Assay Detail
Binding
CHEMBL660894
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Inhibition of [14C]palmitoyl-CoA and carnitine binding to carnitine palmitoyltransferase I from rat liver mitochondria
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Mitochondria |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Carnitine O-palmitoyltransferase 1, liver isoform (CHEMBL3858) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of a long-chain carbamoyl aminocarnitine derivative, a reversible carnitine palmitoyltransferase inhibitor with antiketotic and antidiabetic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.27 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309568 | — | — | 1 | 6.16 |
| CHEMBL3559493 | — | — | 1 | 6.10 |
| CHEMBL3559494 | — | — | 1 | 5.96 |
| CHEMBL3559495 | — | — | 1 | 5.75 |
| CHEMBL3559496 | — | — | 1 | 5.50 |
| CHEMBL307495 | — | — | 1 | 5.22 |
| CHEMBL3559492 | — | — | 1 | 5.22 |
| CHEMBL3559498 | — | — | 1 | 5.02 |
| CHEMBL3559501 | — | — | 1 | 4.50 |
| CHEMBL3559497 | — | — | 1 | 4.36 |
| CHEMBL1231506 | TEGLICAR | 2.0 | 1 | 4.23 |
| CHEMBL3559499 | — | — | 1 | - |
| CHEMBL3559500 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309568 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3559493 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3559494 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3559495 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3559496 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL307495 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3559492 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3559498 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL3559501 | — | IC50 | = | 31300.0 | nM | 4.50 |
| CHEMBL3559497 | — | IC50 | = | 43600.0 | nM | 4.36 |
| CHEMBL1231506 | TEGLICAR | IC50 | = | 58800.0 | nM | 4.23 |
| CHEMBL3559499 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3559500 | — | IC50 | > | 300000.0 | nM | - |