Bookmark and Share
BioAssay: AID 636765

Displacement of [3H]E2 from human recombinant ERalpha after 1 hr by liquid scintillation counting relative to estradiol

E2 deficiency in elderly people has directly an effect on the skeleton and can lead to osteoporosis. As 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) catalyses the conversion between active 17beta-hydroxysteroid estradiol (E2) and testosterone (T) into their less active 17-ketosteroid and has been found in bones, 17beta-HSD2 inhibitor may provide a new approach in the onset of more ..
_
   
 Tested Compounds
 Tested Compounds
All(8)
 
 
Unspecified(8)
 
 
 Tested Substances
 Tested Substances
All(8)
 
 
Unspecified(8)
 
 
 Related BioAssays
 Related BioAssays
AID: 636765
Data Source: ChEMBL (794213)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-11-17

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Estrogen receptor; Short=ER; AltName: Full=ER-alpha; AltName: Full=Estradiol receptor; AltName: Full=Nuclear receptor subfamily 3 group A member 1
Description ..   
Protein Family: Ligand binding domain of Estrogen receptor, which are activated by the hormone 17beta-estradiol (estrogen)
Comment ..   

Gene:ESR1     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Discovery of a new class of bicyclic substituted hydroxyphenylmethanones as 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) inhibitors for the treatment of osteoporosis.

Abstract: E2 deficiency in elderly people has directly an effect on the skeleton and can lead to osteoporosis. As 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) catalyses the conversion between active 17beta-hydroxysteroid estradiol (E2) and testosterone (T) into their less active 17-ketosteroid and has been found in bones, 17beta-HSD2 inhibitor may provide a new approach in the onset of osteoporosis. Bicyclic substituted hydroxyphenylmethanone derivatives were synthesised as steroidomimetics of the substrate E2 and were evaluated for their 17beta-HSD2 inhibition and their selectivity toward 17beta-HSD1, catalysing the reverse reaction the conversion of estrone (E1) into E2. Highly selective compounds (11, 12, 14, 21 and 22) have been identified, the most promising one (12) showing an IC(50) value in the low nanomolar range (101#nM) and a selectivity factor of 13 toward 17beta-HSD1. These results make compound 12 an interesting candidate for further biological evaluation.
(PMID: 21945251)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 19

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1RBA activity commentRBA activity commentString
2RBA standard flagRBA standard flagInteger
3RBA qualifierRBA qualifierString
4RBA published valueRBA published valueFloat%
5RBA standard valueRBA standard valueFloat%

Data Table (Concise)
Classification
PageFrom: