Basic Information
ID: ALA3705323
Type: Binding
Description: DELFIA assay: The kinase activity is measured by DELFIA assay (dissociation-enhanced lanthanide fluorescence immunoassay, Perkin Elmer). The cytoplasmic kinase domain of human IGF-1R (amino acids 964-1370) is expressed as a fusion protein with a glutathione-S-transferase tag (IGF-1R-GST) in High Five Cells (Invitrogen). Enzyme activity is measured in the presence of substances and a control substance. Poly-glutamate-tyrosine peptide (pEY, Sigma Aldrich) and biotinylated pEY (bio-pEY) are used as reaction substrates. 10 uL of substance in 25% DMSO are mixed with 30 uL of IGF-1R-GST solution (67 mM HEPES pH 7.4, 15 ug/mL pEY, 1.7 ug/mL bio-pEY, 13.3 mM MgCl2, 3.3 mM dithiothreitol, 0.0033% Brij 35, 2 ng IGF-1R-GST) in 96-well plates. The reactions are started with 10 uL of a 750 uM ATP solution. After 40 min at RT the reactions are stopped with 50 uL of stop solution (250 mM EDTA, 20 mM HEPES pH 7.4).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705323
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 455.52 | 4.49 | 4.49 |
| 475.94 | 4.83 | 4.83 |
| 481.58 | 5.31 | 5.31 |
| 465.51 | 4.84 | 4.84 |
| 537.67 | 4.38 | 4.38 |
| 544.06 | 4.72 | 4.72 |
| 353.43 | 4.39 | 4.39 |
| 419.92 | 4.82 | 4.82 |
| 383.46 | 4.39 | 4.39 |
| 387.87 | 5.04 | 5.04 |
| 417.90 | 5.05 | 5.05 |
| 391.87 | 3.77 | 3.77 |
| 496.62 | 4.87 | 4.87 |
| 395.47 | 4.32 | 4.32 |
| 481.60 | 4.15 | 4.15 |
| 531.06 | 5.52 | 5.52 |
| 387.87 | 5.04 | 5.04 |
| 401.90 | 5.60 | 5.60 |
| 405.89 | 4.26 | 4.26 |
| 407.48 | 5.44 | 5.44 |
| 349.44 | 3.77 | 3.77 |
| 409.49 | 4.95 | 4.95 |
| 367.46 | 4.69 | 4.69 |
| 408.51 | 3.07 | 3.07 |
| 381.48 | 4.95 | 4.95 |
| 397.48 | 4.79 | 4.79 |
| 437.43 | 5.28 | 5.28 |
| 427.90 | 4.69 | 4.69 |
| 433.95 | 5.38 | 5.38 |
| 419.92 | 4.64 | 4.64 |
| 405.89 | 4.33 | 4.33 |
| 389.51 | 2.78 | 2.78 |
| 515.66 | 4.21 | 4.21 |
| 529.69 | 4.60 | 4.60 |
| 509.66 | 4.63 | 4.63 |
| 509.66 | 4.63 | 4.63 |
| 537.67 | 4.14 | 4.14 |
| 495.63 | 4.07 | 4.07 |
| 509.66 | 4.63 | 4.63 |
| 381.48 | 4.87 | 4.87 |
| 524.67 | 5.35 | 5.35 |
| 401.90 | 4.96 | 4.96 |
| 385.48 | 3.53 | 3.53 |
| 358.41 | 3.30 | 3.30 |
| 417.52 | 5.46 | 5.46 |
| 371.45 | 3.04 | 3.04 |
| 418.50 | 4.86 | 4.86 |
| 567.69 | 4.29 | 4.29 |
| 525.66 | 4.22 | 4.22 |
| 540.67 | 4.94 | 4.94 |
| 540.67 | 4.80 | 4.80 |
| 397.48 | 4.32 | 4.32 |
| 525.66 | 4.08 | 4.08 |
| 567.69 | 4.15 | 4.15 |
| 427.51 | 4.33 | 4.33 |
| 538.70 | 5.74 | 5.74 |
| 540.67 | 4.80 | 4.80 |
| 397.48 | 4.32 | 4.32 |
| 525.66 | 4.08 | 4.08 |
| 567.69 | 4.15 | 4.15 |
| 427.51 | 4.33 | 4.33 |
| 523.69 | 5.02 | 5.02 |
| 565.72 | 5.09 | 5.09 |
| 510.64 | 5.18 | 5.18 |
| 367.46 | 4.69 | 4.69 |
| 495.63 | 4.46 | 4.46 |
| 537.67 | 4.53 | 4.53 |
| 397.48 | 4.70 | 4.70 |
| 526.64 | 4.88 | 4.88 |
| 383.45 | 4.39 | 4.39 |
| 511.63 | 4.16 | 4.16 |
| 553.67 | 4.23 | 4.23 |
| 413.48 | 4.40 | 4.40 |
| 545.09 | 5.83 | 5.83 |
| 401.90 | 5.35 | 5.35 |
| 530.08 | 5.11 | 5.11 |
| 572.11 | 5.18 | 5.18 |
| 431.93 | 5.36 | 5.36 |
| 524.67 | 5.49 | 5.49 |
| 381.48 | 5.00 | 5.00 |
| 509.66 | 4.76 | 4.76 |
| 551.70 | 4.84 | 4.84 |
| 411.51 | 5.01 | 5.01 |
| 545.09 | 6.08 | 6.08 |
| 530.08 | 5.36 | 5.36 |
| 431.93 | 5.61 | 5.61 |
| 500.60 | 4.77 | 4.77 |
| 357.42 | 4.29 | 4.29 |
| 485.59 | 4.05 | 4.05 |
| 527.63 | 4.12 | 4.12 |
| 387.44 | 4.30 | 4.30 |
| 405.89 | 4.26 | 4.26 |
| 447.97 | 5.07 | 5.07 |
| 406.88 | 4.64 | 4.64 |
| 431.93 | 4.65 | 4.65 |
| 441.93 | 4.93 | 4.93 |
| 405.89 | 4.08 | 4.08 |
| 516.05 | 4.80 | 4.80 |
| 371.45 | 3.43 | 3.43 |
| 558.09 | 4.87 | 4.87 |
| 367.46 | 4.31 | 4.31 |
| 359.48 | 4.77 | 4.77 |
| 319.41 | 3.76 | 3.76 |
| 335.41 | 3.43 | 3.43 |
| 412.50 | 4.70 | 4.70 |
| 325.80 | 3.68 | 3.68 |
| 321.38 | 2.87 | 2.87 |
| 412.50 | 4.70 | 4.70 |
| 382.47 | 4.69 | 4.69 |
| 412.50 | 4.70 | 4.70 |
| 412.50 | 4.70 | 4.70 |
| 319.41 | 3.67 | 3.67 |
| 333.44 | 4.02 | 4.02 |
| 331.42 | 3.99 | 3.99 |
| 459.60 | 3.75 | 3.75 |
| 331.42 | 3.67 | 3.67 |
| 501.64 | 3.50 | 3.50 |
| 551.70 | 4.34 | 4.34 |
| 509.66 | 4.26 | 4.26 |
| 381.48 | 4.50 | 4.50 |
| 411.51 | 4.51 | 4.51 |
| 524.67 | 4.99 | 4.99 |
| 373.42 | 3.99 | 3.99 |
| 471.57 | 3.74 | 3.74 |
| 486.58 | 4.46 | 4.46 |
| 343.39 | 3.98 | 3.98 |
| 479.33 | 4.99 | 4.99 |
| 561.09 | 5.53 | 5.53 |
| 417.90 | 5.05 | 5.05 |
| 546.08 | 4.81 | 4.81 |
| 588.11 | 4.88 | 4.88 |
| 447.93 | 5.06 | 5.06 |
| 378.44 | 4.26 | 4.26 |
| 545.09 | 5.83 | 5.83 |
| 401.90 | 5.35 | 5.35 |
| 530.08 | 5.11 | 5.11 |
| 431.93 | 5.36 | 5.36 |
| 572.11 | 5.18 | 5.18 |
| 549.05 | 5.66 | 5.66 |
| 405.86 | 5.18 | 5.18 |
| 534.04 | 4.94 | 4.94 |
| 435.89 | 5.19 | 5.19 |
| 576.08 | 5.01 | 5.01 |
| 523.64 | 4.22 | 4.22 |
| 572.11 | 5.43 | 5.43 |
| 489.62 | 3.68 | 3.68 |
| 461.57 | 2.86 | 2.86 |
| 489.62 | 3.50 | 3.50 |
| 475.60 | 3.25 | 3.25 |
| 503.65 | 3.85 | 3.85 |
| 501.64 | 3.82 | 3.82 |
| 531.66 | 3.45 | 3.45 |
| 362.48 | 3.57 | 3.57 |
| 499.62 | 2.19 | 2.19 |
| 513.65 | 2.85 | 2.85 |
| 415.50 | 3.79 | 3.79 |
| 509.04 | 4.48 | 4.48 |
| 487.63 | 4.21 | 4.21 |
| 435.92 | 3.88 | 3.88 |
| 391.50 | 3.97 | 3.97 |
| 397.90 | 3.83 | 3.83 |
| 393.90 | 5.10 | 5.10 |
| 497.65 | 3.61 | 3.61 |
| 498.59 | 3.77 | 3.77 |
| 454.99 | 3.86 | 3.86 |
| 496.62 | 4.00 | 4.00 |
| 488.62 | 4.14 | 4.14 |
| 441.95 | 3.94 | 3.94 |
| 411.92 | 4.32 | 4.32 |
| 455.57 | 2.49 | 2.49 |
| 441.95 | 3.94 | 3.94 |
| 377.48 | 3.49 | 3.49 |
| 469.60 | 2.83 | 2.83 |
| 482.59 | 4.33 | 4.33 |
| 429.53 | 3.46 | 3.46 |
| 373.49 | 4.76 | 4.76 |
| 434.57 | 3.51 | 3.51 |
| 421.53 | 3.60 | 3.60 |
| 456.55 | 2.92 | 2.92 |
| 449.95 | 3.81 | 3.81 |
| 462.99 | 3.72 | 3.72 |
| 428.54 | 3.71 | 3.71 |
| 478.60 | 4.22 | 4.22 |
| 421.53 | 3.60 | 3.60 |
| 440.56 | 3.68 | 3.68 |
| 458.57 | 3.16 | 3.16 |
| 482.59 | 3.69 | 3.69 |
| 385.48 | 3.53 | 3.53 |
| 414.52 | 3.14 | 3.14 |
| 405.89 | 4.26 | 4.26 |
| 448.96 | 3.80 | 3.80 |
| 415.50 | 3.79 | 3.79 |
| 534.57 | 4.37 | 4.37 |
| 458.57 | 3.08 | 3.08 |
| 387.45 | 3.13 | 3.13 |
| 428.54 | 3.07 | 3.07 |
| 357.42 | 3.12 | 3.12 |
| 481.51 | 3.75 | 3.75 |
| 429.53 | 3.46 | 3.46 |
| 442.57 | 3.38 | 3.38 |
| 496.62 | 4.00 | 4.00 |
| 502.64 | 4.93 | 4.93 |
| 476.63 | 4.89 | 4.89 |
| 401.47 | 3.05 | 3.05 |
| 415.50 | 3.15 | 3.15 |
| 433.95 | 4.74 | 4.74 |
| 458.57 | 3.08 | 3.08 |
| 385.48 | 4.16 | 4.16 |
| 480.52 | 3.75 | 3.75 |
| 482.98 | 4.60 | 4.60 |
| 399.50 | 3.83 | 3.83 |
| 429.53 | 3.46 | 3.46 |
| 462.99 | 3.72 | 3.72 |
| 428.54 | 3.07 | 3.07 |
| 415.50 | 3.15 | 3.15 |
| 399.50 | 4.09 | 4.09 |
| 401.47 | 3.23 | 3.23 |
| 512.62 | 3.70 | 3.70 |
| 503.01 | 4.42 | 4.42 |
| 482.59 | 4.07 | 4.07 |
| 432.51 | 3.28 | 3.28 |
| 387.45 | 3.13 | 3.13 |
| 480.52 | 3.75 | 3.75 |
| 437.45 | 4.20 | 4.20 |
| 391.87 | 3.77 | 3.77 |
| 385.48 | 3.35 | 3.35 |
| 449.95 | 3.81 | 3.81 |
| 445.53 | 3.16 | 3.16 |
| 448.96 | 3.80 | 3.80 |
| 419.92 | 4.18 | 4.18 |
| 449.95 | 3.81 | 3.81 |
| 517.04 | 4.34 | 4.34 |
| 428.54 | 3.45 | 3.45 |
| 419.46 | 3.37 | 3.37 |
| 415.50 | 3.54 | 3.54 |
| 431.50 | 3.24 | 3.24 |
| 458.53 | 2.68 | 2.68 |
| 385.48 | 3.35 | 3.35 |
| 496.54 | 4.09 | 4.09 |
| 478.60 | 4.22 | 4.22 |
| 445.53 | 3.16 | 3.16 |
| 498.59 | 3.77 | 3.77 |
| 415.50 | 3.36 | 3.36 |
| 405.89 | 3.70 | 3.70 |
| 458.57 | 3.08 | 3.08 |
| 446.53 | 3.21 | 3.21 |
| 442.53 | 3.23 | 3.23 |
| 371.45 | 3.60 | 3.60 |
| 375.41 | 3.26 | 3.26 |
| 333.44 | 4.40 | 4.40 |
| 391.87 | 3.77 | 3.77 |
| 405.89 | 3.70 | 3.70 |
| 419.92 | 4.01 | 4.01 |
| 442.53 | 2.59 | 2.59 |
| 385.48 | 3.91 | 3.91 |
| 483.50 | 4.17 | 4.17 |
| 415.50 | 3.79 | 3.79 |
| 444.54 | 3.15 | 3.15 |
| 476.97 | 3.25 | 3.25 |
| 551.48 | 5.00 | 5.00 |
| 415.50 | 3.54 | 3.54 |
| 399.50 | 3.66 | 3.66 |
| 508.53 | 3.20 | 3.20 |
| 453.47 | 4.55 | 4.55 |
| 385.48 | 3.35 | 3.35 |
| 387.45 | 3.13 | 3.13 |
| 435.92 | 3.88 | 3.88 |
| 550.59 | 4.71 | 4.71 |
| 439.45 | 4.06 | 4.06 |
| 363.47 | 4.41 | 4.41 |
| 431.50 | 3.24 | 3.24 |
| 428.50 | 2.67 | 2.67 |
| 419.92 | 4.01 | 4.01 |
| 439.45 | 4.06 | 4.06 |
| 401.47 | 3.44 | 3.44 |
| 446.49 | 2.81 | 2.81 |
| 389.44 | 3.74 | 3.74 |
| 401.47 | 3.61 | 3.61 |
| 437.45 | 4.03 | 4.03 |
| 389.48 | 4.46 | 4.46 |
| 441.49 | 4.40 | 4.40 |
| 461.91 | 4.75 | 4.75 |
| 455.52 | 4.58 | 4.58 |
| 475.94 | 5.31 | 5.31 |
| 441.49 | 4.48 | 4.48 |
| 469.55 | 4.97 | 4.97 |
| 467.55 | 5.22 | 5.22 |
| 445.91 | 4.66 | 4.66 |
| 445.91 | 5.05 | 5.05 |
| 484.56 | 3.77 | 3.77 |
| 607.76 | 5.16 | 5.16 |
| 509.61 | 3.83 | 3.83 |
| 563.71 | 5.14 | 5.14 |
| 537.67 | 4.61 | 4.61 |
| 607.76 | 5.16 | 5.16 |
| 497.60 | 3.69 | 3.69 |
| 535.65 | 4.22 | 4.22 |
| 523.64 | 4.22 | 4.22 |
| 511.63 | 4.08 | 4.08 |
| 646.84 | 5.46 | 5.46 |
| 537.67 | 4.61 | 4.61 |
| 563.71 | 5.04 | 5.04 |
| 567.69 | 4.24 | 4.24 |
| 553.67 | 3.58 | 3.58 |
| 549.68 | 4.75 | 4.75 |
| 593.73 | 4.77 | 4.77 |
| 546.08 | 4.73 | 4.73 |
| 628.18 | 5.42 | 5.42 |
| 588.11 | 4.23 | 4.23 |
| 628.18 | 5.42 | 5.42 |
| 584.12 | 5.40 | 5.40 |
| 602.14 | 4.89 | 4.89 |
| 584.12 | 5.40 | 5.40 |
| 627.19 | 4.95 | 4.95 |
| 586.14 | 5.65 | 5.65 |
| 574.13 | 5.37 | 5.37 |
| 628.18 | 5.42 | 5.42 |
| 574.09 | 4.11 | 4.11 |
| 572.11 | 5.12 | 5.12 |
| 600.17 | 6.04 | 6.04 |
| 601.11 | 3.55 | 3.55 |
| 635.17 | 5.84 | 5.84 |
| 645.18 | 4.90 | 4.90 |
| 635.17 | 5.84 | 5.84 |
| 598.15 | 5.65 | 5.65 |
| 613.17 | 4.56 | 4.56 |
| 600.12 | 4.64 | 4.64 |
| 614.19 | 6.60 | 6.60 |
| 612.18 | 6.21 | 6.21 |
| 586.14 | 5.82 | 5.82 |
| 616.17 | 5.45 | 5.45 |
| 642.20 | 5.98 | 5.98 |
| 602.14 | 4.80 | 4.80 |
| 695.31 | 6.68 | 6.68 |
| 642.20 | 5.98 | 5.98 |
| 544.06 | 4.65 | 4.65 |
| 627.19 | 6.93 | 6.93 |
| 510.04 | 3.77 | 3.77 |
| 497.60 | 4.11 | 4.11 |
| 507.61 | 3.81 | 3.81 |
| 503.65 | 3.98 | 3.98 |
| 547.70 | 4.00 | 4.00 |
| 524.07 | 4.33 | 4.33 |
| 568.12 | 4.35 | 4.35 |
| 538.68 | 5.24 | 5.24 |
| 551.70 | 4.53 | 4.53 |
| 542.09 | 4.79 | 4.79 |
| 523.64 | 3.75 | 3.75 |
| 577.73 | 5.07 | 5.07 |
| 494.62 | 5.23 | 5.23 |
| 524.65 | 4.90 | 4.90 |
| 480.60 | 4.88 | 4.88 |
| 537.69 | 4.82 | 4.82 |
| 521.67 | 4.83 | 4.83 |
| 537.67 | 4.53 | 4.53 |
| 601.11 | 3.73 | 3.73 |
| 614.15 | 5.03 | 5.03 |
| 634.18 | 6.44 | 6.44 |
| 440.51 | 3.75 | 3.75 |
| 495.59 | 3.44 | 3.44 |
| 607.76 | 5.08 | 5.08 |
| 511.63 | 3.99 | 3.99 |
| 567.69 | 3.89 | 3.89 |
| 660.87 | 5.77 | 5.77 |
| 581.72 | 4.54 | 4.54 |
| 607.76 | 5.08 | 5.08 |
| 498.59 | 4.08 | 4.08 |
| 525.66 | 4.38 | 4.38 |
| 509.61 | 3.75 | 3.75 |
| 563.71 | 5.06 | 5.06 |
| 532.05 | 4.34 | 4.34 |
| 681.28 | 6.12 | 6.12 |
| 519.01 | 4.42 | 4.42 |
| 530.03 | 4.09 | 4.09 |
| 542.09 | 5.17 | 5.17 |
| 550.49 | 5.37 | 5.37 |
| 516.05 | 4.64 | 4.64 |
| 568.13 | 5.70 | 5.70 |
| 612.18 | 5.72 | 5.72 |
| 586.14 | 5.19 | 5.19 |
| 572.11 | 4.53 | 4.53 |
| 514.03 | 4.39 | 4.39 |
| 593.73 | 4.77 | 4.77 |
| 535.65 | 4.22 | 4.22 |
| 505.62 | 2.97 | 2.97 |
| 491.60 | 2.70 | 2.70 |
| 531.66 | 3.54 | 3.54 |
| 501.64 | 3.91 | 3.91 |
| 517.68 | 4.55 | 4.55 |
| 517.68 | 4.72 | 4.72 |
| 564.12 | 4.93 | 4.93 |
| 572.11 | 4.80 | 4.80 |
| 543.70 | 4.59 | 4.59 |
| 503.65 | 4.24 | 4.24 |
| 606.56 | 5.45 | 5.45 |
| 529.67 | 4.28 | 4.28 |
| 495.63 | 4.12 | 4.12 |
| 489.03 | 4.65 | 4.65 |
| 579.75 | 5.01 | 5.01 |
| 509.66 | 4.46 | 4.46 |
| 537.71 | 5.24 | 5.24 |
| 600.17 | 5.27 | 5.27 |
| 641.22 | 5.11 | 5.11 |
| 558.13 | 5.50 | 5.50 |
| 544.10 | 5.11 | 5.11 |
| 573.15 | 5.54 | 5.54 |
| 614.20 | 5.37 | 5.37 |
| 533.08 | 4.35 | 4.35 |
| 573.72 | 3.79 | 3.79 |
| 566.71 | 4.51 | 4.51 |
| 531.10 | 6.31 | 6.31 |
| 503.05 | 5.68 | 5.68 |
| 515.06 | 5.82 | 5.82 |
| 489.02 | 5.29 | 5.29 |
| 517.08 | 6.07 | 6.07 |
| 529.09 | 6.21 | 6.21 |
| 490.65 | 5.20 | 5.20 |
| 490.65 | 5.37 | 5.37 |
| 420.93 | 4.06 | 4.06 |