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Assay Detail

CHEMBL5143771

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

Binding
Inhibition of EGFR Del19/T790M/C797S triple mutant (unknown origin)
13
Total Activities
13
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 13 8.16 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5172794 1 9.70
CHEMBL5176129 1 9.70
CHEMBL5174418 1 9.67
CHEMBL5169450 1 9.66
CHEMBL5187838 1 9.10
CHEMBL5195167 1 7.92
CHEMBL4649261 1 7.82
CHEMBL4218431 1 7.75
CHEMBL4207984 1 7.64
CHEMBL4214588 1 7.34
CHEMBL1328065 1 6.83
CHEMBL5190294 1 6.51
CHEMBL4443483 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5172794 IC50 = 0.2 nM 9.70
CHEMBL5176129 IC50 = 0.2 nM 9.70
CHEMBL5174418 IC50 = 0.212 nM 9.67
CHEMBL5169450 IC50 = 0.218 nM 9.66
CHEMBL5187838 IC50 = 0.8 nM 9.10
CHEMBL5195167 IC50 = 12.0 nM 7.92
CHEMBL4649261 IC50 = 15.3 nM 7.82
CHEMBL4218431 IC50 = 17.9 nM 7.75
CHEMBL4207984 IC50 = 23.0 nM 7.64
CHEMBL4214588 IC50 = 46.0 nM 7.34
CHEMBL1328065 IC50 = 149.0 nM 6.83
CHEMBL5190294 IC50 = 310.0 nM 6.51
CHEMBL4443483 IC50 = 331.3 nM 6.48