Target family: Type XIV RTKs: RET (type: catalytic_receptor)
Target: ret proto-oncogene

Ligand: compound 8h [PMID: 21561767] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 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: gilteritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor.
Published in: Blood

Ligand: KBP-7018 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.119999885559082 pIC50
Reference (Journal): Discovery of Indolinone-Based Multikinase Inhibitors as Potential Therapeutics for Idiopathic Pulmonary Fibrosis.
Published in: ACS Med Chem Lett

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.71999979019165 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: 6.699999809265137 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: lunbotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Patent): Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof

Ligand: RG-1530 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pKd
Reference (Journal): Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.
Published in: Cell Cycle

Ligand: lunbotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.989999771118164 pIC50
Reference (Patent): Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof

Ligand: lunbotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.880000114440918 pIC50
Reference (Patent): Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof

Ligand: lunbotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.180000305175781 pIC50
Reference (Patent): Heterocyclic compound, pharmaceutical composition comprising same, preparation method therefor, and use thereof

Ligand: ponatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Ponatinib is a potent inhibitor of wild-type and drug-resistant gatekeeper mutant RET kinase.
Published in: Mol Cell Endocrinol

Ligand: pralsetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: yes
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Precision Targeted Therapy with BLU-667 for <i>RET</i>-Driven Cancers.
Published in: Cancer Discov

Ligand: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: no
Median affinity: 8 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: resencatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.470000267028809 pIC50
Reference (Patent): Inhibitor containing bicyclic derivative, preparation method therefor and use thereof

Ligand: selpercatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Patent): Substituted pyrazolo[1,5-a]pyridine compounds as ret 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: 7.900000095367432 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: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): Activity-based kinase profiling of approved tyrosine kinase inhibitors.
Published in: Genes Cells

Ligand: tafetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 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: tamatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Developmental toxicity associated with receptor tyrosine kinase Ret inhibition in reproductive toxicity testing.
Published in: Birth Defects Res Part A Clin Mol Teratol

Ligand: vandetanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Precision Targeted Therapy with BLU-667 for <i>RET</i>-Driven Cancers.
Published in: Cancer Discov

Ligand: vandetanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: yes
Median affinity: 7.46999979019165 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: vandetanib (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): ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases.
Published in: Cancer Res

Ligand: vepafestinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Patent): Novel fused pyrimidine compound or salt thereof

Ligand: WF-47-JS03 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma
Published in: ACS Med Chem Lett

Ligand: WF-47-JS03 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma
Published in: ACS Med Chem Lett

Ligand: zeteletinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.34000015258789 pIC50
Reference (Patent): Pyridine compound

Ligand: rivoceranib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: 2014 (Chinese NMPA)
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo.
Published in: Cancer Sci

Ligand: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.059999942779541 pIC50
Reference (Journal): The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells.
Published in: Cancer Res

Ligand: cabozantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2014)
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Precision Targeted Therapy with BLU-667 for <i>RET</i>-Driven Cancers.
Published in: Cancer Discov

Ligand: CEP-11981 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 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: compound 1d [PMID: 21493067] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pIC50
Reference (Journal): In vitro and in vivo evaluation of 6-aminopyrazolyl-pyridine-3-carbonitriles as JAK2 kinase inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 1 [PMID: 34917254] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.170000076293945 pIC50
Reference (Journal): Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-<i>d</i>]pyrimidine RET Inhibitors.
Published in: ACS Med Chem Lett