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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
