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Assay Detail

CHEMBL674643

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

Binding
Inhibitory concentration of EGF dependent autophosphorylation of epidermal growth factor receptor kinase
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
Gazit A, Yaish P, Gilon C, Levitzki A.
J Med Chem (1989) 32 : 2344 -2352
PubMed 2552117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 5.03 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76589 1 6.90
CHEMBL77803 1 6.30
CHEMBL78257 TYRPHOSTIN 51 1 6.10
CHEMBL80745 1 5.92
CHEMBL77030 TYRPHOSTIN 47 1 5.62
CHEMBL309334 1 5.60
CHEMBL310798 TYRPHOSTIN 25 1 5.52
CHEMBL80155 1 5.22
CHEMBL296407 1 5.00
CHEMBL309598 1 4.87
CHEMBL47986 ERBSTATIN 1 4.85
CHEMBL73820 1 4.60
CHEMBL76904 TYRPHOSTIN 23 1 4.46
CHEMBL76905 1 4.43
CHEMBL76985 1 4.33
CHEMBL77243 1 4.26
CHEMBL309625 1 4.22
CHEMBL311119 1 4.22
CHEMBL76642 1 4.12
CHEMBL77085 1 4.02
CHEMBL311564 1 -
CHEMBL307248 1 -
CHEMBL307250 1 -
CHEMBL310958 1 -
CHEMBL78005 1 -
CHEMBL77595 1 -
CHEMBL77778 1 -
CHEMBL57712 1 -
CHEMBL77869 1 -
CHEMBL76082 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76589 IC50 = 125.0 nM 6.90
CHEMBL77803 IC50 = 500.0 nM 6.30
CHEMBL78257 TYRPHOSTIN 51 IC50 = 800.0 nM 6.10
CHEMBL80745 IC50 = 1200.0 nM 5.92
CHEMBL77030 TYRPHOSTIN 47 IC50 = 2400.0 nM 5.62
CHEMBL309334 IC50 = 2500.0 nM 5.60
CHEMBL310798 TYRPHOSTIN 25 IC50 = 3000.0 nM 5.52
CHEMBL80155 IC50 = 6000.0 nM 5.22
CHEMBL296407 IC50 = 10000.0 nM 5.00
CHEMBL309598 IC50 = 13500.0 nM 4.87
CHEMBL47986 ERBSTATIN IC50 = 14000.0 nM 4.85
CHEMBL73820 IC50 = 25000.0 nM 4.60
CHEMBL76904 TYRPHOSTIN 23 IC50 = 35000.0 nM 4.46
CHEMBL76905 IC50 = 37000.0 nM 4.43
CHEMBL76985 IC50 = 47000.0 nM 4.33
CHEMBL77243 IC50 = 55000.0 nM 4.26
CHEMBL311119 IC50 = 60000.0 nM 4.22
CHEMBL309625 IC50 = 60000.0 nM 4.22
CHEMBL76642 IC50 = 75000.0 nM 4.12
CHEMBL77085 IC50 = 96000.0 nM 4.02
CHEMBL310400 IC50 = 375000.0 nM -
CHEMBL76602 alpha-CYANO-4-HYDROXYCINNAMIC ACID IC50 = 165000.0 nM -
CHEMBL79064 IC50 = 230000.0 nM -
CHEMBL75718 IC50 = 2400000.0 nM -
CHEMBL77298 IC50 = 153000.0 nM -
CHEMBL77280 IC50 > 1250000.0 nM -
CHEMBL66879 COUMARIC ACID IC50 = 3000000.0 nM -
CHEMBL76979 IC50 = 264000.0 nM -
CHEMBL77724 IC50 > 1250000.0 nM -
CHEMBL420385 IC50 > 625000.0 nM -
CHEMBL1009 LEVODOPA IC50 = 900000.0 nM -
CHEMBL77825 IC50 = 600000.0 nM -
CHEMBL421877 IC50 = 850000.0 nM -
CHEMBL309866 IC50 = 1300000.0 nM -
CHEMBL77381 IC50 = 1360000.0 nM -
CHEMBL307179 IC50 = 160000.0 nM -
CHEMBL308133 IC50 = 1500000.0 nM -
CHEMBL78150 TYRPHOSTIN A9 IC50 = 460000.0 nM -
CHEMBL310514 IC50 = 260000.0 nM -
CHEMBL305695 IC50 = 560000.0 nM -
CHEMBL76082 IC50 = 560000.0 nM -
CHEMBL77869 IC50 = 200000.0 nM -
CHEMBL57712 IC50 = 1300000.0 nM -
CHEMBL77778 IC50 = 450000.0 nM -
CHEMBL77595 IC50 = 850000.0 nM -
CHEMBL78005 IC50 = 350000.0 nM -
CHEMBL310958 IC50 = 225000.0 nM -
CHEMBL307250 IC50 = 325000.0 nM -
CHEMBL307248 IC50 = 640000.0 nM -
CHEMBL311564 IC50 = 450000.0 nM -