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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
