Found 810 with Last Name = 'breslin' and Initial = 'mj' TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.00200nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0400nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.0800nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.110nMAssay Description:Compound potency can be assessed by a radioligand binding assay (described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430) in which ...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.150nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.170nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.220nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.230nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.240nMAssay Description:Antagonist activity at human OX2R by radioligand displacement assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.240nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.240nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.25nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.25nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.280nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Antagonist activity at human OX2R by radioligand displacement assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Antagonist activity at human OX2R by radioligand displacement assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.310nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.340nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.350nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
3D Structure (crystal)
Affinity DataKi: 0.350nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.360nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.370nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.390nMAssay Description:Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expre...More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.390nMAssay Description:Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in C...More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.410nMAssay Description:Antagonist activity at human OX1R by radioligand displacement assayMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.430nM ΔG°: -53.5kJ/moleT: 2°CAssay Description:Fluorescence polarization assay: The compounds of the following examples had activity in reference assays by exhibiting the ability to inhibit the hy...More data for this Ligand-Target Pair
Affinity DataKi: 0.470nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.480nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.5nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.530nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.540nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.550nMAssay Description:Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in C...More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.550nMAssay Description:Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expre...More data for this Ligand-Target Pair
Affinity DataKi: 0.550nMAssay Description:Compound potency can be assessed by a radioligand binding assay (described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430) in which ...More data for this Ligand-Target Pair
Affinity DataKi: 0.560nMAssay Description:Compound potency can be assessed by a radioligand binding assay (described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430) in which ...More data for this Ligand-Target Pair
Affinity DataKi: 0.590nMAssay Description:Displacement of [3H](S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R exp...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.600nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.600nM ΔG°: -52.6kJ/moleT: 2°CAssay Description:Fluorescence polarization assay: The compounds of the following examples had activity in reference assays by exhibiting the ability to inhibit the hy...More data for this Ligand-Target Pair
Affinity DataKi: 0.600nMAssay Description:Antagonist activity at human OX1R by radioligand displacement assayMore data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.630nM ΔG°: -52.5kJ/moleT: 2°CAssay Description:Fluorescence polarization assay: The compounds of the following examples had activity in reference assays by exhibiting the ability to inhibit the hy...More data for this Ligand-Target Pair
Affinity DataKi: 0.670nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.670nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.680nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
Affinity DataKi: 0.710nMAssay Description:Radioligand binding assay described in Bergman et. al. Bioorg. Med. Chem. Lett. 2008, 18, 1425-1430.More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.780nMAssay Description:Displacement of [3H](S)-N-(biphenyl-2-yl)-1-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX1R expressed in C...More data for this Ligand-Target Pair
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories
Curated by ChEMBL
Merck Research Laboratories
Curated by ChEMBL
Affinity DataKi: 0.780nMAssay Description:Displacement of [3H]N-cyclobutyl-5-methyl-N-(2-(1-methyl-1H-benzo[d]imidazol-2-ylthio)ethyl)-2-(2H-1,2,3-triazol-2-yl)benzamide from human OX1R expre...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.780nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.800nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following exper...More data for this Ligand-Target Pair
Affinity DataKi: 0.800nMAssay Description:Antagonist activity at human OX2R by radioligand displacement assayMore data for this Ligand-Target Pair
