Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase

2017-11-07T14:23:46+00:00

71) Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase Richard A. Norman, Anne-Kathrin Schott, David M. Andrews, Jason Breed, Kevin M. Foote, Andrew P. Garner, Derek Ogg, Jonathon P. Orme, Jennifer H. Pink, Karen Roberts, David A. Rudge, Andrew P. Thomas, and Andrew G. Leach J. Med. Chem.,

Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase2017-11-07T14:23:46+00:00

Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation

2017-11-07T14:23:06+00:00

72) Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation Scott, J. S.; Birch, A. M.; Brocklehurst, K. J.; Broo, A.; Brown, H. S.; Butlin, R. J.; Clarke, D. S.; Davidsson, O.; Ertan, A.; Goldberg, K.; Groombridge,

Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation2017-11-07T14:23:06+00:00

“Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.”

2017-11-07T14:22:39+00:00

73) “Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.” Norman, R. A.; Schott, A.-S.; Andrews, D. M.; Breed, J.; Foote, K. M.; Garner, A. P.; Ogg, D.; Orme, J. P; Pink, J. H.; Roberts, K.; Rudge, D. A.; Thomas, A. P.; Leach, A. G.* J. Med. Chem. 2012,

“Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.”2017-11-07T14:22:39+00:00

“Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.”

2017-11-07T14:21:57+00:00

74) “Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.” McCoull, W.; Addie, M. S.; Birch, A. M.; Birtles, S.; Buckett, L. K.; Butlin, R. J.; Bowker, S. S.; Boyd, S.; Chapman, S.; Davies, R. D. M.; Donald, C. S.; Green, C. P.; Jenner, C.; Kemmitt, P.

“Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.”2017-11-07T14:21:57+00:00

1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis

2017-11-07T14:20:59+00:00

76) (1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis. Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, Macfaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page

1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis2017-11-07T14:20:59+00:00

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition

2017-11-07T14:19:48+00:00

77) Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition. Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Macfaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S,

Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition2017-11-07T14:19:48+00:00

A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds

2017-11-07T14:19:02+00:00

78) A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds – identification of those isosteres more likely to have beneficial effects, Alexander G. Dossetter, Adam Douglas and Charles O'Donnell, Med. Chem. Commun., 2012,3, 1164-1169.

A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds2017-11-07T14:19:02+00:00

A matched molecular pair analysis of in-vitro human microsomal metabolic stability measurements for methylene substitution or replacements

2017-11-07T14:18:18+00:00

79) A matched molecular pair analysis of in-vitro human microsomal metabolic stability measurements for methylene substitution or replacements - identification of those transforms more likely to have beneficial effects. Alexander G. Dossetter, Med. Chem. Commun., 2012, 3, 1518.

A matched molecular pair analysis of in-vitro human microsomal metabolic stability measurements for methylene substitution or replacements2017-11-07T14:18:18+00:00

Pharmacokinetic Benefits of 3,4-Dimethoxy Substitution of a Phenyl ring and Design of Isosteres yielding orally available Cathepsin K Inhibitors

2017-11-07T14:16:58+00:00

80) Pharmacokinetic Benefits of 3,4-Dimethoxy Substitution of a Phenyl ring and Design of Isosteres yielding orally available Cathepsin K Inhibitors., Crawford JJ, Bowyer J, Cook CR, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, Macfaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page

Pharmacokinetic Benefits of 3,4-Dimethoxy Substitution of a Phenyl ring and Design of Isosteres yielding orally available Cathepsin K Inhibitors2017-11-07T14:16:58+00:00
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