sufentanil [Ligand Id: 3534] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL658 (R-30730, Sufentanil, IDS-NS-001, R 30,730)
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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]
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 B 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
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
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]