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Assay Detail

CHEMBL805895

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Binding
Inhibition of Src protein tyrosine kinase
10
Total Activities
10
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

Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.
Boschelli DH, Powell D, Golas JM, Boschelli F.
Bioorg Med Chem Lett (2003) 13 : 2977 -2980
PubMed 12941315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.62 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288441 BOSUTINIB 4.0 1 8.92
CHEMBL100551 1 8.64
CHEMBL102000 1 8.48
CHEMBL101917 1 8.37
CHEMBL100172 1 8.01
CHEMBL322689 1 7.80
CHEMBL100651 1 7.52
CHEMBL414013 1 6.30
CHEMBL7137 1 4.50
CHEMBL450015 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288441 BOSUTINIB IC50 = 1.2 nM 8.92
CHEMBL100551 IC50 = 2.3 nM 8.64
CHEMBL102000 IC50 = 3.3 nM 8.48
CHEMBL101917 IC50 = 4.3 nM 8.37
CHEMBL100172 IC50 = 9.8 nM 8.01
CHEMBL322689 IC50 = 16.0 nM 7.80
CHEMBL100651 IC50 = 30.0 nM 7.52
CHEMBL414013 IC50 = 500.0 nM 6.30
CHEMBL7137 IC50 = 32000.0 nM 4.50
CHEMBL450015 IC50 > 10000.0 nM -