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Assay Detail

CHEMBL863589

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Binding
Binding affinity to Grb2-SH2 domain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Application of azide-alkyne cycloaddition 'click chemistry' for the synthesis of Grb2 SH2 domain-binding macrocycles.
Choi WJ, Shi ZD, Worthy KM, Bindu L, Karki RG, Nicklaus MC, Fisher RJ, Burke TR.
Bioorg Med Chem Lett (2006) 16 : 5265 -5269
PubMed 16908148 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.11 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427641 1 8.96
CHEMBL437910 1 8.74
CHEMBL385458 1 6.64
CHEMBL439177 1 -
CHEMBL385364 1 -
CHEMBL385459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427641 Kd = 1.1 nM 8.96
CHEMBL437910 Kd = 1.8 nM 8.74
CHEMBL385458 Kd = 230.0 nM 6.64
CHEMBL439177 Kd > 1000.0 nM -
CHEMBL385364 Kd > 1000.0 nM -
CHEMBL385459 Kd > 1000.0 nM -