LY2828360 [Ligand Id: 12751] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3139186 (Ly2828360, LY-2828360, LY2828360) |
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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 | Agonist activity at human CB1 receptor | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in CHO cells assessed as effect on [35S]-GTPgammaS binding after 30 mins by scintillation counting | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Agonist activity at human CB1 receptor expressed in Sf9 cells by [35S]-GTPgammaS binding assay | F | 4 | pEC50 | >100000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| GtoPdb | Binding affinity | - | 7.39 | pKi | 40.3 | nM | Ki | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
| ChEMBL | Binding affinity to human CB2 receptor | B | 7.4 | pKi | 40 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| ChEMBL | Agonist activity at human CB2 receptor | B | 7.4 | pKi | 40 | nM | Ki | Eur J Med Chem (2019) 165: 347-362 [PMID:30583970] |
| ChEMBL | Displacement of [3H]-CP55940 from human CB2 receptor transfected in CHO cells after 30 mins by liquid scintillation spectrometry | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells assessed as inhibition of accumulation of forskolin-stimulated cAMP level incubated for 35 mins by chemiluminescence based assay | F | 7.16 | pEC50 | 69.18 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1837-1838 [PMID:36518701] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in PathHunter CHO-K1 CNR2 beta-arrestin cells assessed as beta-arrestin recruitment incubated for 3 hrs by plate reader analysis | F | 7.31 | pEC50 | 48.82 | nM | EC50 | ACS Med Chem Lett (2022) 13: 1837-1838 [PMID:36518701] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in CHO cells by [35S]-GTPgammaS binding assay | F | 7.7 | pEC50 | 20.1 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| ChEMBL | Agonist activity at human CB2 receptor expressed in Sf9 membranes assessed as effect on [35S]-GTPgammaS binding after 30 mins by scintillation counting | F | 7.7 | pEC50 | 20 | nM | EC50 | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| GtoPdb | Dtermined in a GTPγS assay | - | 7.7 | pEC50 | 20.1 | nM | EC50 | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
| CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9] | ||||||||
| ChEMBL | Displacement of [3H]-CP55940 from rat CB2 receptor by liquid scintillation spectrometry | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Binding affinity to rat CB2 receptor | B | 7.43 | pKi | 37 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 5572-5575 [PMID:25466177] |
| GtoPdb | Binding affinity | - | 7.44 | pKi | 36.7 | nM | Ki | J Med Chem (2013) 56: 5722-33 [PMID:23795771] |
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]
