Target family: Type V RTKs: FGF (fibroblast growth factor) receptor family (type: catalytic_receptor)
Target: fibroblast growth factor receptor 3

Ligand: compound 29 [PMID: 36356320] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Published in: J Med Chem

Ligand: compound 7 [Nguyen et al., 2023] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.25 pIC50
Reference (Journal): Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach
Published in: ACS Medicinal Chemistry Letters

Ligand: derazantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation.
Published in: PLoS ONE

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: 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: erdafitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Patent): Pyrazolyl quinazoline kinase inhibitors.

Ligand: fexagratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Webpage): AZD4547.

Ligand: futibatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022), EMA (2023)
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Patent): 3,5-disubstituted alkynylbenzene compound and salt thereof

Ligand: infigratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021)
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Published in: J Med Chem

Ligand: LY2874455 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.1899995803833 pIC50
Reference (Journal): A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models.
Published in: Mol Cancer Ther

Ligand: MK-2461 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
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: 6.96999979019165 pIC50
Reference (Journal): BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Published in: Cancer Res

Ligand: pemigatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Substituted tricyclic compounds as FGFR inhibitors

Ligand: PRN1371 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 pIC50
Reference (Journal): Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Published in: J Med Chem

Ligand: rogaratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.610000133514404 pIC50
Reference (Patent): Disubstituted benzothienyl-pyrrolotriazines and their use as FGFR kinase inhibitors

Ligand: segigratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pIC50
Reference (Journal): Preclinical evaluation of 3D185, a novel potent inhibitor of FGFR1/2/3 and CSF-1R, in FGFR-dependent and macrophage-dominant cancer models.
Published in: J Exp Clin Cancer Res

Ligand: TAK-632 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 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: tasurgratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.270000457763672 pIC50
Reference (Patent): Monocyclic pyridine derivative

Ligand: tinengotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Patent): Multi-kinase inhibitor compound, and crystal form and use thereof

Ligand: zoligratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 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