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BioAssay: AID 480270

Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay

The application of frontal affinity chromatography-mass spectrometry (FAC-MS), along with molecular modeling studies, to the screening of potential drug candidates toward the recently deorphanized G-protein-coupled receptor (GPCR) GPR17 is shown. GPR17 is dually activated by uracil nucleotides and cysteinyl-leukotrienes, and is expressed in organs typically undergoing ischemic damage (i.e., more ..
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 Tested Compounds
 Tested Compounds
All(6)
 
 
Active(6)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(6)
 
 
AID: 480270
Data Source: ChEMBL (631133)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Uracil nucleotide/cysteinyl leukotriene receptor; Short=UDP/CysLT receptor; AltName: Full=G-protein coupled receptor 17; AltName: Full=P2Y-like receptor; AltName: Full=R12
Description ..   
Comment ..   

Gene:GPR17     Conserved Domain     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 6
Description:
Title: Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.

Abstract: The application of frontal affinity chromatography-mass spectrometry (FAC-MS), along with molecular modeling studies, to the screening of potential drug candidates toward the recently deorphanized G-protein-coupled receptor (GPCR) GPR17 is shown. GPR17 is dually activated by uracil nucleotides and cysteinyl-leukotrienes, and is expressed in organs typically undergoing ischemic damage (i.e., brain, heart and kidney), thus representing a new pharmacological target for acute and chronic neurodegeneration. GPR17 was entrapped on an immobilized artificial membrane (IAM), and this stationary phase was used to screen a library of nucleotide derivatives by FAC-MS to select high affinity ligands. The chromatographic results have been validated with a reference functional assay ([(35)S]GTPgammaS binding assay). The receptor nucleotide-binding site was studied by setting up a column where a mutated GPR17 receptor (Arg255Ile) has been immobilized. The chromatographic behavior of the tested nucleotide derivatives together with in silico studies have been used to gain insights into the structure requirement of GPR17 ligands.
(PMID: 20394377)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Assay Test Type: In vitro
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6EC50 activity commentEC50 activity commentString
7EC50 standard flagEC50 standard flagInteger
8EC50 qualifierEC50 qualifierString
9EC50 published valueEC50 published valueFloatnM
10EC50 standard valueEC50 standard valueFloatnM
11EC50 binding domainsEC50 binding domainsString
12EC50 activity commentEC50 activity commentString
13EC50 standard flagEC50 standard flagInteger
14EC50 qualifierEC50 qualifierString
15EC50 published valueEC50 published valueFloatpM
16EC50 standard valueEC50 standard valueFloatnM
17EC50 binding domainsEC50 binding domainsString
18EC50 activity commentEC50 activity commentString
19EC50 standard flagEC50 standard flagInteger
20EC50 qualifierEC50 qualifierString
21EC50 published valueEC50 published valueFloatμM
22EC50 standard valueEC50 standard valueFloatnM
23EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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