R-(+)-methanandamide [Ligand Id: 2506] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL120526 ((R)-Methanandamide, Methanandamide)
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
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  • K2P3.1 in Human [GtoPdb: 515] [UniProtKB: O14649]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]CP-55,940 from CB1 receptor in rat brain membranes in absence of FAAH inhibitor PMSF by radioligand binding assay B 7.14 pKi 72 nM Ki J Med Chem (2018) 61: 8639-8657 [PMID:30196704]
ChEMBL Displacement of [3H]CP-55,940 from CB1 receptor in rat brain membranes in presence of FAAH inhibitor PMSF by radioligand binding assay B 7.43 pKi 37 nM Ki J Med Chem (2018) 61: 8639-8657 [PMID:30196704]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the absence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 7.55 pKi 28.3 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Tested for binding affinity to Cannabinoid receptor 1 B 7.7 pKi 20 nM Ki J. Med. Chem. (1999) 42: 896-902 [PMID:10072686]
ChEMBL Displacement of [3H]CP-55940 from Cannabinoid receptor 1 of rat forebrain membranes B 7.7 pKi 20 nM Ki J. Med. Chem. (1996) 39: 4515-4519 [PMID:8893848]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor of rat cerebellar membranes by liquid scintillation counting in presence of serine protease inhibitor PMSF B 7.7 pKi 20 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
GtoPdb - - 7.7 pKi 20 nM Ki J. Med. Chem. (1996) 39: 4515-9 [PMID:8893848]
ChEMBL Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain membrane in presence of phenylmethanesulfonyl fluoride B 7.75 pKi 17.9 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5912-5915 [PMID:18723350]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the presence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 7.75 pKi 17.9 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP-55,940 from human CB2 receptor expressed in HEK293 cell membranes in absence of FAAH inhibitor PMSF by radioligand binding assay B 6.66 pKi 220 nM Ki J Med Chem (2018) 61: 8639-8657 [PMID:30196704]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Displacement of [3H]CP-55,940 from mouse CB2 receptor expressed in HEK293 cell membranes in absence of FAAH inhibitor PMSF by radioligand binding assay B 6 pKi >1000 nM Ki J Med Chem (2018) 61: 8639-8657 [PMID:30196704]
ChEMBL Binding affinity towards Cannabinoid receptor 2 from mouse spleen membranes using 0.8 nM [3H]CP-55940 as radioligand B 6.06 pKi 868 nM Ki J. Med. Chem. (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Displacement of [3H]CP-55940 from cannabinoid CB2 receptor in mouse spleen membrane B 6.06 pKi 868 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5912-5915 [PMID:18723350]
ChEMBL Compound was evaluated for its binding affinity for mouse spleen Cannabinoid receptor 2 B 6.09 pKi 815 nM Ki J. Med. Chem. (1996) 39: 4515-4519 [PMID:8893848]
ChEMBL Binding affinity to mouse spleen CB2 receptor B 6.09 pKi 815 nM Ki J. Med. Chem. (2013) 56: 8224-8256 [PMID:23865723]
K2P3.1 in Human [GtoPdb: 515] [UniProtKB: O14649]
GtoPdb - - 6.15 pIC50 ~700 nM IC50 EMBO J. (2001) 20: 47-54 [PMID:11226154]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]