Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | phosphodiesterase 4B, cAMP-specific | References | |
Homo sapiens | phosphodiesterase 4C, cAMP-specific | References | |
Homo sapiens | phosphodiesterase 4D, cAMP-specific | Starlite/ChEMBL | References |
Rattus norvegicus | Phosphodiesterase 4 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | SH3 domain-binding glutamic acid-rich protein homolog | Phosphodiesterase 4 | 536 aa | 527 aa | 52.6 % |
Toxoplasma gondii | 3'5'-cyclic nucleotide phosphodiesterase domain-containing protein | Phosphodiesterase 4 | 536 aa | 456 aa | 27.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0447 | 1 | 1 |
Toxoplasma gondii | 3'5'-cyclic nucleotide phosphodiesterase domain-containing protein | 0.0447 | 1 | 0.5 |
Echinococcus multilocularis | glutamate receptor NMDA | 0.0243 | 0.4057 | 0.4057 |
Giardia lamblia | CAMP-specific 3,5-cyclic phosphodiesterase 4B | 0.0447 | 1 | 0.5 |
Echinococcus multilocularis | nmda type glutamate receptor | 0.037 | 0.7767 | 0.7767 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 3 | 0.0127 | 0.0666 | 0.0666 |
Echinococcus granulosus | nmda type glutamate receptor | 0.037 | 0.7767 | 0.7767 |
Echinococcus granulosus | glutamate receptor NMDA | 0.0243 | 0.4057 | 0.4057 |
Echinococcus granulosus | cAMP specific 3'5' cyclic phosphodiesterase | 0.0392 | 0.8412 | 0.8412 |
Echinococcus granulosus | cAMP specific 3'5' cyclic phosphodiesterase | 0.0447 | 1 | 1 |
Echinococcus granulosus | nmda type glutamate receptor | 0.0266 | 0.4724 | 0.4724 |
Brugia malayi | Probable 3',5'-cyclic phosphodiesterase R153.1, putative | 0.0392 | 0.8412 | 0.5 |
Echinococcus multilocularis | cAMP specific 3',5' cyclic phosphodiesterase | 0.0447 | 1 | 1 |
Echinococcus multilocularis | cAMP specific 3',5' cyclic phosphodiesterase | 0.0447 | 1 | 1 |
Echinococcus multilocularis | cAMP specific 3',5' cyclic phosphodiesterase | 0.0392 | 0.8412 | 0.8412 |
Echinococcus multilocularis | nmda type glutamate receptor | 0.0266 | 0.4724 | 0.4724 |
Schistosoma mansoni | camp-specific 35-cyclic phosphodiesterase | 0.0447 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
ED50 (functional) | = 0.5 mg kg-1 | Reversal of reserpine-induced hypothermia in the mouse on peroral administration | ChEMBL. | 9526558 |
ED50 (functional) | = 0.5 mg kg-1 | Reversal of reserpine-induced hypothermia in the mouse on peroral administration | ChEMBL. | 9526558 |
IC50 (binding) | = 5 nM | Competition of [3H]-rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosol | ChEMBL. | 9526558 |
IC50 (binding) | = 5 nM | Competition of [3H]-rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosol | ChEMBL. | 9526558 |
IC50 (binding) | = 1200 nM | Inhibition activity against human monocyte dervived PDE4 catalytic activity (LPDE4) | ChEMBL. | 9526558 |
IC50 (binding) | = 1200 nM | Inhibition activity against human monocyte dervived PDE4 catalytic activity (LPDE4) | ChEMBL. | 9526558 |
ID50 (functional) | = 0.5 mg kg-1 | Antigen-induced bronchoconstriction in guinea pigs after iv administration 10 min pre-treatment | ChEMBL. | 9526558 |
ID50 (functional) | = 3 mg kg-1 | Antigen-induced bronchoconstriction in guinea pigs after peroral administration 1 hour pre-treatment | ChEMBL. | 9526558 |
Selectivity (binding) | = 0.04 | Value is the ratio between HPDE4 and LPDE4 | ChEMBL. | 9526558 |
Therapeutic index (ADMET) | = 0.17 | The value for hypothermia against antigen provocation (po) | ChEMBL. | 9526558 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.