Basic Information
ID: ALA3706369
Type: Binding
Description: Binding Assay: The efficacy of compounds of the invention in inhibiting the PI3K induced-lipid phosphorylation may be tested in the following binding assay. The assay combines the scintillation proximity assay technology (SPA, Amersham) with the capacity of neomycin (a polycationic antibiotic) to bind phospholipids with high affinity and specificity. The Scintillation Proximity Assay is based on the properties of weakly emitting isotopes (such as 3H, 125I, 33P). Coating SPA beads with neomycin allows the detection of phosphorylated lipid substrates after incubation with recombinant PI3K and radioactive ATP in the same well, by capturing the radioactive phospholipids to the SPA beads through their specific binding to neomycin. To a 384 wells MTP containing 5 ul of the test compound of Formula (I) (solubilized in 2% DMSO; to yield a final concentration of 20, 5, 1.25, 0.3125, 0.0781, 0.0195, 0.0049, 0.0012, 0.0003 and 0.00075 uM of the test compound).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3706369
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 439.49 | 2.31 | 2.31 |
| 377.42 | 0.86 | 0.86 |
| 333.37 | 0.84 | 0.84 |
| 377.42 | 0.86 | 0.86 |
| 439.49 | 2.31 | 2.31 |
| 423.49 | 2.61 | 2.61 |
| 423.49 | 2.61 | 2.61 |
| 441.48 | 2.75 | 2.75 |
| 439.49 | 2.31 | 2.31 |
| 439.49 | 2.31 | 2.31 |
| 410.46 | 1.69 | 1.69 |
| 415.52 | 2.82 | 2.82 |
| 426.29 | 1.61 | 1.61 |
| 365.39 | 0.99 | 0.99 |
| 427.46 | 2.44 | 2.44 |
| 365.39 | 0.99 | 0.99 |
| 427.46 | 2.44 | 2.44 |
| 488.36 | 3.06 | 3.06 |
| 423.49 | 2.61 | 2.61 |
| 488.36 | 3.06 | 3.06 |
| 427.46 | 2.44 | 2.44 |
| 443.91 | 2.95 | 2.95 |
| 467.50 | 2.07 | 2.07 |
| 480.57 | 3.22 | 3.22 |
| 488.36 | 3.06 | 3.06 |
| 443.91 | 2.95 | 2.95 |
| 488.36 | 3.06 | 3.06 |
| 427.46 | 2.44 | 2.44 |
| 443.91 | 2.95 | 2.95 |
| 451.55 | 3.42 | 3.42 |
| 424.48 | 2.00 | 2.00 |
| 417.49 | 1.66 | 1.66 |
| 409.47 | 2.30 | 2.30 |
| 347.40 | 0.85 | 0.85 |
| 392.39 | 0.76 | 0.76 |
| 454.46 | 2.21 | 2.21 |
| 361.42 | 1.33 | 1.33 |
| 453.52 | 2.37 | 2.37 |
| 375.45 | 1.72 | 1.72 |
| 423.49 | 2.36 | 2.36 |
| 437.52 | 2.55 | 2.55 |
| 404.49 | 0.87 | 0.87 |
| 530.65 | 2.96 | 2.96 |
| 405.48 | 1.35 | 1.35 |
| 417.49 | 1.49 | 1.49 |
| 377.42 | 0.30 | 0.30 |
| 424.48 | 1.75 | 1.75 |
| 389.48 | 2.11 | 2.11 |
| 415.52 | 2.50 | 2.50 |
| 389.48 | 1.97 | 1.97 |
| 429.54 | 2.89 | 2.89 |
| 431.51 | 1.74 | 1.74 |
| 391.45 | 0.96 | 0.96 |
| 391.45 | 0.69 | 0.69 |
| 438.51 | 1.95 | 1.95 |
| 430.53 | 1.31 | 1.31 |
| 499.59 | 4.08 | 4.08 |
| 463.56 | 3.64 | 3.64 |
| 437.52 | 3.25 | 3.25 |
| 522.58 | 1.77 | 1.77 |
| 452.49 | 1.40 | 1.40 |
| 426.29 | 1.61 | 1.61 |
| 488.36 | 3.06 | 3.06 |
| 424.48 | 1.88 | 1.88 |
| 516.60 | 1.35 | 1.35 |
| 434.48 | 2.17 | 2.17 |
| 418.52 | 1.26 | 1.26 |
| 444.56 | 1.65 | 1.65 |
| 444.56 | 1.79 | 1.79 |
| 446.53 | 0.64 | 0.64 |
| 401.49 | 2.42 | 2.42 |
| 416.50 | 1.23 | 1.23 |
| 416.50 | 1.23 | 1.23 |
| 430.53 | 1.58 | 1.58 |
| 429.54 | 3.21 | 3.21 |
| 416.50 | 2.21 | 2.21 |
| 430.53 | 1.62 | 1.62 |
| 402.48 | 0.84 | 0.84 |
| 410.46 | 1.69 | 1.69 |
| 488.61 | 2.87 | 2.87 |
| 471.62 | 4.09 | 4.09 |
| 431.51 | 1.79 | 1.79 |
| 417.49 | 1.66 | 1.66 |
| 466.52 | 2.26 | 2.26 |
| 474.58 | 1.59 | 1.59 |
| 437.52 | 2.63 | 2.63 |
| 481.57 | 3.27 | 3.27 |
| 439.49 | 2.31 | 2.31 |
| 535.63 | 1.69 | 1.69 |
| 480.55 | 2.00 | 2.00 |
| 522.58 | 1.77 | 1.77 |
| 520.61 | 2.93 | 2.93 |
| 502.57 | 1.67 | 1.67 |
| 516.62 | 2.88 | 2.88 |
| 516.62 | 2.88 | 2.88 |
| 460.56 | 0.94 | 0.94 |
| 488.36 | 3.06 | 3.06 |
| 494.60 | 0.91 | 0.91 |
| 535.63 | 1.69 | 1.69 |
| 520.61 | 2.93 | 2.93 |
| 510.57 | 1.68 | 1.68 |
| 429.54 | 3.06 | 3.06 |
| 494.41 | 3.58 | 3.58 |
| 423.49 | 2.61 | 2.61 |
| 487.56 | 1.70 | 1.70 |
| 440.48 | 1.70 | 1.70 |
| 410.46 | 1.69 | 1.69 |
| 474.58 | 1.59 | 1.59 |
| 460.56 | 0.94 | 0.94 |
| 494.60 | 0.91 | 0.91 |
| 508.60 | 2.13 | 2.13 |
| 508.60 | 2.13 | 2.13 |
| 487.56 | 1.70 | 1.70 |
| 423.49 | 2.61 | 2.61 |
| 466.56 | 2.58 | 2.58 |
| 439.49 | 1.79 | 1.79 |
| 550.64 | 2.55 | 2.55 |
| 536.61 | 1.90 | 1.90 |
| 536.61 | 1.90 | 1.90 |
| 550.64 | 2.14 | 2.14 |
| 570.65 | 1.17 | 1.17 |
| 522.58 | 1.77 | 1.77 |
| 536.61 | 2.21 | 2.21 |
| 529.58 | 2.95 | 2.95 |
| 410.46 | 1.69 | 1.69 |
| 520.61 | 2.93 | 2.93 |
| 452.54 | 2.37 | 2.37 |
| 439.49 | 1.79 | 1.79 |
| 494.57 | 2.14 | 2.14 |
| 494.57 | 2.14 | 2.14 |
| 482.56 | 2.36 | 2.36 |
| 485.57 | 3.97 | 3.97 |
| 477.46 | 3.32 | 3.32 |
| 550.64 | 2.55 | 2.55 |
| 499.59 | 4.27 | 4.27 |
| 499.59 | 4.27 | 4.27 |
| 508.60 | 2.13 | 2.13 |
| 423.49 | 2.69 | 2.69 |
| 424.48 | 1.88 | 1.88 |
| 424.48 | 1.88 | 1.88 |
| 500.58 | 4.04 | 4.04 |
| 524.62 | 3.23 | 3.23 |
| 536.65 | 2.91 | 2.91 |
| 506.63 | 3.28 | 3.28 |
| 451.50 | 3.06 | 3.06 |
| 443.57 | 3.45 | 3.45 |
| 488.61 | 1.98 | 1.98 |
| 486.64 | 2.99 | 2.99 |
| 506.63 | 3.15 | 3.15 |
| 529.66 | 1.28 | 1.28 |
| 427.46 | 2.44 | 2.44 |
| 452.54 | 2.37 | 2.37 |
| 506.63 | 3.28 | 3.28 |
| 466.56 | 2.36 | 2.36 |
| 502.57 | 1.67 | 1.67 |
| 478.57 | 2.90 | 2.90 |
| 491.53 | 2.66 | 2.66 |
| 507.60 | 3.13 | 3.13 |
| 504.57 | 3.57 | 3.57 |
| 489.56 | 2.70 | 2.70 |
| 502.56 | 2.34 | 2.34 |
| 486.55 | 3.36 | 3.36 |
| 588.69 | 2.49 | 2.49 |
| 492.58 | 3.42 | 3.42 |
| 488.61 | 1.67 | 1.67 |
| 472.57 | 1.57 | 1.57 |
| 415.50 | 2.36 | 2.36 |
| 526.66 | 3.05 | 3.05 |
| 528.63 | 1.90 | 1.90 |
| 446.51 | 1.06 | 1.06 |
| 491.53 | 2.66 | 2.66 |
| 475.53 | 3.56 | 3.56 |
| 486.55 | 3.36 | 3.36 |
| 505.56 | 2.91 | 2.91 |
| 490.55 | 2.39 | 2.39 |
| 421.54 | 2.88 | 2.88 |
| 423.49 | 2.61 | 2.61 |
| 449.49 | 2.18 | 2.18 |
| 539.62 | 3.70 | 3.70 |
| 415.50 | 2.36 | 2.36 |
| 421.54 | 2.88 | 2.88 |
| 516.60 | 1.55 | 1.55 |
| 444.56 | 1.65 | 1.65 |
| 537.60 | 2.16 | 2.16 |
| 440.48 | 1.00 | 1.00 |
| 509.59 | 1.53 | 1.53 |
| 438.51 | 2.34 | 2.34 |
| 534.60 | 2.41 | 2.41 |
| 521.56 | 2.50 | 2.50 |
| 514.65 | 2.37 | 2.37 |
| 509.59 | 1.53 | 1.53 |
| 525.61 | 2.63 | 2.63 |
| 492.60 | 3.15 | 3.15 |
| 520.66 | 3.19 | 3.19 |
| 500.67 | 3.38 | 3.38 |
| 462.55 | 1.92 | 1.92 |
| 512.55 | 2.90 | 2.90 |
| 594.58 | 4.08 | 4.08 |
| 528.68 | 2.76 | 2.76 |
| 518.64 | 1.61 | 1.61 |
| 466.56 | 2.36 | 2.36 |
| 508.60 | 1.87 | 1.87 |
| 492.60 | 2.89 | 2.89 |
| 570.69 | 1.92 | 1.92 |
| 443.49 | 1.30 | 1.30 |
| 471.49 | 1.74 | 1.74 |
| 453.52 | 2.37 | 2.37 |
| 578.74 | 3.94 | 3.94 |
| 536.65 | 2.91 | 2.91 |
| 578.74 | 3.94 | 3.94 |
| 524.67 | 2.85 | 2.85 |
| 522.63 | 2.26 | 2.26 |
| 439.49 | 2.36 | 2.36 |
| 480.57 | 2.97 | 2.97 |
| 463.97 | 3.07 | 3.07 |
| 524.62 | 3.23 | 3.23 |
| 570.69 | 1.92 | 1.92 |
| 542.61 | 3.53 | 3.53 |
| 492.60 | 2.89 | 2.89 |
| 423.52 | 1.72 | 1.72 |
| 556.67 | 1.53 | 1.53 |
| 453.52 | 2.45 | 2.45 |
| 435.48 | 1.80 | 1.80 |
| 452.49 | 1.40 | 1.40 |
| 507.62 | 2.68 | 2.68 |
| 522.63 | 1.44 | 1.44 |
| 487.63 | 1.51 | 1.51 |
| 502.59 | 2.49 | 2.49 |
| 460.56 | 1.20 | 1.20 |
| 474.58 | 1.59 | 1.59 |
| 530.65 | 3.27 | 3.27 |
| 502.64 | 2.37 | 2.37 |
| 488.61 | 1.98 | 1.98 |
| 542.61 | 3.53 | 3.53 |
| 514.55 | 2.75 | 2.75 |
| 508.60 | 2.13 | 2.13 |
| 510.62 | 1.84 | 1.84 |
| 451.93 | 2.31 | 2.31 |
| 500.62 | 1.98 | 1.98 |
| 522.63 | 2.52 | 2.52 |
| 522.63 | 2.52 | 2.52 |
| 542.61 | 3.53 | 3.53 |
| 542.61 | 3.53 | 3.53 |
| 514.65 | 2.37 | 2.37 |
| 514.55 | 2.75 | 2.75 |
| 508.60 | 2.13 | 2.13 |
| 535.62 | 1.90 | 1.90 |
| 464.98 | 1.80 | 1.80 |
| 515.64 | 0.89 | 0.89 |
| 527.65 | 2.60 | 2.60 |
| 531.65 | 1.99 | 1.99 |
| 453.52 | 2.45 | 2.45 |
| 526.66 | 3.05 | 3.05 |
| 546.67 | 2.90 | 2.90 |
| 545.68 | 2.38 | 2.38 |
| 531.65 | 1.99 | 1.99 |
| 531.65 | 1.99 | 1.99 |
| 563.67 | 2.68 | 2.68 |
| 528.68 | 2.76 | 2.76 |
| 496.59 | 1.45 | 1.45 |
| 528.63 | 1.90 | 1.90 |
| 496.59 | 1.45 | 1.45 |
| 481.56 | 1.08 | 1.08 |
| 529.66 | 1.28 | 1.28 |
| 489.56 | 2.54 | 2.54 |
| 489.56 | 2.54 | 2.54 |
| 500.62 | 2.13 | 2.13 |
| 526.70 | 3.92 | 3.92 |
| 512.59 | 1.84 | 1.84 |
| 523.66 | 2.84 | 2.84 |
| 510.62 | 1.84 | 1.84 |
| 504.58 | 1.87 | 1.87 |
| 488.57 | 1.12 | 1.12 |
| 486.59 | 1.74 | 1.74 |
| 563.12 | 3.42 | 3.42 |
| 532.64 | 2.51 | 2.51 |
| 486.59 | 1.59 | 1.59 |
| 504.58 | 1.73 | 1.73 |
| 514.65 | 2.37 | 2.37 |
| 528.68 | 2.76 | 2.76 |
| 528.68 | 2.76 | 2.76 |
| 517.63 | 1.60 | 1.60 |
| 564.11 | 1.93 | 1.93 |
| 517.63 | 1.60 | 1.60 |
| 521.59 | 1.51 | 1.51 |
| 439.49 | 2.31 | 2.31 |
| 425.47 | 1.15 | 1.15 |
| 435.48 | 2.13 | 2.13 |
| 481.53 | 2.20 | 2.20 |
| 443.57 | 3.31 | 3.31 |
| 466.52 | 2.26 | 2.26 |
| 485.57 | 3.97 | 3.97 |
| 477.50 | 2.35 | 2.35 |
| 480.59 | 3.51 | 3.51 |
| 482.56 | 2.36 | 2.36 |
| 485.57 | 3.97 | 3.97 |
| 439.49 | 1.66 | 1.66 |
| 423.49 | 2.69 | 2.69 |
| 423.49 | 2.69 | 2.69 |
| 526.59 | 2.27 | 2.27 |
| 519.58 | 2.57 | 2.57 |
| 483.55 | 2.32 | 2.32 |
| 403.46 | 1.27 | 1.27 |
| 546.67 | 2.90 | 2.90 |
| 546.67 | 2.90 | 2.90 |
| 474.58 | 1.59 | 1.59 |
| 474.58 | 1.59 | 1.59 |
| 529.66 | 1.28 | 1.28 |
| 547.65 | 1.42 | 1.42 |
| 504.58 | 1.87 | 1.87 |
| 532.64 | 2.51 | 2.51 |
| 504.58 | 1.87 | 1.87 |
| 532.64 | 2.51 | 2.51 |
| 522.63 | 2.52 | 2.52 |
| 416.50 | 1.23 | 1.23 |
| 416.50 | 1.23 | 1.23 |
| 519.58 | 2.57 | 2.57 |
| 514.65 | 2.37 | 2.37 |
| 535.62 | 1.90 | 1.90 |
| 545.68 | 2.38 | 2.38 |
| 531.65 | 1.99 | 1.99 |
| 421.45 | 1.41 | 1.41 |
| 462.55 | 1.92 | 1.92 |
| 531.65 | 1.99 | 1.99 |
| 558.70 | 2.77 | 2.77 |
| 557.72 | 2.06 | 2.06 |
| 515.64 | 1.77 | 1.77 |
| 462.55 | 1.92 | 1.92 |
| 558.70 | 2.77 | 2.77 |
| 500.62 | 2.13 | 2.13 |
| 515.64 | 1.77 | 1.77 |
| 543.69 | 1.67 | 1.67 |
| 557.72 | 2.06 | 2.06 |
| 501.61 | 1.52 | 1.52 |
| 501.61 | 1.52 | 1.52 |
| 565.64 | 1.91 | 1.91 |
| 559.69 | 1.29 | 1.29 |
| 575.71 | 2.39 | 2.39 |
| 543.69 | 1.67 | 1.67 |
| 564.11 | 1.93 | 1.93 |
| 564.11 | 1.93 | 1.93 |
| 530.65 | 2.13 | 2.13 |
| 552.65 | 2.53 | 2.53 |
| 526.59 | 2.27 | 2.27 |
| 526.59 | 2.27 | 2.27 |
| 442.54 | 1.58 | 1.58 |
| 504.61 | 1.60 | 1.60 |
| 530.65 | 1.99 | 1.99 |
| 510.57 | 2.38 | 2.38 |
| 528.63 | 1.90 | 1.90 |
| 542.66 | 2.29 | 2.29 |
| 540.69 | 3.44 | 3.44 |
| 514.65 | 2.52 | 2.52 |
| 514.65 | 2.52 | 2.52 |
| 486.59 | 1.74 | 1.74 |
| 486.59 | 1.74 | 1.74 |
| 518.61 | 2.12 | 2.12 |
| 500.62 | 1.98 | 1.98 |
| 528.61 | 1.98 | 1.98 |
| 501.61 | 0.50 | 0.50 |
| 529.66 | 2.16 | 2.16 |
| 531.65 | 1.99 | 1.99 |
| 531.65 | 1.99 | 1.99 |
| 510.62 | 1.84 | 1.84 |
| 510.62 | 1.84 | 1.84 |
| 547.65 | 1.42 | 1.42 |
| 553.61 | 2.04 | 2.04 |
| 472.57 | 1.35 | 1.35 |
| 529.66 | 2.16 | 2.16 |
| 529.66 | 2.16 | 2.16 |
| 559.69 | 1.29 | 1.29 |
| 518.61 | 2.26 | 2.26 |
| 510.62 | 2.38 | 2.38 |
| 518.61 | 2.26 | 2.26 |
| 504.61 | 1.60 | 1.60 |
| 563.63 | 1.81 | 1.81 |
| 496.56 | 2.45 | 2.45 |
| 496.59 | 2.04 | 2.04 |
| 522.63 | 2.52 | 2.52 |
| 502.59 | 1.51 | 1.51 |
| 492.57 | 1.73 | 1.73 |
| 536.65 | 2.91 | 2.91 |
| 522.63 | 2.57 | 2.57 |
| 536.65 | 2.91 | 2.91 |
| 531.68 | 1.52 | 1.52 |
| 543.69 | 1.67 | 1.67 |
| 527.65 | 1.57 | 1.57 |
| 577.65 | 2.20 | 2.20 |
| 565.64 | 1.91 | 1.91 |
| 547.65 | 1.61 | 1.61 |
| 501.61 | 1.08 | 1.08 |
| 517.65 | 1.18 | 1.18 |
| 529.66 | 1.28 | 1.28 |
| 488.57 | 1.12 | 1.12 |
| 575.73 | 1.54 | 1.54 |
| 452.54 | 2.02 | 2.02 |
| 513.66 | 2.04 | 2.04 |
| 513.66 | 2.04 | 2.04 |
| 459.57 | 0.91 | 0.91 |
| 559.69 | 1.29 | 1.29 |
| 557.72 | 2.06 | 2.06 |
| 522.63 | 2.57 | 2.57 |
| 508.60 | 2.18 | 2.18 |
| 536.65 | 2.87 | 2.87 |
| 508.64 | 3.14 | 3.14 |
| 513.66 | 2.04 | 2.04 |
| 557.72 | 2.06 | 2.06 |
| 550.68 | 2.91 | 2.91 |
| 548.67 | 2.66 | 2.66 |
| 543.69 | 1.40 | 1.40 |
| 553.61 | 2.04 | 2.04 |
| 527.69 | 2.43 | 2.43 |
| 507.62 | 2.54 | 2.54 |
| 488.61 | 1.90 | 1.90 |
| 493.59 | 2.55 | 2.55 |
| 499.64 | 1.70 | 1.70 |
| 438.51 | 1.76 | 1.76 |
| 543.69 | 1.59 | 1.59 |
| 547.65 | 1.42 | 1.42 |
| 507.62 | 2.54 | 2.54 |
| 575.71 | 2.20 | 2.20 |
| 500.50 | 2.13 | 2.13 |
| 493.59 | 2.55 | 2.55 |
| 399.43 | 0.82 | 0.82 |
| 454.51 | 2.12 | 2.12 |
| 424.48 | 2.15 | 2.15 |
| 410.46 | 2.13 | 2.13 |
| 410.48 | 2.44 | 2.44 |