Assay Detail
Binding
CHEMBL1040547
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Inhibition of GSK3-beta expressed in insect Sf9 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Development of 5-benzylpaullones and paullone-9-carboxylic acid alkyl esters as selective inhibitors of mitochondrial malate dehydrogenase (mMDH).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.60 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50894 | ALSTERPAULLONE | — | 1 | 8.40 |
| CHEMBL299756 | PAULLONE 2 | — | 1 | 8.00 |
| CHEMBL325654 | — | — | 1 | 7.75 |
| CHEMBL296586 | KENPAULLONE | — | 1 | 7.64 |
| CHEMBL98153 | — | — | 1 | 7.62 |
| CHEMBL329505 | — | — | 1 | 7.52 |
| CHEMBL99037 | — | — | 1 | 7.10 |
| CHEMBL319373 | — | — | 1 | 7.00 |
| CHEMBL317964 | — | — | 1 | 6.89 |
| CHEMBL318471 | — | — | 1 | 6.70 |
| CHEMBL318208 | — | — | 1 | 6.40 |
| CHEMBL430574 | PAULLONE | — | 1 | 6.21 |
| CHEMBL316485 | — | — | 1 | 5.68 |
| CHEMBL99280 | — | — | 1 | 5.40 |
| CHEMBL95477 | — | — | 1 | 5.37 |
| CHEMBL316512 | — | — | 1 | 5.30 |
| CHEMBL99779 | PAULLONE | — | 1 | 5.00 |
| CHEMBL330398 | — | — | 1 | 4.80 |
| CHEMBL99423 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50894 | ALSTERPAULLONE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL299756 | PAULLONE 2 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL325654 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL296586 | KENPAULLONE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL98153 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL329505 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL99037 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL319373 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL317964 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL318471 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL318208 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL430574 | PAULLONE | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL316485 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL99280 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL95477 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL316512 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL99779 | PAULLONE | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL330398 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL99423 | — | IC50 | = | 140000.0 | nM | - |