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Literature summary extracted from

  • Liu, G.; Lynch, J.K.; Freeman, J.; Liu, B.; Xin, Z.; Zhao, H.; Serby, M.D.; Kym, P.R.; Suhar, T.S.; Smith, H.T.; Cao, N.; Yang, R.; Janis, R.S.; Krauser, J.A.; Cepa, S.P.; Beno, D.W.; Sham, H.L.; Collins, C.A.; Surowy, T.K.; Camp, H.S.
    Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors (2007), J. Med. Chem., 50, 3086-3100.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
 Homo sapiens
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
 Mus musculus
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
-
 Homo sapiens
1.14.19.1 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
-
 Mus musculus
1.14.19.1 3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
-
 Homo sapiens
1.14.19.1 3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
-
 Mus musculus
1.14.19.1 3-(4-phenoxypiperidin-1-yl)-6-(5-propyl-1,2,4-oxadiazol-3-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
-
 Homo sapiens
1.14.19.1 3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
-
 Mus musculus
1.14.19.1 3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
 Homo sapiens
1.14.19.1 3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
 Mus musculus
1.14.19.1 3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-tetrazol-5-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
-
 Mus musculus
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
-
 Homo sapiens
1.14.19.1 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
-
 Mus musculus

Localization

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

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.14.19.1 Mg2+
-
 Mus musculus
1.14.19.1 Mg2+
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+ Mus musculus
-
 oleoyl-CoA + ferricytochrome b5 + H2O
-
 ?
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+ Homo sapiens
-
 oleoyl-CoA + ferricytochrome b5 + H2O
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.14.19.1 Homo sapiens
-
-
-
1.14.19.1 Mus musculus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.14.19.1 liver
-
 Mus musculus
-
1.14.19.1 liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+
-
 Mus musculus oleoyl-CoA + ferricytochrome b5 + H2O
-
 ?
1.14.19.1 stearoyl-CoA + ferrocytochrome b5 + O2 + H+
-
 Homo sapiens oleoyl-CoA + ferricytochrome b5 + H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.14.19.1 SCD1
-
 Mus musculus
1.14.19.1 SCD1
-
 Homo sapiens
1.14.19.1 stearoyl-CoA desaturase 1
-
 Mus musculus
1.14.19.1 stearoyl-CoA desaturase 1
-
 Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.14.19.1 7.5
-
 assay at Mus musculus
1.14.19.1 7.5
-
 assay at Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.14.19.1 ferrocytochrome b5
-
 Mus musculus
1.14.19.1 ferrocytochrome b5
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.14.19.1 0.000004
-
 below, pH 7.5 Mus musculus 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
1.14.19.1 0.000004
-
 below, pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
1.14.19.1 0.000004
-
 pH 7.5 Mus musculus 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
1.14.19.1 0.0000045
-
 pH 7.5 Mus musculus 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
1.14.19.1 0.0000053
-
 pH 7.5 Mus musculus 3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
1.14.19.1 0.0000074
-
 pH 7.5 Mus musculus 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.00001
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
1.14.19.1 0.00001
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
1.14.19.1 0.00001
-
 pH 7.5 Mus musculus 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.000012
-
 pH 7.5 Mus musculus 3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.000014
-
 pH 7.5 Homo sapiens 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
1.14.19.1 0.000017
-
 pH 7.5 Homo sapiens 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
1.14.19.1 0.00002
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
1.14.19.1 0.00002
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
1.14.19.1 0.000026
-
 pH 7.5 Homo sapiens 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
1.14.19.1 0.000026
-
 pH 7.5 Mus musculus 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.000028
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
1.14.19.1 0.000032
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
1.14.19.1 0.000035
-
 pH 7.5 Homo sapiens 3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.00004
-
 pH 7.5 Mus musculus 3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.000041
-
 pH 7.5 Homo sapiens 3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.00007
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
1.14.19.1 0.000076
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
1.14.19.1 0.000076
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
1.14.19.1 0.000085
-
 pH 7.5 Mus musculus 3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
1.14.19.1 0.000088
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
1.14.19.1 0.000091
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
1.14.19.1 0.000092
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
1.14.19.1 0.00014
-
 pH 7.5 Homo sapiens 3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
1.14.19.1 0.000201
-
 pH 7.5 Homo sapiens 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.000208
-
 pH 7.5 Homo sapiens 3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
1.14.19.1 0.000209
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
1.14.19.1 0.00022
-
 pH 7.5 Mus musculus 3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.00037
-
 pH 7.5 Mus musculus 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-tetrazol-5-yl)pyridazine
1.14.19.1 0.000397
-
 pH 7.5 Homo sapiens 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
1.14.19.1 0.000712
-
 pH 7.5 Homo sapiens 3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
1.14.19.1 0.00082
-
 pH 7.5 Mus musculus 3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
1.14.19.1 0.00133
-
 pH 7.5 Mus musculus 3-(4-phenoxypiperidin-1-yl)-6-(5-propyl-1,2,4-oxadiazol-3-yl)pyridazine
1.14.19.1 0.00171
-
 pH 7.5 Homo sapiens 3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
1.14.19.1 0.00486
-
 pH 7.5 Homo sapiens 3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.00581
-
 pH 7.5 Homo sapiens 3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
1.14.19.1 0.00705
-
 pH 7.5 Homo sapiens 3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine