The promise and peril of chemical probes

C.H. Arrowsmith, James E. Audia, Christopher P. Austin, +51

Nature Chemical Biology

Quinazolinone Derivatives as Orally Available Ghrelin Receptor Antagonists for the Treatment of Diabetes and Obesity

Joachim Rudolph, William P. Esler, Stephen O’Connor, +29

Journal of Medicinal Chemistry

Food IntakePharmacotherapyType 1AInsulin SignalingGastrointestinal Peptide Hormone +15

LINGO-1, a Transmembrane Signaling Protein, Inhibits Oligodendrocyte Differentiation and Myelination through Intercellular Self-interactions

Scott Jepson, Bryan W. Vought, Christian H. Gross, +7

Journal of Biological Chemistry

Specific Inhibition of Hormone-Sensitive Lipase Improves Lipid Profile while Reducing Plasma Glucose

Thomas H. Claus, Derek Lowe, Yin Liang, +6

Journal of Pharmacology and Experimental Therapeutics

SCH 57790, a selective muscarinic M2 receptor antagonist, releases acetylcholine and produces cognitive enhancement in laboratory animals

Galen Carey, William Billard, Herbert Binch, +10

European Journal of Pharmacology

Molecular PharmacologyLaboratory AnimalsMedicineNeurotransmitterNeuropharmacology +6

In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase

Derek Lowe, Steven Magnuson, Ning Qi, +14

Bioorganic & Medicinal Chemistry Letters

Pharmaceutical ScienceBiochemistryVitro SarMedicineMechanism Of Action +8

Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3-Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS)

Jon H. Come, Philip N. Collier, James A. Henderson, +27

Journal of Medicinal Chemistry

ImmunologyPharmacotherapyPharmaceutical ChemistryPre-clinical PharmacologyNeuroinflammation +18

SCH 57790: A novel M2 receptor selective antagonist

Jean E. Lachowicz, Derek Lowe, Ruth A. Duffy, +11

Life Sciences

Molecular PharmacologyBiochemistryFunctional SelectivityMedicineMechanism Of Action +5

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17β-hydroxysteroid dehydrogenase. Part 3. Identification of lead candidate

Jill E. Wood, Cedo M. Bagi, Christiana Akuche, +27

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryBiochemistryNatural SciencesMedicineLead Identification +6

4,5-Disubstituted cis-pyrrolidinones as inhibitors of type II 17β-hydroxysteroid dehydrogenase. Part 2. SAR

David Gunn, Christiana Akuche, Jeremy L. Baryza, +27

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryBioorganic ChemistryBiochemistryNatural Sciences +8