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BioAssay: AID 414565

Antagonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as decrease in recombinant luteinizing hormone activation potency at 10 uM by c-AMP-mediated luciferase assay

The luteinizing hormone (LH) receptor plays an important role in fertility and certain cancers. The endogenous ligands human chorionic gonadotropin (hCG) and LH bind to the large N terminal domain of the receptor. We recently reported on the first radiolabeled low molecular weight (LMW) agonist for this receptor, [(3)H]Org 43553, which was now used to screen for new LMW ligands. We identified a more ..
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(2)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(2)
 
 
Unspecified(1)
 
 
AID: 414565
Data Source: ChEMBL (562594)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-16

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=LHR; Short=LSH-R; Flags: Precursor
Description ..   
Comment ..   

Gene:LHCGR     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 2
Description:
Title: Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor.

Abstract: The luteinizing hormone (LH) receptor plays an important role in fertility and certain cancers. The endogenous ligands human chorionic gonadotropin (hCG) and LH bind to the large N terminal domain of the receptor. We recently reported on the first radiolabeled low molecular weight (LMW) agonist for this receptor, [(3)H]Org 43553, which was now used to screen for new LMW ligands. We identified a terphenyl derivative that inhibited [(3)H]Org 43553 binding to the receptor, which led us to synthesize a number of derivatives. The most potent compound of this terphenyl series, 24 (LUF5771), was able to increase the dissociation rate of [(3)H]Org 43553 by 3.3-fold (at 10 muM). In a functional assay, the presence of 24 resulted in a 2- to 3-fold lower potency of both Org 43553 and LH. Thus, the compounds presented in this paper are the first LMW ligands that allosterically inhibit the LH receptor.
(PMID: 19296599)
Categorized Comment
Assay Type: Functional

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO-K1

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat
6Fold change activity commentFold change activity commentString
7Fold change standard flagFold change standard flagInteger
8Fold change qualifierFold change qualifierString
9Fold change published valueFold change published valueFloat
10Fold change standard valueFold change standard valueFloat

Data Table (Concise)
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