Target family: RAF family (type: enzyme)
Target: B-Raf proto-oncogene, serine/threonine kinase

Ligand: vemurafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: yes
Median affinity: 7 pIC50
Reference (Journal): Conformation-specific effects of Raf kinase inhibitors.
Published in: J Med Chem

Ligand: vemurafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Journal): Reducing Skin Toxicities from EGFR Inhibitors with Topical BRAF Inhibitor Therapy.
Published in: Cancer Discov

Ligand: tovorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 5.71999979019165 pIC50
Reference (Journal): A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas.
Published in: Neuro-oncology

Ligand: tinlorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Abstract 1473: Nonclinical development of PF-07284890 (ARRY-461), a potent, brain-penetrant, small molecule inhibitor of BRAF V600-mutation-driven tumors in vitro and in vivo
Published in: Cancer Research

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Published in: J Med Chem

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.079999923706055 pIC50
Reference (Journal): Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
Published in: J Med Chem

Ligand: SZM594 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.489999771118164 pIC50
Reference (Journal): Identification of the Raf kinase inhibitor TAK-632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3.
Published in: Br J Pharmacol

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
Published in: Cancer Res

Ligand: SB590885 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKi
Reference (Journal): Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.
Published in: Cancer Res

Ligand: regorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: yes
Median affinity: 7.550000190734863 pIC50
Reference (Journal): Small molecule inhibitors of BRAF in clinical trials.
Published in: Bioorg Med Chem Lett

Ligand: PLX-4720 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.
Published in: Proc Natl Acad Sci USA

Ligand: PLX-4720 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.480000019073486 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: plixorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): RAF inhibitors that evade paradoxical MAPK pathway activation.
Published in: Nature

Ligand: NST-628 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pKd
Reference (Journal): The pan-RAF-MEK non degrading molecular glue NST-628 is a potent and brain penetrant inhibitor of the RAS-MAPK pathway with activity across diverse RAS- and RAF-driven cancers.
Published in: Cancer Discov