AM281 [Ligand Id: 741] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL476833 (AM-281) |
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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 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting | B | 6.37 | pKi | 422 | nM | Ki | Eur J Med Chem (2009) 44: 593-608 [PMID:18511157] |
| ChEMBL | Antagonist activity at CB1 receptor (unknown origin) | B | 7.88 | pKi | 13.24 | nM | Ki | Med Chem Res (2013) 22: 4133-4145 |
| ChEMBL | Antagonist activity at CB1 receptor (unknown origin) | B | 7.88 | pKi | 13.2 | nM | Ki | Med Chem Res (2013) 22: 4133-4145 |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| GtoPdb | - | - | 7.9 | pKi | 12.6 | nM | Ki | AAPS PharmSci (1999) 1: E4 [PMID:11741201] |
| ChEMBL | Displacement of [3H]CP-55940 from cannabinoid CB1 receptor in rat brain cortical membrane | B | 7.91 | pKi | 12.4 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| ChEMBL | Binding affinity was determined by using a competition assay with [125 I]- AM251 against rat cannabinoid receptor 1 | B | 8.35 | pKi | 4.5 | 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 | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in HEK293 cells | B | 5.38 | pKi | 4200 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Binding affinity to rat spleen cannabinoid CB2 receptor | B | 5.38 | pKi | 4200 | nM | Ki | Bioorg Med Chem (2009) 17: 2842-2851 [PMID:19278853] |
| GPR55/G-protein coupled receptor 55 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075322] [GtoPdb: 109] [UniProtKB: Q9Y2T6] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 |
Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302]; Br J Pharmacol (2010) 160: 604-14 [PMID:20136841] |
| 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 | 4.87 | pEC50 | 13600 | nM | EC50 | Medchemcomm (2014) 5: 632-649 |
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]
