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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 |
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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 HEK cells | B | 5.9 | pKi | 1258.93 | 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]-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 | Displacement of [3H]CP55940 from CB1 receptor (unknown origin) expressed in CHO cell membrane measured after 90 mins by competitive binding assay | B | 6.24 | pKi | 580 | nM | Ki | J Med Chem (2020) 63: 14448-14469 [PMID:33094613] |
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 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 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 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 | 11.48 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
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] |
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 | Displacement of [3H]CP55940 from CB2 receptor (unknown origin) expressed in HEK cell membrane measured after 90 mins by competitive binding assay | B | 8.15 | pKi | 7 | nM | Ki | J Med Chem (2020) 63: 14448-14469 [PMID:33094613] |
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 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]