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ChEMBL ligand: CHEMBL658 (IDS-NS-001, R 30,730, R-30730, Sufentanil, Sufentanilo, 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 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]