Target family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family (type: catalytic_receptor)
Target: fms related receptor tyrosine kinase 3

Ligand: AC710 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 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: AKN-028 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pIC50
Reference (Journal): The novel tyrosine kinase inhibitor AKN-028 has significant antileukemic activity in cell lines and primary cultures of acute myeloid leukemia.
Published in: Blood Cancer J

Ligand: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.28000020980835 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: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.920000076293945 pKi
Reference (Journal): Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells.
Published in: Blood

Ligand: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.100000381469727 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: BAY-985 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.909999847412109 pIC50
Reference (Journal): Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor.
Published in: J Med Chem

Ligand: belizatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.380000114440918 pKd
Reference (Journal): The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Published in: J Med Chem

Ligand: BMS-690514 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.960000038146973 pIC50
Reference (Journal): Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2.
Published in: J Pharm Sci

Ligand: cediranib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 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: ceritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2014), EMA (2015)
Primary target: no
Median affinity: 7.21999979019165 pIC50
Reference (Journal): Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Published in: J Med Chem

Ligand: compound 13ac [PMID: 33256400] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.210000038146973 pIC50
Reference (Journal): <i>N</i>-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
Published in: J Med Chem

Ligand: compound 14k [PMID: 21982499] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.980000019073486 pIC50
Reference (Journal): 7-(4H-1,2,4-Triazol-3-yl)benzo[c][2,6]naphthyridines: a novel class of Pim kinase inhibitors with potent cell antiproliferative activity.
Published in: Bioorg Med Chem Lett

Ligand: compound 18e [PMID: 31670517] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of Potent and Orally Effective Dual Janus Kinase 2/FLT3 Inhibitors for the Treatment of Acute Myelogenous Leukemia and Myeloproliferative Neoplasms.
Published in: J Med Chem

Ligand: compound 1 [Cruz-López et al., 2019] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.269999980926514 pIC50
Reference (Journal): Synthesis and Characterization of a Click-Assembled 18-Atom Macrocycle That Displays Selective AXL Kinase Inhibitory Activity.
Published in: ACS Omega

Ligand: compound 25ap [PMID: 37796543] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Discovery of Novel Fedratinib-Based HDAC/JAK/BRD4 Triple Inhibitors with Remarkable Antitumor Activity against Triple Negative Breast Cancer.
Published in: J Med Chem

Ligand: compound 2c [PMID: 24900538] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.680000305175781 pIC50
Reference (Journal): Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
Published in: ACS Med Chem Lett

Ligand: compound 34f [PMID: 37535845] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-<i>b</i>]pyridazine Derivatives Identified by Scaffold Hopping.
Published in: J Med Chem

Ligand: compound 34f [PMID: 37535845] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Inhibition of FLT3-ITD Kinase in Acute Myeloid Leukemia by New Imidazo[1,2-<i>b</i>]pyridazine Derivatives Identified by Scaffold Hopping.
Published in: J Med Chem

Ligand: compound 5e [PMID: 28580438] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.4399995803833 pKd
Reference (Journal): Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia.
Published in: ACS Omega

Ligand: compound 6li [Chan et al., 2022] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Journal): Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors
Published in: Journal of Nedicinal Chemistry

Ligand: compound 7d [PMID: 29672049] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of N<sup>2</sup>-(4-Amino-cyclohexyl)-9-cyclopentyl- N<sup>6</sup>-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations.
Published in: J Med Chem

Ligand: compound 8h [PMID: 22765894] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.069999694824219 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: 9.100000381469727 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: crenolanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.130000114440918 pKd
Reference (Journal): Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors.
Published in: Clin Cancer Res

Ligand: denfivontinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.399999618530273 pIC50
Reference (Journal): G-749, a novel FLT3 kinase inhibitor, can overcome drug resistance for the treatment of acute myeloid leukemia.
Published in: Blood

Ligand: dorsomorphin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 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: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
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: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.1899995803833 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
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: edicotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.
Published in: J Rheumatol

Ligand: ENMD-2076 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery and development of aurora kinase inhibitors as anticancer agents.
Published in: J Med Chem

Ligand: Flt-3 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.380000114440918 pIC50
Reference (Journal): Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
Published in: Bioorg Med Chem Lett

Ligand: Flt-3 inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.480000019073486 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: Flt-3 inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Aromatic interactions with phenylalanine 691 and cysteine 828: a concept for FMS-like tyrosine kinase-3 inhibition. Application to the discovery of a new class of potential antileukemia agents.
Published in: J Med Chem

Ligand: Fms-related tyrosine kinase 3 ligand (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: gilteritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Preclinical studies of gilteritinib, a next-generation FLT3 inhibitor.
Published in: Blood

Ligand: Gö 6976 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Gö6976, a FLT3 kinase inhibitor, exerts potent cytotoxic activity against acute leukemia via inhibition of survivin and MCL-1.
Published in: Biochem Pharmacol

Ligand: GTP-14564 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.519999980926514 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: 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: JNJ-28312141 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia.
Published in: Mol Cancer Ther

Ligand: KW-2449 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: KW-2449 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.180000305175781 pIC50
Reference (Journal): KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation.
Published in: Blood

Ligand: lestaurtinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.069999694824219 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.199999809265137 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.
Published in: Mol Cancer Ther

Ligand: LWY713 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo activity against acute myeloid leukemia.
Published in: Eur J Med Chem

Ligand: MELK-TI (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Published in: ACS Med Chem Lett

Ligand: merestinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.510000228881836 pIC50
Reference (Journal): LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.
Published in: Invest New Drugs

Ligand: midostaurin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2017)
Primary target: yes
Median affinity: 7.960000038146973 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: mivavotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.34000015258789 pIC50
Reference (Journal): Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
Published in: Bioorg Med Chem Lett

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: nefextinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.550000190734863 pIC50
Reference (Patent): Fused pyrimidine compound, and intermediate, preparation method, composition and application of

Ligand: nefextinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.470000267028809 pIC50
Reference (Patent): Fused pyrimidine compound, and intermediate, preparation method, composition and application of

Ligand: nefextinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Patent): Fused pyrimidine compound, and intermediate, preparation method, composition and application of

Ligand: nuvisertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): A small-molecule inhibitor of PIM kinases as a potential treatment for urothelial carcinomas.
Published in: Neoplasia

Ligand: onvansertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pIC50
Reference (Journal): NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor.
Published in: Bioorg Med Chem Lett

Ligand: pacritinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022)
Primary target: no
Median affinity: 7.659999847412109 pIC50
Reference (Journal): Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
Published in: J Med Chem

Ligand: pexidartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 6.800000190734863 pIC50
Reference (Journal): Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
Published in: N Engl J Med

Ligand: PF-562271 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pIC50
Reference (Journal): Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271.
Published in: Cancer Res

Ligand: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: yes
Median affinity:  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: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: yes
Median affinity: 8.380000114440918 pIC50
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood

Ligand: quizartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2019), FDA (2023)
Primary target: yes
Median affinity:  pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: RG-1530 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pKd
Reference (Journal): Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy.
Published in: Cell Cycle

Ligand: RGB-286638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Published in: Leukemia

Ligand: ruserontinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.260000228881836 pIC50
Reference (Journal): SKLB1028, a novel oral multikinase inhibitor of EGFR, FLT3 and Abl, displays exceptional activity in models of FLT3-driven AML and considerable potency in models of CML harboring Abl mutants.
Published in: Leukemia

Ligand: SGI-1776 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.360000133514404 pIC50
Reference (Journal): Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Published in: J Med Chem

Ligand: sitravatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 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: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: yes
Median affinity: 7.480000019073486 pIC50
Reference (Journal): VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer.
Published in: Cancer Res

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: yes
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: sunitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA and EMA (2006)
Primary target: no
Median affinity: 8.1899995803833 pIC50
Reference (Journal): Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors.
Published in: Bioorg Med Chem

Ligand: tafetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 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: tandutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.659999847412109 pIC50
Reference (Journal): CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML).
Published in: Cancer Cell

Ligand: tandutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: TTT-3002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.140000343322754 pIC50
Reference (Journal): TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo.
Published in: Blood

Ligand: tuspetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Patent): Pyrimidine compounds and pharmaceutical compositions for preventing or treating cancers including the same

Ligand: UNC4203 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.789999961853027 pKi
Reference (Journal): Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Published in: J Med Chem

Ligand: UNC8969 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.150000095367432 pIC50
Reference (Journal): Discovery of Novel Macrocyclic MERTK/AXL Dual Inhibitors.
Published in: J Med Chem

Ligand: URMC-099 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.
Published in: J Med Chem

Ligand: zotiraciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.
Published in: Leukemia

Ligand: zotiraciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer.
Published in: J Med Chem