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Assay Detail

CHEMBL5508616

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

Binding
Inhibition of human FGFR3 (450 to 758 residues) using preincubated for 30 mins followed by ATP plus poly (4:1 glu, tyr) addition and measured after 30 mins by ADP-Glo reagent based plate reader analysis
5
Total Activities
5
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 3 (CHEMBL2742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of selective covalent inhibitors of FGFR4.
Chen X, Li H, Lin Q, Dai S, Qu L, Guo M, Zhang L, Liao J, Wei H, Xu G, Jiang L, Chen Y.
Eur J Med Chem (2024) 268 : 116281 -116281
PubMed 38432058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.35 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5558986 1 6.70
CHEMBL5565446 1 6.33
CHEMBL5560176 1 6.01
CHEMBL5559706 1 -
CHEMBL5556135 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5558986 IC50 = 201.0 nM 6.70
CHEMBL5565446 IC50 = 466.0 nM 6.33
CHEMBL5560176 IC50 = 977.0 nM 6.01
CHEMBL5559706 IC50 > 5000.0 nM -
CHEMBL5556135 IC50 > 5000.0 nM -