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

Ligand: AC710 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 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: BPR1R024 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.28000020980835 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: 7.440000057220459 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: 7.599999904632568 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 8h [PMID: 21561767] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
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: 8.520000457763672 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: 8.699999809265137 pIC50
Reference (Journal): The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: CP-673451 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 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: 8.680000305175781 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: 6.679999828338623 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: elenestinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Patent): Pyrrolotriazine derivatives for treating kit- and pdgfra-mediated diseases

Ligand: ENMD-2076 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.25 pIC50
Reference (Journal): Discovery and development of aurora kinase inhibitors as anticancer agents.
Published in: J Med Chem

Ligand: ibcasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 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: 7.960000038146973 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: lucitanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 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: 7.300000190734863 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: 6.269999980926514 pIC50
Reference (Journal): Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.
Published in: PLoS ONE

Ligand: nintedanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 7.230000019073486 pIC50
Reference (Journal): BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Published in: Cancer Res

Ligand: olaratumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2016)
Primary target: yes
Median affinity: 10.399999618530273 pKd
Reference (Patent): Antibodies against PDGFRa

Ligand: olaratumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: EMA & FDA (2016)
Primary target: yes
Median affinity: 9.239999771118164 pIC50
Reference (Patent): Antibodies against PDGFRa

Ligand: PDGF receptor tyrosine kinase inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.960000038146973 pIC50
Reference (Journal): Bis(1H-2-indolyl)methanones as a novel class of inhibitors of the platelet-derived growth factor receptor kinase.
Published in: J Med Chem

Ligand: PP121 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Published in: Nat Chem Biol

Ligand: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: no
Median affinity: 7.960000038146973 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: seralutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Non-selective kinase inhibitors

Ligand: sitravatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 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: toceranib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors.
Published in: Blood

Ligand: vimseltinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Patent): 2-aminopyrimidin-6-ones and analogs exhibiting anti-cancer and anti-proliferative activities