Inhibition of human ERbeta - BioAssay Summary
A new class of estrogen receptor beta (ERbeta) ligands based on the 6H-chromeno[4,3-b]quinoline scaffold has been prepared. Several C7-substituted analogues displayed high affinity and modest selectivity for ERbeta. ..more
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(21)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(21)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 307630
Data Source: ChEMBL (455656)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2013-05-10

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Steroid hormone receptor ERR2; AltName: Full=ERR beta-2; AltName: Full=Estrogen receptor-like 2; AltName: Full=Estrogen-related receptor beta; Short=ERR-beta; AltName: Full=Nuclear receptor subfamily 3 group B member 2
Description ..   
Protein Family: The ligand binding domain of estrogen receptor-related nuclear receptors
Comment ..   

Gene:ESRRB     Related Protein 3D Structures
BioActive Compounds: 21
Description:
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Title: ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands.

Abstract: A new class of estrogen receptor beta (ERbeta) ligands based on the 6H-chromeno[4,3-b]quinoline scaffold has been prepared. Several C7-substituted analogues displayed high affinity and modest selectivity for ERbeta.
(PMID: 17482813)
Comment
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Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 11254

ChEMBL target type: Target is a single protein chain

Result Definitions
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Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4IC50 activity commentIC50 activity commentString
5IC50 standard flagIC50 standard flagInteger
6IC50 qualifierIC50 qualifierString
7IC50 published valueIC50 published valueFloatnM
8IC50 standard valueIC50 standard valueFloatnM
9IC50 binding domainsIC50 binding domainsString
* Activity Concentration.

Data Table (Concise)
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Classification
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