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Literature summary extracted from

  • Yang, S.M.; Tang, Y.; Zhang, R.; Lu, H.; Kuo, G.H.; Gaul, M.D.; Li, Y.; Ho, G.; Conway, J.G.; Liang, Y.; Lenhard, J.M.; Demarest, K.T.; Murray, W.V.
    4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs (2013), Bioorg. Med. Chem. Lett., 23, 6773-6776.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.19.1 4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(1H-indol-3-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide 15% inhibition at 0.001 mM Rattus norvegicus
1.14.19.1 4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide 20% inhibition at 0.001 mM Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 N-(5-acetyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide 46% inhibition at 0.001 mM Rattus norvegicus
1.14.19.1 N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
Rattus norvegicus
1.14.19.1 N-[3-(methylcarbamoyl)phenyl]-4-(2-oxo-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide 7% inhibition at 0.001 mM Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.14.19.1 microsome
-
Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+ Rattus norvegicus
-
oleoyl-CoA + ferricytochrome b5 + H2O
-
?

Organism

EC Number Organism UniProt Comment Textmining
1.14.19.1 Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+
-
Rattus norvegicus oleoyl-CoA + ferricytochrome b5 + H2O
-
?

Synonyms

EC Number Synonyms Comment Organism
1.14.19.1 SCD1
-
Rattus norvegicus
1.14.19.1 stearoyl-CoA desaturase-1
-
Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.19.1 0.008
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
1.14.19.1 0.014
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.018
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
1.14.19.1 0.02
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
1.14.19.1 0.02 2 pH and temperature not specified in the publication Rattus norvegicus N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
1.14.19.1 0.026
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.029
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
1.14.19.1 0.052
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
1.14.19.1 0.082
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.088
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
1.14.19.1 0.093
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
1.14.19.1 0.096
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
1.14.19.1 0.14
-
pH and temperature not specified in the publication Rattus norvegicus 4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.151
-
pH and temperature not specified in the publication Rattus norvegicus 4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
1.14.19.1 0.153
-
pH and temperature not specified in the publication Rattus norvegicus 4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.17
-
pH and temperature not specified in the publication Rattus norvegicus 4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
1.14.19.1 0.204
-
pH and temperature not specified in the publication Rattus norvegicus N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
1.14.19.1 0.347
-
pH and temperature not specified in the publication Rattus norvegicus 4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.491
-
pH and temperature not specified in the publication Rattus norvegicus 4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.538
-
pH and temperature not specified in the publication Rattus norvegicus 4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
1.14.19.1 0.682
-
pH and temperature not specified in the publication Rattus norvegicus N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide