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Literature summary for 1.14.19.1 extracted from

  • Ramtohul, Y.K.; Black, C.; Chan, C.C.; Crane, S.; Guay, J.; Guiral, S.; Huang, Z.; Oballa, R.; Xu, L.J.; Zhang, L.; Li, C.S.
    SAR and optimization of thiazole analogs as potent stearoyl-CoA desaturase inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 1593-1597.
    View publication on PubMed
Search for more literature for 1.14.19.1

Inhibitors

Inhibitors Comment Organism Structure
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
-
 Homo sapiens
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
-
 Rattus norvegicus
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
-
 Rattus norvegicus
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Homo sapiens
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Rattus norvegicus
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Homo sapiens
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Rattus norvegicus
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Homo sapiens
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Rattus norvegicus
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Homo sapiens
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Rattus norvegicus
1-[5-(5-methyl-1,3,4-thiadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
 Rattus norvegicus
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
-
 Homo sapiens
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
-
 Rattus norvegicus
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
-
 Homo sapiens
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
-
 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)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
 Homo sapiens
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
 Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
-
 Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
-
 Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
-
 Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
-
 Rattus norvegicus
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
-
 Homo sapiens
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
-
 Rattus norvegicus
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
-
 Rattus norvegicus
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
-
 Homo sapiens
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
-
 Rattus norvegicus
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
-
 Homo sapiens
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
-
 Rattus norvegicus
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
-
 Homo sapiens
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
-
 Rattus norvegicus
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
-
 Homo sapiens
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
-
 Rattus norvegicus
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
-
 Homo sapiens
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
-
 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

Localization

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

Organism

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000001
-
 HepG2 whole cell assay, pH not specified in the publication, 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
-
 rat liver microsomal enzyme assay, pH not specified in the publication, 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
0.000003
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
0.000003
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
0.000004
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
0.000004
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000007
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
0.000008
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
0.00001
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
0.000012
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
0.000014
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
0.000014
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000015
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000016
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000024
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
0.000034
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000039
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000041
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
0.000055
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000065
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000076
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000083
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
0.000084
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
0.000106
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000127
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
0.00015
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
0.000153
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000164
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
0.000174
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
0.000199
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
0.000254
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000676
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
0.00075
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
0.00075
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 1-[5-(5-methyl-1,3,4-thiadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
0.000775
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
0.001019
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
0.001634
-
 rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication Rattus norvegicus 3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
0.002823
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
0.006523
-
 HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide