Assay Detail
Binding
CHEMBL1646367
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant SHP2
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Tyrosine-protein phosphatase non-receptor type 11 (CHEMBL3864) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.84 | 5.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL301982 | CELASTROL | — | 1 | 5.48 |
| CHEMBL230006 | ENOXOLONE | 2.0 | 1 | 5.02 |
| CHEMBL1756 | ESTRAMUSTINE PHOSPHATE | 4.0 | 1 | 4.77 |
| CHEMBL1642763 | ESTRADIOL PHOSPHATE | — | 1 | 4.70 |
| CHEMBL432519 | TINGENONE | — | 1 | 4.21 |
| CHEMBL1575 | ESTRAMUSTINE | 3.0 | 1 | - |
| CHEMBL135 | ESTRADIOL | 4.0 | 1 | - |
| CHEMBL1642764 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL301982 | CELASTROL | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL230006 | ENOXOLONE | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL1756 | ESTRAMUSTINE PHOSPHATE | IC50 | = | 17100.0 | nM | 4.77 |
| CHEMBL1642763 | ESTRADIOL PHOSPHATE | IC50 | = | 19900.0 | nM | 4.70 |
| CHEMBL432519 | TINGENONE | IC50 | = | 61600.0 | nM | 4.21 |
| CHEMBL1575 | ESTRAMUSTINE | IC50 | > | 300000.0 | nM | - |
| CHEMBL135 | ESTRADIOL | IC50 | > | 300000.0 | nM | - |
| CHEMBL1642764 | — | IC50 | > | 300000.0 | nM | - |