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Assay Detail

CHEMBL4400501

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

Binding
Inhibition of human FGFR3 V555M mutant using FL-peptide substrate measured after 45 mins in presence of ATP by mobility shift assay
6
Total Activities
6
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

Second-Generation FGFR Inhibitors for the Treatment of Cancers Harboring Mutated FGFRs.
Abdel-Magid AF.
ACS Med Chem Lett (2019) 10 : 1374 -1375
PubMed 31620219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.03 9.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4577380 1 9.67
CHEMBL4568760 1 9.58
CHEMBL4461304 1 9.54
CHEMBL4529789 1 9.39
CHEMBL4443370 1 9.39
CHEMBL4447174 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4577380 IC50 = 0.212 nM 9.67
CHEMBL4568760 IC50 = 0.2645 nM 9.58
CHEMBL4461304 IC50 = 0.2885 nM 9.54
CHEMBL4529789 IC50 = 0.41 nM 9.39
CHEMBL4443370 IC50 = 0.4081 nM 9.39
CHEMBL4447174 IC50 = 254.3 nM 6.59