Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs relative to nociceptin - BioAssay Summary
A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel. ..more
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 Tested Compounds
 Tested Compounds
All(14)
 
 
Unspecified(14)
 
 
 Tested Substances
 Tested Substances
All(15)
 
 
Unspecified(15)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 472098
Data Source: ChEMBL (622961)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2013-05-12

Data Table (Complete):           All
Target
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Sequence: RecName: Full=Nociceptin receptor; AltName: Full=Kappa-type 3 opioid receptor; Short=KOR-3; AltName: Full=Orphanin FQ receptor
Description ..   
Comment ..   

Gene:OPRL1     Conserved Domain     Related Protein 3D Structures
Tested Compounds:
Description:
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Title: Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.

Abstract: A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.
(PMID: 19818611)
Categorized Comment
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ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 138

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
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Classification
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