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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 ):           All
Tested Compounds:
Depositor Specified Assays
AIDNameTypeComment
2703qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Summarysummary
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)
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