Binding affinity to human CCR6 receptor - BioAssay Summary
A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 470290
Data Source: ChEMBL (621153)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2013-05-12

Data Table (Complete):           All
Target
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Sequence: RecName: Full=C-C chemokine receptor type 6; Short=C-C CKR-6; Short=CC-CKR-6; Short=CCR-6; AltName: Full=Chemokine receptor-like 3; Short=CKR-L3; AltName: Full=DRY6; AltName: Full=G-protein coupled receptor 29; AltName: Full=GPR-CY4; Short=GPRCY4; AltName: Full=LARC receptor; AltName: CD_antigen=CD196
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx
Comment ..   

Gene:CCR6     Related Protein 3D Structures
Tested Compound:
Description:
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Title: Spiropiperidine CCR5 antagonists.

Abstract: A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed.
(PMID: 19674898)
Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 100432

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatnM
6IC50 standard valueIC50 standard valueFloatnM
* Activity Concentration.

Data Table (Concise)
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Classification
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