N/OFQ-(1-13)-NH2 [Ligand Id: 1682] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL384755 |
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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 NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2020) 63: 10782-10795 [PMID:32901477] |
| ChEMBL | Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay | B | 8.08 | pEC50 | 8.32 | nM | EC50 | J Med Chem (2020) 63: 10782-10795 [PMID:32901477] |
| 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 | Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis | F | 9.29 | pEC50 | 0.51 | nM | EC50 | J Med Chem (2021) 64: 6656-6669 [PMID:33998786] |
| 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 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]
