Patrick J Brassil
Overview
Explore the profile of Patrick J Brassil including associated specialties, affiliations and a list of published articles.
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Articles
9
Citations
292
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0
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Recent Articles
1.
Bolleddula J, DeMent K, Driscoll J, Worboys P, Brassil P, Bourdet D
Drug Metab Rev
. 2014 Jun;
46(3):379-419.
PMID: 24909234
Aliphatic nitrogen heterocycles such as piperazine, piperidine, pyrrolidine, morpholine, aziridine, azetidine, and azepane are well known building blocks in drug design and important core structures in approved drug therapies. These...
2.
Theoclitou M, Aquila B, Block M, Brassil P, Castriotta L, Code E, et al.
J Med Chem
. 2011 Sep;
54(19):6734-50.
PMID: 21899292
Structure-activity relationship analysis identified (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), from a series of novel kinesin spindle protein (KSP) inhibitors, as exhibiting both excellent biochemical potency and pharmaceutical properties suitable for clinical development. The...
3.
Goteti K, Garner C, Utley L, Dai J, Ashwell S, Moustakas D, et al.
Cancer Chemother Pharmacol
. 2009 Oct;
66(2):245-54.
PMID: 19841922
Purpose: Pharmacokinetic/pharmacodynamic (PK/PD) models have been shown to be useful in predicting tumor growth rates in mouse xenografts. We applied novel PK/PD models to the published anticancer combination therapies of...
4.
Goteti K, Brassil P, Good S, Garner C
J Clin Pharmacol
. 2008 Jun;
48(10):1226-36.
PMID: 18559487
A multiexponential allometry (MA) method was developed to predict human drug clearance from preclinical data. Separate data sets containing clearances from human and preclinical species were chosen for the study....
5.
Janetka J, Almeida L, Ashwell S, Brassil P, Daly K, Deng C, et al.
Bioorg Med Chem Lett
. 2008 Jun;
18(14):4242-8.
PMID: 18547806
Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors...
6.
Harper T, Brassil P
AAPS J
. 2008 May;
10(1):200-7.
PMID: 18446520
Reaction phenotyping studies to identify specific enzymes involved in the metabolism of drug candidates are increasingly important in drug discovery efforts. Experimental approaches used for CYP reaction phenotyping include incubations...
7.
Belema M, Bunker A, Nguyen V, Beaulieu F, Ouellet C, Qiu Y, et al.
Bioorg Med Chem Lett
. 2007 Jun;
17(15):4284-9.
PMID: 17540562
The identification of a potent series of IKK-beta selective inhibitors based on an imidazothienopyrazine template and the oral efficacy of one such analog (22j) in the LPS-induced TNF-alpha release mouse...
8.
Taber M, Wright R, Molski T, Clarke W, Brassil P, Denhart D, et al.
Pharmacol Biochem Behav
. 2005 Mar;
80(3):521-8.
PMID: 15740795
BMS-505130 is a potent and selective serotonin transport inhibitor; K(i) for binding to the serotonin transporter = 0.18 nM (K(i) values for binding to the norepinephrine and dopamine transporters =...
9.
Burke J, Pattoli M, Gregor K, Brassil P, MacMaster J, McIntyre K, et al.
J Biol Chem
. 2002 Oct;
278(3):1450-6.
PMID: 12403772
The signal-inducible phosphorylation of serines 32 and 36 of I kappa B alpha is critical in regulating the subsequent ubiquitination and proteolysis of I kappa B alpha, which then releases...