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Assay Detail

CHEMBL870843

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

Functional
Inhibition of serum-stimulated proliferation of mouse ERBB2 transfected NIH3T3 cell line after 24 hrs
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The combi-targeting concept: synthesis of stable nitrosoureas designed to inhibit the epidermal growth factor receptor (EGFR).
Domarkas J, Dudouit F, Williams C, Qiyu Q, Banerjee R, Brahimi F, Jean-Claude BJ.
J Med Chem (2006) 49 : 3544 -3552
PubMed 16759097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.56 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50344 1 6.77
CHEMBL210378 1 6.17
CHEMBL52765 1 6.17
CHEMBL209343 1 6.05
CHEMBL210660 1 5.94
CHEMBL210444 1 5.87
CHEMBL207009 1 5.75
CHEMBL208594 1 5.68
CHEMBL208240 1 5.68
CHEMBL210893 1 5.51
CHEMBL343352 1 5.48
CHEMBL210659 1 5.27
CHEMBL336113 1 5.19
CHEMBL209818 1 5.16
CHEMBL379047 1 4.96
CHEMBL208849 1 4.93
CHEMBL210502 1 4.91
CHEMBL208144 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50344 IC50 = 170.0 nM 6.77
CHEMBL210378 IC50 = 680.0 nM 6.17
CHEMBL52765 IC50 = 670.0 nM 6.17
CHEMBL209343 IC50 = 890.0 nM 6.05
CHEMBL210660 IC50 = 1150.0 nM 5.94
CHEMBL210444 IC50 = 1350.0 nM 5.87
CHEMBL207009 IC50 = 1770.0 nM 5.75
CHEMBL208594 IC50 = 2070.0 nM 5.68
CHEMBL208240 IC50 = 2100.0 nM 5.68
CHEMBL210893 IC50 = 3060.0 nM 5.51
CHEMBL343352 IC50 = 3290.0 nM 5.48
CHEMBL210659 IC50 = 5400.0 nM 5.27
CHEMBL336113 IC50 = 6390.0 nM 5.19
CHEMBL209818 IC50 = 6880.0 nM 5.16
CHEMBL379047 IC50 = 11080.0 nM 4.96
CHEMBL208849 IC50 = 11800.0 nM 4.93
CHEMBL210502 IC50 = 12180.0 nM 4.91
CHEMBL208144 IC50 = 23030.0 nM 4.64