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Assay Detail

CHEMBL5530494

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Functional
Antiproliferative activity against FGFR4 independent human NCI-H1299 cells assessed as inhibition of cell growth
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1299
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1299 (CHEMBL612255)
Type CELL-LINE
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 13 5.01 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5218465 1 5.89
CHEMBL5571014 1 5.62
CHEMBL5583995 1 5.46
CHEMBL5573605 1 5.37
CHEMBL5566209 1 5.23
CHEMBL5557003 1 4.94
CHEMBL5573735 1 4.93
CHEMBL5584172 1 4.89
CHEMBL3908979 FGF401 2.0 1 4.82
CHEMBL5568669 1 4.69
CHEMBL5574215 1 4.63
CHEMBL5572973 1 4.44
CHEMBL5543045 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5218465 IC50 = 1300.0 nM 5.89
CHEMBL5571014 IC50 = 2400.0 nM 5.62
CHEMBL5583995 IC50 = 3500.0 nM 5.46
CHEMBL5573605 IC50 = 4300.0 nM 5.37
CHEMBL5566209 IC50 = 5900.0 nM 5.23
CHEMBL5557003 IC50 = 11600.0 nM 4.94
CHEMBL5573735 IC50 = 11700.0 nM 4.93
CHEMBL5584172 IC50 = 12900.0 nM 4.89
CHEMBL3908979 FGF401 IC50 = 15300.0 nM 4.82
CHEMBL5568669 IC50 = 20600.0 nM 4.69
CHEMBL5574215 IC50 = 23600.0 nM 4.63
CHEMBL5572973 IC50 = 36600.0 nM 4.44
CHEMBL5543045 IC50 = 56000.0 nM 4.25