Andrew D Morley
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Explore the profile of Andrew D Morley including associated specialties, affiliations and a list of published articles.
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15
Citations
152
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Recent Articles
1.
Morley A, Pugliese A, Birchall K, Bower J, Brennan P, Brown N, et al.
Drug Discov Today
. 2013 Aug;
18(23-24):1221-7.
PMID: 23906694
The identification of high-quality hits during the early phases of drug discovery is essential if projects are to have a realistic chance of progressing into clinical development and delivering marketed...
2.
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...
3.
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...
4.
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...
5.
De Savi C, Morley A, Nash I, Karoutchi G, Page K, Ting A, et al.
Bioorg Med Chem Lett
. 2011 Dec;
22(1):271-7.
PMID: 22153941
Directed screening has identified a novel series of non-zinc binding MMP13 inhibitors that possess good levels of activity whilst demonstrating excellent selectivity over related MMPs. A lead optimisation campaign has...
6.
Morley A, King S, Roberts B, Lever S, Teobald B, Fisher A, et al.
Bioorg Med Chem Lett
. 2011 Nov;
22(1):532-6.
PMID: 22094028
Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with...
7.
Morley A, Cook A, King S, Roberts B, Lever S, Weaver R, et al.
Bioorg Med Chem Lett
. 2011 Sep;
21(21):6456-60.
PMID: 21955939
A series of pyrazole inhibitors of the human FPR1 receptor have been identified from high throughput screening. The compounds demonstrate potent inhibition in human neutrophils and attractive physicochemical and in...
8.
De Savi C, Morley A, Ting A, Nash I, Karabelas K, Wood C, et al.
Bioorg Med Chem Lett
. 2011 Jun;
21(14):4215-9.
PMID: 21669521
Directed screening has identified a novel series of MMP13 inhibitors that possess good levels of activity whilst possessing excellent selectivity over related MMPs. The binding mode of the series has...
9.
Bethel P, Gerhardt S, Jones E, Kenny P, Karoutchi G, Morley A, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4622-5.
PMID: 19616430
A number of molecular recognition features have been exploited in structure-based design of selective Cathepsin inhibitors.
10.
Elliot D, Henshaw E, MacFaul P, Morley A, Newham P, Oldham K, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4832-5.
PMID: 19574045
A novel approach to inhibition of the alphavbeta3 integrin is described, which uses compounds designed to generate nM potency without using the arginine binding site.