Assay Detail
Binding
CHEMBL4628267
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Inhibition of mouse recombinant C-terminal FLAG-tagged SMS2 expressed in mammalian expression system using C14-phosphatidylcholineD72 and C17-ceramide pre-incubated for 60 mins followed by incubation with substrate for 30 mins measured by RapidFire/MS assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylcholine:ceramide cholinephosphotransferase 2 (CHEMBL4523444) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Discovery of 1,8-naphthyridin-2-one derivative as a potent and selective sphingomyelin synthase 2 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.16 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4645607 | — | — | 1 | 8.66 |
| CHEMBL4641888 | — | — | 1 | 8.52 |
| CHEMBL4646354 | — | — | 1 | 8.11 |
| CHEMBL4644293 | — | — | 1 | 7.85 |
| CHEMBL4638337 | — | — | 1 | 7.72 |
| CHEMBL4646540 | — | — | 1 | 7.50 |
| CHEMBL4639746 | — | — | 1 | 7.29 |
| CHEMBL4634697 | — | — | 1 | 6.92 |
| CHEMBL4638097 | — | — | 1 | 6.72 |
| CHEMBL4634669 | — | — | 1 | 6.62 |
| CHEMBL4637599 | — | — | 1 | 6.58 |
| CHEMBL4635147 | — | — | 1 | 6.47 |
| CHEMBL4649105 | — | — | 1 | 6.23 |
| CHEMBL4644982 | — | — | 1 | 6.18 |
| CHEMBL4162182 | — | — | 1 | 5.96 |
| CHEMBL4647686 | — | — | 1 | - |
| CHEMBL4633986 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4645607 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4641888 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4646354 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4644293 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4638337 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4646540 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4639746 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4634697 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4638097 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4634669 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4637599 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4635147 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4649105 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4644982 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4162182 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4647686 | — | IC50 | - | — | - | |
| CHEMBL4633986 | — | IC50 | - | — | - |