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).
Format: BAO_0000357
Organism: Homo sapiens
Target: Insulin-like growth factor I receptor(ALA1957)
Document: ALA3639315
BindingDB Source: 6316
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 |
| 420.93 | 4.06 | 4.06 |