Target family: Type X RTKs: HGF (hepatocyte growth factor) receptor family (type: catalytic_receptor)
Target: MET proto-oncogene, receptor tyrosine kinase

Ligand: alectinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2017), Japan (unknown)
Primary target: no
Median affinity: 5.300000190734863 pIC50
Reference (Journal): Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).
Published in: Bioorg Med Chem

Ligand: altiratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Patent): Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression

Ligand: AM7 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pIC50
Reference (Journal): c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations.
Published in: J Biol Chem

Ligand: AMG-337 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: amivantamab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA (2021)
Primary target: yes
Median affinity: 10.399999618530273 pKd
Reference (Journal): Impact of Cell-surface Antigen Expression on Target Engagement and Function of an Epidermal Growth Factor Receptor × c-MET Bispecific Antibody.
Published in: J Biol Chem

Ligand: BMS-777607 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.40999984741211 pIC50
Reference (Journal): Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
Published in: J Med Chem

Ligand: cabozantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2014)
Primary target: yes
Median affinity: 8.899999618530273 pIC50
Reference (Journal): Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.
Published in: Mol Cancer Ther

Ligand: capmatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2022)
Primary target: yes
Median affinity: 9.890000343322754 pIC50
Reference (Journal): A novel kinase inhibitor, INCB28060, blocks c-MET-dependent signaling, neoplastic activities, and cross-talk with EGFR and HER-3.
Published in: Clin Cancer Res

Ligand: compound 16 [PMID: 18945615] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.070000171661377 pIC50
Reference (Journal): Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 19a [PMID: 30503936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Discovery of N<sup>1</sup>-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N<sup>3</sup>-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment.
Published in: Eur J Med Chem

Ligand: compound 1o [PMID: 24210504] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 27 [PMID: 21123062] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 8i [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.329999923706055 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: compound R-16 [PMID: 21967808] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.
Published in: Bioorg Med Chem

Ligand: crizotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.
Published in: Bioorg Med Chem Lett

Ligand: crizotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
Published in: J Med Chem

Ligand: D6808 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring <i>MET</i> Gene Alteration Treatment.
Published in: J Med Chem

Ligand: dalmelitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.
Published in: Bioorg Med Chem

Ligand: elzovantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pIC50
Reference (Patent): Macrocyclic compounds and uses thereof

Ligand: emibetuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 10 pKd
Reference (Patent): c-Met antibodies.