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Assay Detail

CHEMBL5243510

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

Binding
Inhibition of Src kinase (unknown origin) phosphorylation at Tyr416/419 residues incubated for 24 hrs by Western blot analysis
4
Total Activities
4
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

Proto-oncogene tyrosine-protein kinase Src (CHEMBL267)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Aminopyrazolopyrimidine scaffold and its deformation in the design of tyrosine and serine/threonine kinase inhibitors in medicinal chemistry.
Chen X, Huang Y, Xu W, Cai Y, Yang Y.
RSC Med Chem (2022) 13 : 1008 -1028
PubMed 36324498 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.14 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5268244 1 8.64
CHEMBL5280361 1 8.17
CHEMBL45177 1 8.05
CHEMBL475584 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5268244 IC50 = 2.3 nM 8.64
CHEMBL5280361 IC50 = 6.8 nM 8.17
CHEMBL45177 IC50 = 9.0 nM 8.05
CHEMBL475584 IC50 = 20.0 nM 7.70