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Literature summary for 6.4.1.2 extracted from

  • Chonan, T.; Oi, T.; Yamamoto, D.; Yashiro, M.; Wakasugi, D.; Tanaka, H.; Ohoka-Sugita, A.; Io, F.; Koretsune, H.; Hiratate, A.
    (4-Piperidinyl)-piperazine: a new platform for acetyl-CoA carboxylase inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6645-6648.
    View publication on PubMed

Application

Application Comment Organism
drug development inhibition of ACC demonstrates promising therapeutic potential for treating obesity and type 2 diabetes mellitus in transgenic mice and preclinical animal models Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1-benzoylpiperidin-4-yl)(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
-
Homo sapiens
(2,5-dimethylfuran-3-yl)(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
-
Homo sapiens
(2,6-diphenylpyridin-4-yl)(4-(1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl)piperazin-1-yl)methanone
-
Homo sapiens
(2,6-diphenylpyridin-4-yl)(4-[1-((1-[(methylsulfonyl)carbonyl]piperidin-4-yl)carbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
(2,6-diphenylpyridin-4-yl)(4-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
(2,6-diphenylpyridin-4-yl)(4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
1-(4-([4-(4-([2,6-bis(3-fluorophenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-([4-(4-([2,6-bis(4-fluorophenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-([4-(4-([2,6-bis(4-hydroxyphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-([4-(4-([2,6-bis(4-methoxyphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-([4-(4-([2,6-bis(4-methylphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)-2-hydroxyethanone
-
Homo sapiens
1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)-2-methoxyethanone
-
Homo sapiens
1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)ethanone
-
Homo sapiens
1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)propan-1-one
-
Homo sapiens
1-[4-((4-[4-((2,6-bis[4-(hydroxymethyl)phenyl]pyridin-4-yl)carbonyl)piperazin-1-yl]piperidin-1-yl)carbonyl)piperidin-1-yl]ethanone
-
Homo sapiens
3,3'-(4-[(4-(1-[(1-acetylpiperidin-4-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)carbonyl]pyridine-2,6-diyl)dibenzamide
-
Homo sapiens
4,4'-(4-[(4-(1-[(1-acetylpiperidin-4-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)carbonyl]pyridine-2,6-diyl)dibenzamide
-
Homo sapiens
4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]-N,N-dimethylpiperidine-1-carboxamide
-
Homo sapiens
4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]-N-methylpiperidine-1-carboxamide
-
Homo sapiens
4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxamide
-
Homo sapiens
anthracen-9-yl(4-(1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl(4-[1-(cyclohexylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl(4-[1-(cyclopentylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl(4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl(4-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl(4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
-
Homo sapiens
anthracen-9-yl[(3R)-3-(morpholin-4-ylcarbonyl)-1,4'-bipiperidin-1'-yl]methanone i.e. CP-640186 Homo sapiens
anthracen-9-yl[4-(1-benzoylpiperidin-4-yl)piperazin-1-yl]methanone
-
Homo sapiens
cyclohexyl(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
-
Homo sapiens
methyl 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxylate
-
Homo sapiens
additional information disubstituted (4-piperidinyl)-piperazine derivatives act as ACC1/2 non-selective inhibitors Homo sapiens
propan-2-yl 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxylate
-
Homo sapiens
[4-(1-benzoylpiperidin-4-yl)piperazin-1-yl](2,6-diphenylpyridin-4-yl)methanone
-
Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + acetyl-CoA + HCO3- Homo sapiens
-
ADP + phosphate + malonyl-CoA
-
ir

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
Hep-G2 cell
-
Homo sapiens
-
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + acetyl-CoA + HCO3-
-
Homo sapiens ADP + phosphate + malonyl-CoA
-
ir

Synonyms

Synonyms Comment Organism
ACC1
-
Homo sapiens
ACC2
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000032
-
ACC1/2 Homo sapiens 1-[4-((4-[4-((2,6-bis[4-(hydroxymethyl)phenyl]pyridin-4-yl)carbonyl)piperazin-1-yl]piperidin-1-yl)carbonyl)piperidin-1-yl]ethanone
0.000052
-
ACC1/2 Homo sapiens 1-(4-([4-(4-([2,6-bis(4-hydroxyphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
0.00006
-
ACC1/2 Homo sapiens anthracen-9-yl(4-(1-[(2,5-dimethylfuran-3-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)methanone
0.000066
-
ACC1/2 Homo sapiens anthracen-9-yl[4-(1-benzoylpiperidin-4-yl)piperazin-1-yl]methanone
0.000067
-
ACC1/2 Homo sapiens 4,4'-(4-[(4-(1-[(1-acetylpiperidin-4-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)carbonyl]pyridine-2,6-diyl)dibenzamide
0.000068
-
ACC1/2 Homo sapiens 1-(4-([4-(4-([2,6-bis(4-methoxyphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
0.000073
-
ACC1/2 Homo sapiens 3,3'-(4-[(4-(1-[(1-acetylpiperidin-4-yl)carbonyl]piperidin-4-yl)piperazin-1-yl)carbonyl]pyridine-2,6-diyl)dibenzamide
0.000076
-
ACC1/2 Homo sapiens 1-(4-([4-(4-([2,6-bis(4-methylphenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
0.000091
-
ACC1/2 Homo sapiens anthracen-9-yl(4-[1-(cyclohexylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000095
-
ACC1/2 Homo sapiens anthracen-9-yl(4-[1-(cyclopentylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000095
-
ACC1/2 Homo sapiens 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]-N-methylpiperidine-1-carboxamide
0.000102
-
ACC1/2 Homo sapiens 1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)-2-hydroxyethanone
0.000102
-
ACC1/2 Homo sapiens methyl 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxylate
0.000115
-
ACC1/2 Homo sapiens 1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)propan-1-one
0.000121
-
ACC1/2 Homo sapiens anthracen-9-yl(4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000126
-
ACC1/2 Homo sapiens 1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)ethanone
0.000131
-
ACC1/2 Homo sapiens 1-(4-([4-(4-([2,6-bis(3-fluorophenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
0.000151
-
ACC1/2 Homo sapiens 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxamide
0.000155
-
ACC1/2 Homo sapiens (2,6-diphenylpyridin-4-yl)(4-(1-[(4-methoxycyclohexyl)carbonyl]piperidin-4-yl)piperazin-1-yl)methanone
0.000157
-
ACC1/2 Homo sapiens (2,5-dimethylfuran-3-yl)(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
0.000161
-
ACC1/2 Homo sapiens anthracen-9-yl(4-[1-(furan-2-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000169
-
ACC1/2 Homo sapiens 1-(4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidin-1-yl)-2-methoxyethanone
0.000169
-
ACC1/2 Homo sapiens 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]-N,N-dimethylpiperidine-1-carboxamide
0.000184
-
ACC1/2 Homo sapiens 1-(4-([4-(4-([2,6-bis(4-fluorophenyl)pyridin-4-yl]carbonyl)piperazin-1-yl)piperidin-1-yl]carbonyl)piperidin-1-yl)ethanone
0.000239
-
ACC1/2 Homo sapiens anthracen-9-yl(4-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000244
-
ACC1/2 Homo sapiens cyclohexyl(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
0.000248
-
ACC1/2 Homo sapiens (2,6-diphenylpyridin-4-yl)(4-[1-((1-[(methylsulfonyl)carbonyl]piperidin-4-yl)carbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.00029
-
ACC1/2 Homo sapiens (1-benzoylpiperidin-4-yl)(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)methanone
0.000411
-
ACC1/2 Homo sapiens propan-2-yl 4-[(4-(4-[(2,6-diphenylpyridin-4-yl)carbonyl]piperazin-1-yl)piperidin-1-yl)carbonyl]piperidine-1-carboxylate
0.000434
-
ACC1/2 Homo sapiens (2,6-diphenylpyridin-4-yl)(4-[1-(piperidin-1-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.000693
-
ACC1/2 Homo sapiens [4-(1-benzoylpiperidin-4-yl)piperazin-1-yl](2,6-diphenylpyridin-4-yl)methanone
0.000869
-
ACC1/2 Homo sapiens (2,6-diphenylpyridin-4-yl)(4-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]piperazin-1-yl)methanone
0.002112
-
ACC1/2 Homo sapiens anthracen-9-yl[4-(1-benzoylpiperidin-4-yl)piperazin-1-yl]methanone

General Information

General Information Comment Organism
metabolism acetyl-CoA carboxylase is the rate limiting enzyme in de novo lipid synthesis Homo sapiens
physiological function acetyl-CoA carboxylase plays important roles in modulating energy metabolism Homo sapiens