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Assay Detail

CHEMBL5623901

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

Functional
Antiproliferative activity against mouse BaF3 cells harbouring ETV6-FGFR4-V550L mutant measured after 24 to 48 hrs by MTT assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.
Yang Y, He X, Li Z, Ran K, Wang N, Zhao L, Liu Z, Zeng J, Chang B, Feng Q, Zhang Q, Yu L.
Eur J Med Chem (2023) 258 : 115628 -115628
PubMed 37437349 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.40 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5630358 1 9.00
CHEMBL5625076 1 9.00
CHEMBL5630522 1 8.70
CHEMBL5630288 1 8.70
CHEMBL5630586 1 8.70
CHEMBL5625083 1 8.52
CHEMBL3828009 LY-2874455 1.0 1 8.15
CHEMBL4514636 FISOGATINIB 2.0 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5630358 IC50 = 1.0 nM 9.00
CHEMBL5625076 IC50 = 1.0 nM 9.00
CHEMBL5630522 IC50 = 2.0 nM 8.70
CHEMBL5630288 IC50 = 2.0 nM 8.70
CHEMBL5630586 IC50 = 2.0 nM 8.70
CHEMBL5625083 IC50 = 3.0 nM 8.52
CHEMBL3828009 LY-2874455 IC50 = 7.0 nM 8.15
CHEMBL4514636 FISOGATINIB IC50 = 396.0 nM 6.40