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

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ChEMBL ligand: CHEMBL120526 (Methanandamide, (R)-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/Potassium channel subfamily K member 3 in Human [ChEMBL: CHEMBL2321613] [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/Potassium channel subfamily K member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
GtoPdb - - 6.15 pIC50 ~700 nM IC50 EMBO J (2001) 20: 47-54 [PMID:11226154]
ChEMBL Inhibition of human TASK1 expressed in African green monkey COS cells by whole cell patch clamp assay B 7 pIC50 100 nM IC50 J Med Chem (2019) 62: 10044-10058 [PMID:31260312]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]