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Assay Detail

CHEMBL1060803

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

Binding
Inhibition of human SCD1 expressed in HEK293A cells assessed as conversion of [14C]stearate to [14C]oleate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-A
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 13 7.41 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557445 1 8.10
CHEMBL561588 1 8.05
CHEMBL552126 1 7.89
CHEMBL550800 1 7.89
CHEMBL552270 1 7.77
CHEMBL552173 1 7.58
CHEMBL559108 1 7.47
CHEMBL557652 1 7.47
CHEMBL562268 1 7.23
CHEMBL552269 1 6.94
CHEMBL556495 1 6.37
CHEMBL561530 1 6.19
CHEMBL564689 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557445 IC50 = 8.0 nM 8.10
CHEMBL561588 IC50 = 9.0 nM 8.05
CHEMBL552126 IC50 = 13.0 nM 7.89
CHEMBL550800 IC50 = 13.0 nM 7.89
CHEMBL552270 IC50 = 17.0 nM 7.77
CHEMBL552173 IC50 = 26.0 nM 7.58
CHEMBL559108 IC50 = 34.0 nM 7.47
CHEMBL557652 IC50 = 34.0 nM 7.47
CHEMBL562268 IC50 = 59.0 nM 7.23
CHEMBL552269 IC50 = 116.0 nM 6.94
CHEMBL556495 IC50 = 429.0 nM 6.37
CHEMBL561530 IC50 = 639.0 nM 6.19
CHEMBL564689 IC50 - -