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Assay Detail

CHEMBL5143776

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

Binding
Inhibition of EGFR L858R/T790M double mutant (unknown origin)
7
Total Activities
7
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

Emerging Approaches to Overcome Acquired Drug Resistance Obstacles to Osimertinib in Non-Small-Cell Lung Cancer.
Shaikh M, Shinde Y, Pawara R, Noolvi M, Surana S, Ahmad I, Patel H.
J Med Chem (2022) 65 : 1008 -1046
PubMed 34323489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.48 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443062 1 9.59
CHEMBL4214567 1 8.52
CHEMBL5193027 1 7.82
CHEMBL4284413 1 7.62
CHEMBL4649261 1 6.80
CHEMBL4228518 1 6.72
CHEMBL5206476 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443062 IC50 = 0.26 nM 9.59
CHEMBL4214567 IC50 = 3.0 nM 8.52
CHEMBL5193027 IC50 = 15.0 nM 7.82
CHEMBL4284413 IC50 = 24.0 nM 7.62
CHEMBL4649261 IC50 = 156.6 nM 6.80
CHEMBL4228518 IC50 = 189.0 nM 6.72
CHEMBL5206476 IC50 = 5300.0 nM 5.28