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Information on EC 1.14.19.1 - stearoyl-CoA 9-desaturase and Organism(s) Homo sapiens and UniProt Accession O00767

for references in articles please use BRENDA:EC1.14.19.1

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IUBMB Comments

An iron protein. The rat liver enzyme is an enzyme system involving cytochrome b5 and EC 1.6.2.2, cytochrome-b5 reductase. The ferricytochrome b5 produced is reduced by NADH and cytochrome-b5 reductase (EC 1.6.2.2).

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms

Synonyms
scd, stearoyl-coa desaturase, fatty acid desaturase, scd-1, stearoyl-coa desaturase 1, stearoyl-coa desaturase-1, stearoyl coa desaturase, stearoyl-coenzyme a desaturase, delta9-desaturase, delta9 desaturase, more

SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
DELTA-9 fatty acyl desaturase
-
stearoyl-CoA desaturase
-
stearoyl-CoA desaturase 1
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stearoyl-CoA desaturase-1
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ACOD4
-
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acyl coenzyme A desaturase
-
-
-
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acyl-CoA desaturase
-
-
-
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DELTA-9 fatty acyl desaturase
DELTA9 desaturase
-
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DELTA9 stearoyl-coenzyme A desaturase
-
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DELTA9-acyl CoA desaturase
-
-
-
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DELTA9-desaturase
-
-
-
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desaturase 9
-
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eicosatrienoyl-CoA desaturase
-
-
-
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fatty acid 9-desaturase
-
-
-
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fatty acid DELTA9-desaturase
-
-
-
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fatty acid desaturase
fatty acyl CoA DELTA9-desaturase
-
-
-
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fatty acyl DELTA9-desaturase
-
-
-
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fatty acyl-CoA desaturase
-
-
-
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hSCD1
-
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long-chain fatty acid DELTA9-desaturase
-
-
-
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palmitoyl CoA desaturase
-
-
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palmitoyl-CoA desaturase
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-
-
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stearoyl coenzyme A desaturase
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-
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stearoyl coenzyme-A desaturase 1
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stearoyl-CoA (DELTA8) desaturase
-
-
-
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stearoyl-CoA desaturase
stearoyl-CoA desaturase 1
-
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stearoyl-CoA desaturase 5
stearoyl-CoA desaturase enzyme-1
-
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stearoyl-CoA desaturase-1
-
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stearoyl-CoA desaturase-5
stearyl coenzyme A desaturase
-
-
-
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stearyl-CoA desaturase
-
-
-
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REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
the DELTA9-desaturase SCD-1 introduces a cis-double bond into saturated fatty acids between carbons 9 and 10. Preferred substrates of SCD-1 are long-chain acyl-CoAs with 13 to 19 carbons, among them stearoyl-CoA and palmitoyl-CoA, the most abundant saturated fatty acid-CoA ester in mammalians. Dehydrogenation of the pro-R hydrogens at C9 and C10 requires molecular oxygen which is activated at the di-iron center and reduced to water. Two of the electrons transferred to molecular oxygen derive from the acyl-CoA substrate and two others from the di-iron center. The ferrous catalytic center is regenerated by electron transfer from cytochrome b5, which has been suggested to bind to a groove at the cytoplasmic domain and to transmit electrons via two histidine residues (H157 and H298) bridging the distance. Ferrocytochrome b5 is provided by cytochrome b5 reductase using NAD(P)H as co-substrate
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
it is suggested that in HepG2 cells the trans-10,cis-12 conjugated linoleic acid isomer regulates human desaturase activity mainly by a posttranslational mechanism
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
redox reaction
-
-
-
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oxidation
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-
-
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reduction
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-
-
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PATHWAY SOURCE
PATHWAYS
MetaCyc
oleate biosynthesis II (animals and fungi), palmitoleate biosynthesis IV (fungi and animals), sorgoleone biosynthesis
SYSTEMATIC NAME
IUBMB Comments
stearoyl-CoA,ferrocytochrome-b5:oxygen oxidoreductase (9,10-dehydrogenating)
An iron protein. The rat liver enzyme is an enzyme system involving cytochrome b5 and EC 1.6.2.2, cytochrome-b5 reductase. The ferricytochrome b5 produced is reduced by NADH and cytochrome-b5 reductase (EC 1.6.2.2).
CAS REGISTRY NUMBER
COMMENTARY hide
9014-34-0
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SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
Reversibility
r=reversible
ir=irreversible
?=not specified
palmitoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearic acid + AH2 + O2
oleic acid + A + H2O
show the reaction diagram
Substrates: -
Products: -
?
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
Substrates: -
Products: -
?
palmitoyl-CoA + ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + ferricytochrome b5 + 2 H2O
show the reaction diagram
palmitoyl-CoA + NADH + H+ + O2
palmitoleoyl-CoA + NAD+ + H2O
show the reaction diagram
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearoyl-CoA + AH2 + H+ + O2
oleoyl-CoA + A + H2O
show the reaction diagram
-
Substrates: -
Products: -
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
show the reaction diagram
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
show the reaction diagram
additional information
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
LITERATURE
COMMENTARY hide
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
palmitoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
Substrates: -
Products: -
?
palmitoyl-CoA + ferrocytochrome b5 + O2 + 2 H+
palmitoleoyl-CoA + ferricytochrome b5 + 2 H2O
show the reaction diagram
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Substrates: a key step in triglyceride synthesis in the fatty acid metabolic network
Products: -
?
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+
oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
show the reaction diagram
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
show the reaction diagram
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
cytochrome b5
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ferrocytochrome b5
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cytochrome b5
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ferrocytochrome b5
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METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(2-(1-(3,4,5-trichlorobenzyl)-1H-1,2,3-triazol-4-yl)imidazo[1,2-a]pyridin-7-yl)methanol
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(2-(4-[(2-benzyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
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(2-(4-[(2-butyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
-
(2-(4-[(2-chloro-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
-
(2-(4-[(2-hexyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
-
(2-(4-[(2-octyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
-
(2-[(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazol-5-yl)-acetic acid
-
(2-[(5-([2-(3-methyl-butyl)-phenylamino]-methyl)-thiophene-2-carbonyl)-amino]-thiazol-4-yl)-acetic acid
-
(2-[4-(biphenyl-2-ylaminomethyl)-benzoylamino]-thiazol-4-yl)-acetic acid
-
(2-[4-(o-tolylamino-methyl)-benzoylamino]-thiazol-4-yl)-acetic acid
-
(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-acetic acid
-
(3(2)R,3(5)S,5S)-5-(tert-butyl)-N-((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-4,7-dioxo-2,8-dioxa-6-aza-1(1,7)-isoquinolina-3(2,1)-pyrrolidinacyclotridecaphane-3(5)-carboxamide
-
(5-(6-(3-(2-(trifluoromethyl)phenoxy)azetidin-1-yl)pyridazin-3-yl)-1,3,4-oxadiazol-2-yl)methanol
-
(5-(6-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)pyridazin-3-yl)-1,3,4-oxadiazol-2-yl)methanol
-
(5-(6-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)pyridazin-3-yl)pyridin-3-yl)methanol
-
2-((4-((5-methylthiazol-2-yl)carbamoyl)benzyl)amino)benzoic acid
-
2-(1-((2,2-difluorocyclopropyl)methyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
2-(1-(1-(4-fluorophenyl)ethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
-
2-(1-(2-(4-fluorophenoxy)ethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
2-(1-(3,5-difluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((1-methyl-1H-imidazol-4-yl)methyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((1-methyl-1H-pyrazol-4-yl)methyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((2-methylthiazol-5-yl)methyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((3-methyl-1H-pyrazol-5-yl)methyl)-thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((5-methylpyrazin-2-yl)methyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((6-(trifluoromethyl)pyridin-3-yl)methyl)-thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(oxazol-2-ylmethyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(oxazol-4-ylmethyl)thiazole-5-carboxamide
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2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(piperidin-3-ylmethyl)thiazole-5-carboxamide trifluoroacetic acid salt
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
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2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(thiazol-2-ylmethyl)thiazole-5-carboxamide
-
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxamide
-
2-(1-(cyclopropylmethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
2-(2-(5-(((2-butylphenyl)amino)methyl)thiophene-2-carboxamido)thiazol-4-yl)acetate
the thiazole-4-acetic acid analogue is a potent and liver-selective SCD1 inhibitor. It exhibits significant effects in rodent models of diabetes, hepatic steatosis, and obesity, with sufficient safety margins in a rat toxicology study with repeated dosing
2-(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazole-5-carboxylic acid
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2-[4-(o-tolylamino-methyl)-benzoylamino]-thiazole-4-carboxylic acid
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3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-((1-methyl-1H-pyrazol-4-yl)methyl)-1H-pyrazole-5-carboxamide
-
3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(oxazol-4-ylmethyl)-1H-pyrazole-5-carboxamide
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3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-2-ylmethyl)-1H-pyrazole-5-carboxamide
-
3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)-1H-pyrazole-5-carboxamide
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3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-4-ylmethyl)-1H-pyrazole-5-carboxamide
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3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-methyl-1H-pyrazole-5-carboxamide
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3-(2-(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazol-5-yl)-propionic acid
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3-(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-propionic acid
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4-(((3-chlorophenyl)amino)methyl)eN-(5-methylthiazol-2-yl)benzamide
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4-(((4-chlorophenyl)amino)methyl)eN-(5-methylthiazol-2-yl)benzamide
-
4-((2-chlorophenoxy)methyl)eN-(pyridin-4-yl)benzamide
-
4-(2-chlorophenoxy)-N-[3-[(methylamino)carbonyl]phenyl]-1-piperidinecarboxamide
i.e. A939 or A939572, an SCD1 inhibitor, causes significantly delayed tumor growth, which is reversed by L-cycloserine, an inhibitor of ceramide biosynthesis. A939 can significantly inhibit LOVO cell proliferation, which can be dose-dependently reversed by oleic acid, but not by palmitic acid
4-(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-butyric acid
-
4-hydroxymethyl-2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazole-5-carboxylic acid
-
4-methyl-2-(5-oxo-1-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
4-methyl-2-(5-oxo-1-(4,4,4-trifluorobutyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
-
4-methyl-2-(5-oxo-1-(4-(trifluoromethyl)benzyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
-
4-methyl-2-(5-oxo-1-(4-(trifluoromethyl)benzyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
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4-oxo-N-(4-hydroxyphenyl)retinamide
-
4-[(2-butyl-phenylamino)-methyl]eN-(4-hydroxymethylthiazol-2-yl)-benzamide
-
4-[(2-butyl-phenylamino)-methyl]eN-[4-(2-hydroxyethyl)-thiazol-2-yl]-benzamide
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4-[(2-chloro-phenylamino)-methyl]eN-(4-hydroxymethylthiazol-2-yl)-benzamide
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4-[(2-chloro-phenylamino)-methyl]eN-(4-methyl-thiazol-2-yl)-benzamide
-
4-[(2-chloro-phenylamino)-methyl]eN-[4-(2-hydroxyethyl)-thiazol-2-yl]-benzamide
-
5-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)thiazolo[5,4-d]pyrimidin-2-amine
-
5-[(2-hexyl-phenylamino)-methyl]-thiophene-2-carboxylic acid [4-(2-hydroxy-ethyl)-thiazol-2-yl]-amide
-
5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carboxylic acid (4-hydroxymethyl-thiazol-2-yl)-amide
-
5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carboxylic acid [4-(2-hydroxy-ethyl)-thiazol-2-yl]-amide
-
A939572
Cay10566
fenretinide
i.e. N-(4-hydroxyphenyl)retinamide, a synthetic retinoid, leads to an increase in C16 and C18 dihydroceramide substrate accumulation. Fenretinide induces degradation of SCD1 in human Rretinal pigment epithelium cells
N,N-dimethyl-2-((4-((5-methylthiazol-2-yl)carbamoyl)benzyl)amino)benzamide
-
N-((1H-pyrazol-3-yl)methyl)-2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxamide
-
N-(2-(7-((4-chloro-3-(trifluoromethyl)benzyl)amino)-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl)ethyl)acetamide
-
N-(4-hydroxymethyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
-
N-(4-methyl-thiazol-2-yl)-4-(o-tolylamino-methyl)-benzamide
-
N-(4-methyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
-
N-(4-methylthiazol-2-yl)-4-(((2-(trifluoromethyl)phenyl)amino)methyl)piperidine-1-carboxamide
-
N-(4-methylthiazol-2-yl)-5-(((2-(trifluoromethyl)phenyl)amino)methyl)thiophene-2-carboxamide
-
N-(4-methylthiazol-2-yl)-5-((o-tolylamino)methyl)picolinamide
-
N-(4-methylthiazol-2-yl)-6-((o-tolylamino)methyl)nicotinamide
-
N-(5-hydroxymethyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
-
N-(5-methylthiazol-2-yl)-4-(((2-propylphenyl)amino)methyl)benzamide
-
N-(5-methylthiazol-2-yl)-4-((phenylamino)methyl)benzamide
-
N-[4-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
-
N-[4-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[[2-(3-methylbutyl)-phenylamino]-methyl]-benzamide
-
N-[4-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
-
N-[5-(2-hydroxy-ethyl)-4-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
-
N-[5-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
-
N-[5-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
-
[2-((5-[(2-benzyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetic acid
-
[2-((5-[(2-hexyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetate
-
[2-((5-[(2-octyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetate
-
[2-((5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetic acid
-
[2-(4-([2-(3-methyl-butyl)-phenylamino]-methyl)-benzoylamino)-thiazol-4-yl]-acetic acid
-
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
EC50 value is 62 nM. SCD-1 inhibition with the inhibitor increases susceptibility of hepatitis C virus RNA to exogenously added nucleases in digitonin permeabilized cells. Low dose treatment with the inhibitor decreases the number of membranous webs and alters their structure while having no effect on lipid droplets in Huh7-SGR cells
(1-[6-[3-(3-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]pyridazin-3-yl]piperidin-4-yl)[2-(trifluoromethyl)phenyl]methanone
-
-
(2-[[(5-[[(4-fluoro-2-heptylphenyl)amino]methyl]thiophen-2-yl)carbonyl]amino]-1,3-thiazol-4-yl)acetic acid
-
-
(2E)-3-(4-methoxyphenyl)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]prop-2-enamide
-
-
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
-
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
-
-
(3-[5-[(3S)-3-(2-bromo-5-fluorophenoxy)pyrrolidin-1-yl]-1,3,4-thiadiazol-2-yl]-1,2,4-oxadiazol-5-yl)methanol
-
-
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
-
-
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
-
-
(5R)-5-(hydroxymethyl)-3-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridin-3-yl)-1,3-oxazolidin-2-one
-
-
(E)-N-(2-cyclopropylethyl)-N2-(pyridin-2-yl[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]methylidene)glycinamide
-
-
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
-
-
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
-
-
1'-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]-2,3-dihydrospiro[indene-1,4'-piperidine]
-
-
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
-
-
1-hydroxy-3-[5-(6-[3-[2-(trifluoromethyl)benzyl]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]propan-2-one
-
-
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
-
-
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
-
-
1-[5-(benzylcarbamoyl)-4-methyl-1,3-thiazol-2-yl]-N-(4-fluorobenzyl)-1H-1,2,3-triazole-4-carboxamide
-
-
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
-
-
2-(2-cyclopropylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1H-isoindole-1,3(2H)-dione
-
-
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
MF-152
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
-
-
2-(4-[[5-(hexylamino)-2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-N-pentylpyridine-4-carboxamide
-
-
2-(5-[1-[(2,5-dichlorophenyl)carbonyl]piperidin-4-ylidene]-2,4-dioxo-1,3-thiazolidin-3-yl)-N-pentylacetamide
-
-
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
-
-
2-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylbenzamide
-
-
2-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylbenzamide
-
-
2-acetyl-N-[1-(3,4-dichlorobenzyl)-1H-pyrazol-4-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
-
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
-
-
2-methyl-5-(6-(4-(2-(trifluoromethyl)phenoxy) piperidin-1-yl)pyridazin-3-yl)-1,3,4-thiadiazole
-
MF-438, known enzyme inhibitor
-
2-[(2,5-dichlorophenoxy)methyl]-N-[4-(1H-pyrazol-1-ylmethyl)phenyl]pyridine-4-carboxamide
-
-
2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]benzamide
-
-
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[1-[2-(4-fluorophenyl)ethyl]-1H-1,2,3-triazol-4-yl]-4-methyl-N-(pyridin-3-ylmethyl)-1,3-thiazole-5-carboxamide
-
-
2-[3-(4-fluorobenzyl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-N-(pyridin-3-ylmethyl)-4-(trifluoromethyl)-1,3-thiazole-5-carboxamide
-
-
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
-
-
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
-
-
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
-
-
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-[6-(benzyloxy)pyridazin-3-yl]-5-(1-[2-(trifluoromethyl)phenyl]ethenyl)-1,2,3,4,5,6-hexahydropyrrolo[3,4-c]pyrrole
-
i.e. SAR707, known enzyme inhibitor
-
2-[[4-(2-chlorophenoxy)piperidine-1-carbonyl]amino]-N-methylpyridine-4-carboxamide
-
2-[[4-(2-chlorophenoxy)piperidine-1-carbonyl]amino]-N-methylpyridine-4-carboxamide attenuates tumor progression and demonstrates excellent bioavailability
3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3,4-dimethoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3,4-dimethyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2,2-dihydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2,3-dihydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxy-2-methylpropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxy-ethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-(5-[[3-(trifluoromethyl)phenyl]carbonyl]-1,3-thiazol-2-yl)benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
highly potent and orally bioavailable thiazole-based SCD-1 inhibitor
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethoxy)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}benzamide
-
-
3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-4-[(methylsulfonyl)amino]-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(3-hydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
-
-
3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
-
-
3-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-one
-
-
3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
-
-
3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
-
-
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
-
-
3-([2-[4-(2,3-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2,5-dichlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-bromophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(2-hydroxyethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-4-ylmethyl)pyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-ethylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylpyrazine-2-carboxamide
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbaldehyde
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbonitrile
-
-
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
3-chloro-N-[2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]pyrazin-2-amine
-
-
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
3-methoxy-4-(2-morpholin-4-ylethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(2-phenylethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-3-ylmethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-4-ylmethyl)pyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-pentylpyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-propylpyridine-2-carboxamide
-
-
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
3-[([4-[2-(acetylamino)ethyl]-2-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-6-yl]amino)methyl]benzoic acid
-
-
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
-
-
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]propanamide
-
-
3-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]propanamide
-
-
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
-
-
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
-
-
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
-
-
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
-
-
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-(4-methoxyphenyl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
3-[7-oxo-6-(4-pyridin-3-ylphenyl)-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
-
-
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
-
-
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
-
-
4-(2-bromo-5-fluorophenoxy)-1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3,4-thiadiazol-2-yl]piperidine
-
-
4-(2-bromophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-4-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-5-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-6-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chloro-phenoxy)-piperidine-1-carboxylic acid tert-butyl ester
-
i.e. Abbott 10b
-
4-(2-chlorophenoxy)-N-phenylpiperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(1H-imidazol-2-yl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(ethylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-chlorophenoxy)-N-[3-[(1-methylethyl)carbamoyl]phenyl]piperidine-1-carboxamide
-
-
4-(2-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-hydroxyethoxy)-3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(2-methoxyphenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(3-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-([6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazin-3-yl]ethynyl)phenol
-
-
4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
-
-
4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
4-methyl-2-[2-oxo-3-[4-(trifluoromethyl)benzyl]-2,3-dihydro-1H-imidazol-1-yl]-N-(pyridin-3-ylmethyl)-1,3-thiazole-5-carboxamide
-
-
4-[(7-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-5,6,7,7a-tetrahydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl)methoxy]benzoic acid
-
-
4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
-
-
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
-
-
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
-
-
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
-
-
6'-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-2,3'-bipyridine-5-carboxylic acid
-
-
6-(3,4-dihydro-1'H-spiro[chromene-2,4'-piperidin]-1'-yl)-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
-
6-(3-bromobenzyl)-5,7-dimethyl-N-(tetrahydrofuran-2-ylmethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
6-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)pyridine-3-carboxylic acid
-
-
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
-
-
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
-
-
6-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
-
-
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
-
-
6-tert-butyl-2-(2'-fluoro[1,1'-biphenyl]-4-yl)-1H-1,3-benzimidazole
-
-
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
-
-
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
-
-
6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine-3-carbohydrazide
-
-
6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine-3-carboxamide
-
-
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
-
-
6-[4-[(2-bromo-5-methoxyphenyl)carbonyl]piperazin-1-yl]-N-(3-phenylpropyl)pyridine-3-carboxamide
-
-
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
-
-
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-2-amine
-
-
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
-
-
6-[5-chloro-2-(trifluoromethyl)benzyl]-N-hexyl-5,6,7,8-tetrahydro-1,6-naphthyridine-2-carboxamide
-
-
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
-
-
8-(trifluoromethyl)-2,5,21,24,25-pentaazatetracyclo[21.2.2.2-2,5.1-7,11]triaconta-1(25),7(28),8,10,23,26-hexaene-6,22-dione
-
-
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
-
-
A939572
-
known enzyme inhibitor
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
-
-
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
-
-
CGX0168
-
-
-
CGX0290
-
-
-
cis-10,trans-12-conjugated linoleic acid
-
-
CP-24879
-
9% inhibition at 0.01 mM
CVT-11,563
-
-
CVT-11127
-
specific small molecule inhibitor
CVT-12-012
-
-
-
cyclosporin A
-
-
ethyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-oxadiazol-2-yl]acetate
-
-
GSK-993
-
potent and orally available SCD1 inhibitor, almost complete inhibition at 0.01 mM
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
-
-
methyl 3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxylate
-
-
methyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-thiadiazol-2-yl]acetate
-
-
MF-152
-
-
N,N-dimethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-(2-amino-2-oxoethyl)-6-(2,3-dichlorobenzyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-3-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1H-pyrazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3,4-thiadiazole-2-carboxamide
-
-
N-(2-cyclopropylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-(4-[[5-fluoro-2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-[(1-[[2-(trifluoromethyl)phenyl]carbonyl]azetidin-3-yl)amino]pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-6-[4-[3-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-(2-hydroxyethyl)-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
-
-
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
-
-
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
-
-
N-(2-[2-[(3,4-dichlorobenzyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)benzamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)methanesulfonamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)propanamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)thiophene-3-carboxamide
-
-
N-(2-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3-chloro-4-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(3-chlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[2-[(4-chloro-3-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(2-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
-
-
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(3-methoxybenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxopyrido[3,4-b]pyrazin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
-
-
N-(3-carbamoylphenyl)-4-(2-chlorophenoxy)piperidine-1-carboxamide
-
-
N-(3-methylbutyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(3-methylbutyl)-6-oxo-8-[[2-(trifluoromethyl)phenyl]carbonyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1',2':1,6]pyrazino[2,3-c]pyridazine-3-carboxamide
-
-
N-(3-methylbutyl)-6-[[2-(trifluoromethyl)phenyl]carbonyl]-4,5,6,7-tetrahydrofuro[2,3-c]pyridine-2-carboxamide
-
-
N-(cyclopentylmethyl)-6-[5-[[2-(trifluoromethyl)phenyl]carbonyl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl]pyridine-3-carboxamide
-
-
N-benzyl-2-(5-hydroxy-1-oxoisoquinolin-2(1H)-yl)-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-2-[3-(4-fluorobenzyl)-2-oxopyrrolidin-1-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-2-[3-(4-fluorophenoxy)-2-oxopiperidin-1-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyridine-2-carboxamide
-
-
N-benzyl-4-(morpholin-4-ylmethyl)-2-[(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide
-
-
N-benzyl-4-methyl-2-(1-[2-[methyl(phenyl)amino]ethyl]-1H-pyrazol-3-yl)-1,3-thiazole-5-carboxamide
-
-
N-benzyl-4-methyl-2-[6-(2-phenylethyl)pyrazin-2-yl]-1,3-thiazole-5-carboxamide
-
-
N-benzyl-6-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-ethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-methoxy-3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
N-methyl-2-(2-oxo-2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]ethoxy)benzamide
-
-
N-methyl-2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-3-carboxamide
-
-
N-methyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-phenoxypiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-3-[[2-oxo-2-(4-[[2-(trifluoromethyl)phenyl]amino]piperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
-
-
N-methyl-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-imidazo[4,5-c]pyridin-4-amine
-
-
N-tert-butyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
-
-
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-[(6-chloropyridin-3-yl)methyl]-2-[4-[(4-fluorobenzyl)oxy]-2-oxopyridin-1(2H)-yl]-4-methyl-1,3-thiazole-5-carboxamide
-
-
N-[1-[5-chloro-2-(cyclopropylmethoxy)benzyl]-5-methyl-1H-pyrazol-3-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
-
-
N-[2-(4-[[2-fluoro-5-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-2-oxoethyl]-5-(2-methoxyphenyl)-1H-pyrazole-3-carboxamide
-
-
N-[2-(4-[[2-fluoro-5-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-2-oxoethyl]biphenyl-4-carboxamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[6-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(2,2,2-trifluoroethoxy)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[4-(2,2,2-trifluoroethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-(4-methoxyphenyl)-6-[[(5-methylisoxazol-3-yl)methyl]amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
-
-
N-[2-[6-(benzylamino)-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[2-fluoro-5-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
-
-
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
-
-
N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
-
-
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
-
-
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
-
-
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[3-(methylcarbamoyl)phenyl]-4-(2-methylphenoxy)piperidine-1-carboxamide
-
-
N-[3-(methylcarbamoyl)phenyl]-4-phenoxypiperidine-1-carboxamide
-
-
N-[3-(tert-butylcarbamoyl)phenyl]-4-(2-chlorophenoxy)piperidine-1-carboxamide
-
-
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
N-[5-(2,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,4-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,4-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3,5-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-chloro-4-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-chlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-fluoro-4-methylbenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-(3-tert-butylbenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-methyl-1-[3-(trifluoromethyl)benzyl]-1H-pyrazol-3-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
-
N-[5-[(2-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-1,2,3,4-tetrahydroisoquinoline-6-carboxamide
-
complete inhibition at 0.1 mM
N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[5-[4-fluoro-3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
-
-
N-[[2-(benzyloxy)pyridin-4-yl]methyl]-4-[2-(trifluoromethyl)benzoyl]piperazine-1-carboxamide
-
-
N-{5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl}naphthalene-2-carboxamide
-
-
Rapamycin
-
-
Sterculic acid
trans-10,cis-12 conjugated linoleic acid
[(5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-5,7a-dihydro[1,3]thiazolo[4,5-d]pyrimidin-7-yl)oxy]acetic acid
-
-
[2-((5-[(2-benzyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetic acid
-
-
[2-([[4-([[2-(2-cyclopentylethyl)phenyl]amino]methyl)phenyl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
99% inhibition at 0.01 mM
[2-([[4-([[2-(trifluoromethyl)phenyl]amino]methyl)piperidin-1-yl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
complete inhibition at 0.01 mM
[2-methoxy-4-([5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]carbamoyl)phenoxy]acetic acid
-
-
[2-methoxy-5-([5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]carbamoyl)phenoxy]acetic acid
-
-
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
-
-
[3-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)-1H-1,2,4-triazol-1-yl]acetic acid
-
-
[5-(2-[3-[2-bromo-5-(trifluoromethyl)phenoxy]propoxy]-1,3-thiazol-5-yl)-2H-tetrazol-2-yl]acetic acid
-
-
[5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)-1H-tetrazol-1-yl]acetic acid
-
-
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
-
-
[5-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazin-3-yl)-1,3,4-thiadiazol-2-yl]acetic acid
-
-
[5-[2-([(2S)-3-[2-bromo-5-(trifluoromethoxy)phenoxy]-2-methylpropyl]oxy)-1,3-thiazol-5-yl]-2H-tetrazol-2-yl]acetic acid
-
-
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
additional information
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000055
(2-(4-[(2-benzyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000055
(2-(4-[(2-butyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000013
(2-(4-[(2-chloro-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000003
(2-(4-[(2-hexyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000045
(2-(4-[(2-octyl-phenylamino)-methyl]-benzoylamino)-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000058
(2-[(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazol-5-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000067
(2-[(5-([2-(3-methyl-butyl)-phenylamino]-methyl)-thiophene-2-carbonyl)-amino]-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000087
(2-[4-(biphenyl-2-ylaminomethyl)-benzoylamino]-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000014
(2-[4-(o-tolylamino-methyl)-benzoylamino]-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000051
(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0036
2-((4-((5-methylthiazol-2-yl)carbamoyl)benzyl)amino)benzoic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000306
2-(1-((2,2-difluorocyclopropyl)methyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000066
2-(1-(1-(4-fluorophenyl)ethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000009
2-(1-(2-(4-fluorophenoxy)ethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000125
2-(1-(3,5-difluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000504
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((1-methyl-1H-imidazol-4-yl)methyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000477
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((1-methyl-1H-pyrazol-4-yl)methyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000032
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((2-methylthiazol-5-yl)methyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00028
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((3-methyl-1H-pyrazol-5-yl)methyl)-thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000194
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-((5-methylpyrazin-2-yl)methyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000214
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(oxazol-2-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000039
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(oxazol-4-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000067
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000268
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000009
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(thiazol-2-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000945
2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00014
2-(1-(cyclopropylmethyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methyl-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000088
2-(2-(5-(((2-butylphenyl)amino)methyl)thiophene-2-carboxamido)thiazol-4-yl)acetate
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000081
2-(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazole-5-carboxylic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.01
2-[4-(o-tolylamino-methyl)-benzoylamino]-thiazole-4-carboxylic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00072
3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-2-ylmethyl)-1H-pyrazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000103
3-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)-1H-pyrazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.00057
3-(2-(4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino)-thiazol-5-yl)-propionic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000063
3-(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-propionic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000018
4-(((3-chlorophenyl)amino)methyl)eN-(5-methylthiazol-2-yl)benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00076
4-(((4-chlorophenyl)amino)methyl)eN-(5-methylthiazol-2-yl)benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00015 - 0.0014
4-((2-chlorophenoxy)methyl)eN-(pyridin-4-yl)benzamide
0.0027
4-(2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazol-4-yl)-butyric acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000022
4-hydroxymethyl-2-[4-[(2-trifluoromethyl-phenylamino)-methyl]-benzoylamino]-thiazole-5-carboxylic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000008
4-methyl-2-(5-oxo-1-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000398
4-methyl-2-(5-oxo-1-(4,4,4-trifluorobutyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000227
4-methyl-2-(5-oxo-1-(4-(trifluoromethyl)benzyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-2-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.000046
4-methyl-2-(5-oxo-1-(4-(trifluoromethyl)benzyl)-1H-1,2,4-triazol-4(5H)-yl)-N-(pyridin-3-ylmethyl)thiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000032
4-[(2-butyl-phenylamino)-methyl]eN-(4-hydroxymethylthiazol-2-yl)-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000003
4-[(2-butyl-phenylamino)-methyl]eN-[4-(2-hydroxyethyl)-thiazol-2-yl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000043
4-[(2-chloro-phenylamino)-methyl]eN-(4-hydroxymethylthiazol-2-yl)-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000092
4-[(2-chloro-phenylamino)-methyl]eN-(4-methyl-thiazol-2-yl)-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000064
4-[(2-chloro-phenylamino)-methyl]eN-[4-(2-hydroxyethyl)-thiazol-2-yl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000045
5-[(2-hexyl-phenylamino)-methyl]-thiophene-2-carboxylic acid [4-(2-hydroxy-ethyl)-thiazol-2-yl]-amide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000051
5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carboxylic acid (4-hydroxymethyl-thiazol-2-yl)-amide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000039
5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carboxylic acid [4-(2-hydroxy-ethyl)-thiazol-2-yl]-amide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0027
N,N-dimethyl-2-((4-((5-methylthiazol-2-yl)carbamoyl)benzyl)amino)benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000105
N-((1H-pyrazol-3-yl)methyl)-2-(1-(4-fluorobenzyl)-5-oxo-1H-1,2,4-triazol-4(5H)-yl)-4-methylthiazole-5-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000038
N-(4-hydroxymethyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000064
N-(4-methyl-thiazol-2-yl)-4-(o-tolylamino-methyl)-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000041
N-(4-methyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00003
N-(4-methylthiazol-2-yl)-4-(((2-(trifluoromethyl)phenyl)amino)methyl)piperidine-1-carboxamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000097
N-(4-methylthiazol-2-yl)-5-(((2-(trifluoromethyl)phenyl)amino)methyl)thiophene-2-carboxamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000046
N-(4-methylthiazol-2-yl)-5-((o-tolylamino)methyl)picolinamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00031
N-(4-methylthiazol-2-yl)-6-((o-tolylamino)methyl)nicotinamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000028
N-(5-hydroxymethyl-thiazol-2-yl)-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000089
N-(5-methylthiazol-2-yl)-4-(((2-propylphenyl)amino)methyl)benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000095
N-(5-methylthiazol-2-yl)-4-((phenylamino)methyl)benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000042
N-[4-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000053
N-[4-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[[2-(3-methylbutyl)-phenylamino]-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000052
N-[4-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000031
N-[5-(2-hydroxy-ethyl)-4-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000038
N-[5-(2-hydroxy-ethyl)-thiazol-2-yl]-4-[(2-trifluoromethylphenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.00026
N-[5-(3-hydroxy-propyl)-thiazol-2-yl]-4-[(2-trifluoromethyl-phenylamino)-methyl]-benzamide
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000075
[2-((5-[(2-benzyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetic acid
Homo sapiens
pH 7.4, 22°C,ex vivo
0.0000048
[2-((5-[(2-hexyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetate
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000017
[2-((5-[(2-octyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetate
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.000009
[2-((5-[(2-trifluoromethyl-phenylamino)-methyl]-thiophene-2-carbonyl)-amino)-thiazol-4-yl]-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0000048
[2-(4-([2-(3-methyl-butyl)-phenylamino]-methyl)-benzoylamino)-thiazol-4-yl]-acetic acid
Homo sapiens
pH 7.4, 22°C, recombinant enzyme
0.0001
(1-[6-[3-(3-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]pyridazin-3-yl]piperidin-4-yl)[2-(trifluoromethyl)phenyl]methanone
Homo sapiens
-
IC50 below 0.0001 mM
0.000003
(2E)-3-(4-methoxyphenyl)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]prop-2-enamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.03
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Homo sapiens
-
IC50 above 0.03 mM
0.03
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Homo sapiens
-
IC50 above 0.03 mM
0.0000056
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00005
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000168
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000053
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
Homo sapiens
-
pH and temperature not specified in the publication
0.000174
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.001
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
Homo sapiens
-
IC50 above 0.001 mM
0.000016
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000065
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000055
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000039
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000068
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Homo sapiens
-
-
0.000255
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000074
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000096
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000027
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000113
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000015
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00003
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000024
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000024
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00006
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00058
2-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylbenzamide
Homo sapiens
-
-
0.0000027
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0000061
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00136
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Homo sapiens
-
-
0.00342
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Homo sapiens
-
-
0.0002
2-[(2,5-dichlorophenoxy)methyl]-N-[4-(1H-pyrazol-1-ylmethyl)phenyl]pyridine-4-carboxamide
Homo sapiens
-
-
0.000037
2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]benzamide
Homo sapiens
-
-
0.000084
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.01064
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
Homo sapiens
-
pH and temperature not specified in the publication
0.001705
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000253 - 0.000254
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
0.000153
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.006523
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00001
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.001019
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000378
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000319
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
Homo sapiens
-
pH and temperature not specified in the publication
0.000257
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Homo sapiens
-
pH and temperature not specified in the publication
0.000755
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
pH and temperature not specified in the publication
0.000029
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000268
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000019
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000016
3,4-bis(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000145
3,4-dimethoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.002162
3-(2,2-dihydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.009999
3-(2,3-dihydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37°C
0.0000006
3-(2-hydroxyethoxy)-4-(2-methoxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000828
3-(2-hydroxyethoxy)-4-methoxy-N-methyl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000003
3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Homo sapiens
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37°C
0.000059
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethoxy)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000008
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3,4-thiadiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000003 - 0.000015
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
0.000145
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]thiophen-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.001
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)phenoxy]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.001 mM, n 100 mM sodium phosphate, pH 7.4, at 37°C
0.000012
3-(2-hydroxyethoxy)-4-morpholin-4-yl-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000884
3-(2-hydroxyethoxy)-N-(5-[hydroxy[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-2-yl)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.00486
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000201
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.000397
3-(3-benzyl-1,2,4-oxadiazol-5-yl)-6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.009999
3-(3-hydroxypropoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM, in 100 mM sodium phosphate, pH 7.4, at 37°C
0.00171
3-(3-methyl-1,2,4-oxadiazol-5-yl)-6-[4-[2-(phenoxymethyl)phenoxy]piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.00705
3-(4-phenoxypiperidin-1-yl)-6-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]pyridazine
Homo sapiens
-
pH 7.5
0.000035
3-(5-benzyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000041
3-(5-benzyl-1,3,4-oxadiazol-2-yl)-6-[4-(2-chlorophenoxy)piperidin-1-yl]pyridazine
Homo sapiens
-
pH 7.5
0.00581
3-(5-methyl-1,2,4-oxadiazol-3-yl)-6-(4-phenoxypiperidin-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000009
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000021
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00047
3-([2-[4-(2,3-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000038
3-([2-[4-(2,5-dichlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000058
3-([2-[4-(2-bromophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000035
3-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000051
3-([2-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.0001
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(2-hydroxyethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00011
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-2-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000099
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-3-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00011
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-(pyridin-4-ylmethyl)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000039
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-ethylpyrazine-2-carboxamide
Homo sapiens
-
-
0.000051
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylpyrazine-2-carboxamide
Homo sapiens
-
-
0.00055
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-phenylpyrazine-2-carboxamide
Homo sapiens
-
-
0.00021
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbaldehyde
Homo sapiens
-
-
0.00034
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carbonitrile
Homo sapiens
-
-
0.000094
3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00003
3-chloro-N-[2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]pyrazin-2-amine
Homo sapiens
-
-
0.001402
3-methoxy-4-(2-morpholin-4-ylethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000915
3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.00078
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(2-phenylethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.00043
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-3-ylmethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.00035
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-(pyridin-4-ylmethyl)pyridine-2-carboxamide
Homo sapiens
-
-
0.01
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-pentylpyridine-2-carboxamide
Homo sapiens
-
above
0.00039
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]-N-propylpyridine-2-carboxamide
Homo sapiens
-
-
0.00009
3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00012
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
Homo sapiens
-
-
0.0000028
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Homo sapiens
-
-
0.000177
3-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.000513
3-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.02434
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
-
pH and temperature not specified in the publication
0.00004
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000019
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000023
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000022
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00014
3-[4-(2-benzylphenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000014
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000017
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000026 - 0.000037
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
0.000208
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-4H-1,2,4-triazol-3-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000076
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(1H-pyrrol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000091
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(2-methyl-1H-imidazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000712
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3,5-dimethyl-1H-pyrazol-1-yl)pyridazine
Homo sapiens
-
pH 7.5
0.00007
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(3-methyl-1,2,4-oxadiazol-5-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000076
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,2,4-oxadiazol-3-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000209
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Homo sapiens
-
pH 7.5
0.000088
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-furan-3-ylpyridazine
Homo sapiens
-
pH 7.5
0.000028
3-[4-(2-chlorophenoxy)piperidin-1-yl]-6-pyridin-3-ylpyridazine
Homo sapiens
-
pH 7.5
0.000014
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00033
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.000134
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.000145
3-[6-(4-methoxyphenyl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.000016
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Homo sapiens
-
-
0.00189
3-[7-oxo-6-(4-pyridin-3-ylphenyl)-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Homo sapiens
-
-
0.000342
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.002326
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00003
4-(2-bromophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000058
4-(2-chloro-4-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000018
4-(2-chloro-5-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.0097
4-(2-chloro-6-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.0075
4-(2-chlorophenoxy)-N-phenylpiperidine-1-carboxamide
Homo sapiens
-
-
0.00036
4-(2-chlorophenoxy)-N-[3-(1H-imidazol-2-yl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00011
4-(2-chlorophenoxy)-N-[3-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00015
4-(2-chlorophenoxy)-N-[3-(ethylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000037
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.0071
4-(2-chlorophenoxy)-N-[3-[(1-methylethyl)carbamoyl]phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00068
4-(2-fluorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00001
4-(2-hydroxyethoxy)-3-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.0019
4-(2-methoxyphenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.00027
4-(3-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Homo sapiens
-
-
0.000011
4-(acetylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000004
4-(diethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000015
4-(dimethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.00000004
4-(ethylamino)-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000002
4-ethoxy-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.00000004
4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Homo sapiens
-
in 250 mM sucrose, 150 mM KCl, 40 mM NaF, 5 mM MgCl2, 100 mM sodium phosphate, pH 7.4, at 37°C
0.001218
4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.009999
4-[2-(dimethylamino)ethoxy]-3-(2-hydroxyethoxy)-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
Homo sapiens
-
IC50 above 0.009999 mM
0.000016
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000059
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Homo sapiens
-
pH and temperature not specified in the publication
0.000182
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
Homo sapiens
-
pH and temperature not specified in the publication
0.000047
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.000199
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000007
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.002823
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.001
6-(3,4-dihydro-1'H-spiro[chromene-2,4'-piperidin]-1'-yl)-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
Homo sapiens
-
IC50 below 0.001 mM
0.001308
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.00176
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.004246
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000231
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000009
6-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]naphthalene-2-carboxamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000731
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Homo sapiens
-
pH not specified in the publication, temperature not specified in the publication
0.000015
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Homo sapiens
-
-
0.000013
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Homo sapiens
-
-
0.000039
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
Homo sapiens
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication
0.000118
6-[4-[(4-fluorophenyl)carbonyl]piperidin-1-yl]-N-(2-hydroxy-2-phenylethyl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000048
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.000034
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.00004
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Homo sapiens
-
-
0.000162
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
Homo sapiens
-
pH and temperature not specified in the publication
0.03
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens
-
IC50 above 0.03 mM
0.000251
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens
-
-
0.00025
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens
-
-
0.000865
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens
-
-
0.00026
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Homo sapiens
-
-
0.0032
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
Homo sapiens
-
-
0.00172 - 0.00187
CGX0168
-
0.00058 - 0.00152
CGX0290
-
0.000119
CVT-11,563
Homo sapiens
-
-
0.00017
GSK-993
Homo sapiens
-
in 50 mM Tris-HCl, pH 7.4, at 25°C
0.000775
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.000039
methyl 3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxylate
Homo sapiens
-
-
0.01
N,N-dimethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
above
0.00001
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethoxy)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000007
N-(2-hydroxy-2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperidin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000292
N-(2-hydroxy-2-phenylethyl)-6-[4-(phenylcarbonyl)piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000311
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methoxyphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000015
N-(2-hydroxy-2-phenylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.00018
N-(2-hydroxy-2-pyridin-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000028
N-(2-hydroxy-2-pyridin-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000187
N-(2-hydroxy-2-pyridin-4-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000044
N-(2-hydroxy-2-thiophen-2-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000007
N-(2-hydroxy-2-thiophen-3-ylethyl)-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.00012
N-(2-hydroxyethyl)-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00082
N-(2-phenylethyl)-4-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)benzamide
Homo sapiens
-
-
0.00025
N-(2-phenylethyl)-5-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-2-carboxamide
Homo sapiens
-
-
0.000009
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000099
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridine-3-carboxamide
Homo sapiens
-
-
0.00028
N-(2-[2-[(3,4-dichlorobenzyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00021
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00056
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)benzamide
Homo sapiens
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)methanesulfonamide
Homo sapiens
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)propanamide
Homo sapiens
-
-
0.00047
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)thiophene-3-carboxamide
Homo sapiens
-
-
0.00027
N-(2-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00075
N-(2-[2-[(3-chloro-4-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0013
N-(2-[2-[(3-chlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0009
N-(2-[2-[(4-chloro-3-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.000081
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000005
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Homo sapiens
-
-
0.000047
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0001
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00011
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000001
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxopyrido[3,4-b]pyrazin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000086
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.00013
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.0000031
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Homo sapiens
-
-
0.000059
N-(3-carbamoylphenyl)-4-(2-chlorophenoxy)piperidine-1-carboxamide
Homo sapiens
-
-
0.00014
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.00056
N-benzyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyridine-2-carboxamide
Homo sapiens
-
-
0.0073
N-benzyl-6-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.00011
N-ethyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.001
N-methyl-2-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-3-carboxamide
Homo sapiens
-
above
0.000097
N-methyl-3-[(2-oxo-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]ethyl)amino]pyridine-2-carboxamide
Homo sapiens
-
-
0.0063
N-methyl-3-[[2-oxo-2-(4-phenoxypiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
-
0.001
N-methyl-3-[[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
above
0.0001
N-methyl-3-[[2-oxo-2-(4-[[2-(trifluoromethyl)phenyl]amino]piperidin-1-yl)ethyl]amino]pyrazine-2-carboxamide
Homo sapiens
-
-
0.00026
N-tert-butyl-3-([2-[4-(2-chlorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)pyrazine-2-carboxamide
Homo sapiens
-
-
0.000025
N-[(2R)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000081
N-[(2S)-2-hydroxy-2-phenylethyl]-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Homo sapiens
-
-
0.000022
N-[2-(2-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000006
N-[2-(3-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.000005
N-[2-(4-fluorophenyl)-2-hydroxyethyl]-6-[4-[(2-methylphenyl)carbonyl]piperidin-1-yl]pyridazine-3-carboxamide
Homo sapiens
-
-
0.00018
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00021
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(2,2,2-trifluoroethoxy)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000047
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0025
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[4-(2,2,2-trifluoroethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000096
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000013
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00032
N-[2-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-5-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.0000032
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0000065
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.0000033 - 0.000033
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
0.000013
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00012
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000051
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.000016
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Homo sapiens
-
-
0.00000005 - 0.00005
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
0.000032
N-[3-(2-hydroxyethoxy)-4-methoxyphenyl]-5-[3-(trifluoromethyl)benzyl]-1,3-thiazole-2-carboxamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000208
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.000261
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.000268
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
Homo sapiens
-
-
0.0116
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
Homo sapiens
-
-
0.00386
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
Homo sapiens
-
-
0.000348
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00269
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00258
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00117
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00797
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
Homo sapiens
-
-
0.00312
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00385
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Homo sapiens
-
-
0.00012
N-[3-(methylcarbamoyl)phenyl]-4-(2-methylphenoxy)piperidine-1-carboxamide
Homo sapiens
-
-
0.004
N-[3-(methylcarbamoyl)phenyl]-4-phenoxypiperidine-1-carboxamide
Homo sapiens
-
-
0.01
N-[3-(tert-butylcarbamoyl)phenyl]-4-(2-chlorophenoxy)piperidine-1-carboxamide
Homo sapiens
-
above
0.00011 - 0.00019
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
0.000429
N-[5-(2,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000013
N-[5-(3,4-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000034
N-[5-(3,4-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000013
N-[5-(3,5-dichlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000116
N-[5-(3,5-difluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000017
N-[5-(3-chloro-4-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000009
N-[5-(3-chlorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000639
N-[5-(3-fluoro-4-methylbenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000034
N-[5-(3-fluorobenzyl)-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.0000003 - 0.000026
N-[5-[3,5-bis(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
0.000008
N-[5-[4-fluoro-3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]-3-(2-hydroxyethoxy)-4-methoxybenzamide
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.004377
[2-methoxy-4-([5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]carbamoyl)phenoxy]acetic acid
Homo sapiens
-
in 100 mM sodium phosphate, pH 7.4, at 37°C
0.000001
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
0.000026
[5-(2-[3-[2-bromo-5-(trifluoromethyl)phenoxy]propoxy]-1,3-thiazol-5-yl)-2H-tetrazol-2-yl]acetic acid
Homo sapiens
-
-
0.000013
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
Homo sapiens
-
HepG2 whole cell assay, pH not specified in the publication, temperature not specified in the publication
0.00009
[5-[2-([(2S)-3-[2-bromo-5-(trifluoromethoxy)phenoxy]-2-methylpropyl]oxy)-1,3-thiazol-5-yl]-2H-tetrazol-2-yl]acetic acid
Homo sapiens
-
-
0.00089
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
Homo sapiens
-
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
assay at
7.4
assay at
7.4
-
assay at
7.5
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
assay at room temperature
25
-
assay at
top print hide Go to Organism Search
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
top print hide Go to Source Tissue Search
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
retinal pigment epithelial cells
Manually annotated by BRENDA team
enzyme SCD1 is upregulated in enriched liver tumor-initiating cell populations and sporadically expressed in human hepatocellular carcinoma specimens, elevated SCD1 expression in hepatocellular carcinoma tumors
Manually annotated by BRENDA team
EVT cell line
Manually annotated by BRENDA team
stably expressing the full-length HCV genotype 1b replicon with a S2204I adaptive mutation in NS5A (Huh7.5 FGR)
Manually annotated by BRENDA team
upregulation of SCD1 of self-renewing liver cancer cells in chemoresistant hepatospheres
Manually annotated by BRENDA team
colorectal adenocarcinoma cells
Manually annotated by BRENDA team
SV40-transformed human lung fibroblasts, SV40-WI38
Manually annotated by BRENDA team
-
normal lung fibroblasts WI38 and the derived SV40-tranformed strain cells SV40-WI38, SCD protein content 3.3fold increased in SV40-WI38 cells compared to WI38 cells
Manually annotated by BRENDA team
-
obesity shows a 3fold increase in transcript level of SCD1
Manually annotated by BRENDA team
additional information
top print hide Go to Localization Search
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
SCD1 protein consists of four transmembrane domains with both NH2(N) and C-termini directed to cytosol. It contains 8 histidine (His) residues. They form three His regions, one of which is located in C-terminus and the other two in the cytoplasmatic loop
Manually annotated by BRENDA team
Highest Expressing Human Cell Lines
Cell Line Links Gene Links
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
physiological function
evolution
although SCD5 has been initially thought to be present exclusively in primates, SCD5 orthologues have also been found in a variety of vertebrates, including ruminants, pigs, dogs, and birds. Several phylogenetic analyses of mammalian SCD variants hint at the possibility that a primordial DELTA9-desaturase gene diverged into scd1 and scd5 as independently duplicated genes early in vertebrate evolution. The pattern of gene expression after gene duplication may have resulted in functional specialization of SCD5, which may help explain its distinct expression profile in tissues and organs when compared to SCD1
malfunction
metabolism
role of SCD5 in metabolism, and in cell proliferation, differentiation and survival, overview. Isozyme SCD5, similar to isozyme SCD1, may not only determine the MUFA:SFA ratio but also the rate of polar and neutral lipid synthesis in fast-replicating cells. Further supporting a role for SCD5 in lipid regulation, it is observed that in mice with a global SCD1 knockout the liver-specific expression of human SCD5 fully reverses the decreased levels of hepatic triacylglycerol observed in SCD1-ablated animals
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
SCD_HUMAN
359
4
41523
Swiss-Prot
-
PDB
SCOP
CATH
UNIPROT
ORGANISM
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
37000
-
Western Blot using an antibody against SCD1
58000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
purified enzyme in complex with its substrate stearoyl-CoA, X-ray diffraction structure determination and analysis at 3.25 A resolution. The two iron cations are replaced by zinc cations in the crystal structure
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
SCD1 protein is a short-lived protein with a half-life of 2-4 hours and is stabilized by the PPAR agonist clofibric acid
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
near complete transfer of the in vitro expressed enzyme integral membrane protein into the liposomes, followed by single step purification via centrifugation in a density gradient yielded proteoliposomes with the desaturase in high purity as judged by capillary electrophoresis, method optimization of cell-free translation to the assembly and purification of integral membrane protein complexes, overview
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
cDNA fragment corresponding to bp 278-2005 of the sequence was subcloned into a pcDNA3 vector in antisense orientation and stably transfected into SV40-WI38 lung fibroblasts cells, enzyme activity reduced in these stable cell clones, reduced protein level, reduced enzyme expression slows the rate of cell proliferation and suppresses anchorage-independent proliferation, SCD deficiency promotes apoptosis in a ceramide-independent manner
expressed in HEK-293 cell
gene scd, lentiviral-based overexpression and knockdown of SCD in tumor-initiating cells
gene SCD, semiquantitative and quantitative RT-PCR enzyme expression analysis
gene SCD1, localized in chromosome 10
gene scd1, quantitative real-time PCR enzyme expression analysis
gene scd1, quantitative real-time PCR expression analysis
in vitro translation using a wheat germ cell-free extract in the presence of unilamelar liposomes, method optimization of cell-free translation to the assembly and purification of integral membrane protein complexes
expressed in HEK-293 cells
-
expressed in HEK-293A cells
-
expressed in primary human skeletal muscle cells from obese and lean donors, SCD1 mRNA levels are increased 2.8fold, protein levels are increased 5.7fold in myotubes from obese compared to lean subjects
-
gender- and age-related quantitative expression analysis of SCD in brains in relation to the fatty acid composition, overview
-
gene SCD5, localized in chromosome 4
gene scd5, located on chromosome 4, recombinant expression of human SCD5 in mouse 3T3-L1 preadipocytes leading to elevation of oleic acid without modifying the content of palmitoleic acid. Lentivirus-mediated expression of SCD5 in human melanoma and murine mammary carcinoma cells markedly increase the oleic acid/stearic acid ratio with minimal changes in the palmitoleic acid/palmitic acid ratio. Liver-specific overexpression of human SCD5 in mice with global SCD1 depletion increases the levels of oleic acid, but not palmitoleic acid
hSCD1 and GFP-hSCD1 expressed in HEK-293 cells
hSCD5 and GFP-fused hSCD5 expressed in HEK-293 cells
isozyme SCD5 liver-specific overexpression in isozyme SCD1 global knockout mutants
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
elanocortin receptor agonist MT II and leptin suppress the liver Scd1 independently of insulin and SREBP-1c
enzyme SCD1 is 28fold upregulated in enriched liver tumor-initiating cell populations and sporadically expressed in human hepatocellular carcinoma specimens, upregulation of SCD1 of self-renewing liver cancer cells in chemoresistant hepatospheres
Scd1 is both transcriptionally and post-transcriptionally regulated. Scd1 transcription is induced by binding of liver X receptor (LXR) to LXR response element (LXRE) and that of sterol regulatory-element binding protein-1c (SREBP-1c) to the SREBP element (SRE). As LXR activates Srebp-1c transcription, LXR is capable of activating Scd1 directly and indirectly. Dietary carbohydrate such as glucose, fructose and sucrose, increases the expression of liver Scd1 in both SREBP-1c dependent and independent manners and the latter is caused by carbohydrate-induced LXR and the activation of carbohydrate response-element binding protein (ChREBP). Scd1 is upregulated by activation of the xenobiotic nuclear receptor pregnane-X-receptor (PXR), but this regulation may be mediated by the ability of PXR agonists to activate both PXR and LXR and to induce CD36 which takes up native lipoproteins, oxidized LDL, oxidized phospholipids, and long-chain fatty acids (FA). Toll-like receptor 2 (TLR2)-NF-kappaB activation transcriptionally induces SCD1 in human sebocytes and this underlies antimicrobial defense facilitated by MUFA in skin. SCD1 protein is a short-lived protein with a half-life of 2-4 hours and is stabilized by the PPAR agonist clofibric acid, which also stimulates Scd1 transcription
C-reactive protein concentrations are positively associated with estimated SCD-1 activity
-
elanocortin receptor agonist MT II and leptin suppress the liver Scd1 independently of insulin and SREBP-1c
linolenic acid and eicosapentaenoic acid decrease SCD mRNA (EC50 of 0.50 and 1.67 mM), whereas alpha-linolenic acid does not, GW-9662 at a pan-peroxisome proliferation activator receptor antagonistic dose does not obviate the effects of linolenic acid and eicosapentaenoic acid on SCD mRNA
-
SCD-1 expression is about 2fold upregulated in coronary artery smooth muscle cells, myotubes, and Hep-G2 cells at 0.5 mM palmitate, SCD-1 is upregulated using 0.01 mM TO-901317 in HAEC cells, inhibition of SCD-1 with cis-10,trans-12-conjugated linoleic acid blocks the upregulating effect of TO-901317
-
SCD-1 is not upregulated in HAEC cells upon palmitate treatment
-
SCD1 expression is induced by palmitate, high SCD1 inducibility is associated with a low inflammatory and endoplasmic reticulum stress response to palmitate exposure
-
Scd1 is both transcriptionally and post-transcriptionally regulated. Scd1 transcription is induced by binding of liver X receptor (LXR) to LXR response element (LXRE) and that of sterol regulatory-element binding protein-1c (SREBP-1c) to the SREBP element (SRE). As LXR activates Srebp-1c transcription, LXR is capable of activating Scd1 directly and indirectly. Dietary carbohydrate such as glucose, fructose and sucrose, increases the expression of liver Scd1 in both SREBP-1c dependent and independent manners and the latter is caused by carbohydrate-induced LXR and the activation of carbohydrate response-element binding protein (ChREBP). Scd1 is upregulated by activation of the xenobiotic nuclear receptor pregnane-X-receptor (PXR), but this regulation may be mediated by the ability of PXR agonists to activate both PXR and LXR and to induce CD36 which takes up native lipoproteins, oxidized LDL, oxidized phospholipids, and long-chain fatty acids (FA). Toll-like receptor 2 (TLR2)-NF-kappaB activation transcriptionally induces SCD1 in human sebocytes and this underlies antimicrobial defense facilitated by MUFA in skin. SCD1 protein is a short-lived protein with a half-life of 2-4 hours and is stabilized by the PPAR agonist clofibric acid, which also stimulates Scd1 transcription. Human SCD1/5 may gain the stability by forming dimers and oligomers
the enzyme level is increased in human lung tumors
-
RENATURED/Commentary
ORGANISM
UNIPROT
LITERATURE
in vitro reconstitution of the non-heme iron and heme active sites to a functional reconstituted enzyme complex after in vitro translation and protein integration into liposomes, method optimization, overview
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
medicine
pharmacology
targeting SCD1 in combination with sorafenib may be another therapeutic strategy against liver cancer. Clinically, SCD1 serves as a good predictive marker for patient responses to sorafenib treatment. Targeting SCD1 synergizes the effect of sorafenib both in vitro and in vivo
drug development
-
accelerated bottom-up drug design platform enables the discovery of stearoyl-CoA desaturase 1 inhibitors for cancer therapy
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Choi, Y.; Park, Y.; Pariza, M.W.; Ntambi, J.M.
Regulation of stearoyl-CoA desaturase activity by the trans-10,cis-12 isomer of conjugated linoleic acid in HepG2 cells
Biochem. Biophys. Res. Commun.
284
689-693
2001
Homo sapiens
Manually annotated by BRENDA team
Wang, J.; Yu, L.; Schmidt, R.E.; Su, C.; Huang, X.; Gould, K.; Cao, G.
Characterization of HSCD5, a novel human stearoyl-CoA desaturase unique to primates
Biochem. Biophys. Res. Commun.
332
735-742
2005
Homo sapiens, Homo sapiens (Q86SK9)
Manually annotated by BRENDA team
Scaglia, N.; Caviglia, J.M.; Igal, R.A.
High stearoyl-CoA desaturase protein and activity levels in simian virus 40 transformed-human lung fibroblasts
Biochim. Biophys. Acta
1687
141-151
2005
Homo sapiens
Manually annotated by BRENDA team
Hulver, M.W.; Berggren, J.R.; Carper, M.J.; Miyazaki, M.; Ntambi, J.M.; Hoffman, E.P.; Thyfault, J.P.; Stevens, R.; Dohm, G.L.; Houmard, J.A.; Muoio, D.M.
Elevated stearoyl-CoA desaturase-1 expression in skeletal muscle contributes to abnormal fatty acid partitioning in obese humans
Cell Metab.
2
251-261
2005
Homo sapiens
Manually annotated by BRENDA team
Riserus, U.; Tan, G.D.; Fielding, B.A.; Neville, M.J.; Currie, J.; Savage, D.B.; Chatterjee, V.K.; Frayn, K.N.; ORahilly, S.; Karpe, F.
Rosiglitazone increases indexes of stearoyl-CoA desaturase activity in humans: link to insulin sensitization and the role of dominant-negative mutation in peroxisome proliferator-activated receptor-gamma
Diabetes
54
1379-1384
2005
Homo sapiens
Manually annotated by BRENDA team
Scaglia, N.; Igal, R.A.
Stearoyl-CoA desaturase is involved in the control of proliferation, anchorage-independent growth, and survival in human transformed cells
J. Biol. Chem.
280
25339-25349
2005
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
Chong, M.F.; Hodson, L.; Bickerton, A.S.; Roberts, R.; Neville, M.; Karpe, F.; Frayn, K.N.; Fielding, B.A.
Parallel activation of de novo lipogenesis and stearoyl-CoA desaturase activity after 3 d of high-carbohydrate feeding
Am. J. Clin. Nutr.
87
817-823
2008
Homo sapiens
Manually annotated by BRENDA team
Mar-Heyming, R.; Miyazaki, M.; Weissglas-Volkov, D.; Kolaitis, N.A.; Sadaat, N.; Plaisier, C.; Pajukanta, P.; Cantor, R.M.; de Bruin, T.W.; Ntambi, J.M.; Lusis, A.J.
Association of stearoyl-CoA desaturase 1 activity with familial combined hyperlipidemia
Arterioscler. Thromb. Vasc. Biol.
28
1193-1199
2008
Homo sapiens
Manually annotated by BRENDA team
Zhao, H.; Serby, M.D.; Smith, H.T.; Cao, N.; Suhar, T.S.; Surowy, T.K.; Camp, H.S.; Collins, C.A.; Sham, H.L.; Liu, G.
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors
Bioorg. Med. Chem. Lett.
17
3388-3391
2007
Homo sapiens
Manually annotated by BRENDA team
Xin, Z.; Zhao, H.; Serby, M.D.; Liu, B.; Liu, M.; Szczepankiewicz, B.G.; Nelson, L.T.; Smith, H.T.; Suhar, T.S.; Janis, R.S.; Cao, N.; Camp, H.S.; Collins, C.A.; Sham, H.L.; Surowy, T.K.; Liu, G.
Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors
Bioorg. Med. Chem. Lett.
18
4298-4302
2008
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Stefan, N.; Peter, A.; Cegan, A.; Staiger, H.; Machann, J.; Schick, F.; Claussen, C.D.; Fritsche, A.; Haering, H.U.; Schleicher, E.
Low hepatic stearoyl-CoA desaturase 1 activity is associated with fatty liver and insulin resistance in obese humans
Diabetologia
51
648-656
2008
Homo sapiens
Manually annotated by BRENDA team
Yee, J.K.; Mao, C.S.; Hummel, H.S.; Lim, S.; Sugano, S.; Rehan, V.K.; Xiao, G.; Lee, W.N.
Compartmentalization of stearoyl-CoA desaturase enzyme-1 activity in HepG2 cells
J. Lipid Res.
49
2124-2134
2008
Homo sapiens
Manually annotated by BRENDA team
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
J. Med. Chem.
50
3086-3100
2007
Mus musculus, Homo sapiens
Manually annotated by BRENDA team
Paillard, F.; Catheline, D.; Duff, F.L.; Bouriel, M.; Deugnier, Y.; Pouchard, M.; Daubert, J.C.; Legrand, P.
Plasma palmitoleic acid, a product of stearoyl-coA desaturase activity, is an independent marker of triglyceridemia and abdominal adiposity
Nutr. Metab. Cardiovasc. Dis.
18
436-440
2008
Homo sapiens
Manually annotated by BRENDA team
Melhus, H.; Riserus, U.; Warensjoe, E.; Wernroth, L.; Jensevik, K.; Berglund, L.; Vessby, B.; Michaelsson, K.
A high activity index of stearoyl-CoA desaturase is associated with increased risk of fracture in men
Osteoporos. Int.
19
929-934
2008
Homo sapiens
Manually annotated by BRENDA team
McNamara, R.K.; Liu, Y.; Jandacek, R.; Rider, T.; Tso, P.
The aging human orbitofrontal cortex: decreasing polyunsaturated fatty acid composition and associated increases in lipogenic gene expression and stearoyl-CoA desaturase activity
Prostaglandins Leukot. Essent. Fatty Acids
78
293-304
2008
Homo sapiens
Manually annotated by BRENDA team
Goren, M.A.; Fox, B.G.
Wheat germ cell-free translation, purification, and assembly of a functional human stearoyl-CoA desaturase complex
Protein Expr. Purif.
62
171-178
2008
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
Peter, A.; Weigert, C.; Staiger, H.; Rittig, K.; Cegan, A.; Lutz, P.; Machicao, F.; Haering, H.U.; Schleicher, E.
Induction of stearoyl-CoA desaturase protects human arterial endothelial cells against lipotoxicity
Am. J. Physiol. Endocrinol. Metab.
295
E339-E349
2008
Homo sapiens
Manually annotated by BRENDA team
Dillon, R.; Greig, M.J.; Bhat, B.G.
Development of a novel LC/MS method to quantitate cellular stearoyl-CoA desaturase activity
Anal. Chim. Acta
627
99-104
2008
Homo sapiens
Manually annotated by BRENDA team
Koltun, D.O.; Parkhill, E.Q.; Vasilevich, N.I.; Glushkov, A.I.; Zilbershtein, T.M.; Ivanov, A.V.; Cole, A.G.; Henderson, I.; Zautke, N.A.; Brunn, S.A.; Mollova, N.; Leung, K.; Chisholm, J.W.; Zablocki, J.
Novel, potent, selective, and metabolically stable stearoyl-CoA desaturase (SCD) inhibitors
Bioorg. Med. Chem. Lett.
19
2048-2052
2009
Rattus norvegicus, Homo sapiens
Manually annotated by BRENDA team
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
Bioorg. Med. Chem. Lett.
19
3050-3053
2009
Rattus norvegicus, Homo sapiens
Manually annotated by BRENDA team
Koltun, D.O.; Zilbershtein, T.M.; Migulin, V.A.; Vasilevich, N.I.; Parkhill, E.Q.; Glushkov, A.I.; McGregor, M.J.; Brunn, S.A.; Chu, N.; Hao, J.; Mollova, N.; Leung, K.; Chisholm, J.W.; Zablocki, J.
Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors
Bioorg. Med. Chem. Lett.
19
4070-4074
2009
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Uto, Y.; Ogata, T.; Harada, J.; Kiyotsuka, Y.; Ueno, Y.; Miyazawa, Y.; Kurata, H.; Deguchi, T.; Watanabe, N.; Takagi, T.; Wakimoto, S.; Okuyama, R.; Abe, M.; Kurikawa, N.; Kawamura, S.; Yamato, M.; Osumi, J.
Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide
Bioorg. Med. Chem. Lett.
19
4151-4158
2009
Mus musculus, Homo sapiens
Manually annotated by BRENDA team
Uto, Y.; Ogata, T.; Kiyotsuka, Y.; Miyazawa, Y.; Ueno, Y.; Kurata, H.; Deguchi, T.; Yamada, M.; Watanabe, N.; Takagi, T.; Wakimoto, S.; Okuyama, R.; Konishi, M.; Kurikawa, N.; Kono, K.; Osumi, J.
Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part II: Identification of 4-ethylamino-3-(2-hydroxyethoxy)-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide and its biological evaluation
Bioorg. Med. Chem. Lett.
19
4159-4166
2009
Mus musculus, Homo sapiens
Manually annotated by BRENDA team
Uto, Y.; Ogata, T.; Kiyotsuka, Y.; Ueno, Y.; Miyazawa, Y.; Kurata, H.; Deguchi, T.; Watanabe, N.; Konishi, M.; Okuyama, R.; Kurikawa, N.; Takagi, T.; Wakimoto, S.; Ohsumi, J.
Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats
Bioorg. Med. Chem. Lett.
20
341-345
2010
Mus musculus, Homo sapiens
Manually annotated by BRENDA team
Petersson, H.; Basu, S.; Cederholm, T.; Riserus, U.
Serum fatty acid composition and indices of stearoyl-CoA desaturase activity are associated with systemic inflammation: Longitudinal analyses in middle-aged men
Br. J. Nutr.
99
1186-1189
2008
Homo sapiens
Manually annotated by BRENDA team
Peter, A.; Weigert, C.; Staiger, H.; Machicao, F.; Schick, F.; Machann, J.; Stefan, N.; Thamer, C.; Haering, H.U.; Schleicher, E.
Individual stearoyl-CoA desaturase 1 expression modulates endoplasmic reticulum stress and inflammation in human myotubes and is associated with skeletal muscle lipid storage and insulin sensitivity in vivo
Diabetes
58
1757-1765
2009
Homo sapiens
Manually annotated by BRENDA team
Kotronen, A.; Seppaenen-Laakso, T.; Westerbacka, J.; Kiviluoto, T.; Arola, J.; Ruskeepaeae, A.L.; Oresic, M.; Yki-Jaervinen, H.
Hepatic stearoyl-CoA desaturase (SCD)-1 activity and diacylglycerol but not ceramide concentrations are increased in the nonalcoholic human fatty liver
Diabetes
58
203-208
2009
Homo sapiens
Manually annotated by BRENDA team
Issandou, M.; Bouillot, A.; Brusq, J.M.; Forest, M.C.; Grillot, D.; Guillard, R.; Martin, S.; Michiels, C.; Sulpice, T.; Daugan, A.
Pharmacological inhibition of stearoyl-CoA desaturase 1 improves insulin sensitivity in insulin-resistant rat models
Eur. J. Pharmacol.
618
28-36
2009
Rattus norvegicus, Homo sapiens
Manually annotated by BRENDA team
Dobrzyn, A.; Dobrzyn, P.
Inhibition of stearoyI-CoA desaturase by cyclic amine derivatives
Expert Opin. Ther. Pat.
18
457-460
2008
Rattus norvegicus, Homo sapiens
-
Manually annotated by BRENDA team
Liu, G.
Stearoyl-CoA desaturase inhibitors: update on patented compounds
Expert Opin. Ther. Pat.
19
1169-1191
2009
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Velliquette, R.; Gillies, P.; Kris-Etherton, P.; Green, J.; Zhao, G.; Vanden Heuvel, J.
Regulation of human stearoyl-CoA desaturase by omega-3 and omega-6 fatty acids: Implications for the dietary management of elevated serum triglycerides
J. Clin. Lipidol.
3
281-288
2009
Homo sapiens
Manually annotated by BRENDA team
Zhou, Y.E.; Egeland, G.M.; Meltzer, S.J.; Kubow, S.
The association of desaturase 9 and plasma fatty acid composition with insulin resistance-associated factors in female adolescents
Metab. Clin. Exp.
58
158-166
2009
Homo sapiens
Manually annotated by BRENDA team
Lausada, N.; de Gomez Dumm, I.N.; Raimondi, J.C.; de Alaniz, M.J.
Effect of cyclosporine and sirolimus on fatty acid desaturase activities in cultured HEPG2 cells
Transplant. Proc.
41
1865-1870
2009
Homo sapiens
Manually annotated by BRENDA team
Wu, Z.; Li, D.; Gou, K.
Overexpression of stearoyl-CoA desaturase-1 results in an increase of conjugated linoleic acid (CLA) and n-7 fatty acids in 293 cells
Biochem. Biophys. Res. Commun.
398
473-476
2010
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
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
Bioorg. Med. Chem. Lett.
20
1593-1597
2010
Rattus norvegicus, Homo sapiens
Manually annotated by BRENDA team
Powell, D.A.; Ramtohul, Y.; Lebrun, M.E.; Oballa, R.; Bhat, S.; Falgueyret, J.P.; Guiral, S.; Huang, Z.; Skorey, K.; Tawa, P.; Zhang, L.
2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors
Bioorg. Med. Chem. Lett.
20
6366-6369
2010
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Isabel, E.; Powell, D.A.; Black, W.C.; Chan, C.C.; Crane, S.; Gordon, R.; Guay, J.; Guiral, S.; Huang, Z.; Robichaud, J.; Skorey, K.; Tawa, P.; Xu, L.; Zhang, L.; Oballa, R.
Biological activity and preclinical efficacy of azetidinyl pyridazines as potent systemically-distributed stearoyl-CoA desaturase inhibitors
Bioorg. Med. Chem. Lett.
21
479-483
2011
Rattus norvegicus, Homo sapiens
Manually annotated by BRENDA team
Igal, R.A.
Stearoyl-CoA desaturase-1: a novel key player in the mechanisms of cell proliferation, programmed cell death and transformation to cancer
Carcinogenesis
31
1509-1515
2010
Homo sapiens
Manually annotated by BRENDA team
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
Bioorg. Med. Chem. Lett.
21
5692-5696
2011
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
Nashed, M.; Chisholm, J.W.; Igal, R.A.
Stearoyl-CoA desaturase activity modulates the activation of epidermal growth factor receptor in human lung cancer cells
Exp. Biol. Med. (Maywood)
237
1007-1017
2012
Homo sapiens
Manually annotated by BRENDA team
Takahashi, H.; Nakayama, R.; Hayashi, S.; Nemoto, T.; Murase, Y.; Nomura, K.; Takahashi, T.; Kubo, K.; Marui, S.; Yasuhara, K.; Nakamura, T.; Sueo, T.; Takahashi, A.; Tsutsumiuchi, K.; Ohta, T.; Kawai, A.; Sugita, S.; Yamamoto, S.; Kobayashi, T.; Honda, H.; Yoshida, T.; Hasegawa, T.
Macrophage migration inhibitory factor and stearoyl-CoA desaturase 1: potential prognostic markers for soft tissue sarcomas based on bioinformatics analyses
PLoS ONE
8
e78250
2013
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
Koeberle, A.; Loeser, K.; Thuermer, M.
Stearoyl-CoA desaturase-1 and adaptive stress signaling
Biochim. Biophys. Acta
1861
1719-1726
2016
Mus musculus (P13516), Homo sapiens (O00767)
Manually annotated by BRENDA team
Sun, S.; Zhang, Z.; Pokrovskaia, N.; Chowdhury, S.; Jia, Q.; Chang, E.; Khakh, K.; Kwan, R.; McLaren, D.G.; Radomski, C.C.; Ratkay, L.G.; Fu, J.; Dales, N.A.; Winther, M.D.
Discovery of triazolone derivatives as novel, potent stearoyl-CoA desaturase-1 (SCD1) inhibitors
Bioorg. Med. Chem.
23
455-465
2015
Homo sapiens (O00767), Mus musculus (P13516)
Manually annotated by BRENDA team
Ma, M.K.F.; Lau, E.Y.T.; Leung, D.H.W.; Lo, J.; Ho, N.P.Y.; Cheng, L.K.W.; Ma, S.; Lin, C.H.; Copland, J.A.; Ding, J.; Lo, R.C.L.; Ng, I.O.L.; Lee, T.K.W.
Stearoyl-CoA desaturase regulates sorafenib resistance via modulation of ER stress-induced differentiation
J. Hepatol.
67
979-990
2017
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
Yang, C.; Lim, W.; Bazer, F.W.; Song, G.
Oleic acid stimulation of motility of human extravillous trophoblast cells is mediated by stearoyl-CoA desaturase-1 activity
Mol. Hum. Reprod.
23
755-770
2017
Homo sapiens (O00767), Homo sapiens
Manually annotated by BRENDA team
Poliakov, E.; Samuel, W.; Duncan, T.; Gutierrez, D.B.; Mata, N.L.; Redmond, T.M.
Inhibitory effects of fenretinide metabolites N-[4-methoxyphenyl]retinamide (MPR) and 4-oxo-N-(4-hydroxyphenyl)retinamide (3-keto-HPR) on fenretinide molecular targets beta-carotene oxygenase 1, stearoyl-CoA desaturase 1 and dihydroceramide DELTA4-desaturase 1
PLoS ONE
12
e0176487
2017
Homo sapiens (O00767)
Manually annotated by BRENDA team
Lyn, R.K.; Singaravelu, R.; Kargman, S.; OHara, S.; Chan, H.; Oballa, R.; Huang, Z.; Jones, D.M.; Ridsdale, A.; Russell, R.S.; Partridge, A.W.; Pezacki, J.P.
Stearoyl-CoA desaturase inhibition blocks formation of hepatitis C virus-induced specialized membranes
Sci. Rep.
4
4549
2014
Homo sapiens (O00767)
Manually annotated by BRENDA team
Chen, L.; Ren, J.; Yang, L.; Li, Y.; Fu, J.; Li, Y.; Tian, Y.; Qiu, F.; Liu, Z.; Qiu, Y.
Stearoyl-CoA desaturase-1 mediated cell apoptosis in colorectal cancer by promoting ceramide synthesis
Sci. Rep.
6
19665
2016
Homo sapiens (O00767)
Manually annotated by BRENDA team
ALJohani, A.M.; Syed, D.N.; Ntambi, J.M.
Insights into stearoyl-CoA desaturase-1 regulation of systemic metabolism
Trends Endocrinol. Metab.
28
831-842
2017
Homo sapiens (Q86SK9), Homo sapiens (O00767), Mus musculus (P13011), Mus musculus (P13516), Mus musculus (Q8BNZ5), Mus musculus (Q8CFY4)
Manually annotated by BRENDA team
Igal, R.A.; Sinner, D.I.
Stearoyl-CoA desaturase 5 (SCD5), a DELTA-9 fatty acyl desaturase in search of a function
Biochim. Biophys. Acta
1866
158840
2021
Homo sapiens (Q86SK9)
Manually annotated by BRENDA team
Tesfay, L.; Paul, B.T.; Konstorum, A.; Deng, Z.; Cox, A.O.; Lee, J.; Furdui, C.M.; Hegde, P.; Torti, F.M.; Torti, S.V.
Stearoyl-CoA desaturase 1 protects ovarian cancer cells from ferroptotic cell death
Cancer Res.
79
5355-5366
2019
Homo sapiens (O00767)
Manually annotated by BRENDA team
Kikuchi, K.; Tsukamoto, H.
Stearoyl-CoA desaturase and tumorigenesis
Chem. Biol. Interact.
316
108917
2020
Homo sapiens, Homo sapiens (O00767)
Manually annotated by BRENDA team
Wu, Y.; Baylin, A.; Colacino, J.A.
Iron, oxidative stress, and DELTA9 stearoyl-coenzyme A desaturase index (C16 1/C16 0) An analysis applying the national health and nutrition examination survey 2003-04
Curr. Dev. Nutr.
2
1-8
2018
Homo sapiens
Manually annotated by BRENDA team
Iida, T.; Ubukata, M.; Mitani, I.; Nakagawa, Y.; Maeda, K.; Imai, H.; Ogoshi, Y.; Hotta, T.; Sakata, S.; Sano, R.; Morinaga, H.; Negoro, T.; Oshida, S.; Tanaka, M.; Inaba, T.
Discovery of potent liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitors, thiazole-4-acetic acid derivatives, for the treatment of diabetes, hepatic steatosis, and obesity
Eur. J. Med. Chem.
158
832-852
2018
Homo sapiens (O00767), Mus musculus (P13516)
Manually annotated by BRENDA team
von Roemeling, C.A.; Caulfield, T.R.; Marlow, L.; Bok, I.; Wen, J.; Miller, J.L.; Hughes, R.; Hazlehurst, L.; Pinkerton, A.B.; Radisky, D.C.; Tun, H.W.; Kim, Y.S.B.; Lane, A.L.; Copland, J.A.
Accelerated bottom-up drug design platform enables the discovery of novel stearoyl-CoA desaturase 1 inhibitors for cancer therapy
Oncotarget
9
3-20
2018
Homo sapiens
Manually annotated by BRENDA team