Basic Information
ID: ALA3887290
Type: Binding
Description: Biological Assay: Endothelial lipase activity was measured using a fluorescent substrate, A10070, (Invitrogen, CA) doped into an artificial vesicle containing DMPG (Avanti Polar Lipids) as the excipient. Vesicles were prepared by combining 285 uL, of 1 mM DMPG in a 1:1 mixture of MeOH and CHCl3 with 15 uL, of 1 mM A10070 in a 1:1 mixture of MeOH and CHCl3. The mixture was dried under nitrogen and resuspended in 150 uL, of 50 mM HEPES pH 8.0 buffer containing 100 mM NaCl and 0.2 mM EDTA. The sample was allowed to sit at rt for 15 min and then was sonicated 3x4 mins on ice with a Branson Sonicator using duty cycle 1. This preparation provides vesicles with a mole fraction of 0.05 for the FRET substrate.The enzymatic assay was measured using white, opaque 96-well half area plates. Each well contained 60 uL, of assay buffer (50 mM HEPES pH 8.0, 50 mM NaCl and 1 mM CaCl2) and 2 ul of a DMSO solution containing compound of interest. Conditioned media obtained from HT-1080 cells.
Organism: Homo sapiens
Cell type: HT-1080
Activity Charts
Bioactivity
Activity Types for Assay ALA3887290
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 523.57 | 4.00 | 4.00 |
| 572.58 | 3.22 | 3.22 |
| 450.48 | 1.43 | 1.43 |
| 516.61 | 3.25 | 3.25 |
| 607.57 | 3.71 | 3.71 |
| 588.59 | 4.18 | 4.18 |
| 505.60 | 4.91 | 4.91 |
| 568.62 | 2.76 | 2.76 |
| 482.45 | 2.53 | 2.53 |
| 493.59 | 1.95 | 1.95 |
| 627.60 | 5.92 | 5.92 |
| 470.53 | 3.35 | 3.35 |
| 564.58 | 1.13 | 1.13 |
| 434.48 | 2.33 | 2.33 |
| 479.56 | 4.60 | 4.60 |
| 501.59 | 2.44 | 2.44 |
| 483.54 | 2.20 | 2.20 |
| 491.53 | 1.79 | 1.79 |
| 486.58 | 2.50 | 2.50 |
| 540.56 | 2.09 | 2.09 |
| 477.50 | 1.40 | 1.40 |
| 574.56 | 5.27 | 5.27 |
| 569.69 | 3.52 | 3.52 |
| 573.59 | 2.69 | 2.69 |