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Assay Detail

CHEMBL2217014

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Binding
Inhibition of carnitine palmitoyltransferase in rat liver mitochondria assessed as conversion of [14C]palmitic acid to [14C]palmitoylcarnitine by radiometric assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Mitochondria
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6 6.13 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2216784 1 6.92
CHEMBL2216785 1 6.89
CHEMBL307495 1 6.16
CHEMBL308869 1 6.10
CHEMBL1231506 TEGLICAR 2.0 1 5.96
CHEMBL114113 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2216784 IC50 = 120.0 nM 6.92
CHEMBL2216785 IC50 = 130.0 nM 6.89
CHEMBL307495 IC50 = 700.0 nM 6.16
CHEMBL308869 IC50 = 800.0 nM 6.10
CHEMBL1231506 TEGLICAR IC50 = 1100.0 nM 5.96
CHEMBL114113 IC50 = 17400.0 nM 4.76