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Assay Detail

CHEMBL815615

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Functional
Inhibition of EGFR and erbB2 overexpressing tumor cell proliferation
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

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 6.20 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL160303 1 7.05
CHEMBL155761 1 6.96
CHEMBL160846 1 6.54
CHEMBL422347 1 5.88
CHEMBL157084 1 5.61
CHEMBL269620 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL160303 IC50 = 89.0 nM 7.05
CHEMBL155761 IC50 = 110.0 nM 6.96
CHEMBL160846 IC50 = 290.0 nM 6.54
CHEMBL422347 IC50 = 1320.0 nM 5.88
CHEMBL157084 IC50 = 2450.0 nM 5.61
CHEMBL269620 IC50 = 7400.0 nM 5.13