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Assay Detail

CHEMBL677880

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

Binding
In vitro inhibitory activity against epidermal growth factor receptor
39
Total Activities
39
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

4-(Phenylamino)pyrrolopyrimidines: potent and selective, ATP site directed inhibitors of the EGF-receptor protein tyrosine kinase.
Traxler PM, Furet P, Mett H, Buchdunger E, Meyer T, Lydon N.
J Med Chem (1996) 39 : 2285 -2292
PubMed 8691423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.33 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29197 1 8.40
CHEMBL306315 1 8.22
CHEMBL311129 1 8.00
CHEMBL74722 1 7.60
CHEMBL306081 1 7.57
CHEMBL75177 1 7.54
CHEMBL72393 1 7.34
CHEMBL307209 1 7.02
CHEMBL74481 1 6.96
CHEMBL73406 1 6.77
CHEMBL75208 1 6.70
CHEMBL308593 1 6.64
CHEMBL268868 DAPH 1 6.52
CHEMBL433305 1 6.51
CHEMBL440873 1 6.44
CHEMBL72322 1 6.38
CHEMBL76444 1 6.30
CHEMBL308582 1 6.26
CHEMBL73710 1 6.25
CHEMBL307026 1 6.24
CHEMBL307062 1 6.09
CHEMBL431191 1 6.07
CHEMBL421686 1 5.97
CHEMBL73301 1 5.92
CHEMBL74778 1 5.90
CHEMBL306029 1 5.72
CHEMBL75049 1 5.72
CHEMBL307599 1 5.68
CHEMBL76116 1 5.60
CHEMBL4106341 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29197 IC50 = 4.0 nM 8.40
CHEMBL306315 IC50 = 6.0 nM 8.22
CHEMBL311129 IC50 = 10.0 nM 8.00
CHEMBL74722 IC50 = 25.0 nM 7.60
CHEMBL306081 IC50 = 27.0 nM 7.57
CHEMBL75177 IC50 = 29.0 nM 7.54
CHEMBL72393 IC50 = 46.0 nM 7.34
CHEMBL307209 IC50 = 96.0 nM 7.02
CHEMBL74481 IC50 = 110.0 nM 6.96
CHEMBL73406 IC50 = 170.0 nM 6.77
CHEMBL75208 IC50 = 200.0 nM 6.70
CHEMBL308593 IC50 = 230.0 nM 6.64
CHEMBL268868 DAPH IC50 = 300.0 nM 6.52
CHEMBL433305 IC50 = 310.0 nM 6.51
CHEMBL440873 IC50 = 360.0 nM 6.44
CHEMBL72322 IC50 = 420.0 nM 6.38
CHEMBL76444 IC50 = 500.0 nM 6.30
CHEMBL308582 IC50 = 550.0 nM 6.26
CHEMBL73710 IC50 = 560.0 nM 6.25
CHEMBL307026 IC50 = 570.0 nM 6.24
CHEMBL307062 IC50 = 820.0 nM 6.09
CHEMBL431191 IC50 = 860.0 nM 6.07
CHEMBL421686 IC50 = 1080.0 nM 5.97
CHEMBL73301 IC50 = 1200.0 nM 5.92
CHEMBL74778 IC50 = 1250.0 nM 5.90
CHEMBL306029 IC50 = 1900.0 nM 5.72
CHEMBL75049 IC50 = 1900.0 nM 5.72
CHEMBL307599 IC50 = 2100.0 nM 5.68
CHEMBL76116 IC50 = 2500.0 nM 5.60
CHEMBL4106341 IC50 = 6920.0 nM 5.16
CHEMBL431001 IC50 = 16300.0 nM 4.79
CHEMBL74645 IC50 = 25700.0 nM 4.59
CHEMBL73625 IC50 = 75100.0 nM 4.12
CHEMBL309937 IC50 = 77500.0 nM 4.11
CHEMBL310923 IC50 > 100000.0 nM -
CHEMBL72984 IC50 > 50000.0 nM -
CHEMBL72560 IC50 > 50000.0 nM -
CHEMBL73402 IC50 > 100000.0 nM -
CHEMBL72976 IC50 > 100000.0 nM -