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Assay Detail

CHEMBL5217749

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

Binding
Inhibition of N-terminal 6His-tagged FGFR4 (unknown origin) 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

Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2-<i>b</i>]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.
Yang F, Chen X, Song X, Ortega R, Lin X, Deng W, Guo J, Tu Z, Patterson AV, Smaill JB, Chen Y, Lu X.
J Med Chem (2022) 65 : 14809 -14831
PubMed 36278929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.70 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5220871 1 8.80
CHEMBL5218602 1 8.72
CHEMBL5218768 1 8.62
CHEMBL5220411 1 8.52
CHEMBL5219987 1 8.19
CHEMBL5218465 1 8.00
CHEMBL5220465 1 7.96
CHEMBL3908979 FGF401 2.0 1 7.92
CHEMBL5220013 1 7.92
CHEMBL5219759 1 7.89
CHEMBL5218776 1 7.85
CHEMBL5219980 1 7.82
CHEMBL5220583 1 7.80
CHEMBL5220381 1 7.80
CHEMBL5219850 1 7.75
CHEMBL5220764 1 7.75
CHEMBL5220620 1 7.75
CHEMBL5218566 1 7.72
CHEMBL5220860 1 7.68
CHEMBL5219709 1 7.57
CHEMBL5218951 1 7.57
CHEMBL5219434 1 7.57
CHEMBL5219757 1 7.55
CHEMBL5220291 1 7.46
CHEMBL5219465 1 7.41
CHEMBL5219501 1 7.40
CHEMBL5221064 1 7.40
CHEMBL5220403 1 7.38
CHEMBL5218808 1 7.35
CHEMBL5218837 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5220871 IC50 = 1.6 nM 8.80
CHEMBL5218602 IC50 = 1.9 nM 8.72
CHEMBL5218768 IC50 = 2.4 nM 8.62
CHEMBL5220411 IC50 = 3.0 nM 8.52
CHEMBL5219987 IC50 = 6.4 nM 8.19
CHEMBL5218465 IC50 = 10.0 nM 8.00
CHEMBL5220465 IC50 = 11.0 nM 7.96
CHEMBL3908979 FGF401 IC50 = 12.0 nM 7.92
CHEMBL5220013 IC50 = 12.0 nM 7.92
CHEMBL5219759 IC50 = 13.0 nM 7.89
CHEMBL5218776 IC50 = 14.0 nM 7.85
CHEMBL5219980 IC50 = 15.0 nM 7.82
CHEMBL5220583 IC50 = 16.0 nM 7.80
CHEMBL5220381 IC50 = 16.0 nM 7.80
CHEMBL5220764 IC50 = 18.0 nM 7.75
CHEMBL5220620 IC50 = 18.0 nM 7.75
CHEMBL5219850 IC50 = 18.0 nM 7.75
CHEMBL5218566 IC50 = 19.0 nM 7.72
CHEMBL5220860 IC50 = 21.0 nM 7.68
CHEMBL5219709 IC50 = 27.0 nM 7.57
CHEMBL5218951 IC50 = 27.0 nM 7.57
CHEMBL5219434 IC50 = 27.0 nM 7.57
CHEMBL5219757 IC50 = 28.0 nM 7.55
CHEMBL5220291 IC50 = 35.0 nM 7.46
CHEMBL5219465 IC50 = 39.0 nM 7.41
CHEMBL5219501 IC50 = 40.0 nM 7.40
CHEMBL5221064 IC50 = 40.0 nM 7.40
CHEMBL5220403 IC50 = 42.0 nM 7.38
CHEMBL5218808 IC50 = 45.0 nM 7.35
CHEMBL5218837 IC50 = 178.0 nM 6.75
CHEMBL5219150 IC50 = 362.0 nM 6.44
CHEMBL5219257 IC50 = 578.0 nM 6.24