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Assay Detail

CHEMBL675384

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

Binding
Inhibition of Grb-SH2 domain binding to phosphorylated carboxy-terminal intracellular domain of epidermal growth factor receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Growth factor receptor-bound protein 2 (CHEMBL3663)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly potent inhibitors of the Grb2-SH2 domain.
Schoepfer J, Fretz H, Gay B, Furet P, García-Echeverría C, End N, Caravatti G.
Bioorg Med Chem Lett (1999) 9 : 221 -226
PubMed 10021933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.20 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73003 1 9.52
CHEMBL72036 1 9.40
CHEMBL72694 1 9.05
CHEMBL431982 1 8.92
CHEMBL72525 1 8.47
CHEMBL72996 1 8.04
CHEMBL70852 1 7.85
CHEMBL72437 1 7.83
CHEMBL431381 1 7.23
CHEMBL72114 1 7.09
CHEMBL71034 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73003 IC50 = 0.3 nM 9.52
CHEMBL72036 IC50 = 0.4 nM 9.40
CHEMBL72694 IC50 = 0.9 nM 9.05
CHEMBL431982 IC50 = 1.2 nM 8.92
CHEMBL72525 IC50 = 3.4 nM 8.47
CHEMBL72996 IC50 = 9.2 nM 8.04
CHEMBL70852 IC50 = 14.0 nM 7.85
CHEMBL72437 IC50 = 14.7 nM 7.83
CHEMBL431381 IC50 = 59.0 nM 7.23
CHEMBL72114 IC50 = 81.0 nM 7.09
CHEMBL71034 IC50 = 155.0 nM 6.81