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Assay Detail

CHEMBL4723295

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

Binding
Inhibition of FGFR4 in mouse BAF3 cells assessed as decrease in FGFR4 phosphorylation incubated for 40 mins
76
Total Activities
76
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 76 7.58 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4796410 1 8.60
CHEMBL4781882 1 8.54
CHEMBL4790514 1 8.43
CHEMBL3946444 1 8.42
CHEMBL4752511 1 8.41
CHEMBL3973674 1 8.37
CHEMBL4745780 1 8.35
CHEMBL3968334 1 8.35
CHEMBL4791610 1 8.32
CHEMBL4784243 1 8.30
CHEMBL4758510 1 8.30
CHEMBL4745615 1 8.28
CHEMBL4787060 1 8.24
CHEMBL4754106 1 8.24
CHEMBL4784921 1 8.23
CHEMBL4786195 1 8.21
CHEMBL4764394 1 8.15
CHEMBL4778828 1 8.15
CHEMBL3972276 1 8.12
CHEMBL4284069 1 8.08
CHEMBL3912070 1 8.06
CHEMBL3983290 1 8.06
CHEMBL4742811 1 8.02
CHEMBL3828009 LY-2874455 1.0 1 8.00
CHEMBL4789692 1 7.96
CHEMBL4781381 1 7.92
CHEMBL4106685 1 7.92
CHEMBL4756889 1 7.89
CHEMBL3916036 1 7.85
CHEMBL3955498 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4796410 IC50 = 2.5 nM 8.60
CHEMBL4781882 IC50 = 2.9 nM 8.54
CHEMBL4790514 IC50 = 3.7 nM 8.43
CHEMBL3946444 IC50 = 3.8 nM 8.42
CHEMBL4752511 IC50 = 3.9 nM 8.41
CHEMBL3973674 IC50 = 4.3 nM 8.37
CHEMBL4745780 IC50 = 4.5 nM 8.35
CHEMBL3968334 IC50 = 4.5 nM 8.35
CHEMBL4791610 IC50 = 4.8 nM 8.32
CHEMBL4784243 IC50 = 5.0 nM 8.30
CHEMBL4758510 IC50 = 5.0 nM 8.30
CHEMBL4745615 IC50 = 5.3 nM 8.28
CHEMBL4787060 IC50 = 5.7 nM 8.24
CHEMBL4754106 IC50 = 5.8 nM 8.24
CHEMBL4784921 IC50 = 5.9 nM 8.23
CHEMBL4786195 IC50 = 6.1 nM 8.21
CHEMBL4764394 IC50 = 7.0 nM 8.15
CHEMBL4778828 IC50 = 7.1 nM 8.15
CHEMBL3972276 IC50 = 7.5 nM 8.12
CHEMBL4284069 IC50 = 8.3 nM 8.08
CHEMBL3912070 IC50 = 8.7 nM 8.06
CHEMBL3983290 IC50 = 8.7 nM 8.06
CHEMBL4742811 IC50 = 9.5 nM 8.02
CHEMBL3828009 LY-2874455 IC50 = 10.0 nM 8.00
CHEMBL4789692 IC50 = 11.0 nM 7.96
CHEMBL4781381 IC50 = 12.0 nM 7.92
CHEMBL4106685 IC50 = 12.0 nM 7.92
CHEMBL4756889 IC50 = 13.0 nM 7.89
CHEMBL3916036 IC50 = 14.0 nM 7.85
CHEMBL3955498 IC50 = 17.0 nM 7.77
CHEMBL3904499 IC50 = 17.0 nM 7.77
CHEMBL4764678 IC50 = 17.0 nM 7.77
CHEMBL4780066 IC50 = 17.0 nM 7.77
CHEMBL3925900 IC50 = 18.0 nM 7.75
CHEMBL3908044 IC50 = 18.0 nM 7.75
CHEMBL4777580 IC50 = 19.0 nM 7.72
CHEMBL4759211 IC50 = 20.0 nM 7.70
CHEMBL3951479 IC50 = 21.0 nM 7.68
CHEMBL4758832 IC50 = 23.0 nM 7.64
CHEMBL3950552 IC50 = 23.0 nM 7.64
CHEMBL4744460 IC50 = 23.0 nM 7.64
CHEMBL3940572 IC50 = 24.0 nM 7.62
CHEMBL4752290 IC50 = 27.0 nM 7.57
CHEMBL3904341 IC50 = 28.0 nM 7.55
CHEMBL3973588 IC50 = 29.0 nM 7.54
CHEMBL3964830 IC50 = 34.0 nM 7.47
CHEMBL3966721 IC50 = 39.0 nM 7.41
CHEMBL4779862 IC50 = 40.0 nM 7.40
CHEMBL4287768 IC50 = 41.0 nM 7.39
CHEMBL3905155 IC50 = 42.0 nM 7.38