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

CHEMBL1920033

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

Binding
Inhibition of EGFR by Z-LYTE assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.
Kaspersen SJ, Sørum C, Willassen V, Fuglseth E, Kjøbli E, Bjørkøy G, Sundby E, Hoff BH.
Eur J Med Chem (2011) 46 : 6002 -6014
PubMed 22018877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.64 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL587723 AEE-788 2.0 1 8.70
CHEMBL105053 1 8.48
CHEMBL1914461 1 8.48
CHEMBL1914653 1 8.43
CHEMBL1914654 1 8.42
CHEMBL1914665 1 8.40
CHEMBL1914667 1 8.33
CHEMBL1914668 1 8.18
CHEMBL1914658 1 8.10
CHEMBL1914660 1 8.05
CHEMBL1914670 1 7.92
CHEMBL1914674 1 7.85
CHEMBL1914659 1 7.77
CHEMBL1914662 1 7.58
CHEMBL1914672 1 7.57
CHEMBL1914673 1 7.54
CHEMBL1914671 1 7.48
CHEMBL1914663 1 7.35
CHEMBL1914664 1 7.28
CHEMBL1914655 1 7.21
CHEMBL1914669 1 7.20
CHEMBL1914661 1 7.02
CHEMBL1914656 1 6.35
CHEMBL1914666 1 6.00
CHEMBL1914657 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL587723 AEE-788 IC50 = 2.0 nM 8.70
CHEMBL105053 IC50 = 3.3 nM 8.48
CHEMBL1914461 IC50 = 3.3 nM 8.48
CHEMBL1914653 IC50 = 3.7 nM 8.43
CHEMBL1914654 IC50 = 3.8 nM 8.42
CHEMBL1914665 IC50 = 4.0 nM 8.40
CHEMBL1914667 IC50 = 4.7 nM 8.33
CHEMBL1914668 IC50 = 6.6 nM 8.18
CHEMBL1914658 IC50 = 8.0 nM 8.10
CHEMBL1914660 IC50 = 9.0 nM 8.05
CHEMBL1914670 IC50 = 12.0 nM 7.92
CHEMBL1914674 IC50 = 14.0 nM 7.85
CHEMBL1914659 IC50 = 17.0 nM 7.77
CHEMBL1914662 IC50 = 26.0 nM 7.58
CHEMBL1914672 IC50 = 27.0 nM 7.57
CHEMBL1914673 IC50 = 29.0 nM 7.54
CHEMBL1914671 IC50 = 33.0 nM 7.48
CHEMBL1914663 IC50 = 45.0 nM 7.35
CHEMBL1914664 IC50 = 52.0 nM 7.28
CHEMBL1914655 IC50 = 62.0 nM 7.21
CHEMBL1914669 IC50 = 63.0 nM 7.20
CHEMBL1914661 IC50 = 95.0 nM 7.02
CHEMBL1914656 IC50 = 450.0 nM 6.35
CHEMBL1914666 IC50 = 1008.0 nM 6.00
CHEMBL1914657 IC50 = 4608.0 nM 5.34