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Assay Detail

CHEMBL4723266

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

Binding
Inhibition of recombinant non-phosphorylated FGFR4 N535K mutant kinase domain (442 to 753) (unknown origin) expressed in Sf9 insect cells using 5-Fluo-Ahx-KKKKEEIYFFFG-NH2 peptide as substrate in presence of ATP measured after 60 mins by caliper microfluidic mobility shift assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
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
IC50 1 9.05 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3973674 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3973674 IC50 = 0.9 nM 9.05