4F64
 
 | | Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 6 | | 分子名称: | 1,2-ETHANEDIOL, 5-bromo-N~4~-[3-(3-methoxypropyl)-1H-pyrazol-5-yl]-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1, ... | | 著者 | Norman, R.A, Breed, J, Ogg, D. | | 登録日 | 2012-05-14 | | 公開日 | 2012-06-06 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.05 Å) | | 主引用文献 | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.
J.Med.Chem., 55, 2012
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4F63
 | | Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 1 | | 分子名称: | 1,2-ETHANEDIOL, 5-bromo-N~4~-(3-methyl-1H-pyrazol-5-yl)-N~2~-[2-(pyridin-3-yl)ethyl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1 | | 著者 | Norman, R.A, Breed, J, Ogg, D. | | 登録日 | 2012-05-14 | | 公開日 | 2012-06-06 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2.55 Å) | | 主引用文献 | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.
J.Med.Chem., 55, 2012
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4F65
 | | Crystal structure of Human Fibroblast Growth Factor Receptor 1 Kinase domain in complex with compound 8 | | 分子名称: | 1,2-ETHANEDIOL, 5-bromo-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]-N~4~-[3-(2-phenylethyl)-1H-pyrazol-5-yl]pyrimidine-2,4-diamine, Fibroblast growth factor receptor 1, ... | | 著者 | Norman, R.A, Breed, J, Ogg, D. | | 登録日 | 2012-05-14 | | 公開日 | 2012-06-06 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.26 Å) | | 主引用文献 | Protein-Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.
J.Med.Chem., 55, 2012
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1UOU
 | | Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor | | 分子名称: | 5-CHLORO-6-(1-(2-IMINOPYRROLIDINYL) METHYL) URACIL, THYMIDINE PHOSPHORYLASE | | 著者 | Norman, R.A, Barry, S.T, Bate, M, Breed, J, Colls, J.G, Ernill, R.J, Luke, R.W.A, Minshull, C.A, McAlister, M.S.B, McCall, E.J, McMiken, H.H.J, Paterson, D.S, Timms, D, Tucker, J.A, Pauptit, R.A. | | 登録日 | 2003-09-23 | | 公開日 | 2004-01-22 | | 最終更新日 | 2023-12-13 | | 実験手法 | X-RAY DIFFRACTION (2.11 Å) | | 主引用文献 | Crystal Structure of Human Thymidine Phosphorylase in Complex with a Small Molecule Inhibitor
Structure, 12, 2004
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1GR0
 | | myo-inositol 1-phosphate synthase from Mycobacterium tuberculosis in complex with NAD and zinc. | | 分子名称: | CACODYLATE ION, INOSITOL-3-PHOSPHATE SYNTHASE, NICOTINAMIDE-ADENINE-DINUCLEOTIDE, ... | | 著者 | Norman, R.A, Murray-Rust, J, McDonald, N.Q, TB Structural Genomics Consortium (TBSGC) | | 登録日 | 2001-12-10 | | 公開日 | 2002-03-12 | | 最終更新日 | 2019-08-21 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Crystal Structure of Inositol 1-Phosphate Synthase from Mycobacterium Tuberculosis, a Key Enzyme in Phosphatidylinositol Synthesis
Structure, 10, 2002
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2WOT
 | | ALK5 IN COMPLEX WITH 4-((5,6-dimethyl-2-(2-pyridyl)-3-pyridyl)oxy)-N-(3,4,5-trimethoxyphenyl)pyridin-2-amine | | 分子名称: | 1,2-ETHANEDIOL, 4-[(5,6-DIMETHYL-2,2'-BIPYRIDIN-3-YL)OXY]-N-(3,4,5-TRIMETHOXYPHENYL)PYRIDIN-2-AMINE, TGF-BETA RECEPTOR TYPE-1 | | 著者 | Norman, R.A, Debreczeni, J.E, Goldberg, F.W, Ward, R.A, Finlay, R, Powell, S.J, Roberts, N.J, Dishington, A.P, Gingell, H.J, Wickson, K.F, Roberts, A.L. | | 登録日 | 2009-07-28 | | 公開日 | 2009-09-22 | | 最終更新日 | 2019-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Rapid Generation of a High Quality Lead for Transforming Growth Factor-Beta (Tgf-Beta) Type I Receptor (Alk5).
J.Med.Chem., 52, 2009
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5AAU
 | | Optimization of a novel binding motif to to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H- pyrido(3,4-b)indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist | | 分子名称: | 3-(1-(4-Chlorophenyl)-3,4-dihydro-1H-pyrido(3,4-b)indol-2(9H)-yl)propanoic acid, ESTROGEN RECEPTOR | | 著者 | Norman, R.A, Bradbury, R.H, de Almeida, C, Andrews, D.M, Ballard, P, Buttar, D, Callis, R.J, Currie, G.S, Curwen, J.O, Davies, C.D, de Savi, C, Donald, C.S, Feron, L.J.L, Glossop, S.C, Hayter, B.R, Karoutchi, G, Lamont, S.G, MacFaul, P, Moss, T, Pearson, S.E, Rabow, A.A, Tonge, M, Walker, G.E, Weir, H.M, Wilson, Z. | | 登録日 | 2015-07-28 | | 公開日 | 2015-10-14 | | 最終更新日 | 2016-10-12 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
J.Med.Chem., 58, 2015
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5AAV
 | | Optimization of a novel binding motif to to (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H- pyrido(3,4-b)indol-1-yl)phenyl)acrylic acid (AZD9496), a potent and orally bioavailable selective estrogen receptor downregulator and antagonist | | 分子名称: | (2E)-3-{4-[(1E)-1,2-DIPHENYLBUT-1-ENYL]PHENYL}ACRYLIC ACID, ESTROGEN RECEPTOR | | 著者 | Norman, R.A, Bradbury, R.H, de Almeida, C, Andrews, D.M, Ballard, P, Buttar, D, Callis, R.J, Currie, G.S, Curwen, J.O, Davies, C.D, de Savi, C, Donald, C.S, Feron, L.J.L, Glossop, S.C, Hayter, B.R, Karoutchi, G, Lamont, S.G, MacFaul, P, Moss, T, Pearson, S.E, Rabow, A.A, Tonge, M, Walker, G.E, Weir, H.M, Wilson, Z. | | 登録日 | 2015-07-29 | | 公開日 | 2015-10-14 | | 最終更新日 | 2016-10-12 | | 実験手法 | X-RAY DIFFRACTION (1.95 Å) | | 主引用文献 | Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
J.Med.Chem., 58, 2015
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5ACC
 | | A Novel Oral Selective Estrogen Receptor Down-regulator, AZD9496, drives Tumour Growth Inhibition in Estrogen Receptor positive and ESR1 Mutant Models | | 分子名称: | (E)-3-(3,5-DIFLUORO-4-((1R,3R)-2-(2-FLUORO-2- METHYLPROPYL)-3-METHYL-2,3,4,9-TETRAHYDRO-1H-PYRIDO(3,4-B)INDOL-1-YL)PHENYL)ACRYLIC ACID, ESTROGEN RECEPTOR | | 著者 | Norman, R.A, Weir, H.M, Bradbury, R.H, Lawson, M, Rabow, A.A, Buttar, D, Callis, R.J, Curwen, J.O, de Almeida, C, Ballard, P, Hulse, M, Donald, C.S, Feron, L.J.L, Gingell, H, Karoutchi, G, MacFaul, P, Moss, T, Pearson, S.E, Tonge, M, Davies, G, Walker, G.E, Wilson, Z, Rowlinson, R, Powell, S, Hemsley, P, Linney, E, Campbell, H, Ghazoui, Z, Sadler, C, Richmond, G, Pazolli, E, Mazzola, A.M, DCruz, C, De Savi, C. | | 登録日 | 2015-08-15 | | 公開日 | 2015-12-16 | | 実験手法 | X-RAY DIFFRACTION (1.88 Å) | | 主引用文献 | Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist.
J.Med.Chem., 58, 2015
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4NK9
 | | Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 1 | | 分子名称: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1, N~4~-{5-[2-(3,5-dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl}-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, ... | | 著者 | Norman, R.A, Klein, T. | | 登録日 | 2013-11-12 | | 公開日 | 2013-12-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.57 Å) | | 主引用文献 | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
ACS Med Chem Lett, 5, 2014
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4NKS
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4NKA
 | | Crystal structure of human fibroblast growth factor receptor 1 kinase domain in complex with pyrazolaminopyrimidine 2 | | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N~4~-{3-[2-(3,4-dimethoxyphenyl)ethyl]-1H-pyrazol-5-yl}-N~2~-[(3-methyl-1,2-oxazol-5-yl)methyl]pyrimidine-2,4-diamine, ... | | 著者 | Norman, R.A, Klein, T. | | 登録日 | 2013-11-12 | | 公開日 | 2013-12-18 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.19 Å) | | 主引用文献 | FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
ACS Med Chem Lett, 5, 2014
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2WOU
 | | ALK5 IN COMPLEX WITH 4-((4-((2,6-dimethyl-3-pyridyl)oxy)-2-pyridyl) amino)benzenesulfonamide | | 分子名称: | 1,2-ETHANEDIOL, 4-({4-[(2,6-DIMETHYLPYRIDIN-3-YL)OXY]PYRIDIN-2-YL}AMINO)BENZENESULFONAMIDE, TGF-BETA RECEPTOR TYPE-1 | | 著者 | Debreczeni, J.E, Norman, R.A, Goldberg, F.W, Ward, R.A, Finlay, R, Powell, S.J, Roberts, N.J, Dishington, A.P, Gingell, H.J, Wickson, K.F, Roberts, A.L. | | 登録日 | 2009-07-28 | | 公開日 | 2009-09-22 | | 最終更新日 | 2019-05-08 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Rapid Generation of a High Quality Lead for Transforming Growth Factor-Beta (Tgf-Beta) Type I Receptor (Alk5).
J.Med.Chem., 52, 2009
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4V04
 | | FGFR1 in complex with ponatinib. | | 分子名称: | 1,2-ETHANEDIOL, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-09-10 | | 公開日 | 2014-12-10 | | 最終更新日 | 2018-04-04 | | 実験手法 | X-RAY DIFFRACTION (2.12 Å) | | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4
Structure, 22, 2014
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2BAL
 | | p38alpha MAP kinase bound to pyrazoloamine | | 分子名称: | Mitogen-activated protein kinase 14, [5-AMINO-1-(4-FLUOROPHENYL)-1H-PYRAZOL-4-YL][3-(PIPERIDIN-4-YLOXY)PHENYL]METHANONE | | 著者 | Gerhardt, S, Pauptit, R.A, Read, J, Tucker, J, Norman, R.A, Breed, J. | | 登録日 | 2005-10-14 | | 公開日 | 2005-12-06 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Prevention of MKK6-Dependent Activation by Binding to p38alpha MAP Kinase.
Biochemistry, 44, 2005
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2BAJ
 | | p38alpha bound to pyrazolourea | | 分子名称: | 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(2,3-dichlorophenyl)urea, Mitogen-activated protein kinase 14 | | 著者 | Gerhardt, S, Pauptit, R.A, Read, J, Breed, J, Norman, R.A, Ward, W.H. | | 登録日 | 2005-10-14 | | 公開日 | 2005-12-06 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.25 Å) | | 主引用文献 | Prevention of MKK6-Dependent Activation by Binding to p38alpha MAP Kinase
Biochemistry, 44, 2005
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2BAQ
 | | p38alpha bound to Ro3201195 | | 分子名称: | Mitogen-activated protein kinase 14, [5-AMINO-1-(4-FLUOROPHENYL)-1H-PYRAZOL-4-YL](3-{[(2R)-2,3-DIHYDROXYPROPYL]OXY}PHENYL)METHANONE | | 著者 | Gerhardt, S, Pauptit, R.A, Breed, J, Read, J, Tucker, J, Norman, R.A. | | 登録日 | 2005-10-14 | | 公開日 | 2005-12-06 | | 最終更新日 | 2021-10-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Prevention of MKK6-Dependent Activation by Binding to p38alpha MAP Kinase.
Biochemistry, 44, 2005
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2BAK
 | | p38alpha MAP kinase bound to MPAQ | | 分子名称: | Mitogen-activated protein kinase 14, N-(3-{[7-METHOXY-6-(2-PYRROLIDIN-1-YLETHOXY)QUINAZOLIN-4-YL]AMINO}-4-METHYLPHENYL)-2-MORPHOLIN-4-YLISONICOTINAMIDE | | 著者 | Gerhardt, S, Breed, J, Pauptit, R.A, Read, J, Norman, R.A, Ward, W.H. | | 登録日 | 2005-10-14 | | 公開日 | 2005-12-06 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | | 主引用文献 | Prevention of MKK6-Dependent Activation by Binding to p38alpha MAP Kinase
Biochemistry, 44, 2005
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4V01
 | | FGFR1 in complex with ponatinib (co-crystallisation). | | 分子名称: | 1,2-ETHANEDIOL, 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, ... | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-09-10 | | 公開日 | 2014-12-10 | | 最終更新日 | 2018-04-04 | | 実験手法 | X-RAY DIFFRACTION (2.33 Å) | | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4
Structure, 22, 2014
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4V05
 | | FGFR1 in complex with AZD4547. | | 分子名称: | 1,2-ETHANEDIOL, FIBROBLAST GROWTH FACTOR RECEPTOR 1 (FMS-RELATED TYROSINE KINASE 2, PFEIFFER SYNDROME), ... | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-09-10 | | 公開日 | 2014-12-10 | | 最終更新日 | 2014-12-17 | | 実験手法 | X-RAY DIFFRACTION (2.57 Å) | | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4
Structure, 22, 2014
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4UXQ
 | | FGFR4 in complex with Ponatinib | | 分子名称: | 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide, FIBROBLAST GROWTH FACTOR RECEPTOR 4, SULFATE ION | | 著者 | Tucker, J, Klein, T, Breed, J, Breeze, A, Overman, R, Phillips, C, Norman, R.A. | | 登録日 | 2014-08-27 | | 公開日 | 2014-12-03 | | 最終更新日 | 2014-12-17 | | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | | 主引用文献 | Structural Insights Into Fgfr Kinase Isoform Selectivity: Diverse Binding Modes of Azd4547 and Ponatinib in Complex with Fgfr1 and Fgfr4
Structure, 22, 2014
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1URW
 | | CDK2 IN COMPLEX WITH AN IMIDAZO[1,2-b]PYRIDAZINE | | 分子名称: | 2-[4-(N-(3-DIMETHYLAMINOPROPYL)SULPHAMOYL)ANILINO]-, CELL DIVISION PROTEIN KINASE 2 | | 著者 | Byth, K.F, Cooper, N, Culshaw, J.D, Heaton, D.W, Oakes, S.E, Minshull, C.A, Norman, R.A, Pauptit, R.A, Tucker, J.A, Breed, J, Pannifer, A, Rowsell, S, Stanway, J.J, Valentine, A.L, Thomas, A.P. | | 登録日 | 2003-11-11 | | 公開日 | 2004-04-23 | | 最終更新日 | 2011-07-13 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Imidazo[1,2-B]Pyridazines: A Potent and Selective Class of Cyclin-Dependent Kinase Inhibitors
Bioorg.Med.Chem.Lett., 14, 2004
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5FQT
 | | Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 4. | | 分子名称: | (E)-3-[4-(6-hydroxy-2-isobutyl-5-methyl-3,4-dihydro-1H-isoquinolin-1-yl)phenyl]prop-2-enoic acid, ESTROGEN RECEPTOR ALPHA | | 著者 | Scott, J.S, Bailey, A, Davies, R.D.M, Degorce, S.L, MacFaul, P.A, Gingell, H, Moss, T, Norman, R.A, Pink, J.H, Rabow, A.A, Roberts, B, Smith, P.D. | | 登録日 | 2015-12-14 | | 公開日 | 2016-02-10 | | 最終更新日 | 2018-09-19 | | 実験手法 | X-RAY DIFFRACTION (1.99 Å) | | 主引用文献 | Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Acs Med.Chem.Lett., 7, 2016
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5FQP
 | | Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 1. | | 分子名称: | (E)-3-[4-[(1R,3R)-6-hydroxy-2-isobutyl-3-methyl-3,4-dihydro-1H-isoquinolin-1-yl]phenyl]prop-2-enoic acid, ESTROGEN RECEPTOR ALPHA | | 著者 | Scott, J.S, Bailey, A, Davies, R.D.M, Degorce, S.L, MacFaul, P.A, Gingell, H, Moss, T, Norman, R.A, Pink, J.H, Rabow, A.A, Roberts, B, Smith, P.D. | | 登録日 | 2015-12-14 | | 公開日 | 2016-02-10 | | 最終更新日 | 2020-03-11 | | 実験手法 | X-RAY DIFFRACTION (1.88 Å) | | 主引用文献 | Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Acs Med.Chem.Lett., 7, 2016
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5FQR
 | | Selective estrogen receptor downregulator antagonists: Tetrahydroisoquinoline phenols 2. | | 分子名称: | (E)-3-[4-[(1R)-6-HYDROXY-2-ISOBUTYL-3,4-DIHYDRO-1H-ISOQUINOLIN-1-YL]PHENYL]PROP-2-ENOIC ACID, ESTROGEN RECEPTOR | | 著者 | Scott, J.S, bailey, A, Davies, R.D.M, Degorce, S.L, MacFaul, P.A, Gingell, H, Moss, T, Norman, R.A, Pink, J.H, Rabow, A.A, Roberts, B, Smith, P.D. | | 登録日 | 2015-12-14 | | 公開日 | 2016-02-10 | | 最終更新日 | 2016-10-12 | | 実験手法 | X-RAY DIFFRACTION (1.88 Å) | | 主引用文献 | Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Acs Med.Chem.Lett., 7, 2016
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