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ORL1 (h) CEREP panel
Assay data:1 Tested
SummaryRelated BioAssays by Target
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells by scintillation counting analysis
Assay data:1 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 11 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay relative to control
Assay data:2 Tested
SummaryPubMed CitationRelated BioAssays by Target
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 2 Activity ≤ 1 µM, 3 Tested
Agonist activity at human NOP receptor expressed in CHO cells assessed as maximal stimulation of calcium mobilization by Fluo-4 AM dye based analysis relative to control
Assay data:34 Tested
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
Assay data:34 Active, 2 Activity ≤ 1 nM, 34 Activity ≤ 1 µM, 35 Tested
Cell-Based NOP Assay from US Patent US11365191: "Substituted cyclohexyl compounds as NOP inhibiiors"
Assay data:161 Active, 17 Activity ≤ 1 nM, 185 Activity ≤ 1 µM, 185 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Receptor Binding Assay from US Patent US10829480: "3-((hetero-)aryl)-alkyl-8-amino-2-oxo-l,3-diaza-spiro-[4.5]-decane derivatives"
Assay data:144 Active, 84 Activity ≤ 1 µM, 144 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Human Nociceptin/Orphanin FQ Peptide (hNOP) Receptor Binding Assay from US Patent US10807989: "3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives"
Assay data:288 Active, 19 Activity ≤ 1 nM, 286 Activity ≤ 1 µM, 288 Tested
Human Nociceptin/Orphanin FQ Peptide (hNOP) Receptor Binding Assay from US Patent US10807988: "3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives"
Assay data:373 Active, 19 Activity ≤ 1 nM, 371 Activity ≤ 1 µM, 373 Tested
Receptor Binding Assay from US Patent US10793556: "8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives"
Assay data:34 Active, 3 Activity ≤ 1 nM, 34 Activity ≤ 1 µM, 34 Tested
Scintillation Proximity Assay from US Patent US10738015: "1,3-diaza-spiro-[3.4]-octane derivatives"
Assay data:42 Active, 1 Activity ≤ 1 nM, 40 Activity ≤ 1 µM, 42 Tested
Ligand Binding Assay from US Patent US9480684: "Orvinol and thevinol derivatives useful in the treatment of anxiety or a compulsive disorder"
Assay data:11 Active, 9 Activity ≤ 1 nM, 11 Activity ≤ 1 µM, 11 Tested
Binding Assay from US Patent US9403767: "Substituted 4-aminocyclohexane derivatives"
Assay data:69 Active, 5 Activity ≤ 1 nM, 58 Activity ≤ 1 µM, 69 Tested
Ligand Binding Assays from US Patent US9259422: "Orvinol and thevinol derivatives useful in the treatment of depression"
ORL-1 Receptor Binding Assay from US Patent US8637502: "2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating pain"
Assay data:28 Active, 23 Activity ≤ 1 µM, 31 Tested
Radioligand Binding Assay from US Patent US8481743: "Phenylpropionamide compounds and the use thereof"
Assay data:1 Active, 4 Tested
SummaryCompounds, ActiveRelated BioAssays by DepositorRelated BioAssays by Target
ORL-1 Receptor Binding Assay from US Patent US8476271: "Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators"
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
Radioligand Binding Assay from Article 10.1016/j.bmcl.2009.04.022: "Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity."
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
In Vitro Binding Assay (IC50) and In Vitro Agonism/Antagonism Measurements (EC50/IC50) from Article 10.1016/j.bmcl.2009.04.022: "Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity."
Assay data:20 Active, 2 Activity ≤ 1 nM, 20 Activity ≤ 1 µM, 22 Tested
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