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Assay Detail

CHEMBL964131

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

Binding
Inhibition of ErbB2 by time resolved fluorescence assay
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 Intermediate

Target

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

Publication

Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.
Hubbard RD, Bamaung NY, Fidanze SD, Erickson SA, Palazzo F, Wilsbacher JL, Zhang Q, Tucker LA, Hu X, Kovar P, Osterling DJ, Johnson EF, Bouska J, Wang J, Davidsen SK, Bell RL, Sheppard GS.
Bioorg Med Chem Lett (2009) 19 : 1718 -1721
PubMed 19217287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.09 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446250 1 7.89
CHEMBL448628 1 7.77
CHEMBL455208 1 7.36
CHEMBL437584 1 7.28
CHEMBL443098 1 7.27
CHEMBL452717 1 7.23
CHEMBL249496 1 6.73
CHEMBL248877 1 6.60
CHEMBL503638 1 6.57
CHEMBL251732 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446250 IC50 = 13.0 nM 7.89
CHEMBL448628 IC50 = 17.0 nM 7.77
CHEMBL455208 IC50 = 44.0 nM 7.36
CHEMBL437584 IC50 = 53.0 nM 7.28
CHEMBL443098 IC50 = 54.0 nM 7.27
CHEMBL452717 IC50 = 59.0 nM 7.23
CHEMBL249496 IC50 = 186.0 nM 6.73
CHEMBL248877 IC50 = 250.0 nM 6.60
CHEMBL503638 IC50 = 270.0 nM 6.57
CHEMBL251732 IC50 = 664.0 nM 6.18