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Assay Detail

CHEMBL869274

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

Binding
Inhibition of human FAS
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Fatty acid synthase (CHEMBL4158)
Type SINGLE PROTEIN
Organism Homo sapiens

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 25 6.63 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213634 1 7.72
CHEMBL375390 1 7.28
CHEMBL214037 1 7.27
CHEMBL213583 1 7.17
CHEMBL377865 1 7.00
CHEMBL385709 1 6.90
CHEMBL213458 1 6.87
CHEMBL376206 1 6.71
CHEMBL380035 1 6.68
CHEMBL209656 1 6.40
CHEMBL373985 1 6.14
CHEMBL213635 1 6.13
CHEMBL213299 1 5.89
CHEMBL413773 1 5.85
CHEMBL215910 1 5.38
CHEMBL209733 1 -
CHEMBL209897 1 -
CHEMBL209576 1 -
CHEMBL209582 1 -
CHEMBL214361 1 -
CHEMBL386578 1 -
CHEMBL211799 1 -
CHEMBL214093 1 -
CHEMBL212973 1 -
CHEMBL436792 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213634 IC50 = 19.0 nM 7.72
CHEMBL375390 IC50 = 52.0 nM 7.28
CHEMBL214037 IC50 = 54.0 nM 7.27
CHEMBL213583 IC50 = 68.0 nM 7.17
CHEMBL377865 IC50 = 101.0 nM 7.00
CHEMBL385709 IC50 = 127.0 nM 6.90
CHEMBL213458 IC50 = 136.0 nM 6.87
CHEMBL376206 IC50 = 194.0 nM 6.71
CHEMBL380035 IC50 = 207.0 nM 6.68
CHEMBL209656 IC50 = 402.0 nM 6.40
CHEMBL373985 IC50 = 728.0 nM 6.14
CHEMBL213635 IC50 = 734.0 nM 6.13
CHEMBL213299 IC50 = 1294.0 nM 5.89
CHEMBL413773 IC50 = 1403.0 nM 5.85
CHEMBL215910 IC50 = 4164.0 nM 5.38
CHEMBL209733 IC50 - -
CHEMBL209897 IC50 > 15000.0 nM -
CHEMBL209576 IC50 > 15000.0 nM -
CHEMBL209582 IC50 > 15000.0 nM -
CHEMBL214361 IC50 > 15000.0 nM -
CHEMBL386578 IC50 > 15000.0 nM -
CHEMBL211799 IC50 > 15000.0 nM -
CHEMBL214093 IC50 > 15000.0 nM -
CHEMBL212973 IC50 > 15000.0 nM -
CHEMBL436792 IC50 > 15000.0 nM -