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Assay Detail

CHEMBL673953

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Binding
Inhibition of ErbB-2
6
Total Activities
6
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

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

Publication

Discovery and biological evaluation of potent dual ErbB-2/EGFR tyrosine kinase inhibitors: 6-thiazolylquinazolines.
Gaul MD, Guo Y, Affleck K, Cockerill GS, Gilmer TM, Griffin RJ, Guntrip S, Keith BR, Knight WB, Mullin RJ, Murray DM, Rusnak DW, Smith K, Tadepalli S, Wood ER, Lackey K.
Bioorg Med Chem Lett (2003) 13 : 637 -640
PubMed 12639547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.26 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160846 1 7.85
CHEMBL155761 1 7.85
CHEMBL160303 1 7.55
CHEMBL422347 1 7.32
CHEMBL157084 1 6.70
CHEMBL269620 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160846 IC50 = 14.0 nM 7.85
CHEMBL155761 IC50 = 14.0 nM 7.85
CHEMBL160303 IC50 = 28.0 nM 7.55
CHEMBL422347 IC50 = 48.0 nM 7.32
CHEMBL157084 IC50 = 200.0 nM 6.70
CHEMBL269620 IC50 = 550.0 nM 6.26