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Assay Detail

CHEMBL677832

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Binding
Inhibitory activity against epidermal growth factor receptor tyrosine kinase.
35
Total Activities
35
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

Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.
Traxler P, Bold G, Frei J, Lang M, Lydon N, Mett H, Buchdunger E, Meyer T, Mueller M, Furet P.
J Med Chem (1997) 40 : 3601 -3616
PubMed 9357527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 7.11 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121954 1 9.00
CHEMBL332906 1 8.70
CHEMBL332612 1 8.30
CHEMBL332882 1 8.30
CHEMBL118130 1 8.22
CHEMBL29197 1 8.22
CHEMBL122245 1 8.15
CHEMBL121796 1 8.15
CHEMBL120979 1 8.10
CHEMBL123189 1 8.10
CHEMBL122182 1 8.10
CHEMBL119977 1 7.72
CHEMBL331906 1 7.58
CHEMBL333231 1 7.58
CHEMBL332765 1 7.54
CHEMBL122411 1 7.52
CHEMBL332333 1 7.24
CHEMBL121260 1 7.08
CHEMBL332971 1 7.02
CHEMBL120069 1 6.89
CHEMBL120319 1 6.89
CHEMBL121190 1 6.80
CHEMBL122068 1 6.66
CHEMBL118904 1 6.57
CHEMBL420885 1 6.57
CHEMBL333038 1 6.48
CHEMBL122243 1 6.10
CHEMBL119982 1 6.06
CHEMBL319540 1 5.57
CHEMBL65063 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121954 IC50 = 1.0 nM 9.00
CHEMBL332906 IC50 = 2.0 nM 8.70
CHEMBL332612 IC50 = 5.0 nM 8.30
CHEMBL332882 IC50 = 5.0 nM 8.30
CHEMBL118130 IC50 = 6.0 nM 8.22
CHEMBL29197 IC50 = 6.0 nM 8.22
CHEMBL122245 IC50 = 7.0 nM 8.15
CHEMBL121796 IC50 = 7.0 nM 8.15
CHEMBL120979 IC50 = 8.0 nM 8.10
CHEMBL123189 IC50 = 8.0 nM 8.10
CHEMBL122182 IC50 = 8.0 nM 8.10
CHEMBL119977 IC50 = 19.0 nM 7.72
CHEMBL331906 IC50 = 26.0 nM 7.58
CHEMBL333231 IC50 = 26.0 nM 7.58
CHEMBL332765 IC50 = 29.0 nM 7.54
CHEMBL122411 IC50 = 30.0 nM 7.52
CHEMBL332333 IC50 = 58.0 nM 7.24
CHEMBL121260 IC50 = 84.0 nM 7.08
CHEMBL332971 IC50 = 96.0 nM 7.02
CHEMBL120069 IC50 = 130.0 nM 6.89
CHEMBL120319 IC50 = 130.0 nM 6.89
CHEMBL121190 IC50 = 160.0 nM 6.80
CHEMBL122068 IC50 = 220.0 nM 6.66
CHEMBL118904 IC50 = 270.0 nM 6.57
CHEMBL420885 IC50 = 270.0 nM 6.57
CHEMBL333038 IC50 = 330.0 nM 6.48
CHEMBL122243 IC50 = 800.0 nM 6.10
CHEMBL119982 IC50 = 870.0 nM 6.06
CHEMBL319540 IC50 = 2710.0 nM 5.57
CHEMBL65063 IC50 = 2700.0 nM 5.57
CHEMBL62756 IC50 = 15000.0 nM 4.82
CHEMBL334026 IC50 = 24200.0 nM 4.62
CHEMBL306081 IC50 = 27000.0 nM 4.57
CHEMBL120667 IC50 = 450000.0 nM -
CHEMBL120703 IC50 > 10000.0 nM -