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Assay Detail

CHEMBL2383984

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

Binding
Inhibition of wild type EGFR (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.
Han C, Huang Z, Zheng C, Wan L, Zhang L, Peng S, Ding K, Ding K, Ji H, Tian J, Zhang Y.
J Med Chem (2013) 56 : 4738 -4748
PubMed 23668441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.44 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 10.00
CHEMBL1229592 1 8.49
CHEMBL2381516 1 7.41
CHEMBL2381504 1 7.38
CHEMBL2381514 1 7.29
CHEMBL2381509 1 7.28
CHEMBL2381506 1 7.23
CHEMBL2381515 1 7.23
CHEMBL2381505 1 7.14
CHEMBL2381510 1 7.00
CHEMBL2381507 1 7.00
CHEMBL2381508 1 6.76
CHEMBL2381511 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 0.1 nM 10.00
CHEMBL1229592 IC50 = 3.2 nM 8.49
CHEMBL2381516 IC50 = 39.0 nM 7.41
CHEMBL2381504 IC50 = 42.0 nM 7.38
CHEMBL2381514 IC50 = 51.0 nM 7.29
CHEMBL2381509 IC50 = 52.0 nM 7.28
CHEMBL2381506 IC50 = 59.0 nM 7.23
CHEMBL2381515 IC50 = 59.0 nM 7.23
CHEMBL2381505 IC50 = 73.0 nM 7.14
CHEMBL2381510 IC50 = 101.0 nM 7.00
CHEMBL2381507 IC50 = 99.0 nM 7.00
CHEMBL2381508 IC50 = 174.0 nM 6.76
CHEMBL2381511 IC50 = 292.0 nM 6.54