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Assay Detail

CHEMBL5350190

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

Binding
Inhibition of FGFR2 (unknown origin) incubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo luminescence assay
3
Total Activities
3
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 2 (CHEMBL4142)
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 3 8.25 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5439595 1 8.51
CHEMBL5436527 1 8.28
CHEMBL1289601 LENVATINIB 4.0 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5439595 IC50 = 3.1 nM 8.51
CHEMBL5436527 IC50 = 5.2 nM 8.28
CHEMBL1289601 LENVATINIB IC50 = 11.0 nM 7.96