N/OFQ-(1-13)-NH2 [Ligand Id: 1682] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL384755
  • 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]
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1 CHEMBL384755_lig_chart_1 Nociceptin receptor HumanMouseRat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells B 9.21 pKi 0.62 nM Ki J. Med. Chem. (2008) 51: 4385-4387 [PMID:18624395]
ChEMBL Binding affinity to human NOP receptor B 9.46 pKi 0.35 nM Ki J. Med. Chem. (2008) 51: 4385-4387 [PMID:18624395]
GtoPdb - - 10.4 pKi - - - Br J Pharmacol (2003) 140: 61-70 [PMID:12967935];
Br J Pharmacol (1999) 127: 123-30 [PMID:10369464];
Naunyn Schmiedebergs Arch Pharmacol (2002) 365: 442-9 [PMID:12070757];
J Med Chem (1997) 40: 1789-93 [PMID:9191955]
ChEMBL Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane B 9.45 pIC50 0.35 nM IC50 J. Med. Chem. (2001) 44: 4015-4018 [PMID:11689089]
ChEMBL Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 8.11 pEC50 7.82 nM EC50 J. Med. Chem. (2008) 51: 4385-4387 [PMID:18624395]
ChEMBL Efficacy for human ORL1 receptor expressing HEK293 cells F 8.95 pEC50 1.12 nM EC50 J. Med. Chem. (2001) 44: 4015-4018 [PMID:11689089]
ChEMBL Agonist activity at human NOP receptor by [35S]GTPgammaS binding assay F 9.11 pEC50 0.78 nM EC50 J. Med. Chem. (2008) 51: 4385-4387 [PMID:18624395]
ChEMBL Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor F 9.49 pEC50 0.32 nM EC50 J. Med. Chem. (2001) 44: 3956-3964 [PMID:11689082]
NOP receptor/Nociceptin receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621] [GtoPdb: 320] [UniProtKB: P35377]
ChEMBL Inhibition of [3H]NC-NH2 binding to mouse forebrain membranes B 9.04 pKi 0.91 nM Ki J. Med. Chem. (2001) 44: 3956-3964 [PMID:11689082]
ChEMBL Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement. B 9.1 pKi 0.79 nM Ki J. Med. Chem. (2000) 43: 2805-2813 [PMID:10956188]
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]
NOP receptor/Nociceptin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4503] [GtoPdb: 320] [UniProtKB: P35370]
ChEMBL Activity against LFES-evoked contraction of Wistar rat vas deferens F 6.24 pEC50 575.44 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 4071-4074 [PMID:16714110]
ChEMBL Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone F 6.4 pEC50 398.11 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 4071-4074 [PMID:16714110]
ChEMBL Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction B 7.29 pEC50 51.29 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4052-4055 [PMID:23768905]

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]