Target family: RAF family (type: enzyme)
Target: Raf-1 proto-oncogene, serine/threonine kinase

Ligand: ZM336372 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The specificities of protein kinase inhibitors: an update.
Published in: Biochem J

Ligand: ZM336372 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: vemurafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Published in: Cancer Cell

Ligand: vemurafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity:  pIC50
Reference (Journal): Conformation-specific effects of Raf kinase inhibitors.
Published in: J Med Chem

Ligand: tinlorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 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: 8.850000381469727 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: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.279999732971191 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: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 8.220000267028809 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: 8.760000228881836 pIC50
Reference (Journal): Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885.
Published in: Cancer Res

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: plixorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): RAF inhibitors that evade paradoxical MAPK pathway activation.
Published in: Nature

Ligand: OSI-930 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.389999866485596 pIC50
Reference (Journal): OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models.
Published in: Cancer Res

Ligand: NST-628 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.409999847412109 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

Ligand: naporafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 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

Ligand: LY3009120 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.
Published in: Cancer Cell

Ligand: L779450 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pIC50
Reference (Journal): Pharmacophore identification of Raf-1 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: GW5074 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.050000190734863 pIC50
Reference (Journal): The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism.
Published in: J Neurochem

Ligand: exarafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pIC50
Reference (Journal): The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition
Published in: J Med Chem

Ligand: exarafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Inhibitors of raf kinases

Ligand: CCT241161 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.
Published in: Cancer Cell

Ligand: CCT196969 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.
Published in: Cancer Cell

Ligand: brimarafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.720000267028809 pIC50
Reference (Patent): Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors

Ligand: belvarafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Patent): THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES

Ligand: balamapimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.940000057220459 pIC50
Reference (Patent): 3-quinolinecarbonitrile protein kinase inhibitors

Ligand: avutometinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.25 pIC50
Reference (Journal): Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Published in: ACS Med Chem Lett

Ligand: agerafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.409999847412109 pKd
Reference (Journal): Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Published in: J Med Chem