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Assay Detail

CHEMBL4723294

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

Binding
Inhibition of FGFR4 in mouse BAF3 cells assessed as reduction in cell viability incubated for 2 days by cell proliferation assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 4 (CHEMBL3839)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA,Knoepfel T,Buschmann N,Leblanc C,Mah R,Todorov M,Nimsgern P,Ripoche S,Niklaus M,Warin N,Luu VH,Madoerin M,Wirth J,Graus-Porta D,Weiss A,Kiffe M,Wartmann M,Kinyamu-Akunda J,Sterker D,Stamm C,Adler F,Buhles A,Schadt H,Couttet P,Blank J,Galuba I,Trappe J,Voshol J,Ostermann N,Zou C,Berghausen J,Del Rio Espinola A,Jahnke W,Furet P
J Med Chem (2020) 63 : 12542 -12573
PubMed 32930584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.99 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284069 1 8.31
CHEMBL3983290 1 8.02
CHEMBL3973674 1 7.92
CHEMBL3972276 1 7.89
CHEMBL3940572 1 7.75
CHEMBL3908044 1 7.66
CHEMBL4106685 1 7.66
CHEMBL3904499 1 7.66
CHEMBL3973588 1 7.55
CHEMBL4791610 1 7.48
CHEMBL3916036 1 7.44
CHEMBL4745615 1 7.41
CHEMBL4752511 1 7.34
CHEMBL4790514 1 7.18
CHEMBL4787060 1 7.17
CHEMBL3966721 1 7.14
CHEMBL3828009 LY-2874455 1.0 1 7.12
CHEMBL4786195 1 7.10
CHEMBL4758510 1 7.10
CHEMBL3973808 1 7.09
CHEMBL4781381 1 6.99
CHEMBL3920470 1 6.99
CHEMBL4754106 1 6.94
CHEMBL4294665 1 6.86
CHEMBL4780066 1 6.83
CHEMBL3971213 1 6.77
CHEMBL4789692 1 6.73
CHEMBL4744460 1 6.71
CHEMBL3954670 1 6.68
CHEMBL3953738 1 6.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284069 IC50 = 4.9 nM 8.31
CHEMBL3983290 IC50 = 9.5 nM 8.02
CHEMBL3973674 IC50 = 12.0 nM 7.92
CHEMBL3972276 IC50 = 13.0 nM 7.89
CHEMBL3940572 IC50 = 18.0 nM 7.75
CHEMBL3908044 IC50 = 22.0 nM 7.66
CHEMBL4106685 IC50 = 22.0 nM 7.66
CHEMBL3904499 IC50 = 22.0 nM 7.66
CHEMBL3973588 IC50 = 28.0 nM 7.55
CHEMBL4791610 IC50 = 33.0 nM 7.48
CHEMBL3916036 IC50 = 36.0 nM 7.44
CHEMBL4745615 IC50 = 39.0 nM 7.41
CHEMBL4752511 IC50 = 46.0 nM 7.34
CHEMBL4790514 IC50 = 66.0 nM 7.18
CHEMBL4787060 IC50 = 68.0 nM 7.17
CHEMBL3966721 IC50 = 72.0 nM 7.14
CHEMBL3828009 LY-2874455 IC50 = 76.0 nM 7.12
CHEMBL4786195 IC50 = 79.0 nM 7.10
CHEMBL4758510 IC50 = 80.0 nM 7.10
CHEMBL3973808 IC50 = 82.0 nM 7.09
CHEMBL4781381 IC50 = 103.0 nM 6.99
CHEMBL3920470 IC50 = 102.0 nM 6.99
CHEMBL4754106 IC50 = 114.0 nM 6.94
CHEMBL4294665 IC50 = 139.0 nM 6.86
CHEMBL4780066 IC50 = 148.0 nM 6.83
CHEMBL3971213 IC50 = 171.0 nM 6.77
CHEMBL4789692 IC50 = 185.0 nM 6.73
CHEMBL4744460 IC50 = 193.0 nM 6.71
CHEMBL3954670 IC50 = 211.0 nM 6.68
CHEMBL3953738 IC50 = 244.0 nM 6.61
CHEMBL3977760 IC50 = 301.0 nM 6.52
CHEMBL3957240 IC50 = 317.0 nM 6.50
CHEMBL3348846 FEXAGRATINIB IC50 = 348.0 nM 6.46
CHEMBL4785725 IC50 = 403.0 nM 6.39
CHEMBL3929437 IC50 = 441.0 nM 6.36
CHEMBL4777580 IC50 = 504.0 nM 6.30
CHEMBL3969343 IC50 = 537.0 nM 6.27
CHEMBL4778828 IC50 = 547.0 nM 6.26
CHEMBL4779862 IC50 = 573.0 nM 6.24
CHEMBL1852688 INFIGRATINIB IC50 = 581.0 nM 6.24
CHEMBL3905155 IC50 = 638.0 nM 6.20
CHEMBL4752290 IC50 = 1775.0 nM 5.75
CHEMBL3971045 IC50 > 3000.0 nM -
CHEMBL3926134 IC50 > 3000.0 nM -
CHEMBL4277111 IC50 > 3000.0 nM -