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BioAssay: AID 306715

Efficacy at LH receptor in Sprague-Dawley rat Leydig cells assessed as production of testosterone after 3 hrs

In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 306715
Data Source: ChEMBL (454741)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-24

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Lutropin-choriogonadotropic hormone receptor; Short=LH/CG-R; AltName: Full=Luteinizing hormone receptor; Short=LSH-R; Flags: Precursor
Description ..   
Comment ..   

Gene:LHCGR     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Identification, synthesis, and biological evaluation of novel pyrazoles as low molecular weight luteinizing hormone receptor agonists.

Abstract: In the course of a high throughput screening, a series of pyrazole compounds were identified with luteinizing hormone receptor (LH-R) agonist activity. A focused pyrazole library was produced by solid-phase synthesis and key pyrazole regioisomers were obtained selectively in solution. Evaluation of those compounds in a cAMP assay in CHO cells transfected with h-LH receptor allowed us to propose a structure-activity relationship model for this series and led to the identification of the first low molecular weight molecule with in vitro activity in a Leydig cells assay (ED(50)=1.31 microM) and in vivo in a model of testosterone induction in rats (significant effect at 32 mpk ip).
(PMID: 17321742)
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: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1ED50*ED50 PubChem standard valueFloatμM
2ED50 activity commentED50 activity commentString
3ED50 standard flagED50 standard flagInteger
4ED50 qualifierED50 qualifierString
5ED50 published valueED50 published valueFloatμM
6ED50 standard valueED50 standard valueFloatnM
7Efficacy activity commentEfficacy activity commentString
8Efficacy standard flagEfficacy standard flagInteger
9Efficacy qualifierEfficacy qualifierString
10Efficacy published valueEfficacy published valueFloat%
11Efficacy standard valueEfficacy standard valueFloat%

* Activity Concentration.

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