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 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]
