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Assay Detail

CHEMBL1932339

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

Binding
Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA
12
Total Activities
12
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 Autocuration

Target

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

Publication

N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.
Gangjee A, Kurup S, Ihnat MA, Thorpe JE, Disch B.
Bioorg Med Chem (2012) 20 : 910 -914
PubMed 22204741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.82 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 6.64
CHEMBL1095465 1 6.62
CHEMBL553 ERLOTINIB 4.0 1 5.92
CHEMBL1095464 1 5.04
CHEMBL1929555 1 4.90
CHEMBL474538 1 -
CHEMBL1929552 1 -
CHEMBL1929553 1 -
CHEMBL1929554 1 -
CHEMBL1929556 1 -
CHEMBL1929557 1 -
CHEMBL535 SUNITINIB 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 230.0 nM 6.64
CHEMBL1095465 IC50 = 240.0 nM 6.62
CHEMBL553 ERLOTINIB IC50 = 1200.0 nM 5.92
CHEMBL1095464 IC50 = 9190.0 nM 5.04
CHEMBL1929555 IC50 = 12620.0 nM 4.90
CHEMBL474538 IC50 > 200000.0 nM -
CHEMBL1929552 IC50 > 50000.0 nM -
CHEMBL1929553 IC50 > 200000.0 nM -
CHEMBL1929554 IC50 = 112100.0 nM -
CHEMBL1929556 IC50 = 112700.0 nM -
CHEMBL1929557 IC50 > 200000.0 nM -
CHEMBL535 SUNITINIB IC50 = 172100.0 nM -