Inhibition of human GHS-R1a - BioAssay Summary
This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit. ..more
 _
   
 Tested Compounds
 Tested Compounds
All(29)
 
 
Active(29)
 
 
 Tested Substances
 Tested Substances
All(29)
 
 
Active(29)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 468975
Data Source: ChEMBL (619838)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2013-05-12

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Growth hormone secretagogue receptor type 1; Short=GHS-R; AltName: Full=GH-releasing peptide receptor; Short=GHRP; AltName: Full=Ghrelin receptor
Description ..   
Comment ..   

Gene:GHSR     Conserved Domain     Related Protein 3D Structures
BioActive Compounds: 29
Description:
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Title: Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.

Abstract: This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.
(PMID: 19767208)
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: 11536

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
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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