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Assay Detail

CHEMBL1044832

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Binding
Inhibition of stearoyl-CoA delta9 desaturase in human HepG2 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Stearoyl-CoA desaturase (CHEMBL5555)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Koltun DO, Zilbershtein TM, Migulin VA, Vasilevich NI, Parkhill EQ, Glushkov AI, McGregor MJ, Brunn SA, Chu N, Hao J, Mollova N, Leung K, Chisholm JW, Zablocki J.
Bioorg Med Chem Lett (2009) 19 : 4070 -4074
PubMed 19577469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.11 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494748 1 10.30
CHEMBL572876 1 9.30
CHEMBL575817 1 8.57
CHEMBL573829 1 8.21
CHEMBL493960 1 8.07
CHEMBL493961 1 7.48
CHEMBL577141 1 7.17
CHEMBL466674 1 6.96
CHEMBL444433 1 6.92
CHEMBL576780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494748 IC50 = 0.05 nM 10.30
CHEMBL572876 IC50 = 0.5 nM 9.30
CHEMBL575817 IC50 = 2.7 nM 8.57
CHEMBL573829 IC50 = 6.1 nM 8.21
CHEMBL493960 IC50 = 8.6 nM 8.07
CHEMBL493961 IC50 = 33.0 nM 7.48
CHEMBL577141 IC50 = 68.0 nM 7.17
CHEMBL466674 IC50 = 110.0 nM 6.96
CHEMBL444433 IC50 = 119.0 nM 6.92
CHEMBL576780 IC50 > 1000.0 nM -