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Assay Detail

CHEMBL957461

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

Binding
Inhibition of EGFR expressed in human tumor cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.
Gangjee A, Namjoshi OA, Yu J, Ihnat MA, Thorpe JE, Warnke LA.
Bioorg Med Chem (2008) 16 : 5514 -5528
PubMed 18467105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.67 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 6.70
CHEMBL485320 1 6.52
CHEMBL502015 1 5.91
CHEMBL483313 1 5.88
CHEMBL499344 1 5.78
CHEMBL485321 1 5.66
CHEMBL519147 1 5.50
CHEMBL482489 1 5.47
CHEMBL499345 1 5.37
CHEMBL484109 1 5.33
CHEMBL484108 1 5.32
CHEMBL504416 1 4.64
CHEMBL520803 1 -
CHEMBL483312 1 -
CHEMBL483108 1 -
CHEMBL482715 1 -
CHEMBL474538 1 -
CHEMBL499067 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 200.0 nM 6.70
CHEMBL485320 IC50 = 300.0 nM 6.52
CHEMBL502015 IC50 = 1240.0 nM 5.91
CHEMBL483313 IC50 = 1320.0 nM 5.88
CHEMBL499344 IC50 = 1670.0 nM 5.78
CHEMBL485321 IC50 = 2200.0 nM 5.66
CHEMBL519147 IC50 = 3180.0 nM 5.50
CHEMBL482489 IC50 = 3400.0 nM 5.47
CHEMBL499345 IC50 = 4310.0 nM 5.37
CHEMBL484109 IC50 = 4700.0 nM 5.33
CHEMBL484108 IC50 = 4800.0 nM 5.32
CHEMBL504416 IC50 = 22800.0 nM 4.64
CHEMBL520803 IC50 > 200000.0 nM -
CHEMBL483312 IC50 > 200000.0 nM -
CHEMBL483108 IC50 > 200000.0 nM -
CHEMBL482715 IC50 = 122000.0 nM -
CHEMBL474538 IC50 > 50000.0 nM -
CHEMBL499067 IC50 > 200000.0 nM -