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Assay Detail

CHEMBL5161322

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

Binding
Inhibition of FGFR4 V550L mutant (unknown orgin) using poly(Glu, Tyr) 4:1 peptide as substrate incubated for 30 mins in presence of 50 uM ATP by ADP-Glo fluorescence assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
Shao M, Chen X, Yang F, Song X, Zhou Y, Lin Q, Fu Y, Ortega R, Lin X, Tu Z, Patterson AV, Smaill JB, Chen Y, Lu X.
J Med Chem (2022) 65 : 5113 -5133
PubMed 35271262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.29 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5194425 1 9.60
CHEMBL5169893 1 8.89
CHEMBL5198859 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5194425 IC50 = 0.25 nM 9.60
CHEMBL5169893 IC50 = 1.3 nM 8.89
CHEMBL5198859 IC50 = 407.0 nM 6.39