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ChEMBL ligand: CHEMBL658 (IDS-NS-001, R 30,730, R-30730, Sufentanil, Sufentanyl) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
GtoPdb | - | - | 9.9 | pKi | 0.14 | nM | Ki | Regul Toxicol Pharmacol (2011) 59: 385-90 [PMID:21215785] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay | B | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
ChEMBL | Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay | F | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
GtoPdb | - | - | 9.1 | pKi | 0.77 | nM | Ki | Neuropharmacology (1988) 27: 345-8 [PMID:2843777] |
ChEMBL | Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (1990) 33: 2876-2882 [PMID:2170652] |
ChEMBL | Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method | B | 9.4 | pIC50 | 0.4 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] | ||||||||
ChEMBL | TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells | F | 5.35 | pIC50 | 4500 | nM | IC50 | Anesthesiology (2002) 96: 913-920 [PMID:11964599] |
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492] | ||||||||
ChEMBL | Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method | B | 5.68 | pIC50 | 2077 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
ChEMBL | Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis | B | 4.71 | pIC50 | 19360 | nM | IC50 | J Med Chem (2019) 62: 9890-9905 [PMID:31597043] |
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]