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Literature summary extracted from

  • Uto, Y.; Ogata, T.; Kiyotsuka, Y.; Miyazawa, Y.; Ueno, Y.; Kurata, H.; Deguchi, T.; Yamada, M.; Watanabe, N.; Takagi, T.; Wakimoto, S.; Okuyama, R.; Konishi, M.; Kurikawa, N.; Kono, K.; Osumi, J.
    Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part II: Identification of 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide and its biological evaluation (2009), Bioorg. Med. Chem. Lett., 19, 4159-4166.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
1.14.19.1 expressed in HEK-293A cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.19.1 3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide potent and orally efficacious SCD-1 inhibitor Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide potent and orally efficacious SCD-1 inhibitor Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
-
 Homo sapiens
1.14.19.1 3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
-
 Mus musculus
1.14.19.1 4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Homo sapiens
1.14.19.1 4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
 Mus musculus
1.14.19.1 N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
 Homo sapiens
1.14.19.1 N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
 Mus musculus
1.14.19.1 N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
-
 Homo sapiens
1.14.19.1 N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
-
 Mus musculus
1.14.19.1 N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
 Homo sapiens
1.14.19.1 N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
 Mus musculus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.19.1 microsome
-
 Mus musculus
-
-
1.14.19.1 microsome
-
 Homo sapiens
-
-

Organism

EC Number Organism UniProt Comment Textmining
1.14.19.1 Homo sapiens
-
-
-
1.14.19.1 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.19.1 liver
-
 Mus musculus
-
1.14.19.1 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.19.1 stearoyl-CoA + NADH + H+ + O2
-
 Homo sapiens oleoyl-CoA + NAD+ + H2O
-
 ?
1.14.19.1 stearoyl-CoA + NADH + O2
-
 Mus musculus oleoyl-CoA + NAD+ + H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.19.1 SCD-1
-
 Mus musculus
1.14.19.1 SCD-1
-
 Homo sapiens
1.14.19.1 stearoyl-CoA desaturase-1
-
 Mus musculus
1.14.19.1 stearoyl-CoA desaturase-1
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.19.1 0.00000004
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.00000004
-
 in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
1.14.19.1 0.0000003
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
1.14.19.1 0.0000004
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.0000004
-
 in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
1.14.19.1 0.0000006
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
1.14.19.1 0.0000006
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000002
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000002
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000002
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000003
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000003
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000004
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000004
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000006
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000007
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000008
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
1.14.19.1 0.000008
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.00001
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
1.14.19.1 0.000011
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000012
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000015
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000016
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000022
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000032
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
1.14.19.1 0.000044
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
1.14.19.1 0.000049
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
1.14.19.1 0.000076
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
1.14.19.1 0.000145
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
1.14.19.1 0.000276
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
1.14.19.1 0.00032
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
1.14.19.1 0.000828
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000836
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.000884
-
 in 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
1.14.19.1 0.001
-
 IC50 above 0.001 mM, in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.001
-
 IC50 above 0.001 mM, in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
1.14.19.1 0.001
-
 IC50 above 0.001 mM, n 100 mM sodium phosphate, pH 7.4, at 37°C Homo sapiens 3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.009999
-
 IC50 above 0.009999 mM Homo sapiens 4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
1.14.19.1 0.009999
-
 IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37°C Mus musculus 3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide