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Assay Detail

CHEMBL680026

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Functional
Tested for ability to inhibit autophosphorylation of the Epidermal growth factor receptor in human epidermoid carcinoma cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.
Rewcastle GW, Bridges AJ, Fry DW, Rubin JR, Denny WA.
J Med Chem (1997) 40 : 1820 -1826
PubMed 9191958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.00 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294475 1 8.51
CHEMBL53426 1 8.29
CHEMBL53777 1 7.66
CHEMBL299622 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294475 IC50 = 3.1 nM 8.51
CHEMBL53426 IC50 = 5.1 nM 8.29
CHEMBL53777 IC50 = 22.0 nM 7.66
CHEMBL299622 IC50 = 30.0 nM 7.52