BDBM21130 N-methyl-2-phenyl-N-[(5R,7S,8S)-7-(pyrrolidin-1-yl)-1-oxaspiro[4.5]decan-8-yl]acetamide::N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec-8-yl)benzeneacetamide::U-69593::U69,593::[3H]U69593
SMILES CN([C@H]1CC[C@@]2(CCCO2)C[C@@H]1N1CCCC1)C(=O)Cc1ccccc1
InChI Key InChIKey=PGZRDDYTKFZSFR-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 127 hits for monomerid = 21130
Affinity DataEC50: 0.190nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Binding affinity to KOR (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
Affinity DataIC50: 0.630nMAssay Description:Binding affinity against rat kappa-opioid receptor expressed in CHO cells was determined by competitive inhibition of 2 nM [3H]-U 69593More data for this Ligand-Target Pair
Affinity DataKi: 0.730nMAssay Description:Inhibition of KOR in guinea pig brain membrane by liquid scintillation counter analysisMore data for this Ligand-Target Pair
Affinity DataEC50: 0.800nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by luminescence assa...More data for this Ligand-Target Pair
Affinity DataKi: 0.900nMAssay Description:Displacement of [3H]U69593 from human KOR expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 0.970nMAssay Description:Displacement of [3H]U-69,593 from KOR in guinea pig brain membranes after 120 mins by scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 0.970nMAssay Description:Displacement of [3H]U-69,593 from kappa-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation countingMore data for this Ligand-Target Pair
Affinity DataKd: 1nMAssay Description:Binding affinity to rat kappa opioid receptor expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataEC50: 1nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 1.10nMAssay Description:Tested for inhibitory effect on binding of [3H]bremazocine to opioid receptor kappa in guinea pig cerebellum membranesMore data for this Ligand-Target Pair
Affinity DataKi: 1.10nMAssay Description:Displacement of [3H]U69593 from human KOR expressed in CHO cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 1.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 1.40nMAssay Description:Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellumMore data for this Ligand-Target Pair
Affinity DataKi: 1.60nMAssay Description:Binding affinity to human Kappa-opioid receptor expressed in CHO cell membrane assessed as inhibition of [3H]-U69593 binding to KOR by measuring inhi...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of [125I]-(D-Pro10)-Dynorphin A binding to human kappa opioid receptor from membranes of HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Binding affinity towards Opioid receptor kappa 1 by the displacement of [125I]-(D-Pro10)-Dynorphin AMore data for this Ligand-Target Pair
Affinity DataKi: 2.5nM ΔG°: -11.7kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
Affinity DataEC50: 2.60nMAssay Description:Agonist activity at human KOR expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by HTRF assayMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [3H]diprenorphine from human KOR expressed in HEK293 cells assessed as inhibition constant incubated for 60 mins by liquid scintillat...More data for this Ligand-Target Pair
Affinity DataEC50: 2.80nMAssay Description:Agonist activity at KOR (unknown origin) expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 60 mins by ...More data for this Ligand-Target Pair
Affinity DataEC50: 3nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 3.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 3.30nM ΔG°: -11.6kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
Affinity DataEC50: 3.30nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 3.5nMAssay Description:Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting...More data for this Ligand-Target Pair
Affinity DataKi: 3.5nMAssay Description:Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 4nMAssay Description:Displacement of [3H]U-69,593 from kappa opioid receptor in rat brain after 60 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataEC50: 4.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 4.20nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKd: 4.30nMAssay Description:Binding affinity at Opioid receptor kappa 1 in guinea pig brain membrane determined by using [3H]U-69593 as radioligandMore data for this Ligand-Target Pair
Affinity DataEC50: 4.30nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 4.70nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 4.80nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 5.30nMAssay Description:Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataEC50: 5.40nMAssay Description:Agonist activity at human kappa opioid receptor expressed in human U2OS cells assessed as increase in ERK1/2 phosphorylation after 10 mins by Western...More data for this Ligand-Target Pair
Affinity DataEC50: 5.60nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataIC50: 6.70nMAssay Description:Displacement of [3H]diprenorphine from human KOR expressed in HEK293 cells incubated for 60 mins by liquid scintillation methodMore data for this Ligand-Target Pair
Affinity DataKi: 7.30nMAssay Description:Binding affinity for the Opioid receptor kappa 1More data for this Ligand-Target Pair
Affinity DataKi: 7.60nM ΔG°: -11.1kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
Affinity DataEC50: 8.10nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataEC50: 9.10nMpH: 7.4Assay Description:HEK293T cells were co-transfected with plasmids encoding the cAMP biosensor GloSensor-22F (Promega) and the different human KOR variants as described...More data for this Ligand-Target Pair
Affinity DataKi: 10nM ΔG°: -10.9kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
Affinity DataKi: 11nM ΔG°: -10.8kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair
Affinity DataKi: 11nM ΔG°: -10.8kcal/molepH: 7.4 T: 2°CAssay Description:Radioligand binding assays were performed as previously detailed [Yan et al., Biochemistry, 48:6898-6908]. In brief, crude cell membranes were prepar...More data for this Ligand-Target Pair