nociceptin/orphanin FQ [Ligand Id: 1681] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL396460 (Nociceptin, Orphanin FQ, Nociceptin/orphanin FQ)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
  • NOP receptor/Nociceptin receptor in Mouse [ChEMBL: CHEMBL3621] [GtoPdb: 320] [UniProtKB: P35377]
  • NOP receptor/Nociceptin receptor in Rat [ChEMBL: CHEMBL4503] [GtoPdb: 320] [UniProtKB: P35370]
  • Nociceptin receptor in Guinea pig [ChEMBL: CHEMBL5492] [UniProtKB: P47748]
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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 Displacement of [3H]naltrindole from human delta opioid receptor expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2008) 51: 1058-1062 [PMID:18232652]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor delta 1 expressed in membrane homogenates of COS-1 or CHO cells B 5.52 pKi 3000 nM Ki J. Med. Chem. (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Displacement of [3H]Cl-DPDPE from human DOP receptor expressed in CHO cells after 60 mins by scintillation counting B 5.55 pKi 2846 nM Ki J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Inhibition of [3H]naltrindole binding to human Opioid receptor delta 1 B 5.7 pKi >2000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5045-5050 [PMID:15380196]
ChEMBL Displacement of [3H]DPDPE from human delta opioid receptor expressed in CHOK1 cells B 6 pKi >1000 nM Ki J. Med. Chem. (2009) 52: 610-625 [PMID:19125610]
ChEMBL Displacement of [3H]DPDPE from human DOP receptor expressed in CHO-K1 cells after 45 mins B 6 pKi >1000 nM Ki Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2008) 51: 1058-1062 [PMID:18232652]
ChEMBL Inhibition of [3H]U-69593 binding to human Opioid receptor kappa 1 B 5.7 pKi >2000 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5045-5050 [PMID:15380196]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor kappa 1 expressed in membrane homogenates of COS-1 or CHO cells B 5.82 pKi 1500 nM Ki J. Med. Chem. (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Displacement of [3H]enadoline from human kappa opioid receptor expressed in HEK293 cells B 6 pKi >1000 nM Ki J. Med. Chem. (2009) 52: 610-625 [PMID:19125610]
ChEMBL Displacement of [3H]enadoline from human KOP receptor expressed in HEK-293 cells after 45 mins B 6 pKi >1000 nM Ki Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Displacement of [3H]U69593 from human KOP receptor expressed in CHO cells after 60 mins by scintillation counting B 6.83 pKi 147 nM Ki J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting F 7.11 pEC50 78.5 nM EC50 J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO cells B 5.52 pKi 3030 nM Ki J. Med. Chem. (2008) 51: 1058-1062 [PMID:18232652]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHOK1 cells B 6 pKi >1000 nM Ki J. Med. Chem. (2009) 52: 610-625 [PMID:19125610]
ChEMBL Displacement of [3H]DAMGO from human MOP receptor expressed in CHO-K1 cells after 45 mins B 6 pKi >1000 nM Ki Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Displacement of [3H]DAMGO from human MOP receptor expressed in CHO cells after 60 mins by scintillation counting B 6.36 pKi 437 nM Ki J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor mu 1 expressed in membrane homogenates of COS-1 or CHO cells B 6.57 pKi 270 nM Ki J. Med. Chem. (2002) 45: 5353-5357 [PMID:12431062]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis B 9.72 pKd 0.19 nM Kd Bioorg. Med. Chem. (2014) 22: 5902-5909 [PMID:25284251]
ChEMBL Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay B 10.04 pKd 0.09 nM Kd Bioorg. Med. Chem. (2009) 17: 7904-7908 [PMID:19879767]
ChEMBL Displacement of radiolabeled nociceptin from human ORL1 receptor B 9.26 pKi 0.55 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human NOP receptor by radioligand displacement assay B 9.32 pKi 0.48 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins B 9.41 pKi 0.39 nM Ki Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells B 9.41 pKi 0.39 nM Ki J. Med. Chem. (2009) 52: 610-625 [PMID:19125610]
ChEMBL Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2002) 45: 5280-5286 [PMID:12431054]
ChEMBL Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting B 9.67 pKi 0.21 nM Ki J. Med. Chem. (2014) 57: 3418-3429 [PMID:24678969]
ChEMBL Inhibition of [3H]nociceptin binding to human Opioid receptor like 1 B 9.74 pKi 0.18 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 5045-5050 [PMID:15380196]
ChEMBL Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells B 9.89 pKi 0.13 nM Ki J. Med. Chem. (2008) 51: 1058-1062 [PMID:18232652]
ChEMBL Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes B 9.92 pKi 0.12 nM Ki Bioorg. Med. Chem. (2014) 22: 2508-2516 [PMID:24657054]
ChEMBL Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells B 10 pKi 0.1 nM Ki J. Med. Chem. (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting B 10.1 pKi 0.08 nM Ki J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells B 10.22 pKi 0.06 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 181-185 [PMID:14684324]
ChEMBL Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells B 10.31 pKi 0.05 nM Ki J. Med. Chem. (2005) 48: 1421-1427 [PMID:15743186]
GtoPdb - - 10.4 pKi - - - Br J Pharmacol (1999) 127: 123-30 [PMID:10369464];
Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 442-9 [PMID:12070757];
Neuropeptides (1997) 31: 403-8 [PMID:9413015]
ChEMBL Inhibition of human ORL1 receptor B 8.68 pIC50 2.1 nM IC50 J. Med. Chem. (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis B 8.74 pIC50 1.83 nM IC50 Bioorg. Med. Chem. (2014) 22: 5902-5909 [PMID:25284251]
ChEMBL Displacement of radiolabeled nociceptin from human ORL1 receptor B 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human NOP receptor by radioligand displacement assay B 8.82 pIC50 1.5 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells B 8.89 pIC50 1.3 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay B 9.14 pIC50 0.72 nM IC50 Bioorg. Med. Chem. (2009) 17: 7904-7908 [PMID:19879767]
ChEMBL Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis B 9.19 pIC50 0.65 nM IC50 Bioorg. Med. Chem. (2014) 22: 5902-5909 [PMID:25284251]
ChEMBL Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells B 9.22 pIC50 0.6 nM IC50 Bioorg. Med. Chem. (2008) 16: 2635-2644 [PMID:18068993]
ChEMBL Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay B 9.54 pIC50 0.29 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay B 9.68 pIC50 0.21 nM IC50 Bioorg. Med. Chem. (2009) 17: 7904-7908 [PMID:19879767]
ChEMBL Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis B 10.08 pIC50 0.08 nM IC50 Bioorg. Med. Chem. (2014) 22: 5902-5909 [PMID:25284251]
ChEMBL Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay B 7.2 pEC50 63 nM EC50 J. Med. Chem. (2000) 43: 1329-1338 [PMID:10753470]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1 F 7.62 pEC50 24 nM EC50 J. Med. Chem. (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding B 7.89 pEC50 13 nM EC50 Bioorg. Med. Chem. (2009) 17: 7904-7908 [PMID:19879767]
ChEMBL Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting F 8.09 pEC50 8.1 nM EC50 J. Med. Chem. (2011) 54: 6531-6537 [PMID:21866885]
ChEMBL Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding F 8.41 pEC50 3.91 nM EC50 Bioorg. Med. Chem. (2008) 16: 2635-2644 [PMID:18068993]
ChEMBL Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis F 8.44 pEC50 3.6 nM EC50 Bioorg. Med. Chem. (2014) 22: 2508-2516 [PMID:24657054]
ChEMBL Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting F 8.82 pEC50 1.5 nM EC50 Bioorg. Med. Chem. (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding F 8.82 pEC50 1.5 nM EC50 J. Med. Chem. (2009) 52: 610-625 [PMID:19125610]
ChEMBL Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding B 8.96 pEC50 1.1 nM EC50 Bioorg. Med. Chem. (2009) 17: 7904-7908 [PMID:19879767]
ChEMBL Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP) B 8.98 pEC50 1.05 nM EC50 J. Med. Chem. (2005) 48: 1421-1427 [PMID:15743186]
ChEMBL Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 9.04 pEC50 0.91 nM EC50 Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells B 9.35 pEC50 0.45 nM EC50 J. Med. Chem. (2002) 45: 5280-5286 [PMID:12431054]
ChEMBL Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization F 9.41 pEC50 0.39 nM EC50 J. Med. Chem. (2009) 52: 4068-4071 [PMID:19473027]
ChEMBL Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay B 9.64 pEC50 0.23 nM EC50 J. Med. Chem. (2016) 59: 3777-3792 [PMID:27035422]
ChEMBL Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay B 9.68 pEC50 0.21 nM EC50 MedChemComm (2014) 5: 973-983
GtoPdb - - 9.8 pEC50 - - - J Pharmacol Exp Ther (1997) 283: 735-41 [PMID:9353393]
ChEMBL Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP) F 9.94 pEC50 0.11 nM EC50 J. Med. Chem. (2005) 48: 1421-1427 [PMID:15743186]
ChEMBL Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1 F 10.05 pEC50 0.09 nM EC50 Bioorg. Med. Chem. Lett. (2004) 14: 5045-5050 [PMID:15380196]
ChEMBL Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data F 10.1 pEC50 0.08 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 3157-3160 [PMID:12372523]
NOP receptor/Nociceptin receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621] [GtoPdb: 320] [UniProtKB: P35377]
GtoPdb - - 9.4 pKi - - - J Pharmacol Exp Ther (1997) 283: 735-41 [PMID:9353393]
ChEMBL Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay F 7.45 pEC50 35.48 nM EC50 Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay F 7.94 pEC50 11.48 nM EC50 J. Med. Chem. (2010) 53: 8400-8408 [PMID:21067234]
ChEMBL Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay F 7.96 pEC50 11 nM EC50 J. Med. Chem. (2010) 53: 8400-8408 [PMID:21067234]
ChEMBL Inhibition of electrically evoked contraction of mouse vas deferens F 8.27 pEC50 5.37 nM EC50 J. Med. Chem. (2005) 48: 1421-1427 [PMID:15743186]
NOP receptor/Nociceptin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4503] [GtoPdb: 320] [UniProtKB: P35370]
ChEMBL Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1 B 10 pKd 0.1 nM Kd Bioorg. Med. Chem. Lett. (2000) 10: 831-834 [PMID:10782696]
ChEMBL Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells B 9.14 pIC50 0.73 nM IC50 Bioorg. Med. Chem. (2008) 16: 9261-9267 [PMID:18818087]
ChEMBL Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions F 6.83 pEC50 147.91 nM EC50 Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor F 7.2 pEC50 63.1 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 831-834 [PMID:10782696]
ChEMBL Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay F 7.89 pEC50 13 nM EC50 Bioorg. Med. Chem. (2008) 16: 9261-9267 [PMID:18818087]
Nociceptin receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5492] [UniProtKB: P47748]
ChEMBL Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions F 8.05 pEC50 8.91 nM EC50 Bioorg. Med. Chem. (2007) 15: 4434-4443 [PMID:17490886]
ChEMBL Inhibition of electrically evoked contraction of guinea pig ileum F 8.28 pEC50 5.25 nM EC50 J. Med. Chem. (2005) 48: 1421-1427 [PMID:15743186]

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]