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Found 429 with Last Name = 'schreier' and Initial = 'jd'
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500526(CHEMBL3747517)
Affinity DataKi:  0.00600nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500538(CHEMBL3745790)
Affinity DataKi:  0.0100nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500520(CHEMBL3746993)
Affinity DataKi:  0.0100nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500521(CHEMBL3746277)
Affinity DataKi:  0.0100nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147136(US8957077, M-3)
Affinity DataKi:  0.0120nMAssay 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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500519(CHEMBL3746917)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500535(CHEMBL3747450)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM126823(US8785467, 1-20)
Affinity DataKi:  0.0300nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM126823(US8785467, 1-20)
Affinity DataKi:  0.0300nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104700(US8569311, 1-10)
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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147143(US8957077, 1-18)
Affinity DataKi:  0.0800nMAssay 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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147138(US8957077, 1-4)
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 exper...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM120778(US8710076, F-2)
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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147142(US8957077, 1-15)
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 exper...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318697(6-Fluoro-2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-...)
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
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147146(US8957077, 1-23)
Affinity DataKi:  0.180nMAssay 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
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50314676((4-(6-fluoroquinazolin-2-yl)-1,4-diazepan-1-yl)(5-...)
Affinity DataKi:  0.200nMAssay Description:Binding affinity to OX2 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147134(US8957077, J-5)
Affinity DataKi:  0.230nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104689(US8569311, A-9)
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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147135(US8957077, L-4)
Affinity DataKi:  0.240nMAssay 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
In DepthDetails US Patent
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104697(US8569311, 1-1)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318698(6,7-Fluoro-2-{(5R)-5-Methyl-4-[2-(2H-1,2,3-triazol...)
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
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318699(2-{(5R)-5-Methyl-4-[2-(2H-1,2,3-triazol-2-yl)benzo...)
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
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50028040(CHEMBL3338846)
Affinity DataKi:  0.300nMAssay Description:Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-([3H]-1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R ex...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50028045(CHEMBL3338852)
Affinity DataKi:  0.300nMAssay Description:Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-([3H]-1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R ex...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104692(US8569311, E-5)
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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147134(US8957077, J-5)
Affinity DataKi:  0.320nMAssay 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
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104701(US8569311, 1-15)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318701(CHEMBL1083659 | MK-4305 | [(7R)-4-(5-Chloro-1,3-be...)
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318695(2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2...)
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
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM147140(US8957077, 1-10)
Affinity DataKi:  0.370nMAssay 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
In DepthDetails US Patent
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104698(US8569311, 1-4)
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
In DepthDetails US Patent
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318695(2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2...)
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
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318695(2-{(5R)-5-Methyl-4-[5-methyl-2-(2H-1,2,3-triazol-2...)
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
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50314681((5-chloro-2-(2H-1,2,3-triazol-2-yl)phenyl)(6-(6-fl...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to OX1 receptor by radioligand displacement assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50500537(CHEMBL3746162)
Affinity DataKi:  0.400nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50321509((5-chloro-2-(2H-1,2,3-triazol-2-yl)phenyl)((1R,5R)...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to OX1RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50321510((3-(7-fluoroquinazolin-2-yl)-3,9-di azabicyclo[4.2...)
Affinity DataKi:  0.400nMAssay Description:Binding affinity to OX2RMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM98538(US8492392, T-1)
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
In DepthDetails US Patent
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM126830(US8785467, 1-39)
Affinity DataKi:  0.440nMAssay Description:Inhibition of PDE10A (unknown origin) by IMAP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM50318696(2-{(5R)-5-Methyl-4-[2-(2H-1,2,3-triazol-2-yl)benzo...)
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
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104703(US8569311, 1-21)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104699(US8569311, 1-8)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM106968(US8592457, 1-5)
Affinity DataKi:  0.5nMAssay Description:Displacement of (S)-N-(2-(1H-pyrrol-1-yl)phenyl)-1-(2-([3H]-1-methyl-1H-benzo[d]imidazol-2-ylthio)acetyl)pyrrolidine-2-carboxamide from human OX2R ex...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104702(US8569311, 1-19)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Rattus norvegicus (Rat))
Merch Sharp & Dohme

US Patent
LigandPNGBDBM104690(US8569311, B-3)
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
In DepthDetails US Patent
TargetOrexin/Hypocretin receptor type 1(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50318701(CHEMBL1083659 | MK-4305 | [(7R)-4-(5-Chloro-1,3-be...)
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
LigandPNGBDBM50318701(CHEMBL1083659 | MK-4305 | [(7R)-4-(5-Chloro-1,3-be...)
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
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM120777(US8710076, E-2)
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
In DepthDetails US Patent
TargetOrexin receptor type 2(Homo sapiens (Human))
Merck Sharp & Dohme

US Patent
LigandPNGBDBM120779(US8710076, H-4)
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
In DepthDetails US Patent
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