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Assay Detail

CHEMBL2217072

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Binding
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.
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 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 -