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Assay Detail

CHEMBL4625258

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

Binding
Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) by ELISA
8
Total Activities
8
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

Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation.
Su Z, Yang T, Wang J, Lai M, Tong L, Wumaier G, Chen Z, Li S, Li H, Xie H, Zhao Z.
Bioorg Med Chem Lett (2020) 30 : 127327 -127327
PubMed 32631532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.42 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545311 BRIGATINIB 4.0 1 8.82
CHEMBL4649261 1 7.82
CHEMBL4645434 1 7.75
CHEMBL4647073 1 7.39
CHEMBL4639459 1 7.14
CHEMBL4641096 1 7.14
CHEMBL4640686 1 7.09
CHEMBL4642177 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545311 BRIGATINIB IC50 = 1.5 nM 8.82
CHEMBL4649261 IC50 = 15.3 nM 7.82
CHEMBL4645434 IC50 = 17.9 nM 7.75
CHEMBL4647073 IC50 = 40.4 nM 7.39
CHEMBL4639459 IC50 = 72.5 nM 7.14
CHEMBL4641096 IC50 = 73.0 nM 7.14
CHEMBL4640686 IC50 = 80.5 nM 7.09
CHEMBL4642177 IC50 = 663.4 nM 6.18