Assay Detail
Binding
CHEMBL680002
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Inhibition of Grb2-SH2 domain binding to phospho-EGF receptor intracellular C-terminal domain
3
Total Activities
3
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
Structure-based design, synthesis, and X-ray crystallography of a high-affinity antagonist of the Grb2-SH2 domain containing an asparagine mimetic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.90 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL77689 | — | — | 1 | 9.00 |
| CHEMBL307890 | — | — | 1 | 8.80 |
| CHEMBL310056 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL77689 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL307890 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL310056 | — | IC50 | > | 5000.0 | nM | - |