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BioAssay: AID 328866

Binding affinity to Pyrococcus horikoshii sodium-coupled aspartate transporter

Secondary transporters are integral membrane proteins that catalyse the movement of substrate molecules across the lipid bilayer by coupling substrate transport to one or more ion gradients, thereby providing a mechanism for the concentrative uptake of substrates. Here we describe crystallographic and thermodynamic studies of Glt(Ph), a sodium (Na+)-coupled aspartate transporter, defining sites more ..
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 Tested Compounds
 Tested Compounds
All(7)
 
 
Active(3)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(7)
 
 
Active(3)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 328866
Data Source: ChEMBL (476892)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-25
Modify Date: 2014-05-14

Data Table ( Complete ):           Active    All
BioActive Compounds: 3
Description:
Title: Coupling substrate and ion binding to extracellular gate of a sodium-dependent aspartate transporter.

Abstract: Secondary transporters are integral membrane proteins that catalyse the movement of substrate molecules across the lipid bilayer by coupling substrate transport to one or more ion gradients, thereby providing a mechanism for the concentrative uptake of substrates. Here we describe crystallographic and thermodynamic studies of Glt(Ph), a sodium (Na+)-coupled aspartate transporter, defining sites for aspartate, two sodium ions and d,l-threo-beta-benzyloxyaspartate, an inhibitor. We further show that helical hairpin 2 is the extracellular gate that controls access of substrate and ions to the internal binding sites. At least two sodium ions bind in close proximity to the substrate and these sodium-binding sites, together with the sodium-binding sites in another sodium-coupled transporter, LeuT, define an unwound alpha-helix as the central element of the ion-binding motif, a motif well suited to the binding of sodium and to participation in conformational changes that accompany ion binding and unbinding during the transport cycle.
(PMID: 17230192)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
2Kd activity commentKd activity commentString
3Kd standard flagKd standard flagInteger
4Kd qualifierKd qualifierString
5Kd published valueKd published valueFloatμM
6Kd standard valueKd standard valueFloatnM
7Kd data validityKd data validityString

* Activity Concentration.

Data Table (Concise)
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