of benzothiazole ethyl urea inhibitors of bacterial type II topoisomerases. Antimicrobial Agents and Chemotherapy. 57: 5977-86. PMID 24041906 DOI: 10.1128/Aac.00719-13 |
0.366 |
|
| 2013 |
Allen CE, Chow CL, Caldwell JJ, Westwood IM, van Montfort RL, Collins I. Synthesis and evaluation of heteroaryl substituted diazaspirocycles as scaffolds to probe the ATP-binding site of protein kinases. Bioorganic & Medicinal Chemistry. 21: 5707-24. PMID 23920481 DOI: 10.1016/J.Bmc.2013.07.021 |
0.472 |
|
| 2013 |
Touchefeu Y, Khan AA, Borst G, Zaidi SH, McLaughlin M, Roulstone V, Mansfield D, Kyula J, Pencavel T, Karapanagiotou EM, Clayton J, Federspiel MJ, Russell SJ, Garrett M, Collins I, et al. Optimising measles virus-guided radiovirotherapy with external beam radiotherapy and specific checkpoint kinase 1 inhibition. Radiotherapy and Oncology : Journal of the European Society For Therapeutic Radiology and Oncology. 108: 24-31. PMID 23849174 DOI: 10.1016/J.Radonc.2013.05.036 |
0.307 |
|
| 2013 |
Silva-Santisteban MC, Westwood IM, Boxall K, Brown N, Peacock S, McAndrew C, Barrie E, Richards M, Mirza A, Oliver AW, Burke R, Hoelder S, Jones K, Aherne GW, Blagg J, ... Collins I, et al. Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2. Plos One. 8: e65689. PMID 23776527 DOI: 10.1371/Journal.Pone.0065689 |
0.43 |
|
| 2013 |
Matthews TP, Jones AM, Collins I. Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies. Expert Opinion On Drug Discovery. 8: 621-40. PMID 23594139 DOI: 10.1517/17460441.2013.788496 |
0.41 |
|
| 2013 |
Newbatt Y, Hardcastle A, McAndrew PC, Strover JA, Mirza A, Morgan GJ, Burke R, Davies FE, Collins I, van Montfort RL. Identification of autophosphorylation inhibitors of the inositol-requiring enzyme 1 alpha (IRE1α) by high-throughput screening using a DELFIA assay. Journal of Biomolecular Screening. 18: 298-308. PMID 23139381 DOI: 10.1177/1087057112465647 |
0.414 |
|
| 2013 |
Stokes NR, Baker N, Bennett JM, Berry J, Collins I, Czaplewski LG, Logan A, Macdonald R, Macleod L, Peasley H, Mitchell JP, Nayal N, Yadav A, Srivastava A, Haydon DJ. An improved small-molecule inhibitor of FtsZ with superior in vitro potency, drug-like properties, and in vivo efficacy. Antimicrobial Agents and Chemotherapy. 57: 317-25. PMID 23114779 DOI: 10.1128/Aac.01580-12 |
0.37 |
|
| 2013 |
Borst GR, McLaughlin M, Kyula JN, Neijenhuis S, Khan A, Good J, Zaidi S, Powell NG, Meier P, Collins I, Garrett MD, Verheij M, Harrington KJ. Targeted radiosensitization by the Chk1 inhibitor SAR-020106. International Journal of Radiation Oncology, Biology, Physics. 85: 1110-8. PMID 22981708 DOI: 10.1016/J.Ijrobp.2012.08.006 |
0.321 |
|
| 2012 |
Lainchbury M, Matthews TP, McHardy T, Boxall KJ, Walton MI, Eve PD, Hayes A, Valenti MR, de Haven Brandon AK, Box G, Aherne GW, Reader JC, Raynaud FI, Eccles SA, Garrett MD, ... Collins I, et al. Discovery of 3-alkoxyamino-5-(pyridin-2-ylamino)pyrazine-2-carbonitriles as selective, orally bioavailable CHK1 inhibitors. Journal of Medicinal Chemistry. 55: 10229-40. PMID 23082860 DOI: 10.1021/Jm3012933 |
0.451 |
|
| 2012 |
Walton MI, Eve PD, Hayes A, Valenti MR, De Haven Brandon AK, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, ... ... Collins I, et al. CCT244747 is a novel potent and selective CHK1 inhibitor with oral efficacy alone and in combination with genotoxic anticancer drugs. Clinical Cancer Research : An Official Journal of the American Association For Cancer Research. 18: 5650-61. PMID 22929806 DOI: 10.1158/1078-0432.Ccr-12-1322 |
0.404 |
|
| 2012 |
Mallinson J, Collins I. Macrocycles in new drug discovery. Future Medicinal Chemistry. 4: 1409-38. PMID 22857532 DOI: 10.4155/Fmc.12.93 |
0.322 |
|
| 2012 |
Sharp SY, Prodromou C, Cheung K, Roe M, Lynch C, Pearl L, Collins I, McDonald E, Jones K, Workman P. Abstract 4749: Insights into the molecular mechanism of HSP90 binding of methoxy-substituted resorcinylic isoxazole amide inhibitors reveal different isoform selectivity profiles Cancer Research. 72: 4749-4749. DOI: 10.1158/1538-7445.Am2012-4749 |
0.429 |
|
| 2012 |
Caldwell JJ, Veillard N, Collins I. Design and synthesis of 2(1H)-pyrazinones as inhibitors of protein kinases Tetrahedron. 68: 9713-9728. DOI: 10.1016/J.Tet.2012.09.039 |
0.451 |
|
| 2011 |
Reader JC, Matthews TP, Klair S, Cheung KM, Scanlon J, Proisy N, Addison G, Ellard J, Piton N, Taylor S, Cherry M, Fisher M, Boxall K, Burns S, Walton MI, ... ... Collins I, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. Journal of Medicinal Chemistry. 54: 8328-42. PMID 22111927 DOI: 10.1021/Jm2007326 |
0.46 |
|
| 2011 |
Lainchbury M, Collins I. Checkpoint kinase inhibitors: a patent review (2009 - 2010). Expert Opinion On Therapeutic Patents. 21: 1191-210. PMID 21599421 DOI: 10.1517/13543776.2011.586632 |
0.362 |
|
| 2011 |
Smyth LA, Matthews TP, Collins I. Design and evaluation of 3-aminopyrazolopyridinone kinase inhibitors inspired by the natural product indirubin. Bioorganic & Medicinal Chemistry. 19: 3569-78. PMID 21536449 DOI: 10.1016/J.Bmc.2011.03.069 |
0.45 |
|
| 2011 |
Garrett MD, Collins I. Anticancer therapy with checkpoint inhibitors: what, where and when? Trends in Pharmacological Sciences. 32: 308-16. PMID 21458083 DOI: 10.1016/J.Tips.2011.02.014 |
0.422 |
|
| 2011 |
Ali MM, Bagratuni T, Davenport EL, Nowak PR, Silva-Santisteban MC, Hardcastle A, McAndrews C, Rowlands MG, Morgan GJ, Aherne W, Collins I, Davies FE, Pearl LH. Structure of the Ire1 autophosphorylation complex and implications for the unfolded protein response. The Embo Journal. 30: 894-905. PMID 21317875 DOI: 10.1038/Emboj.2011.18 |
0.377 |
|
| 2011 |
Anderson VE, Walton MI, Eve PD, Boxall KJ, Antoni L, Caldwell JJ, Aherne W, Pearl LH, Oliver AW, Collins I, Garrett MD. CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Cancer Research. 71: 463-72. PMID 21239475 DOI: 10.1158/0008-5472.Can-10-1252 |
0.412 |
|
| 2011 |
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, ... ... Collins I, et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Molecular Cancer Therapeutics. 10: 360-71. PMID 21191045 DOI: 10.1158/1535-7163.Mct-10-0760 |
0.446 |
|
| 2011 |
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, et al. Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. Journal of Medicinal Chemistry. 54: 580-90. PMID 21186793 DOI: 10.1021/Jm101150B |
0.45 |
|
| 2011 |
Matthews TP, Klair S, Cheung KJ, Scanlon J, Lainchbury M, Piton N, Fisher M, Cherry M, Boxall K, Walton MI, Westwood IM, Hayes A, Eve P, Valenti M, Brandon AdH, ... ... Collins I, et al. Abstract A235: Structure-guided evolution of potent and selective oral inhibitors of CHK1 through scaffold morphing. Molecular Cancer Therapeutics. 10. DOI: 10.1158/1535-7163.Targ-11-A235 |
0.459 |
|
| 2011 |
Walton MI, Eve PE, Hayes A, Valenti MR, Brandon AKdH, Box G, Hallsworth A, Smith EL, Boxall KJ, Lainchbury M, Matthews TP, Jamin Y, Robinson SP, Aherne GW, Reader JC, ... ... Collins I, et al. Abstract A228: CCT244747 is a novel, potent and selective inhibitor of CHK1 with oral efficacy both alone in neuroblastoma and in combination with genotoxic chemotherapeutic agents. Molecular Cancer Therapeutics. 10. DOI: 10.1158/1535-7163.Targ-11-A228 |
0.437 |
|
| 2010 |
Whelligan DK, Solanki S, Taylor D, Thomson DW, Cheung KM, Boxall K, Mas-Droux C, Barillari C, Burns S, Grummitt CG, Collins I, van Montfort RL, Aherne GW, Bayliss R, Hoelder S. Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization. Journal of Medicinal Chemistry. 53: 7682-98. PMID 20936789 DOI: 10.1021/jm1008727 |
0.341 |
|
| 2010 |
Hayward DG, Newbatt Y, Pickard L, Byrne E, Mao G, Burns S, Sahota NK, Workman P, Collins I, Aherne W, Fry AM. Identification by high-throughput screening of viridin analogs as biochemical and cell-based inhibitors of the cell cycle-regulated nek2 kinase. Journal of Biomolecular Screening. 15: 918-27. PMID 20664067 DOI: 10.1177/1087057110376537 |
0.441 |
|
| 2010 |
Matthews TP, McHardy T, Klair S, Boxall K, Fisher M, Cherry M, Allen CE, Addison GJ, Ellard J, Aherne GW, Westwood IM, van Montfort R, Garrett MD, Reader JC, Collins I. Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases. Bioorganic & Medicinal Chemistry Letters. 20: 4045-9. PMID 20561787 DOI: 10.1016/J.Bmcl.2010.05.096 |
0.445 |
|
| 2010 |
Haydon DJ, Bennett JM, Brown D, Collins I, Galbraith G, Lancett P, Macdonald R, Stokes NR, Chauhan PK, Sutariya JK, Nayal N, Srivastava A, Beanland J, Hall R, Henstock V, et al. Creating an antibacterial with in vivo efficacy: synthesis and characterization of potent inhibitors of the bacterial cell division protein FtsZ with improved pharmaceutical properties. Journal of Medicinal Chemistry. 53: 3927-36. PMID 20426423 DOI: 10.1021/Jm9016366 |
0.434 |
|
| 2010 |
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, ... ... Collins I, et al. 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). Journal of Medicinal Chemistry. 53: 2239-49. PMID 20151677 DOI: 10.1021/Jm901788J |
0.444 |
|
| 2010 |
Walton MI, Eve PD, Hayes A, Valenti M, De Haven Brandon A, Box G, Boxall KJ, Aherne GW, Eccles SA, Raynaud FI, Williams DH, Reader JC, Collins I, Garrett MD. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Molecular Cancer Therapeutics. 9: 89-100. PMID 20053762 DOI: 10.1158/1535-7163.Mct-09-0938 |
0.389 |
|
| 2010 |
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. Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2. Bioorganic & Medicinal Chemistry. 18: 707-18. PMID 20022510 DOI: 10.1016/J.Bmc.2009.11.058 |
0.457 |
|
| 2010 |
Yap TA, Walton MI, Hunter L, Grimshaw K, Valenti M, Eve P, Heaton SP, Pickard L, Caldwell JJ, Thompson N, Bono JSd, Kaye SB, Eccles SA, Workman P, Collins I, et al. Abstract 4481: First report of preclinical pharmacology of two novel potent AKT inhibitors and development of pharmacodynamic (PD) biomarkers in tumor and surrogate tissue Cancer Research. 70: 4481-4481. DOI: 10.1158/1538-7445.Am10-4481 |
0.383 |
|
| 2010 |
Walton MI, Eve PD, Hayes A, Valenti M, Brandon ADH, Box G, Aherne GW, Eccles SA, Raynaud FI, Williams DH, Reader JC, Collins I, Garrett MD. Abstract 3518: Preclinical pharmacology of the novel, potent & selective CHK1 inhibitor SAR-020106 Cancer Research. 70: 3518-3518. DOI: 10.1158/1538-7445.Am10-3518 |
0.408 |
|
| 2010 |
Anderson VE, Eve PD, Walton MI, Caldwell JJ, Pearl LH, Oliver AW, Collins I, Garrett MD. Abstract 3503: CCT241533 is a novel, potent and selective inhibitor of CHK2 and potentiates the cellular effects of PARP inhibitors Cancer Research. 70: 3503-3503. DOI: 10.1158/1538-7445.Am10-3503 |
0.468 |
|
| 2010 |
Sharp SY, Jones K, Cheung K, Prodromou C, Roe SM, Pearl LH, Collins I, McDonald E, Workman P. Abstract 2677: A detailed analysis of protein binding and biological activity of methoxy-substituted resorcinylic isoxazole amide HSP90 inhibitors Cancer Research. 70: 2677-2677. DOI: 10.1158/1538-7445.Am10-2677 |
0.414 |
|
| 2010 |
Smyth LA, Matthews TP, Horton PN, Hursthouse MB, Collins I. Synthesis and reactivity of 3-amino-1H-pyrazolo[4,3-c]pyridin-4(5H)-ones: development of a novel kinase-focussed library Tetrahedron. 66: 2843-2854. DOI: 10.1016/J.Tet.2010.02.047 |
0.363 |
|
| 2010 |
Hilton S, Naud S, Caldwell JJ, Boxall K, Burns S, Anderson VE, Antoni L, Allen CE, Pearl LH, Oliver AW, Aherne GW, Garrett MD, Collins I. Corrigendum to "Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2" [Bioorg. Med. Chem. 18 (2010) 707] (DOI:10.1016/j.bmc.2009.11.058) Bioorganic and Medicinal Chemistry. 18: 4591. DOI: 10.1016/J.Bmc.2010.05.014 |
0.378 |
|
| 2009 |
Davies TG, Woodhead SJ, Collins I. Fragment-based discovery of inhibitors of protein kinase B. Current Topics in Medicinal Chemistry. 9: 1705-17. PMID 19929839 DOI: 10.2174/156802609790102419 |
0.457 |
|
| 2009 |
Matthews TP, Klair S, Burns S, Boxall K, Cherry M, Fisher M, Westwood IM, Walton MI, McHardy T, Cheung KM, Van Montfort R, Williams D, Aherne GW, Garrett MD, Reader J, ... Collins I, et al. Identification of inhibitors of checkpoint kinase 1 through template screening. Journal of Medicinal Chemistry. 52: 4810-9. PMID 19572549 DOI: 10.1021/Jm900314J |
0.416 |
|
| 2009 |
Smyth LA, Collins I. Measuring and interpreting the selectivity of protein kinase inhibitors. Journal of Chemical Biology. 2: 131-51. PMID 19568781 DOI: 10.1007/S12154-009-0023-9 |
0.435 |
|
| 2009 |
Keown LE, Collins I, Cooper LC, Harrison T, Madin A, Mistry J, Reilly M, Shaimi M, Welch CJ, Clarke EE, Lewis HD, Wrigley JD, Best JD, Murray F, Shearman MS. Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity. Journal of Medicinal Chemistry. 52: 3441-4. PMID 19432431 DOI: 10.1021/Jm900056P |
0.332 |
|
| 2009 |
Collins I. Targeted small-molecule inhibitors of protein kinase B as anticancer agents. Anti-Cancer Agents in Medicinal Chemistry. 9: 32-50. PMID 19149480 DOI: 10.2174/187152009787047734 |
0.457 |
|
| 2009 |
Czaplewski LG, Collins I, Boyd EA, Brown D, East SP, Gardiner M, Fletcher R, Haydon DJ, Henstock V, Ingram P, Jones C, Noula C, Kennison L, Rockley C, Rose V, et al. Antibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ Bioorganic and Medicinal Chemistry Letters. 19: 524-527. PMID 19064318 DOI: 10.1016/J.Bmcl.2008.11.021 |
0.378 |
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| 2009 |
Davies BR, Dudley P, Cosulich S, Luke R, Thompson N, Collins I, McHardy T, Garrett M, Ogilvie D. Abstract C208: CCT129254 (AT11854) is a well tolerated, orally bioavailable inhibitor of AKT/PKB with pharmacodynamic and antitumor activity in a range of xenograft models Molecular Cancer Therapeutics. 8. DOI: 10.1158/1535-7163.Targ-09-C208 |
0.38 |
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| 2009 |
Proisy N, Taylor S, Nelson A, Collins I. Rapid Synthesis of 3-Aminoisoquinoline-5-sulfonamides Using the Buchwald-Hartwig Reaction Synthesis. 2009: 561-566. DOI: 10.1055/S-0028-1083336 |
0.346 |
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| 2009 |
East SP, Bantry White C, Barker O, Barker S, Bennett J, Brown D, Andrew Boyd E, Brennan C, Chowdhury C, Collins I, Convers-Reignier E, Dymock BW, Fletcher R, Haydon DJ, Gardiner M, et al. Corrigendum to "DNA gyrase (GyrB)/topoisomerase IV (ParE) inhibitors: Synthesis and antibacterial activity" [Bioorg. Med. Chem. Lett. 19 (2009) 894] (DOI:10.1016/j.bmcl.2008.11.102) Bioorganic and Medicinal Chemistry Letters. 19: 2606. DOI: 10.1016/J.Bmcl.2008.11.120 |
0.352 |
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| 2008 |
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. Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration. Journal of Medicinal Chemistry. 51: 2147-57. PMID 18345609 DOI: 10.1021/Jm701437D |
0.456 |
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| 2008 |
Brough PA, Aherne W, Barril X, Borgognoni J, Boxall K, Cansfield JE, Cheung KM, Collins I, Davies NG, Drysdale MJ, Dymock B, Eccles SA, Finch H, Fink A, Hayes A, et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. Journal of Medicinal Chemistry. 51: 196-218. PMID 18020435 DOI: 10.1021/Jm701018H |
0.402 |
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| 2007 |
Antoni L, Sodha N, Collins I, Garrett MD. CHK2 kinase: cancer susceptibility and cancer therapy - two sides of the same coin? Nature Reviews. Cancer. 7: 925-36. PMID 18004398 DOI: 10.1038/Nrc2251 |
0.331 |
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| 2007 |
Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I. Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design. Journal of Medicinal Chemistry. 50: 2289-92. PMID 17451235 DOI: 10.1021/Jm0700924 |
0.439 |
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| 2007 |
Hardcastle A, Tomlin P, Norris C, Richards J, Cordwell M, Boxall K, Rowlands M, Jones K, Collins I, McDonald E, Workman P, Aherne W. A duplexed phenotypic screen for the simultaneous detection of inhibitors of the molecular chaperone heat shock protein 90 and modulators of cellular acetylation. Molecular Cancer Therapeutics. 6: 1112-22. PMID 17363504 DOI: 10.1158/1535-7163.Mct-06-0496 |
0.386 |
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| 2007 |
Davies TG, Verdonk ML, Graham B, Saalau-Bethell S, Hamlett CC, McHardy T, Collins I, Garrett MD, Workman P, Woodhead SJ, Jhoti H, Barford D. A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera. Journal of Molecular Biology. 367: 882-94. PMID 17275837 DOI: 10.1016/J.Jmb.2007.01.004 |
0.408 |
|
| 2006 |
Collins I, Workman P. New approaches to molecular cancer therapeutics. Nature Chemical Biology. 2: 689-700. PMID 17108987 DOI: 10.1038/Nchembio840 |
0.304 |
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| 2006 |
Honma M, Stubbs M, Collins I, Workman P, Aherne W, Watt FM. Identification of novel keratinocyte differentiation modulating compounds by high-throughput screening. Journal of Biomolecular Screening. 11: 977-84. PMID 17092913 DOI: 10.1177/1087057106292556 |
0.407 |
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| 2006 |
Burns S, Travers J, Collins I, Rowlands MG, Newbatt Y, Thompson N, Garrett MD, Workman P, Aherne W. Identification of small-molecule inhibitors of protein kinase B (PKB/AKT) in an AlphaScreenTM high-throughput screen. Journal of Biomolecular Screening. 11: 822-7. PMID 16902245 DOI: 10.1177/1087057106290992 |
0.425 |
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| 2006 |
Collins I, Caldwell J, Fonseca T, Donald A, Bavetsias V, Hunter LJ, Garrett MD, Rowlands MG, Aherne GW, Davies TG, Berdini V, Woodhead SJ, Davis D, Seavers LC, Wyatt PG, et al. Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B. Bioorganic & Medicinal Chemistry. 14: 1255-73. PMID 16249095 DOI: 10.1016/J.Bmc.2005.09.055 |
0.439 |
|
| 2006 |
Collins I, Workman P. Design and development of signal transduction inhibitors for cancer treatment: Experience and challenges with kinase targets Current Signal Transduction Therapy. 1: 13-23. DOI: 10.2174/157436206775269181 |
0.432 |
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| 2006 |
Large JM, Clarke M, Williamson DM, McDonald E, Collins I. Synthesis of trisubstituted pyrimidines by regioselective SNAr and Suzuki reactions of polyhalopyrimidines Synlett. 861-864. DOI: 10.1055/S-2006-939050 |
0.347 |
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| 2005 |
Collins I, Garrett MD. Targeting the cell division cycle in cancer: CDK and cell cycle checkpoint kinase inhibitors. Current Opinion in Pharmacology. 5: 366-73. PMID 15964238 DOI: 10.1016/J.Coph.2005.04.009 |
0.365 |
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| 2005 |
Chau NM, Rogers P, Aherne W, Carroll V, Collins I, McDonald E, Workman P, Ashcroft M. Identification of novel small molecule inhibitors of hypoxia-inducible factor-1 that differentially block hypoxia-inducible factor-1 activity and hypoxia-inducible factor-1α induction in response to hypoxic stress and growth factors Cancer Research. 65: 4918-4928. PMID 15930314 DOI: 10.1158/0008-5472.Can-04-4453 |
0.356 |
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| 2004 |
Thompson SA, Wheat L, Brown NA, Wingrove PB, Pillai GV, Whiting PJ, Adkins C, Woodward CH, Smith AJ, Simpson PB, Collins I, Wafford KA. Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptors. British Journal of Pharmacology. 142: 97-106. PMID 15100159 DOI: 10.1038/Sj.Bjp.0705689 |
0.318 |
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| 2004 |
Garrett MD, Hunter LJ, Fonseca TFD, Caldwell J, Rowlands MG, Hardcastle A, Collins I, McDonald E, Thompson N, Workman P. 322 Novel isoquinoline-5-sulfonamides as biochemical and cellular inhibitors of PKB/AKt Ejc Supplements. 2: 98. DOI: 10.1016/S1359-6349(04)80329-X |
0.417 |
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| 2004 |
Aherne W, Burns S, Travers J, Newbatt Y, Rowlands M, Barford D, Collins I, Thompson N, Garrett M, Workman P. 109 Identification of small molecule inhibitors of PKB/AKT in a high throughput screen Ejc Supplements. 2: 35-36. DOI: 10.1016/S1359-6349(04)80117-4 |
0.339 |
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| 2000 |
Collins I. Rapid analogue syntheses of heteroaromatic compounds Journal of the Chemical Society-Perkin Transactions 1. 1921-1940. DOI: 10.1039/B108580H |
0.329 |
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| 2000 |
Collins I, Castro JL, Street LJ. Rapid analogue synthesis of trisubstituted triazolo[4,3-b]pyridazines Tetrahedron Letters. 41: 781-784. DOI: 10.1016/S0040-4039(99)02153-X |
0.335 |
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| 1999 |
van Niel MB, Collins I, Beer MS, Broughton HB, Cheng SK, Goodacre SC, Heald A, Locker KL, MacLeod AM, Morrison D, Moyes CR, O'Connor D, Pike A, Rowley M, Russell MG, et al. Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles. Journal of Medicinal Chemistry. 42: 2087-104. PMID 10377215 DOI: 10.1021/Jm981133M |
0.346 |
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| 1999 |
Harrison JR, Holmes AB, Collins I. Enantioselective Synthesis of Alkyl-substituted Eight-membered Lactones by Claisen Rearrangement Synlett. 1999: 972-974. DOI: 10.1055/S-1999-3099 |
0.317 |
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| 1999 |
Collins I, Castro J. A convenient synthesis of highly substituted 2-pyridones Tetrahedron Letters. 40: 4069-4072. DOI: 10.1016/S0040-4039(99)00651-6 |
0.345 |
|
| 1998 |
Bourrain S, Collins I, Neduvelil JG, Rowley M, Leeson PD, Patel S, Emms F, Marwood R, Chapman KL, Fletcher AE, Showell GA. Substituted pyrazoles as novel selective ligands for the human dopamine D4 receptor Bioorganic and Medicinal Chemistry. 6: 1731-1743. PMID 9839003 DOI: 10.1016/S0968-0896(98)00134-5 |
0.312 |
|
| 1994 |
Rudge AJ, Collins I, Holmes AB, Baker R. Enantioselektive Synthese von Desoxynojirimycin Angewandte Chemie. 106: 2416-2418. DOI: 10.1002/Ange.19941062229 |
0.301 |
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