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Assay Detail

CHEMBL885033

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

Functional
Inhibitory activity against non-receptor tyrosine kinase Src in cell assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles.
Boschelli DH, Wu B, Barrios Sosa AC, Chen JJ, Golas JM, Boschelli F.
Bioorg Med Chem Lett (2005) 15 : 4681 -4684
PubMed 16125383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.12 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288441 BOSUTINIB 4.0 1 7.00
CHEMBL197094 1 6.58
CHEMBL370693 1 6.44
CHEMBL373101 1 6.38
CHEMBL194664 1 6.37
CHEMBL193452 1 6.19
CHEMBL364955 1 6.14
CHEMBL193392 1 5.92
CHEMBL193695 1 5.72
CHEMBL192652 1 5.62
CHEMBL372178 1 5.54
CHEMBL370371 1 5.51
CHEMBL193751 1 -
CHEMBL194674 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288441 BOSUTINIB IC50 = 100.0 nM 7.00
CHEMBL197094 IC50 = 260.0 nM 6.58
CHEMBL370693 IC50 = 360.0 nM 6.44
CHEMBL373101 IC50 = 420.0 nM 6.38
CHEMBL194664 IC50 = 430.0 nM 6.37
CHEMBL193452 IC50 = 650.0 nM 6.19
CHEMBL364955 IC50 = 720.0 nM 6.14
CHEMBL193392 IC50 = 1200.0 nM 5.92
CHEMBL193695 IC50 = 1900.0 nM 5.72
CHEMBL192652 IC50 = 2400.0 nM 5.62
CHEMBL372178 IC50 = 2900.0 nM 5.54
CHEMBL370371 IC50 = 3100.0 nM 5.51
CHEMBL193751 IC50 > 5000.0 nM -
CHEMBL194674 IC50 > 5000.0 nM -