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Assay Detail

CHEMBL4313069

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

Binding
Inhibition of human FGFR3 using poly (Glu, Tyr)4:1 as substrate measured after 60 mins by ELISA
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fibroblast growth factor receptor 3 (CHEMBL2742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Development of a Series of Pyrazolo[3,4-<i>d</i>]pyridazinone Compounds as the Novel Covalent Fibroblast Growth Factor Receptor Inhibitors by the Rational Drug Design.
Wang Y, Dai Y, Wu X, Li F, Liu B, Li C, Liu Q, Zhou Y, Wang B, Zhu M, Cui R, Tan X, Xiong Z, Liu J, Tan M, Xu Y, Geng M, Jiang H, Liu H, Ai J, Zheng M.
J Med Chem (2019) 62 : 7473 -7488
PubMed 31335138 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.06 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3348846 FEXAGRATINIB 2.0 1 8.47
CHEMBL4541330 1 7.90
CHEMBL4446835 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3348846 FEXAGRATINIB IC50 = 3.4 nM 8.47
CHEMBL4541330 IC50 = 12.5 nM 7.90
CHEMBL4446835 IC50 = 15.0 nM 7.82