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BioAssay: AID 650868

Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting

To identify potent EP2/EP4 dual agonists with excellent subtype selectivity, a series of I(3)-lactam prostaglandin E analogs bearing a 16-phenyl I ..more
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 Tested Compounds
 Tested Compounds
All(22)
 
 
Active(22)
 
 
 Tested Substances
 Tested Substances
All(22)
 
 
Active(22)
 
 
AID: 650868
Data Source: ChEMBL (808316)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Prostaglandin E2 receptor EP4 subtype; Short=PGE receptor EP4 subtype; Short=PGE2 receptor EP4 subtype; AltName: Full=Prostanoid EP4 receptor
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srx
Comment ..   

Gene:PTGER4     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 22
Description:
Title: Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists.

Abstract: To identify potent EP2/EP4 dual agonists with excellent subtype selectivity, a series of I(3)-lactam prostaglandin E analogs bearing a 16-phenyl I
(PMID: 22386979)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO

Target Type: Target is a single protein chain

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Ki*Ki PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Ki activity commentKi activity commentString
7Ki standard flagKi standard flagInteger
8Ki qualifierKi qualifierString
9Ki published valueKi published valueFloatnM
10Ki standard valueKi standard valueFloatnM
11Ki binding domainsKi binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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