spiradoline [Ligand Id: 1653] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL70586 (U-62066) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against opioid receptor delta from guinea pig brain membranes using [3H]DADLE as radioligand | B | 5.03 | pKi | 9400 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 8.48 | pKi | 3.32 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Opiate kappa (OP2, KOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 8.08 | pIC50 | 8.3 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Incorporation of [35S]GTP-gamma-S, into CHO membranes expressing human Opioid receptor kappa 1 | F | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2003) 46: 838-849 [PMID:12593663] |
| κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
| ChEMBL | Evaluated for the binding affinity at kappa receptor | B | 8.95 | pKi | 1.13 | nM | Ki | J Med Chem (1994) 37: 3482-3491 [PMID:7932577] |
| GtoPdb | - | - | 9 | pIC50 | - | - | - | Proc Natl Acad Sci USA (1993) 90: 6736-40 [PMID:8393575] |
| κ receptor in Rat [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| GtoPdb | - | - | 9 | pKi | - | - | - | Biochem J (1993) 295 ( Pt 3): 625-8 [PMID:8240267] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity for the Opioid receptor kappa 1 | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Binding affinity against opioid receptor kappa from guinea pig brain membranes using [3H]ethylketocyclazocine as radioligand | B | 8.07 | pKi | 8.6 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 7.02 | pKi | 95 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Opiate mu (OP3, MOP) radioligand binding (ligand: [3H] Diprenorphine) | B | 6.63 | pIC50 | 234 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity for the Opioid receptor mu 1 | B | 5.19 | pKi | 6400 | nM | Ki | J Med Chem (1988) 31: 831-836 [PMID:2832603] |
| ChEMBL | Binding affinity against opioid receptor mu from guinea pig brain membranes using [3H]naloxone as radioligand | B | 6.6 | pKi | 252 | nM | Ki | J Med Chem (1992) 35: 2243-2247 [PMID:1319495] |
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]
