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Assay Detail

CHEMBL5114502

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

Binding
Inhibition of EGFR del19/T790M mutant (unknown origin)
2
Total Activities
2
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 evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFR<sup>del19/T790M/C797S</sup> and EGFR<sup>L858R/T790M/C797S</sup>).
Fang H, Wu Y, Xiao Q, He D, Zhou T, Liu W, Yang CH, Xie Y.
Bioorg Med Chem Lett (2022) 72 : 128729 -128729
PubMed 35413415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.58 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5206715 1 10.00
CHEMBL3545311 BRIGATINIB 4.0 1 9.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5206715 IC50 = 0.1 nM 10.00
CHEMBL3545311 BRIGATINIB IC50 = 0.7 nM 9.15