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Assay Detail

CHEMBL964133

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

Binding
Inhibition of EGFR phosphorylation in IGF1 and EGF-stimulated human MiaPaCa2 cells pretreated for 6 hrs before IGF1 and EGF stimulation by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MiaPaCa2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.
Hubbard RD, Bamaung NY, Fidanze SD, Erickson SA, Palazzo F, Wilsbacher JL, Zhang Q, Tucker LA, Hu X, Kovar P, Osterling DJ, Johnson EF, Bouska J, Wang J, Davidsen SK, Bell RL, Sheppard GS.
Bioorg Med Chem Lett (2009) 19 : 1718 -1721
PubMed 19217287 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.51 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443098 1 7.07
CHEMBL446250 1 7.04
CHEMBL455208 1 6.47
CHEMBL503638 1 6.28
CHEMBL452717 1 6.13
CHEMBL448628 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443098 EC50 = 85.0 nM 7.07
CHEMBL446250 EC50 = 91.0 nM 7.04
CHEMBL455208 EC50 = 335.0 nM 6.47
CHEMBL503638 EC50 = 520.0 nM 6.28
CHEMBL452717 EC50 = 742.0 nM 6.13
CHEMBL448628 EC50 = 808.0 nM 6.09