Basic Information
ID: ALA3887297
Type: Binding
Description: AKT Enzyme Assay: A TTP Mosquito liquid handling instrument is used to place 125 nl of the appropriate concentration of inhibitor in 100% DMSO (for a dose response curve calculation) into each well of a 384-well plate. To this reaction components are added to a final volume of 12.5 .mu.l: 0.1 ng/.mu.l His-AKT (Full Length), (Invitrogen, Part # P2999, Lot #641228C). 160 uM ATP (Fluka, 02055) 1 mM DTT (Sigma, D0632) 1 mM MgCl2 (Sigma, M1028) 1 .mu.M substrate peptide (sequence FITC-AHA-GRPRTSSFAEG-NH2), synthesized by Tufts Peptide Synthesis service. 100 mM HEPES pH 7.5 (Calbiochem, 391338)0.015% Brij-35 (Sigma, B4184)The reaction is incubated for 90 min at 25 C, and then stopped by the addition of 70 .mu.l of Stop buffer (100 mM HEPES pH 7.5, 0.015% Brij-35, 10 mM EDTA (Sigma, E7889)).The plate is read on a Caliper LC 3000 in an Off-Chip mobility shift assay format, using the following parameters for a 12-sipper chip: screening pressure -2.3 psi, upstream voltage -500, and downstream voltage -3000.
Format: BAO_0000357
Organism: Homo sapiens
Target: Serine/threonine-protein kinase AKT(ALA4282)
Document: ALA3886265
BindingDB Source: 7230
Activity Charts
Bioactivity
Activity Types for Assay ALA3887297
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 490.51 | 4.66 | 4.66 |
| 535.57 | 4.68 | 4.68 |
| 502.55 | 3.43 | 3.43 |
| 484.30 | 5.18 | 5.18 |
| 554.60 | 5.09 | 5.09 |
| 452.28 | 5.03 | 5.03 |
| 587.54 | 5.11 | 5.11 |
| 521.52 | 5.54 | 5.54 |
| 545.63 | 5.37 | 5.37 |
| 517.58 | 4.90 | 4.90 |
| 511.53 | 5.37 | 5.37 |
| 549.62 | 4.60 | 4.60 |
| 543.61 | 5.45 | 5.45 |
| 448.42 | 3.81 | 3.81 |
| 611.69 | 5.92 | 5.92 |
| 512.52 | 4.65 | 4.65 |
| 547.60 | 4.96 | 4.96 |
| 462.60 | 2.98 | 2.98 |
| 467.02 | 3.62 | 3.62 |
| 485.28 | 4.75 | 4.75 |
| 467.02 | 3.62 | 3.62 |
| 615.63 | 6.51 | 6.51 |
| 521.52 | 5.54 | 5.54 |
| 526.54 | 5.16 | 5.16 |
| 505.56 | 4.59 | 4.59 |
| 502.52 | 3.90 | 3.90 |
| 597.64 | 6.37 | 6.37 |
| 531.60 | 5.29 | 5.29 |
| 499.31 | 4.76 | 4.76 |
| 500.57 | 3.99 | 3.99 |
| 517.56 | 5.43 | 5.43 |
| 570.60 | 4.07 | 4.07 |
| 467.02 | 3.62 | 3.62 |
| 434.59 | 3.26 | 3.26 |
| 514.50 | 5.81 | 5.81 |
| 467.29 | 4.61 | 4.61 |
| 555.58 | 4.56 | 4.56 |
| 450.44 | 3.49 | 3.49 |
| 530.60 | 4.21 | 4.21 |
| 498.49 | 4.46 | 4.46 |
| 548.63 | 4.48 | 4.48 |
| 503.55 | 4.67 | 4.67 |
| 533.57 | 4.57 | 4.57 |
| 529.59 | 5.20 | 5.20 |
| 611.66 | 6.76 | 6.76 |
| 494.58 | 2.26 | 2.26 |
| 571.60 | 5.83 | 5.83 |
| 553.56 | 4.98 | 4.98 |
| 479.60 | 3.72 | 3.72 |
| 520.54 | 3.12 | 3.12 |
| 611.64 | 5.48 | 5.48 |
| 476.56 | 3.03 | 3.03 |
| 517.58 | 4.95 | 4.95 |
| 516.57 | 6.04 | 6.04 |
| 480.98 | 3.68 | 3.68 |
| 445.42 | 3.87 | 3.87 |
| 556.57 | 4.82 | 4.82 |
| 446.60 | 3.28 | 3.28 |
| 597.64 | 6.37 | 6.37 |
| 497.53 | 3.30 | 3.30 |
| 611.66 | 6.76 | 6.76 |
| 532.55 | 3.27 | 3.27 |
| 543.61 | 5.59 | 5.59 |
| 504.64 | 2.68 | 2.68 |
| 500.57 | 3.99 | 3.99 |
| 587.88 | 4.70 | 4.70 |
| 519.55 | 4.18 | 4.18 |
| 517.58 | 5.06 | 5.06 |
| 515.54 | 2.52 | 2.52 |
| 596.47 | 5.71 | 5.71 |
| 497.50 | 5.06 | 5.06 |
| 516.57 | 3.82 | 3.82 |
| 460.56 | 3.33 | 3.33 |
| 556.41 | 4.79 | 4.79 |
| 452.61 | 2.49 | 2.49 |
| 498.99 | 2.90 | 2.90 |
| 492.60 | 2.81 | 2.81 |
| 514.53 | 4.04 | 4.04 |
| 531.60 | 4.98 | 4.98 |
| 463.44 | 3.10 | 3.10 |
| 450.44 | 4.01 | 4.01 |
| 570.54 | 4.37 | 4.37 |
| 446.60 | 3.28 | 3.28 |
| 554.60 | 5.17 | 5.17 |
| 500.57 | 3.99 | 3.99 |
| 494.55 | 3.49 | 3.49 |
| 478.58 | 2.56 | 2.56 |
| 543.61 | 5.59 | 5.59 |
| 512.57 | 2.71 | 2.71 |
| 569.61 | 4.67 | 4.67 |
| 547.60 | 5.03 | 5.03 |
| 551.42 | 4.19 | 4.19 |
| 611.66 | 6.76 | 6.76 |
| 497.50 | 5.06 | 5.06 |
| 597.62 | 5.39 | 5.39 |
| 500.48 | 5.80 | 5.80 |
| 515.58 | 4.47 | 4.47 |
| 510.54 | 5.98 | 5.98 |
| 582.44 | 5.32 | 5.32 |
| 526.54 | 5.68 | 5.68 |