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Assay Detail

CHEMBL3223699

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

Functional
Cytotoxicity against human HCC827 cells expressing EGFR kinase E746 to A750 deletion mutant after 72 hrs by MTS assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCC827
Confidence 1 — Organism
Curated By Autocuration

Publication

Design, synthesis and biological evaluation of new molecules inhibiting epidermal growth factor receptor threonine790 methionine790 mutant
Xu S, Zhang L, Chang S, Luo J, Lu X, Tu Z, Liu Y, zhang Z, Xu Y, Ren X, Ding K
Medchemcomm (2012) 3 : 1155 -1159
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.70 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229592 1 7.62
CHEMBL3219133 1 7.62
CHEMBL939 GEFITINIB 4.0 1 7.39
CHEMBL3219127 1 7.17
CHEMBL3219129 1 7.16
CHEMBL3219347 1 7.15
CHEMBL3219348 1 7.06
CHEMBL3219128 1 6.89
CHEMBL3219132 1 6.85
CHEMBL3219134 1 6.55
CHEMBL3219135 1 6.52
CHEMBL3219130 1 6.22
CHEMBL3219125 1 5.78
CHEMBL3219131 1 5.42
CHEMBL3219126 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229592 IC50 = 24.0 nM 7.62
CHEMBL3219133 IC50 = 24.0 nM 7.62
CHEMBL939 GEFITINIB IC50 = 41.0 nM 7.39
CHEMBL3219127 IC50 = 68.0 nM 7.17
CHEMBL3219129 IC50 = 69.0 nM 7.16
CHEMBL3219347 IC50 = 71.0 nM 7.15
CHEMBL3219348 IC50 = 87.0 nM 7.06
CHEMBL3219128 IC50 = 130.0 nM 6.89
CHEMBL3219132 IC50 = 140.0 nM 6.85
CHEMBL3219134 IC50 = 280.0 nM 6.55
CHEMBL3219135 IC50 = 300.0 nM 6.52
CHEMBL3219130 IC50 = 600.0 nM 6.22
CHEMBL3219125 IC50 = 1680.0 nM 5.78
CHEMBL3219131 IC50 = 3820.0 nM 5.42
CHEMBL3219126 IC50 = 6900.0 nM 5.16