Journal: Journal of Pharmaceutical Analysis

Article Title: Scaffold and SAR studies on c-MET inhibitors using machine learning approaches

doi: 10.1016/j.jpha.2025.101303

Figure Lengend Snippet: Representative examples of types I, II, and III small-molecule c-mesenchymal-epithelial transition (c-MET) kinase inhibitors launched or in different clinical phase trials. FDA: Food and Drug Administration; NMPA: The National Medical Products Administration, China.

Article Snippet: Type II inhibitors (compounds 10–13) are multitarget c-MET and ATP-competitive inhibitors.

Techniques:

Journal: Journal of Pharmaceutical Analysis

Article Title: Scaffold and SAR studies on c-MET inhibitors using machine learning approaches

doi: 10.1016/j.jpha.2025.101303

Figure Lengend Snippet: Trends in the number of published small-molecule c-mesenchymal-epithelial transition (c-MET) kinase inhibitors. (A) Number of compounds reported from the year 2004−2022. (B) Histogram of published percentage of active molecules.

Article Snippet: Type II inhibitors (compounds 10–13) are multitarget c-MET and ATP-competitive inhibitors.

Techniques:

Journal: Journal of Pharmaceutical Analysis

Article Title: Scaffold and SAR studies on c-MET inhibitors using machine learning approaches

doi: 10.1016/j.jpha.2025.101303

Figure Lengend Snippet: Distribution of c-mesenchymal-epithelial transition (c-MET) active inhibitors (red) and inactive inhibitors (blue) with respect to the four rule-of-five descriptors: molecular weight, logarithm of the partition coefficient (logP), and the numbers of hydrogen bond donors and acceptors.

Article Snippet: Type II inhibitors (compounds 10–13) are multitarget c-MET and ATP-competitive inhibitors.

Techniques: Molecular Weight

Journal: Slas Discovery

Article Title: Development of a 3D Tissue Culture–Based High-Content Screening Platform That Uses Phenotypic Profiling to Discriminate Selective Inhibitors of Receptor Tyrosine Kinases

doi: 10.1177/1087057116657269

Figure Lengend Snippet: c-Met–dependent phenotypic changes. ( A ) Inhibition of hepatocyte growth factor (HGF)–induced invasion in 3D-cultured PC-3 cells by function blocking c-Met Fab antibody 5D5 (Genentech, South San Francisco, CA) and stimulation of invasion by the crosslinking and activating bivalent IgG isoform. Principal components analysis (PCA) trained on unstimulated and stimulated control, PC0 shown and scaled as Z score to unstimulated control. Results are shown as means of quadruplicate wells and standard deviations. ( B ) 5D5 Fab (triangles) causes a shift in phenotype from stimulated (empty circles) back to unstimulated control (filled circles). Point size of markers for Fab treatment increases with concentration (seven concentrations; range, 0.316–316 nM). Individual data points are shown as a 3D scatterplot with PC0, PC1, and PC2.

Article Snippet: Compounds that induced such a shift in the c-Met PC0 included various established c-Met reference inhibitors that were included in the screen, including the Genentech 5D5 Fab antibody, foretinib, and lower doses of PHA-665752.

Techniques: Inhibition, Cell Culture, Blocking Assay, Control, Concentration Assay

Journal: Slas Discovery

Article Title: Development of a 3D Tissue Culture–Based High-Content Screening Platform That Uses Phenotypic Profiling to Discriminate Selective Inhibitors of Receptor Tyrosine Kinases

doi: 10.1177/1087057116657269

Figure Lengend Snippet: c-Met–dependent phenotypic changes. ( A ) Inhibition of hepatocyte growth factor (HGF)–induced invasion in 3D-cultured PC-3 cells by function blocking c-Met Fab antibody 5D5 (Genentech, South San Francisco, CA) and stimulation of invasion by the crosslinking and activating bivalent IgG isoform. Principal components analysis (PCA) trained on unstimulated and stimulated control, PC0 shown and scaled as Z score to unstimulated control. Results are shown as means of quadruplicate wells and standard deviations. ( B ) 5D5 Fab (triangles) causes a shift in phenotype from stimulated (empty circles) back to unstimulated control (filled circles). Point size of markers for Fab treatment increases with concentration (seven concentrations; range, 0.316–316 nM). Individual data points are shown as a 3D scatterplot with PC0, PC1, and PC2.

Article Snippet: Compounds that induced such a shift in the c-Met PC0 included various established c-Met reference inhibitors that were included in the screen, including the Genentech 5D5 Fab antibody, foretinib, and lower doses of PHA-665752.

Techniques: Inhibition, Cell Culture, Blocking Assay, Concentration Assay