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Assay Detail

CHEMBL1060792

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

Binding
Inhibition of SCD1 in human microsomes assessed as conversion of [14C]stearate to [14C]oleate after 60 mins
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.
Uto Y, Ogata T, Harada J, Kiyotsuka Y, Ueno Y, Miyazawa Y, Kurata H, Deguchi T, Watanabe N, Takagi T, Wakimoto S, Okuyama R, Abe M, Kurikawa N, Kawamura S, Yamato M, Osumi J.
Bioorg Med Chem Lett (2009) 19 : 4151 -4158
PubMed 19540759 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.71 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552173 1 9.70
CHEMBL557445 1 9.22
CHEMBL550800 1 9.00
CHEMBL552126 1 9.00
CHEMBL552270 1 8.70
CHEMBL552269 1 8.54
CHEMBL560271 1 8.52
CHEMBL550172 1 8.52
CHEMBL562268 1 8.40
CHEMBL561588 1 8.40
CHEMBL564822 1 8.05
CHEMBL557652 1 8.05
CHEMBL561073 1 8.00
CHEMBL559108 1 7.96
CHEMBL561530 1 7.09
CHEMBL556495 1 6.90
CHEMBL562988 1 6.84
CHEMBL562737 1 6.04
CHEMBL559739 1 5.91
CHEMBL564721 1 5.85
CHEMBL562592 1 5.67
CHEMBL558451 1 5.36
CHEMBL559107 1 -
CHEMBL560193 1 -
CHEMBL564689 1 -
CHEMBL564046 1 -
CHEMBL550726 1 -
CHEMBL562531 1 -
CHEMBL558808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552173 IC50 = 0.2 nM 9.70
CHEMBL557445 IC50 = 0.6 nM 9.22
CHEMBL550800 IC50 = 1.0 nM 9.00
CHEMBL552126 IC50 = 1.0 nM 9.00
CHEMBL552270 IC50 = 2.0 nM 8.70
CHEMBL552269 IC50 = 2.9 nM 8.54
CHEMBL560271 IC50 = 3.0 nM 8.52
CHEMBL550172 IC50 = 3.0 nM 8.52
CHEMBL562268 IC50 = 4.0 nM 8.40
CHEMBL561588 IC50 = 4.0 nM 8.40
CHEMBL564822 IC50 = 9.0 nM 8.05
CHEMBL557652 IC50 = 9.0 nM 8.05
CHEMBL561073 IC50 = 10.0 nM 8.00
CHEMBL559108 IC50 = 11.0 nM 7.96
CHEMBL561530 IC50 = 82.0 nM 7.09
CHEMBL556495 IC50 = 125.0 nM 6.90
CHEMBL562988 IC50 = 145.0 nM 6.84
CHEMBL562737 IC50 = 915.0 nM 6.04
CHEMBL559739 IC50 = 1218.0 nM 5.91
CHEMBL564721 IC50 = 1402.0 nM 5.85
CHEMBL562592 IC50 = 2162.0 nM 5.67
CHEMBL558451 IC50 = 4377.0 nM 5.36
CHEMBL559107 IC50 - -
CHEMBL560193 IC50 > 9999.0 nM -
CHEMBL564689 IC50 - -
CHEMBL564046 IC50 > 9999.0 nM -
CHEMBL550726 IC50 - -
CHEMBL562531 IC50 - -
CHEMBL558808 IC50 - -