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Assay Detail

CHEMBL679551

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Binding
Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor in A431 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.
Smaill JB, Palmer BD, Rewcastle GW, Denny WA, McNamara DJ, Dobrusin EM, Bridges AJ, Zhou H, Showalter HD, Winters RT, Leopold WR, Fry DW, Nelson JM, Slintak V, Elliot WL, Roberts BJ, Vincent PW, Patmore SJ.
J Med Chem (1999) 42 : 1803 -1815
PubMed 10346932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.01 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53637 1 8.64
CHEMBL430571 1 8.38
CHEMBL53690 1 8.35
CHEMBL31815 1 8.33
CHEMBL52913 1 7.28
CHEMBL297968 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53637 IC50 = 2.3 nM 8.64
CHEMBL430571 IC50 = 4.2 nM 8.38
CHEMBL53690 IC50 = 4.5 nM 8.35
CHEMBL31815 IC50 = 4.7 nM 8.33
CHEMBL52913 IC50 = 53.0 nM 7.28
CHEMBL297968 IC50 = 90.0 nM 7.05