Compounds > jd5037
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jd5037

Description

JD5037: a cannabinoid-1 receptor inverse agonist; structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID66553204
CHEMBL ID2153670
SCHEMBL ID15451761
SCHEMBL ID17748178
SCHEMBL ID21804892
SCHEMBL ID22925180
MeSH IDM0580170

Synonyms (33)

Synonym
bdbm50392283
CHEMBL2153670 ,
S6735
SCHEMBL15451761
jd-5037
SCHEMBL17748178
unii-enz75dg2z6
CS-6325
HY-18697
1392116-14-1
jd5037
(s)-2-((z)-(((s)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1h-pyrazol-1-yl)(4-chlorophenylsulfonamido)methylene)amino)-3-methylbutanamide
(s)-2-((((s)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1h-pyrazol-1-yl)(4-chlorophenylsulfonamido)methylene)amino)-3-methylbutanamide
BCP23654
jd-5037; jd 5037
SCHEMBL21804892
EX-A2516
(s)-2-(((e)-((s)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1h-pyrazol-1-yl)((4-chlorophenyl)sulfonamido)methylene)amino)-3-methylbutanamide
ENZ75DG2Z6 ,
butanamide, 2-((((4s)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1h-pyrazol-1-yl)(((4-chlorophenyl)sulfonyl)amino)methylene)amino)-3-methyl-, (2s)-
crb-4001
bdbm286106
us9517228, example 4 (2s,4's)
(2s)-2-[[[(4s)-5-(4-chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-[(4-chlorophenyl)sulfonylamino]methylidene]amino]-3-methylbutanamide
jd 5037
MS-30319
gtpl10690
SCHEMBL22925180
A904239
(s)-2-((z)-(((s)-3-(4-chlorophenyl)-4-phenyl-4,5-dihydro-1h-pyrazol-1-yl)(4-chlorophenylsulfonamido)methylene)amino)-3-methylbutanamide;jd5037
DTXSID301030409
AC-36112
AKOS040758590

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Cannabinoid receptor 1Homo sapiens (human)IC500.0005AID690736
Cannabinoid receptor 2 Homo sapiens (human)IC501.0000AID690737
Cannabinoid receptor 1Mus musculus (house mouse)IC501.0000AID690737

Bioassays (6)

Assay IDTitleYearJournalArticle
AID690746In vivo receptor occupancy at CB1 receptor in mouse hippocampus assessed as inhibition of [3H]SR141716A binding at 3 mg/kg, po for 3 days measured after 1 hr post last dose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
AID690737Displacement of 3[H]ligand from recombinant human CB2 receptor2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
AID690748In vivo receptor occupancy at CB1 receptor in mouse cerebellum assessed as inhibition of [3H]SR141716A binding at 3 mg/kg, po for 3 days measured after 1 hr post last dose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
AID690736Displacement of 3[H]ligand from recombinant human CB1 receptor2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
AID690747In vivo receptor occupancy at CB1 receptor in mouse hippocampus assessed as inhibition of [3H]SR141716A binding at 30 mg/kg, po for 3 days measured after 1 hr post last dose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
AID690749In vivo receptor occupancy at CB1 receptor in mouse cerebellum assessed as inhibition of [3H]SR141716A binding at 30 mg/kg, po for 3 days measured after 1 hr post last dose2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
ISSN: 1464-3405		JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's11 (91.67)24.3611
2020's1 (8.33)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
sr141716
1
amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist		2012201212.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
losartan
1
biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist		2014201410.0low000010
cyclohexanol
1
cyclohexanols;
secondary alcohol		solvent202120213.0low000001
sr141716
3
amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles		anti-obesity agent;
appetite depressant;
CB1 receptor antagonist		201320217.3medium000021
angiotensin ii
1
amino acid zwitterion;
angiotensin II		human metabolite2014201410.0low000010
cocaine
1
benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid		adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic		2013201311.0low000010
3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol
1
alkylbenzene;
ring assembly		202120213.0low000001
glyceryl 2-arachidonate
2
2-acylglycerol 20:4;
endocannabinoid		human metabolite201620196.5medium000020
arachidonyl-2-chloroethylamide
1
fatty amide;
organochlorine compound;
secondary carboxamide;
synthetic cannabinoid		CB1 receptor agonist;
CB2 receptor agonist;
neuroprotective agent		2014201410.0low000010
slv 319
1
2012201212.0low000010
neuropeptide y
1
201720177.0low000010
piperidines
2
201320169.5medium000020
am6545
1
2013201311.0low000010
leptin
2
201220179.5medium000020
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acquired Metabolic Diseases, Brain0
1
2012201212.0low000010
Albuminuria0
1
201820186.0low000010
Alcohol Abuse0
1
201920195.0low000010
Alcohol Drinking0
2
201920214.0low000011
Alcoholism0
1
201920195.0low000010
Anochlesia0
1
202120213.0low000001
Anxiety0
1
202120213.0low000001
Body Weight0
4
201220179.2low000040
Cirrhosis0
1
201820186.0low000010
Diabetes Mellitus, Adult-Onset0
1
2014201410.0low000010
Diabetes Mellitus, Type 20
1
2014201410.0low000010
Diabetic Glomerulosclerosis0
2
201420188.0low000020
Diabetic Nephropathies0
2
201420188.0low000020
Disease Models, Animal0
1
201620168.0low000010
Diseases, Metabolic0
2
201320169.5low000020
Endotoxemia0
1
202120213.0low000001
Fatty Liver0
2
2012201411.0low000020
Fibrosis0
1
201820186.0low000010
Insulin Resistance0
2
2012201411.0low000020
Insulin Sensitivity0
2
2012201411.0low000020
Labhart-Willi Syndrome0
1
201620168.0low000010
Liver Diseases0
1
2013201311.0low000010
Liver Dysfunction0
1
2013201311.0low000010
Liver Steatosis0
2
2012201411.0low000020
Metabolic Diseases0
2
201320169.5low000020
Obesity0
4
2012201710.0low000040
Prader-Willi Syndrome0
1
201620168.0low000010
Weight Loss0
1
201620168.0low000010
Weight Reduction0
1
201620168.0low000010