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Assay Detail

CHEMBL1105109

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

Binding
Inhibition of SCD1 in Wistar rat liver microsome assessed as [3H]stearoyl-CoA to [3H]oleoyl-CoA conversion pretreated 1 hr before [3H]stearoyl-CoA addition measured after 60 mins by HPLC based scintillation assay
23
Total Activities
23
Compounds Tested
1
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

Acyl-CoA desaturase 1 (CHEMBL5424)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors.
Ramtohul YK, Black C, Chan CC, Crane S, Guay J, Guiral S, Huang Z, Oballa R, Xu LJ, Zhang L, Li CS.
Bioorg Med Chem Lett (2010) 20 : 1593 -1597
PubMed 20137926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.39 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1087015 1 9.00
CHEMBL1080909 1 8.52
CHEMBL1081257 1 8.52
CHEMBL1076688 1 8.40
CHEMBL1087772 1 8.40
CHEMBL1081111 1 8.10
CHEMBL1081255 1 7.92
CHEMBL1081996 1 7.85
CHEMBL1087014 1 7.82
CHEMBL1081997 1 7.47
CHEMBL1081112 1 7.39
CHEMBL1080559 1 7.12
CHEMBL1081258 1 7.08
CHEMBL576820 1 6.97
CHEMBL1080941 1 6.90
CHEMBL1081825 1 6.82
CHEMBL1081113 1 6.79
CHEMBL1076698 1 6.17
CHEMBL1081826 1 6.12
CHEMBL1081827 1 6.12
CHEMBL1080940 1 5.79
CHEMBL1081256 1 -
CHEMBL1080558 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1087015 IC50 = 1.0 nM 9.00
CHEMBL1080909 IC50 = 3.0 nM 8.52
CHEMBL1081257 IC50 = 3.0 nM 8.52
CHEMBL1076688 IC50 = 4.0 nM 8.40
CHEMBL1087772 IC50 = 4.0 nM 8.40
CHEMBL1081111 IC50 = 8.0 nM 8.10
CHEMBL1081255 IC50 = 12.0 nM 7.92
CHEMBL1081996 IC50 = 14.0 nM 7.85
CHEMBL1087014 IC50 = 15.0 nM 7.82
CHEMBL1081997 IC50 = 34.0 nM 7.47
CHEMBL1081112 IC50 = 41.0 nM 7.39
CHEMBL1080559 IC50 = 76.0 nM 7.12
CHEMBL1081258 IC50 = 83.0 nM 7.08
CHEMBL576820 IC50 = 106.0 nM 6.97
CHEMBL1080941 IC50 = 127.0 nM 6.90
CHEMBL1081825 IC50 = 150.0 nM 6.82
CHEMBL1081113 IC50 = 164.0 nM 6.79
CHEMBL1076698 IC50 = 676.0 nM 6.17
CHEMBL1081826 IC50 = 750.0 nM 6.12
CHEMBL1081827 IC50 = 750.0 nM 6.12
CHEMBL1080940 IC50 = 1634.0 nM 5.79
CHEMBL1081256 IC50 > 20000.0 nM -
CHEMBL1080558 IC50 > 3000.0 nM -