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Assay Detail

CHEMBL869275

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of rat FAS
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Fatty acid synthase (CHEMBL3783)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
Rivkin A, Kim YR, Goulet MT, Bays N, Hill AD, Kariv I, Krauss S, Ginanni N, Strack PR, Kohl NE, Chung CC, Varnerin JP, Goudreau PN, Chang A, Tota MR, Munoz B.
Bioorg Med Chem Lett (2006) 16 : 4620 -4623
PubMed 16784844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.38 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212547 1 7.30
CHEMBL380035 1 7.14
CHEMBL378610 1 7.07
CHEMBL379396 1 6.91
CHEMBL214763 1 6.87
CHEMBL214764 1 6.76
CHEMBL211838 1 6.76
CHEMBL437299 1 6.35
CHEMBL413773 1 6.26
CHEMBL378095 1 6.16
CHEMBL212778 1 5.58
CHEMBL377646 1 5.52
CHEMBL214353 1 5.47
CHEMBL212823 1 5.22
CHEMBL213299 1 -
CHEMBL209582 1 -
CHEMBL213458 1 -
CHEMBL377915 1 -
CHEMBL209897 1 -
CHEMBL209576 1 -
CHEMBL209733 1 -
CHEMBL324519 1 -
CHEMBL209656 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212547 IC50 = 50.0 nM 7.30
CHEMBL380035 IC50 = 73.0 nM 7.14
CHEMBL378610 IC50 = 86.0 nM 7.07
CHEMBL379396 IC50 = 122.0 nM 6.91
CHEMBL214763 IC50 = 134.0 nM 6.87
CHEMBL214764 IC50 = 172.0 nM 6.76
CHEMBL211838 IC50 = 173.0 nM 6.76
CHEMBL437299 IC50 = 443.0 nM 6.35
CHEMBL413773 IC50 = 550.0 nM 6.26
CHEMBL378095 IC50 = 700.0 nM 6.16
CHEMBL212778 IC50 = 2600.0 nM 5.58
CHEMBL377646 IC50 = 3000.0 nM 5.52
CHEMBL214353 IC50 = 3400.0 nM 5.47
CHEMBL212823 IC50 = 6000.0 nM 5.22
CHEMBL213299 IC50 - -
CHEMBL209582 IC50 > 15000.0 nM -
CHEMBL213458 IC50 - -
CHEMBL377915 IC50 > 15000.0 nM -
CHEMBL209897 IC50 > 15000.0 nM -
CHEMBL209576 IC50 > 15000.0 nM -
CHEMBL209733 IC50 > 15000.0 nM -
CHEMBL324519 IC50 > 15000.0 nM -
CHEMBL209656 IC50 - -