Basic Information
ID: ALA3705834
Type: Binding
Description: Fluorescence-Polarization Binding Assay: The binding affinity of the MDM2 inhibitors was determined using an optimized, sensitive and quantitative fluorescence polarization-based (FP-based) binding assay using a recombinant human His-tagged MDM2 protein (residues 1-118) and a fluorescently tagged p53-based peptide.The design of the fluorescence probe was based upon a previously reported high-affinity p53-based peptidomimetic compound (5-FAM-beta Ala-beta Ala-Phe-Met-Aib-pTyr-(6-Cl-LTrp)-Glu-Ac3c-Leu-Asn-NH2 (SEQ ID NO: 1)) Garcia-Echeverria et al., J. Med. Chem. 43: 3205-3208 (2000)). This tagged peptide is called PMDM6-F. The Kd value of PMDM6-F with the recombinant MDM2 protein was determined from the saturation curve. MDM2 protein was serially double diluted in a Dynex 96-well, black, round-bottom plate, and the PMDM6-F peptide was added at 1 nM concentration. The assay was performed in the buffer: 100 mM potassium phosphate, pH 7.5; 100 ug/mL bovine gamma globulin; 0.02% sodium azide, 0.01% Triton X-100).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705834
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 548.49 | 4.91 | 4.91 |
| 600.52 | 4.33 | 4.33 |
| 552.47 | 3.74 | 3.74 |
| 536.43 | 3.11 | 3.11 |
| 592.52 | 4.00 | 4.00 |
| 566.50 | 4.08 | 4.08 |
| 614.55 | 4.67 | 4.67 |
| 606.55 | 4.39 | 4.39 |
| 620.57 | 4.73 | 4.73 |
| 578.51 | 4.28 | 4.28 |
| 592.54 | 4.62 | 4.62 |
| 606.55 | 4.34 | 4.34 |
| 576.45 | 3.53 | 3.53 |
| 578.51 | 4.28 | 4.28 |
| 568.04 | 3.71 | 3.71 |
| 566.50 | 4.13 | 4.13 |
| 579.06 | 3.96 | 3.96 |
| 582.06 | 4.10 | 4.10 |
| 594.56 | 4.91 | 4.91 |
| 594.56 | 4.77 | 4.77 |
| 608.58 | 5.11 | 5.11 |
| 534.48 | 3.60 | 3.60 |
| 608.58 | 5.25 | 5.25 |
| 580.53 | 4.52 | 4.52 |
| 621.14 | 4.98 | 4.98 |
| 612.55 | 4.91 | 4.91 |
| 596.09 | 4.39 | 4.39 |
| 626.57 | 5.25 | 5.25 |
| 610.12 | 4.74 | 4.74 |
| 578.10 | 4.25 | 4.25 |
| 596.09 | 4.39 | 4.39 |
| 592.13 | 4.60 | 4.60 |
| 610.12 | 4.74 | 4.74 |
| 601.55 | 4.96 | 4.96 |
| 669.62 | 5.29 | 5.29 |
| 576.54 | 5.55 | 5.55 |
| 576.54 | 5.55 | 5.55 |
| 532.06 | 3.16 | 3.16 |
| 582.50 | 2.79 | 2.79 |
| 551.49 | 3.71 | 3.71 |
| 656.51 | 3.91 | 3.91 |
| 706.55 | 6.09 | 6.09 |
| 597.53 | 4.45 | 4.45 |
| 566.50 | 4.08 | 4.08 |
| 583.51 | 4.11 | 4.11 |
| 634.58 | 3.14 | 3.14 |
| 553.46 | 3.14 | 3.14 |
| 553.46 | 3.14 | 3.14 |
| 582.50 | 3.10 | 3.10 |
| 608.54 | 3.64 | 3.64 |
| 590.52 | 4.37 | 4.37 |
| 535.45 | 3.31 | 3.31 |
| 554.01 | 3.37 | 3.37 |
| 536.02 | 3.23 | 3.23 |
| 554.01 | 3.37 | 3.37 |
| 519.56 | 2.71 | 2.71 |
| 537.55 | 2.85 | 2.85 |
| 536.02 | 3.23 | 3.23 |
| 518.03 | 3.09 | 3.09 |
| 532.06 | 3.43 | 3.43 |
| 522.45 | 4.38 | 4.38 |
| 451.37 | 4.88 | 4.88 |
| 618.63 | 5.03 | 5.03 |
| 560.09 | 5.04 | 5.04 |
| 561.53 | 5.09 | 5.09 |
| 575.56 | 5.34 | 5.34 |
| 547.50 | 4.88 | 4.88 |
| 643.55 | 6.42 | 6.42 |
| 579.52 | 5.04 | 5.04 |
| 611.54 | 5.38 | 5.38 |
| 583.48 | 4.95 | 4.95 |
| 548.49 | 4.91 | 4.91 |
| 548.49 | 4.91 | 4.91 |
| 532.03 | 4.40 | 4.40 |
| 532.03 | 4.40 | 4.40 |
| 530.50 | 4.77 | 4.77 |
| 532.03 | 4.40 | 4.40 |
| 550.02 | 4.54 | 4.54 |
| 532.03 | 4.40 | 4.40 |
| 550.02 | 4.54 | 4.54 |
| 566.48 | 5.05 | 5.05 |
| 530.50 | 4.77 | 4.77 |
| 548.49 | 4.91 | 4.91 |
| 566.48 | 5.05 | 5.05 |
| 550.02 | 4.54 | 4.54 |
| 548.49 | 4.91 | 4.91 |
| 550.46 | 3.95 | 3.95 |
| 550.46 | 3.95 | 3.95 |
| 607.60 | 5.14 | 5.14 |
| 548.49 | 4.91 | 4.91 |
| 605.58 | 4.85 | 4.85 |
| 621.58 | 3.82 | 3.82 |
| 566.50 | 4.13 | 4.13 |
| 577.53 | 4.07 | 4.07 |
| 578.51 | 4.13 | 4.13 |
| 575.56 | 5.48 | 5.48 |
| 478.40 | 4.63 | 4.63 |
| 464.37 | 4.37 | 4.37 |
| 575.56 | 5.48 | 5.48 |
| 589.58 | 5.88 | 5.88 |
| 632.65 | 5.42 | 5.42 |
| 604.60 | 4.64 | 4.64 |
| 630.64 | 5.17 | 5.17 |
| 654.64 | 3.58 | 3.58 |
| 464.37 | 4.37 | 4.37 |
| 548.49 | 4.91 | 4.91 |
| 548.49 | 4.91 | 4.91 |
| 593.55 | 5.43 | 5.43 |
| 611.57 | 4.08 | 4.08 |
| 536.48 | 4.77 | 4.77 |
| 576.54 | 3.90 | 3.90 |
| 590.57 | 4.25 | 4.25 |
| 604.60 | 4.64 | 4.64 |
| 566.50 | 4.13 | 4.13 |
| 593.55 | 5.62 | 5.62 |
| 625.59 | 4.42 | 4.42 |
| 618.58 | 5.19 | 5.19 |
| 533.48 | 4.31 | 4.31 |
| 547.50 | 4.66 | 4.66 |
| 575.51 | 4.57 | 4.57 |
| 618.58 | 4.12 | 4.12 |
| 632.61 | 4.51 | 4.51 |
| 591.56 | 4.46 | 4.46 |
| 671.64 | 5.25 | 5.25 |
| 593.55 | 5.66 | 5.66 |
| 617.55 | 4.08 | 4.08 |
| 603.52 | 3.69 | 3.69 |
| 547.50 | 4.75 | 4.75 |
| 589.54 | 5.01 | 5.01 |
| 591.55 | 4.46 | 4.46 |
| 619.61 | 5.23 | 5.23 |
| 679.56 | 5.31 | 5.31 |
| 591.56 | 4.45 | 4.45 |
| 604.55 | 4.80 | 4.80 |
| 563.50 | 3.68 | 3.68 |
| 644.62 | 5.73 | 5.73 |
| 647.58 | 4.55 | 4.55 |
| 561.49 | 4.23 | 4.23 |
| 618.58 | 5.19 | 5.19 |
| 618.58 | 5.15 | 5.15 |
| 586.49 | 3.94 | 3.94 |
| 524.42 | 3.11 | 3.11 |
| 592.52 | 4.00 | 4.00 |
| 581.54 | 4.23 | 4.23 |
| 576.54 | 5.69 | 5.69 |
| 544.52 | 5.16 | 5.16 |
| 633.59 | 5.20 | 5.20 |
| 564.05 | 4.93 | 4.93 |
| 546.06 | 4.79 | 4.79 |
| 546.06 | 4.79 | 4.79 |
| 546.06 | 4.79 | 4.79 |
| 675.67 | 6.23 | 6.23 |
| 709.69 | 6.42 | 6.42 |
| 564.05 | 4.93 | 4.93 |
| 675.67 | 6.23 | 6.23 |
| 580.50 | 5.44 | 5.44 |
| 562.51 | 5.30 | 5.30 |
| 562.51 | 5.30 | 5.30 |
| 633.59 | 5.20 | 5.20 |
| 639.62 | 4.86 | 4.86 |
| 647.62 | 5.59 | 5.59 |
| 661.65 | 5.84 | 5.84 |
| 661.65 | 5.84 | 5.84 |
| 566.50 | 4.13 | 4.13 |
| 619.56 | 4.81 | 4.81 |
| 566.50 | 4.13 | 4.13 |
| 561.53 | 5.27 | 5.27 |
| 534.46 | 4.52 | 4.52 |
| 693.59 | 5.75 | 5.75 |
| 572.51 | 5.37 | 5.37 |
| 574.52 | 5.45 | 5.45 |