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Assay Detail

CHEMBL674693

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

Binding
Inhibition of Epidermal growth factor receptor (EGF-R) tyrosine kinase activity
19
Total Activities
19
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

7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Widler L, Green J, Missbach M, Susa M, Altmann E.
Bioorg Med Chem Lett (2001) 11 : 849 -852
PubMed 11277535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.06 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169390 1 7.10
CHEMBL169570 1 6.60
CHEMBL355330 1 6.52
CHEMBL354310 1 6.48
CHEMBL352801 1 6.38
CHEMBL171311 1 6.36
CHEMBL355191 1 6.35
CHEMBL168382 1 6.34
CHEMBL168550 1 6.31
CHEMBL352954 1 6.30
CHEMBL170724 1 6.24
CHEMBL166765 1 6.22
CHEMBL166766 1 6.14
CHEMBL168285 1 6.10
CHEMBL168266 1 5.55
CHEMBL169467 1 5.47
CHEMBL168555 1 5.01
CHEMBL170438 1 4.88
CHEMBL171256 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169390 IC50 = 80.0 nM 7.10
CHEMBL169570 IC50 = 250.0 nM 6.60
CHEMBL355330 IC50 = 300.0 nM 6.52
CHEMBL354310 IC50 = 330.0 nM 6.48
CHEMBL352801 IC50 = 420.0 nM 6.38
CHEMBL171311 IC50 = 440.0 nM 6.36
CHEMBL355191 IC50 = 450.0 nM 6.35
CHEMBL168382 IC50 = 460.0 nM 6.34
CHEMBL168550 IC50 = 490.0 nM 6.31
CHEMBL352954 IC50 = 500.0 nM 6.30
CHEMBL170724 IC50 = 570.0 nM 6.24
CHEMBL166765 IC50 = 600.0 nM 6.22
CHEMBL166766 IC50 = 730.0 nM 6.14
CHEMBL168285 IC50 = 790.0 nM 6.10
CHEMBL168266 IC50 = 2820.0 nM 5.55
CHEMBL169467 IC50 = 3400.0 nM 5.47
CHEMBL168555 IC50 = 9700.0 nM 5.01
CHEMBL170438 IC50 = 13200.0 nM 4.88
CHEMBL171256 IC50 = 14400.0 nM 4.84