Evidence for a Significant Role of α3-Containing GABA_AReceptors in Mediating the Anxiolytic Effects of Benzodiazepines

Rebecca Dias, Wayne F. A. Sheppard, Rosa Fradley, +19

Journal of Neuroscience

Anesthetic MechanismPsychopharmacologyPharmacotherapyAlpha2 PotentiationExperimental Pharmacology +17

Fluorination of 3-(3-(Piperidin-1-yl)propyl)indoles and 3-(3-(Piperazin-1-yl)propyl)indoles Gives Selective Human 5-HT_1D Receptor Ligands with Improved Pharmacokinetic Profiles

Monique B. van Niel, Ian Collins, Margaret S. Beer, +18

Journal of Medicinal Chemistry

Combinatorial ChemistryMolecular PharmacologyMedicinal ChemistryPharmaceutical Science5-Ht1d Receptor Ligands +13

Imidazo[1,2<i>-a</i>]pyrimidines as Functionally Selective and Orally Bioavailable GABA_Aα2/α3 Binding Site Agonists for the Treatment of Anxiety Disorders

Simon Goodacre, Leslie J. Street, David J. Hallett, +16

Journal of Medicinal Chemistry

PsychopharmacologyPharmacotherapyExperimental PharmacologySocial SciencesMolecular Pharmacology +17

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer

Jun Liang, Robert A. Blake, Jae H. Chang, +43

Journal of Medicinal Chemistry

8-Fluoroimidazo[1,2-a]pyridine: Synthesis, physicochemical properties and evaluation as a bioisosteric replacement for imidazo[1,2-a]pyrimidine in an allosteric modulator ligand of the GABAA receptor

Alexander C. Humphries, Emanuela Gancia, Myra T. Gilligan, +4

Bioorganic & Medicinal Chemistry Letters

Bioisosteric ReplacementAllosteric Modulator LigandMedicinal ChemistryBioorganic ChemistryBiochemistry +10

3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as High Affinity, Selective, and Orally Bioavailable h5-HT_2A Receptor Antagonists

Michael Rowley, David J. Hallett, Simon Goodacre, +13

Journal of Medicinal Chemistry

Differential contribution of GABA_A receptor subtypes to the anticonvulsant efficacy of benzodiazepine site ligands

Rosa Fradley, Martin R. Guscott, Sharlene Bull, +11

Journal of Psychopharmacology

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling

Mark Zak, Emily J. Hanan, Patrick J. Lupardus, +26

Bioorganic & Medicinal Chemistry Letters

Effective Cell-based BlockadeSignaling PathwayNovel TherapyMedicineReceptor Tyrosine Kinase +7

Discovery of Imidazo[1,2-<i>b</i>][1,2,4]triazines as GABA_A α2/3 Subtype Selective Agonists for the Treatment of Anxiety

Michael G. N. Russell, Robert W. Carling, Leslie J. Street, +22

Journal of Medicinal Chemistry

Molecular PharmacologyMedicinal ChemistryAllergyPsychiatryFunctional Selectivity +9

Imidazo[1,2-a]pyrimidines as functionally selective GABAA ligands

Wesley Blackaby, John Atack, Frances A. Bromidge, +10

Bioorganic & Medicinal Chemistry Letters

Selective Gabaa LigandsCombinatorial ChemistryBioorganic ChemistryMedicinePharmacology +1