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Assay Detail

CHEMBL685573

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

Binding
The compound was evaluated for its potency to inhibit the interaction between Growth factor receptor bound protein 2 and phosphotyrosine-containing peptides derived from Shc Y317
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Small peptides containing phosphotyrosine and adjacent alphaMe-phosphotyrosine or its mimetics as highly potent inhibitors of Grb2 SH2 domain.
Liu WQ, Vidal M, Gresh N, Roques BP, Garbay C.
J Med Chem (1999) 42 : 3737 -3741
PubMed 10479306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.76 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3142999 1 7.96
CHEMBL77689 1 6.92
CHEMBL3143002 1 6.82
CHEMBL3143003 1 6.70
CHEMBL3143006 1 6.63
CHEMBL3142993 1 6.30
CHEMBL3143004 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3142999 IC50 = 11.0 nM 7.96
CHEMBL77689 IC50 = 120.0 nM 6.92
CHEMBL3143002 IC50 = 153.0 nM 6.82
CHEMBL3143003 IC50 = 198.0 nM 6.70
CHEMBL3143006 IC50 = 235.0 nM 6.63
CHEMBL3142993 IC50 = 497.0 nM 6.30
CHEMBL3143004 IC50 = 1098.0 nM 5.96