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ChEMBL ligand: CHEMBL285932 (AM-251) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]