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Literature summary for 1.14.19.1 extracted from

  • Ramtohul, Y.K.; Powell, D.; Leclerc, J.P.; Leger, S.; Oballa, R.; Black, C.; Isabel, E.; Li, C.S.; Crane, S.; Robichaud, J.; Guay, J.; Guiral, S.; Zhang, L.; Huang, Z.
    Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors (2011), Bioorg. Med. Chem. Lett., 21, 5692-5696.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
-
Homo sapiens
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
-
Rattus norvegicus
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
-
Homo sapiens
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
-
Rattus norvegicus
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
-
Homo sapiens
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
Homo sapiens
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
-
Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
-
Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
-
Rattus norvegicus
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
-
Homo sapiens
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
-
Rattus norvegicus
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Homo sapiens
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Rattus norvegicus
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Homo sapiens
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
Rattus norvegicus
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
-
Homo sapiens
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
-
Rattus norvegicus
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
-
Homo sapiens
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
-
Rattus norvegicus
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
-
Homo sapiens
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
-
Rattus norvegicus
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
-
Homo sapiens
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
-
Rattus norvegicus
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
Homo sapiens
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
Rattus norvegicus
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
-
Homo sapiens
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
-
Rattus norvegicus
MF-152
-
Homo sapiens
MF-152
-
Rattus norvegicus
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
-
Homo sapiens
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
-
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
0.000001
-
pH and temperature not specified in the publication Homo sapiens [3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
0.000001
-
pH and temperature not specified in the publication Rattus norvegicus [3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
0.000001
-
pH and temperature not specified in the publication Rattus norvegicus 5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
0.000001
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication Rattus norvegicus 6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
0.000002
-
pH and temperature not specified in the publication Rattus norvegicus 5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.000003
-
pH and temperature not specified in the publication Rattus norvegicus 5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
0.000004
-
pH and temperature not specified in the publication Rattus norvegicus ([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
0.000007
-
pH and temperature not specified in the publication Rattus norvegicus ([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
0.000007
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.000008
-
pH and temperature not specified in the publication Rattus norvegicus 5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.00001
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
0.00001
-
pH and temperature not specified in the publication Rattus norvegicus 6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
0.000016
-
pH and temperature not specified in the publication Homo sapiens 5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.000017
-
pH and temperature not specified in the publication Homo sapiens 5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
0.000029
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.000038
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
0.000039
-
pH and temperature not specified in the publication Rattus norvegicus 8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
0.000039
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication Homo sapiens 6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
0.000047
-
pH and temperature not specified in the publication Homo sapiens 5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
0.000048
-
pH and temperature not specified in the publication Homo sapiens 6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
0.000053
-
pH and temperature not specified in the publication Homo sapiens ([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
0.000054
-
pH and temperature not specified in the publication Rattus norvegicus 5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
0.000056
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
0.000059
-
pH and temperature not specified in the publication Homo sapiens 5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
0.000083
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
0.000085
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
0.000097
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
0.000106
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000162
-
pH and temperature not specified in the publication Homo sapiens 8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
0.000168
-
pH and temperature not specified in the publication Homo sapiens ([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
0.000182
-
pH and temperature not specified in the publication Homo sapiens 5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
0.000253
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000257
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
0.000266
-
pH and temperature not specified in the publication Rattus norvegicus 3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
0.000268
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
0.000319
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
0.000378
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
0.000477
-
pH and temperature not specified in the publication Rattus norvegicus 2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
0.000755
-
pH and temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
0.01064
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
0.02434
-
pH and temperature not specified in the publication Homo sapiens 3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid