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Assay Detail

CHEMBL4819611

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

Binding
Inhibition of N-terminal GST-tagged human recombinant EGFR T790M mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay
8
Total Activities
8
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

Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.
Zhang W, Zhang K, Yao Y, Liu Y, Ni Y, Liao C, Tu Z, Qiu Y, Wang D, Chen D, Qiang L, Li Z, Jiang S.
Eur J Med Chem (2021) 211 : 113022 -113022
PubMed 33239261 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.82 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1229592 1 8.70
CHEMBL4851176 1 6.82
CHEMBL4852664 1 6.64
CHEMBL4860398 1 6.49
CHEMBL4873506 1 6.49
CHEMBL4859375 1 6.35
CHEMBL4868614 1 6.24
CHEMBL566757 DAPORINAD 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1229592 IC50 = 1.98 nM 8.70
CHEMBL4851176 IC50 = 153.0 nM 6.82
CHEMBL4852664 IC50 = 228.0 nM 6.64
CHEMBL4860398 IC50 = 323.0 nM 6.49
CHEMBL4873506 IC50 = 326.0 nM 6.49
CHEMBL4859375 IC50 = 448.0 nM 6.35
CHEMBL4868614 IC50 = 581.0 nM 6.24
CHEMBL566757 DAPORINAD IC50 - -