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Assay Detail

CHEMBL5143769

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

Binding
Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin)
37
Total Activities
36
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 37 7.69 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5169450 1 9.80
CHEMBL5174418 1 9.59
CHEMBL4443483 1 8.66
CHEMBL5190204 1 8.40
CHEMBL5180839 1 8.30
CHEMBL4090686 1 8.15
CHEMBL4061829 1 8.12
CHEMBL4100860 1 8.10
CHEMBL4799276 1 8.07
CHEMBL4753389 1 8.07
CHEMBL4649261 2 8.07
CHEMBL4089892 1 8.05
CHEMBL5205022 1 8.03
CHEMBL4071368 1 7.96
CHEMBL4558528 1 7.89
CHEMBL4795878 1 7.75
CHEMBL4533337 1 7.72
CHEMBL5206817 1 7.72
CHEMBL4101719 1 7.68
CHEMBL4744973 1 7.66
CHEMBL4530686 1 7.64
CHEMBL5206600 1 7.56
CHEMBL5194245 1 7.42
CHEMBL4786787 1 7.40
CHEMBL5183865 1 7.39
CHEMBL5195167 1 7.32
CHEMBL5200385 1 7.32
CHEMBL5180830 1 7.28
CHEMBL5195321 1 7.28
CHEMBL4520903 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5169450 IC50 = 0.16 nM 9.80
CHEMBL5174418 IC50 = 0.26 nM 9.59
CHEMBL4443483 IC50 = 2.2 nM 8.66
CHEMBL5190204 IC50 = 4.0 nM 8.40
CHEMBL5180839 IC50 = 5.0 nM 8.30
CHEMBL4090686 IC50 = 7.0 nM 8.15
CHEMBL4061829 IC50 = 7.64 nM 8.12
CHEMBL4100860 IC50 = 8.0 nM 8.10
CHEMBL4649261 IC50 = 8.5 nM 8.07
CHEMBL4753389 IC50 = 8.5 nM 8.07
CHEMBL4799276 IC50 = 8.6 nM 8.07
CHEMBL4089892 IC50 = 8.83 nM 8.05
CHEMBL5205022 IC50 = 9.4 nM 8.03
CHEMBL4071368 IC50 = 11.0 nM 7.96
CHEMBL4558528 IC50 = 13.0 nM 7.89
CHEMBL4795878 IC50 = 18.0 nM 7.75
CHEMBL4533337 IC50 = 19.0 nM 7.72
CHEMBL5206817 IC50 = 19.0 nM 7.72
CHEMBL4101719 IC50 = 21.0 nM 7.68
CHEMBL4744973 IC50 = 22.0 nM 7.66
CHEMBL4530686 IC50 = 23.0 nM 7.64
CHEMBL5206600 IC50 = 27.5 nM 7.56
CHEMBL5194245 IC50 = 38.1 nM 7.42
CHEMBL4786787 IC50 = 40.0 nM 7.40
CHEMBL5183865 IC50 = 41.0 nM 7.39
CHEMBL5195167 IC50 = 48.2 nM 7.32
CHEMBL5200385 IC50 = 47.8 nM 7.32
CHEMBL5195321 IC50 = 53.0 nM 7.28
CHEMBL5180830 IC50 = 52.0 nM 7.28
CHEMBL4520903 IC50 = 59.0 nM 7.23
CHEMBL4090601 IC50 = 88.0 nM 7.06
CHEMBL4098072 IC50 = 90.0 nM 7.05
CHEMBL4228518 IC50 = 114.0 nM 6.94
CHEMBL4649261 IC50 = 218.3 nM 6.66
CHEMBL5190294 IC50 = 290.0 nM 6.54
CHEMBL24828 VANDETANIB IC50 = 369.2 nM 6.43
CHEMBL4209019 IC50 = 662.0 nM 6.18