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Assay Detail

CHEMBL806436

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

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

Assay Information

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

Target

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

Publication

Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.
Vu CB, Luke GP, Kawahata N, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA, Keenan TP, Pradeepan S, Corpuz E, Merry T, Bohacek RS, Dalgarno DC, Narula SS, van Schravendijk MR, Ram MK, Adams S, Liou S, Keats JA, Violette SM, Guan W, Weigele M, Sawyer TK.
Bioorg Med Chem Lett (2003) 13 : 3071 -3074
PubMed 12941336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.41 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421024 1 9.52
CHEMBL419360 1 8.70
CHEMBL301612 1 7.80
CHEMBL106442 1 7.11
CHEMBL102801 1 6.70
CHEMBL102217 1 6.12
CHEMBL320374 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421024 IC50 = 0.3 nM 9.52
CHEMBL419360 IC50 = 2.0 nM 8.70
CHEMBL301612 IC50 = 16.0 nM 7.80
CHEMBL106442 IC50 = 77.0 nM 7.11
CHEMBL102801 IC50 = 200.0 nM 6.70
CHEMBL102217 IC50 = 750.0 nM 6.12
CHEMBL320374 IC50 = 1300.0 nM 5.89