Basic Information
ID: ALA3705138
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-βAla-βAla-Phe-Met-Aib-pTyr-(6-Cl-LTrp)-Glu-Ac3c-Leu-Asn-NH2 (SEQ ID NO: 1)) (García-Echeverría et al., J. Med. Chem. 43: 3205-3208 (2000)). This tagged peptide is called PMDM6-F. 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 μg/mL bovine gamma globulin; 0.02% sodium azide, 0.01% Triton X-100) and the polarization values were measured after 3 h of incubation using an ULTRA READER (Tecan U.S. Inc).
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705138
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 552.47 | 3.74 | 3.74 |
| 548.49 | 4.91 | 4.91 |
| 566.50 | 4.08 | 4.08 |
| 578.51 | 4.28 | 4.28 |
| 552.47 | 3.74 | 3.74 |
| 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 |
| 548.49 | 4.91 | 4.91 |
| 576.54 | 5.64 | 5.64 |
| 562.51 | 5.25 | 5.25 |
| 576.54 | 5.69 | 5.69 |
| 827.80 | 8.13 | 8.13 |
| 544.52 | 5.16 | 5.16 |
| 568.48 | 5.24 | 5.24 |
| 564.05 | 4.93 | 4.93 |
| 546.06 | 4.79 | 4.79 |
| 562.51 | 5.30 | 5.30 |
| 546.06 | 4.79 | 4.79 |
| 562.51 | 5.30 | 5.30 |
| 546.06 | 4.79 | 4.79 |
| 564.05 | 4.93 | 4.93 |
| 580.50 | 5.44 | 5.44 |
| 562.51 | 5.30 | 5.30 |
| 560.54 | 5.92 | 5.92 |
| 530.07 | 4.52 | 4.52 |
| 524.11 | 4.59 | 4.59 |
| 562.51 | 5.30 | 5.30 |
| 568.04 | 3.71 | 3.71 |