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Assay Detail

CHEMBL674017

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Binding
Inhibition of EGF-stimulated autophosphorylation of epidermal growth factor receptor (EGFR) in A431 cells
13
Total Activities
13
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 13 8.13 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54091 1 8.68
CHEMBL280757 1 8.57
CHEMBL31373 1 8.51
CHEMBL53555 1 8.48
CHEMBL51659 1 8.47
CHEMBL285063 1 8.37
CHEMBL296168 1 8.25
CHEMBL54088 1 8.08
CHEMBL51741 1 8.00
CHEMBL443523 1 7.85
CHEMBL53665 1 7.75
CHEMBL28418 1 7.75
CHEMBL49986 1 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54091 IC50 = 2.1 nM 8.68
CHEMBL280757 IC50 = 2.7 nM 8.57
CHEMBL31373 IC50 = 3.1 nM 8.51
CHEMBL53555 IC50 = 3.3 nM 8.48
CHEMBL51659 IC50 = 3.4 nM 8.47
CHEMBL285063 IC50 = 4.3 nM 8.37
CHEMBL296168 IC50 = 5.6 nM 8.25
CHEMBL54088 IC50 = 8.3 nM 8.08
CHEMBL51741 IC50 = 9.9 nM 8.00
CHEMBL443523 IC50 = 14.0 nM 7.85
CHEMBL53665 IC50 = 18.0 nM 7.75
CHEMBL28418 IC50 = 18.0 nM 7.75
CHEMBL49986 IC50 = 108.0 nM 6.97