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BioAssay: AID 151890

Inhibition of binding of [3H]DAMGO to opioid receptor mu 1 from rat brain membrane.

Piperazinyl benzamidines were prepared and found to bind to the rat delta (delta) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide (27) with a 1.22nM K(i) for the rat delta opioid receptor and ca. 1000 x selectivity relative to the mu opioid subtype. ..more
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 Tested Compounds
 Tested Compounds
All(30)
 
 
Active(16)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(30)
 
 
Active(16)
 
 
Unspecified(14)
 
 
 Related BioAssays
 Related BioAssays
AID: 151890
Data Source: ChEMBL (149137)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2014-05-18

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 16
Description:
Title: Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor.

Abstract: Piperazinyl benzamidines were prepared and found to bind to the rat delta (delta) opioid receptor. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. The most potent among these was N,N-diethyl-4-[4-(phenylmethyl)-1-piperazinyl][2-(trifluoromethyl)phenyl]iminomethyl]benzamide (27) with a 1.22nM K(i) for the rat delta opioid receptor and ca. 1000 x selectivity relative to the mu opioid subtype.
(PMID: 11425550)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 10529
Target Type: SINGLE PROTEIN
Pref Name: Mu opioid receptor
Synonyms: M-OR-1;MOR-1;Mu-type opioid receptor;Opioid receptor B;
Gene Name: Oprm1;Ror-b;
Protein Accession: P33535;
Protein GI: 464314;
Organism: Rattus norvegicus
Tax ID: 10116
Target Classification: membrane receptor 7tm1 peptide short peptide opioid receptor
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatnM
10Ki standard valueKi standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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