Assay Detail
Binding
CHEMBL1787264
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Inhibition of TPA-induced degradation of Pdcd4 (amino acid 39-91) expressed in human HEK293 cells assessed as minimum compound concentration required for 50% recovery of Pdcd4-luciferase signal incubated for 8 hrs by luciferase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Cryptocaryols A-H, α-pyrone-containing 1,3-polyols from Cryptocarya sp. implicated in stabilizing the tumor suppressor Pdcd4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 5.84 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | 7.30 |
| CHEMBL1784378 | CRYPTOCARYOL G | — | 1 | 5.89 |
| CHEMBL1784375 | CRYPTOCARYOL D | — | 1 | 5.82 |
| CHEMBL1784374 | CRYPTOCARYOL C | — | 1 | 5.80 |
| CHEMBL1784376 | CRYPTOCARYOL E | — | 1 | 5.75 |
| CHEMBL1784379 | CRYPTOCARYOL H | — | 1 | 5.75 |
| CHEMBL1784373 | CRYPTOCARYOL B | — | 1 | 5.52 |
| CHEMBL1784377 | CRYPTOCARYOL F | — | 1 | 5.46 |
| CHEMBL1784372 | CRYPTOCARYOL A | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1784378 | CRYPTOCARYOL G | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1784375 | CRYPTOCARYOL D | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL1784374 | CRYPTOCARYOL C | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1784376 | CRYPTOCARYOL E | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1784379 | CRYPTOCARYOL H | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1784373 | CRYPTOCARYOL B | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1784377 | CRYPTOCARYOL F | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1784372 | CRYPTOCARYOL A | EC50 | = | 4900.0 | nM | 5.31 |