H
H. Gingell
Researcher at AstraZeneca
Publications - 4
Citations - 265
H. Gingell is an academic researcher from AstraZeneca. The author has contributed to research in topics: Estrogen receptor & TGF beta signaling pathway. The author has an hindex of 4, co-authored 4 publications receiving 223 citations.
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Journal ArticleDOI
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.
Chris De Savi,Robert Hugh Bradbury,Alfred A. Rabow,Richard A. Norman,Camila de Almeida,David M. Andrews,Peter Ballard,David Buttar,Rowena Callis,Gordon S. Currie,Jon Curwen,Christopher D. Davies,Craig S. Donald,Lyman Feron,H. Gingell,Steven C. Glossop,Barry R. Hayter,Syeed Hussain,Galith Karoutchi,Scott G. Lamont,Philip A. MacFaul,Thomas A. Moss,Stuart E. Pearson,Michael Tonge,Graeme Walker,Hazel M. Weir,Zena Wilson +26 more
TL;DR: The discovery of an orally bioavailable selective estrogen receptor downregulator (SERD) with equivalent potency and preclinical pharmacology to the intramuscular SERD fulvestrant is described.
Journal ArticleDOI
Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA
Ruben C. Hartkoorn,Florence Pojer,Jon Read,H. Gingell,João Neres,Oliver P. Horlacher,Karl-Heinz Altmann,Stewart T. Cole +7 more
TL;DR: This work unveiling the co-crystal structure and unique ability of pyridomycin to block both the NADH cofactor- and lipid substrate-binding pockets of InhA reveals a first-of-a-kind binding mode that discloses a new means of InHA inhibition.
Journal ArticleDOI
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
James S. Scott,Andrew Bailey,Robert D. M. Davies,Sébastien L. Degorce,Philip A. MacFaul,H. Gingell,Thomas A. Moss,Richard A. Norman,Jennifer H. Pink,Alfred A. Rabow,Bryan Roberts,Peter D. Smith +11 more
TL;DR: A series of tetrahydroisoquinoline phenols was modified to give an estrogen receptor downregulator-antagonist profile that was compatible with obtaining high oral bioavailabilities in rat.
Journal ArticleDOI
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Frederick W. Goldberg,Richard A. Ward,Steven Powell,Judit E. Debreczeni,Richard A. Norman,Nicola J. Roberts,Allan Dishington,H. Gingell,Kate F. Wickson,Andrew L Roberts +9 more
TL;DR: A novel class of 4-pyridinoxy-2-anilinopyridine-based TGF-beta type I receptor-based ALK5 inhibitors is reported and the binding mode of this scaffold was successfully predicted by analyzing possible docked binding modes of literature inhibitors and novel synthetic ideas.