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Assay Detail

CHEMBL916320

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

Functional
Inhibition of human EGFR tyrosine kinase phosphorylation expressed in mouse BaF3 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes.
VanBrocklin HF, Lim JK, Coffing SL, Hom DL, Negash K, Ono MY, Gilmore JL, Bryant I, Riese DJ.
J Med Chem (2005) 48 : 7445 -7456
PubMed 16279804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.20 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540068 1 9.10
CHEMBL2447950 1 8.92
CHEMBL1204168 1 8.59
CHEMBL1204199 1 8.49
CHEMBL1204262 1 8.34
CHEMBL541586 1 8.20
CHEMBL1204261 1 8.19
CHEMBL1204305 1 8.19
CHEMBL1203937 1 8.18
CHEMBL1203938 1 7.96
CHEMBL1204360 1 7.89
CHEMBL1203939 1 7.80
CHEMBL1203934 1 7.72
CHEMBL1203936 1 7.72
CHEMBL1203940 1 7.64
CHEMBL1203935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540068 IC50 = 0.8 nM 9.10
CHEMBL2447950 IC50 = 1.2 nM 8.92
CHEMBL1204168 IC50 = 2.6 nM 8.59
CHEMBL1204199 IC50 = 3.2 nM 8.49
CHEMBL1204262 IC50 = 4.6 nM 8.34
CHEMBL541586 IC50 = 6.3 nM 8.20
CHEMBL1204261 IC50 = 6.5 nM 8.19
CHEMBL1204305 IC50 = 6.4 nM 8.19
CHEMBL1203937 IC50 = 6.6 nM 8.18
CHEMBL1203938 IC50 = 10.9 nM 7.96
CHEMBL1204360 IC50 = 12.8 nM 7.89
CHEMBL1203939 IC50 = 15.8 nM 7.80
CHEMBL1203934 IC50 = 19.1 nM 7.72
CHEMBL1203936 IC50 = 19.1 nM 7.72
CHEMBL1203940 IC50 = 23.1 nM 7.64
CHEMBL1203935 IC50 > 50.0 nM -