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Binding affinity to human CB2 receptor transfected in HEK293 cells

PubChem AID
414287
Primary Citation
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands [PMID: 19230659]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2010-05-26
  • Modify:
    2022-08-30
Description
This bioassay record (AID 414287) reports results from the above primary citation. Additional data from the same publication are reported in a total of 2 BioAssay records in PubChem.

1 Description

Title: Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.

Abstract: A novel series of cannabinoid ligands with a structurally unique tri-aryl core has been designed, synthesized and assayed. Receptor binding assays show that these compounds possess CB2 receptor sub-type selectivity with binding affinities ranging from 1.07 (+/-0.05) for 7 to 4.77 (+/-0.57) nM for 6. The selectivity of the compounds was enhanced 9-600-fold for the CB2 receptor over the CB1 receptor. The results of our present study identify a novel, highly selective cannabinoid scaffold with a non-classical core.

2 Comment

Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: Bioorg Med Chem Lett

Year: 2009

Volume: 19

Issue: 6

First Page: 1691

Last Page: 1693

DOI: 10.1016/j.bmcl.2009.01.100

Target ChEMBL ID: CHEMBL253

ChEMBL Target Name: Cannabinoid CB2 receptor

ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain

Relationship Type: D - Direct protein target assigned

Confidence: Direct single protein target assigned

3 Result Definitions

4 Data Table

5 Target

8 Identity

8.1 BioAssay Name

Binding affinity to human CB2 receptor transfected in HEK293 cells

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2010-05-26

8.7 Modify Date

Version 1.1
Version 2.1
Version 2.2
Version 2.3
Version 2.4
Version 3.1
Version 3.2
Version 3.3
Version 4.1
Version 4.2
Version 5.1
Version 6.1
Version 7.1
Version 7.2
Version 8.1
Version 8.2
Version 8.3
Version 8.4
Version 8.5
Version 9.1
Version 9.2
2022-08-30 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Format
Cell-based
Assay Type
Binding
Assay Cell Type
Assay Organism

11 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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