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Assay Detail

CHEMBL990363

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Functional
Antiproliferative activity against human BT474 cells expressing ErbB2 by MEB assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-474
Confidence 1 — Organism
Curated By Autocuration

Target

BT-474 (CHEMBL614529)
Type CELL-LINE
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 6 6.25 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201179 LAPATINIB DITOSYLATE 4.0 1 7.00
CHEMBL473436 1 6.27
CHEMBL474431 1 6.22
CHEMBL473428 1 6.14
CHEMBL475769 1 6.14
CHEMBL475600 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201179 LAPATINIB DITOSYLATE IC50 = 100.0 nM 7.00
CHEMBL473436 IC50 = 540.0 nM 6.27
CHEMBL474431 IC50 = 600.0 nM 6.22
CHEMBL473428 IC50 = 720.0 nM 6.14
CHEMBL475769 IC50 = 730.0 nM 6.14
CHEMBL475600 IC50 = 1980.0 nM 5.70