Assay Detail
Binding
CHEMBL2330403
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Inhibition of PLD1 in human Calu-1 cells assessed as deuterated 1-butanol incorporation pretreated for 5 mins prior to substrate addition measured after 30 mins by mass spectrometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Calu-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.60 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2325485 | — | — | 1 | 8.22 |
| CHEMBL2325482 | — | — | 1 | 7.70 |
| CHEMBL2325486 | — | — | 1 | 7.12 |
| CHEMBL2325487 | — | — | 1 | 7.07 |
| CHEMBL2325483 | — | — | 1 | 6.12 |
| CHEMBL2325488 | — | — | 1 | 5.85 |
| CHEMBL2325484 | — | — | 1 | 5.81 |
| CHEMBL1254654 | — | — | 1 | 4.93 |
| CHEMBL1907089 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325485 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2325482 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2325486 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2325487 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2325483 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2325488 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2325484 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL1254654 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL1907089 | — | IC50 | > | 20000.0 | nM | - |