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Assay Detail

CHEMBL5548031

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

Binding
Inhibition of full length nanoluc-fused FGFR4 transfected in HEK293T cells assessed as target engagement incubated for 3 hrs in presence of K10 tracer by Nano BRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on S<sub>N</sub>Ar Electrophiles.
Schwarz M, Kurkunov M, Wittlinger F, Rudalska R, Wang G, Schwalm MP, Rasch A, Wagner B, Laufer SA, Knapp S, Dauch D, Gehringer M.
J Med Chem (2024) 67 : 6549 -6569
PubMed 38604131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.01 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068896 1 7.57
CHEMBL5570033 1 7.52
CHEMBL5571683 1 7.28
CHEMBL5575075 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068896 EC50 = 27.0 nM 7.57
CHEMBL5570033 EC50 = 30.0 nM 7.52
CHEMBL5571683 EC50 = 52.0 nM 7.28
CHEMBL5575075 EC50 = 2256.0 nM 5.65