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]
ChEMBL Antagonist activity at rat forebrain CB1R assessed as inhibition constant B 5.64 pKi 2290 nM Ki RSC Med Chem (2022) 13: 497-510 [PMID:35694688]
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 Antagonist activity at rat forebrain CB1R assessed as inhibition constant B 8.13 pKi 7.49 nM Ki RSC Med Chem (2022) 13: 497-510 [PMID:35694688]
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 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]