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Assay Detail

CHEMBL5258351

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

Binding
Inhibition of FGFR3 phosphorylation in mouse BaF3 cells incubated for 2 hrs
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 3 (CHEMBL4066)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.
Nguyen MH, Ye HF, Xu Y, Truong L, Horsey A, Zhao P, Styduhar ED, Frascella M, Leffet L, Federowicz K, Behshad E, Wang A, Zhang K, Witten MR, Qi C, Jalluri R, Lai CT, Atasoylu O, Harris JJ, Hess R, Lin L, Zhang G, Covington M, Diamond S, Yao W, Vechorkin O.
ACS Med Chem Lett (2023) 14 : 312 -318
PubMed 36923909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.48 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5286909 1 7.80
CHEMBL5290074 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5286909 IC50 = 16.0 nM 7.80
CHEMBL5290074 IC50 = 70.0 nM 7.16