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Assay Detail

CHEMBL3375345

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

Binding
Inhibition of wild type EGFR (unknown origin) by Z'-Lyte kinase assay
23
Total Activities
23
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

Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.
Cheng W, Yuan Y, Qiu N, Peng P, Sheng R, Hu Y.
Bioorg Med Chem (2014) 22 : 6796 -6805
PubMed 25468044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.90 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360608 1 9.59
CHEMBL3360603 1 9.51
CHEMBL3360606 1 9.49
CHEMBL3360619 1 9.48
CHEMBL3360618 1 9.43
CHEMBL939 GEFITINIB 4.0 1 9.35
CHEMBL3360609 1 9.33
CHEMBL3360617 1 9.31
CHEMBL3360604 1 9.28
CHEMBL3360611 1 9.27
CHEMBL3360610 1 9.24
CHEMBL3360607 1 9.19
CHEMBL3360602 1 9.11
CHEMBL3352899 1 9.11
CHEMBL3360620 1 9.09
CHEMBL3360605 1 8.84
CHEMBL3360613 1 7.92
CHEMBL3360614 1 7.78
CHEMBL3360616 1 7.70
CHEMBL3360612 1 7.52
CHEMBL3360615 1 7.45
CHEMBL553 ERLOTINIB 4.0 1 -
CHEMBL50882 TIRAPAZAMINE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360608 IC50 = 0.26 nM 9.59
CHEMBL3360603 IC50 = 0.31 nM 9.51
CHEMBL3360606 IC50 = 0.32 nM 9.49
CHEMBL3360619 IC50 = 0.33 nM 9.48
CHEMBL3360618 IC50 = 0.37 nM 9.43
CHEMBL939 GEFITINIB IC50 = 0.45 nM 9.35
CHEMBL3360609 IC50 = 0.47 nM 9.33
CHEMBL3360617 IC50 = 0.49 nM 9.31
CHEMBL3360604 IC50 = 0.52 nM 9.28
CHEMBL3360611 IC50 = 0.54 nM 9.27
CHEMBL3360610 IC50 = 0.57 nM 9.24
CHEMBL3360607 IC50 = 0.65 nM 9.19
CHEMBL3360602 IC50 = 0.77 nM 9.11
CHEMBL3352899 IC50 = 0.78 nM 9.11
CHEMBL3360620 IC50 = 0.82 nM 9.09
CHEMBL3360605 IC50 = 1.44 nM 8.84
CHEMBL3360613 IC50 = 11.9 nM 7.92
CHEMBL3360614 IC50 = 16.6 nM 7.78
CHEMBL3360616 IC50 = 20.1 nM 7.70
CHEMBL3360612 IC50 = 30.5 nM 7.52
CHEMBL3360615 IC50 = 35.5 nM 7.45
CHEMBL553 ERLOTINIB IC50 - -
CHEMBL50882 TIRAPAZAMINE IC50 - -