Target family: Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family (type: catalytic_receptor)
Target: fms related receptor tyrosine kinase 1

Ligand: ZM-306416 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.
Published in: J Med Chem

Ligand: ZM-306416 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.
Published in: J Biomol Screen

Ligand: VEGF receptor tyrosine kinase inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: VEGFB (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: VEGFA (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: vatalanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
Published in: Bioorg Med Chem Lett

Ligand: tivozanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA (2017), FDA (2021)
Primary target: yes
Median affinity: 9.680000305175781 pIC50
Reference (Journal): Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
Published in: J Med Chem

Ligand: tinengotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pIC50
Reference (Patent): Multi-kinase inhibitor compound, and crystal form and use thereof

Ligand: SU-14813 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity.
Published in: Mol Cancer Ther

Ligand: sitravatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 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: semaxanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.
Published in: J Med Chem

Ligand: RG-1530 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.050000190734863 pKd
Reference (Journal): Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.
Published in: Cell Cycle

Ligand: pexmetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.329999923706055 pIC50
Reference (Journal): Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia.
Published in: Cancer Res

Ligand: pexidartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 6.059999942779541 pIC50
Reference (Journal): Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
Published in: N Engl J Med

Ligand: pazopanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009), EMA (2010)
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
Published in: J Med Chem

Ligand: OSI-930 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 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: nintedanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Published in: Cancer Res

Ligand: motesanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
Published in: J Med Chem

Ligand: MK-2461 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Published in: Cancer Res

Ligand: lucitanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Journal): AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR.
Published in: J Cell Mol Med

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.
Published in: Mol Cancer Ther

Ligand: ilorasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.
Published in: J Pharmacol Exp Ther

Ligand: ibcasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency.
Published in: Cancer Sci

Ligand: fruquintinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2018), FDA (2023)
Primary target: yes
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
Published in: Cancer Biol Ther

Ligand: foretinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.
Published in: J Med Chem

Ligand: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Published in: J Med Chem

Ligand: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.
Published in: Blood

Ligand: dorsomorphin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.
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: 7.539999961853027 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: compound 8i [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 8h [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.140000343322754 pIC50
Reference (Journal): The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 25 [PMID: 17935989] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pKi
Reference (Journal): Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Published in: Bioorg Med Chem Lett

Ligand: CEP-11981 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Published in: J Med Chem

Ligand: cediranib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer.
Published in: Cancer Res

Ligand: Cdk1/2 inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.
Published in: J Med Chem

Ligand: catequentinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2018)
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Patent): Spiro substituted compounds as angiogenesis inhibitors

Ligand: brivanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.420000076293945 pIC50
Reference (Journal): Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Published in: J Med Chem