VU0364739 |
VU0364739 : Inhibitor of PLD2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PLD2 |
|
|
Inhibitor
1 µM up to 5- 10 µM
Selectivity
In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selective against PLD1 in biochemical assay (PLD1: IC50 of 7500 nM).
In Cell Selectivity Assessment
Selectivity Assessment Description:
Selective against PLD1 (IC50 1500 nM) in cellular assay.
Potency Cellular
In Vitro
PLD2
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/jm100814g
In Vivo Validations
Rat
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.52 h
Systemic clearance:
61.5 mL/min/Kg
Fb :
97.9%
Volume of Distribution at Steady-State:
8.1 L/Kg
DOI Reference: 10.1021/jm100814g
Dose: 10 mg/Kg
Route of delivery:
Oral
Organ of interest (O):
brain
Target engagement assay:
levels: plasma 39.9 ng/mL, brain 29 ng/mL
brain/plasma distribution 0.73
DOI Reference: 10.1021/jm100814g
Negative Control Compounds
Chemical Information
| Molecular Formula | C26H27FN4O2 |
| SMILEs | O=C(NCCN1CCC2(CC1)C(=O)NCN2c1cccc(F)c1)c1ccc2ccccc2c1 |
| InChI | InChI=1S/C26H27FN4O2/c27-22-6-3-7-23(17-22)31-18-29-25(33)26(31)10-13-30(14-11-26)15-12-28-24(32)21-9-8-19-4-1-2-5-20(19)16-21/h1-9,16-17H,10-15,18H2,(H,28,32)(H,29,33) |
| Molecular weight | 446.21 Da |
| AlogP | 0.0 |
| HBond acceptors | 6 |
| HBond donors | 2 |
| Atoms | 60 |
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