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Assay Detail

CHEMBL1028080

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of EGFR
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Epidermal growth factor receptor (CHEMBL203)
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 24 7.85 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475768 1 9.00
CHEMBL475594 1 8.70
CHEMBL473428 1 8.52
CHEMBL473429 1 8.52
CHEMBL474431 1 8.52
CHEMBL475769 1 8.40
CHEMBL473437 1 8.40
CHEMBL475761 GW784684X 1 8.30
CHEMBL473438 1 8.22
CHEMBL475446 1 8.15
CHEMBL473427 1 8.10
CHEMBL506414 GW684626B 1 8.05
CHEMBL479800 1 8.00
CHEMBL1201179 LAPATINIB DITOSYLATE 4.0 1 7.96
CHEMBL480349 1 7.92
CHEMBL514938 GSK-969786A 1 7.82
CHEMBL519757 1 7.27
CHEMBL473436 1 7.17
CHEMBL475767 1 7.17
CHEMBL481324 1 7.02
CHEMBL475600 1 6.94
CHEMBL480348 1 6.92
CHEMBL481331 1 6.86
CHEMBL475599 GSK-300014A 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475768 IC50 = 1.0 nM 9.00
CHEMBL475594 IC50 = 2.0 nM 8.70
CHEMBL473428 IC50 = 3.0 nM 8.52
CHEMBL473429 IC50 = 3.0 nM 8.52
CHEMBL474431 IC50 = 3.0 nM 8.52
CHEMBL475769 IC50 = 4.0 nM 8.40
CHEMBL473437 IC50 = 4.0 nM 8.40
CHEMBL475761 GW784684X IC50 = 5.0 nM 8.30
CHEMBL473438 IC50 = 6.0 nM 8.22
CHEMBL475446 IC50 = 7.0 nM 8.15
CHEMBL473427 IC50 = 8.0 nM 8.10
CHEMBL506414 GW684626B IC50 = 9.0 nM 8.05
CHEMBL479800 IC50 = 10.0 nM 8.00
CHEMBL1201179 LAPATINIB DITOSYLATE IC50 = 11.0 nM 7.96
CHEMBL480349 IC50 = 12.0 nM 7.92
CHEMBL514938 GSK-969786A IC50 = 15.0 nM 7.82
CHEMBL519757 IC50 = 54.0 nM 7.27
CHEMBL473436 IC50 = 68.0 nM 7.17
CHEMBL475767 IC50 = 68.0 nM 7.17
CHEMBL481324 IC50 = 96.0 nM 7.02
CHEMBL475600 IC50 = 115.0 nM 6.94
CHEMBL480348 IC50 = 121.0 nM 6.92
CHEMBL481331 IC50 = 138.0 nM 6.86
CHEMBL475599 GSK-300014A IC50 = 304.0 nM 6.52