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Assay Detail

CHEMBL4723223

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

Functional
In vivo inhibition of FGFR4 in mouse xenografted with human Hep3B cells assessed as decrease in FGFR4 phosphorylation
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC90 1 - -
IC50 1 8.54 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3973674 2 8.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3973674 IC50 = 2.9 nM 8.54
CHEMBL3973674 IC90 = 72.0 nM -