Gregory E Peckham
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Explore the profile of Gregory E Peckham including associated specialties, affiliations and a list of published articles.
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8
Citations
23
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Recent Articles
1.
Santiago B, Eisennagel S, Peckham G, Liebhardt A, Alburn C, Roethke T, et al.
Bioanalysis
. 2023 Mar;
15(3):177-191.
PMID: 36917553
As the desire for a shortened design/make/test/learn cycle increases in early drug discovery, the pressure to rapidly deliver drug metabolism pharmacokinetic data continues to rise. From a bioanalytical standpoint, assays...
2.
Schulte C, Deaton D, Diaz E, Do Y, Gampe R, Guss J, et al.
Bioorg Med Chem Lett
. 2021 May;
47:128113.
PMID: 33991628
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally...
3.
Cadilla R, Deaton D, Do Y, Elkins P, Ennulat D, Guss J, et al.
Bioorg Med Chem
. 2020 Oct;
28(23):115791.
PMID: 33059303
GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC = 9.9 nM) as part of a fragment-based drug discovery collaboration with Astex Pharmaceuticals....
4.
Deaton D, Do Y, Holt J, Jeune M, Kramer H, Larkin A, et al.
Bioorg Med Chem
. 2019 Mar;
27(8):1456-1478.
PMID: 30858025
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits...
5.
Katamreddy S, Carpenter A, Ammala C, Boros E, Brashear R, Briscoe C, et al.
J Med Chem
. 2012 Dec;
55(24):10972-94.
PMID: 23214471
GPR119 is a 7-transmembrane receptor that is expressed in the enteroendocrine cells in the intestine and in the islets of Langerhans in the pancreas. Indolines and 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines were discovered as...
6.
Cheung M, Harris P, Badiang J, Peckham G, Chamberlain S, Alberti M, et al.
Bioorg Med Chem Lett
. 2008 Sep;
18(20):5428-30.
PMID: 18818075
A series of pyrazolo[1,5-a]pyridine derivatives was designed and synthesized as novel potent p38 kinase inhibitors. Our approaches towards improving in vitro metabolism and in vivo pharmacokinetic properties of the series...
7.
Carpenter A, Al-Barazanji K, Barvian K, Bishop M, S Britt C, Cooper J, et al.
Bioorg Med Chem Lett
. 2006 Aug;
16(19):4994-5000.
PMID: 16904318
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are...
8.
Stevens K, Jung D, Alberti M, Badiang J, Peckham G, Veal J, et al.
Org Lett
. 2005 Oct;
7(21):4753-6.
PMID: 16209527
[reaction: see text] A convergent synthesis of substituted pyrazolo[1,5-a]pyridines has been achieved either via a regioselective [3 + 2] cycloaddition of N-aminopyridines with alkynes or by thermal cyclization of disubstituted...