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Patent code US9394311

Compile Data Set for Download or QSAR
Found 136 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239752
PNG
(US9394311, 35)
Show SMILES Cc1cc(Cl)c(C)n2nc(\C=C\c3nc(N4CCCC4)n(C)n3)nc12
Show InChI InChI=1S/C17H20ClN7/c1-11-10-13(18)12(2)25-16(11)19-14(22-25)6-7-15-20-17(23(3)21-15)24-8-4-5-9-24/h6-7,10H,4-5,8-9H2,1-3H3/b7-6+
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n/an/a 0.150n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239785
PNG
(US9394311, 68)
Show SMILES Cc1c(Cl)cc(Cl)c2nc(CCc3n[nH]c(n3)N3CCCC3)nn12
Show InChI InChI=1S/C15H17Cl2N7/c1-9-10(16)8-11(17)14-18-13(22-24(9)14)5-4-12-19-15(21-20-12)23-6-2-3-7-23/h8H,2-7H2,1H3,(H,19,20,21)
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n/an/a 0.220n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239837
PNG
(US9394311, 119)
Show SMILES COCCOc1cc(Cl)c(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C19H26ClN7O2/c1-13-14(20)12-15(29-11-10-28-3)18-21-16(23-27(13)18)6-7-17-22-19(24-25(17)2)26-8-4-5-9-26/h12H,4-11H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239812
PNG
(US9394311, 95)
Show SMILES Cc1c(Cl)cc(OC(F)F)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C17H20ClF2N7O/c1-10-11(18)9-12(28-16(19)20)15-21-13(23-27(10)15)5-6-14-22-17(24-25(14)2)26-7-3-4-8-26/h9,16H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239755
PNG
(US9394311, 38)
Show SMILES Cc1cc(Cl)c(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C17H22ClN7/c1-11-10-13(18)12(2)25-16(11)19-14(21-25)6-7-15-20-17(22-23(15)3)24-8-4-5-9-24/h10H,4-9H2,1-3H3
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n/an/a 0.280n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239826
PNG
(US9394311, 109)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3-c3ccccc3)N3CCCC3)nn12
Show InChI InChI=1S/C21H24N8/c1-15-14-22-16(2)20-23-18(25-28(15)20)10-11-19-24-21(27-12-6-7-13-27)26-29(19)17-8-4-3-5-9-17/h3-5,8-9,14H,6-7,10-13H2,1-2H3
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n/an/a 0.290n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239840
PNG
(US9394311, 122)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C3CCOCC3)N3CCCC3)nn12)C(F)(F)F
Show InChI InChI=1S/C21H25ClF3N7O/c1-13-16(22)12-15(21(23,24)25)19-26-17(28-31(13)19)4-5-18-27-20(30-8-2-3-9-30)29-32(18)14-6-10-33-11-7-14/h12,14H,2-11H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239838
PNG
(US9394311, 120)
Show SMILES Cc1c(Cl)cc(OC2CCOCC2)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C21H28ClN7O2/c1-14-16(22)13-17(31-15-7-11-30-12-8-15)20-23-18(25-29(14)20)5-6-19-24-21(26-27(19)2)28-9-3-4-10-28/h13,15H,3-12H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239822
PNG
(US9394311, 105)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(N4CCCC4)n(C)n3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H19ClF3N7/c1-10-12(18)9-11(17(19,20)21)15-22-13(25-28(10)15)5-6-14-23-16(26(2)24-14)27-7-3-4-8-27/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239793
PNG
(US9394311, 76)
Show SMILES COc1cc(Cl)c(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C17H22ClN7O/c1-11-12(18)10-13(26-3)16-19-14(21-25(11)16)6-7-15-20-17(22-23(15)2)24-8-4-5-9-24/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239799
PNG
(US9394311, 82)
Show SMILES Cc1c(Br)cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H19BrF3N7/c1-10-12(18)9-11(17(19,20)21)15-22-13(24-28(10)15)5-6-14-23-16(25-26(14)2)27-7-3-4-8-27/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239786
PNG
(US9394311, 128 | US9394311, 69)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H19ClF3N7/c1-10-12(18)9-11(17(19,20)21)15-22-13(24-28(10)15)5-6-14-23-16(25-26(14)2)27-7-3-4-8-27/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239815
PNG
(US9394311, 98)
Show SMILES Cc1c(Cl)cc(OCC(F)(F)F)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C18H21ClF3N7O/c1-11-12(19)9-13(30-10-18(20,21)22)16-23-14(25-29(11)16)5-6-15-24-17(26-27(15)2)28-7-3-4-8-28/h9H,3-8,10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239823
PNG
(US9394311, 106)
Show SMILES Cc1c(Cl)cc(OC(F)F)c2nc(CCc3nc(N4CCCC4)n(C)n3)nn12
Show InChI InChI=1S/C17H20ClF2N7O/c1-10-11(18)9-12(28-16(19)20)15-21-13(24-27(10)15)5-6-14-22-17(25(2)23-14)26-7-3-4-8-26/h9,16H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239753
PNG
(US9394311, 36)
Show SMILES Cc1cc(Cl)c(C)n2nc(CCc3nc(N4CCCC4)n(C)n3)nc12
Show InChI InChI=1S/C17H22ClN7/c1-11-10-13(18)12(2)25-16(11)19-14(22-25)6-7-15-20-17(23(3)21-15)24-8-4-5-9-24/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239769
PNG
(US9394311, 52)
Show SMILES Cc1c(Cl)cc(Cl)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H19Cl2N7/c1-10-11(17)9-12(18)15-19-13(21-25(10)15)5-6-14-20-16(22-23(14)2)24-7-3-4-8-24/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239778
PNG
(US9394311, 61)
Show SMILES COc1ccc(Cn2nc(nc2CCc2nc3c(Cl)cc(Cl)c(C)n3n2)N2CCCC2)cc1
Show InChI InChI=1S/C23H25Cl2N7O/c1-15-18(24)13-19(25)22-26-20(28-32(15)22)9-10-21-27-23(30-11-3-4-12-30)29-31(21)14-16-5-7-17(33-2)8-6-16/h5-8,13H,3-4,9-12,14H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239851
PNG
(US9394311, 132)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C3CC3)N3CCCC3)nn12)C(F)(F)F
Show InChI InChI=1S/C19H21ClF3N7/c1-11-14(20)10-13(19(21,22)23)17-24-15(26-29(11)17)6-7-16-25-18(28-8-2-3-9-28)27-30(16)12-4-5-12/h10,12H,2-9H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239786
PNG
(US9394311, 128 | US9394311, 69)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H19ClF3N7/c1-10-12(18)9-11(17(19,20)21)15-22-13(24-28(10)15)5-6-14-23-16(25-26(14)2)27-7-3-4-8-27/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239825
PNG
(US9394311, 108)
Show SMILES Cc1cnc(C)c2nc(nn12)C#Cc1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C16H18N8/c1-11-10-17-12(2)15-18-13(20-24(11)15)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h10H,4-5,8-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239808
PNG
(US9394311, 91)
Show SMILES Cc1c(Cl)cc(c2nc(nn12)C#Cc1nc(nn1C)N1CCCC1)C(F)(F)F
Show InChI InChI=1S/C17H15ClF3N7/c1-10-12(18)9-11(17(19,20)21)15-22-13(24-28(10)15)5-6-14-23-16(25-26(14)2)27-7-3-4-8-27/h9H,3-4,7-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239849
PNG
(US9394311, 130)
Show SMILES Cc1c(Cl)cc(C(F)F)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C17H20ClF2N7/c1-10-12(18)9-11(15(19)20)16-21-13(23-27(10)16)5-6-14-22-17(24-25(14)2)26-7-3-4-8-26/h9,15H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239744
PNG
(US9394311, 27)
Show SMILES Cc1c(Cl)ccc2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H20ClN7/c1-11-12(17)5-7-15-18-13(20-24(11)15)6-8-14-19-16(21-22(14)2)23-9-3-4-10-23/h5,7H,3-4,6,8-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239788
PNG
(US9394311, 71)
Show SMILES Cc1c(Cl)cc(Br)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H19BrClN7/c1-10-12(18)9-11(17)15-19-13(21-25(10)15)5-6-14-20-16(22-23(14)2)24-7-3-4-8-24/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239789
PNG
(US9394311, 72)
Show SMILES Cc1c(Br)cc(Cl)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H19BrClN7/c1-10-11(17)9-12(18)15-19-13(21-25(10)15)5-6-14-20-16(22-23(14)2)24-7-3-4-8-24/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239834
PNG
(US9394311, 117a)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3CC3CC3)N3CCCC3)nn12
Show InChI InChI=1S/C19H26N8/c1-13-11-20-14(2)18-21-16(23-27(13)18)7-8-17-22-19(25-9-3-4-10-25)24-26(17)12-15-5-6-15/h11,15H,3-10,12H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239839
PNG
(US9394311, 121)
Show SMILES Cc1c(Cl)cc(OCCN2CCOCC2)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C22H31ClN8O2/c1-16-17(23)15-18(33-14-11-29-9-12-32-13-10-29)21-24-19(26-31(16)21)5-6-20-25-22(27-28(20)2)30-7-3-4-8-30/h15H,3-14H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239727
PNG
(US9394311, 10)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC3)nn12
Show InChI InChI=1S/C15H20N8/c1-10-9-16-11(2)14-17-12(19-23(10)14)5-6-13-18-15(20-21(13)3)22-7-4-8-22/h9H,4-8H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239801
PNG
(US9394311, 84)
Show SMILES Cc1cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn2c1C)C(F)(F)F
Show InChI InChI=1S/C18H22F3N7/c1-11-10-13(18(19,20)21)16-22-14(24-28(16)12(11)2)6-7-15-23-17(25-26(15)3)27-8-4-5-9-27/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239850
PNG
(US9394311, 131)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(N4CCCC4)n(n3)C3CC3)nn12)C(F)(F)F
Show InChI InChI=1S/C19H21ClF3N7/c1-11-14(20)10-13(19(21,22)23)17-24-15(26-29(11)17)6-7-16-25-18(28-8-2-3-9-28)30(27-16)12-4-5-12/h10,12H,2-9H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239726
PNG
(US9394311, 8)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(n[nH]3)N3CCCC3)nn12
Show InChI InChI=1S/C15H20N8/c1-10-9-16-11(2)14-17-13(21-23(10)14)6-5-12-18-15(20-19-12)22-7-3-4-8-22/h9H,3-8H2,1-2H3,(H,18,19,20)
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239841
PNG
(US9394311, 123a)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C3CC3)N3CCCC3)nn12
Show InChI InChI=1S/C18H24N8/c1-12-11-19-13(2)17-20-15(22-25(12)17)7-8-16-21-18(24-9-3-4-10-24)23-26(16)14-5-6-14/h11,14H,3-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239844
PNG
(US9394311, 125)
Show SMILES Cc1c(Cl)cc(OCC(=O)N2CCCOC2)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C22H29ClN8O3/c1-15-16(23)12-17(34-13-20(32)30-10-5-11-33-14-30)21-24-18(26-31(15)21)6-7-19-25-22(27-28(19)2)29-8-3-4-9-29/h12H,3-11,13-14H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239745
PNG
(US9394311, 28)
Show SMILES Cc1c(Cl)ccc2nc(CCc3nc(N4CCCC4)n(C)n3)nn12
Show InChI InChI=1S/C16H20ClN7/c1-11-12(17)5-8-15-18-13(21-24(11)15)6-7-14-19-16(22(2)20-14)23-9-3-4-10-23/h5,8H,3-4,6-7,9-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239791
PNG
(US9394311, 74)
Show SMILES Cc1c(cc(Cl)c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C#N
Show InChI InChI=1S/C17H19ClN8/c1-11-12(10-19)9-13(18)16-20-14(22-26(11)16)5-6-15-21-17(23-24(15)2)25-7-3-4-8-25/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239796
PNG
(US9394311, 79)
Show SMILES Cc1c(Cl)cc(C#N)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C17H19ClN8/c1-11-13(18)9-12(10-19)16-20-14(22-26(11)16)5-6-15-21-17(23-24(15)2)25-7-3-4-8-25/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239735
PNG
(US9394311, 18)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(N4CCCC4)n(C)n3)nn12
Show InChI InChI=1S/C16H22N8/c1-11-10-17-12(2)15-18-13(21-24(11)15)6-7-14-19-16(22(3)20-14)23-8-4-5-9-23/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239846
PNG
(US9394311, 127)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CC[C@@H](F)C3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H18ClF4N7/c1-9-12(18)7-11(17(20,21)22)15-23-13(25-29(9)15)3-4-14-24-16(26-27(14)2)28-6-5-10(19)8-28/h7,10H,3-6,8H2,1-2H3/t10-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239779
PNG
(US9394311, 62)
Show SMILES COc1ccc(Cn2nc(CCc3nc4c(Cl)cc(Cl)c(C)n4n3)nc2N2CCCC2)cc1
Show InChI InChI=1S/C23H25Cl2N7O/c1-15-18(24)13-19(25)22-26-20(29-32(15)22)9-10-21-27-23(30-11-3-4-12-30)31(28-21)14-16-5-7-17(33-2)8-6-16/h5-8,13H,3-4,9-12,14H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239827
PNG
(US9394311, 110)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3CC(F)F)N3CCCC3)nn12
Show InChI InChI=1S/C17H22F2N8/c1-11-9-20-12(2)16-21-14(23-27(11)16)5-6-15-22-17(25-7-3-4-8-25)24-26(15)10-13(18)19/h9,13H,3-8,10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239803
PNG
(US9394311, 86)
Show SMILES CCc1cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn2c1C)C(F)(F)F
Show InChI InChI=1S/C19H24F3N7/c1-4-13-11-14(19(20,21)22)17-23-15(25-29(17)12(13)2)7-8-16-24-18(26-27(16)3)28-9-5-6-10-28/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239787
PNG
(US9394311, 70)
Show SMILES Cc1c(ccc2nc(CCc3nc(nn3C)N3CCCC3)nn12)C#N
Show InChI InChI=1S/C17H20N8/c1-12-13(11-18)5-7-16-19-14(21-25(12)16)6-8-15-20-17(22-23(15)2)24-9-3-4-10-24/h5,7H,3-4,6,8-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239792
PNG
(US9394311, 75)
Show SMILES CCc1cnc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C17H24N8/c1-4-13-11-18-12(2)25-16(13)19-14(21-25)7-8-15-20-17(22-23(15)3)24-9-5-6-10-24/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239754
PNG
(US9394311, 37)
Show SMILES Cc1ccc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C17H23N7/c1-12-6-7-13(2)24-16(12)18-14(20-24)8-9-15-19-17(21-22(15)3)23-10-4-5-11-23/h6-7H,4-5,8-11H2,1-3H3
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n/an/a 4.21n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239802
PNG
(US9394311, 85)
Show SMILES Cc1c(Cl)cc(O)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H20ClN7O/c1-10-11(17)9-12(25)15-18-13(20-24(10)15)5-6-14-19-16(21-22(14)2)23-7-3-4-8-23/h9,25H,3-8H2,1-2H3
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n/an/a 4.22n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239764
PNG
(US9394311, 47)
Show SMILES CCn1nc(nc1N1CCCC1)C#Cc1nc2c(C)ncc(C)n2n1
Show InChI InChI=1S/C17H20N8/c1-4-24-17(23-9-5-6-10-23)20-15(21-24)8-7-14-19-16-13(3)18-11-12(2)25(16)22-14/h11H,4-6,9-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239748
PNG
(US9394311, 31)
Show SMILES Cc1ccn2nc(CCc3nc(nn3C)N3CCCC3)nc2c1C
Show InChI InChI=1S/C17H23N7/c1-12-8-11-24-16(13(12)2)18-14(20-24)6-7-15-19-17(21-22(15)3)23-9-4-5-10-23/h8,11H,4-7,9-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239767
PNG
(US9394311, 50)
Show SMILES CCc1ncc(C)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C17H24N8/c1-4-14-18-11-12(2)16-19-13(21-25(14)16)7-8-15-20-17(22-23(15)3)24-9-5-6-10-24/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239763
PNG
(US9394311, 46)
Show SMILES Cc1cc(Cl)c(C)n2nc(nc12)[C@H]1C[C@@H]1c1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C18H22ClN7/c1-10-8-14(19)11(2)26-16(10)20-15(22-26)12-9-13(12)17-21-18(23-24(17)3)25-6-4-5-7-25/h8,12-13H,4-7,9H2,1-3H3/t12-,13-/m0/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239737
PNG
(US9394311, 20)
Show SMILES COc1ccc(Cn2nc(nc2CCc2nc3c(C)ncc(C)n3n2)N2CCCC2)cc1
Show InChI InChI=1S/C23H28N8O/c1-16-14-24-17(2)22-25-20(27-31(16)22)10-11-21-26-23(29-12-4-5-13-29)28-30(21)15-18-6-8-19(32-3)9-7-18/h6-9,14H,4-5,10-13,15H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239855
PNG
(US9394311, 136)
Show SMILES Cc1nc2ccc(Cl)cc2nc1C#Cc1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C18H17ClN6/c1-12-14(21-16-11-13(19)5-6-15(16)20-12)7-8-17-22-18(23-24(17)2)25-9-3-4-10-25/h5-6,11H,3-4,9-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239832
PNG
(US9394311, 115)
Show SMILES C[C@H]1CCN(C1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-7-8-24(10-11)17-20-15(23(4)22-17)6-5-14-19-16-13(3)18-9-12(2)25(16)21-14/h9,11H,5-8,10H2,1-4H3/t11-/m0/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239817
PNG
(US9394311, 100)
Show SMILES C[C@H]1CCCN1c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-6-5-9-24(11)17-20-15(23(4)22-17)8-7-14-19-16-13(3)18-10-12(2)25(16)21-14/h10-11H,5-9H2,1-4H3/t11-/m0/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239721
PNG
(US9394311, 2)
Show SMILES CCn1nc(nc1CCc1nc2c(C)ncc(C)n2n1)N1CCCC1
Show InChI InChI=1S/C17H24N8/c1-4-24-15(20-17(22-24)23-9-5-6-10-23)8-7-14-19-16-13(3)18-11-12(2)25(16)21-14/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239731
PNG
(US9394311, 14)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H22N8/c1-11-10-17-12(2)15-18-13(20-24(11)15)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239835
PNG
(US9394311, 117b)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(N4CCCC4)n(CC4CC4)n3)nn12
Show InChI InChI=1S/C19H26N8/c1-13-11-20-14(2)18-21-16(24-27(13)18)7-8-17-22-19(25-9-3-4-10-25)26(23-17)12-15-5-6-15/h11,15H,3-10,12H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239734
PNG
(US9394311, 17)
Show SMILES Cc1cnc(C)c2nc(\C=C\c3nc(N4CCCC4)n(C)n3)nn12
Show InChI InChI=1S/C16H20N8/c1-11-10-17-12(2)15-18-13(21-24(11)15)6-7-14-19-16(22(3)20-14)23-8-4-5-9-23/h6-7,10H,4-5,8-9H2,1-3H3/b7-6+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239800
PNG
(US9394311, 83)
Show SMILES Cc1c(cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C(F)(F)F)C#N
Show InChI InChI=1S/C18H19F3N8/c1-11-12(10-22)9-13(18(19,20)21)16-23-14(25-29(11)16)5-6-15-24-17(26-27(15)2)28-7-3-4-8-28/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239749
PNG
(US9394311, 32)
Show SMILES Cc1ccn2nc(CCc3nc(N4CCCC4)n(C)n3)nc2c1C
Show InChI InChI=1S/C17H23N7/c1-12-8-11-24-16(13(12)2)18-14(21-24)6-7-15-19-17(22(3)20-15)23-9-4-5-10-23/h8,11H,4-7,9-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239842
PNG
(US9394311, 123b)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(N4CCCC4)n(n3)C3CC3)nn12
Show InChI InChI=1S/C18H24N8/c1-12-11-19-13(2)17-20-15(22-25(12)17)7-8-16-21-18(24-9-3-4-10-24)26(23-16)14-5-6-14/h11,14H,3-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239775
PNG
(US9394311, 58)
Show SMILES Cc1cnc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc12
Show InChI InChI=1S/C16H22N8/c1-11-10-17-12(2)24-15(11)18-13(20-24)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239833
PNG
(US9394311, 116)
Show SMILES C[C@@H]1CCN(C1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-7-8-24(10-11)17-20-15(23(4)22-17)6-5-14-19-16-13(3)18-9-12(2)25(16)21-14/h9,11H,5-8,10H2,1-4H3/t11-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239829
PNG
(US9394311, 112)
Show SMILES C[C@H]1CCCN1c1nc(CCc2nc3c(C)cnc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-10-18-13(3)25-16(11)19-14(21-25)7-8-15-20-17(22-23(15)4)24-9-5-6-12(24)2/h10,12H,5-9H2,1-4H3/t12-/m0/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239761
PNG
(US9394311, 44)
Show SMILES Cc1nc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc2c1Cl
Show InChI InChI=1S/C16H21ClN8/c1-10-14(17)15-19-12(21-25(15)11(2)18-10)6-7-13-20-16(22-23(13)3)24-8-4-5-9-24/h4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239805
PNG
(US9394311, 88)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CCC(F)(F)C3)nn12)C(F)(F)F
Show InChI InChI=1S/C17H17ClF5N7/c1-9-11(18)7-10(17(21,22)23)14-24-12(26-30(9)14)3-4-13-25-15(27-28(13)2)29-6-5-16(19,20)8-29/h7H,3-6,8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239794
PNG
(US9394311, 77)
Show SMILES Cc1c(Cl)cc(C2CC2)c2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C19H24ClN7/c1-12-15(20)11-14(13-5-6-13)18-21-16(23-27(12)18)7-8-17-22-19(24-25(17)2)26-9-3-4-10-26/h11,13H,3-10H2,1-2H3
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n/an/a 9.99n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239820
PNG
(US9394311, 103)
Show SMILES Cc1nc(n2nc(CCc3nc(nn3C)N3CCCC3)nc2c1C)C(F)(F)F
Show InChI InChI=1S/C17H21F3N8/c1-10-11(2)21-15(17(18,19)20)28-14(10)22-12(24-28)6-7-13-23-16(25-26(13)3)27-8-4-5-9-27/h4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239757
PNG
(US9394311, 40)
Show SMILES Cc1ccc2nc(CCc3nc(nn3C)N3CCCC3)nn2c1C
Show InChI InChI=1S/C17H23N7/c1-12-6-8-16-18-14(20-24(16)13(12)2)7-9-15-19-17(21-22(15)3)23-10-4-5-11-23/h6,8H,4-5,7,9-11H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239813
PNG
(US9394311, 96)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC[C@@H](F)C3)nn12
Show InChI InChI=1S/C16H21FN8/c1-10-8-18-11(2)15-19-13(21-25(10)15)4-5-14-20-16(22-23(14)3)24-7-6-12(17)9-24/h8,12H,4-7,9H2,1-3H3/t12-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239854
PNG
(US9394311, 135)
Show SMILES Cc1nc2cc(Cl)ccc2nc1C#Cc1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C18H17ClN6/c1-12-14(21-15-6-5-13(19)11-16(15)20-12)7-8-17-22-18(23-24(17)2)25-9-3-4-10-25/h5-6,11H,3-4,9-10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239723
PNG
(US9394311, 4)
Show SMILES CCn1nc(nc1CCc1nc2nc(C)cc(C)n2n1)N1CCCC1
Show InChI InChI=1S/C17H24N8/c1-4-24-15(20-17(22-24)23-9-5-6-10-23)8-7-14-19-16-18-12(2)11-13(3)25(16)21-14/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239720
PNG
(US9394311, 1)
Show SMILES CCn1nc(nc1\C=C\c1nc2c(C)ncc(C)n2n1)N1CCCC1
Show InChI InChI=1S/C17H22N8/c1-4-24-15(20-17(22-24)23-9-5-6-10-23)8-7-14-19-16-13(3)18-11-12(2)25(16)21-14/h7-8,11H,4-6,9-10H2,1-3H3/b8-7+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239759
PNG
(US9394311, 42)
Show SMILES Cc1nc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc2c1C
Show InChI InChI=1S/C17H24N8/c1-11-12(2)18-13(3)25-16(11)19-14(21-25)7-8-15-20-17(22-23(15)4)24-9-5-6-10-24/h5-10H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239809
PNG
(US9394311, 92)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC4(CC4)C3)nn12
Show InChI InChI=1S/C18H24N8/c1-12-10-19-13(2)16-20-14(22-26(12)16)4-5-15-21-17(23-24(15)3)25-9-8-18(11-25)6-7-18/h10H,4-9,11H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239843
PNG
(US9394311, 124)
Show SMILES COC[C@H]1CCCN1c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C18H26N8O/c1-12-10-19-13(2)17-20-15(22-26(12)17)7-8-16-21-18(23-24(16)3)25-9-5-6-14(25)11-27-4/h10,14H,5-9,11H2,1-4H3/t14-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239725
PNG
(US9394311, 7)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3CC(F)(F)F)N3CCCC3)nn12
Show InChI InChI=1S/C17H21F3N8/c1-11-9-21-12(2)15-22-13(24-28(11)15)5-6-14-23-16(26-7-3-4-8-26)25-27(14)10-17(18,19)20/h9H,3-8,10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239852
PNG
(US9394311, 133)
Show SMILES COc1ccc(Cn2nc(nc2N2CCCC2)C#Cc2cnc3ccc(Cl)cc3n2)cc1
Show InChI InChI=1S/C24H21ClN6O/c1-32-20-8-4-17(5-9-20)16-31-24(30-12-2-3-13-30)28-23(29-31)11-7-19-15-26-21-10-6-18(25)14-22(21)27-19/h4-6,8-10,14-15H,2-3,12-13,16H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239828
PNG
(US9394311, 111)
Show SMILES CC1CCCN1c1nc(CCc2nc3c(C)cnc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-10-18-13(3)25-16(11)19-14(21-25)7-8-15-20-17(22-23(15)4)24-9-5-6-12(24)2/h10,12H,5-9H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239739
PNG
(US9394311, 22)
Show SMILES Cc1cc(C)n2nc(CCc3nc(nn3CC(F)(F)F)N3CCCC3)nc2n1
Show InChI InChI=1S/C17H21F3N8/c1-11-9-12(2)28-15(21-11)22-13(24-28)5-6-14-23-16(26-7-3-4-8-26)25-27(14)10-17(18,19)20/h9H,3-8,10H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239741
PNG
(US9394311, 24)
Show SMILES Cc1cc(C)n2nc(CCc3nc(nn3C)N3CCCC3)nc2n1
Show InChI InChI=1S/C16H22N8/c1-11-10-12(2)24-15(17-11)18-13(20-24)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239836
PNG
(US9394311, 118)
Show SMILES Cc1cnc(C)n2nc(CCc3nc(nn3C)N3CCC[C@@H]3C(F)(F)F)nc12
Show InChI InChI=1S/C17H21F3N8/c1-10-9-21-11(2)28-15(10)22-13(24-28)6-7-14-23-16(25-26(14)3)27-8-4-5-12(27)17(18,19)20/h9,12H,4-8H2,1-3H3/t12-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239730
PNG
(US9394311, 13)
Show SMILES Cc1cnc(C)c2nc(\C=C\c3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H20N8/c1-11-10-17-12(2)15-18-13(20-24(11)15)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h6-7,10H,4-5,8-9H2,1-3H3/b7-6+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239768
PNG
(US9394311, 51)
Show SMILES CC1CCCN1c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-6-5-9-24(11)17-20-15(23(4)22-17)8-7-14-19-16-13(3)18-10-12(2)25(16)21-14/h10-11H,5-9H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239765
PNG
(US9394311, 48)
Show SMILES CCn1nc(CCc2nc3c(C)ncc(C)n3n2)nc1N1CCCC1
Show InChI InChI=1S/C17H24N8/c1-4-24-17(23-9-5-6-10-23)20-15(21-24)8-7-14-19-16-13(3)18-11-12(2)25(16)22-14/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239773
PNG
(US9394311, 56)
Show SMILES Cn1nc(nc1CCc1nc2ccc3ccccc3n2n1)N1CCCC1
Show InChI InChI=1S/C19H21N7/c1-24-17(21-19(23-24)25-12-4-5-13-25)11-9-16-20-18-10-8-14-6-2-3-7-15(14)26(18)22-16/h2-3,6-8,10H,4-5,9,11-13H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239795
PNG
(US9394311, 78)
Show SMILES Cc1c(cc(C#N)c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C#N
Show InChI InChI=1S/C18H19N9/c1-12-13(10-19)9-14(11-20)17-21-15(23-27(12)17)5-6-16-22-18(24-25(16)2)26-7-3-4-8-26/h9H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239766
PNG
(US9394311, 49)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCCCC3)nn12
Show InChI InChI=1S/C17H24N8/c1-12-11-18-13(2)16-19-14(21-25(12)16)7-8-15-20-17(22-23(15)3)24-9-5-4-6-10-24/h11H,4-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239780
PNG
(US9394311, 63)
Show SMILES Cn1nc(nc1CCc1nc2cc(c(F)c(N)n2n1)C(F)(F)F)N1CCCC1
Show InChI InChI=1S/C16H18F4N8/c1-26-11(23-15(25-26)27-6-2-3-7-27)5-4-10-22-12-8-9(16(18,19)20)13(17)14(21)28(12)24-10/h8H,2-7,21H2,1H3
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n/an/a 32.4n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239853
PNG
(US9394311, 134)
Show SMILES Clc1ccc2ncc(CCc3n[nH]c(n3)N3CCCC3)nc2c1
Show InChI InChI=1S/C16H17ClN6/c17-11-3-5-13-14(9-11)19-12(10-18-13)4-6-15-20-16(22-21-15)23-7-1-2-8-23/h3,5,9-10H,1-2,4,6-8H2,(H,20,21,22)
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239831
PNG
(US9394311, 114)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC[C@@H]3C(F)(F)F)nn12
Show InChI InChI=1S/C17H21F3N8/c1-10-9-21-11(2)15-22-13(24-28(10)15)6-7-14-23-16(25-26(14)3)27-8-4-5-12(27)17(18,19)20/h9,12H,4-8H2,1-3H3/t12-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239782
PNG
(US9394311, 65)
Show SMILES Cn1nc(nc1CCc1nc2c(Br)cc(cn2n1)C(F)(F)F)N1CCCC1
Show InChI InChI=1S/C16H17BrF3N7/c1-25-13(22-15(24-25)26-6-2-3-7-26)5-4-12-21-14-11(17)8-10(16(18,19)20)9-27(14)23-12/h8-9H,2-7H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239758
PNG
(US9394311, 41)
Show SMILES Cc1nc(C)c2nc(CCc3nc(nn3C)N3CCCC3)nn2c1C
Show InChI InChI=1S/C17H24N8/c1-11-13(3)25-16(12(2)18-11)19-14(21-25)7-8-15-20-17(22-23(15)4)24-9-5-6-10-24/h5-10H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239728
PNG
(US9394311, 11 | US9394311, 25)
Show SMILES CN(C1CC1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H22N8/c1-10-9-17-11(2)15-18-13(20-24(10)15)7-8-14-19-16(21-23(14)4)22(3)12-5-6-12/h9,12H,5-8H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239728
PNG
(US9394311, 11 | US9394311, 25)
Show SMILES CN(C1CC1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H22N8/c1-10-9-17-11(2)15-18-13(20-24(10)15)7-8-14-19-16(21-23(14)4)22(3)12-5-6-12/h9,12H,5-8H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239848
PNG
(US9394311, 129)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC(C3)C(F)F)nn12
Show InChI InChI=1S/C17H22F2N8/c1-10-8-20-11(2)16-21-13(23-27(10)16)4-5-14-22-17(24-25(14)3)26-7-6-12(9-26)15(18)19/h8,12,15H,4-7,9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239776
PNG
(US9394311, 59)
Show SMILES CCN(CC)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H24N8/c1-6-23(7-2)16-19-14(22(5)21-16)9-8-13-18-15-12(4)17-10-11(3)24(15)20-13/h10H,6-9H2,1-5H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239750
PNG
(US9394311, 33)
Show SMILES CCn1nc(nc1CCc1nc2ccccc2nc1C)N1CCCC1
Show InChI InChI=1S/C19H24N6/c1-3-25-18(22-19(23-25)24-12-6-7-13-24)11-10-15-14(2)20-16-8-4-5-9-17(16)21-15/h4-5,8-9H,3,6-7,10-13H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239756
PNG
(US9394311, 39)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC(F)C3)nn12
Show InChI InChI=1S/C15H19FN8/c1-9-6-17-10(2)14-18-12(20-24(9)14)4-5-13-19-15(21-22(13)3)23-7-11(16)8-23/h6,11H,4-5,7-8H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239746
PNG
(US9394311, 29)
Show SMILES Cc1cccc2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C16H21N7/c1-12-6-5-7-15-17-13(19-23(12)15)8-9-14-18-16(20-21(14)2)22-10-3-4-11-22/h5-7H,3-4,8-11H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239781
PNG
(US9394311, 64)
Show SMILES Cn1nc(nc1CCc1nc2cccc(n2n1)C(F)(F)F)N1CCCC1
Show InChI InChI=1S/C16H18F3N7/c1-24-13(21-15(23-24)25-9-2-3-10-25)8-7-12-20-14-6-4-5-11(16(17,18)19)26(14)22-12/h4-6H,2-3,7-10H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239818
PNG
(US9394311, 101)
Show SMILES C[C@@H]1CCCN1c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-6-5-9-24(11)17-20-15(23(4)22-17)8-7-14-19-16-13(3)18-10-12(2)25(16)21-14/h10-11H,5-9H2,1-4H3/t11-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239747
PNG
(US9394311, 30)
Show SMILES CN(C1CC1)c1nc(\C=C\c2nc3nc(C)cc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H20N8/c1-10-9-11(2)24-15(17-10)18-13(20-24)7-8-14-19-16(21-23(14)4)22(3)12-5-6-12/h7-9,12H,5-6H2,1-4H3/b8-7+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239762
PNG
(US9394311, 45)
Show SMILES Cc1cc2nc(CCc3nc(nn3C)N3CCCC3)nn2c(C)n1
Show InChI InChI=1S/C16H22N8/c1-11-10-15-18-13(20-24(15)12(2)17-11)6-7-14-19-16(21-22(14)3)23-8-4-5-9-23/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239733
PNG
(US9394311, 16)
Show SMILES Cc1nc2ccccc2nc1CCc1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C18H22N6/c1-13-14(20-16-8-4-3-7-15(16)19-13)9-10-17-21-18(22-23(17)2)24-11-5-6-12-24/h3-4,7-8H,5-6,9-12H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239743
PNG
(US9394311, 26)
Show SMILES Cn1nc(nc1CCc1nc2ccc(Cl)cn2n1)N1CCCC1
Show InChI InChI=1S/C15H18ClN7/c1-21-13(18-15(20-21)22-8-2-3-9-22)7-5-12-17-14-6-4-11(16)10-23(14)19-12/h4,6,10H,2-3,5,7-9H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239798
PNG
(US9394311, 81)
Show SMILES Cc1cnc(C)n2nc(\C=C\c3nc(nn3C)N3CCC3)nc12
Show InChI InChI=1S/C15H18N8/c1-10-9-16-11(2)23-14(10)17-12(19-23)5-6-13-18-15(20-21(13)3)22-7-4-8-22/h5-6,9H,4,7-8H2,1-3H3/b6-5+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239797
PNG
(US9394311, 80)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)C(C)(C)O
Show InChI InChI=1S/C19H26ClN7O/c1-12-14(20)11-13(19(2,3)28)17-21-15(23-27(12)17)7-8-16-22-18(24-25(16)4)26-9-5-6-10-26/h11,28H,5-10H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239814
PNG
(US9394311, 97)
Show SMILES CN(CC1CC1)c1nc(\C=C\c2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H22N8/c1-11-9-18-12(2)16-19-14(21-25(11)16)7-8-15-20-17(22-24(15)4)23(3)10-13-5-6-13/h7-9,13H,5-6,10H2,1-4H3/b8-7+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239760
PNG
(US9394311, 43)
Show SMILES COC1CCN(C1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8O/c1-11-9-18-12(2)16-19-14(21-25(11)16)5-6-15-20-17(22-23(15)3)24-8-7-13(10-24)26-4/h9,13H,5-8,10H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239790
PNG
(US9394311, 73)
Show SMILES Cc1c(Cl)cc(c2nc(CCc3nc(nn3C)N3CCCC3)nn12)S(C)(=O)=O
Show InChI InChI=1S/C17H22ClN7O2S/c1-11-12(18)10-13(28(3,26)27)16-19-14(21-25(11)16)6-7-15-20-17(22-23(15)2)24-8-4-5-9-24/h10H,4-9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239738
PNG
(US9394311, 21)
Show SMILES Cc1cc(C)n2nc(CCc3nc(nn3C)N3CCC3)nc2n1
Show InChI InChI=1S/C15H20N8/c1-10-9-11(2)23-14(16-10)17-12(19-23)5-6-13-18-15(20-21(13)3)22-7-4-8-22/h9H,4-8H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239772
PNG
(US9394311, 55)
Show SMILES Cc1ccn2nc(CCc3nc(nn3C)N3CCCC3)nc2c1[NH+](O)[O-]
Show InChI InChI=1S/C16H22N8O2/c1-11-7-10-23-15(14(11)24(25)26)17-12(19-23)5-6-13-18-16(20-21(13)2)22-8-3-4-9-22/h7,10,24-25H,3-6,8-9H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239740
PNG
(US9394311, 23)
Show SMILES CCN(C)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C15H22N8/c1-6-21(4)15-18-13(22(5)20-15)8-7-12-17-14-11(3)16-9-10(2)23(14)19-12/h9H,6-8H2,1-5H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239771
PNG
(US9394311, 54)
Show SMILES Cn1nc(nc1CCc1nc2c(Cl)cc(cn2n1)C(F)(F)F)N1CCCC1
Show InChI InChI=1S/C16H17ClF3N7/c1-25-13(22-15(24-25)26-6-2-3-7-26)5-4-12-21-14-11(17)8-10(16(18,19)20)9-27(14)23-12/h8-9H,2-7H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239732
PNG
(US9394311, 15)
Show SMILES Cc1nc2ccccc2nc1\C=C\c1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C18H20N6/c1-13-14(20-16-8-4-3-7-15(16)19-13)9-10-17-21-18(22-23(17)2)24-11-5-6-12-24/h3-4,7-10H,5-6,11-12H2,1-2H3/b10-9+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239806
PNG
(US9394311, 89)
Show SMILES CC1CN(C1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H22N8/c1-10-8-23(9-10)16-19-14(22(4)21-16)6-5-13-18-15-12(3)17-7-11(2)24(15)20-13/h7,10H,5-6,8-9H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239811
PNG
(US9394311, 94)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC[C@H](F)C3)nn12
Show InChI InChI=1S/C16H21FN8/c1-10-8-18-11(2)15-19-13(21-25(10)15)4-5-14-20-16(22-23(14)3)24-7-6-12(17)9-24/h8,12H,4-7,9H2,1-3H3/t12-/m0/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239751
PNG
(US9394311, 34)
Show SMILES CN(C1CC1)c1nc(CCc2nc3nc(C)cc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H22N8/c1-10-9-11(2)24-15(17-10)18-13(20-24)7-8-14-19-16(21-23(14)4)22(3)12-5-6-12/h9,12H,5-8H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239830
PNG
(US9394311, 113)
Show SMILES C[C@@H]1CCCN1c1nc(CCc2nc3c(C)cnc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-11-10-18-13(3)25-16(11)19-14(21-25)7-8-15-20-17(22-23(15)4)24-9-5-6-12(24)2/h10,12H,5-9H2,1-4H3/t12-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239821
PNG
(US9394311, 104)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC(O)C3)nn12
Show InChI InChI=1S/C16H22N8O/c1-10-8-17-11(2)15-18-13(20-24(10)15)4-5-14-19-16(21-22(14)3)23-7-6-12(25)9-23/h8,12,25H,4-7,9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239810
PNG
(US9394311, 93)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCC(F)(F)C3)nn12
Show InChI InChI=1S/C16H20F2N8/c1-10-8-19-11(2)14-20-12(22-26(10)14)4-5-13-21-15(23-24(13)3)25-7-6-16(17,18)9-25/h8H,4-7,9H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239824
PNG
(US9394311, 107)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC[C@H](C3)NC(=O)OC(C)(C)C)nn12
Show InChI InChI=1S/C21H31N9O2/c1-13-11-22-14(2)18-24-16(26-30(13)18)7-8-17-25-19(27-28(17)6)29-10-9-15(12-29)23-20(31)32-21(3,4)5/h11,15H,7-10,12H2,1-6H3,(H,23,31)/t15-/m1/s1
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239819
PNG
(US9394311, 102)
Show SMILES Cc1cnc(C)c2nc(\C=C\c3nc(nn3C)N3CCCCCC3)nn12
Show InChI InChI=1S/C18H24N8/c1-13-12-19-14(2)17-20-15(22-26(13)17)8-9-16-21-18(23-24(16)3)25-10-6-4-5-7-11-25/h8-9,12H,4-7,10-11H2,1-3H3/b9-8+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239777
PNG
(US9394311, 60)
Show SMILES CCN(C1CC1)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C17H24N8/c1-5-24(13-6-7-13)17-20-15(23(4)22-17)9-8-14-19-16-12(3)18-10-11(2)25(16)21-14/h10,13H,5-9H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239722
PNG
(US9394311, 3)
Show SMILES CCn1nc(nc1\C=C\c1nc2nc(C)cc(C)n2n1)N1CCCC1
Show InChI InChI=1S/C17H22N8/c1-4-24-15(20-17(22-24)23-9-5-6-10-23)8-7-14-19-16-18-12(2)11-13(3)25(16)21-14/h7-8,11H,4-6,9-10H2,1-3H3/b8-7+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239774
PNG
(US9394311, 57)
Show SMILES Cc1cncc2nc(CCc3nc(nn3C)N3CCCC3)nn12
Show InChI InChI=1S/C15H20N8/c1-11-9-16-10-14-17-12(19-23(11)14)5-6-13-18-15(20-21(13)2)22-7-3-4-8-22/h9-10H,3-8H2,1-2H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239729
PNG
(US9394311, 12)
Show SMILES CN(C1CC1)c1nc(\C=C\c2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C16H20N8/c1-10-9-17-11(2)15-18-13(20-24(10)15)7-8-14-19-16(21-23(14)4)22(3)12-5-6-12/h7-9,12H,5-6H2,1-4H3/b8-7+
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239816
PNG
(US9394311, 99)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC4CCC4C3)nn12
Show InChI InChI=1S/C18H24N8/c1-11-8-19-12(2)17-20-15(22-26(11)17)6-7-16-21-18(23-24(16)3)25-9-13-4-5-14(13)10-25/h8,13-14H,4-7,9-10H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239804
PNG
(US9394311, 87)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CCCC3=O)nn12
Show InChI InChI=1S/C16H20N8O/c1-10-9-17-11(2)15-18-12(20-24(10)15)6-7-13-19-16(21-22(13)3)23-8-4-5-14(23)25/h9H,4-8H2,1-3H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239784
PNG
(US9394311, 67)
Show SMILES Cn1nc(nc1CCc1nc2cc(ccn2n1)C#N)N1CCCC1
Show InChI InChI=1S/C16H18N8/c1-22-14(19-16(21-22)23-7-2-3-8-23)5-4-13-18-15-10-12(11-17)6-9-24(15)20-13/h6,9-10H,2-5,7-8H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239845
PNG
(US9394311, 126)
Show SMILES CC(Cc1nc2c(C)ncc(C)n2n1)c1nc(nn1C)N1CCCC1
Show InChI InChI=1S/C17H24N8/c1-11(15-20-17(22-23(15)4)24-7-5-6-8-24)9-14-19-16-13(3)18-10-12(2)25(16)21-14/h10-11H,5-9H2,1-4H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239783
PNG
(US9394311, 66)
Show SMILES Cn1nc(nc1CCc1nc2cc(ccn2n1)C(F)(F)F)N1CCCC1
Show InChI InChI=1S/C16H18F3N7/c1-24-13(21-15(23-24)25-7-2-3-8-25)5-4-12-20-14-10-11(16(17,18)19)6-9-26(14)22-12/h6,9-10H,2-5,7-8H2,1H3
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n/an/a 331n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239724
PNG
(US9394311, 6)
Show SMILES CN(C)c1nc(CCc2nc3c(C)ncc(C)n3n2)n(C)n1
Show InChI InChI=1S/C14H20N8/c1-9-8-15-10(2)13-16-11(18-22(9)13)6-7-12-17-14(20(3)4)19-21(12)5/h8H,6-7H2,1-5H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239770
PNG
(US9394311, 53)
Show SMILES Cn1nc(nc1CCc1nc2ccc(cn2n1)C#N)N1CCCC1
Show InChI InChI=1S/C16H18N8/c1-22-14(19-16(21-22)23-8-2-3-9-23)7-5-13-18-15-6-4-12(10-17)11-24(15)20-13/h4,6,11H,2-3,5,7-9H2,1H3
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Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239807
PNG
(US9394311, 90)
Show SMILES Cc1cnc(C)c2nc(CCc3nc(nn3C)N3CC(F)(F)C3)nn12
Show InChI InChI=1S/C15H18F2N8/c1-9-6-18-10(2)13-19-11(21-25(9)13)4-5-12-20-14(22-23(12)3)24-7-15(16,17)8-24/h6H,4-5,7-8H2,1-3H3
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n/an/a 475n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A


(Homo sapiens (Human))
BDBM239736
PNG
(US9394311, 19)
Show SMILES COc1ccc(Cn2nc(nc2N2CCCC2)C#Cc2nc3cc(Cl)ccn3n2)cc1
Show InChI InChI=1S/C22H20ClN7O/c1-31-18-6-4-16(5-7-18)15-30-22(28-11-2-3-12-28)25-20(27-30)9-8-19-24-21-14-17(23)10-13-29(21)26-19/h4-7,10,13-14H,2-3,11-12,15H2,1H3
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n/an/a 477n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

US Patent


Assay Description
The human PDE10A full length assay was performed in 96-well micro titer plates. The reaction mixture of 50 μl contained 20 mM HEPES pH=7.5/10 mM M...


Citation and Details
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%