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Assay Detail

CHEMBL4425261

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

ADMET
Binding affinity to wild type partial length human EGFR expressed in bacterial system by KINOMEscan assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.
Song Z, Ge Y, Wang C, Huang S, Shu X, Liu K, Zhou Y, Ma X.
J Med Chem (2016) 59 : 6580 -6594
PubMed 26882288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 7.06 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229592 1 8.92
CHEMBL4454373 1 7.77
CHEMBL4464614 1 6.96
CHEMBL4459080 1 6.85
CHEMBL4438135 1 6.51
CHEMBL4446485 1 6.38
CHEMBL4474541 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229592 Kd = 1.2 nM 8.92
CHEMBL4454373 Kd = 17.0 nM 7.77
CHEMBL4464614 Kd = 110.0 nM 6.96
CHEMBL4459080 Kd = 140.0 nM 6.85
CHEMBL4438135 Kd = 310.0 nM 6.51
CHEMBL4446485 Kd = 420.0 nM 6.38
CHEMBL4474541 Kd = 950.0 nM 6.02