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Found 341 hits Enz. Inhib. hit(s) with Target = 'mGluR2 and G alpha 16'   
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
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213143
PNG
(US9278960, 8-50 | US9636337, 8-50)
Show SMILES COc1ccc(cc1F)-c1cc(nc2cc(CCc3cnc(C)nc3)ccc12)C(N)=O
Show InChI InChI=1S/C24H21FN4O2/c1-14-27-12-16(13-28-14)4-3-15-5-7-18-19(11-22(24(26)30)29-21(18)9-15)17-6-8-23(31-2)20(25)10-17/h5-13H,3-4H2,1-2H3,(H2,26,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212882
PNG
(US9278960, 2-29 | US9663506, Example 2-29)
Show SMILES Cc1ccc(cc1)-c1cc(nc2cc(CN3C(=O)CCC3=O)ccc12)C(N)=O
Show InChI InChI=1S/C22H19N3O3/c1-13-2-5-15(6-3-13)17-11-19(22(23)28)24-18-10-14(4-7-16(17)18)12-25-20(26)8-9-21(25)27/h2-7,10-11H,8-9,12H2,1H3,(H2,23,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213110
PNG
(US9278960, 8-17 | US9278960, 8-18 | US9636337, 8-1...)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(cc2n1)C(O)Cc1cccnc1
Show InChI InChI=1/C23H18FN3O2/c24-17-6-3-15(4-7-17)19-12-21(23(25)29)27-20-11-16(5-8-18(19)20)22(28)10-14-2-1-9-26-13-14/h1-9,11-13,22,28H,10H2,(H2,25,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213110
PNG
(US9278960, 8-17 | US9278960, 8-18 | US9636337, 8-1...)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(cc2n1)C(O)Cc1cccnc1
Show InChI InChI=1/C23H18FN3O2/c24-17-6-3-15(4-7-17)19-12-21(23(25)29)27-20-11-16(5-8-18(19)20)22(28)10-14-2-1-9-26-13-14/h1-9,11-13,22,28H,10H2,(H2,25,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213133
PNG
(US9278960, 8-40 | US9278960, 8-41 | US9636337, 8-4...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1cccnc1)C(N)=O
Show InChI InChI=1/C25H23N3O2/c1-16(12-17-4-3-11-27-15-17)19-7-10-21-22(18-5-8-20(30-2)9-6-18)14-24(25(26)29)28-23(21)13-19/h3-11,13-16H,12H2,1-2H3,(H2,26,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213144
PNG
(US9278960, 8-51 | US9636337, 8-51)
Show SMILES COc1cc(F)c(c(F)c1)-c1cc(nc2cc(CCc3cnc(C)nc3)ccc12)C(N)=O
Show InChI InChI=1S/C24H20F2N4O2/c1-13-28-11-15(12-29-13)4-3-14-5-6-17-18(10-22(24(27)31)30-21(17)7-14)23-19(25)8-16(32-2)9-20(23)26/h5-12H,3-4H2,1-2H3,(H2,27,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213074
PNG
(US9278960, 6-21 | US9663506, Example 6-21)
Show SMILES Cn1cc(cn1)-c1cc(nc2cc(Cc3ccnc(c3)C(F)(F)F)ccc12)C(N)=O
Show InChI InChI=1S/C21H16F3N5O/c1-29-11-14(10-27-29)16-9-18(20(25)30)28-17-7-12(2-3-15(16)17)6-13-4-5-26-19(8-13)21(22,23)24/h2-5,7-11H,6H2,1H3,(H2,25,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213104
PNG
(US9278960, 8-10 | US9278960, 8-11)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1cnc(C)nc1)C(N)=O
Show InChI InChI=1/C25H23FN4O2/c1-14(8-16-12-28-15(2)29-13-16)17-4-6-20-21(11-24(25(27)31)30-23(20)9-17)19-7-5-18(32-3)10-22(19)26/h4-7,9-14H,8H2,1-3H3,(H2,27,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213113
PNG
(US9278960, 8-20 | US9278960, 8-27 | US9278960, 8-2...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(O)Cc1ccc(Cl)nc1)C(N)=O
Show InChI InChI=1/C24H20ClN3O3/c1-31-17-6-3-15(4-7-17)19-12-21(24(26)30)28-20-11-16(5-8-18(19)20)22(29)10-14-2-9-23(25)27-13-14/h2-9,11-13,22,29H,10H2,1H3,(H2,26,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213122
PNG
(US9278960, 8-29 | US9636337, 8-29)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(CCc3cnc(C)nc3)ccc12)C(N)=O
Show InChI InChI=1S/C24H21FN4O2/c1-14-27-12-16(13-28-14)4-3-15-5-7-19-20(11-23(24(26)30)29-22(19)9-15)18-8-6-17(31-2)10-21(18)25/h5-13H,3-4H2,1-2H3,(H2,26,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213126
PNG
(US9278960, 8-33 | US9636337, 8-33)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(CCc3cnc(nc3)C#N)ccc12)C(N)=O
Show InChI InChI=1S/C24H18FN5O2/c1-32-16-5-7-17(20(25)9-16)19-10-22(24(27)31)30-21-8-14(4-6-18(19)21)2-3-15-12-28-23(11-26)29-13-15/h4-10,12-13H,2-3H2,1H3,(H2,27,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212880
PNG
(US9278960, 2-27 | US9663506, Example 2-27)
Show SMILES CC1CCC(=CC1)c1cc(nc2cc(CN3C(=O)CCC3=O)ccc12)C(N)=O
Show InChI InChI=1/C22H23N3O3/c1-13-2-5-15(6-3-13)17-11-19(22(23)28)24-18-10-14(4-7-16(17)18)12-25-20(26)8-9-21(25)27/h4-5,7,10-11,13H,2-3,6,8-9,12H2,1H3,(H2,23,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213078
PNG
(US9278960, 6-25 | US9663506, Example 6-25)
Show SMILES Cn1cc(cn1)-c1cc(nc2cc(Cc3cc(Cl)nc(c3)C(F)(F)F)ccc12)C(N)=O
Show InChI InChI=1S/C21H15ClF3N5O/c1-30-10-13(9-27-30)15-8-17(20(26)31)28-16-5-11(2-3-14(15)16)4-12-6-18(21(23,24)25)29-19(22)7-12/h2-3,5-10H,4H2,1H3,(H2,26,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213104
PNG
(US9278960, 8-10 | US9278960, 8-11)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1cnc(C)nc1)C(N)=O
Show InChI InChI=1/C25H23FN4O2/c1-14(8-16-12-28-15(2)29-13-16)17-4-6-20-21(11-24(25(27)31)30-23(20)9-17)19-7-5-18(32-3)10-22(19)26/h4-7,9-14H,8H2,1-3H3,(H2,27,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213108
PNG
(US9278960, 8-15 | US9636337, 8-15)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CCc3cncnc3)cc2n1
Show InChI InChI=1S/C22H17FN4O/c23-17-6-4-16(5-7-17)19-10-21(22(24)28)27-20-9-14(3-8-18(19)20)1-2-15-11-25-13-26-12-15/h3-13H,1-2H2,(H2,24,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213125
PNG
(US9278960, 8-32 | US9636337, 8-32)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(CCc3cnc(nc3)C#N)ccc12)C(N)=O
Show InChI InChI=1S/C24H19N5O2/c1-31-18-7-5-17(6-8-18)20-11-22(24(26)30)29-21-10-15(4-9-19(20)21)2-3-16-13-27-23(12-25)28-14-16/h4-11,13-14H,2-3H2,1H3,(H2,26,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213128
PNG
(US9278960, 8-35 | US9636337, 8-35)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(CCc3cncnc3N)ccc12)C(N)=O
Show InChI InChI=1S/C23H21N5O2/c1-30-17-7-5-15(6-8-17)19-11-21(23(25)29)28-20-10-14(3-9-18(19)20)2-4-16-12-26-13-27-22(16)24/h3,5-13H,2,4H2,1H3,(H2,25,29)(H2,24,26,27)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212892
PNG
(US9278960, 2-39 | US9663506, Example 2-39)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(CN3C(=O)CCC3=O)ccc12)C(N)=O
Show InChI InChI=1S/C22H18FN3O4/c1-30-13-3-5-14(17(23)9-13)16-10-19(22(24)29)25-18-8-12(2-4-15(16)18)11-26-20(27)6-7-21(26)28/h2-5,8-10H,6-7,11H2,1H3,(H2,24,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213006
PNG
(US9278960, 4-90 | US9663506, Example 4-90)
Show SMILES C[C@@H]1CO[C@H](CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1cnn(C)c1)C(F)(F)F
Show InChI InChI=1/C21H22F3N5O2/c1-12-11-31-19(21(22,23)24)10-29(12)8-13-3-4-15-16(14-7-26-28(2)9-14)6-18(20(25)30)27-17(15)5-13/h3-7,9,12,19H,8,10-11H2,1-2H3,(H2,25,30)/t12-,19-/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213007
PNG
(US9278960, 4-91 | US9663506, Example 4-91)
Show SMILES C[C@H]1CO[C@H](CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1cnn(C)c1)C(F)(F)F
Show InChI InChI=1/C21H22F3N5O2/c1-12-11-31-19(21(22,23)24)10-29(12)8-13-3-4-15-16(14-7-26-28(2)9-14)6-18(20(25)30)27-17(15)5-13/h3-7,9,12,19H,8,10-11H2,1-2H3,(H2,25,30)/t12-,19+/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213012
PNG
(US9278960, 4-96 | US9663506, Example 4-96)
Show SMILES Cn1cc(cn1)-c1cc(nc2cc(CN3C[C@@H](OCC3(C)C)C(F)(F)F)ccc12)C(N)=O
Show InChI InChI=1/C22H24F3N5O2/c1-21(2)12-32-19(22(23,24)25)11-30(21)9-13-4-5-15-16(14-8-27-29(3)10-14)7-18(20(26)31)28-17(15)6-13/h4-8,10,19H,9,11-12H2,1-3H3,(H2,26,31)/t19-/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213051
PNG
(US9278960, 4-135 | US9663506, Example 4-135)
Show SMILES C[C@@H]1CN(Cc2ccc3c(cc(nc3c2)C(N)=O)-c2cn(C)nc2C)C[C@@H](O1)C(F)(F)F
Show InChI InChI=1/C22H24F3N5O2/c1-12-8-30(11-20(32-12)22(23,24)25)9-14-4-5-15-16(17-10-29(3)28-13(17)2)7-19(21(26)31)27-18(15)6-14/h4-7,10,12,20H,8-9,11H2,1-3H3,(H2,26,31)/t12-,20-/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213060
PNG
(US9278960, 6-7 | US9663506, Example 6-7)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(Cc3ccnc(CO)c3)cc2n1
Show InChI InChI=1S/C23H18FN3O2/c24-17-4-2-16(3-5-17)20-12-22(23(25)29)27-21-11-14(1-6-19(20)21)9-15-7-8-26-18(10-15)13-28/h1-8,10-12,28H,9,13H2,(H2,25,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213091
PNG
(US9278960, 7-29 | US9636337, 7-29)
Show SMILES CCC(O)(c1cn(Cc2ccc3c(cc(nc3c2F)C(N)=O)-c2ccc(OC)cc2F)cn1)C(F)(F)F
Show InChI InChI=1/C25H21F5N4O3/c1-3-24(36,25(28,29)30)20-11-34(12-32-20)10-13-4-6-16-17(15-7-5-14(37-2)8-18(15)26)9-19(23(31)35)33-22(16)21(13)27/h4-9,11-12,36H,3,10H2,1-2H3,(H2,31,35)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213127
PNG
(US9278960, 8-34 | US9636337, 8-34)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1cnc(nc1)C#N)C(N)=O
Show InChI InChI=1/C25H21N5O2/c1-15(9-16-13-28-24(12-26)29-14-16)18-5-8-20-21(17-3-6-19(32-2)7-4-17)11-23(25(27)31)30-22(20)10-18/h3-8,10-11,13-15H,9H2,1-2H3,(H2,27,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213137
PNG
(US9278960, 8-44 | US9278960, 8-45 | US9636337, 8-4...)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1cccnc1)C(N)=O
Show InChI InChI=1/C25H22FN3O2/c1-15(10-16-4-3-9-28-14-16)17-5-7-20-21(13-24(25(27)30)29-23(20)11-17)19-8-6-18(31-2)12-22(19)26/h3-9,11-15H,10H2,1-2H3,(H2,27,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213139
PNG
(US9278960, 8-46 | US9278960, 8-47 | US9636337, 8-4...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1ccc(CF)nc1)C(N)=O
Show InChI InChI=1/C26H24FN3O2/c1-16(11-17-3-7-20(14-27)29-15-17)19-6-10-22-23(18-4-8-21(32-2)9-5-18)13-25(26(28)31)30-24(22)12-19/h3-10,12-13,15-16H,11,14H2,1-2H3,(H2,28,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212860
PNG
(US9278960, 2-7 | US9663506, Example 2-7)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CN3C(=O)CCC3=O)cc2n1
Show InChI InChI=1S/C21H16FN3O3/c22-14-4-2-13(3-5-14)16-10-18(21(23)28)24-17-9-12(1-6-15(16)17)11-25-19(26)7-8-20(25)27/h1-6,9-10H,7-8,11H2,(H2,23,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212937
PNG
(US9278960, 4-22-A | US9278960, 4-22-B)
Show SMILES C[C@H]1CNC(CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1ccc(F)cc1)C(F)(F)F
Show InChI InChI=1/C23H22F4N4O/c1-13-10-29-21(23(25,26)27)12-31(13)11-14-2-7-17-18(15-3-5-16(24)6-4-15)9-20(22(28)32)30-19(17)8-14/h2-9,13,21,29H,10-12H2,1H3,(H2,28,32)/t13-,21?/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212967
PNG
(US9278960, 4-51 | US9663506, Example 4-51)
Show SMILES Cc1ncc(s1)-c1cc(nc2cc(CN3CCOC(C3)C(F)(F)F)ccc12)C(N)=O
Show InChI InChI=1/C20H19F3N4O2S/c1-11-25-8-17(30-11)14-7-16(19(24)28)26-15-6-12(2-3-13(14)15)9-27-4-5-29-18(10-27)20(21,22)23/h2-3,6-8,18H,4-5,9-10H2,1H3,(H2,24,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213002
PNG
(US9278960, 4-86 | US9663506, Example 4-86)
Show SMILES NC(=O)c1cc(-c2cnn(CF)c2)c2ccc(CN3CCO[C@H](C3)C(F)(F)F)cc2n1
Show InChI InChI=1/C20H19F4N5O2/c21-11-29-9-13(7-26-29)15-6-17(19(25)30)27-16-5-12(1-2-14(15)16)8-28-3-4-31-18(10-28)20(22,23)24/h1-2,5-7,9,18H,3-4,8,10-11H2,(H2,25,30)/t18-/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213123
PNG
(US9278960, 8-30 | US9636337, 8-30)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(CCc3cccnc3N)ccc12)C(N)=O
Show InChI InChI=1S/C24H22N4O2/c1-30-18-9-7-16(8-10-18)20-14-22(24(26)29)28-21-13-15(5-11-19(20)21)4-6-17-3-2-12-27-23(17)25/h2-3,5,7-14H,4,6H2,1H3,(H2,25,27)(H2,26,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213124
PNG
(US9278960, 8-31 | US9636337, 8-31)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(CCc3cccnc3N)ccc12)C(N)=O
Show InChI InChI=1S/C24H21FN4O2/c1-31-16-7-9-17(20(25)12-16)19-13-22(24(27)30)29-21-11-14(5-8-18(19)21)4-6-15-3-2-10-28-23(15)26/h2-3,5,7-13H,4,6H2,1H3,(H2,26,28)(H2,27,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213141
PNG
(US9278960, 8-48 | US9278960, 8-49 | US9636337, 8-4...)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1ccc(CF)nc1)C(N)=O
Show InChI InChI=1/C26H23F2N3O2/c1-15(9-16-3-5-18(13-27)30-14-16)17-4-7-21-22(12-25(26(29)32)31-24(21)10-17)20-8-6-19(33-2)11-23(20)28/h3-8,10-12,14-15H,9,13H2,1-2H3,(H2,29,32)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212932
PNG
(US9278960, 3-51 | US9663506, Example 3-51)
Show SMILES CCC(O)(c1cn(Cc2ccc3c(cc(nc3c2)C(N)=O)-c2ccc(OC)cc2)cn1)C(F)(F)F
Show InChI InChI=1/C25H23F3N4O3/c1-3-24(34,25(26,27)28)22-13-32(14-30-22)12-15-4-9-18-19(16-5-7-17(35-2)8-6-16)11-21(23(29)33)31-20(18)10-15/h4-11,13-14,34H,3,12H2,1-2H3,(H2,29,33)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213017
PNG
(US9278960, 4-101 | US9278960, 4-102 | US9663506, E...)
Show SMILES C[C@@H]1CNC(CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1ccc(F)cc1)C(F)(F)F
Show InChI InChI=1/C23H22F4N4O/c1-13-10-29-21(23(25,26)27)12-31(13)11-14-2-7-17-18(15-3-5-16(24)6-4-15)9-20(22(28)32)30-19(17)8-14/h2-9,13,21,29H,10-12H2,1H3,(H2,28,32)/t13-,21?/s2
PDB

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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213017
PNG
(US9278960, 4-101 | US9278960, 4-102 | US9663506, E...)
Show SMILES C[C@@H]1CNC(CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1ccc(F)cc1)C(F)(F)F
Show InChI InChI=1/C23H22F4N4O/c1-13-10-29-21(23(25,26)27)12-31(13)11-14-2-7-17-18(15-3-5-16(24)6-4-15)9-20(22(28)32)30-19(17)8-14/h2-9,13,21,29H,10-12H2,1H3,(H2,28,32)/t13-,21?/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213062
PNG
(US9278960, 6-11 | US9278960, 6-9 | US9663506, Exam...)
Show SMILES COc1ncc(Cc2ccc3c(cc(nc3c2)C(N)=O)-c2ccc(F)cc2)cn1
Show InChI InChI=1S/C22H17FN4O2/c1-29-22-25-11-14(12-26-22)8-13-2-7-17-18(15-3-5-16(23)6-4-15)10-20(21(24)28)27-19(17)9-13/h2-7,9-12H,8H2,1H3,(H2,24,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213085
PNG
(US9278960, 7-23 | US9636337, 7-23)
Show SMILES COc1ncc(Cc2ccc3c(cc(nc3c2F)C(N)=O)-c2ccc(F)cc2)cn1
Show InChI InChI=1S/C22H16F2N4O2/c1-30-22-26-10-12(11-27-22)8-14-4-7-16-17(13-2-5-15(23)6-3-13)9-18(21(25)29)28-20(16)19(14)24/h2-7,9-11H,8H2,1H3,(H2,25,29)
PDB

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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213090
PNG
(US9278960, 7-28 | US9636337, 7-28)
Show SMILES CCC(O)(c1cn(Cc2ccc3c(cc(nc3c2F)C(N)=O)-c2ccc(OC)c(F)c2)cn1)C(F)(F)F
Show InChI InChI=1/C25H21F5N4O3/c1-3-24(36,25(28,29)30)20-11-34(12-32-20)10-14-4-6-15-16(13-5-7-19(37-2)17(26)8-13)9-18(23(31)35)33-22(15)21(14)27/h4-9,11-12,36H,3,10H2,1-2H3,(H2,31,35)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213101
PNG
(US9278960, 8-1 | US9636337, 8-1)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(cc2n1)[C@@H](O)Cc1ccc(Cl)nc1
Show InChI InChI=1/C23H17ClFN3O2/c24-22-8-1-13(12-27-22)9-21(29)15-4-7-17-18(14-2-5-16(25)6-3-14)11-20(23(26)30)28-19(17)10-15/h1-8,10-12,21,29H,9H2,(H2,26,30)/t21-/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213109
PNG
(US9278960, 8-16 | US9636337, 8-16)
Show SMILES NC(=O)c1cc(-c2ccc(F)cc2)c2ccc(CCc3cccnc3)cc2n1
Show InChI InChI=1S/C23H18FN3O/c24-18-8-6-17(7-9-18)20-13-22(23(25)28)27-21-12-15(5-10-19(20)21)3-4-16-2-1-11-26-14-16/h1-2,5-14H,3-4H2,(H2,25,28)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213133
PNG
(US9278960, 8-40 | US9278960, 8-41 | US9636337, 8-4...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1cccnc1)C(N)=O
Show InChI InChI=1/C25H23N3O2/c1-16(12-17-4-3-11-27-15-17)19-7-10-21-22(18-5-8-20(30-2)9-6-18)14-24(25(26)29)28-23(21)13-19/h3-11,13-16H,12H2,1-2H3,(H2,26,29)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213135
PNG
(US9278960, 8-42 | US9278960, 8-43 | US9636337, 8-4...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1ccc(C)nc1)C(N)=O
Show InChI InChI=1/C26H25N3O2/c1-16(12-18-5-4-17(2)28-15-18)20-8-11-22-23(19-6-9-21(31-3)10-7-19)14-25(26(27)30)29-24(22)13-20/h4-11,13-16H,12H2,1-3H3,(H2,27,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213137
PNG
(US9278960, 8-44 | US9278960, 8-45 | US9636337, 8-4...)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1cccnc1)C(N)=O
Show InChI InChI=1/C25H22FN3O2/c1-15(10-16-4-3-9-28-14-16)17-5-7-20-21(13-24(25(27)30)29-23(20)11-17)19-8-6-18(31-2)12-22(19)26/h3-9,11-15H,10H2,1-2H3,(H2,27,30)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213139
PNG
(US9278960, 8-46 | US9278960, 8-47 | US9636337, 8-4...)
Show SMILES COc1ccc(cc1)-c1cc(nc2cc(ccc12)C(C)Cc1ccc(CF)nc1)C(N)=O
Show InChI InChI=1/C26H24FN3O2/c1-16(11-17-3-7-20(14-27)29-15-17)19-6-10-22-23(18-4-8-21(32-2)9-5-18)13-25(26(28)31)30-24(22)12-19/h3-10,12-13,15-16H,11,14H2,1-2H3,(H2,28,31)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213141
PNG
(US9278960, 8-48 | US9278960, 8-49 | US9636337, 8-4...)
Show SMILES COc1ccc(c(F)c1)-c1cc(nc2cc(ccc12)C(C)Cc1ccc(CF)nc1)C(N)=O
Show InChI InChI=1/C26H23F2N3O2/c1-15(9-16-3-5-18(13-27)30-14-16)17-4-7-21-22(12-25(26(29)32)31-24(21)10-17)20-8-6-19(33-2)11-23(20)28/h3-8,10-12,14-15H,9,13H2,1-2H3,(H2,29,32)
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212934
PNG
(US9278960, 4-9 | US9663506, Example 4-9)
Show SMILES C[C@@H]1CN(Cc2ccc3c(cc(nc3c2)C(N)=O)-c2cnn(C)c2)C[C@@H](O1)C(F)(F)F
Show InChI InChI=1/C21H22F3N5O2/c1-12-8-29(11-19(31-12)21(22,23)24)9-13-3-4-15-16(14-7-26-28(2)10-14)6-18(20(25)30)27-17(15)5-13/h3-7,10,12,19H,8-9,11H2,1-2H3,(H2,25,30)/t12-,19-/s2
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n/an/a 11n/an/an/an/an/an/a



Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM212937
PNG
(US9278960, 4-22-A | US9278960, 4-22-B)
Show SMILES C[C@H]1CNC(CN1Cc1ccc2c(cc(nc2c1)C(N)=O)-c1ccc(F)cc1)C(F)(F)F
Show InChI InChI=1/C23H22F4N4O/c1-13-10-29-21(23(25,26)27)12-31(13)11-14-2-7-17-18(15-3-5-16(24)6-4-15)9-20(22(28)32)30-19(17)8-14/h2-9,13,21,29H,10-12H2,1H3,(H2,28,32)/t13-,21?/s2
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
mGluR2 and G alpha 16


(Homo sapiens (Human))
BDBM213000
PNG
(US9278960, 4-84 | US9663506, Example 4-84)
Show SMILES NC(=O)c1cc(-c2cnn(c2)C(F)F)c2ccc(CN3CCOC(C3)C(F)(F)F)cc2n1
Show InChI InChI=1/C20H18F5N5O2/c21-19(22)30-9-12(7-27-30)14-6-16(18(26)31)28-15-5-11(1-2-13(14)15)8-29-3-4-32-17(10-29)20(23,24)25/h1-2,5-7,9,17,19H,3-4,8,10H2,(H2,26,31)
PDB

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Merck Sharp & Dohme Corp.

US Patent


Assay Description
The utility of the compounds in accordance with the present invention as antagonists of metabotropic glutamate receptor activity, in particular mGluR...


Citation and Details
More data for this
Ligand-Target Pair
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