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Assay Detail

CHEMBL3761494

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

Binding
Inhibition of EGFR T790M/L858R mutant autophosphorylation in human H1975 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type H1975
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP.
Bioorg Med Chem Lett (2016) 26 : 534 -539
PubMed 26639762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.06 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3758739 1 6.43
CHEMBL3758502 1 6.22
CHEMBL3759096 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3758739 IC50 = 370.0 nM 6.43
CHEMBL3758502 IC50 = 600.0 nM 6.22
CHEMBL3759096 IC50 = 3000.0 nM 5.52