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| ChEMBL ligand: CHEMBL244403 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CB1 receptor/Cannabinoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Displacement of [3H]-CP55,940 from human CB1 receptor expressed in HEK293 cells | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1619-1624 [PMID:22284817] |
| ChEMBL | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells | B | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| GtoPdb | - | - | 7.46 | pKi | 35 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1619-24 [PMID:22284817] |
| ChEMBL | Displacement of [3H]SR141716A from membrane bound human CB1 receptor after 1 hr by beta scintillation counting method | B | 5.8 | pIC50 | 1580 | nM | IC50 | Bioorg Med Chem (2018) 26: 5069-5078 [PMID:30217464] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as [35S]GTPgamma binding | F | 7.14 | pEC50 | 73 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgamma binding assay | F | 7.14 | pEC50 | 72 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1619-1624 [PMID:22284817] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in HEK293 cells assessed as reversal of forskolin-evoked cAMP accumulation | F | 8.21 | pEC50 | 6.1 | nM | EC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| CB1 receptor/Cannabinoid receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Inhibition of rat CB1 receptor | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| CB2 receptor/Cannabinoid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| GtoPdb | - | - | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1619-24 [PMID:22284817] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 1619-1624 [PMID:22284817] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 7.72 | pKi | 19 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 3884-3889 [PMID:22607668] |
| ChEMBL | Displacement of [3H]CP55940 from membrane bound human CB2 receptor after 1 hr by beta scintillation counting method | B | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem (2018) 26: 5069-5078 [PMID:30217464] |
| ChEMBL | Displacement of [3H]CP-55940 human CB2 receptor expressed in CHOK1 cells | B | 7.01 | pIC50 | 98 | nM | IC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHOK1 cells assessed as reversal of forskolin-evoked cAMP accumulation | F | 7.55 | pEC50 | 27.9 | nM | EC50 | J Med Chem (2007) 50: 3851-3856 [PMID:17630726] |
ChEMBL data shown on this page come from version 36:
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]