Assay Detail

CHEMBL990365

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Binding

Inhibition of ErbB2 intracellular autophosphorylation of ErbB2 in human BT474 cells by DELFIA assay

ChEMBL ↗

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Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗

Open DB target context

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Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Receptor tyrosine-protein kinase erbB-2

CHEMBL1824

Anchored from Assay target.

Protein identity Receptor tyrosine-protein kinase erbB-2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	BT-474
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Thienopyrimidine-based dual EGFR/ErbB-2 inhibitors.

Rheault TR, Caferro TR, Dickerson SH, Donaldson KH, Gaul MD, Goetz AS, Mullin RJ, McDonald OB, Petrov KG, Rusnak DW, Shewchuk LM, Spehar GM, Truesdale AT, Vanderwall DE, Wood ER, Uehling DE.
Bioorg Med Chem Lett (2009) 19 : 817 -820
PubMed 19111461 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	6.23	6.37

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL475446	—	—	1	6.37
CHEMBL473436	—	—	1	6.08

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL475446	—	IC50	=	431.0	nM	6.37
CHEMBL473436	—	IC50	=	826.0	nM	6.08