| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T56367 | ||||
| Target Name | Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1 | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | ZAPRINAST | Drug Info | IC50 = 6000 nM | [527549] | |
| Vinpocetine | Drug Info | IC50 = 15~30 uM | [553047] | ||
| 3-Isobutyl-1-methyl-3,9-dihydro-purine-2,6-dione | Drug Info | IC50 = 3400 nM | [533395] | ||
| BUFROLIN | Drug Info | IC50 = 16000 nM | [533395] | ||
| Action against Disease Model | Vinpocetine | HERG-Lite monitors the expression of hERG at the cell surface in two different stable mammalian cell lines. One cell line acts as a biosensor for drugs that inhibit hERG trafficking, while the other predicts hERG blockers based on their ability to act as pharmacological chaperones. In this study, we have validated the HERG-Lite assay using a panel of 100 drugs: 50 hERG blockers and 50 nonblockers.HERG-Lite correctly predicted hERG risk for all 100 test compounds with no false positives or negatives. All 50 hERG blockers were detected as drugs with hERG risk in the HERG-Lite assay, and fell into two classes: B (for blocker) and C (for complex; block and trafficking inhibition).IC50 on hERG: 32nM | [552526] | Drug Info | |
| References | |||||
| Ref 552526 | HERG-Lite: a novel comprehensive high-throughput screen for drug-induced hERG risk. J Pharmacol Toxicol Methods. 2005 Jul-Aug;52(1):136-45. | ||||
| Ref 527549 | J Med Chem. 2005 May 19;48(10):3449-62.The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. | ||||
| Ref 553047 | Vinpocetine inhibits NF-kappaB-dependent inflammation via an IKK-dependent but PDE-independent mechanism. Proc Natl Acad Sci U S A. 2010 May 25;107(21):9795-800. doi: 10.1073/pnas.0914414107. Epub 2010 May 6. | ||||
| Ref 533395 | J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. | ||||
| Ref 533395 | J Med Chem. 1985 May;28(5):537-45.A new generation of phosphodiesterase inhibitors: multiple molecular forms of phosphodiesterase and the potential for drug selectivity. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.