brorphine [Ligand Id: 12956] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4203403 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Agonist activity at human mu opioid receptor expressed in human USOS-beta-arrestin-hMOR-PathHunter cells incubated for 90 mins by beta-arrestin-2 enzyme fragment complementation assay | F | 6.74 | pEC50 | 182 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by scintillation counting method | F | 8.32 | pEC50 | 4.8 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| GtoPdb | Potency in a GTPγS binding assay | - | 8.32 | pEC50 | 4.8 | nM | EC50 | J Med Chem (2018) 61: 8895-8907 [PMID:30199635] |
| GtoPdb | Potency determined in a cAMP accumulation assay in HEK cells expressing hMOR | - | 8.69 | pEC50 | 2.06 | nM | EC50 | Drug Alcohol Depend (2023) 249: 109939 [PMID:37276825] |
| μ receptor in Rat [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| GtoPdb | Binding affinity for rat brain MOR, determined in a radiologand displacement assay | - | 7.62 | pKi | 24.2 | nM | Ki | Drug Alcohol Depend (2023) 249: 109939 [PMID:37276825] |
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]
