Assay Detail
Binding
CHEMBL4043572
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Inhibition of Wistar rat heart mitochondrial CPT-1 assessed as reduction in conversion of palmitoyl CoA and L-carnitine into palmitoylcarnitine preincubated for 3 mins followed by L-carnitine and palmitoyl CoA addition measured for 3.5 mins by spectrophotometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Carnitine O-palmitoyltransferase 1, muscle isoform (CHEMBL3216) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.79 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1234355 | MALONYL-COENZYME A | — | 1 | 5.92 |
| CHEMBL75880 | PERHEXILINE | 4.0 | 1 | 4.96 |
| CHEMBL4097976 | — | — | 1 | 4.96 |
| CHEMBL1592481 | — | — | 1 | 4.85 |
| CHEMBL4077250 | — | — | 1 | 4.72 |
| CHEMBL1334033 | PERHEXILINE MALEATE | 4.0 | 1 | 4.50 |
| CHEMBL4081530 | — | — | 1 | 4.35 |
| CHEMBL4068222 | — | — | 1 | 4.06 |
| CHEMBL4059578 | — | — | 1 | - |
| CHEMBL4079982 | — | — | 1 | - |
| CHEMBL4097557 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1234355 | MALONYL-COENZYME A | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL75880 | PERHEXILINE | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4097976 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1592481 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4077250 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1334033 | PERHEXILINE MALEATE | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL4081530 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4068222 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL4059578 | — | IC50 | = | 215000.0 | nM | - |
| CHEMBL4079982 | — | IC50 | = | 475000.0 | nM | - |
| CHEMBL4097557 | — | IC50 | = | 715000.0 | nM | - |