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Assay Detail

CHEMBL1839595

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Binding
Inhibition of human FAS assessed as synthesis of long chain fatty acids from malonyl CoA after 60 mins by fluorescence assay
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 Autocuration

Target

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

Publication

Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.
Kley JT, Mack J, Hamilton B, Scheuerer S, Redemann N.
Bioorg Med Chem Lett (2011) 21 : 5924 -5927
PubMed 21873051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.23 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1834184 BI 99179 1 7.10
CHEMBL1834182 1 6.72
CHEMBL1834192 1 6.70
CHEMBL1834194 1 6.57
CHEMBL1834197 1 6.55
CHEMBL1834185 1 6.54
CHEMBL1834179 1 6.52
CHEMBL1834183 1 6.51
CHEMBL1834188 1 6.40
CHEMBL1834193 1 6.38
CHEMBL1834045 1 6.38
CHEMBL1834044 1 6.32
CHEMBL1834196 1 6.28
CHEMBL1834198 1 6.24
CHEMBL1834189 1 6.16
CHEMBL1834195 1 6.04
CHEMBL1834186 1 5.89
CHEMBL1834190 1 5.85
CHEMBL1834187 1 5.82
CHEMBL1834178 1 5.82
CHEMBL1834180 1 5.70
CHEMBL1834191 1 5.62
CHEMBL45627 CERULENIN 1 5.24
CHEMBL1834181 1 -
CHEMBL1834199 BI 99990 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1834184 BI 99179 IC50 = 79.0 nM 7.10
CHEMBL1834182 IC50 = 190.0 nM 6.72
CHEMBL1834192 IC50 = 200.0 nM 6.70
CHEMBL1834194 IC50 = 270.0 nM 6.57
CHEMBL1834197 IC50 = 280.0 nM 6.55
CHEMBL1834185 IC50 = 290.0 nM 6.54
CHEMBL1834179 IC50 = 300.0 nM 6.52
CHEMBL1834183 IC50 = 310.0 nM 6.51
CHEMBL1834188 IC50 = 400.0 nM 6.40
CHEMBL1834193 IC50 = 420.0 nM 6.38
CHEMBL1834045 IC50 = 420.0 nM 6.38
CHEMBL1834044 IC50 = 480.0 nM 6.32
CHEMBL1834196 IC50 = 530.0 nM 6.28
CHEMBL1834198 IC50 = 580.0 nM 6.24
CHEMBL1834189 IC50 = 700.0 nM 6.16
CHEMBL1834195 IC50 = 910.0 nM 6.04
CHEMBL1834186 IC50 = 1300.0 nM 5.89
CHEMBL1834190 IC50 = 1400.0 nM 5.85
CHEMBL1834187 IC50 = 1500.0 nM 5.82
CHEMBL1834178 IC50 = 1500.0 nM 5.82
CHEMBL1834180 IC50 = 2000.0 nM 5.70
CHEMBL1834191 IC50 = 2400.0 nM 5.62
CHEMBL45627 CERULENIN IC50 = 5800.0 nM 5.24
CHEMBL1834181 IC50 > 10000.0 nM -
CHEMBL1834199 BI 99990 IC50 > 3000.0 nM -