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Assay Detail

CHEMBL4625061

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

Binding
Inhibition of recombinant human partial length EGFR L858R mutant (669 to 1011 residues) expressed in bacterial expression system by competitive binding assay
2
Total Activities
2
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

Potent dual EGFR/Her4 tyrosine kinase inhibitors containing novel (1,2-dithiolan-4-yl)acetamides.
Mansour TS, Pallepati RR, Basetti V.
Bioorg Med Chem Lett (2020) 30 : 127288 -127288
PubMed 32631510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.30 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554 LAPATINIB 4.0 1 8.55
CHEMBL4646030 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554 LAPATINIB Kd = 2.8 nM 8.55
CHEMBL4646030 Kd = 9.2 nM 8.04