Bookmark and Share
BioAssay: AID 703459

Antagonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as inhibition of AVP-induced 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 ..
_
   
 Tested Compounds
 Tested Compounds
All(15)
 
 
Active(13)
 
 
Unspecified(2)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Active(13)
 
 
Unspecified(2)
 
 
AID: 703459
Data Source: ChEMBL (864203)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
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 Compounds: 13
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
Assay Type: Functional

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO

Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat
6Kinact activity commentKinact activity commentString
7Kinact standard flagKinact standard flagInteger
8Kinact qualifierKinact qualifierString
9Kinact published valueKinact published valueFloatnM
10Kinact standard valueKinact standard valueFloatnM

Data Table (Concise)
Classification
PageFrom: