fentanyl [Ligand Id: 1626] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL596 (Pecfent, Victanyl, Matrifen, Fentanyl-25, Osmach, Innovar, Yemex, Durogesic dtrans, Actiq, Breakyl, Effentora, Fentanyl-12, Duragesic-25, N02AB03, Ionsys, Fentanyl-100, Mylafent, Leptanal, Fentora, Duragesic-12, Duragesic-37, Durogesic, Tilofyl, Duragesic-75, Fencino, Duragesic, Recivit, Fentanyl-75, Mezolar matrix, AD-923, Fentalis reservoir, R 4263, Fentanyl cii, Fentanyl, Fentanyl-37, Opiodur, Osmanil, IDS-NF-001, Duragesic-50, AD 923, Oralet, Duragesic-100, Fentanyl-50, Subsys, Sublimaze, Abstral, Fentanyl-62, Fentanyl-87)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
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  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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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
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]
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 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 B 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 B 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 B 7.37 pEC50 43 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
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 B 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
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
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Displacement of [3H]PPP from sigma1 receptor (unknown origin) B 6.45 pIC50 354 nM IC50 MedChemComm (2019) 10: 1187-1191
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
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 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]