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Assay Detail

CHEMBL683042

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

Binding
Inhibition of human epidermal growth factor receptor
13
Total Activities
13
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

Development of a binding model to protein tyrosine kinases for substituted pyrido[2,3-d]pyrimidine inhibitors.
Trumpp-Kallmeyer S, Rubin JR, Humblet C, Hamby JM, Showalter HD.
J Med Chem (1998) 41 : 1752 -1763
PubMed 9599227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.87 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301612 1 7.11
CHEMBL49120 PD-0166285 1.0 1 6.46
CHEMBL45827 1 6.41
CHEMBL298679 1 6.14
CHEMBL51028 1 6.06
CHEMBL51485 1 6.01
CHEMBL50470 1 5.87
CHEMBL49596 1 5.25
CHEMBL299194 1 5.06
CHEMBL299763 1 4.30
CHEMBL50977 1 -
CHEMBL51573 1 -
CHEMBL299347 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301612 IC50 = 78.0 nM 7.11
CHEMBL49120 PD-0166285 IC50 = 350.0 nM 6.46
CHEMBL45827 IC50 = 390.0 nM 6.41
CHEMBL298679 IC50 = 720.0 nM 6.14
CHEMBL51028 IC50 = 880.0 nM 6.06
CHEMBL51485 IC50 = 980.0 nM 6.01
CHEMBL50470 IC50 = 1350.0 nM 5.87
CHEMBL49596 IC50 = 5600.0 nM 5.25
CHEMBL299194 IC50 = 8700.0 nM 5.06
CHEMBL299763 IC50 = 50000.0 nM 4.30
CHEMBL50977 IC50 > 50000.0 nM -
CHEMBL51573 IC50 > 50000.0 nM -
CHEMBL299347 IC50 > 50000.0 nM -