PMID

Data

Article Title

Organization

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

Soochow University

Orally active 7-substituted (4-benzylphthalazin-1-yl)-2-methylpiperazin-1-yl]nicotinonitriles as active-site inhibitors of sphingosine 1-phosphate lyase for the treatment of multiple sclerosis.

Novartis Institutes For Biomedical Research

Scaffold hopping approach to a new series of smoothened antagonists.

Soochow University

Synthesis and biological evaluation of novel benzamide derivatives as potent smoothened antagonists.

Sichuan 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

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.

Astrazeneca

Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.

Universit£

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

Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.

Merck Research Laboratories

N-(2-alkylaminoethyl)-4-(1,2,4-oxadiazol-5-yl)piperazine-1-carboxamides as highly potent smoothened antagonists.

Merck Research Laboratories

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 2.

Merck Research Laboratories

Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclopropyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydroimid azo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, part 1.

Merck Research Laboratories

Purmorphamine activates the Hedgehog pathway by targeting Smoothened.

Stanford University School of Medicine

Smoothened antagonists for hair inhibition.

Pfizer

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

Amgen

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

Amgen

Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926).

Infinity Pharmaceuticals

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

Novartis Institutes For Biomedical Research

Current approaches and strategies to identify Hedgehog signaling pathway inhibitors for cancer therapy.

Chinese Academy of Medical Sciences and Peking Union Medical College

Tetracyclic Steroids Bearing a Bicyclo[4.4.1] Ring System as Potent Antiosteoporosis Agents from the Deep-Sea-Derived Fungus

Third Institute of Oceanography

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

University of Connecticut

Design, synthesis and biological evaluation of anthranilamide derivatives as potent SMO inhibitors.

China Pharmaceutical University

Discovery of [1,2,4]triazolo[4,3-a]pyridines as potent Smoothened inhibitors targeting the Hedgehog pathway with improved antitumor activity in vivo.

Southern Medical 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

Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.

Irbm-Merck Research Laboratories 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

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer.

Universit£