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BioAssay: AID 703460

Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by TR-FRET based HTRF assay

A series of fluorescent benzazepine ligands for the arginine-vasopressin V# receptor (AVP V#R) was synthesized using "Click" chemistry. Their in vitro pharmacological profile at AVP V#R, V(1a)R, V(1b)R, and oxytocin receptor was measured by binding assay and functional studies. Compound 9p, labeled with Lissamine Rhodamine B using novel solid-phase organic tagging (SPOrT) resin, more ..
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 Tested Compounds
 Tested Compounds
All(16)
 
 
Active(1)
 
 
Inactive(15)
 
 
 Tested Substances
 Tested Substances
All(16)
 
 
Active(1)
 
 
Inactive(15)
 
 
AID: 703460
Data Source: ChEMBL (864204)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-08-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Vasopressin V2 receptor; Short=V2R; AltName: Full=AVPR V2; AltName: Full=Antidiuretic hormone receptor; AltName: Full=Renal-type arginine vasopressin receptor
Description ..   
Comment ..   

Gene:AVPR2     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Selective fluorescent nonpeptidic antagonists for vasopressin V# GPCR: application to ligand screening and oligomerization assays.

Abstract: A series of fluorescent benzazepine ligands for the arginine-vasopressin V# receptor (AVP V#R) was synthesized using "Click" chemistry. Their in vitro pharmacological profile at AVP V#R, V(1a)R, V(1b)R, and oxytocin receptor was measured by binding assay and functional studies. Compound 9p, labeled with Lissamine Rhodamine B using novel solid-phase organic tagging (SPOrT) resin, exhibited a high affinity for V#R (4.0 nM), an excellent selectivity toward V#R and antagonist properties. By changing the nature of the dye, DY647 and Lumi4-Tb probes 44 and 47 still display a high affinity for V#R (5.6 and 5.8 nM, respectively). These antagonists constitute the first high-affinity selective nonpeptidic fluorescent ligands for V#R. They enabled the development of V#R time-resolved FRET-based assay readily amenable to high-throughput screening. Taking advantage of their selectivity, these compounds were also successfully involved in the study of V(1a)R-V#R dimerization on cell surface.
(PMID: 22984902)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Functional
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Cell Type: CHO
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat
6Kact activity commentKact activity commentString
7Kact standard flagKact standard flagInteger
8Kact qualifierKact qualifierString
9Kact published valueKact published valueFloatnM
10Kact standard valueKact standard valueFloatnM

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