Research Topics
| Brian J StockmanSummaryAffiliation: Pfizer Global Research and Development Country: USA Publications
| Collaborators
|
Detail Information
Publications
Identification of allosteric PIF-pocket ligands for PDK1 using NMR-based fragment screening and 1H-15N TROSY experimentsBrian J Stockman
Pfizer Global Research and Development, Groton, CT 06340, USA
Chem Biol Drug Des 73:179-88. 2009..Caliper assay data and 19F NMR assay data on the PDK1 Interacting Fragment pocket fragments and structurally related compounds identified them as potential allosteric activators of PDK1 function...
2-Fluoro-ATP as a versatile tool for 19F NMR-based activity screeningBrian J Stockman
Pfizer Global Research and Development, Groton, Connecticut 06340, USA
J Am Chem Soc 130:5870-1. 2008....
A nuclear magnetic resonance-based functional assay for nicotinamide adenine dinucleotide synthetaseBrian J Stockman
Pfizer Global Research and Development, Groton, Connecticut 06340, USA
J Biomol Screen 12:457-63. 2007..The assay has been used to screen fragment libraries for NadE inhibitors...
Resonance assignments for stromelysin complexed with a beta-sulfonyl hydroxamate inhibitorParag V Sahasrabudhe
Exploratory Medicinal Sciences, Pfizer Global Research and Development, MS 8118A 2024, Eastern Point Road, Groton, CT 06340, USA
Biomol NMR Assign 3:183-6. 2009..Almost 70% of assignable backbone and side-chain atoms were assigned in this highly dynamic protein...
Physical methods to determine the binding mode of putative ligands for hepatitis C virus NS3 helicaseRonald W Sarver
Structural, Analytical and Medicinal Chemistry, 301 Henrietta Street, Kalamazoo, MI 49001, USA
Anal Biochem 309:186-95. 2002..A combination of physical methods was required to discern the mode of action of compounds identified by HTS and remove undesirable lead templates from further consideration...
Multi-selective one dimensional proton NMR experiments for rapid screening and binding affinity measurementsClaudio Dalvit
Chemistry Department, Pharmacia, Viale Pasteur 10, 20014 Nerviano, MI, Italy
Comb Chem High Throughput Screen 6:445-53. 2003..For a simple competition binding mechanism, the rapidly-derived NMR binding constants are in good agreement with the values derived from full-titration ITC and fluorescence spectroscopy measurements...
Fluorine-NMR experiments for high-throughput screening: theoretical aspects, practical considerations, and range of applicabilityClaudio Dalvit
Chemistry Department, Pharmacia, Viale Pasteur 10, 20014 Nerviano MI, Italy
J Am Chem Soc 125:7696-703. 2003..The experimental conditions together with the detection limits and binding constant measurements are investigated using human serum albumin as the target...
Competition binding experiments for rapidly ranking lead molecules for their binding affinity to human serum albuminClaudio Dalvit
Chemistry Department, Pharmacia, Viale Pasteur 10, Nerviano MI, 20014, Italy
Comb Chem High Throughput Screen 5:645-50. 2002..This review will summarize some of the NMR-based efforts towards developing universal, rapid, accurate, and site-specific assays for estimating protein binding...
Fluorine-NMR competition binding experiments for high-throughput screening of large compound mixturesClaudio Dalvit
Chemistry Department, Pharmacia, Viale Pasteur 10, Nerviano MI, 20014, Italy
Comb Chem High Throughput Screen 5:605-11. 2002..Finally, a novel approach for HTS using a reference molecule in combination with a control molecule is presented...
High-throughput NMR-based screening with competition binding experimentsClaudio Dalvit
Chemistry Department, Pharmacia, Viale Pasteur 10, 20014 Nerviano MI, Milan, Italy
J Am Chem Soc 124:7702-9. 2002..With this approach it is possible to screen thousands of compounds in a short period of time against protein or DNA and RNA fragments. The methodology can also be applied for screening plant and fungi extracts...
1H nuclear magnetic resonance study of oxazolidinone binding to bacterial ribosomesCasey Chun Zhou
Pharmacia Corporation, Kalamazoo, Michigan 49001, USA
Antimicrob Agents Chemother 46:625-9. 2002....
