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Ken M Page

Explore the profile of Ken M Page including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 7
Citations 50
Followers 0
Related Specialties
Chemistry
Biochemistry
Pharmacology
Top 10 Co-Authors
Jonathan Bowyer
Caroline Smith
Andrew D Morley
Philip A MacFaul
Stephan Krapp
Jeffrey J Morris
Stefan Steinbacher
Thomas M McGuire
Julian A Hudson
Lyn Rosenbrier Ribeiro
Published In
J Med Chem
Bioorg Med Chem Lett
Mol Pharm
J Comput Aided Mol Des
Affiliations
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Recent Articles
1.
Validation of Early Human Dose Prediction: A Key Metric for Compound Progression in Drug Discovery
Page K
Mol Pharm . 2015 Dec; 13(2):609-20. PMID: 26696327
Human dose prediction is increasingly recognized as an important parameter in Drug Discovery. Validation of a method using only in vitro and predicted parameters incorporated into a PK model was...
2.
Time dependent analysis of assay comparability: a novel approach to understand intra- and inter-site variability over time
Winiwarter S, Middleton B, Jones B, Courtney P, Lindmark B, Page K, et al.
J Comput Aided Mol Des . 2015 Feb; 29(9):795-807. PMID: 25697964
We demonstrate here a novel use of statistical tools to study intra- and inter-site assay variability of five early drug metabolism and pharmacokinetics in vitro assays over time. Firstly, a...
3.
Hydantoin based inhibitors of MMP13--discovery of AZD6605
De Savi C, Waterson D, Pape A, Lamont S, Hadley E, Mills M, et al.
Bioorg Med Chem Lett . 2013 Jul; 23(16):4705-12. PMID: 23810497
Piperidine ether and aryl piperazine hydantoins are reported as potent inhibitors of MMP13. A medicinal chemistry campaign focused on replacing the reverse hydroxamate zinc binding group associated with historical inhibitors...
4.
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors
Crawford J, Kenny P, Bowyer J, Cook C, Finlayson J, Heyes C, et al.
J Med Chem . 2012 Sep; 55(20):8827-37. PMID: 22984809
Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and pharmacokinetics. Compounds with a 3,4-(CH₃O)₂Ph motif, such as 31, were...
5.
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition
Dossetter A, Bowyer J, Cook C, Crawford J, Finlayson J, Heron N, et al.
Bioorg Med Chem Lett . 2012 Aug; 22(17):5563-8. PMID: 22858142
The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bioavailability in dog is described. The compound was used to demonstrate target engagement and...
6.
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis
Dossetter A, Beeley H, Bowyer J, Cook C, Crawford J, Finlayson J, et al.
J Med Chem . 2012 Jun; 55(14):6363-74. PMID: 22742641
Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to microsomes. Synthesis of compounds with reduced...
7.
Aminoimidazolylmethyluracil analogues as potent inhibitors of thymidine phosphorylase and their bioreductive nitroimidazolyl prodrugs
Reigan P, Edwards P, Gbaj A, Cole C, Barry S, Page K, et al.
J Med Chem . 2005 Jan; 48(2):392-402. PMID: 15658853
Thymidine phosphorylase (TP) is an important target enzyme for cancer chemotherapy because it is expressed at high levels in the hypoxic regions of many tumors and inhibitors of TP have...