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Assay Detail

CHEMBL1050612

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

Binding
Inhibition of human recombinant Src
19
Total Activities
19
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

Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Antczak C, Veach DR, Ramirez CN, Minchenko MA, Shum D, Calder PA, Frattini MG, Clarkson B, Djaballah H.
Bioorg Med Chem Lett (2009) 19 : 6872 -6876
PubMed 19889540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.07 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576218 1 8.04
CHEMBL566635 1 7.75
CHEMBL585666 1 7.52
CHEMBL565366 1 7.46
CHEMBL566636 1 7.44
CHEMBL567068 1 7.42
CHEMBL577269 1 7.42
CHEMBL566850 1 7.37
CHEMBL327127 1 7.37
CHEMBL321193 1 7.37
CHEMBL566834 1 7.18
CHEMBL565801 1 6.82
CHEMBL565609 1 6.67
CHEMBL323405 1 6.65
CHEMBL565372 1 6.63
CHEMBL570175 1 6.47
CHEMBL565587 1 6.36
CHEMBL111339 1 6.31
CHEMBL574059 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576218 IC50 = 9.2 nM 8.04
CHEMBL566635 IC50 = 18.0 nM 7.75
CHEMBL585666 IC50 = 30.0 nM 7.52
CHEMBL565366 IC50 = 35.0 nM 7.46
CHEMBL566636 IC50 = 36.0 nM 7.44
CHEMBL567068 IC50 = 38.0 nM 7.42
CHEMBL577269 IC50 = 38.0 nM 7.42
CHEMBL566850 IC50 = 43.0 nM 7.37
CHEMBL327127 IC50 = 43.0 nM 7.37
CHEMBL321193 IC50 = 43.0 nM 7.37
CHEMBL566834 IC50 = 66.0 nM 7.18
CHEMBL565801 IC50 = 150.0 nM 6.82
CHEMBL565609 IC50 = 213.0 nM 6.67
CHEMBL323405 IC50 = 223.0 nM 6.65
CHEMBL565372 IC50 = 234.0 nM 6.63
CHEMBL570175 IC50 = 341.0 nM 6.47
CHEMBL565587 IC50 = 433.0 nM 6.36
CHEMBL111339 IC50 = 492.0 nM 6.31
CHEMBL574059 IC50 = 921.0 nM 6.04