Binding affinity to human CB2 receptor transfected in HEK293 cells
- Deposit:2010-05-26
- Modify:2022-08-30
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.
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
- PubChem
- ChEMBLLICENSEAccess 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