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Assay Detail

CHEMBL677470

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

Binding
Inhibitory concentration compound against EFGR tyrosine kinase obtained from plasma membrane vesicles from cultured A431 cells
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
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. 4. Structure-activity relationships among N- and 3-substituted 2,2'-dithiobis(1H-indoles) for in vitro inhibition of receptor and nonreceptor protein tyrosine kinases.
Palmer BD, Rewcastle GW, Thompson AM, Boyd M, Showalter HD, Sercel AD, Fry DW, Kraker AJ, Denny WA.
J Med Chem (1995) 38 : 58 -67
PubMed 7837241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 4.96 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158275 1 5.77
CHEMBL342929 1 5.75
CHEMBL336174 1 5.48
CHEMBL79704 1 5.38
CHEMBL293889 1 5.37
CHEMBL157807 1 5.33
CHEMBL158805 1 5.28
CHEMBL346770 1 5.26
CHEMBL351920 1 5.25
CHEMBL161226 1 5.21
CHEMBL346553 1 5.21
CHEMBL160566 1 5.16
CHEMBL160935 1 5.11
CHEMBL345211 1 5.00
CHEMBL304414 1 4.96
CHEMBL345837 1 4.92
CHEMBL347659 1 4.89
CHEMBL347160 1 4.82
CHEMBL347161 1 4.77
CHEMBL348554 1 4.76
CHEMBL160207 1 4.67
CHEMBL347854 1 4.54
CHEMBL158797 1 4.37
CHEMBL435054 1 4.33
CHEMBL345862 1 4.33
CHEMBL422540 1 4.00
CHEMBL345641 1 4.00
CHEMBL348069 1 -
CHEMBL158879 1 -
CHEMBL349762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158275 IC50 = 1700.0 nM 5.77
CHEMBL342929 IC50 = 1800.0 nM 5.75
CHEMBL336174 IC50 = 3300.0 nM 5.48
CHEMBL79704 IC50 = 4200.0 nM 5.38
CHEMBL293889 IC50 = 4300.0 nM 5.37
CHEMBL157807 IC50 = 4700.0 nM 5.33
CHEMBL158805 IC50 = 5300.0 nM 5.28
CHEMBL346770 IC50 = 5500.0 nM 5.26
CHEMBL351920 IC50 = 5600.0 nM 5.25
CHEMBL161226 IC50 = 6100.0 nM 5.21
CHEMBL346553 IC50 = 6100.0 nM 5.21
CHEMBL160566 IC50 = 6900.0 nM 5.16
CHEMBL160935 IC50 = 7700.0 nM 5.11
CHEMBL345211 IC50 = 10000.0 nM 5.00
CHEMBL304414 IC50 = 10900.0 nM 4.96
CHEMBL345837 IC50 = 12000.0 nM 4.92
CHEMBL347659 IC50 = 13000.0 nM 4.89
CHEMBL347160 IC50 = 15000.0 nM 4.82
CHEMBL347161 IC50 = 16900.0 nM 4.77
CHEMBL348554 IC50 = 17500.0 nM 4.76
CHEMBL160207 IC50 = 21200.0 nM 4.67
CHEMBL347854 IC50 = 28700.0 nM 4.54
CHEMBL158797 IC50 = 43000.0 nM 4.37
CHEMBL435054 IC50 = 47000.0 nM 4.33
CHEMBL345862 IC50 = 47000.0 nM 4.33
CHEMBL422540 IC50 = 100000.0 nM 4.00
CHEMBL345641 IC50 = 100000.0 nM 4.00
CHEMBL352010 IC50 > 100000.0 nM -
CHEMBL158596 IC50 > 100000.0 nM -
CHEMBL347256 IC50 > 100000.0 nM -
CHEMBL345622 IC50 > 100000.0 nM -
CHEMBL314029 IC50 > 100000.0 nM -
CHEMBL61278 IC50 > 100000.0 nM -
CHEMBL156281 IC50 > 100000.0 nM -
CHEMBL349322 IC50 > 100000.0 nM -
CHEMBL156020 IC50 > 100000.0 nM -
CHEMBL349762 IC50 > 100000.0 nM -
CHEMBL158879 IC50 > 100000.0 nM -
CHEMBL348069 IC50 > 100000.0 nM -