AM251 [Ligand Id: 3317] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL285932 (AM-251)
  • 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]
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  • GPR18 in Human [GtoPdb: 89] [UniProtKB: Q14330]
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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 Antagonist activity at CB1 receptor (unknown origin) B 8.12 pKi 7.5 nM Ki Med Chem Res (2013) 22: 4133-4145
ChEMBL Binding affinity to cannabinoid CB1 receptor B 8.13 pKi 7.49 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Antagonist activity at CB1 receptor (unknown origin) B 8.13 pKi 7.48 nM Ki Med Chem Res (2013) 22: 4133-4145
ChEMBL Binding affinity to human CB1 receptor B 8.52 pKi 3 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3978-3982 [PMID:17513109]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. (2009) 17: 5549-5564 [PMID:19595596]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 8.64 pKi 2.3 nM Ki Bioorg. Med. Chem. (2008) 16: 7510-7515 [PMID:18579386]
ChEMBL Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells B 8.64 pKi 2.3 nM Ki Eur. J. Med. Chem. (2010) 45: 5878-5886 [PMID:20943290]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2008) 51: 1560-1576 [PMID:18293908]
ChEMBL Displacement of [3H]CP-55940 from human CB1R F170L mutant expressed in CHO cells B 6.47 pIC50 340 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R W279A mutant expressed in CHO cells B 6.72 pIC50 190 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R K192L mutant expressed in CHO cells B 7.22 pIC50 60 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R F200L mutant expressed in CHO cells B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human wild type CB1R expressed in CHO cells B 8.46 pIC50 3.5 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]SR-141716 from human CBR1 S383A mutant expressed in CHO cells B 9.23 pIC50 0.59 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]SR-141716 from human wild type CB1R expressed in CHO cells B 9.49 pIC50 0.32 nM IC50 J. Med. Chem. (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay B 7.15 pEC50 70 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay B 7.17 pEC50 67.61 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4209-4214 [PMID:25096297]
ChEMBL Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP by scintillation counting in presence of CP55940 B 7.24 pEC50 57.54 nM EC50 Bioorg. Med. Chem. (2014) 22: 3938-3946 [PMID:24984935]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
GtoPdb - - 8.1 pKi 7.94 nM Ki J Med Chem (1999) 42: 769-76 [PMID:10052983]
ChEMBL Binding affinity against Cannabinoid receptor 1 in rat forebrain B 8.13 pKi 7.49 nM Ki J. Med. Chem. (1999) 42: 769-776 [PMID:10052983]
ChEMBL Inhibition of [3H]CP-55940 binding to cannabinoid receptor 1 in rat brain membranes. B 8.22 pKi 6 nM Ki J. Med. Chem. (2002) 45: 1447-1459 [PMID:11906286]
ChEMBL Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1 B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2003) 46: 642-645 [PMID:12570386]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Binding affinity to cannabinoid CB2 receptor B 5.64 pKi 2290 nM Ki J. Med. Chem. (2010) 53: 4332-4353 [PMID:20218623]
ChEMBL Displacement of [3H]CP 55940 from human CB2 receptor in cell free system B 6.95 pKi 112.2 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 6.95 pKi 112 nM Ki J. Med. Chem. (2008) 51: 1560-1576 [PMID:18293908]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells B 6.95 pKi 112 nM Ki Bioorg. Med. Chem. (2009) 17: 5549-5564 [PMID:19595596]
ChEMBL Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells B 6.95 pKi 112 nM Ki Eur. J. Med. Chem. (2010) 45: 5878-5886 [PMID:20943290]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells B 6.96 pKi 110 nM Ki Bioorg. Med. Chem. (2008) 16: 7510-7515 [PMID:18579386]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Binding affinity against Cannabinoid receptor 2 in mouse spleen B 5.64 pKi 2290 nM Ki J. Med. Chem. (1999) 42: 769-776 [PMID:10052983]
GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6]
ChEMBL Agonist activity at human GPR55 expressed in HEK293 cells assessed as increase in oscillation Ca2+ transients by fura-2 dye based fluorescence analysis F 6.2 pEC50 630 nM EC50 MedChemComm (2014) 5: 632-649
GtoPdb - - 7.41 pEC50 39 nM EC50 Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302];
Br J Pharmacol (2010) 160: 604-14 [PMID:20136841];
J Biol Chem (2009) 284: 29817-27 [PMID:19723626]
GPR18 in Human [GtoPdb: 89] [UniProtKB: Q14330]
GtoPdb - - 4.02 pEC50 96400 nM EC50 Br J Pharmacol (2012) 165: 2414-24 [PMID:21595653]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]