null
SMILES CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(O)=O
InChI Key InChIKey=OVVIBUHLQIYUEU-IWIISZHXSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 62 hits for monomerid = 214798
Affinity DataKi: 0.0900nMAssay Description:Displacement of [3H]U69,593 from human KOR expressed in mouse HN9.10 cell membranes incubated for 2 hrs by liquid scintillation counting based radiol...More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Positive allosteric modulator activity in mouse kappa opioid receptor stably expressed in HEK293 cell membrane assessed as binding affinity of dyn A1...More data for this Ligand-Target Pair
TargetKappa-type opioid receptor [K227A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 2.20nM ΔG°: -11.8kcal/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: 3.80nMAssay Description:Displacement of [3H]DPDPE from human delta opioid receptor expressed in mouse HN9.10 cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 4nMAssay Description:Displacement of [3H]DAMGO from rat mu opioid receptor expressed in mouse HN9.10 cell membranesMore data for this Ligand-Target Pair
TargetKappa-type opioid receptor [K200A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 4.80nM ΔG°: -11.3kcal/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
TargetKappa-type opioid receptor [K212A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 5.40nM ΔG°: -11.3kcal/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
TargetKappa-type opioid receptor [I135A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 6.20nM ΔG°: -11.2kcal/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
TargetKappa-type opioid receptor [Y320A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 6.60nM ΔG°: -11.2kcal/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
TargetKappa-type opioid receptor [M226A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 7.10nM 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 DataKi: 8nMAssay Description:Displacement of [3H]diprenorphine from human MOR expressed in mouse NG108-15 cell membranes incubated for 2 hrs by liquid scintillation counting base...More data for this Ligand-Target Pair
Affinity DataKi: 8nM ΔG°: -11.0kcal/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: 8.30nMAssay Description:Displacement of [3H]deltorphin-II from human DOR expressed in CHO cell membranes incubated for 2 hrs by liquid scintillation counting based radioliga...More data for this Ligand-Target Pair
TargetKappa-type opioid receptor [Y313F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
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
TargetKappa-type opioid receptor [Y312A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
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
TargetKappa-type opioid receptor [M142A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 16nM ΔG°: -10.6kcal/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
TargetKappa-type opioid receptor [H291F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 17nM ΔG°: -10.6kcal/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
TargetKappa-type opioid receptor [Y320F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 18nM ΔG°: -10.6kcal/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
TargetKappa-type opioid receptor [Y312F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 19nM ΔG°: -10.5kcal/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
TargetKappa-type opioid receptor [Y119F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 20nM ΔG°: -10.5kcal/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
TargetKappa-type opioid receptor [Y139F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 29nM ΔG°: -10.3kcal/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
TargetKappa-type opioid receptor [Y139A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 35nM ΔG°: -10.2kcal/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
TargetKappa-type opioid receptor [Y313A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 45nM ΔG°: -10.0kcal/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
TargetKappa-type opioid receptor [E297A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 48nM ΔG°: -9.98kcal/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
TargetKappa-type opioid receptor [Y66A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 78nM ΔG°: -9.69kcal/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
TargetKappa-type opioid receptor [H291A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 91nM ΔG°: -9.60kcal/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
TargetKappa-type opioid receptor [Q115A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 120nM ΔG°: -9.43kcal/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
TargetKappa-type opioid receptor [I294A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 140nM ΔG°: -9.34kcal/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
TargetKappa-type opioid receptor [I316A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 200nM ΔG°: -9.13kcal/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
TargetKappa-type opioid receptor [Y119A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 200nM ΔG°: -9.13kcal/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
TargetKappa-type opioid receptor [D138N](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 1.60E+3nM ΔG°: -7.90kcal/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
TargetKappa-type opioid receptor [D138A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataKi: 5.20E+3nM ΔG°: -7.20kcal/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
TargetKappa-type opioid receptor [Y139F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 22nMpH: 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
TargetKappa-type opioid receptor [M142A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 110nMpH: 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
TargetKappa-type opioid receptor [K200A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 2nMpH: 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
TargetKappa-type opioid receptor [K212A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 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
TargetKappa-type opioid receptor [M226A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 1.40nMpH: 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
TargetKappa-type opioid receptor [K227A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 12nMpH: 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
TargetKappa-type opioid receptor [H291A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 260nMpH: 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
TargetKappa-type opioid receptor [H291F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 81nMpH: 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
TargetKappa-type opioid receptor [I294A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 72nMpH: 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
TargetKappa-type opioid receptor [E297A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 44nMpH: 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
TargetKappa-type opioid receptor [Y312A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 47nMpH: 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
TargetKappa-type opioid receptor [Y312F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 5.80nMpH: 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
TargetKappa-type opioid receptor [Y313A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 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
TargetKappa-type opioid receptor [Y313F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 5.90nMpH: 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
TargetKappa-type opioid receptor [I316A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 100nMpH: 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
TargetKappa-type opioid receptor [Y320F](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 76nMpH: 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
TargetKappa-type opioid receptor [Y320A](Homo sapiens (Human))
University of North Carolina School of Medicine
University of North Carolina School of Medicine
Affinity DataEC50: 100nMpH: 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: 1.20nMAssay Description:Inhibition of mu opioid receptor in guinea pig ileum/longitudinal muscle with myenteric plexus assessed as inhibition of electrically-stimulated musc...More data for this Ligand-Target Pair