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Literature summary for 1.14.19.1 extracted from

  • Koltun, D.O.; Vasilevich, N.I.; Parkhill, E.Q.; Glushkov, A.I.; Zilbershtein, T.M.; Mayboroda, E.I.; Boze, M.A.; Cole, A.G.; Henderson, I.; Zautke, N.A.; Brunn, S.A.; Chu, N.; Hao, J.; Mollova, N.; Leung, K.; Chisholm, J.W.; Zablocki, J.
    Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 3050-3053.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
Homo sapiens
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
Rattus norvegicus
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
Homo sapiens
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
Rattus norvegicus
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
Homo sapiens
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
Rattus norvegicus
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
Homo sapiens
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
Rattus norvegicus
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Homo sapiens
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Rattus norvegicus
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Homo sapiens
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Rattus norvegicus
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Homo sapiens
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Rattus norvegicus
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Homo sapiens
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Rattus norvegicus
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Homo sapiens
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
Rattus norvegicus
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
-
Homo sapiens
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
-
Rattus norvegicus
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
Homo sapiens
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
Rattus norvegicus
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
Rattus norvegicus
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
Homo sapiens
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
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
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
-
Homo sapiens
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
-
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
Hep-G2 cell
-
Homo sapiens
-
liver
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
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
0.00019
-
-
Homo sapiens N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.00019
-
-
Rattus norvegicus N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000208
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
0.000208
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
0.00025
-
-
Homo sapiens benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.00025
-
-
Rattus norvegicus benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.000251
-
-
Homo sapiens benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.000251
-
-
Rattus norvegicus benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.00026
-
-
Homo sapiens benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.00026
-
-
Rattus norvegicus benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.000261
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000261
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000268
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
0.000268
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
0.000348
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.000348
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.000865
-
-
Homo sapiens benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.000865
-
-
Rattus norvegicus benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.00089
-
-
Homo sapiens [[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
0.00089
-
-
Rattus norvegicus [[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
0.00117
-
-
Homo sapiens N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.00117
-
-
Rattus norvegicus N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.00136
-
-
Homo sapiens 2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
0.00136
-
-
Rattus norvegicus 2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
0.00258
-
-
Homo sapiens N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
0.00258
-
-
Rattus norvegicus N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
0.00269
-
-
Homo sapiens N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.00269
-
-
Rattus norvegicus N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.00312
-
-
Homo sapiens N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.00312
-
-
Rattus norvegicus N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
0.0032
-
-
Homo sapiens benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
0.0032
-
-
Rattus norvegicus benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
0.00342
-
-
Homo sapiens 2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
0.00342
-
-
Rattus norvegicus 2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
0.00385
-
-
Homo sapiens N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.00385
-
-
Rattus norvegicus N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.00386
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
0.00386
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
0.00797
-
-
Homo sapiens N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
0.00797
-
-
Rattus norvegicus N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
0.0116
-
-
Homo sapiens N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
0.0116
-
-
Rattus norvegicus N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
0.03
-
IC50 above 0.03 mM Homo sapiens benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.03
-
IC50 above 0.03 mM Rattus norvegicus benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
0.03
-
IC50 above 0.03 mM Homo sapiens (2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
0.03
-
IC50 above 0.03 mM Rattus norvegicus (2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
0.03
-
IC50 above 0.03 mM Homo sapiens (2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
0.03
-
IC50 above 0.03 mM Rattus norvegicus (2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide