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Literature summary for 1.14.19.1 extracted from

  • Koltun, D.O.; Zilbershtein, T.M.; Migulin, V.A.; Vasilevich, N.I.; Parkhill, E.Q.; Glushkov, A.I.; McGregor, M.J.; Brunn, S.A.; Chu, N.; Hao, J.; Mollova, N.; Leung, K.; Chisholm, J.W.; Zablocki, J.
    Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 4070-4074.
    View publication on PubMed
Search for more literature for 1.14.19.1

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Homo sapiens
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Rattus norvegicus
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Homo sapiens
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Rattus norvegicus
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
-
 Homo sapiens
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
-
 Rattus norvegicus
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Homo sapiens
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Rattus norvegicus
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Homo sapiens
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
 Rattus norvegicus
CVT-11,563
-
 Homo sapiens
CVT-11,563
-
 Rattus norvegicus
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Homo sapiens
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Rattus norvegicus
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Homo sapiens
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Rattus norvegicus
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Homo sapiens
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
 Rattus norvegicus
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
 Homo sapiens
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
 Rattus norvegicus
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
-
 Homo sapiens
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
-
 Rattus norvegicus
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
 Homo sapiens
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
 Rattus norvegicus
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
 Homo sapiens
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
 Rattus norvegicus

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-
Hep-G2 cell
-
 Homo sapiens
-
liver
-
 Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
DELTA9 desaturase
-
 Homo sapiens
DELTA9 desaturase
-
 Rattus norvegicus
SCD
-
 Homo sapiens
SCD
-
 Rattus norvegicus
stearoyl-CoA desaturase
-
 Homo sapiens
stearoyl-CoA desaturase
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000005
-
-
 Homo sapiens N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
0.0000005
-
-
 Homo sapiens N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
0.0000006
-
-
 Rattus norvegicus N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
0.0000014
-
-
 Rattus norvegicus N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
0.0000019
-
-
 Rattus norvegicus 2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.0000027
-
-
 Homo sapiens 2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.0000061
-
-
 Homo sapiens 2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.0000086
-
-
 Homo sapiens N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
0.000012
-
-
 Rattus norvegicus N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
0.000015
-
-
 Rattus norvegicus 2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.000033
-
-
 Homo sapiens N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.000038
-
-
 Rattus norvegicus (2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
0.000068
-
-
 Homo sapiens 2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
0.00008
-
-
 Rattus norvegicus N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
0.000093
-
-
 Rattus norvegicus N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.00011
-
-
 Rattus norvegicus N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
0.00011
-
-
 Homo sapiens N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000119
-
-
 Homo sapiens CVT-11,563
0.000162
-
-
 Rattus norvegicus 2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.00019
-
-
 Rattus norvegicus N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000261
-
-
 Rattus norvegicus CVT-11,563
0.000261
-
-
 Rattus norvegicus N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.000268
-
-
 Rattus norvegicus 1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
0.001
-
 IC50 above 0.001 mM Homo sapiens 1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
0.0011
-
-
 Rattus norvegicus 2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
0.0028
-
-
 Rattus norvegicus N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
0.0039
-
-
 Rattus norvegicus 3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
0.008
-
-
 Rattus norvegicus (2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide