nociceptin/orphanin FQ [Ligand Id: 1681] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL396460 (Nociceptin, Nociceptin/orphanin FQ, Orphanin FQ) |
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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 | F | 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 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 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 recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 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 | Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay | F | 9.37 | pEC50 | 0.43 | nM | EC50 | J Med Chem (2021) 64: 6656-6669 [PMID:33998786] |
| 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 | F | 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 | F | 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 | Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay | B | 9.15 | pKd | 0.71 | nM | Kd | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay | B | 9.17 | pKd | 0.67 | nM | Kd | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay | B | 9.31 | pKd | 0.49 | nM | Kd | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| 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 | Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay | B | 10.06 | pKd | 0.09 | nM | Kd | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 8.99 | pIC50 | 1.02 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.04 | pIC50 | 0.91 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| 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 | Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.19 | pIC50 | 0.65 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.27 | pIC50 | 0.54 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.34 | pIC50 | 0.46 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.66 | pIC50 | 0.22 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay | B | 9.66 | pIC50 | 0.22 | nM | IC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| 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 | Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 7.68 | pEC50 | 21 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 7.89 | pEC50 | 13 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| 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] |
| ChEMBL | Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 8.25 | pEC50 | 5.6 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 8.92 | pEC50 | 1.2 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| ChEMBL | Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding | F | 8.96 | pEC50 | 1.1 | nM | EC50 | Bioorg Med Chem (2009) 17: 7904-7908 [PMID:19879767] |
| 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 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]
