Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4388560

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

Binding
Binding affinity to human partial length EGFR L858R mutant (R669 to V1011 residues) expressed in bacterial expression system under full equilibrating condition by scanKINETIC assay
3
Total Activities
3
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

Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
Mansour TS, Potluri V, Pallepati RR, Basetti V, Keesara M, Moghudula AG, Maiti P.
Bioorg Med Chem Lett (2019) 29 : 1435 -1439
PubMed 31023512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 8.62 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4517633 1 9.15
CHEMBL4513286 1 8.68
CHEMBL4457447 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4517633 Kd = 0.7 nM 9.15
CHEMBL4513286 Kd = 2.1 nM 8.68
CHEMBL4457447 Kd = 9.6 nM 8.02