Basic Information
ID: ALA3887984
Type: Binding
Description: In Vitro Assay hPDE10a: Human recombinant PDE10A2 was expressed in Sf9 cells, using a recombinant baculovirus construct containing the full length sequence containing a 6×His sequence following the start Met to allow metal affinity purification of the recombinant protein. Cells were harvested and the phosphodiesterase protein was purified by metal chelate chromatography on Ni-sepharose 6FF.The affinity of the compounds of Formula (I) for phophodiesterases (PDE) was measured by a scintillation proximity assay (SPA). PDE Yttrium Silicate SPA beads allow PDE activity to be measured by direct binding of the primary phosphate groups of non-cyclic AMP or GMP to the beads via a complex iron chelation mechanism. The amount of bound tritiated product ([3H]-AMP) is measured by liquid scintillation counting.The compounds were dissolved and diluted in 100% DMSO in polystyrene plates to a concentration of 100-fold the final concentration in the assay. Human PDE10A enzyme solution (10 uL) was added to 20 μL, of incub
Organism: Homo sapiens
Cell type: Sf9
Activity Charts
Bioactivity
Activity Types for Assay ALA3887984
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 473.54 | 1.41 | 1.41 |
| 517.64 | 4.81 | 4.81 |
| 539.62 | 4.06 | 4.06 |
| 550.62 | 4.37 | 4.37 |
| 507.55 | 3.84 | 3.84 |
| 581.66 | 4.14 | 4.14 |
| 518.63 | 3.76 | 3.76 |
| 570.68 | 2.56 | 2.56 |
| 582.11 | 3.84 | 3.84 |
| 553.66 | 4.61 | 4.61 |
| 567.63 | 4.12 | 4.12 |
| 511.54 | 3.25 | 3.25 |
| 516.57 | 3.83 | 3.83 |
| 505.58 | 5.14 | 5.14 |
| 438.49 | 3.76 | 3.76 |
| 574.64 | 4.64 | 4.64 |
| 576.66 | 4.26 | 4.26 |
| 495.51 | 4.79 | 4.79 |
| 502.58 | 2.96 | 2.96 |
| 550.67 | 3.94 | 3.94 |
| 579.66 | 3.77 | 3.77 |
| 559.61 | 2.44 | 2.44 |
| 505.58 | 5.14 | 5.14 |
| 538.59 | 3.38 | 3.38 |
| 550.62 | 3.77 | 3.77 |
| 502.54 | 3.53 | 3.53 |
| 523.60 | 3.59 | 3.59 |
| 457.49 | 3.51 | 3.51 |
| 514.59 | 4.39 | 4.39 |
| 536.64 | 3.51 | 3.51 |
| 547.67 | 3.19 | 3.19 |
| 481.54 | 3.94 | 3.94 |
| 531.58 | 3.83 | 3.83 |
| 547.67 | 3.19 | 3.19 |
| 540.61 | 3.00 | 3.00 |
| 551.65 | 4.99 | 4.99 |
| 518.58 | 3.85 | 3.85 |
| 553.63 | 4.87 | 4.87 |
| 578.67 | 4.41 | 4.41 |
| 517.57 | 2.40 | 2.40 |
| 534.58 | 4.36 | 4.36 |
| 521.63 | 4.22 | 4.22 |
| 536.64 | 3.29 | 3.29 |
| 450.55 | 4.15 | 4.15 |
| 503.57 | 3.75 | 3.75 |
| 563.67 | 3.00 | 3.00 |
| 518.58 | 3.44 | 3.44 |
| 444.54 | 3.16 | 3.16 |
| 519.61 | 3.15 | 3.15 |
| 534.58 | 3.87 | 3.87 |
| 567.63 | 3.80 | 3.80 |
| 571.66 | 3.65 | 3.65 |
| 532.56 | 4.26 | 4.26 |
| 523.62 | 2.08 | 2.08 |
| 529.63 | 3.33 | 3.33 |
| 481.56 | 3.82 | 3.82 |
| 558.62 | 3.18 | 3.18 |
| 521.62 | 5.55 | 5.55 |
| 479.50 | 2.46 | 2.46 |
| 505.54 | 3.54 | 3.54 |
| 481.52 | 2.85 | 2.85 |
| 501.55 | 4.13 | 4.13 |
| 537.63 | 2.90 | 2.90 |
| 518.58 | 3.44 | 3.44 |
| 540.63 | 4.99 | 4.99 |
| 548.60 | 4.75 | 4.75 |
| 516.57 | 4.24 | 4.24 |
| 537.61 | 4.02 | 4.02 |
| 574.69 | 3.76 | 3.76 |
| 478.51 | 4.04 | 4.04 |
| 538.68 | 3.88 | 3.88 |
| 523.60 | 2.56 | 2.56 |
| 490.53 | 3.93 | 3.93 |
| 556.65 | 3.22 | 3.22 |
| 506.57 | 4.45 | 4.45 |
| 532.61 | 4.07 | 4.07 |
| 523.60 | 2.56 | 2.56 |
| 516.58 | 3.01 | 3.01 |
| 520.55 | 3.30 | 3.30 |
| 496.53 | 3.38 | 3.38 |
| 555.62 | 3.04 | 3.04 |
| 548.60 | 4.16 | 4.16 |
| 576.66 | 4.79 | 4.79 |
| 554.63 | 3.64 | 3.64 |
| 492.54 | 3.54 | 3.54 |
| 480.53 | 3.66 | 3.66 |
| 520.64 | 3.37 | 3.37 |
| 536.59 | 3.98 | 3.98 |
| 469.55 | 2.00 | 2.00 |
| 534.65 | 4.84 | 4.84 |
| 560.66 | 5.25 | 5.25 |
| 599.54 | 6.26 | 6.26 |
| 445.44 | 2.45 | 2.45 |
| 522.61 | 3.16 | 3.16 |
| 544.62 | 4.40 | 4.40 |
| 518.54 | 3.69 | 3.69 |
| 504.56 | 3.14 | 3.14 |
| 492.54 | 4.00 | 4.00 |
| 479.54 | 4.26 | 4.26 |
| 452.52 | 4.06 | 4.06 |
| 506.53 | 2.94 | 2.94 |
| 425.45 | 2.73 | 2.73 |
| 554.63 | 3.78 | 3.78 |
| 531.60 | 3.13 | 3.13 |
| 548.65 | 5.47 | 5.47 |
| 535.61 | 2.84 | 2.84 |
| 522.60 | 3.65 | 3.65 |
| 401.43 | 2.98 | 2.98 |
| 474.53 | 4.22 | 4.22 |
| 535.61 | 4.07 | 4.07 |
| 519.61 | 4.13 | 4.13 |
| 535.61 | 2.26 | 2.26 |
| 537.61 | 4.02 | 4.02 |
| 564.64 | 4.61 | 4.61 |