AM1241 [Ligand Id: 3316] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL408430 (AM-1241) |
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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 from human CB1 receptor in cell free system | B | 5.3 | pKi | 5000 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Binding affinity to CB1 receptor | B | 5.3 | pKi | 5000 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cell membrane by competitive displacement assay | B | 5.68 | pKi | 2080 | nM | Ki | Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 5.9 | pKi | 1269 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 5.9 | pKi | 1269 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB1 receptor by liquid scintillation counting | B | 6.24 | pKi | 580 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to CB1 receptor | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 5.98 | pEC50 | 1038 | nM | EC50 | Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB1 receptor of rat brain | B | 6.55 | pKi | 280 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHO-K1 cell membrane by competitive displacement assay | B | 7.66 | pKi | 21.8 | nM | Ki | Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197] |
| ChEMBL | Binding affinity to CB2 receptor | B | 7.82 | pKi | 15.1 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 7.94 | pKi | 11.5 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 7.94 | pKi | 11.5 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 7.94 | pKi | 11.5 | 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 HEK293 cells | B | 7.94 | pKi | 11.48 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 7.94 | pKi | 11.48 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| GtoPdb | - | - | 8.1 | pKi | 7.94 | nM | Ki | Br J Pharmacol (2006) 149: 145-54 [PMID:16894349] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor expressed in HEK cells by liquid scintillation counting | B | 8.15 | pKi | 7.1 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to CB2 receptor | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem (2008) 16: 1111-1124 [PMID:18006322] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 7.79 | pEC50 | 16.4 | nM | EC50 | Bioorg Med Chem Lett (2014) 25: 88-91 [PMID:25466197] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from CB2 receptor of mouse spleen membranes | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Inverse agonist activity at rat CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation | F | 6.5 | pEC50 | 315 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Inverse agonist activity at rat CB2 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation | F | 6.67 | pEC50 | 216 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
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]
