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Literature summary for 1.14.19.1 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
Search for more literature for 1.14.19.1

Inhibitors

Inhibitors Comment Organism Structure
4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 Rattus norvegicus
4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 Rattus norvegicus
4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
 Rattus norvegicus
4-(1H-indol-3-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide 15% inhibition at 0.001 mM Rattus norvegicus
4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 Rattus norvegicus
4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
 Rattus norvegicus
4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 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
-
 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
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 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
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
 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
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
 Rattus norvegicus
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
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
 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
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
 Rattus norvegicus
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
 Rattus norvegicus
N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
 Rattus norvegicus
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
N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
 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
-
 Rattus norvegicus
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

Localization Comment Organism GeneOntology No. Textmining
microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
SCD1
-
 Rattus norvegicus
stearoyl-CoA desaturase-1
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
0.17
-
 pH and temperature not specified in the publication Rattus norvegicus 4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
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
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
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
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
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