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Assay Detail

CHEMBL806525

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Functional
Inhibition of c-Src transfected 3T3 cell proliferation
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type 3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery of a new class of anilinoquinazoline inhibitors with high affinity and specificity for the tyrosine kinase domain of c-Src.
Plé PA, Green TP, Hennequin LF, Curwen J, Fennell M, Allen J, Lambert-Van Der Brempt C, Costello G.
J Med Chem (2004) 47 : 871 -887
PubMed 14761189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.59 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL173799 1 7.22
CHEMBL354145 1 7.05
CHEMBL369360 1 7.00
CHEMBL169186 1 6.96
CHEMBL170984 1 6.92
CHEMBL167890 1 6.52
CHEMBL352977 1 6.51
CHEMBL171125 1 6.51
CHEMBL172450 1 6.51
CHEMBL169643 1 6.47
CHEMBL353070 1 6.42
CHEMBL422564 1 6.35
CHEMBL352992 1 6.28
CHEMBL169797 1 6.16
CHEMBL352877 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL173799 IC50 = 60.0 nM 7.22
CHEMBL354145 IC50 = 90.0 nM 7.05
CHEMBL369360 IC50 = 100.0 nM 7.00
CHEMBL169186 IC50 = 110.0 nM 6.96
CHEMBL170984 IC50 = 120.0 nM 6.92
CHEMBL167890 IC50 = 300.0 nM 6.52
CHEMBL352977 IC50 = 310.0 nM 6.51
CHEMBL171125 IC50 = 310.0 nM 6.51
CHEMBL172450 IC50 = 310.0 nM 6.51
CHEMBL169643 IC50 = 340.0 nM 6.47
CHEMBL353070 IC50 = 380.0 nM 6.42
CHEMBL422564 IC50 = 450.0 nM 6.35
CHEMBL352992 IC50 = 530.0 nM 6.28
CHEMBL169797 IC50 = 690.0 nM 6.16
CHEMBL352877 IC50 = 1160.0 nM 5.94