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Assay Detail

CHEMBL1816084

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

Binding
Inhibition of recombinant EGFR expressed in baculovirus infected Sf9 cells after 1 hr by DELFIA/time-resolved fluorimetry assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The combination of 4-anilinoquinazoline and cinnamic acid: a novel mode of binding to the epidermal growth factor receptor tyrosine kinase.
Li DD, Lv PC, Zhang H, Zhang HJ, Hou YP, Liu K, Ye YH, Zhu HL.
Bioorg Med Chem (2011) 19 : 5012 -5022
PubMed 21763148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.91 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 7.52
CHEMBL52765 1 7.40
CHEMBL1812572 1 6.92
CHEMBL1812573 1 6.72
CHEMBL343352 1 6.70
CHEMBL1812571 1 6.03
CHEMBL1812560 1 5.99
CHEMBL1812431 1 5.92
CHEMBL1812569 1 5.55
CHEMBL1812570 1 5.46
CHEMBL1812564 1 5.46
CHEMBL1812561 1 5.44
CHEMBL1812434 1 5.37
CHEMBL1812559 1 5.29
CHEMBL1812556 1 5.22
CHEMBL1812566 1 5.18
CHEMBL1812435 1 5.14
CHEMBL1812555 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 30.0 nM 7.52
CHEMBL52765 IC50 = 40.0 nM 7.40
CHEMBL1812572 IC50 = 120.0 nM 6.92
CHEMBL1812573 IC50 = 190.0 nM 6.72
CHEMBL343352 IC50 = 200.0 nM 6.70
CHEMBL1812571 IC50 = 940.0 nM 6.03
CHEMBL1812560 IC50 = 1020.0 nM 5.99
CHEMBL1812431 IC50 = 1210.0 nM 5.92
CHEMBL1812569 IC50 = 2810.0 nM 5.55
CHEMBL1812570 IC50 = 3450.0 nM 5.46
CHEMBL1812564 IC50 = 3490.0 nM 5.46
CHEMBL1812561 IC50 = 3610.0 nM 5.44
CHEMBL1812434 IC50 = 4280.0 nM 5.37
CHEMBL1812559 IC50 = 5160.0 nM 5.29
CHEMBL1812556 IC50 = 6020.0 nM 5.22
CHEMBL1812566 IC50 = 6630.0 nM 5.18
CHEMBL1812435 IC50 = 7220.0 nM 5.14
CHEMBL1812555 IC50 = 7710.0 nM 5.11