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Assay Detail

CHEMBL5239776

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

Functional
Cytotoxicity against mouse BaF3 cells expressing wild type TEL-fused FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
5
Total Activities
5
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

Discovery of 2-Amino-7-sulfonyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidine Derivatives as Potent Reversible FGFR Inhibitors with Gatekeeper Mutation Tolerance: Design, Synthesis, and Biological Evaluation.
Xie W, Yang S, Liang L, Wang M, Zuo W, Lei Y, Zhang Y, Tang W, Lu T, Chen Y, Jiang Y.
J Med Chem (2022) 65 : 16570 -16588
PubMed 36480917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.11 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5290554 1 7.23
CHEMBL5283096 1 7.19
CHEMBL5281307 1 7.14
CHEMBL5278656 1 7.08
CHEMBL5289886 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5290554 IC50 = 58.3 nM 7.23
CHEMBL5283096 IC50 = 64.0 nM 7.19
CHEMBL5281307 IC50 = 71.8 nM 7.14
CHEMBL5278656 IC50 = 82.5 nM 7.08
CHEMBL5289886 IC50 = 126.4 nM 6.90