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

CHEMBL3606412

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

Binding
Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells by enzyme kinetics assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting Drug Resistance in EGFR with Covalent Inhibitors: A Structure-Based Design Approach.
Engel J, Richters A, Getlik M, Tomassi S, Keul M, Termathe M, Lategahn J, Becker C, Mayer-Wrangowski S, Grütter C, Uhlenbrock N, Krüll J, Schaumann N, Eppmann S, Kibies P, Hoffgaard F, Heil J, Menninger S, Ortiz-Cuaran S, Heuckmann JM, Tinnefeld V, Zahedi RP, Sos ML, Schultz-Fademrecht C, Thomas RK, Kast SM, Rauh D.
J Med Chem (2015) 58 : 6844 -6863
PubMed 26275028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.70 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3604943 1 8.80
CHEMBL3545308 ROCILETINIB 3.0 1 8.76
CHEMBL3604921 1 7.15
CHEMBL3604937 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3604943 Ki = 1.58 nM 8.80
CHEMBL3545308 ROCILETINIB Ki = 1.75 nM 8.76
CHEMBL3604921 Ki = 70.2 nM 7.15
CHEMBL3604937 Ki = 833.0 nM 6.08