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Assay Detail

CHEMBL675521

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

Binding
Inhibition of Epidermal growth factor receptor (EGFr) tyrosine kinase
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.
Hamby JM, Connolly CJ, Schroeder MC, Winters RT, Showalter HD, Panek RL, Major TC, Olsewski B, Ryan MJ, Dahring T, Lu GH, Keiser J, Amar A, Shen C, Kraker AJ, Slintak V, Nelson JM, Fry DW, Bradford L, Hallak H, Doherty AM.
J Med Chem (1997) 40 : 2296 -2303
PubMed 9240345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.92 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57347 1 6.82
CHEMBL45827 1 6.62
CHEMBL57366 1 6.35
CHEMBL57323 1 6.21
CHEMBL301483 1 5.90
CHEMBL432738 1 5.87
CHEMBL299026 1 5.21
CHEMBL56236 1 5.17
CHEMBL75188 1 5.16
CHEMBL299763 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57347 IC50 = 150.0 nM 6.82
CHEMBL45827 IC50 = 240.0 nM 6.62
CHEMBL57366 IC50 = 450.0 nM 6.35
CHEMBL57323 IC50 = 610.0 nM 6.21
CHEMBL301483 IC50 = 1260.0 nM 5.90
CHEMBL432738 IC50 = 1360.0 nM 5.87
CHEMBL299026 IC50 = 6200.0 nM 5.21
CHEMBL56236 IC50 = 6680.0 nM 5.17
CHEMBL75188 IC50 = 7000.0 nM 5.16
CHEMBL299763 IC50 > 50000.0 nM -