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Assay Detail

CHEMBL1022370

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

Binding
Inhibition of Src kinase
7
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-based virtual screening of Src kinase inhibitors.
Lee K, Kim J, Jeong KW, Lee KW, Lee Y, Song JY, Kim MS, Lee GS, Kim Y.
Bioorg Med Chem (2009) 17 : 3152 -3161
PubMed 19321350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.01 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 2 9.22
CHEMBL288441 BOSUTINIB 4.0 1 8.92
CHEMBL217092 SARACATINIB 3.0 2 8.52
CHEMBL523122 1 7.05
CHEMBL485304 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 0.6 nM 9.22
CHEMBL288441 BOSUTINIB IC50 = 1.2 nM 8.92
CHEMBL217092 SARACATINIB IC50 = 3.0 nM 8.52
CHEMBL217092 SARACATINIB IC50 = 10.0 nM 8.00
CHEMBL5416410 DASATINIB IC50 = 14.0 nM 7.85
CHEMBL523122 IC50 = 89.0 nM 7.05
CHEMBL485304 IC50 = 300.0 nM 6.52