Found 12 hits of ki for UniProtKB: O60658 Target/Host
(Institution) | Ligand | Target/Host
Links | Ligand
Links | Trg + Lig
Links | Ki
nM | ΔG°
kcal/mole | IC50
nM | Kd
nM | EC50/IC50
nM | koff
s-1 | kon
M-1s-1 | pH | Temp
°C |
|---|
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50150119
(CHEMBL3769414)Show SMILES [H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c(Nc3ccccc3)n(Cc3ccc(cc3)-c3cccc(F)n3)nc12 |r,c:9| Show InChI InChI=1S/C29H26FN7O/c1-35-28(38)25-26(31-20-7-3-2-4-8-20)36(34-27(25)37-23-11-5-10-22(23)33-29(35)37)17-18-13-15-19(16-14-18)21-9-6-12-24(30)32-21/h2-4,6-9,12-16,22-23,31H,5,10-11,17H2,1H3/t22-,23+/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet 
| Purchase
CHEMBL
MCE
PC cid
PC sid
PDB
UniChem
Similars
| Article
PubMed
| 3.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Intra-Cellular Therapies, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full lenght human PDE8A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay |
J Med Chem 59: 1149-64 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01751
BindingDB Entry DOI: 10.7270/Q2X068W7 |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50150264
(CHEMBL3769817)Show SMILES [H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c(Nc3ccccc3)n(Cc3ccc(cc3)-c3ccccn3)nc12 |r,c:9| Show InChI InChI=1S/C29H27N7O/c1-34-28(37)25-26(31-21-8-3-2-4-9-21)35(33-27(25)36-24-12-7-11-23(24)32-29(34)36)18-19-13-15-20(16-14-19)22-10-5-6-17-30-22/h2-6,8-10,13-17,23-24,31H,7,11-12,18H2,1H3/t23-,24+/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| 8.20E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Intra-Cellular Therapies, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full lenght human PDE8A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay |
J Med Chem 59: 1149-64 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01751
BindingDB Entry DOI: 10.7270/Q2X068W7 |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362033
(CHEMBL1939912)Show SMILES COc1cc(C)c2nc3[nH]nc(C)c3c(CN3CC[C@@H](O)C3)c2c1 |r| Show InChI InChI=1S/C18H22N4O2/c1-10-6-13(24-3)7-14-15(9-22-5-4-12(23)8-22)16-11(2)20-21-18(16)19-17(10)14/h6-7,12,23H,4-5,8-9H2,1-3H3,(H,19,20,21)/t12-/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362047
(CHEMBL1940057)Show SMILES COCCOc1cc(C)c2nc3[nH]nc(C)c3c(CN3CCCOCC3)c2c1 Show InChI InChI=1S/C21H28N4O3/c1-14-11-16(28-10-9-26-3)12-17-18(13-25-5-4-7-27-8-6-25)19-15(2)23-24-21(19)22-20(14)17/h11-12H,4-10,13H2,1-3H3,(H,22,23,24) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362046
(CHEMBL1940056)Show InChI InChI=1S/C18H22N4O2/c1-11-8-13(23)9-14-15(10-22-4-3-6-24-7-5-22)16-12(2)20-21-18(16)19-17(11)14/h8-9,23H,3-7,10H2,1-2H3,(H,19,20,21) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362048
(CHEMBL1940058)Show SMILES CC(C)Oc1cc(C)c2nc3[nH]nc(C)c3c(CN3CCCOCC3)c2c1 Show InChI InChI=1S/C21H28N4O2/c1-13(2)27-16-10-14(3)20-17(11-16)18(12-25-6-5-8-26-9-7-25)19-15(4)23-24-21(19)22-20/h10-11,13H,5-9,12H2,1-4H3,(H,22,23,24) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362035
(CHEMBL1939914)Show InChI InChI=1S/C18H22N4O2/c1-11-8-13(23-3)9-14-15(10-22-4-6-24-7-5-22)16-12(2)20-21-18(16)19-17(11)14/h8-9H,4-7,10H2,1-3H3,(H,19,20,21) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
MMDB
PC cid
PC sid
PDB
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362036
(CHEMBL1939915)Show SMILES COc1cc(C)c2nc3[nH]nc(C)c3c(CN3CCOC(C)C3)c2c1 Show InChI InChI=1S/C19H24N4O2/c1-11-7-14(24-4)8-15-16(10-23-5-6-25-12(2)9-23)17-13(3)21-22-19(17)20-18(11)15/h7-8,12H,5-6,9-10H2,1-4H3,(H,20,21,22) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50362043
(CHEMBL1940053)Show InChI InChI=1S/C19H24N4O2/c1-12-9-14(24-3)10-15-16(11-23-5-4-7-25-8-6-23)17-13(2)21-22-19(17)20-18(12)15/h9-10H,4-8,11H2,1-3H3,(H,20,21,22) | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Merck Research Laboratories
Curated by ChEMBL
| Assay Description
Displacement of [3H]cAMP from PDE8A1 by competitive binding assay |
Bioorg Med Chem Lett 22: 235-9 (2011)
Article DOI: 10.1016/j.bmcl.2011.11.023
BindingDB Entry DOI: 10.7270/Q2862GWC |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50150171
(CHEMBL3770470)Show SMILES [H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c1nn(Cc1ccc(cc1)-c1ccccc1)c2Nc1ccccc1 |r,c:9| Show InChI InChI=1S/C30H28N6O/c1-34-29(37)26-27(31-23-11-6-3-7-12-23)35(33-28(26)36-25-14-8-13-24(25)32-30(34)36)19-20-15-17-22(18-16-20)21-9-4-2-5-10-21/h2-7,9-12,15-18,24-25,31H,8,13-14,19H2,1H3/t24-,25+/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| 3.30E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Intra-Cellular Therapies, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full lenght human PDE8A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay |
J Med Chem 59: 1149-64 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01751
BindingDB Entry DOI: 10.7270/Q2X068W7 |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50150239
(CHEMBL3769461)Show SMILES [H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c(Nc3ccccc3)n(Cc3ccc(cc3)C(F)(F)F)nc12 |r,c:9| Show InChI InChI=1S/C25H23F3N6O/c1-32-23(35)20-21(29-17-6-3-2-4-7-17)33(14-15-10-12-16(13-11-15)25(26,27)28)31-22(20)34-19-9-5-8-18(19)30-24(32)34/h2-4,6-7,10-13,18-19,29H,5,8-9,14H2,1H3/t18-,19+/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Patents
| Article
PubMed
| 5.40E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Intra-Cellular Therapies, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full lenght human PDE8A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay |
J Med Chem 59: 1149-64 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01751
BindingDB Entry DOI: 10.7270/Q2X068W7 |
More data for this
Ligand-Target Pair | |
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
(Homo sapiens (Human)) | BDBM50150238
(CHEMBL3770107)Show SMILES [H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c(Nc3ccccc3)n(Cc3ccc(nc3)C(F)(F)F)nc12 |r,c:9| Show InChI InChI=1S/C24H22F3N7O/c1-32-22(35)19-20(29-15-6-3-2-4-7-15)33(13-14-10-11-18(28-12-14)24(25,26)27)31-21(19)34-17-9-5-8-16(17)30-23(32)34/h2-4,6-7,10-12,16-17,29H,5,8-9,13H2,1H3/t16-,17+/m1/s1 | PDB
MMDB
Reactome pathway
KEGG
UniProtKB/SwissProt
B.MOAD
DrugBank
antibodypedia
GoogleScholar
AffyNet
| CHEMBL
PC cid
PC sid
UniChem
Similars
| Article
PubMed
| >1.00E+5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Intra-Cellular Therapies, Inc.
Curated by ChEMBL
| Assay Description
Inhibition of recombinant full lenght human PDE8A using fluorescent labeled cAMP as substrate after 15 mins by IMAP assay |
J Med Chem 59: 1149-64 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01751
BindingDB Entry DOI: 10.7270/Q2X068W7 |
More data for this
Ligand-Target Pair | |
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