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Assay Detail

CHEMBL990360

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Functional
Antiproliferative activity against human BT474 cells expressing ErbB2 after 72 hrs by CTG assay
8
Total Activities
8
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 8 5.73 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475768 1 6.38
CHEMBL480349 1 6.38
CHEMBL475446 1 6.20
CHEMBL475594 1 5.73
CHEMBL506414 GW684626B 1 5.49
CHEMBL473427 1 5.24
CHEMBL479800 1 4.67
CHEMBL514938 GSK-969786A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475768 IC50 = 420.0 nM 6.38
CHEMBL480349 IC50 = 420.0 nM 6.38
CHEMBL475446 IC50 = 630.0 nM 6.20
CHEMBL475594 IC50 = 1880.0 nM 5.73
CHEMBL506414 GW684626B IC50 = 3220.0 nM 5.49
CHEMBL473427 IC50 = 5770.0 nM 5.24
CHEMBL479800 IC50 = 21250.0 nM 4.67
CHEMBL514938 GSK-969786A IC50 > 30000.0 nM -