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Assay Detail

CHEMBL2212889

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Binding
Inhibition of DGAT in rat liver microsomes
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Diacylglycerol O-acyltransferase 1 (CHEMBL6129)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of a novel series of benzimidazole derivatives as diacylglycerol acyltransferase inhibitors.
Lee K, Goo JI, Jung HY, Kim M, Boovanahalli SK, Park HR, Kim MO, Kim DH, Lee HS, Choi Y.
Bioorg Med Chem Lett (2012) 22 : 7456 -7460
PubMed 23141914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 4.93 5.51
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473967 1 5.51
CHEMBL2207805 1 5.36
CHEMBL2207808 1 5.06
CHEMBL2207794 1 5.05
CHEMBL2207809 1 5.02
CHEMBL243796 KURARINONE 1 4.96
CHEMBL2207799 1 4.95
CHEMBL2207807 1 4.94
CHEMBL2207804 1 4.70
CHEMBL2207798 1 4.70
CHEMBL2205735 1 4.64
CHEMBL2207806 1 4.59
CHEMBL2207800 1 4.56
CHEMBL253896 XANTHOHUMOL 2.0 1 -
CHEMBL2207810 1 -
CHEMBL2207803 1 -
CHEMBL2207802 1 -
CHEMBL2207801 1 -
CHEMBL2207811 1 -
CHEMBL2207812 1 -
CHEMBL2207797 1 -
CHEMBL2207796 1 -
CHEMBL2207795 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473967 IC50 = 3100.0 nM 5.51
CHEMBL2207805 IC50 = 4400.0 nM 5.36
CHEMBL2207808 IC50 = 8700.0 nM 5.06
CHEMBL2207794 IC50 = 9000.0 nM 5.05
CHEMBL2207809 IC50 = 9500.0 nM 5.02
CHEMBL243796 KURARINONE IC50 = 10900.0 nM 4.96
CHEMBL2207799 IC50 = 11300.0 nM 4.95
CHEMBL2207807 IC50 = 11400.0 nM 4.94
CHEMBL2207804 IC50 = 20000.0 nM 4.70
CHEMBL2207798 IC50 = 20000.0 nM 4.70
CHEMBL2205735 IC50 = 23000.0 nM 4.64
CHEMBL2207806 IC50 = 25400.0 nM 4.59
CHEMBL2207800 IC50 = 27500.0 nM 4.56
CHEMBL253896 XANTHOHUMOL Inhibition - % -
CHEMBL2207810 IC50 > 50000.0 nM -
CHEMBL2207803 IC50 > 50000.0 nM -
CHEMBL2207802 IC50 > 50000.0 nM -
CHEMBL2207801 IC50 > 50000.0 nM -
CHEMBL2207811 IC50 > 50000.0 nM -
CHEMBL2207812 IC50 > 50000.0 nM -
CHEMBL2207797 IC50 > 50000.0 nM -
CHEMBL2207796 IC50 > 50000.0 nM -
CHEMBL2207795 IC50 > 50000.0 nM -