Assay Detail
Binding
CHEMBL874517
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In vitro inhibition of [14C]palmitoyl-CoA and carnitine binding to carnitine palmitoyltransferase I of rat heart 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, muscle isoform (CHEMBL3216) ↗| 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 | 4.70 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL309568 | — | — | 1 | 5.47 |
| CHEMBL3559493 | — | — | 1 | 5.24 |
| CHEMBL3559494 | — | — | 1 | 4.36 |
| CHEMBL3559501 | — | — | 1 | 4.33 |
| CHEMBL3559498 | — | — | 1 | 4.10 |
| CHEMBL3559499 | — | — | 1 | - |
| CHEMBL1231506 | TEGLICAR | 2.0 | 1 | - |
| CHEMBL3559496 | — | — | 1 | - |
| CHEMBL307495 | — | — | 1 | - |
| CHEMBL3559500 | — | — | 1 | - |
| CHEMBL3559495 | — | — | 1 | - |
| CHEMBL3559492 | — | — | 1 | - |
| CHEMBL3559497 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL309568 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3559493 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3559494 | — | IC50 | = | 43400.0 | nM | 4.36 |
| CHEMBL3559501 | — | IC50 | = | 46200.0 | nM | 4.33 |
| CHEMBL3559498 | — | IC50 | = | 80100.0 | nM | 4.10 |
| CHEMBL3559499 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL1231506 | TEGLICAR | IC50 | = | 167400.0 | nM | - |
| CHEMBL3559496 | — | IC50 | = | 118400.0 | nM | - |
| CHEMBL307495 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3559500 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3559495 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL3559492 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3559497 | — | IC50 | > | 300000.0 | nM | - |