Pharos : Ligand Details - erdafitinib

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Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer.

Ligand Summary

Ligand Structure

Rendered image for the query structure

Synonyms & Links

UNII: 890E37NHMV

PubChem: 67462786

Guide to Pharmacology: 9039

ChEMBL: CHEMBL3545376

DrugCentral: 5327

LyCHI: YQ15HNNJQ6JG

Target Activities

Explore Associated and Predicted Targets

FGFR3

Tclin

Fibroblast growth factor receptor 3

9 Activities

Items per page:

1 – 9 of 9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	8.52

IC50	8.52		MedChemComm, (2019) 10:9:1509

IC50	8.52		J Med Chem, (2019) 62:6:2905	30403487

IC50	8.52		Bioorg Med Chem, (2020) 28:10:115453	32278710

IC50	8.42		None, (2014) None:None:None

IC50	8.42

IC50	7.8		None, (2014) None:None:None

IC50	7.8

IC50	8.52	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf

FGFR1

Tclin

Fibroblast growth factor receptor 1

5 Activities

Items per page:

1 – 5 of 5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	8.94

IC50	8.92		J Med Chem, (2019) 62:6:2905	30403487

IC50	8.73		None, (2014) None:None:None

IC50	8.73

IC50	8.92	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf

FGFR2

Tclin

Fibroblast growth factor receptor 2

5 Activities

Items per page:

1 – 5 of 5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	8.64

IC50	8.6		J Med Chem, (2019) 62:6:2905	30403487

IC50	8.35		None, (2014) None:None:None

IC50	8.35

IC50	8.6	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf

FGFR4

Tclin

Fibroblast growth factor receptor 4

5 Activities

Items per page:

1 – 5 of 5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	8.25

IC50	8.24		J Med Chem, (2019) 62:6:2905	30403487

IC50	8.18		None, (2014) None:None:None

IC50	8.18

IC50	8.24	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf

KDR

Tclin

Vascular endothelial growth factor receptor 2

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.44

IC50	7.43	INHIBITOR	https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212018s000lbl.pdf