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Found 190 hits Enz. Inhib. hit(s) with Target = 'Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D'   
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
Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM194401
PNG
(US9200016, 83)
Show SMILES CCc1ncc(Cc2ccc3cccc(O)c3n2)c2cc(OC)c(OC)cc12
Show InChI InChI=1S/C23H22N2O3/c1-4-19-18-12-22(28-3)21(27-2)11-17(18)15(13-24-19)10-16-9-8-14-6-5-7-20(26)23(14)25-16/h5-9,11-13,26H,4,10H2,1-3H3
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US Patent
n/an/a 439n/an/an/an/a7.437



Allergan, Inc.; Exonhit Therapeutics, SA

US Patent


Assay Description
The phosphodiesterase assay was developed using the LANCE cAMP kit (PerkinElmer). The assay buffer contained HBSS with 5 mM HEPES, 0.1% BSA, and 1....


US Patent US9200016 (2015)


BindingDB Entry DOI: 10.7270/Q2ZC81PH
More data for this
Ligand-Target Pair
Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM194487
PNG
(US9200016, 169)
Show SMILES COCc1ncc(Cc2cnc3ccc(O)c(c3c2)C(F)(F)F)c2cc(OC)c(OC)cc12
Show InChI InChI=1S/C24H21F3N2O4/c1-31-12-19-16-9-22(33-3)21(32-2)8-15(16)14(11-29-19)6-13-7-17-18(28-10-13)4-5-20(30)23(17)24(25,26)27/h4-5,7-11,30H,6,12H2,1-3H3
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n/an/a 194n/an/an/an/a7.437



Allergan, Inc.; Exonhit Therapeutics, SA

US Patent


Assay Description
The phosphodiesterase assay was developed using the LANCE cAMP kit (PerkinElmer). The assay buffer contained HBSS with 5 mM HEPES, 0.1% BSA, and 1....


US Patent US9200016 (2015)


BindingDB Entry DOI: 10.7270/Q2ZC81PH
More data for this
Ligand-Target Pair
Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM194480
PNG
(US9200016, 162)
Show SMILES CCCc1ncc(Cc2cnc3ccc(O)c(c3c2)C(F)(F)F)c2cc(OC)c(OC)cc12
Show InChI InChI=1S/C25H23F3N2O3/c1-4-5-19-17-11-23(33-3)22(32-2)10-16(17)15(13-30-19)8-14-9-18-20(29-12-14)6-7-21(31)24(18)25(26,27)28/h6-7,9-13,31H,4-5,8H2,1-3H3
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n/an/a 232n/an/an/an/a7.437



Allergan, Inc.; Exonhit Therapeutics, SA

US Patent


Assay Description
The phosphodiesterase assay was developed using the LANCE cAMP kit (PerkinElmer). The assay buffer contained HBSS with 5 mM HEPES, 0.1% BSA, and 1....


US Patent US9200016 (2015)


BindingDB Entry DOI: 10.7270/Q2ZC81PH
More data for this
Ligand-Target Pair
Isoform 3 of cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM194411
PNG
(US9200016, 93)
Show SMILES CCc1ncc(Cc2ccc3cccc(NC(=O)C(N)=O)c3n2)c2cc(OC)c(OC)cc12
Show InChI InChI=1S/C25H24N4O4/c1-4-19-18-12-22(33-3)21(32-2)11-17(18)15(13-27-19)10-16-9-8-14-6-5-7-20(23(14)28-16)29-25(31)24(26)30/h5-9,11-13H,4,10H2,1-3H3,(H2,26,30)(H,29,31)
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Allergan, Inc.; Exonhit Therapeutics, SA

US Patent


Assay Description
The phosphodiesterase assay was developed using the LANCE cAMP kit (PerkinElmer). The assay buffer contained HBSS with 5 mM HEPES, 0.1% BSA, and 1....


US Patent US9200016 (2015)


BindingDB Entry DOI: 10.7270/Q2ZC81PH
More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285528
PNG
(Azetidin-1-yl[3-(4-chlorophenyl)imidazo[1,2-b]pyri...)
Show SMILES Clc1ccc(cc1)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C16H13ClN4O/c17-12-6-4-11(5-7-12)15-14(16(22)20-9-2-10-20)19-13-3-1-8-18-21(13)15/h1,3-8H,2,9-10H2
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n/an/a 130n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285528
PNG
(Azetidin-1-yl[3-(4-chlorophenyl)imidazo[1,2-b]pyri...)
Show SMILES Clc1ccc(cc1)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C16H13ClN4O/c17-12-6-4-11(5-7-12)15-14(16(22)20-9-2-10-20)19-13-3-1-8-18-21(13)15/h1,3-8H,2,9-10H2
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n/an/a 1.03E+4n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285529
PNG
(3-(4-Chlorophenyl)-N-cyclopropylimidazo[1,2-b]pyri...)
Show SMILES Clc1ccc(cc1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C16H13ClN4O/c17-11-5-3-10(4-6-11)15-14(16(22)19-12-7-8-12)20-13-2-1-9-18-21(13)15/h1-6,9,12H,7-8H2,(H,19,22)
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n/an/a 27.9n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285529
PNG
(3-(4-Chlorophenyl)-N-cyclopropylimidazo[1,2-b]pyri...)
Show SMILES Clc1ccc(cc1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C16H13ClN4O/c17-11-5-3-10(4-6-11)15-14(16(22)19-12-7-8-12)20-13-2-1-9-18-21(13)15/h1-6,9,12H,7-8H2,(H,19,22)
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n/an/a 4.34E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285530
PNG
(Azetidin-1-yl[3-(3,5-difluoro-4-methoxyphenyl)imid...)
Show SMILES COc1c(F)cc(cc1F)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C17H14F2N4O2/c1-25-16-11(18)8-10(9-12(16)19)15-14(17(24)22-6-3-7-22)21-13-4-2-5-20-23(13)15/h2,4-5,8-9H,3,6-7H2,1H3
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n/an/a 51.9n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285530
PNG
(Azetidin-1-yl[3-(3,5-difluoro-4-methoxyphenyl)imid...)
Show SMILES COc1c(F)cc(cc1F)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C17H14F2N4O2/c1-25-16-11(18)8-10(9-12(16)19)15-14(17(24)22-6-3-7-22)21-13-4-2-5-20-23(13)15/h2,4-5,8-9H,3,6-7H2,1H3
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n/an/a 2.41E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285531
PNG
(N-Cyclopropyl-3-(2-methoxypyrimidin-5-yl)imidazo[1...)
Show SMILES COc1ncc(cn1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C15H14N6O2/c1-23-15-16-7-9(8-17-15)13-12(14(22)19-10-4-5-10)20-11-3-2-6-18-21(11)13/h2-3,6-8,10H,4-5H2,1H3,(H,19,22)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285531
PNG
(N-Cyclopropyl-3-(2-methoxypyrimidin-5-yl)imidazo[1...)
Show SMILES COc1ncc(cn1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C15H14N6O2/c1-23-15-16-7-9(8-17-15)13-12(14(22)19-10-4-5-10)20-11-3-2-6-18-21(11)13/h2-3,6-8,10H,4-5H2,1H3,(H,19,22)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285532
PNG
(3-(6-Cyanopyridin-3-yl)-N-cyclopropylimidazo[1,2-b...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc(nc1)C#N
Show InChI InChI=1S/C16H12N6O/c17-8-12-4-3-10(9-18-12)15-14(16(23)20-11-5-6-11)21-13-2-1-7-19-22(13)15/h1-4,7,9,11H,5-6H2,(H,20,23)
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n/an/a 208n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285532
PNG
(3-(6-Cyanopyridin-3-yl)-N-cyclopropylimidazo[1,2-b...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc(nc1)C#N
Show InChI InChI=1S/C16H12N6O/c17-8-12-4-3-10(9-18-12)15-14(16(23)20-11-5-6-11)21-13-2-1-7-19-22(13)15/h1-4,7,9,11H,5-6H2,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285533
PNG
(N-Cyclopropyl-3-([1,2,4]triazolo[1,5-a]pyridin-6-y...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc2ncnn2c1
Show InChI InChI=1S/C16H13N7O/c24-16(20-11-4-5-11)14-15(23-13(21-14)2-1-7-18-23)10-3-6-12-17-9-19-22(12)8-10/h1-3,6-9,11H,4-5H2,(H,20,24)
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n/an/a 326n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285533
PNG
(N-Cyclopropyl-3-([1,2,4]triazolo[1,5-a]pyridin-6-y...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc2ncnn2c1
Show InChI InChI=1S/C16H13N7O/c24-16(20-11-4-5-11)14-15(23-13(21-14)2-1-7-18-23)10-3-6-12-17-9-19-22(12)8-10/h1-3,6-9,11H,4-5H2,(H,20,24)
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n/an/a 4.89E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285534
PNG
(3-(4-Chloro-3-fluorophenyl)-N-(1-methyl-1H-pyrazol...)
Show SMILES Cn1cc(NC(=O)c2nc3cccnn3c2-c2ccc(Cl)c(F)c2)cn1
Show InChI InChI=1S/C17H12ClFN6O/c1-24-9-11(8-21-24)22-17(26)15-16(10-4-5-12(18)13(19)7-10)25-14(23-15)3-2-6-20-25/h2-9H,1H3,(H,22,26)
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n/an/a 2.35n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285534
PNG
(3-(4-Chloro-3-fluorophenyl)-N-(1-methyl-1H-pyrazol...)
Show SMILES Cn1cc(NC(=O)c2nc3cccnn3c2-c2ccc(Cl)c(F)c2)cn1
Show InChI InChI=1S/C17H12ClFN6O/c1-24-9-11(8-21-24)22-17(26)15-16(10-4-5-12(18)13(19)7-10)25-14(23-15)3-2-6-20-25/h2-9H,1H3,(H,22,26)
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n/an/a 34.5n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285535
PNG
(Azetidin-1-yl[3-(pyrazolo[1,5-a]pyridin-6-yl)imida...)
Show SMILES O=C(N1CCC1)c1nc2cccnn2c1-c1ccc2ccnn2c1
Show InChI InChI=1S/C17H14N6O/c24-17(21-9-2-10-21)15-16(23-14(20-15)3-1-7-19-23)12-4-5-13-6-8-18-22(13)11-12/h1,3-8,11H,2,9-10H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285535
PNG
(Azetidin-1-yl[3-(pyrazolo[1,5-a]pyridin-6-yl)imida...)
Show SMILES O=C(N1CCC1)c1nc2cccnn2c1-c1ccc2ccnn2c1
Show InChI InChI=1S/C17H14N6O/c24-17(21-9-2-10-21)15-16(23-14(20-15)3-1-7-19-23)12-4-5-13-6-8-18-22(13)11-12/h1,3-8,11H,2,9-10H2
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n/an/a 5.44E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285536
PNG
(3-(4-Chloro-2,5-difluorophenyl)-N-cyclopropylimida...)
Show SMILES Fc1cc(-c2c(nc3cccnn23)C(=O)NC2CC2)c(F)cc1Cl
Show InChI InChI=1S/C16H11ClF2N4O/c17-10-7-11(18)9(6-12(10)19)15-14(16(24)21-8-3-4-8)22-13-2-1-5-20-23(13)15/h1-2,5-8H,3-4H2,(H,21,24)
PDB

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n/an/a 40.9n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285536
PNG
(3-(4-Chloro-2,5-difluorophenyl)-N-cyclopropylimida...)
Show SMILES Fc1cc(-c2c(nc3cccnn23)C(=O)NC2CC2)c(F)cc1Cl
Show InChI InChI=1S/C16H11ClF2N4O/c17-10-7-11(18)9(6-12(10)19)15-14(16(24)21-8-3-4-8)22-13-2-1-5-20-23(13)15/h1-2,5-8H,3-4H2,(H,21,24)
PDB

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n/an/a 1.49E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285537
PNG
(3-(4-chloro-3-fluoro-phenyl)-N-cyclopropyl-imidazo...)
Show SMILES Fc1cc(ccc1Cl)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C16H12ClFN4O/c17-11-6-3-9(8-12(11)18)15-14(16(23)20-10-4-5-10)21-13-2-1-7-19-22(13)15/h1-3,6-8,10H,4-5H2,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285537
PNG
(3-(4-chloro-3-fluoro-phenyl)-N-cyclopropyl-imidazo...)
Show SMILES Fc1cc(ccc1Cl)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C16H12ClFN4O/c17-11-6-3-9(8-12(11)18)15-14(16(23)20-10-4-5-10)21-13-2-1-7-19-22(13)15/h1-3,6-8,10H,4-5H2,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285538
PNG
(N-cyclopropyl-3-(3,4-di-chlorophenyl)imidazo[1,2-b...)
Show SMILES Clc1ccc(cc1Cl)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C16H12Cl2N4O/c17-11-6-3-9(8-12(11)18)15-14(16(23)20-10-4-5-10)21-13-2-1-7-19-22(13)15/h1-3,6-8,10H,4-5H2,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285539
PNG
(3-(4-chloro-2-methyl-phenyl)-N-cyclopropyl-imidazo...)
Show SMILES Cc1cc(Cl)ccc1-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C17H15ClN4O/c1-10-9-11(18)4-7-13(10)16-15(17(23)20-12-5-6-12)21-14-3-2-8-19-22(14)16/h2-4,7-9,12H,5-6H2,1H3,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285539
PNG
(3-(4-chloro-2-methyl-phenyl)-N-cyclopropyl-imidazo...)
Show SMILES Cc1cc(Cl)ccc1-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C17H15ClN4O/c1-10-9-11(18)4-7-13(10)16-15(17(23)20-12-5-6-12)21-14-3-2-8-19-22(14)16/h2-4,7-9,12H,5-6H2,1H3,(H,20,23)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285540
PNG
(US10077269, Example 13 | US9598421, Example 13 | a...)
Show SMILES Fc1cc(ccc1Cl)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C16H12ClFN4O/c17-11-5-4-10(9-12(11)18)15-14(16(23)21-7-2-8-21)20-13-3-1-6-19-22(13)15/h1,3-6,9H,2,7-8H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285540
PNG
(US10077269, Example 13 | US9598421, Example 13 | a...)
Show SMILES Fc1cc(ccc1Cl)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C16H12ClFN4O/c17-11-5-4-10(9-12(11)18)15-14(16(23)21-7-2-8-21)20-13-3-1-6-19-22(13)15/h1,3-6,9H,2,7-8H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285541
PNG
(3-(5-chloropyridin-3-yl)-N-cyclopropylimidazo[1,2-...)
Show SMILES Clc1cncc(c1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C15H12ClN5O/c16-10-6-9(7-17-8-10)14-13(15(22)19-11-3-4-11)20-12-2-1-5-18-21(12)14/h1-2,5-8,11H,3-4H2,(H,19,22)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285541
PNG
(3-(5-chloropyridin-3-yl)-N-cyclopropylimidazo[1,2-...)
Show SMILES Clc1cncc(c1)-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C15H12ClN5O/c16-10-6-9(7-17-8-10)14-13(15(22)19-11-3-4-11)20-12-2-1-5-18-21(12)14/h1-2,5-8,11H,3-4H2,(H,19,22)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285542
PNG
(US10077269, Example 15 | US9598421, Example 15 | a...)
Show SMILES Clc1cncc(c1)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C15H12ClN5O/c16-11-7-10(8-17-9-11)14-13(15(22)20-5-2-6-20)19-12-3-1-4-18-21(12)14/h1,3-4,7-9H,2,5-6H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285542
PNG
(US10077269, Example 15 | US9598421, Example 15 | a...)
Show SMILES Clc1cncc(c1)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C15H12ClN5O/c16-11-7-10(8-17-9-11)14-13(15(22)20-5-2-6-20)19-12-3-1-4-18-21(12)14/h1,3-4,7-9H,2,5-6H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285543
PNG
(US10077269, Example 16 | US9598421, Example 16 | a...)
Show SMILES O=C(N1CCC1)c1nc2cccnn2c1-c1ccc2ncnn2c1
Show InChI InChI=1S/C16H13N7O/c24-16(21-7-2-8-21)14-15(23-13(20-14)3-1-6-18-23)11-4-5-12-17-10-19-22(12)9-11/h1,3-6,9-10H,2,7-8H2
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285544
PNG
(3-(4-cyano-2-fluoro-5-methylphenyl)-N-cyclopropyl-...)
Show SMILES Cc1cc(-c2c(nc3cccnn23)C(=O)NC2CC2)c(F)cc1C#N
Show InChI InChI=1S/C18H14FN5O/c1-10-7-13(14(19)8-11(10)9-20)17-16(18(25)22-12-4-5-12)23-15-3-2-6-21-24(15)17/h2-3,6-8,12H,4-5H2,1H3,(H,22,25)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285544
PNG
(3-(4-cyano-2-fluoro-5-methylphenyl)-N-cyclopropyl-...)
Show SMILES Cc1cc(-c2c(nc3cccnn23)C(=O)NC2CC2)c(F)cc1C#N
Show InChI InChI=1S/C18H14FN5O/c1-10-7-13(14(19)8-11(10)9-20)17-16(18(25)22-12-4-5-12)23-15-3-2-6-21-24(15)17/h2-3,6-8,12H,4-5H2,1H3,(H,22,25)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285545
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Cc1cc(-c2c(nc3cccnn23)C(=O)N2CCC2)c(F)cc1C#N
Show InChI InChI=1S/C18H14FN5O/c1-11-8-13(14(19)9-12(11)10-20)17-16(18(25)23-6-3-7-23)22-15-4-2-5-21-24(15)17/h2,4-5,8-9H,3,6-7H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285545
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Cc1cc(-c2c(nc3cccnn23)C(=O)N2CCC2)c(F)cc1C#N
Show InChI InChI=1S/C18H14FN5O/c1-11-8-13(14(19)9-12(11)10-20)17-16(18(25)23-6-3-7-23)22-15-4-2-5-21-24(15)17/h2,4-5,8-9H,3,6-7H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285546
PNG
(3-(4-cyano-5-fluoro-2-methylphenyl)-N-cyclo-propyl...)
Show SMILES Cc1cc(C#N)c(F)cc1-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C18H14FN5O/c1-10-7-11(9-20)14(19)8-13(10)17-16(18(25)22-12-4-5-12)23-15-3-2-6-21-24(15)17/h2-3,6-8,12H,4-5H2,1H3,(H,22,25)
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285546
PNG
(3-(4-cyano-5-fluoro-2-methylphenyl)-N-cyclo-propyl...)
Show SMILES Cc1cc(C#N)c(F)cc1-c1c(nc2cccnn12)C(=O)NC1CC1
Show InChI InChI=1S/C18H14FN5O/c1-10-7-11(9-20)14(19)8-13(10)17-16(18(25)22-12-4-5-12)23-15-3-2-6-21-24(15)17/h2-3,6-8,12H,4-5H2,1H3,(H,22,25)
PDB

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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285547
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Cc1cc(C#N)c(F)cc1-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C18H14FN5O/c1-11-8-12(10-20)14(19)9-13(11)17-16(18(25)23-6-3-7-23)22-15-4-2-5-21-24(15)17/h2,4-5,8-9H,3,6-7H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285547
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Cc1cc(C#N)c(F)cc1-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C18H14FN5O/c1-11-8-12(10-20)14(19)9-13(11)17-16(18(25)23-6-3-7-23)22-15-4-2-5-21-24(15)17/h2,4-5,8-9H,3,6-7H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285548
PNG
(3-(4-chloro-3-fluorophenyl)-N-cyclopropyl-N-methyl...)
Show SMILES CN(C1CC1)C(=O)c1nc2cccnn2c1-c1ccc(Cl)c(F)c1
Show InChI InChI=1S/C17H14ClFN4O/c1-22(11-5-6-11)17(24)15-16(10-4-7-12(18)13(19)9-10)23-14(21-15)3-2-8-20-23/h2-4,7-9,11H,5-6H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285548
PNG
(3-(4-chloro-3-fluorophenyl)-N-cyclopropyl-N-methyl...)
Show SMILES CN(C1CC1)C(=O)c1nc2cccnn2c1-c1ccc(Cl)c(F)c1
Show InChI InChI=1S/C17H14ClFN4O/c1-22(11-5-6-11)17(24)15-16(10-4-7-12(18)13(19)9-10)23-14(21-15)3-2-8-20-23/h2-4,7-9,11H,5-6H2,1H3
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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285549
PNG
(N-cyclopropyl-3-(pyrazolo[1,5-a]pyridin-6-yl)imida...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc2ccnn2c1
Show InChI InChI=1S/C17H14N6O/c24-17(20-12-4-5-12)15-16(23-14(21-15)2-1-8-19-23)11-3-6-13-7-9-18-22(13)10-11/h1-3,6-10,12H,4-5H2,(H,20,24)
PDB

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Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285549
PNG
(N-cyclopropyl-3-(pyrazolo[1,5-a]pyridin-6-yl)imida...)
Show SMILES O=C(NC1CC1)c1nc2cccnn2c1-c1ccc2ccnn2c1
Show InChI InChI=1S/C17H14N6O/c24-17(20-12-4-5-12)15-16(23-14(21-15)2-1-8-19-23)11-3-6-13-7-9-18-22(13)10-11/h1-3,6-10,12H,4-5H2,(H,20,24)
PDB

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n/an/a 1.89E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285550
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Fc1cc(ccc1C#N)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C17H12FN5O/c18-13-9-11(4-5-12(13)10-19)16-15(17(24)22-7-2-8-22)21-14-3-1-6-20-23(14)16/h1,3-6,9H,2,7-8H2
PDB

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UniChem
US Patent
n/an/a 45.8n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285550
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Fc1cc(ccc1C#N)-c1c(nc2cccnn12)C(=O)N1CCC1
Show InChI InChI=1S/C17H12FN5O/c18-13-9-11(4-5-12(13)10-19)16-15(17(24)22-7-2-8-22)21-14-3-1-6-20-23(14)16/h1,3-6,9H,2,7-8H2
PDB

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UniChem
US Patent
n/an/a 4.13E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4C isoform 1


(Homo sapiens (human))
BDBM285551
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Fc1cc(-c2c(nc3cccnn23)C(=O)N2CCC2)c(F)cc1C#N
Show InChI InChI=1S/C17H11F2N5O/c18-12-8-11(13(19)7-10(12)9-20)16-15(17(25)23-5-2-6-23)22-14-3-1-4-21-24(14)16/h1,3-4,7-8H,2,5-6H2
PDB

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UniChem
US Patent
n/an/a 59.7n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
cAMP-specific 3',5'-cyclic phosphodiesterase 4D


(Homo sapiens (human))
BDBM285551
PNG
(4-[2-(azetidin-1-ylcarbonyl)imidazo[1,2-b]pyridazi...)
Show SMILES Fc1cc(-c2c(nc3cccnn23)C(=O)N2CCC2)c(F)cc1C#N
Show InChI InChI=1S/C17H11F2N5O/c18-12-8-11(13(19)7-10(12)9-20)16-15(17(25)23-5-2-6-23)22-14-3-1-4-21-24(14)16/h1,3-4,7-8H,2,5-6H2
PDB

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PC sid
UniChem
US Patent
n/an/a>2.15E+3n/an/an/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
The PDE4A3, PDE4B1, PDE4C1 and PDE4D3 assays use the Scintillation Proximity Assay (SPA) technology to measure the inhibition of human recombinant PD...


US Patent US10077269 (2018)

More data for this
Ligand-Target Pair
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