Assay Detail
Binding
CHEMBL2217072
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Inhibition of human CPT1A
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Carnitine O-palmitoyltransferase 1, liver isoform (CHEMBL1293194) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.54 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2216778 | — | — | 1 | 7.80 |
| CHEMBL2216774 | — | — | 1 | 7.70 |
| CHEMBL2216779 | — | — | 1 | 7.68 |
| CHEMBL2216776 | — | — | 1 | 7.58 |
| CHEMBL2216775 | — | — | 1 | 7.19 |
| CHEMBL2216777 | — | — | 1 | 6.80 |
| CHEMBL2216780 | — | — | 1 | 6.72 |
| CHEMBL1231506 | TEGLICAR | 2.0 | 1 | 5.98 |
| CHEMBL2216785 | — | — | 1 | 5.77 |
| CHEMBL2216771 | — | — | 1 | 5.62 |
| CHEMBL1231507 | PALMITOYLAMINOCARNITINE | — | 1 | 5.57 |
| CHEMBL2114397 | — | — | 1 | 4.12 |
| CHEMBL203266 | TRIMETAZIDINE | 3.0 | 1 | - |
| CHEMBL633 | AMIODARONE | 4.0 | 1 | - |
| CHEMBL75880 | PERHEXILINE | 4.0 | 1 | - |
| CHEMBL1232077 | OXFENICINE | 2.0 | 1 | - |
| CHEMBL129918 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2216778 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2216774 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2216779 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2216776 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2216775 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL2216777 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2216780 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1231506 | TEGLICAR | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL2216785 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2216771 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1231507 | PALMITOYLAMINOCARNITINE | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL2114397 | — | IC50 | = | 76400.0 | nM | 4.12 |
| CHEMBL203266 | TRIMETAZIDINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL633 | AMIODARONE | IC50 | = | 140000.0 | nM | - |
| CHEMBL75880 | PERHEXILINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL1232077 | OXFENICINE | IC50 | > | 100000.0 | nM | - |
| CHEMBL129918 | — | IC50 | > | 100000.0 | nM | - |