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Literature summary for 1.14.19.1 extracted from

  • Uto, Y.; Ogata, T.; Kiyotsuka, Y.; Ueno, Y.; Miyazawa, Y.; Kurata, H.; Deguchi, T.; Watanabe, N.; Konishi, M.; Okuyama, R.; Kurikawa, N.; Takagi, T.; Wakimoto, S.; Ohsumi, J.
    Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats (2010), Bioorg. Med. Chem. Lett., 20, 341-345.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide MF-152 Homo sapiens
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide MF-152 Mus musculus
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide CVT-12,012 Homo sapiens
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide CVT-12,012 Mus musculus
3-(2-hydroxyethoxy)-4-methoxy-N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}benzamide
-
Homo sapiens
3-(2-hydroxyethoxy)-4-methoxy-N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}benzamide
-
Mus musculus
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
Homo sapiens
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
Mus musculus
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
Homo sapiens
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
Mus musculus
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
Homo sapiens
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
-
Homo sapiens
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
-
Mus musculus
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
-
Homo sapiens
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
-
Mus musculus
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Homo sapiens
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Mus musculus
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
-
Homo sapiens
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
-
Mus musculus
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Homo sapiens
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Mus musculus
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Homo sapiens
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
Mus musculus
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Homo sapiens
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
Mus musculus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide CVT-11,563 Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide CVT-11,563 Mus musculus

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293A cell
-
Homo sapiens
-
liver
-
Mus musculus
-

Substrates and Products (Substrate)

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

Synonyms

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

Cofactor

Cofactor Comment Organism Structure
NADH
-
Mus musculus
NADH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
-
Mus musculus N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
0.000003
-
-
Mus musculus N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000005
-
-
Mus musculus N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
0.000005
-
-
Mus musculus N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000005
-
-
Homo sapiens N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000006
-
-
Mus musculus N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000006
-
-
Homo sapiens N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000007
-
-
Homo sapiens N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
0.000007
-
-
Mus musculus N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000007
-
-
Mus musculus N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000007
-
-
Homo sapiens N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000007
-
-
Mus musculus N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000009
-
-
Homo sapiens N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000009
-
-
Mus musculus N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.00001
-
-
Homo sapiens N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
0.000015
-
-
Homo sapiens N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000022
-
-
Homo sapiens N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000025
-
-
Mus musculus N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000025
-
-
Homo sapiens N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000028
-
-
Homo sapiens N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000034
-
-
Mus musculus N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000037
-
-
Mus musculus N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000044
-
-
Homo sapiens N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000052
-
-
Mus musculus N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000066
-
-
Mus musculus N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000074
-
-
Mus musculus 6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
0.000081
-
-
Homo sapiens N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
0.000095
-
-
Mus musculus N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000099
-
-
Homo sapiens N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
0.000118
-
-
Homo sapiens 6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
0.00015
-
-
Mus musculus N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
0.000153
-
-
Mus musculus N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
0.00018
-
-
Homo sapiens N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000187
-
-
Homo sapiens N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.000194
-
-
Mus musculus N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
0.00025
-
-
Homo sapiens N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
0.000292
-
-
Homo sapiens N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
0.000311
-
-
Homo sapiens N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
0.00037
-
-
Mus musculus N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
0.00082
-
-
Homo sapiens N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide