erdafitinib
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
UNII: 890E37NHMV
PubChem: 67462786
Guide to Pharmacology: 9039
ChEMBL: CHEMBL3545376
DrugCentral: 5327
LyCHI: YQ15HNNJQ6JG
Target Activities
FGFR3
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 | ||||
IC50 | 8.52 | Bioorg Med Chem, (2020) 28:10:115453 | ||||
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 | ||||
FGFR1
Fibroblast growth factor receptor 1
5 Activities
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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 | ||||
IC50 | 8.73 | None, (2014) None:None:None | ||||
IC50 | 8.73 | |||||
IC50 | 8.92 | INHIBITOR | ||||
FGFR2
Fibroblast growth factor receptor 2
5 Activities
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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 | ||||
IC50 | 8.35 | None, (2014) None:None:None | ||||
IC50 | 8.35 | |||||
IC50 | 8.6 | INHIBITOR | ||||
FGFR4
Fibroblast growth factor receptor 4
5 Activities
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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 | ||||
IC50 | 8.18 | None, (2014) None:None:None | ||||
IC50 | 8.18 | |||||
IC50 | 8.24 | INHIBITOR | ||||
KDR
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 | ||||