AM1241 [Ligand Id: 3316] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL408430 (AM-1241)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • 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]
  • CB2 receptor/Cannabinoid CB2 receptor in Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP 55940 from human CB1 receptor in cell free system B 5.3 pKi 5000 nM Ki Eur J Med Chem (2011) 46: 547-555 [PMID:21183257]
ChEMBL Binding affinity to CB1 receptor B 5.3 pKi 5000 nM Ki J Med Chem (2009) 52: 369-378 [PMID:19143566]
ChEMBL Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cell membrane by competitive displacement assay B 5.68 pKi 2080 nM Ki Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 5.9 pKi 1269 nM Ki J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 5.9 pKi 1269 nM Ki J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 5.9 pKi 1258.93 nM Ki J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells B 5.9 pKi 1258.93 nM Ki J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL Displacement of [3H]-CP55940 from human CB1 receptor by liquid scintillation counting B 6.24 pKi 580 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]CP55940 from CB1 receptor (unknown origin) expressed in CHO cell membrane measured after 90 mins by competitive binding assay B 6.24 pKi 580 nM Ki J Med Chem (2020) 63: 14448-14469 [PMID:33094613]
ChEMBL Binding affinity to CB1 receptor (unknown origin) B 6.55 pKi 280 nM Ki J Med Chem (2013) 56: 7161-7176 [PMID:23672690]
ChEMBL Binding affinity to CB1 receptor B 6.55 pIC50 280 nM IC50 Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322]
ChEMBL Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production F 5.98 pEC50 1038 nM EC50 Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor of rat brain B 6.55 pKi 280 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO-K1 cell membrane by competitive displacement assay B 7.66 pKi 21.8 nM Ki Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197]
ChEMBL Binding affinity to CB2 receptor B 7.82 pKi 15.1 nM Ki J Med Chem (2009) 52: 369-378 [PMID:19143566]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 7.94 pKi 11.5 nM Ki Eur J Med Chem (2011) 46: 547-555 [PMID:21183257]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells B 7.94 pKi 11.5 nM Ki J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells B 7.94 pKi 11.5 nM Ki J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells B 7.94 pKi 11.48 nM Ki J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells B 7.94 pKi 11.48 nM Ki J Med Chem (2010) 53: 295-315 [PMID:19921781]
GtoPdb - - 8.1 pKi 7.94 nM Ki Br J Pharmacol (2006) 149: 145-54 [PMID:16894349]
ChEMBL Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK cells by liquid scintillation counting B 8.15 pKi 7.1 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Displacement of [3H]CP55940 from CB2 receptor (unknown origin) expressed in HEK cell membrane measured after 90 mins by competitive binding assay B 8.15 pKi 7 nM Ki J Med Chem (2020) 63: 14448-14469 [PMID:33094613]
ChEMBL Binding affinity to CB2 receptor (unknown origin) B 8.47 pKi 3.4 nM Ki J Med Chem (2013) 56: 7161-7176 [PMID:23672690]
ChEMBL Binding affinity to CB2 receptor B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR F 5 pEC50 >10000 nM EC50 J Med Chem (2008) 51: 1904-1912 [PMID:18311894]
ChEMBL Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay F 5 pEC50 >10000 nM EC50 J Med Chem (2010) 53: 295-315 [PMID:19921781]
ChEMBL Agonist activity at human CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production F 7.79 pEC50 16.4 nM EC50 Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Displacement of [3H]-CP55940 from CB2 receptor of mouse spleen membranes B 8.47 pKi 3.4 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
ChEMBL Inverse agonist activity at rat CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation F 6.5 pEC50 315 nM EC50 J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
ChEMBL Inverse agonist activity at rat CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation F 6.67 pEC50 216 nM EC50 J Med Chem (2013) 56: 8224-8256 [PMID:23865723]

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]