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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 ..
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 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 ):           View Active Data    View All Data
BioActive Compounds: 5
Related Experiments
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AIDNameTypeComment
2703qHTS Assay for Agonists of the Relaxin Receptor RXFP1: SummarySummarydepositor-specified cross reference: Summary AID
2676qHTS Assay for Agonists of the Relaxin Receptor RXFP1Confirmatorysame project related to Summary assay
489012qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 Hit ValidationConfirmatorysame project related to Summary assay
489043qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 Hit ValidationConfirmatorysame project related to Summary assay
492948qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B Hit ValidationConfirmatorysame project related to Summary assay
492949qHTS Assay for Agonists of the Relaxin Receptor RXFP1: THP1 Hit ValidationConfirmatorysame project related to Summary assay
602256qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 SARConfirmatorysame project related to Summary assay
602258qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 SARConfirmatorysame project related to Summary assay
602262qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B SARConfirmatorysame project related to Summary assay
602287qHTS Assay for Agonists of the Relaxin Receptor RXFP1: PBS SolubilityOthersame project related to Summary assay
602288qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Cytotoxicity SARConfirmatorysame project related to Summary assay
602290qHTS Assay for Agonists of the Relaxin Receptor RXFP1: VEGF expressionOthersame project related to Summary assay
602291qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Cell ImpedanceOthersame project related to Summary assay
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)
Data Table ( Complete ):     View Active Data    View All Data
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