Christopher N Johnson

Summary

Affiliation: GlaxoSmithKline Research and Development
Country: USA

Publications

  1. ncbi request reprint 3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity
    Peter J Atkinson
    Psychiatry Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:737-41. 2005
  2. ncbi request reprint Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands
    Simon E Ward
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 17:5214-7. 2007
  3. ncbi request reprint 5-HT6 receptor antagonists: prospects for the treatment of cognitive disorders including dementia
    Christopher N Johnson
    Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline plc, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK
    Curr Opin Drug Discov Devel 11:642-54. 2008
  4. ncbi request reprint Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
    David R Witty
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 16:4872-8. 2006
  5. ncbi request reprint Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists
    Mahmood Ahmed
    Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:4867-71. 2005
  6. ncbi request reprint SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849
    David R Witty
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 16:4865-71. 2006
  7. doi request reprint Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists
    Giancarlo Trani
    Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 18:5698-700. 2008
  8. ncbi request reprint SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue
    Claire Scott
    Psychiatry and Neurology and GI Centres of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW and Via Fleming 4, Verona, Italy
    Eur J Pharmacol 536:54-61. 2006
  9. doi request reprint Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate
    Susan M Westaway
    Immuno Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts, SG1 2NY, UK
    J Med Chem 52:1180-9. 2009
  10. doi request reprint The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor
    Susan M Westaway
    Immuno Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK
    Bioorg Med Chem Lett 18:6429-36. 2008

Collaborators

Detail Information

Publications13

  1. ncbi request reprint 3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity
    Peter J Atkinson
    Psychiatry Center of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:737-41. 2005
    ..2). This compound also had good oral bioavailability and brain penetration in the rat...
  2. ncbi request reprint Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands
    Simon E Ward
    Psychiatry Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 17:5214-7. 2007
    ..Furthermore, they have improved pharmacokinetic profiles and CNS penetration...
  3. ncbi request reprint 5-HT6 receptor antagonists: prospects for the treatment of cognitive disorders including dementia
    Christopher N Johnson
    Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline plc, New Frontiers Science Park, Third Avenue, Harlow, Essex, UK
    Curr Opin Drug Discov Devel 11:642-54. 2008
    ....
  4. ncbi request reprint Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849
    David R Witty
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 16:4872-8. 2006
    ....
  5. ncbi request reprint Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists
    Mahmood Ahmed
    Neurology and GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 15:4867-71. 2005
    ..5-Chloroindole 699929 combined high 5-HT6 receptor affinity with excellent brain penetration and also had good oral bioavailability in both rat and dog...
  6. ncbi request reprint SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): discovery of antagonist SB-568849
    David R Witty
    GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 16:4865-71. 2006
    ..This compound proved to be an antagonist with stability in vivo, an acceptable brain-blood ratio and oral bioavailability...
  7. doi request reprint Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists
    Giancarlo Trani
    Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK
    Bioorg Med Chem Lett 18:5698-700. 2008
    ....
  8. ncbi request reprint SB-649915, a novel, potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue
    Claire Scott
    Psychiatry and Neurology and GI Centres of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW and Via Fleming 4, Verona, Italy
    Eur J Pharmacol 536:54-61. 2006
    ..9 and 9.7, respectively. In summary, SB-649915 is a novel, potent 5-HT1A/1B autoreceptor antagonist and 5-HT re-uptake inhibitor in native tissue systems and represents a novel mechanism that could offer fast acting antidepressant action...
  9. doi request reprint Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate
    Susan M Westaway
    Immuno Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts, SG1 2NY, UK
    J Med Chem 52:1180-9. 2009
    ....
  10. doi request reprint The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor
    Susan M Westaway
    Immuno Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK
    Bioorg Med Chem Lett 18:6429-36. 2008
    ..Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent...
  11. doi request reprint Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain
    James W Myatt
    Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, UK
    Bioorg Med Chem Lett 20:4683-8. 2010
    ..An in-house P-gp prediction programme and the MetaSite software package were used to help solve the specific problems of high P-gp efflux and high in vivo clearance...
  12. doi request reprint BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells
    Paul Beswick
    Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline R and D, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK
    Bioorg Med Chem Lett 18:1022-6. 2008
    ..Optimization of the non-prime side of our inhibitors and introduction of a 6-membered sultam substituent binding to Asn-294 as well as a fluorine in the C-2 position led to derivatives with nanomolar potency in cell-based assays...
  13. ncbi request reprint Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist
    Gregor J Macdonald
    GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK
    J Med Chem 46:4952-64. 2003
    ....