TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(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
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(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
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.00300nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.00400nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.00500nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.00500nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.00780nMAssay Description:Binding affinity to human BK1 receptor E273 mutantMore data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0100nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0230nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0270nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0270nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0280nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.0340nMAssay Description:Binding affinity to human BK1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.0350nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 0.0370nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 0.0380nMAssay Description:Binding affinity to human BK1 receptor N298 mutantMore data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.0400nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 0.0410nMpH: 7.4Assay Description:Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.More data for this Ligand-Target Pair
Affinity DataKi: 0.0450nMAssay Description:Binding affinity to human BK1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.0490nMAssay Description:Binding affinity to human BK1 receptor D291 mutantMore data for this Ligand-Target Pair
Affinity DataKi: 0.0500nMAssay Description:Binding affinity to human BK1 receptor E273 mutantMore data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.0500nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.0500nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 0.0500nMpH: 7.4Assay Description:Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0560nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.0570nMAssay Description:Receptor binding assay.More data for this Ligand-Target Pair
Affinity DataKi: 0.0620nMAssay Description:Receptor binding assay.More data for this Ligand-Target Pair
Affinity DataKi: 0.0650nMpH: 7.4Assay Description:Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0650nM ΔG°: -58.1kJ/molepH: 7.2 T: 2°CAssay Description:The fluorescence polarization assay for cyclic nucleotide phosphodiesterases was performed using an IMAP® FP kit supplied by Molecular Devices, S...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0680nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0730nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.0800nMAssay Description:Binding affinity to human BK1 receptor D291 mutantMore data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.0800nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.0850nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.0900nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 0.100nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.110nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
Affinity DataKi: 0.110nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.120nM ΔG°: -56.6kJ/molepH: 7.2 T: 2°CAssay Description:The fluorescence polarization assay for cyclic nucleotide phosphodiesterases was performed using an IMAP® FP kit supplied by Molecular Devices, S...More data for this Ligand-Target Pair
Affinity DataKi: 0.120nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 0.130nMpH: 7.4Assay Description:Inhibition of the binding of 125I-CGRP to receptors and functional antagonism of CGRP receptors were determined using native receptor binding assay.More data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.130nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.130nM ΔG°: -56.4kJ/molepH: 7.2 T: 2°CAssay Description:The fluorescence polarization assay for cyclic nucleotide phosphodiesterases was performed using an IMAP® FP kit supplied by Molecular Devices, S...More data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.130nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
TargetCalcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1(Homo sapiens (Human))
Merck
Curated by ChEMBL
Merck
Curated by ChEMBL
Affinity DataKi: 0.130nMAssay Description:Displacement of [125I]-hCGRP from human CALCRL/RAMP1 expressed in HEK293 cell membranesMore data for this Ligand-Target Pair
Affinity DataKi: 0.130nMAssay Description:Displacement of [3H]des-Arg10 Leu9 kallidin from human bradykinin B1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
Affinity DataKi: 0.130nMAssay Description:Displacement of [125I]hCGRP from human cloned CGRP receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 0.140nMAssay Description:Receptor binding assay.More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.140nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair
TargetIsoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)(Homo sapiens (Human))
Merck Sharp & Dohme
US Patent
Merck Sharp & Dohme
US Patent
Affinity DataKi: 0.140nMAssay Description:In a typical experiment the PDE10 inhibitory activity of the compounds
of the present invention was determined in accordance with the following
exp...More data for this Ligand-Target Pair