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 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]
