Target family: Type V RTKs: FGF (fibroblast growth factor) receptor family (type: catalytic_receptor)
Target: fibroblast growth factor receptor 4

Ligand: aldafermin (Peptide)
Interaction type: Agonist
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Separating Tumorigenicity from Bile Acid Regulatory Activity for Endocrine Hormone FGF19.
Published in: Cancer Res

Ligand: BLU-9931 (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway.
Published in: Cancer Discov

Ligand: compound 29 [PMID: 36356320] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 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: 6.449999809265137 pIC50
Reference (Journal): Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach
Published in: ACS Medicinal Chemistry Letters

Ligand: compound A34 [PMID: 35635004] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.270000457763672 pIC50
Reference (Journal): Discovery of 1,6-Naphthyridin-2(1<i>H</i>)-one Derivatives as Novel, Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma.
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: 8.25 pIC50
Reference (Patent): Pyrazolyl quinazoline kinase inhibitors.

Ligand: fexagratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.78000020980835 pIC50
Reference (Webpage): AZD4547.

Ligand: FGF-19 (Peptide)
Interaction type: Agonist
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): FGF-19, a novel fibroblast growth factor with unique specificity for FGFR4.
Published in: Cytokine

Ligand: fisogatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.0600004196167 pIC50
Reference (Journal): Discovery of 1,6-Naphthyridin-2(1<i>H</i>)-one Derivatives as Novel, Potent, and Selective FGFR4 Inhibitors for the Treatment of Hepatocellular Carcinoma.
Published in: J Med Chem

Ligand: fisogatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8 pIC50
Reference (Patent): Inhibitors of the fibroblast growth factor receptor

Ligand: futibatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2022), EMA (2023)
Primary target: no
Median affinity: 8.470000267028809 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: no
Median affinity: 7.21999979019165 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: irpagratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.069999694824219 pIC50
Reference (Patent): FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof

Ligand: LY2874455 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 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: nintedanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 6.210000038146973 pIC50
Reference (Journal): BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.
Published in: Cancer Res

Ligand: PRN1371 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.710000038146973 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: roblitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.720000267028809 pIC50
Reference (Patent): Ring-fused bicyclic pyridyl derivatives as FGFR4 inhibitors

Ligand: segigratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.289999961853027 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: tasurgratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.190000057220459 pIC50
Reference (Patent): Monocyclic pyridine derivative

Ligand: zoligratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.539999961853027 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