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Assay Detail

CHEMBL5350192

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of FGFR4 (unknown origin) incubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo luminescence assay
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 4 (CHEMBL3973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structural Optimization of Novel Quinolone Derivatives as Potent Irreversible Pan-Fibroblast Growth Factor Receptor Inhibitors for Treating Solid Tumors.
Hu S, Liu Y, Ma J, Ding W, Chen H, Jiang H, Chen H, Wei S, Liu Y, Jin Q, Yuan H, Yan L.
J Med Chem (2023) 66 : 8858 -8875
PubMed 37335602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.90 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439595 1 8.74
CHEMBL1289601 LENVATINIB 4.0 2 8.72
CHEMBL5425019 1 8.60
CHEMBL5434390 1 8.54
CHEMBL5431098 1 8.34
CHEMBL5439019 1 8.33
CHEMBL5427478 1 8.24
CHEMBL5420584 1 8.15
CHEMBL5419075 1 7.91
CHEMBL5440092 1 7.84
CHEMBL5411218 1 7.82
CHEMBL5409484 1 7.77
CHEMBL5404060 1 7.74
CHEMBL5436527 1 6.64
CHEMBL5403709 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439595 IC50 = 1.8 nM 8.74
CHEMBL1289601 LENVATINIB IC50 = 1.9 nM 8.72
CHEMBL5425019 IC50 = 2.49 nM 8.60
CHEMBL5434390 IC50 = 2.88 nM 8.54
CHEMBL5431098 IC50 = 4.6 nM 8.34
CHEMBL5439019 IC50 = 4.65 nM 8.33
CHEMBL5427478 IC50 = 5.73 nM 8.24
CHEMBL5420584 IC50 = 7.04 nM 8.15
CHEMBL5419075 IC50 = 12.36 nM 7.91
CHEMBL5440092 IC50 = 14.48 nM 7.84
CHEMBL5411218 IC50 = 15.0 nM 7.82
CHEMBL5409484 IC50 = 17.02 nM 7.77
CHEMBL5404060 IC50 = 18.04 nM 7.74
CHEMBL5436527 IC50 = 230.0 nM 6.64
CHEMBL5403709 IC50 = 294.2 nM 6.53
CHEMBL1289601 LENVATINIB IC50 = 311.0 nM 6.51