Simon Taylor

发表

Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor

I. McLay, Shawn P. Williams, I. Uings, 2009, Proceedings of the National Academy of Sciences.

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.

Christophe Simon, P. Bamborough, R. Prinjha, 2014, Journal of medicinal chemistry.

Modification of the ultrafiltration technique to overcome solubility and non-specific binding challenges associated with the measurement of plasma protein binding of corticosteroids.

Simon Taylor, A. Harker, 2006, Journal of pharmaceutical and biomedical analysis.

Navigating CYP1A Induction and Arylhydrocarbon Receptor Agonism in Drug Discovery. A Case History with S1P1 Agonists.

E. Demont, J. Witherington, Simon Taylor, 2015, Journal of medicinal chemistry.

Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, Journal of medicinal chemistry.

Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.

P. Grandi, A. Michon, I. Wall, 2021, Journal of medicinal chemistry.

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

P. Grandi, A. Michon, G. Drewes, 2020, Science.

The utility of pharmacokinetic–pharmacodynamic modeling in the discovery and optimization of selective S1P1 agonists

S. Dowell, E. Demont, J. Witherington, 2012, Xenobiotica; the fate of foreign compounds in biological systems.

Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.

S. Dowell, E. Demont, J. Witherington, 2016, Journal of medicinal chemistry.

Aryl aminopyrazole benzamides as oral non-steroidal selective glucocorticoid receptor agonists.

H. T. Jones, James M. Woolven, I. McLay, 2009, Bioorganic & medicinal chemistry letters.

Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.

P. Grandi, I. Wall, James M. Woolven, 2021, Journal of medicinal chemistry.

Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

S. Dowell, K. Philpott, T. Heightman, 2011, Journal of medicinal chemistry.

The Optimisation of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.

P. Grandi, A. Michon, I. Wall, 2020, Journal of medicinal chemistry.

Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.

I. Wall, K. Philpott, T. Heightman, 2014, Journal of medicinal chemistry.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

Andrew J. Bannister, S. Robson, S. Knapp, 2015, Cancer research.

BET bromodomain inhibitors show anti‐papillomavirus activity in vitro and block CRPV wart growth in vivo

R. Prinjha, Kevin Lee, S. Brendle, 2018, Antiviral research.

Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.

R. Prinjha, P. Soden, C. Chung, 2021, Journal of medicinal chemistry.

Discovery of a Highly Selective BET BD2 Inhibitor from a DNA-Encoded Library Technology Screening Hit.

P. Grandi, I. Wall, R. Prinjha, 2021, Journal of medicinal chemistry.

Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate.

S. Dowell, E. Demont, J. Witherington, 2011, ACS medicinal chemistry letters.

Discovery of a potent series of non-steroidal non α-trifluoromethyl carbinol glucocorticoid receptor agonists with reduced lipophilicity.

I. McLay, Hawa Diallo, I. Uings, 2011, Bioorganic & medicinal chemistry letters.

GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.

P. Grandi, A. Michon, I. Wall, 2020, ACS Medicinal Chemistry Letters.

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype.

James M. Woolven, P. Bamborough, R. Prinjha, 2020, Journal of medicinal chemistry.

The Design and Synthesis of a Highly Selective and In Vivo Capable Inhibitor of the Second Bromodomain (BD2) of the Bromodomain and Extra Terminal Domain (BET) Family of Proteins.

P. Grandi, A. Michon, I. Wall, 2020, Journal of medicinal chemistry.

The Integrated Optimization of Safety and DMPK Properties Enabling Preclinical Development: A Case History with S1P1Agonists

Simon Taylor, 2018, Early Drug Development.

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

Andrew J. Bannister, S. Robson, S. Knapp, 2015, Cancer research.

Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins

P. Grandi, A. Michon, James M. Woolven, 2020, Journal of Medicinal Chemistry.