PMID

Data

Article Title

Organization

Design, Palladium-Catalyzed Synthesis, and Biological Investigation of 2-Substituted 3-Aroylquinolin-4(1H)-ones as Inhibitors of the Hedgehog Signaling Pathway.

Sapienza University of Rome

Design, Synthesis, and Pharmacological Evaluation of 2-(2,5-Dimethyl-5,6,7,8-tetrahydroquinolin-8-yl)-N-aryl Propanamides as Novel Smoothened (Smo) Antagonists.

University of Chinese Academy of Sciences

Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.

Universit£

Discovery of a 6-(pyridin-3-yl)benzo[d]thiazole template for optimization of hedgehog and PI3K/AKT/mTOR dual inhibitors.

Soochow University

Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling.

Duke University Medical Center

Design, synthesis, and structure-activity-relationship of phenyl imidazoles as potent Smoothened antagonists.

Genomics Institute of The Novartis Research Foundation

Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies.

TBA

Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.

TBA

Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway.

Novartis Institutes For Biomedical Research

Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.

Amgen

Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.

Amgen

Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.

Amgen

1-amino-4-benzylphthalazines as orally bioavailable smoothened antagonists with antitumor activity.

Novartis Institutes For Biomedical Research

Design, synthesis and biological evaluation of novel 4-aminopiperidine derivatives as SMO/ERK dual inhibitors.

China Pharmaceutical University

Medulloblastoma drugs in development: Current leads, trials and drawbacks.

University of Connecticut

Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.

Shanghaitech University

Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).

Astrazeneca

Colocalization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor.

Shanghaitech University

Structural optimization on a virtual screening hit of smoothened receptor.

Soochow University

Structure-Activity Relationships for Itraconazole-Based Triazolone Analogues as Hedgehog Pathway Inhibitors.

University of Connecticut

Synergistic inhibition of the Hedgehog pathway by newly designed Smo and Gli antagonists bearing the isoflavone scaffold.

Sapienza University of Rome

Discovery and characterization of a potent Wnt and hedgehog signaling pathways dual inhibitor.

Soochow University

Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays.

Soochow University