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Found 1401 hits Enz. Inhib. hit(s) with Target = 'Phosphodiesterase Type 10 (PDE10A)'   
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
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14754
PNG
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)
Show SMILES COc1ccc(Cc2nccc3cc(OC)c(OC)cc23)cc1OC
Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3
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17 -43.9n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14755
PNG
(6,7-dimethoxy-4-[8-(4-methylpiperazin-1-yl)sulfony...)
Show SMILES COc1cc2ncnc(N3CCc4cccc(c4C3)S(=O)(=O)N3CCN(C)CC3)c2cc1OC
Show InChI InChI=1S/C24H29N5O4S/c1-27-9-11-29(12-10-27)34(30,31)23-6-4-5-17-7-8-28(15-19(17)23)24-18-13-21(32-2)22(33-3)14-20(18)25-16-26-24/h4-6,13-14,16H,7-12,15H2,1-3H3
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25 -43.0n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14748
PNG
((R)-4-[3-(4-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Show SMILES CCOc1ccc(O[C@@H]2CCN(C2)c2ncnc3cc(OC)c(OC)cc23)cc1
Show InChI InChI=1S/C22H25N3O4/c1-4-28-15-5-7-16(8-6-15)29-17-9-10-25(13-17)22-18-11-20(26-2)21(27-3)12-19(18)23-14-24-22/h5-8,11-12,14,17H,4,9-10,13H2,1-3H3/t17-/m1/s1
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54 -41.1n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14745
PNG
((R)-4-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidi...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc(cc3)C#N)c2cc1OC
Show InChI InChI=1S/C21H20N4O3/c1-26-19-9-17-18(10-20(19)27-2)23-13-24-21(17)25-8-7-16(12-25)28-15-5-3-14(11-22)4-6-15/h3-6,9-10,13,16H,7-8,12H2,1-2H3/t16-/m1/s1
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56 -41.0n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14753
PNG
((R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-...)
Show SMILES COc1ccc(O[C@@H]2CCN(C2)c2ncnc3cc(OC)c(OC)cc23)cc1OC
Show InChI InChI=1S/C22H25N3O5/c1-26-18-6-5-14(9-19(18)27-2)30-15-7-8-25(12-15)22-16-10-20(28-3)21(29-4)11-17(16)23-13-24-22/h5-6,9-11,13,15H,7-8,12H2,1-4H3/t15-/m1/s1
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67 -40.5n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14752
PNG
((R)-4-[3-(Indan-5-yloxy)-pyrrolidin-1-yl]-6,7-dime...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc4CCCc4c3)c2cc1OC
Show InChI InChI=1S/C23H25N3O3/c1-27-21-11-19-20(12-22(21)28-2)24-14-25-23(19)26-9-8-18(13-26)29-17-7-6-15-4-3-5-16(15)10-17/h6-7,10-12,14,18H,3-5,8-9,13H2,1-2H3/t18-/m1/s1
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68 -40.5n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14751
PNG
((R)-4-[3-(3-Ethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Show SMILES CCOc1cccc(O[C@@H]2CCN(C2)c2ncnc3cc(OC)c(OC)cc23)c1
Show InChI InChI=1S/C22H25N3O4/c1-4-28-15-6-5-7-16(10-15)29-17-8-9-25(13-17)22-18-11-20(26-2)21(27-3)12-19(18)23-14-24-22/h5-7,10-12,14,17H,4,8-9,13H2,1-3H3/t17-/m1/s1
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94 -39.7n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14747
PNG
((R)-4-[3-(4-tert-Butyl-phenoxy)-pyrrolidin-1-yl]-6...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc(cc3)C(C)(C)C)c2cc1OC
Show InChI InChI=1S/C24H29N3O3/c1-24(2,3)16-6-8-17(9-7-16)30-18-10-11-27(14-18)23-19-12-21(28-4)22(29-5)13-20(19)25-15-26-23/h6-9,12-13,15,18H,10-11,14H2,1-5H3/t18-/m1/s1
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100 -39.6n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14744
PNG
((R)-2-[1-(6,7-Dimethoxy-quinazolin-4-yl)-pyrrolidi...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccccc3C#N)c2cc1OC
Show InChI InChI=1S/C21H20N4O3/c1-26-19-9-16-17(10-20(19)27-2)23-13-24-21(16)25-8-7-15(12-25)28-18-6-4-3-5-14(18)11-22/h3-6,9-10,13,15H,7-8,12H2,1-2H3/t15-/m1/s1
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130 -38.9n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14750
PNG
((R)-4-[3-(Biphenyl-3-yloxy)-pyrrolidin-1-yl]-6,7-d...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3cccc(c3)-c3ccccc3)c2cc1OC
Show InChI InChI=1S/C26H25N3O3/c1-30-24-14-22-23(15-25(24)31-2)27-17-28-26(22)29-12-11-21(16-29)32-20-10-6-9-19(13-20)18-7-4-3-5-8-18/h3-10,13-15,17,21H,11-12,16H2,1-2H3/t21-/m1/s1
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136 -38.8n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14749
PNG
((R)-4-[3-(3-Isopropyl-phenoxy)-pyrrolidin-1-yl]-6,...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3cccc(c3)C(C)C)c2cc1OC
Show InChI InChI=1S/C23H27N3O3/c1-15(2)16-6-5-7-17(10-16)29-18-8-9-26(13-18)23-19-11-21(27-3)22(28-4)12-20(19)24-14-25-23/h5-7,10-12,14-15,18H,8-9,13H2,1-4H3/t18-/m1/s1
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171 -38.2n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14746
PNG
((R)-6,7-Dimethoxy-4-[3-(4-trifluoromethoxy-phenoxy...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc(OC(F)(F)F)cc3)c2cc1OC
Show InChI InChI=1S/C21H20F3N3O4/c1-28-18-9-16-17(10-19(18)29-2)25-12-26-20(16)27-8-7-15(11-27)30-13-3-5-14(6-4-13)31-21(22,23)24/h3-6,9-10,12,15H,7-8,11H2,1-2H3/t15-/m1/s1
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185 -38.0n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14743
PNG
((R)-4-[3-(2-Chloro-phenoxy)-pyrrolidin-1-yl]-6,7-d...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccccc3Cl)c2cc1OC
Show InChI InChI=1S/C20H20ClN3O3/c1-25-18-9-14-16(10-19(18)26-2)22-12-23-20(14)24-8-7-13(11-24)27-17-6-4-3-5-15(17)21/h3-6,9-10,12-13H,7-8,11H2,1-2H3/t13-/m1/s1
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198 -37.9n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14741
PNG
((R)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrroli...)
Show SMILES COc1ccccc1O[C@@H]1CCN(C1)c1ncnc2cc(OC)c(OC)cc12
Show InChI InChI=1S/C21H23N3O4/c1-25-17-6-4-5-7-18(17)28-14-8-9-24(12-14)21-15-10-19(26-2)20(27-3)11-16(15)22-13-23-21/h4-7,10-11,13-14H,8-9,12H2,1-3H3/t14-/m1/s1
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240 -37.4n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14740
PNG
((R)-6,7-Dimethoxy-4-(3-o-tolyloxy-pyrrolidin-1-yl)...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccccc3C)c2cc1OC
Show InChI InChI=1S/C21H23N3O3/c1-14-6-4-5-7-18(14)27-15-8-9-24(12-15)21-16-10-19(25-2)20(26-3)11-17(16)22-13-23-21/h4-7,10-11,13,15H,8-9,12H2,1-3H3/t15-/m1/s1
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326 -36.7n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14742
PNG
((S)-6,7-Dimethoxy-4-[3-(2-methoxy-phenoxy)-pyrroli...)
Show SMILES COc1ccccc1O[C@H]1CCN(C1)c1ncnc2cc(OC)c(OC)cc12
Show InChI InChI=1S/C21H23N3O4/c1-25-17-6-4-5-7-18(17)28-14-8-9-24(12-14)21-15-10-19(26-2)20(27-3)11-16(15)22-13-23-21/h4-7,10-11,13-14H,8-9,12H2,1-3H3/t14-/m0/s1
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641 -35.0n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14739
PNG
((R)-6,7-Dimethoxy-4-[3-(2-trifluoromethyl-phenoxy)...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccccc3C(F)(F)F)c2cc1OC
Show InChI InChI=1S/C21H20F3N3O3/c1-28-18-9-14-16(10-19(18)29-2)25-12-26-20(14)27-8-7-13(11-27)30-17-6-4-3-5-15(17)21(22,23)24/h3-6,9-10,12-13H,7-8,11H2,1-2H3/t13-/m1/s1
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811 -34.4n/an/an/an/an/a7.522



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31607
PNG
(methyl substituted pyrazole, 28)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2nc3ccccn3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C22H18N6O/c1-27-14-19(16-9-11-23-12-10-16)22(26-27)17-5-7-18(8-6-17)29-15-20-24-21-4-2-3-13-28(21)25-20/h2-14H,15H2,1H3
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n/an/a 3.40n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31595
PNG
(substituted pyrazole, 12)
Show SMILES CCn1ncc(c1-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C26H22N4O/c1-2-30-26(24(17-28-30)19-13-15-27-16-14-19)21-8-11-23(12-9-21)31-18-22-10-7-20-5-3-4-6-25(20)29-22/h3-17H,2,18H2,1H3
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n/an/a 4.76n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31606
PNG
(methyl substituted pyrazole, 27)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2cn3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C23H19N5O/c1-27-15-21(17-9-11-24-12-10-17)23(26-27)18-5-7-20(8-6-18)29-16-19-14-28-13-3-2-4-22(28)25-19/h2-15H,16H2,1H3
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n/an/a 0.790n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31605
PNG
(methyl substituted pyrazole, 26)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2nc3ccccc3n2C)cc1)-c1ccncc1
Show InChI InChI=1S/C24H21N5O/c1-28-15-20(17-11-13-25-14-12-17)24(27-28)18-7-9-19(10-8-18)30-16-23-26-21-5-3-4-6-22(21)29(23)2/h3-15H,16H2,1-2H3
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n/an/a 1.29n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31604
PNG
(methyl substituted pyrazole, 25)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2cnc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C24H19N5O/c1-29-15-21(17-10-12-25-13-11-17)24(28-29)18-6-8-20(9-7-18)30-16-19-14-26-22-4-2-3-5-23(22)27-19/h2-15H,16H2,1H3
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n/an/a 5.09n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31603
PNG
(pyrazole, 20)
Show SMILES Cc1cc(on1)-c1c[nH]nc1-c1ccc(OCc2ccc3ccccc3n2)cc1
Show InChI InChI=1S/C23H18N4O2/c1-15-12-22(29-27-15)20-13-24-26-23(20)17-7-10-19(11-8-17)28-14-18-9-6-16-4-2-3-5-21(16)25-18/h2-13H,14H2,1H3,(H,24,26)
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n/an/a 413n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31602
PNG
(pyrazole, 19)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1-c1ccccn1)c1ccc2ccccc2n1
Show InChI InChI=1S/C24H18N4O/c1-2-6-22-17(5-1)8-11-19(27-22)16-29-20-12-9-18(10-13-20)24-21(15-26-28-24)23-7-3-4-14-25-23/h1-15H,16H2,(H,26,28)
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n/an/a 371n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31601
PNG
(pyrazole, 18)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1-c1ccccc1)c1ccc2ccccc2n1
Show InChI InChI=1S/C25H19N3O/c1-2-6-18(7-3-1)23-16-26-28-25(23)20-11-14-22(15-12-20)29-17-21-13-10-19-8-4-5-9-24(19)27-21/h1-16H,17H2,(H,26,28)
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n/an/a 258n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31600
PNG
(pyrazole, 17)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1-c1ccnnc1)c1ccc2ccccc2n1
Show InChI InChI=1S/C23H17N5O/c1-2-4-22-16(3-1)5-8-19(27-22)15-29-20-9-6-17(7-10-20)23-21(14-26-28-23)18-11-12-24-25-13-18/h1-14H,15H2,(H,26,28)
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n/an/a 11.9n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31599
PNG
(pyrazole, 16)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1-c1ccncn1)c1ccc2ccccc2n1
Show InChI InChI=1S/C23H17N5O/c1-2-4-21-16(3-1)5-8-18(27-21)14-29-19-9-6-17(7-10-19)23-20(13-26-28-23)22-11-12-24-15-25-22/h1-13,15H,14H2,(H,26,28)
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n/an/a 27.2n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31598
PNG
(pyrimidine, 15)
Show SMILES Cc1ncc(-c2ccncc2)c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1
Show InChI InChI=1S/C26H20N4O/c1-18-28-16-24(19-12-14-27-15-13-19)26(29-18)21-7-10-23(11-8-21)31-17-22-9-6-20-4-2-3-5-25(20)30-22/h2-16H,17H2,1H3
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n/an/a 1.69E+3n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31597
PNG
(isoxazole, 14)
Show SMILES C(Oc1ccc(cc1)-c1oncc1-c1ccncc1)c1ccc2ccccc2n1
Show InChI InChI=1S/C24H17N3O2/c1-2-4-23-18(3-1)5-8-20(27-23)16-28-21-9-6-19(7-10-21)24-22(15-26-29-24)17-11-13-25-14-12-17/h1-15H,16H2
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n/an/a 11.7n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31596
PNG
(substituted pyrazole, 13)
Show SMILES FC(F)(F)Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C26H19F3N4O/c27-26(28,29)17-33-15-23(18-11-13-30-14-12-18)25(32-33)20-6-9-22(10-7-20)34-16-21-8-5-19-3-1-2-4-24(19)31-21/h1-15H,16-17H2
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n/an/a 1.41n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31589
PNG
(triaryl imidazole, 1)
Show SMILES COc1ccc(cc1)-c1nc([nH]c1-c1ccc(OC)cc1)-c1cccs1
Show InChI InChI=1S/C21H18N2O2S/c1-24-16-9-5-14(6-10-16)19-20(15-7-11-17(25-2)12-8-15)23-21(22-19)18-4-3-13-26-18/h3-13H,1-2H3,(H,22,23)
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n/an/a 35n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31590
PNG
(pyrazole, 2)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1Cc1ccncc1)c1ccc2ccccc2n1
Show InChI InChI=1S/C25H20N4O/c1-2-4-24-19(3-1)5-8-22(28-24)17-30-23-9-6-20(7-10-23)25-21(16-27-29-25)15-18-11-13-26-14-12-18/h1-14,16H,15,17H2,(H,27,29)
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n/an/a 11.5n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31591
PNG
(pyrazole, 3)
Show SMILES C(Oc1ccc(cc1)-c1n[nH]cc1-c1ccncc1)c1ccc2ccccc2n1
Show InChI InChI=1S/C24H18N4O/c1-2-4-23-18(3-1)5-8-20(27-23)16-29-21-9-6-19(7-10-21)24-22(15-26-28-24)17-11-13-25-14-12-17/h1-15H,16H2,(H,26,28)
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n/an/a 0.420n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31592
PNG
(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3
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n/an/a 0.370n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31593
PNG
(substituted pyrazole, 10)
Show SMILES Cn1ncc(c1-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C25H20N4O/c1-29-25(23(16-27-29)18-12-14-26-15-13-18)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)28-21/h2-16H,17H2,1H3
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n/an/a 1.54n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31594
PNG
(substituted pyrazole, 11)
Show SMILES CCn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C26H22N4O/c1-2-30-17-24(19-13-15-27-16-14-19)26(29-30)21-8-11-23(12-9-21)31-18-22-10-7-20-5-3-4-6-25(20)28-22/h3-17H,2,18H2,1H3
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n/an/a 0.920n/an/an/an/a7.523



Pfizer



Assay Description
PDE activity was measured using a plate-based Scintillation Proximity Assay (SPA). For competitive enzyme inhibition assays, the substrate [3H]cAMP c...


J Med Chem 52: 5188-96 (2009)


Article DOI: 10.1021/jm900521k
BindingDB Entry DOI: 10.7270/Q290223B
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM31592
PNG
(PF-2545920 | US9138494, MP-10 | substituted pyraz...)
Show SMILES Cn1cc(c(n1)-c1ccc(OCc2ccc3ccccc3n2)cc1)-c1ccncc1
Show InChI InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3
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0.170n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatum


J Med Chem 55: 4776-87 (2012)


Article DOI: 10.1021/jm3002372
BindingDB Entry DOI: 10.7270/Q2WM1FFG
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM50365964
PNG
(CHEMBL1956235 | CHEMBL2070530)
Show SMILES COc1cc2nncc(-c3cnc(NC(C)C)c(C)c3)c2cc1OC
Show InChI InChI=1S/C19H22N4O2/c1-11(2)22-19-12(3)6-13(9-20-19)15-10-21-23-16-8-18(25-5)17(24-4)7-14(15)16/h6-11H,1-5H3,(H,20,22)
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1.18n/an/an/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Displacement of [3H]5-(6,7-dimethoxycinnolin-4-yl)-N-isopropyl-3-methylpyridin-2-amine from PDE10A in Sprague-Dawley rat striatum


J Med Chem 55: 4776-87 (2012)


Article DOI: 10.1021/jm3002372
BindingDB Entry DOI: 10.7270/Q2WM1FFG
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14768
PNG
((R)-6,7-Dimethoxy-4-[3-(quinoxalin-2-yloxy)-pyrrol...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3cnc4ccccc4n3)c2cc1OC
Show InChI InChI=1S/C22H21N5O3/c1-28-19-9-15-18(10-20(19)29-2)24-13-25-22(15)27-8-7-14(12-27)30-21-11-23-16-5-3-4-6-17(16)26-21/h3-6,9-11,13-14H,7-8,12H2,1-2H3/t14-/m1/s1
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4n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14766
PNG
((R)-6,7-Dimethoxy-4-[3-(quinolin-7-yloxy)-pyrrolid...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc4cccnc4c3)c2cc1OC
Show InChI InChI=1S/C23H22N4O3/c1-28-21-11-18-20(12-22(21)29-2)25-14-26-23(18)27-9-7-17(13-27)30-16-6-5-15-4-3-8-24-19(15)10-16/h3-6,8,10-12,14,17H,7,9,13H2,1-2H3/t17-/m1/s1
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12n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14760
PNG
((R)-6,7-Dimethoxy-4-[3-(naphthalen-2-yloxy)-pyrrol...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc4ccccc4c3)c2cc1OC
Show InChI InChI=1S/C24H23N3O3/c1-28-22-12-20-21(13-23(22)29-2)25-15-26-24(20)27-10-9-19(14-27)30-18-8-7-16-5-3-4-6-17(16)11-18/h3-8,11-13,15,19H,9-10,14H2,1-2H3/t19-/m1/s1
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12n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14764
PNG
((R)-6,7-Dimethoxy-4-[3-(quinolin-6-yloxy)-pyrrolid...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc4ncccc4c3)c2cc1OC
Show InChI InChI=1S/C23H22N4O3/c1-28-21-11-18-20(12-22(21)29-2)25-14-26-23(18)27-9-7-17(13-27)30-16-5-6-19-15(10-16)4-3-8-24-19/h3-6,8,10-12,14,17H,7,9,13H2,1-2H3/t17-/m1/s1
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12n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14763
PNG
((R)-6,7-Dimethoxy-4-[3-(7-methoxy-naphthalen-2-ylo...)
Show SMILES COc1ccc2ccc(O[C@@H]3CCN(C3)c3ncnc4cc(OC)c(OC)cc34)cc2c1
Show InChI InChI=1S/C25H25N3O4/c1-29-18-6-4-16-5-7-19(11-17(16)10-18)32-20-8-9-28(14-20)25-21-12-23(30-2)24(31-3)13-22(21)26-15-27-25/h4-7,10-13,15,20H,8-9,14H2,1-3H3/t20-/m1/s1
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17n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14765
PNG
((R)-6,7-Dimethoxy-4-[3-(2-methyl-quinolin-6-yloxy)...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccc4nc(C)ccc4c3)c2cc1OC
Show InChI InChI=1S/C24H24N4O3/c1-15-4-5-16-10-17(6-7-20(16)27-15)31-18-8-9-28(13-18)24-19-11-22(29-2)23(30-3)12-21(19)25-14-26-24/h4-7,10-12,14,18H,8-9,13H2,1-3H3/t18-/m1/s1
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18n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14762
PNG
((R)-6,7-Dimethoxy-4-[3-(6-methoxy-naphthalen-2-ylo...)
Show SMILES COc1ccc2cc(O[C@@H]3CCN(C3)c3ncnc4cc(OC)c(OC)cc34)ccc2c1
Show InChI InChI=1S/C25H25N3O4/c1-29-18-6-4-17-11-19(7-5-16(17)10-18)32-20-8-9-28(14-20)25-21-12-23(30-2)24(31-3)13-22(21)26-15-27-25/h4-7,10-13,15,20H,8-9,14H2,1-3H3/t20-/m1/s1
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18n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14767
PNG
((R)-4-[3-(Isoquinolin-3-yloxy)-pyrrolidin-1-yl]-6,...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3cc4ccccc4cn3)c2cc1OC
Show InChI InChI=1S/C23H22N4O3/c1-28-20-10-18-19(11-21(20)29-2)25-14-26-23(18)27-8-7-17(13-27)30-22-9-15-5-3-4-6-16(15)12-24-22/h3-6,9-12,14,17H,7-8,13H2,1-2H3/t17-/m1/s1
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19n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14756
PNG
((R)-4-[3-(5-Chloro-pyrimidin-2-yloxy)-pyrrolidin-1...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ncc(Cl)cn3)c2cc1OC
Show InChI InChI=1S/C18H18ClN5O3/c1-25-15-5-13-14(6-16(15)26-2)22-10-23-17(13)24-4-3-12(9-24)27-18-20-7-11(19)8-21-18/h5-8,10,12H,3-4,9H2,1-2H3/t12-/m1/s1
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44n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14759
PNG
((R)-6,7-Dimethoxy-4-[3-(pyridin-4-yloxy)-pyrrolidi...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccncc3)c2cc1OC
Show InChI InChI=1S/C19H20N4O3/c1-24-17-9-15-16(10-18(17)25-2)21-12-22-19(15)23-8-5-14(11-23)26-13-3-6-20-7-4-13/h3-4,6-7,9-10,12,14H,5,8,11H2,1-2H3/t14-/m1/s1
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112n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14757
PNG
((R)-6,7-Dimethoxy-4-[3-(pyridin-2-yloxy)-pyrrolidi...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3ccccn3)c2cc1OC
Show InChI InChI=1S/C19H20N4O3/c1-24-16-9-14-15(10-17(16)25-2)21-12-22-19(14)23-8-6-13(11-23)26-18-5-3-4-7-20-18/h3-5,7,9-10,12-13H,6,8,11H2,1-2H3/t13-/m1/s1
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123n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
Phosphodiesterase Type 10 (PDE10A)


(Rattus norvegicus (rat))
BDBM14758
PNG
((R)-6,7-Dimethoxy-4-[3-(pyridin-3-yloxy)-pyrrolidi...)
Show SMILES COc1cc2ncnc(N3CC[C@H](C3)Oc3cccnc3)c2cc1OC
Show InChI InChI=1S/C19H20N4O3/c1-24-17-8-15-16(9-18(17)25-2)21-12-22-19(15)23-7-5-14(11-23)26-13-4-3-6-20-10-13/h3-4,6,8-10,12,14H,5,7,11H2,1-2H3/t14-/m1/s1
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128n/an/an/an/an/an/an/an/a



Pfizer



Assay Description
PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by...


J Med Chem 50: 182-5 (2007)


Article DOI: 10.1021/jm060653b
BindingDB Entry DOI: 10.7270/Q2930RDX
More data for this
Ligand-Target Pair
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