Target family: Type XVI RTKs: DDR (collagen receptor) family (type: catalytic_receptor)
Target: discoidin domain receptor tyrosine kinase 2

Ligand: compound 1 [PMID: 31477924] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.630000114440918 pIC50
Reference (Journal): Deep learning enables rapid identification of potent DDR1 kinase inhibitors.
Published in: Nat Biotechnol

Ligand: DDR1/2 inhibitor 5n (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pKd
Reference (Journal): Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Published in: J Med Chem

Ligand: nilotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2007)
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Published in: ACS Chem Biol

Ligand: RIPK3 inhibitor 18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
Published in: ACS Med Chem Lett

Ligand: sitravatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma.
Published in: Oncotarget

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Median affinity: 8 pIC50
Reference (Journal): Activity-based kinase profiling of approved tyrosine kinase inhibitors.
Published in: Genes Cells

Ligand: DDR1/2 inhibitor 5n (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.690000057220459 pIC50
Reference (Journal): Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Published in: J Med Chem

Ligand: DDR-IN-1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.380000114440918 pIC50
Reference (Journal): Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Published in: ACS Chem Biol

Ligand: imatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2001)
Primary target: no
Median affinity: 6.170000076293945 pIC50
Reference (Journal): Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.
Published in: ACS Chem Biol

Ligand: naporafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pKd
Reference (Journal): Design and Discovery of <i>N</i>-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Published in: J Med Chem