onternabez [Ligand Id: 746] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL497392 (HU-308) |
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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 | Binding affinity to CB1 receptor | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Binding affinity to cannabinoid CB1 receptor | B | 5 | pKi | >=10000 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 5 | pKi | 10000 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | 25.1 | nM | Ki | Proc Natl Acad Sci USA (1999) 96: 14228-33 [PMID:10588688] |
| ChEMBL | Binding affinity to CB2 receptor | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2009) 52: 369-378 [PMID:19143566] |
| ChEMBL | Binding affinity to cannabinoid CB2 receptor | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2010) 53: 4332-4353 [PMID:20218623] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 7.64 | pKi | 22.7 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in HEK293 cell membranes assessed as induction of [35S]-GTPgammaS binding after 60 mins by liquid scintillation spectrometric method | F | 7.19 | pEC50 | 64.5 | nM | EC50 | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Displacement of [3H]HU-243 from rat CB2 receptor expressed in African green monkey COS7 cell membranes after 90 mins | B | 7.64 | pKi | 22.7 | nM | Ki | J Med Chem (2016) 59: 6753-6771 [PMID:27309150] |
| glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | 1100 | nM | IC50 | |
| glycine receptor α3 subunit in Human [GtoPdb: 425] [UniProtKB: O75311] | ||||||||
| GtoPdb | - | - | 7 | pIC50 | 97 | nM | IC50 | |
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]
