Assay Detail
Binding
CHEMBL998624
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Inhibition of GFP-labeled PLD2 in human HEK293 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.22 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL471257 | — | — | 1 | 7.52 |
| CHEMBL471054 | — | — | 1 | 7.05 |
| CHEMBL511475 | — | — | 1 | 6.96 |
| CHEMBL471056 | — | — | 1 | 6.85 |
| CHEMBL511648 | — | — | 1 | 6.70 |
| CHEMBL471261 | — | — | 1 | 6.26 |
| CHEMBL471258 | — | — | 1 | 6.00 |
| CHEMBL471055 | — | — | 1 | 5.80 |
| CHEMBL513060 | — | — | 1 | 4.57 |
| CHEMBL471259 | — | — | 1 | 4.52 |
| CHEMBL470847 | — | — | 1 | - |
| CHEMBL471463 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL471257 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL471054 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL511475 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL471056 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL511648 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL471261 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL471258 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL471055 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL513060 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL471259 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL470847 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL471463 | — | IC50 | > | 20000.0 | nM | - |