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Assay Detail

CHEMBL676233

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

Binding
Inhibition of tyrosine/glutamic acid copolymer phosphorylation by epidermal growth factor receptor prepared of human A431
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.
Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA.
J Med Chem (1998) 41 : 742 -751
PubMed 9513602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.85 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162821 1 9.35
CHEMBL433520 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162821 IC50 = 0.45 nM 9.35
CHEMBL433520 IC50 = 4.6 nM 8.34