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Assay Detail

CHEMBL3999846

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

Binding
Inhibition of recombinant human GST-tagged EGFR L858R mutant cytoplasmic domain (695-end residues) expressed in insect cells by Z'-Lyte assay
13
Total Activities
11
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 conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents.
Yang J, Tu Z, Xu X, Luo J, Yan X, Ran C, Mao X, Ding K, Qiao C.
Bioorg Med Chem Lett (2017) 27 : 1341 -1345
PubMed 28236592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.40 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 9.77
CHEMBL343352 1 8.39
CHEMBL4063301 1 8.16
CHEMBL4100647 1 7.77
CHEMBL4094823 1 7.31
CHEMBL4094174 1 6.95
CHEMBL4082840 2 6.95
CHEMBL4091166 1 6.88
CHEMBL4088200 2 6.83
CHEMBL4067373 1 6.43
CHEMBL1830034 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 0.17 nM 9.77
CHEMBL343352 IC50 = 4.053 nM 8.39
CHEMBL4063301 IC50 = 6.963 nM 8.16
CHEMBL4100647 IC50 = 17.15 nM 7.77
CHEMBL4094823 IC50 = 48.9 nM 7.31
CHEMBL4094174 IC50 = 112.2 nM 6.95
CHEMBL4082840 IC50 = 112.4 nM 6.95
CHEMBL4091166 IC50 = 132.1 nM 6.88
CHEMBL4088200 IC50 = 146.2 nM 6.83
CHEMBL4082840 IC50 = 174.9 nM 6.76
CHEMBL4088200 IC50 = 235.6 nM 6.63
CHEMBL4067373 IC50 = 373.7 nM 6.43
CHEMBL1830034 IC50 > 10000.0 nM -