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Information on EC 1.14.19.1 - stearoyl-CoA 9-desaturase and Organism(s) Rattus norvegicus and UniProt Accession P07308
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1.14.19.1 stearoyl-CoA 9-desaturaseIUBMB 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).
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Word Map
- 1.14.19.1
-
sickle
- cardiac
- children
- ventricular
- pain
- hemoglobin
- arrhythmia
-
vaso-occlusive
-
transfusion
- anemia
- infarct
- cardiomyopathy
- episode
- cardiovascular
- coronary
- myocardial
- artery
-
stratification
-
polyunsaturated
-
ejection
- hydroxyurea
- stroke
-
monounsaturated
- crises
- chest
-
defibrillator
-
desaturation
-
lipogenesis
-
arrhythmogenic
- tachycardia
- hemoglobinopathy
-
all-cause
-
cardioverter
-
pufas
-
cardioverter-defibrillator
-
desaturases
-
electrocardiogram
-
lipogenic
-
transfused
- pharmacology
- thalassemia
-
12-lead
-
palmitoleic
- agriculture
- tachyarrhythmias
-
caregiver
-
out-of-hospital
-
resynchronization
- medicine
-
transcranial
- syncope
- drug development
-
holter
-
alloimmunization
The taxonomic range for the selected organisms is: Rattus norvegicus
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
The expected taxonomic range for this enzyme is: Bacteria, Eukaryota, Archaea
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
topSYNONYM 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
acyl coenzyme A desaturase
-
-
-
-
acyl-CoA desaturase
-
-
-
-
DELTA9-acyl CoA desaturase
-
-
-
-
DELTA9-desaturase
-
-
-
-
eicosatrienoyl-CoA desaturase
-
-
-
-
fatty acid 9-desaturase
-
-
-
-
fatty acid DELTA9-desaturase
-
-
-
-
fatty acid desaturase
-
-
-
-
fatty acyl CoA DELTA9-desaturase
-
-
-
-
fatty acyl DELTA9-desaturase
-
-
-
-
fatty acyl-CoA desaturase
-
-
-
-
long-chain fatty acid DELTA9-desaturase
-
-
-
-
palmitoyl CoA desaturase
-
-
-
-
palmitoyl-CoA desaturase
-
-
-
-
SCD1
-
-
stearoyl coenzyme A desaturase
-
-
-
-
stearoyl-CoA (DELTA8) desaturase
-
-
-
-
stearoyl-CoA desaturase
stearyl coenzyme A desaturase
-
-
-
-
stearyl-CoA desaturase
-
-
-
-
stearoyl-CoA desaturase
-
-
-
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT
LITERATURE
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
the reducing equivalents required for the desaturation site seem to be supplied from NADPH via cytochrome b5 as electron carrier
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
introduction of double bonds at fixed positions from the carboxyl group of the fatty acid. D-hydrogen atoms are removed during desaturation. Mixed-function oxidase, acting via hydroxy acid intermediates. Acetyl-CoA desaturase, carboxylase and fatty acid synthetase are all controlled together as a unit and influenced by dietary components
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
cytochrome b5, cytochrome b5 reductase and lipid and/or detergent are needed for all assays. A cis-hydrogen abstraction mechanism is involved in desaturation
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
the synthesis is transcriptionally regulated by fat-free diet and sterols. Cholesterol-supplemented media as well as the transient transfection induces the expression of stearoyl-CoA desaturase RNA
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
multienzyme, insertion of a double bond in 9,10 position
-
stearoyl-CoA + 2 ferrocytochrome b5 + O2 + 2 H+ = oleoyl-CoA + 2 ferricytochrome b5 + 2 H2O
electron flow from NADH to cytochrome b5, via cytochrome b5 reductase. Different types of acyl-CoA desaturation show immunological differences
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
redox reaction
-
-
-
-
oxidation
-
-
-
-
reduction
-
-
-
-
PATHWAY SOURCE
PATHWAYS
BRENDA
-
-, -, -
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
9014-34-0
-
SUBSTRATE
PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
activity measured via the generation of tritium enriched water from the substrate 9,10-3H-steaoryl-CoA
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
?
N-hydroxy-benzenecarboximidamide + NADH + H+ + O2
benzamidine + NAD+ + H2O
-
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
-
?
stearoyl-CoA + NAD(P)H + O2
oleoyl-CoA + NAD(P)+ + H2O
-
fatty acid desaturation
-
?
stearoyl-CoA + NADH + H+ + O2
oleoyl-CoA + NAD+ + H2O
-
-
-
-
?
stearate + AH2 + O2
oleate + A + 2 H2O
-
biosynthesis of unsaturated fatty acid, synthesis of triacylglycerol from oleate
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
-
also other fatty acyl-CoA substrates
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
-
maximal activity
-
?
stearoyl-CoA + NADH + O2
oleoyl-CoA + NAD+ + H2O
-
terminal component in the enzyme system
-
?
additional information
?
-
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
?
additional information
?
-
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
?
additional information
?
-
-
12-19 carbon fatty acyl chains undergo 9,10 desaturation. Dephospho-, deamino- and (1-N6-etheno)-CoA analogs of stearoyl-CoA are poorer substrates than stearoyl-CoA
-
-
?
additional information
?
-
-
specific for C14-C19 fatty acyl-CoA substrates
-
-
?
additional information
?
-
-
key enzyme in the synthesis of unsaturated fatty acyl-CoAs
-
-
?
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate)
(Substrate)
LITERATURE
(Substrate)
(Substrate)
COMMENTARY
(Product)
(Product)
LITERATURE
(Product)
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
r=reversible
ir=irreversible
?=not specified
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
?
stearate + AH2 + O2
oleate + A + 2 H2O
-
biosynthesis of unsaturated fatty acid, synthesis of triacylglycerol from oleate
-
?
stearoyl-CoA + AH2 + O2
oleoyl-CoA + A + H2O
-
also other fatty acyl-CoA substrates
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
-
?
stearoyl-CoA + ferrocytochrome b5 + O2 + H+
oleoyl-CoA + ferricytochrome b5 + H2O
-
-
-
?
additional information
?
-
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
?
additional information
?
-
decreased degradation of SCD is responsible for the increase in palmitoyl-CoA chain elongase activity in addition to increased transcription of SCD1 in the rats treated with clofibric acid, overview
-
-
?
additional information
?
-
-
key enzyme in the synthesis of unsaturated fatty acyl-CoAs
-
-
?
COFACTOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
Fe2+
Fe2+
-
contains one atom of non-heme iron per enzyme molecule, catalytic function
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
(1-[6-[3-(3-hydroxybenzyl)-1,2,4-oxadiazol-5-yl]pyridazin-3-yl]piperidin-4-yl)[2-(trifluoromethyl)phenyl]methanone
-
-
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-imidazol-4-yl)methanol
-
-
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)methanol
-
-
(2-[[(5-[[(4-fluoro-2-heptylphenyl)amino]methyl]thiophen-2-yl)carbonyl]amino]-1,3-thiazol-4-yl)acetic acid
-
-
(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
-
-
(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]phenyl)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
-
-
(5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]pyridin-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-(1-[6-[1-(2-ethoxyethyl)-1H-pyrazol-4-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
-
-
1-(1-[6-[4-(ethoxymethyl)-1H-pyrazol-1-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
-
-
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
-
-
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
-
-
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-[1-[6-(1-ethyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-fluoro-2,3-dihydro-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-(trifluoromethyl)-2,3-dihydro-1H-indole
-
-
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-(5-methyl-1,3,4-thiadiazol-2-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-(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)ethanol
-
-
2-(2'-fluorobiphenyl-4-yl)-1-methyl-5-(methylsulfonyl)-2,3-dihydro-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'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(4-phenoxyphenyl)-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
-
-
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)-N-methylacetamide
-
-
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)ethanol
-
-
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
MF-152
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxylic acid
-
-
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'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
-
-
2-(5-[1-[(2,5-dichlorophenyl)carbonyl]piperidin-4-ylidene]-2,4-dioxo-1,3-thiazolidin-3-yl)-N-pentylacetamide
-
-
2-(thiophen-2-yl)-N-(2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1H-benzimidazol-5-yl)acetamide
-
-
2-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylbenzamide
-
-
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-[(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-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-(2-cyclopropylethyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-(3-methylbutyl)-1H-benzimidazole-5-carboxamide
-
-
2-[4-(2-chlorophenoxy)phenyl]-N-[(5-chlorothiophen-2-yl)methyl]-1H-benzimidazole-5-carboxamide
-
-
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][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
-
-
3-(2-hydroxyethoxy)-4-methoxy-N-[5-[3-(trifluoromethyl)benzyl]-1,3-thiazol-2-yl]benzamide
-
-
3-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazino[3,4-b][1,5]benzoxazepin-5(6H)-one
-
-
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(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-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)-N-(1,3-thiazol-2-ylmethyl)benzamide
-
-
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
-
-
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-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
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-chloro-5-fluorophenoxy)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-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-(2-chloro-5-fluorophenoxy)piperidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
-
-
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
-
-
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-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(1H-indol-3-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
15% inhibition at 0.001 mM
4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(2-bromo-5-fluorophenoxy)-1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3,4-thiadiazol-2-yl]piperidine
-
-
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
-
-
4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
20% inhibition at 0.001 mM
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
-
-
4-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
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-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]benzoic acid
-
-
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
-
-
5-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
5-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
5-fluoro-3-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1,2-benzoxazole
-
-
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
-
-
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N,N-dimethylpyridin-2-amine
-
-
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N-methylpyridine-2-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-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxylic acid
-
-
6-(5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazol-2-yl)pyridine-3-carboxylic acid
-
-
6-(methylsulfonyl)-2-[4-(3-methylthiophen-2-yl)phenyl]-1H-benzimidazole
-
-
6-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-(1-[6-[4-(trifluoromethyl)phenyl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
-
-
6-fluoro-1-(1-[6-[6-(trifluoromethyl)pyridin-3-yl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indazole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
-
-
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(1-propyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-fluorophenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1H-imidazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(4-methylphenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(5-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(5-methylthiophen-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(6-methoxypyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-fluoro-1-[1-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-methoxy-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
6-methyl-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
-
-
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-methoxyphenyl)carbonyl]piperazin-1-yl]-N-(3-phenylpropyl)pyridine-3-carboxamide
-
-
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
-
-
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-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
-
-
ethyl 2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxylate
-
-
ethyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-oxadiazol-2-yl]acetate
-
-
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
-
-
methyl [5-(4-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]phenyl)-1,3,4-thiadiazol-2-yl]acetate
-
-
N-(1,3-thiazol-2-yl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(1,3-thiazol-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(2-amino-2-oxoethyl)-6-(2,3-dichlorobenzyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
-
-
N-(2-cyclopropyl-2-hydroxyethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-4-carboxamide
-
-
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-(2-cyclopropylethyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-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-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-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-methylbutyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-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-(3-phenylpropyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
-
N-(5-acetyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
46% inhibition at 0.001 mM
N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
-
N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-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-(cyclopropylmethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
-
-
N-(thiophen-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-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-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-methoxy-3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
-
-
N-methyl-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
-
-
N-methyl-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-methyl-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-imidazo[4,5-c]pyridin-4-amine
-
-
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
-
-
N-[(5-chlorothiophen-2-yl)methyl]-3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)benzamide
-
-
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-(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-(5-chlorothiophen-2-yl)ethyl]-2-(4-phenoxyphenyl)-1H-benzimidazole-5-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-(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-(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-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-oxo-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
-
7% inhibition at 0.001 mM
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
-
-
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
-
-
stearoyl-CoA
-
inhibits SCD activity in concentrations greater than 0.05 mM
[(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-([[4-([[2-(2-cyclopentylethyl)phenyl]amino]methyl)phenyl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
-
[2-([[4-([[2-(trifluoromethyl)phenyl]amino]methyl)piperidin-1-yl]carbonyl]amino)-1,3-thiazol-4-yl]acetic acid
-
-
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanol
-
-
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanone
-
-
[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
-
-
[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl][2-(trifluoromethyl)phenyl]methanone
-
-
[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
-
-
[5-[6-(benzyloxy)pyridazin-3-yl]-3,4,5,6-tetrahydropyrrolo[3,4-c]pyrrol-2(1H)-yl][2-(trifluoromethyl)phenyl]methanone
-
-
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
-
-
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
-
-
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
-
MF-438
additional information
-
phenylalanine, indolepyruvic acid and 2-amino-1-phenylethanol show no inhibitory effect
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
bovine serum albumin
-
stimulates activity in the microsomal fraction
-
stearoyl-CoA-binding protein
-
stimulates activity in the crude microsomal fraction
-
cytochrome b5 reductase
-
NADH-specific, required, EC 1.6.2.2
-
protein
-
basic cytoplasmic protein from rat liver stimulates activity in crude extract, no activity of partially purified enzyme
additional information
treatment of rats with 2-(4-chlorophenoxy)-2-methylpropionic acid, i.e. clofibric acid, or feeding of a fat-free diet markedly elevated hepatic activity of SCD by increasing the steady-state level of SCD1 mRNA and enhancing transcriptional rate, metabolic effects, overview
-
additional information
treatment of rats with 2-(4-chlorophenoxy)-2-methylpropionic acid, i.e. clofibric acid, or feeding of a fat-free diet markedly elevated hepatic activity of SCD by increasing the steady-state level of SCD1 mRNA and enhancing transcriptional rate, metabolic effects, overview
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.0105
stearoyl-CoA
-
in 150 mM KCl, 40 mM NaF, 100 mM sodium phosphate buffer, pH 7.4, at 37°C
additional information
additional information
-
substrates with 14-19 carbon fatty acyl chains show similar Km values of 0.0045-0.005 mM
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.35
stearoyl-CoA
-
fatty acyl-CoA substrates with chain length of 14-19 carbon atoms show similar turnover number of about 22
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
IMAGE
0.000011
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-imidazol-4-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000017
(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008
(2R)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.03
(2R)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Rattus norvegicus
-
IC50 above 0.03 mM
0.000038
(2S)-2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.03
(2S)-N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxypropanamide
Rattus norvegicus
-
IC50 above 0.03 mM
0.000022
(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]phenyl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000034
(5-[6-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000049
(5-[6-[3-(2-bromophenoxy)azetidin-1-yl]pyridazin-3-yl]-1,3,4-oxadiazol-2-yl)methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000009
(5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]pyridin-2-yl)methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00014
(5R)-5-(hydroxymethyl)-3-(6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridin-3-yl)-1,3-oxazolidin-2-one
Rattus norvegicus
-
-
0.000004
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]amino)acetic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000007
([5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[5,4-d]pyrimidin-2-yl]oxy)acetic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.003
1-(1,3-thiazol-2-yl)-4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazine
Rattus norvegicus
-
-
0.000012
1-(1-[6-[1-(2-ethoxyethyl)-1H-pyrazol-4-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000008
1-(1-[6-[4-(ethoxymethyl)-1H-pyrazol-1-yl]pyridazin-3-yl]piperidin-4-yl)-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000164
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)pyrrolidin-2-one
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00015
1-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)urea
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000017
1-[1-[6-(1-ethyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-fluoro-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000422
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000394
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000173
1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-6-(trifluoromethyl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000268
1-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]urea
Rattus norvegicus
-
-
0.000004
1-[5-(1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000034
1-[5-(1,3,4-oxadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000014
1-[5-(1,3-oxazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000015
1-[5-(5-methyl-1,2,4-oxadiazol-3-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00075
1-[5-(5-methyl-1,3,4-thiadiazol-2-yl)-1,3-thiazol-2-yl]-4-[2-(trifluoromethyl)phenoxy]piperidine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0011
2,3-dihydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.00002
2-(1-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-4-yl)ethanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.004489
2-(2'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.002488
2-(2'-fluorobiphenyl-4-yl)-1-methyl-5-(methylsulfonyl)-2,3-dihydro-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000343
2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole-6-sulfonamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000697
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfanyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000472
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfinyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000065
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000156
2-(2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-imidazo[4,5-b]pyridine
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000528
2-(2'-fluorobiphenyl-4-yl)-N,N-dimethyl-1H-benzimidazole-6-sulfonamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.003863
2-(2'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000095
2-(3'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000148
2-(3'-chlorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000021
2-(3'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000319
2-(3'-methylbiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000025
2-(4'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00651
2-(4-phenoxyphenyl)-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0283
2-(4-phenoxyphenyl)-N-(2-phenylethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000015
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)-N-methylacetamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000022
2-(4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-1H-pyrazol-1-yl)ethanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0001
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.007
2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxylic acid
Rattus norvegicus
-
-
0.000004
2-(4-[[2-(trifluoromethyl)phenyl]sulfanyl]piperidin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000278
2-(5'-chloro-2'-fluorobiphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00002
2-(biphenyl-4-yl)-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000042
2-(biphenyl-4-yl)-7-(methylsulfonyl)imidazo[1,2-a]pyridine
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.0032
2-(thiophen-2-yl)-N-(2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1H-benzimidazol-5-yl)acetamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00025
2-([2-[4-(2-chloro-3,5-difluorophenoxy)piperidin-1-yl]-2-oxoethyl]amino)-N-methylbenzamide
Rattus norvegicus
-
-
0.000015
2-hydroxy-N-[2-[2-oxo-3-(trifluoromethyl)-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000019
2-hydroxy-N-[2-[3-(1-methylethyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000162
2-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00136
2-hydroxy-N-[4-oxo-3-[3-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Rattus norvegicus
-
-
0.00342
2-hydroxy-N-[4-oxo-3-[4-(trifluoromethyl)benzyl]-3,4-dihydroquinazolin-6-yl]acetamide
Rattus norvegicus
-
-
0.000012
2-[(3S)-3-[2-(trifluoromethyl)phenoxy]pyrrolidin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000477
2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3-benzothiazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000115 - 0.000212
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
0.000966
2-[4-(2-chlorophenoxy)phenyl]-N-(2-cyclopropylethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00272
2-[4-(2-chlorophenoxy)phenyl]-N-(3-methylbutyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000832
2-[4-(2-chlorophenoxy)phenyl]-N-[(5-chlorothiophen-2-yl)methyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000395
2-[4-(furan-3-yl)phenyl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000076
2-[4-[2-(trifluoromethyl)benzyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000676
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-4-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000003
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000041
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazole-5-sulfonamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000097
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,4,5,9-tetrahydro-6H-purin-6-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000038
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-8-ol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00001
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000083
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-b]pyridine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000007
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000056
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000085
2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[5,4-c]pyridin-4(5H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000227
2-[5-(2-fluorophenyl)pyridin-2-yl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000058
2-[6-(2-fluorophenyl)pyridin-3-yl]-6-(methylsulfonyl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000027
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.001992
3-(5-methyl-1,3,4-oxadiazol-2-yl)-6-[3-[3-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000023
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
0.0013
3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)-N-(1,3-thiazol-2-ylmethyl)benzamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0039
3-hydroxy-N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]propanamide
Rattus norvegicus
-
-
0.03
3-[([4-[2-(acetylamino)ethyl]-2-(4-methoxyphenyl)-3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-6-yl]amino)methyl]benzoic acid
Rattus norvegicus
-
IC50 above 0.03 mM
0.00036
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]-N-methylpropanamide
Rattus norvegicus
-
-
0.000027
3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.000177
3-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000513
3-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000266
3-[2-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-7-oxo-6,7-dihydro[1,3]thiazolo[4,5-d]pyrimidin-5-yl]propanoic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008167
3-[3-(2,6-dichloro-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000067
3-[3-(2-bromo-4-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000028
3-[3-(2-bromo-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000021
3-[3-(2-bromophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000163
3-[3-(2-chloro-5-fluorophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000072
3-[3-(2-iodophenoxy)azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.03
3-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.003385
3-[3-[2-chloro-3-(trifluoromethyl)phenoxy]azetidin-1-yl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.001634
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2,4-oxadiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000008
3-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,2-oxazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0033
3-[6-(4'-chlorobiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.00134
3-[6-(4'-methylbiphenyl-4-yl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000145
3-[6-(4-methoxyphenyl)-7-oxo-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000029
3-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.00189
3-[7-oxo-6-(4-pyridin-3-ylphenyl)-2-[[3-(trifluoromethyl)phenyl]amino]pteridin-8(7H)-yl]propanamide
Rattus norvegicus
-
-
0.000336
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-2-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000396
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-3-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000304
4'-[6-(methylsulfonyl)-1H-benzimidazol-2-yl]biphenyl-4-ol
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.14
4-(1,2-benzoxazol-3-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.538
4-(1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.17
4-(1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.153
4-(2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.151
4-(2,3-dihydro-1H-indol-1-yl)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000078
4-(2-chlorophenoxy)-N-[3-(methylcarbamoyl)phenyl]piperidine-1-carboxamide
Rattus norvegicus
-
-
0.491
4-(3,4-dihydroquinolin-1(2H)-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.347
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.029
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000026 - 0.026
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
0.018
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.082
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(5-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.014
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(6-hydroxy-4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.02
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.052
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[4-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.008
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(2-hydroxyethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.096
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxyacetyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridin-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.088
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(hydroxymethyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.093
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-[5-(methylcarbamoyl)-1,3-thiazol-2-yl]piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000022
4-([6-[4-(2-fluorophenoxy)piperidin-1-yl]pyridazin-3-yl]ethynyl)phenol
Rattus norvegicus
-
-
0.000678
4-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000349
4-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]benzoic acid
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000002
5-(hydroxymethyl)-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000181
5-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000165
5-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000125
5-fluoro-3-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1,2-benzoxazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000008
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidin-7(6H)-one
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000054
5-methyl-2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl][1,3]thiazolo[4,5-d]pyrimidine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000003
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1H-imidazo[4,5-b]pyrazine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000001
5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl][1,3]thiazolo[4,5-b]pyrazin-2-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000083
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-oxadiazole-2-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000003
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3,4-thiadiazole-2-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000127
5-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1H-1,2,4-triazole-3-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000017
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N,N-dimethylpyridin-2-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000035
5-[6-[4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidin-1-yl]pyridazin-3-yl]-N-methylpyridine-2-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
10
6-(3-bromobenzyl)-5,7-dimethyl-N-(tetrahydrofuran-2-ylmethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Rattus norvegicus
-
IC50 below 10 mM
0.0007
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
-
0.1
6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxylic acid
Rattus norvegicus
-
IC50 above 0.1 mM
0.000401
6-(cyclopropylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001248
6-(ethylsulfonyl)-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000489
6-(methylsulfonyl)-2-(2-phenylpyrimidin-5-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000472
6-(methylsulfonyl)-2-[4-(3-methylthiophen-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.001713
6-(methylsulfonyl)-2-[4-(pyridin-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000425
6-(methylsulfonyl)-2-[4-(pyridin-3-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.002473
6-(methylsulfonyl)-2-[4-(pyridin-4-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000097
6-(methylsulfonyl)-2-[4-(thiophen-2-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000104
6-(methylsulfonyl)-2-[4-(thiophen-3-yl)phenyl]-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000035
6-chloro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00009
6-fluoro-1-(1-[6-[4-(trifluoromethyl)phenyl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000016
6-fluoro-1-(1-[6-[6-(trifluoromethyl)pyridin-3-yl]pyridazin-3-yl]piperidin-4-yl)-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000038
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indazole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000023
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000037
6-fluoro-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000022
6-fluoro-1-[1-[6-(1-propyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000011
6-fluoro-1-[1-[6-(3-methyl-1,2,4-thiadiazol-5-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000777
6-fluoro-1-[1-[6-(4-fluorophenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000007
6-fluoro-1-[1-[6-(4-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000016
6-fluoro-1-[1-[6-(4-methyl-1H-imidazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000021
6-fluoro-1-[1-[6-(4-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000079
6-fluoro-1-[1-[6-(4-methylphenyl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000031
6-fluoro-1-[1-[6-(5-methyl-1,3-thiazol-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000121
6-fluoro-1-[1-[6-(5-methylthiophen-2-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000012
6-fluoro-1-[1-[6-(6-methoxypyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000013
6-fluoro-1-[1-[6-(6-methylpyridin-3-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000317
6-methoxy-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000286
6-methyl-1-[1-[6-(1-methyl-1H-pyrazol-4-yl)pyridazin-3-yl]piperidin-4-yl]-2,3-dihydro-1H-indole
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000175
6-tert-butyl-2-(2'-fluorobiphenyl-4-yl)-1H-benzimidazole
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.000127
6-[(3,4-dichlorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Rattus norvegicus
-
-
0.000333
6-[(3-chloro-4-fluorobenzyl)amino]-4-(4-oxopentyl)-2-pyridin-3-ylpyrido[2,3-b]pyrazin-3(4H)-one
Rattus norvegicus
-
-
0.000001
6-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-9H-purine
Rattus norvegicus
-
IC50 less than 0.000039 mM, pH and temperature not specified in the publication
0.00001
6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000157
7-[(3-chlorobenzyl)amino]-1-(4-oxopentyl)-3-(3-pyridin-4-ylphenyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.00019
7-[(3-chlorobenzyl)amino]-3-(4-methoxyphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.000343
7-[(3-chlorobenzyl)amino]-3-(4-methylphenyl)-1-(4-oxopentyl)pyrido[3,4-b]pyrazin-2(1H)-one
Rattus norvegicus
-
-
0.000039
8-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-9H-purin-6-amine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.03
benzyl [3-(2,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Rattus norvegicus
-
IC50 above 0.03 mM
0.000251
benzyl [3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Rattus norvegicus
-
-
0.00025
benzyl [3-(3,4-dimethylbenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Rattus norvegicus
-
-
0.000865
benzyl [3-(3-chloro-4-fluorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Rattus norvegicus
-
-
0.00026
benzyl [3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]carbamate
Rattus norvegicus
-
-
0.0032
benzyl [3-[(3,4-dichlorobenzyl)carbamoyl]-4-(pyridin-3-yloxy)phenyl]carbamate
Rattus norvegicus
-
-
0.00088
conjugated linoleic acid
Rattus norvegicus
-
in 150 mM KCl, 40 mM NaF, 100 mM sodium phosphate buffer, pH 7.4, at 37°C
0.0383
ethyl 2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxylate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00075
methyl (2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)carbamate
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00452
N-(1,3-thiazol-2-yl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000078
N-(1,3-thiazol-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
10
N-(2-amino-2-oxoethyl)-6-(2,3-dichlorobenzyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Rattus norvegicus
-
IC50 below 10 mM
0.0025
N-(2-cyclopropyl-2-hydroxyethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
-
0.0249
N-(2-cyclopropylethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.1
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-4-carboxamide
Rattus norvegicus
-
IC50 above 0.1 mM
0.037
N-(2-cyclopropylethyl)-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.000539
N-(2-cyclopropylethyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000006
N-(2-phenylethyl)-6-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)pyridazine-3-carboxamide
Rattus norvegicus
-
pH not specified in the publication, temperature not specified in the publication
0.00021
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00056
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)benzamide
Rattus norvegicus
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)methanesulfonamide
Rattus norvegicus
-
-
0.0028
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)propanamide
Rattus norvegicus
-
-
0.00047
N-(2-[2-[(3,4-dichlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)thiophene-3-carboxamide
Rattus norvegicus
-
-
0.00027
N-(2-[2-[(3,4-dichlorophenyl)amino]-7-oxo-6-(4-pyridin-3-ylphenyl)pteridin-8(7H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00075
N-(2-[2-[(3-chloro-4-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0013
N-(2-[2-[(3-chlorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0009
N-(2-[2-[(4-chloro-3-fluorophenyl)amino]-6-(4-methoxyphenyl)-7-oxopteridin-8(7H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000549
N-(2-[6-[(2-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000012
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2,2-dimethyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00022
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00008
N-(2-[6-[(3,4-dichlorobenzyl)amino]-2-methyl-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.0000014
N-(2-[6-[(3,4-dichlorobenzyl)amino]-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]ethyl)-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00466
N-(2-[6-[(3-chloro-4-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000376
N-(2-[6-[(3-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0176
N-(2-[6-[(3-fluorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00076
N-(2-[6-[(3-methoxybenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0000078
N-(2-[6-[(4-chlorobenzyl)amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.00011
N-(2-[7-[(3,4-dichlorobenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.000026
N-(2-[7-[(3,4-dimethylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0000005
N-(2-[7-[(4-fluoro-3-methylbenzyl)amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl)acetamide
Rattus norvegicus
-
-
0.0216
N-(3-methylbutyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00386
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000434
N-(3-methylbutyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.1
N-(3-phenylpropyl)-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.682
N-(4-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.02 - 2
N-(5-carbamoyl-1,3-thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.204
N-(6,7-dihydro-4H-pyrano[4,3-d][1,3]thiazol-2-yl)-4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0166
N-(cyclopropylmethyl)-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000099
N-(thiophen-2-ylmethyl)-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00093
N-methoxy-3-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]propanamide
Rattus norvegicus
-
-
0.002
N-methyl-2-(4-[[2-(trifluoromethyl)phenyl]carbonyl]piperazin-1-yl)-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
-
0.0272
N-methyl-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000136
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)benzoyl]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000142
N-[(5-chlorothiophen-2-yl)methyl]-2-[4-[2-(trifluoromethyl)phenoxy]phenyl]-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00221
N-[(5-chlorothiophen-2-yl)methyl]-3-(5-[hydroxy[2-(trifluoromethyl)phenyl]methyl]-1H-benzimidazol-2-yl)benzamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00037
N-[2-(5-chlorothiophen-2-yl)ethyl]-2-(4-phenoxyphenyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00033
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
Rattus norvegicus
-
-
0.01379
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
Rattus norvegicus
-
-
0.00026
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
Rattus norvegicus
-
-
0.000206
N-[2-[2-(4-methoxyphenyl)-3-oxo-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00205
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
Rattus norvegicus
-
-
0.00038
N-[2-[2-(4-methoxyphenyl)-6-[(3-methylbenzyl)amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.03
N-[2-[2-(4-methoxyphenyl)-6-[[(5-methylisoxazol-3-yl)methyl]amino]-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
IC50 above 0.03 mM
0.000168
N-[2-[2-oxo-3-pyridin-3-yl-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000056
N-[2-[3-(4-ethylphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000025
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-([[4-(trifluoromethyl)pyridin-2-yl]methyl]amino)quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000093
N-[2-[3-(4-methoxyphenyl)-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000018
N-[2-[3-(4-methoxyphenyl)-7-[(3-methylbenzyl)amino]-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000261
N-[2-[3-methyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0014
N-[2-[3-oxo-2-pyridin-3-yl-6-[[3-(trifluoromethyl)benzyl]amino]pyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0028
N-[2-[3-tert-butyl-2-oxo-7-[[3-(trifluoromethyl)benzyl]amino]quinoxalin-1(2H)-yl]ethyl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00084
N-[2-[6-(benzylamino)-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00148
N-[2-[6-[[2-fluoro-5-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000217
N-[2-[6-[[3,5-bis(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.00002
N-[2-[6-[[4-fluoro-3-(trifluoromethyl)benzyl]amino]-2-(4-methoxyphenyl)-3-oxopyrido[2,3-b]pyrazin-4(3H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.0000006
N-[2-[7-[[4-chloro-3-(trifluoromethyl)benzyl]amino]-3-(4-methoxyphenyl)-2-oxoquinoxalin-1(2H)-yl]ethyl]acetamide
Rattus norvegicus
-
-
0.000208
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.000261
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.000268
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
Rattus norvegicus
-
-
0.0116
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-3-hydroxypropanamide
Rattus norvegicus
-
-
0.00386
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]acetamide
Rattus norvegicus
-
-
0.000348
N-[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00269
N-[3-(3-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00258
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00117
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00797
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-phenoxyacetamide
Rattus norvegicus
-
-
0.00312
N-[3-(4-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-7-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00385
N-[3-(biphenyl-3-ylmethyl)-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00019
N-[3-[4-chloro-3-(trifluoromethyl)benzyl]-4-oxo-3,4-dihydroquinazolin-6-yl]-2-hydroxyacetamide
Rattus norvegicus
-
-
0.00012
Sterculic acid
Rattus norvegicus
-
in 150 mM KCl, 40 mM NaF, 100 mM sodium phosphate buffer, pH 7.4, at 37°C
0.1
[2-(biphenyl-4-yl)-1H-benzimidazol-5-yl](phenyl)methanone
Rattus norvegicus
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.0158
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl](phenyl)methanone
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000082
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0133
[2-[4-(benzyloxy)phenyl]-1H-benzimidazol-5-yl][2-(trifluoromethyl)phenyl]methanone
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000001
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
0.1
[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl][2-(trifluoromethyl)phenyl]methanone
Rattus norvegicus
-
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.0000023
[5-(6-[3-[2-(trifluoromethyl)phenoxy]azetidin-1-yl]pyridazin-3-yl)-1,3,4-oxadiazol-2-yl]methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.00089
[[3-(3,4-dichlorobenzyl)-4-oxo-3,4-dihydroquinazolin-6-yl]amino](oxo)acetic acid
Rattus norvegicus
-
-
0.000115
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000212
2-[4-(2-chlorophenoxy)phenyl]-N-(1,3-thiazol-2-ylmethyl)-1H-benzimidazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000106
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000106
2-[4-[2-(trifluoromethyl)benzoyl]piperazin-1-yl]-1,3-thiazole-5-carboxamide
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.0000023
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000023
3-(5-methyl-1,3,4-thiadiazol-2-yl)-6-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]pyridazine
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
0.000026
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.026
4-(6-fluoro-2,3-dihydro-1H-indol-1-yl)-N-(4-methyl-1,3-thiazol-2-yl)piperidine-1-carboxamide
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000001
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000001
[3-(2-[4-[2-(trifluoromethyl)phenoxy]piperidin-1-yl]-1,3-thiazol-5-yl)-1,2,4-oxadiazol-5-yl]methanol
Rattus norvegicus
-
rat liver microsomal enzyme assay, pH not specified in the publication, temperature not specified in the publication
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
additional information
additional information
Sprague-Dawley rats are food restricted at 50% of their spontaneous food intake for 2 weeks and than are refeeded, enzyme activity is significantly elevated at the end of 2 weeks of semistarvation, +72%, and remains higher on day 7 of refeeding, +44%
additional information
-
maximal activity at a concentration of 0.03 mM stearoyl-CoA
additional information
-
enzyme activity decreases by 50% in the liver after treatment with Scd1 sequence-specific antisense oligodeoxynucleotide compared with animals treated with scrambled antisense oligodeoxynucleotide
additional information
-
long-term glucose oversupply induces rapid increase in SCD expression and enzyme activity
additional information
-
short time (3 weeks) of sucrose feeding decreases mRNA level and enzyme activity, whereas long term (6 months) of sucrose feeding increases enzyme activity and mRNA level
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
7.2
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
30
ORGANISM
COMMENTARY
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
SOURCE
additional information
-
decreased mRNA levels in epididymal fat pads after 2 injections of Scd1 sequence-specific antisense oligodeoxynucleotide over 5 days
-
-
437644, 437645, 437647, 437648, 437649, 437654, 437655, 437657, 437658, 437662, 437664, 695566, 696680, 696683, 696690, 697777, 697824, 701423, 716200, 727140, 734115
-
mRNA decreased by 80% following 2 injections of Scd1 sequence-specific antisense oligodeoxynucleotide over 5 days, real-time PCR
-
increased relative expression level in obese insulin-resistent ZDF rats compared to lean insulin-sensitive rats
-
long-term glucose oversupply induces rapid increase in SCD expression and enzyme activity
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY
GeneOntology No.
LITERATURE
SOURCE
additional information
-
in L6GLUT4myc myoblasts localized in endoplasmic reticulum-like subcellular structures, laser scanning microscopy
-
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable).
The reliability class of the localization prediction ranges from 1 (very reliable) to 5 (not reliable). ACOD1_RAT
358
4
41467
Swiss-Prot
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
53000
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
phospholipoprotein
phospholipoprotein
-
tightly bound phospholipid is removed during purification
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY
LITERATURE
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
STORAGE STABILITY
ORGANISM
UNIPROT
LITERATURE
4°C, microsomes, 24 hours, inhibition of desaturase by the cytosolic fraction rather than stimulation
-
enzyme cannot be stored overnight without loss of 20-50% of activity before fraction 5
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
ammonium sulfate precipitation, gel filtration, ultra filtration, ion-exchange
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in L6GLUT4myc myoblasts, localized in endoplasmic reticulum-like subcellular structures, laser scanning microscopy
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
chronic food restriction and chronic food restriction/refeeding cause increased expression
-
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Oshino, N.; Imai, Y.; Sato, R.
A function of cytochrome b5 in fatty acid desaturation by rat liver microsomes
J. Biochem.
69
155-167
1971
Rattus norvegicus
Strittmatter, P.; Spatz, L.; Corcoran, D.; Rogers, M.J.; Setlow, B.; Redline, R.
Purification and properties of rat liver microsomal stearyl coenzyme A desaturase
Proc. Natl. Acad. Sci. USA
71
4565-4569
1974
Rattus norvegicus, Rattus norvegicus Long-Evans
Jones, D.P.; Gaylor, J.L.
A non-substrate-binding protein that stimulates microsomal stearyl-CoA desaturase
Methods Enzymol.
71
258-263
1981
Rattus norvegicus
Strittmatter, P.; Enoch, H.G.
Purification of stearyl-CoA desaturase from liver
Methods Enzymol.
52
188-193
1978
Rattus norvegicus, Rattus norvegicus Long-Evans
Fujiwara, Y.; Okayasu, T.; Ishibashi, T.; Imai, Y.
Immunochemical evidence for the enzymatic difference of DELTA6-desaturase from DELTA9- and DELTA5-desaturase in rat liver microsomes
Biochem. Biophys. Res. Commun.
110
36-41
1983
Rattus norvegicus
Scott, W.; Foote, J.L.
The inhibition of stearoyl-coenzyme A desaturase by phenyllactate and phenylpyruvate
Biochim. Biophys. Acta
573
197-200
1979
Rattus norvegicus
Jeffcoat, R.; Brawn, P.R.; Safford, R.; James, A.T.
Properties of rat liver microsomal stearoyl-coenzyme A desaturase
Biochem. J.
161
431-437
1977
Rattus norvegicus
Jeffcoat, R.
The physiological role and control of mammalian fatty acyl-coenzyme A desaturases
Biochem. Soc. Trans.
5
811-818
1977
Gallus gallus, Rattus norvegicus
Prasad, M.R.; Joshi, V.C.
Purification and properties of hen liver microsomal terminal enzyme involved in stearoyl coenzyme A desaturation and its quantitation in neonatal chicks
J. Biol. Chem.
254
6362-6369
1979
Gallus gallus, Rattus norvegicus
Oshino, N.; Imai, Y.; Sato, R.
Electron-transfer mechanism associated with fatty acid desaturation catalyzed by liver microsomes
Biochim. Biophys. Acta
128
13-27
1966
Rattus norvegicus
Trueman, R.J.; Tiku, P.E.; Caddick, M.X.; Cossins, A.R.
Thermal thresholds of lipid restructuring and DELTA9-desaturase expression in the liver of carp (Cyprinus carpio L.)
J. Exp. Biol.
203
641-650
2000
Cyprinus carpio, Rattus norvegicus, Cyprinus carpio L.
Mziaut, H.; Korza, G.; Elkahloun, A.G.; Ozols, J.
Induction of stearoyl CoA desaturase is associated with high-level induction of emerin RNA
Biochem. Biophys. Res. Commun.
282
910-915
2001
Cricetinae, Rattus norvegicus
Voss, M.D.; Beha, A.; Tennagels, N.; Tschank, G.; Herling, A.W.; Quint, M.; Gerl, M.; Metz-Weidmann, C.; Haun, G.; Korn, M.
Gene expression profiling in skeletal muscle of Zucker diabetic fatty rats: implications for a role of stearoyl-CoA desaturase 1 in insulin resistance
Diabetologia
48
2622-2630
2005
Rattus norvegicus
Mainieri, D.; Summermatter, S.; Seydoux, J.; Montani, J.P.; Rusconi, S.; Russell, A.P.; Boss, O.; Buchala, A.J.; Dulloo, A.G.
A role for skeletal muscle stearoyl-CoA desaturase 1 in control of thermogenesis
FASEB J.
20
1751-1753
2006
Rattus norvegicus (P07308)
Gutierrez-Juarez, R.; Pocai, A.; Mulas, C.; Ono, H.; Bhanot, S.; Monia, B.P.; Rossetti, L.
Critical role of stearoyl-CoA desaturase-1 (SCD1) in the onset of diet-induced hepatic insulin resistance
J. Clin. Invest.
116
1686-1695
2006
Mus musculus, Rattus norvegicus, Mus musculus C57/BL6J
Dobrzyn, A.; Dobrzyn, P.
Stearoyl-CoA desaturase - a new player in skeletal muscle metabolism regulation
J. Physiol. Pharmacol.
57 Suppl 10
31-42
2006
Mus musculus, Rattus norvegicus, Sus scrofa
Toyama, T.; Kudo, N.; Mitsumoto, A.; Hibino, Y.; Tsuda, T.; Kawashima, Y.
Stearoyl-CoA desaturase activity is elevated by the suppression of its degradation by clofibric acid in the liver of rats
J. Pharmacol. Sci.
103
383-390
2007
Rattus norvegicus (P07308), Rattus norvegicus (Q6P7B9)
Soulard, P.; McLaughlin, M.; Stevens, J.; Connolly, B.; Coli, R.; Wang, L.; Moore, J.; Kuo, M.S.; LaMarr, W.A.; Ozbal, C.C.; Bhat, B.G.
Development of a high-throughput screening assay for stearoyl-CoA desaturase using rat liver microsomes, deuterium labeled stearoyl-CoA and mass spectrometry
Anal. Chim. Acta
627
105-111
2008
Rattus norvegicus
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
Homo sapiens, Rattus norvegicus
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
Homo sapiens, Rattus norvegicus
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
Li, C.S.; Belair, L.; Guay, J.; Murgasva, R.; Sturkenboom, W.; Ramtohul, Y.K.; Zhang, L.; Huang, Z.
Thiazole analog as stearoyl-CoA desaturase 1 inhibitor
Bioorg. Med. Chem. Lett.
19
5214-5217
2009
Rattus norvegicus
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
Homo sapiens, Rattus norvegicus
Dobrzyn, A.; Dobrzyn, P.
Inhibition of stearoyI-CoA desaturase by cyclic amine derivatives
Expert Opin. Ther. Pat.
18
457-460
2008
Homo sapiens, Rattus norvegicus
-
Liu, G.
Stearoyl-CoA desaturase inhibitors: update on patented compounds
Expert Opin. Ther. Pat.
19
1169-1191
2009
Homo sapiens, Rattus norvegicus
Reh, R.; Ozols, J.; Clement, B.
Involvement of stearoyl-CoA desaturase in the reduction of amidoxime prodrugs
Xenobiotica
38
1177-1190
2008
Rattus norvegicus, Sus scrofa
Green, C.; Olson, L.
Modulation of palmitate-induced endoplasmic reticulum stress and apoptosis in pancreatic beta-cells by stearoyl-CoA desaturase and Elovl6
Am. J. Physiol. Endocrinol. Metab.
300
640-649
2011
Rattus norvegicus
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
Homo sapiens, Rattus norvegicus
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
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
Homo sapiens, Rattus norvegicus
Su, C.; Gullberg, H.; Simko, H.; Luthman, M.; Edlund, P.O.; Lundbaeck, T.
A novel assay of cellular stearoyl-CoA desaturase activity of primary rat hepatocytes by HPLC
J. Chromatogr. B
878
2427-2432
2010
Rattus norvegicus
Turyn, J.; Stojek, M.; Swierczynski, J.
Up-regulation of stearoyl-CoA desaturase 1 and elongase 6 genes expression in rat lipogenic tissues by chronic food restriction and chronic food restriction/refeeding
Mol. Cell. Biochem.
345
181-188
2010
Rattus norvegicus
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
Matter, H.; Zoller, G.; Herling, A.W.; Sanchez-Arias, J.A.; Philippo, C.; Namane, C.; Kohlmann, M.; Pfenninger, A.; Voss, M.D.
Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization
Bioorg. Med. Chem. Lett.
23
1817-1822
2013
Rattus norvegicus
Yang, S.M.; Tang, Y.; Zhang, R.; Lu, H.; Kuo, G.H.; Gaul, M.D.; Li, Y.; Ho, G.; Conway, J.G.; Liang, Y.; Lenhard, J.M.; Demarest, K.T.; Murray, W.V.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: urea-based analogs
Bioorg. Med. Chem. Lett.
23
6773-6776
2013
Rattus norvegicus
Yang, S.M.; Tang, Y.; Rano, T.; Lu, H.; Kuo, G.H.; Gaul, M.D.; Li, Y.; Ho, G.; Lang, W.; Conway, J.G.; Liang, Y.; Lenhard, J.M.; Demarest, K.T.; Murray, W.V.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: Part 2. Pyridazine-based analogs
Bioorg. Med. Chem. Lett.
24
1437-1441
2014
Rattus norvegicus
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