Selective Activation of M₄Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

Michael Bubser, Thomas M. Bridges, Ditte Dencker, +19

ACS Chemical Neuroscience

Discovery of 2-Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods

Nicholas F. Pelz, Zhiguo Bian, Bin Zhao, +13

Journal of Medicinal Chemistry

Drug TargetMolecular BiologyTumor BiologyMyeloid NeoplasiaHematological Malignancy +14

Antipsychotic Drug-Like Effects of the Selective M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator VU0152100

Nellie Byun, Michael Grannan, Michael Bubser, +18

Neuropsychopharmacology

PsychiatryFunctional SelectivityMedicinePsychopharmacologySchizophrenia +7

Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design

Subrata Shaw, Zhiguo Bian, Bin Zhao, +13

Journal of Medicinal Chemistry

PharmacotherapyPharmaceutical ChemistryTumor BiologyMedicinal ChemistryDrug Design +14

Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer

Taekyu Lee, Plamen P. Christov, Subrata Shaw, +24

Journal of Medicinal Chemistry

Hematological MalignancyTumor BiologyMouse Xenograft ModelsVivo ActivityCompound 42 +13

Fragment-based screening of programmed death ligand 1 (PD-L1)

Evan Perry, Jonathan J. Mills, Bin Zhao, +8

Bioorganic & Medicinal Chemistry Letters

Molecular DockingMedicinal ChemistryDrug TargetMedicineRational Drug Design +4

Targeting Selective Activation of M₁ for the Treatment of Alzheimer’s Disease: Further Chemical Optimization and Pharmacological Characterization of the M₁ Positive Allosteric Modulator ML169

James C. Tarr, Mark Turlington, Paul R. Reid, +15

ACS Chemical Neuroscience

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

Michael R. Wood, Meredith J. Noetzel, Michael S. Poslusney, +17

Bioorganic & Medicinal Chemistry Letters

Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071

Evan P. Lebois, Gregory J. Digby, Douglas J. Sheffler, +11

Bioorganic & Medicinal Chemistry Letters

Pharmaceutical ScienceMedicineNeuropharmacologyPharmacotherapyBiomedical Engineering +4

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

James C. Tarr, Michael R. Wood, Meredith J. Noetzel, +15

Bioorganic & Medicinal Chemistry Letters