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Assay Detail

CHEMBL5524869

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

Binding
Inhibition of wild-type FGFR2 (458 to 765 residues)(unknown origin) expressed in Escherichia coli using FLPeptide30 as substrate preincubated for 30 mins followed by ATP addition measured after 90 mins
1
Total Activities
1
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 of LHQ490 as a highly selective fibroblast growth factor receptor 2 (FGFR2) inhibitor.
Li H, Ke R, Zhou Y, Chang S, Wang J, Su C, Wu P, Yang B, Wang Z, Ding K, Ma D.
Eur J Med Chem (2024) 272 : 116473 -116473
PubMed 38718625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5314555 LIRAFUGRATINIB 2.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5314555 LIRAFUGRATINIB IC50 = 3.0 nM 8.52