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Assay Detail

CHEMBL806435

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Binding
Inhibition of Src protein tyrosine kinase
14
Total Activities
14
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

Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.
Boschelli DH, Ye F, Wu B, Wang YD, Barrios Sosa AC, Yaczko D, Powell D, Golas JM, Lucas J, Boschelli F.
Bioorg Med Chem Lett (2003) 13 : 3797 -3800
PubMed 14552782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.34 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288441 BOSUTINIB 4.0 1 8.92
CHEMBL290921 1 8.85
CHEMBL124333 1 8.82
CHEMBL42136 1 8.70
CHEMBL41465 1 8.62
CHEMBL338413 1 8.55
CHEMBL127633 1 8.33
CHEMBL436362 1 8.29
CHEMBL43577 1 8.18
CHEMBL440847 1 8.08
CHEMBL122744 1 8.06
CHEMBL123733 1 7.92
CHEMBL127771 1 7.85
CHEMBL419428 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288441 BOSUTINIB IC50 = 1.2 nM 8.92
CHEMBL290921 IC50 = 1.4 nM 8.85
CHEMBL124333 IC50 = 1.5 nM 8.82
CHEMBL42136 IC50 = 2.0 nM 8.70
CHEMBL41465 IC50 = 2.4 nM 8.62
CHEMBL338413 IC50 = 2.8 nM 8.55
CHEMBL127633 IC50 = 4.7 nM 8.33
CHEMBL436362 IC50 = 5.1 nM 8.29
CHEMBL43577 IC50 = 6.6 nM 8.18
CHEMBL440847 IC50 = 8.3 nM 8.08
CHEMBL122744 IC50 = 8.7 nM 8.06
CHEMBL123733 IC50 = 12.0 nM 7.92
CHEMBL127771 IC50 = 14.0 nM 7.85
CHEMBL419428 IC50 = 25.0 nM 7.60