Bookmark and Share
BioAssay: AID 602286

qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Mouse Liver Microsome Stability

The relaxin hormone is involved in the variety of biological functions in normal tissues and diseases. The role of relaxin is well-established in female reproduction and parturition, mammary gland and endometrial development, maintenance of myometrial quiescence during pregnancy. Relaxin signaling through its G protein-coupled receptor (GPCR) RXFP1 results in ECM remodeling through regulation of more ..
_
   
 Tested Compounds
 Tested Compounds
All(5)
 
 
Active(5)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Active(5)
 
 
AID: 602286
Data Source: NCGC (RXFP806)
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-03-02
Hold-until Date: 2013-02-02
Modify Date: 2013-02-02

Data Table ( Complete ):           Active    All
BioActive Compounds: 5
Depositor Specified Assays
AIDNameTypeComment
2703qHTS Assay for Agonists of the Relaxin Receptor RXFP1: SummarysummarySummary AID
Description:
The relaxin hormone is involved in the variety of biological functions in normal tissues and diseases. The role of relaxin is well-established in female reproduction and parturition, mammary gland and endometrial development, maintenance of myometrial quiescence during pregnancy. Relaxin signaling through its G protein-coupled receptor (GPCR) RXFP1 results in ECM remodeling through regulation of collagen deposition, cell invasiveness, proliferation and overall tissue homeostasis. Significantly, the therapeutic effects of relaxin in the treatment of renal, cardiac, skin, lung fibrosis, inflammation, and wound healing in animal models are well-established. Recombinant human relaxin (rhRlx) is currently being tested in clinical trials as a protective agent in congestive heart failure, in treating severe preeclampsia, and as an anti-fibrotic agent in systemic sclerosis.

The resulting probe and analogs from this project were tested in this assays, to asses mouse liver microsome stability.

NIH Chemical Genomics Center [NCGC]
NIH Molecular Libraries Probe Production Centers Network [MLPCN]

MLPCN Grant: R03 MH085705
Assay Submitter (PI): Alexander Agoulnik
Protocol
1 uM of compound in incubated in mouse liver microsome; the reference compound is ketanserin. Compounds are incubated at 37 degrees C for different time periods: 0, 5, 15, 30, 45, and 60 minutes. Samples are analyzed with LC-MS/MS.
Comment
Compounds are "active" if half time is more than 30 minutes; "inconclusive" if half time is between 15 and 30 minutes; "inactive" if half time is less than 15 minutes.

PUBCHEM_ACTIVITY_SCORE is the whole number in minutes of T1/2 of the compound. If halftime is above 100 minutes, a score of 100 is assigned.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1HalftimeFloatmin
2Compound QCString
Additional Information
Grant Number: MH085705

Data Table (Concise)
PageFrom: