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Assay Detail

CHEMBL677389

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

Binding
Inhibition of the phosphorylation of a random polyglutamic acid/tyrosine copolymer by human epidermal growth factor receptor(EGFR) prepared from human A431 carcinoma cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A-431
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. 11. Soluble analogues of pyrrolo- and pyrazoloquinazolines as epidermal growth factor receptor inhibitors: synthesis, biological evaluation, and modeling of the mode of binding.
Palmer BD, Trumpp-Kallmeyer S, Fry DW, Nelson JM, Showalter HD, Denny WA.
J Med Chem (1997) 40 : 1519 -1529
PubMed 9154973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.25 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 10.60
CHEMBL39320 1 9.43
CHEMBL40734 1 9.36
CHEMBL39337 1 9.36
CHEMBL289213 1 9.14
CHEMBL36727 1 9.10
CHEMBL416611 1 8.80
CHEMBL287007 1 8.59
CHEMBL39715 1 8.47
CHEMBL36164 1 8.46
CHEMBL40130 1 8.43
CHEMBL38199 1 8.43
CHEMBL36967 1 8.32
CHEMBL289162 1 8.29
CHEMBL39811 1 8.12
CHEMBL39355 1 8.06
CHEMBL37543 1 7.92
CHEMBL287289 1 7.68
CHEMBL290096 1 7.57
CHEMBL287832 1 7.40
CHEMBL37373 1 7.39
CHEMBL36819 1 7.28
CHEMBL289959 1 6.46
CHEMBL37346 1 5.26
CHEMBL289787 1 -
CHEMBL35820 1 -
CHEMBL37099 1 -
CHEMBL39563 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 0.025 nM 10.60
CHEMBL39320 IC50 = 0.37 nM 9.43
CHEMBL40734 IC50 = 0.44 nM 9.36
CHEMBL39337 IC50 = 0.44 nM 9.36
CHEMBL289213 IC50 = 0.72 nM 9.14
CHEMBL36727 IC50 = 0.8 nM 9.10
CHEMBL416611 IC50 = 1.6 nM 8.80
CHEMBL287007 IC50 = 2.6 nM 8.59
CHEMBL39715 IC50 = 3.4 nM 8.47
CHEMBL36164 IC50 = 3.5 nM 8.46
CHEMBL40130 IC50 = 3.7 nM 8.43
CHEMBL38199 IC50 = 3.7 nM 8.43
CHEMBL36967 IC50 = 4.8 nM 8.32
CHEMBL289162 IC50 = 5.1 nM 8.29
CHEMBL39811 IC50 = 7.5 nM 8.12
CHEMBL39355 IC50 = 8.8 nM 8.06
CHEMBL37543 IC50 = 12.0 nM 7.92
CHEMBL287289 IC50 = 21.0 nM 7.68
CHEMBL290096 IC50 = 27.0 nM 7.57
CHEMBL287832 IC50 = 40.0 nM 7.40
CHEMBL37373 IC50 = 41.0 nM 7.39
CHEMBL36819 IC50 = 53.0 nM 7.28
CHEMBL289959 IC50 = 346.0 nM 6.46
CHEMBL37346 IC50 = 5500.0 nM 5.26
CHEMBL289787 IC50 > 10000.0 nM -
CHEMBL35820 IC50 = 0.006 nM -
CHEMBL37099 IC50 > 10000.0 nM -
CHEMBL39563 IC50 > 100000.0 nM -