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Assay Detail

CHEMBL2217026

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Binding
Inhibition of human CPT2
14
Total Activities
14
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 2, mitochondrial (CHEMBL3238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research.
Ceccarelli SM, Chomienne O, Gubler M, Arduini A.
J Med Chem (2011) 54 : 3109 -3152
PubMed 21504156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.64 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1231507 PALMITOYLAMINOCARNITINE 1 6.85
CHEMBL1231506 TEGLICAR 2.0 1 6.80
CHEMBL2216779 1 6.13
CHEMBL2216777 1 5.55
CHEMBL2114397 1 5.41
CHEMBL2216771 1 5.33
CHEMBL2216774 1 5.32
CHEMBL2216785 1 5.27
CHEMBL75880 PERHEXILINE 4.0 1 4.14
CHEMBL129918 1 -
CHEMBL1232077 OXFENICINE 2.0 1 -
CHEMBL633 AMIODARONE 4.0 1 -
CHEMBL203266 TRIMETAZIDINE 3.0 1 -
CHEMBL2216778 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1231507 PALMITOYLAMINOCARNITINE IC50 = 140.0 nM 6.85
CHEMBL1231506 TEGLICAR IC50 = 160.0 nM 6.80
CHEMBL2216779 IC50 = 740.0 nM 6.13
CHEMBL2216777 IC50 = 2800.0 nM 5.55
CHEMBL2114397 IC50 = 3900.0 nM 5.41
CHEMBL2216771 IC50 = 4700.0 nM 5.33
CHEMBL2216774 IC50 = 4800.0 nM 5.32
CHEMBL2216785 IC50 = 5400.0 nM 5.27
CHEMBL75880 PERHEXILINE IC50 = 72800.0 nM 4.14
CHEMBL129918 IC50 > 100000.0 nM -
CHEMBL1232077 OXFENICINE IC50 > 100000.0 nM -
CHEMBL633 AMIODARONE IC50 > 100000.0 nM -
CHEMBL203266 TRIMETAZIDINE IC50 > 100000.0 nM -
CHEMBL2216778 IC50 > 100000.0 nM -