fentanyl [Ligand Id: 1626] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL596 (Abstral, Abstral-, Actiq, AD 923, AD-923, Breakyl, Duragesic, Duragesic-100, Duragesic-12, Duragesic-25, Duragesic-37, Duragesic-50, Duragesic-75, Durogesic, Durogesic d-trans, Durogesic dtrans, Effentora, En3267, EN-3267, Fencino, Fendrop, Fentalis reservoir, Fentanest, Fentanyl, Fentanyl-100, Fentanyl-12, Fentanyl-25, Fentanyl-37, Fentanyl-50, Fentanyl-62, Fentanyl-75, Fentanyl-87, Fentanyl cii, Fentora, IDS-NF-001, Innovar, Ionsys, Leptanal, Matrifen, Mezolar matrix, Mylafent, N02AB03, Opiodur, Oralet, Osmach, Osmanil, Pecfent, Phentanyl, R 4263, Recivit, Recuvyra, Sublimase, Sublimaze, Subsys, Tilofyl, Victanyl, Yemex) |
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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 1 | B | 5.99 | pKi | 1035 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| ChEMBL | Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes | B | 6.17 | pKi | 679 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| ChEMBL | Displacement of [3H]DPDPE from human delta opioid receptor | B | 6.24 | pKi | 570 | nM | Ki | Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand | B | 6.37 | pIC50 | 431 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| ChEMBL | In vitro binding activity against opioid receptor delta using [3DPDPE] as radioligand | B | 6.73 | pIC50 | 187.4 | nM | IC50 | J Med Chem (1991) 34: 827-841 [PMID:1847432] |
| ChEMBL | Compound was tested in vitro for binding affinity towards delta opioid receptor by measuring displacement of [3H]DPDPE from guinea pig brain membranes | B | 6.73 | pIC50 | 187 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1177-1182 |
| δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300] | ||||||||
| ChEMBL | Displacement of [3H]-DPDPE from Swiss Webster mouse neural membranes delta opioid receptor after 60 mins by liquid scintillation spectrometric analysis | B | 6.25 | pKi | 568 | nM | Ki | Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric stimulation-induced contraction | B | 5.03 | pIC50 | 9400 | nM | IC50 | Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated muscle contraction | B | 8.02 | pIC50 | 9.5 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872] |
| ChEMBL | Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | F | 8.02 | pIC50 | 9.45 | nM | IC50 | J Med Chem (2010) 53: 2875-2881 [PMID:20218625] |
| ChEMBL | Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction | B | 8.03 | pIC50 | 9.4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
| ChEMBL | Agonist activity at delta opioid receptor in beta-funaltrexamine-treated mouse vas deferens | B | 8.46 | pIC50 | 3.45 | nM | IC50 | Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Binding affinity towards Opioid receptor delta 1 using [3H]DADLE as radioligand. | B | 5.99 | pKi | 1035 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
| ChEMBL | Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane | B | 6.25 | pKi | 568 | nM | Ki | J Med Chem (2010) 53: 2875-2881 [PMID:20218625] |
| ChEMBL | Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2003) 46: 623-633 [PMID:12570383] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 4.68 | pKi | 21000 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 4.58 | pKi | 26200 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis | B | 6.26 | pKi | 554 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.74 | pIC50 | 1819.7 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
| ChEMBL | Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | J Med Chem (2012) 55: 7054-7060 [PMID:22793499] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 | B | 6.71 | pKi | 196.5 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| GtoPdb | - | - | 7.1 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand | B | 5.8 | pIC50 | 1580 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against Opioid receptor kappa 1 in guinea pig brain membranes | B | 5.95 | pKi | 1130 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| ChEMBL | Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane | B | 6.53 | pKi | 298 | nM | Ki | J Med Chem (2010) 53: 2875-2881 [PMID:20218625] |
| ChEMBL | Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand. | B | 6.71 | pKi | 196.5 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
| ChEMBL | In vitro binding activity against opioid receptor kappa using [3H]EKC as radioligand | B | 5.23 | pIC50 | 5893 | nM | IC50 | J Med Chem (1991) 34: 827-841 [PMID:1847432] |
| ChEMBL | Compound was tested in vitro for binding affinity towards kappa opioid receptor by measuring displacement of [3H]EKC from guinea pig brain membranes | B | 5.23 | pIC50 | 5893 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1177-1182 |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay | B | 8.28 | pKi | 5.23 | nM | Ki | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Binding affinity against Opioid receptor mu 1 | B | 8.4 | pKi | 3.97 | nM | Ki | J Med Chem (2000) 43: 381-391 [PMID:10669565] |
| ChEMBL | Displacement of [3H]DAMGO (2 nM ) from opioid receptor mu 1 in human brain | B | 8.54 | pKi | 2.9 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 491-493 [PMID:14698188] |
| ChEMBL | Binding affinity to mu opioid receptor (unknown origin) expressed in HEK cells at pH 7.4 | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2018) 61: 5822-5880 [PMID:29400967] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - | NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407] |
| ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay | F | 7.97 | pIC50 | 10.72 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
| ChEMBL | Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay | F | 8.26 | pIC50 | 5.5 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209] |
| ChEMBL | Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2001) 44: 3378-3390 [PMID:11585443] |
| 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 | 7.28 | pEC50 | 53 | 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 | 7.37 | pEC50 | 43 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay | F | 7.76 | pEC50 | 17.38 | nM | EC50 | J Med Chem (2020) 63: 15709-15725 [PMID:33271020] |
| ChEMBL | Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay | F | 7.76 | pEC50 | 17.2 | nM | EC50 | J Med Chem (2020) 63: 15709-15725 [PMID:33271020] |
| ChEMBL | Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay | F | 9.29 | pEC50 | 0.51 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1568-1572 [PMID:31749912] |
| μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866] | ||||||||
| ChEMBL | Displacement of [3H]-DAMGO from Swiss Webster mouse neural membranes mu opioid receptor after 60 mins by liquid scintillation spectrometric analysis | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Displacement of [3H] DAMGO from rat mu-opioid receptor | B | 6.24 | pKi | 570 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2010) 53: 2875-2881 [PMID:20218625] |
| ChEMBL | Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115] |
| ChEMBL | Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand. | B | 8.4 | pKi | 3.97 | nM | Ki | J Med Chem (1995) 38: 1547-1557 [PMID:7739013] |
| ChEMBL | Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. | B | 8.67 | pKi | 2.16 | nM | Ki | J Med Chem (1989) 32: 663-671 [PMID:2563773] |
| ChEMBL | Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. | B | 8.67 | pKi | 2.16 | nM | Ki | J Med Chem (1990) 33: 2876-2882 [PMID:2170652] |
| ChEMBL | Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2003) 46: 623-633 [PMID:12570383] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - | Mol Pharmacol (1994) 45: 330-4 [PMID:8114680] |
| ChEMBL | Displacement of [3H] DAMGO from rat mu-opioid receptor | B | 5.9 | pIC50 | 1258.93 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872] |
| ChEMBL | Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method | B | 8.91 | pIC50 | 1.23 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
| ChEMBL | Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor | F | 7.49 | pEC50 | 32.4 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against mu opioid receptor in guinea pig brain membranes | B | 8.07 | pKi | 8.45 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig isolated ileum assessed as inhibition of electric stimulation-induced contraction | B | 5.47 | pIC50 | 3400 | nM | IC50 | Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115] |
| ChEMBL | Agonist activity at mu opioid receptor in beta-funaltrexamine-treated guinea pig isolated ileum | B | 8.02 | pIC50 | 9.45 | nM | IC50 | Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | F | 8.46 | pIC50 | 3.45 | nM | IC50 | J Med Chem (2010) 53: 2875-2881 [PMID:20218625] |
| ChEMBL | Inhibition of mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418] |
| ChEMBL | Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically stimulated muscle contraction | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872] |
| ChEMBL | Compound was tested in vitro for binding affinity towards mu opioid receptor by measuring displacement of [3H]DAGO from guinea pig brain membranes | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1177-1182 |
| ChEMBL | In vitro binding activity against opioid receptor mu using [3H]-DAGO as radioligand | B | 8.51 | pIC50 | 3.1 | nM | IC50 | J Med Chem (1991) 34: 827-841 [PMID:1847432] |
| 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 | 5.19 | pIC50 | 6500 | 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 | 5.3 | pIC50 | 4973 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Inhibition of sigma 1 receptor (unknown origin) | B | 9.41 | pKi | 0.39 | nM | Ki | Eur J Med Chem (2020) 191: 112144-112144 [PMID:32087465] |
| ChEMBL | Displacement of [3H]PPP from sigma1 receptor (unknown origin) | B | 6.45 | pIC50 | 354 | nM | IC50 | Medchemcomm (2019) 10: 1187-1191 [PMID:31391893] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Displacement of [3H]SKF10047 from rat brain sigma1 receptor incubated for 35 mins by scintillation counting method | B | 6 | pKi | >1000 | nM | Ki | 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 | 4.34 | pIC50 | 46170 | 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]
