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Assay Detail

CHEMBL829239

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

Binding
In vitro binding affinity for growth factor receptor bound protein 2 SH2 domain from human breast cancer cells
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Cancer cell lines
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of conformationally constrained Grb2 SH2 domain binding peptides employing alpha-methylphenylalanyl based phosphotyrosyl mimetics.
Oishi S, Karki RG, Kang SU, Wang X, Worthy KM, Bindu LK, Nicklaus MC, Fisher RJ, Burke TR.
J Med Chem (2005) 48 : 764 -772
PubMed 15689160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.13 10.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175456 4 10.01
CHEMBL424969 1 7.62
CHEMBL175689 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175456 Kd = 0.097 nM 10.01
CHEMBL175456 Kd = 2.28 nM 8.64
CHEMBL175456 Kd = 4.3 nM 8.37
CHEMBL424969 Kd = 23.8 nM 7.62
CHEMBL175456 Kd = 72.0 nM 7.14
CHEMBL175689 Kd = 97.8 nM 7.01