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BioAssay: AID 602287

qHTS Assay for Agonists of the Relaxin Receptor RXFP1: PBS Solubility

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(8)
 
 
Inactive(7)
 
 
Inconclusive(1)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Inactive(7)
 
 
Inconclusive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 602287
Data Source: NCGC (RXFB805)
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 All Data
Tested Compounds:
Related Experiments
Show more
AIDNameTypeComment
2703qHTS Assay for Agonists of the Relaxin Receptor RXFP1: SummarySummarydepositor-specified cross reference
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
602286qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Mouse Liver Microsome StabilityOthersame 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 probe and analogs were tested to assess their PBS solubility in this assay.

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

MLPCN Grant: R03 MH085705
Assay Submitter (PI): Alexander Agoulnik
Protocol
1. 8ul of reference and test compound stock solution were added to 392ul 100mM phosphate buffer (pH 7.4)

2. Sample tubes were shaken for 1 hr (1000 rpm) at room temperature

3. Samples were centrifuged (10 min at 12000 rpm) to precipitate un-dissolved particles

4. Supernatants were transferred to new tubes

5. Concentration of the supernatant was determined by LC-UV or LC-MS/MS
Comment
Compounds are "active" if solubility is greater than 20; "inconclusive" if solubility is between 10 and 20; "inactive" if solubility is less than 10.

PUBCHEM_ACTIVITY_SCORE is the solubility rounded to the closet whole number.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1uMPBS solubilityFloatμM
2Compound QCString
Additional Information
Grant Number: MH085705

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