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BioAssay: AID 772307

Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay

Title: Discovery of ML314, a Brain Penetrant Non-Peptidic beta-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
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 Tested Compounds
 Tested Compounds
All(47)
 
 
Active(32)
 
 
Unspecified(15)
 
 
 Tested Substances
 Tested Substances
All(47)
 
 
Active(32)
 
 
Unspecified(15)
 
 
AID: 772307
Data Source: ChEMBL (986354)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
Deposit Date: 2014-05-03

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Neurotensin receptor type 1; Short=NT-R-1; Short=NTR1; AltName: Full=High-affinity levocabastine-insensitive neurotensin receptor; AltName: Full=NTRH
Description ..   
Protein Family: Serpentine type 7TM GPCR chemoreceptor Srv
Comment ..   

Gene:NTSR1     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 32
Description:
Title: Discovery of ML314, a Brain Penetrant Non-Peptidic beta-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
(PMID: 24611085)
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

Assay Test Type: In vitro

BAO: Assay Format: cell-based format

Target Type: Target is a single protein chain

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
6EC100 activity commentEC100 activity commentString
7EC100 standard flagEC100 standard flagInteger
8EC100 qualifierEC100 qualifierString
9EC100 published valueEC100 published valueFloatμM
10EC100 standard valueEC100 standard valueFloatμM
11EC50 activity commentEC50 activity commentString
12EC50 standard flagEC50 standard flagInteger
13EC50 qualifierEC50 qualifierString
14EC50 published valueEC50 published valueFloatμM
15EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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