Binding affinity to cIAP1/ERalpha in human MCF7 cells assessed as proteasomal degradation of ERalpha at 10 to 30 uM after 6 hrs by Western blot analysis - BioAssay Summary
We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ER## resulting in its proteasomal degradation. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(3)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 646110
Data Source: ChEMBL (803558)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-16

Data Table (Complete):           Active    All
BioActive Compounds: 3
Description:
Helptop of page
Title: Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.

Abstract: We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ER## resulting in its proteasomal degradation.
(PMID: 22277276)
Comment
Helptop of page
Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Multiple direct protein targets may be assigned
Relationship Type: Direct protein target assigned
Categorized Comment
Helptop of page
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 22226

ChEMBL target type: NULL

Result Definitions
Helptop of page
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

Data Table (Concise)
Helptop of page
PageFrom: