Target family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family (type: catalytic_receptor)
Target: platelet derived growth factor receptor beta

Ligand: AC710 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.
Published in: ACS Med Chem Lett

Ligand: AGL 2043 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.050000190734863 pIC50
Reference (Journal): Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit.
Published in: Bioorg Med Chem

Ligand: BPR1R024 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model.
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: CHMFL-KIT-64 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pIC50
Reference (Journal): Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)-<i>N</i>-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors.
Published in: J Med Chem

Ligand: compound 5e [PMID: 28580438] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pKd
Reference (Journal): Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia.
Published in: ACS Omega

Ligand: compound 8h [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): The design, synthesis, and biological evaluation of potent receptor tyrosine kinase 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: 8.819999694824219 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: CP-673451 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451.
Published in: Cancer Res

Ligand: crenolanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.489999771118164 pKd
Reference (Journal): Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors.
Published in: Clin Cancer Res

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: famitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
Published in: J Med Chem

Ligand: Flt-3 inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pIC50
Reference (Journal): Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase.
Published in: J Med Chem

Ligand: flumbatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2019)
Primary target: no
Median affinity: 6.510000228881836 pIC50
Reference (Journal): HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance.
Published in: Leukemia

Ligand: GTP-14564 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3).
Published in: J Biol Chem

Ligand: henatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
Published in: J Med Chem

Ligand: IACS-9439 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.349999904632568 pKd
Reference (Journal): Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Published in: J Med Chem

Ligand: ibcasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.03000020980835 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: ilorasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 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: KBP-7018 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: ACS Med Chem Lett

Ligand: Ki-20227 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.659999847412109 pIC50
Reference (Journal): A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model.
Published in: Mol Cancer Ther

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.179999828338623 pIC50
Reference (Journal): Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.
Published in: Mol Cancer Ther

Ligand: lucitanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 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: M4205 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.59000015258789 pIC50
Reference (Journal): Identification of M4205&#x2500;A Highly Selective Inhibitor of KIT Mutations for Treatment of Unresectable Metastatic or Recurrent Gastrointestinal Stromal Tumors.
Published in: J Med Chem

Ligand: masitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.
Published in: PLoS ONE

Ligand: MK-2461 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Published in: Cancer Res

Ligand: naporafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 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: nintedanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 7.190000057220459 pIC50
Reference (Journal): BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Published in: Cancer Res

Ligand: orantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.300000190734863 pIC50
Reference (Journal): 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
Published in: Bioorg Med Chem Lett

Ligand: pazopanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2009), EMA (2010)
Primary target: no
Median affinity: 7.079999923706055 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: PD166285 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pKi
Reference (Journal): In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: PDGF receptor tyrosine kinase inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
Published in: J Med Chem

Ligand: PDGF receptor tyrosine kinase inhibitor IV (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.380000114440918 pIC50
Reference (Journal): (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.
Published in: J Med Chem

Ligand: PDGF RTK inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.920000076293945 pIC50
Reference (Journal): Identification of potent and selective inhibitors of PDGF receptor autophosphorylation.
Published in: J Med Chem

Ligand: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: no
Median affinity: 8.109999656677246 pKd
Reference (Journal): Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Published in: J Med Chem

Ligand: semaxanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.170000076293945 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: seralutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Non-selective kinase inhibitors

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 7.239999771118164 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: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 7.239999771118164 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: sotuletinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.230000019073486 pIC50
Reference (Journal): CSF1R inhibition delays cervical and mammary tumor growth in murine models by attenuating the turnover of tumor-associated macrophages and enhancing infiltration by CD8(+) T cells.
Published in: Oncoimmunology

Ligand: SU11652 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase.
Published in: J Med Chem

Ligand: SU-14813 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity.
Published in: Mol Cancer Ther

Ligand: SU5402 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pIC50
Reference (Journal): Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases.
Published in: J Med Chem

Ligand: sunitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: yes
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Activity-based kinase profiling of approved tyrosine kinase inhibitors.
Published in: Genes Cells

Ligand: sunitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: yes
Median affinity: 8.100000381469727 pKi
Reference (Journal): In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship.
Published in: Clin Cancer Res

Ligand: tafetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): Preclinical anti-angiogenesis and anti-tumor activity of SIM010603, an oral, multi-targets receptor tyrosine kinases inhibitor.
Published in: Cancer Chemother Pharmacol

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 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: tandutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML).
Published in: Cancer Cell

Ligand: vatalanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.21999979019165 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: zoligratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.25 pIC50
Reference (Journal): The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor.
Published in: Mol Cancer Ther