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Assay Detail

CHEMBL5530491

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

Binding
Inhibition of N-terminal 6His tagged FGFR4 (unknown origin) expressed in Escherichia coli (DE3) (NEB) using Tyr04 peptide as substrate incubated for 1 hr in presence of ATP by FRET based Z'-Lyte assay
32
Total Activities
32
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 of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
Yang F, Lin Q, Song X, Huang H, Chen X, Tan J, Li Y, Zhou Y, Tu Z, Du H, Zhang ZM, Ortega R, Lin X, Patterson AV, Smaill JB, Chen Y, Lu X.
J Med Chem (2024) 67 : 2667 -2689
PubMed 38348819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.52 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5566209 1 8.14
CHEMBL5218465 1 8.00
CHEMBL5574215 1 7.90
CHEMBL5572973 1 7.86
CHEMBL3908979 FGF401 2.0 1 7.82
CHEMBL5574272 1 7.79
CHEMBL5574432 1 7.72
CHEMBL5573876 1 7.71
CHEMBL5592963 1 7.70
CHEMBL5593772 1 7.69
CHEMBL5573924 1 7.69
CHEMBL5572412 1 7.67
CHEMBL5569572 1 7.66
CHEMBL5573260 1 7.65
CHEMBL5570327 1 7.64
CHEMBL5570394 1 7.63
CHEMBL5572074 1 7.61
CHEMBL5569989 1 7.59
CHEMBL5567251 1 7.58
CHEMBL5572370 1 7.57
CHEMBL5573334 1 7.53
CHEMBL5568894 1 7.52
CHEMBL5557003 1 7.47
CHEMBL5583995 1 7.41
CHEMBL5574356 1 7.40
CHEMBL5543045 1 7.25
CHEMBL5573735 1 7.05
CHEMBL5571014 1 6.93
CHEMBL5568669 1 6.93
CHEMBL5570698 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5566209 IC50 = 7.2 nM 8.14
CHEMBL5218465 IC50 = 10.0 nM 8.00
CHEMBL5574215 IC50 = 12.7 nM 7.90
CHEMBL5572973 IC50 = 13.7 nM 7.86
CHEMBL3908979 FGF401 IC50 = 15.0 nM 7.82
CHEMBL5574272 IC50 = 16.3 nM 7.79
CHEMBL5574432 IC50 = 19.1 nM 7.72
CHEMBL5573876 IC50 = 19.5 nM 7.71
CHEMBL5592963 IC50 = 20.0 nM 7.70
CHEMBL5593772 IC50 = 20.6 nM 7.69
CHEMBL5573924 IC50 = 20.5 nM 7.69
CHEMBL5572412 IC50 = 21.3 nM 7.67
CHEMBL5569572 IC50 = 22.1 nM 7.66
CHEMBL5573260 IC50 = 22.3 nM 7.65
CHEMBL5570327 IC50 = 22.9 nM 7.64
CHEMBL5570394 IC50 = 23.5 nM 7.63
CHEMBL5572074 IC50 = 24.5 nM 7.61
CHEMBL5569989 IC50 = 25.4 nM 7.59
CHEMBL5567251 IC50 = 26.1 nM 7.58
CHEMBL5572370 IC50 = 26.9 nM 7.57
CHEMBL5573334 IC50 = 29.7 nM 7.53
CHEMBL5568894 IC50 = 30.3 nM 7.52
CHEMBL5557003 IC50 = 34.0 nM 7.47
CHEMBL5583995 IC50 = 39.4 nM 7.41
CHEMBL5574356 IC50 = 39.8 nM 7.40
CHEMBL5543045 IC50 = 55.8 nM 7.25
CHEMBL5573735 IC50 = 88.9 nM 7.05
CHEMBL5571014 IC50 = 116.9 nM 6.93
CHEMBL5568669 IC50 = 117.9 nM 6.93
CHEMBL5570698 IC50 = 139.8 nM 6.85
CHEMBL5573605 IC50 = 161.2 nM 6.79
CHEMBL5584172 IC50 = 179.1 nM 6.75