Assay Detail
Binding
CHEMBL3889232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: Representative compounds were serially diluted in dimethyl sulfoxide (DMSO) starting at 50 uM (2x starting concentration; 10% DMSO) and 10 uL were transferred into a 384-well plate. Then 10 uL of a protein/probe/antibody mix was added to each well at final concentrations listed in TABLE 1. The samples are then mixed on a shaker for 1 minute and incubated for an additional 3 hours at room temperature. For each assay, the probe/antibody and protein/probe/antibody were included on each assay plate as negative and positive controls, respectively. Fluorescence was measured on the ENVISION plate reader (Perkin Elmer) using a 340/35 nm excitation filter and 520/525 (F-Bak peptide) and 495/510 nm (Tb-labeled anti-Histidine antibody) emission filters Inhibition constants (Ki) are shown in TABLE 2 below and were determined using Wang's equation (Wang Z.-X. An Exact Mathematical Expression For Describing Competitive Binding Of Two Different Ligands To A Protein Molecule. FEBS Lett. 1995, 360:111-4).
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 44 | 7.46 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3926447 | — | — | 1 | 10.41 |
| CHEMBL3950005 | — | — | 1 | 10.28 |
| CHEMBL3964082 | — | — | 1 | 10.19 |
| CHEMBL3914582 | — | — | 1 | 10.08 |
| CHEMBL3923607 | — | — | 1 | 9.51 |
| CHEMBL3935424 | — | — | 1 | 9.39 |
| CHEMBL3948854 | — | — | 1 | 9.19 |
| CHEMBL3903384 | — | — | 1 | 8.79 |
| CHEMBL3935806 | — | — | 1 | 8.76 |
| CHEMBL3921048 | — | — | 1 | 8.75 |
| CHEMBL3973825 | — | — | 1 | 8.69 |
| CHEMBL3911407 | — | — | 1 | 8.17 |
| CHEMBL3912602 | — | — | 1 | 7.69 |
| CHEMBL3962876 | — | — | 1 | 7.69 |
| CHEMBL3954629 | — | — | 1 | 7.61 |
| CHEMBL3978310 | — | — | 1 | 7.42 |
| CHEMBL3926997 | — | — | 1 | 7.33 |
| CHEMBL3965688 | — | — | 1 | 7.32 |
| CHEMBL3930124 | — | — | 1 | 7.29 |
| CHEMBL3905577 | — | — | 1 | 7.29 |
| CHEMBL3893173 | — | — | 1 | 7.08 |
| CHEMBL3941074 | — | — | 1 | 6.89 |
| CHEMBL3910451 | — | — | 1 | 6.86 |
| CHEMBL3902143 | — | — | 1 | 6.75 |
| CHEMBL3905254 | — | — | 1 | 6.75 |
| CHEMBL3897719 | — | — | 1 | 6.72 |
| CHEMBL3913077 | — | — | 1 | 6.63 |
| CHEMBL3905470 | — | — | 1 | 6.57 |
| CHEMBL3919771 | — | — | 1 | 6.55 |
| CHEMBL3947773 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3926447 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL3950005 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL3964082 | — | Ki | = | 0.064 | nM | 10.19 |
| CHEMBL3914582 | — | Ki | = | 0.084 | nM | 10.08 |
| CHEMBL3923607 | — | Ki | = | 0.307 | nM | 9.51 |
| CHEMBL3935424 | — | Ki | = | 0.407 | nM | 9.39 |
| CHEMBL3948854 | — | Ki | = | 0.649 | nM | 9.19 |
| CHEMBL3903384 | — | Ki | = | 1.637 | nM | 8.79 |
| CHEMBL3935806 | — | Ki | = | 1.75 | nM | 8.76 |
| CHEMBL3921048 | — | Ki | = | 1.791 | nM | 8.75 |
| CHEMBL3973825 | — | Ki | = | 2.067 | nM | 8.69 |
| CHEMBL3911407 | — | Ki | = | 6.735 | nM | 8.17 |
| CHEMBL3912602 | — | Ki | = | 20.42 | nM | 7.69 |
| CHEMBL3962876 | — | Ki | = | 20.24 | nM | 7.69 |
| CHEMBL3954629 | — | Ki | = | 24.78 | nM | 7.61 |
| CHEMBL3978310 | — | Ki | = | 37.86 | nM | 7.42 |
| CHEMBL3926997 | — | Ki | = | 46.5 | nM | 7.33 |
| CHEMBL3965688 | — | Ki | = | 48.08 | nM | 7.32 |
| CHEMBL3930124 | — | Ki | = | 51.7 | nM | 7.29 |
| CHEMBL3905577 | — | Ki | = | 51.45 | nM | 7.29 |
| CHEMBL3893173 | — | Ki | = | 82.92 | nM | 7.08 |
| CHEMBL3941074 | — | Ki | = | 128.53 | nM | 6.89 |
| CHEMBL3910451 | — | Ki | = | 138.75 | nM | 6.86 |
| CHEMBL3905254 | — | Ki | = | 177.06 | nM | 6.75 |
| CHEMBL3902143 | — | Ki | = | 176.18 | nM | 6.75 |
| CHEMBL3897719 | — | Ki | = | 188.23 | nM | 6.72 |
| CHEMBL3913077 | — | Ki | = | 234.12 | nM | 6.63 |
| CHEMBL3905470 | — | Ki | = | 269.18 | nM | 6.57 |
| CHEMBL3919771 | — | Ki | = | 282.11 | nM | 6.55 |
| CHEMBL3947773 | — | Ki | = | 293.81 | nM | 6.53 |
| CHEMBL3973043 | — | Ki | = | 339.99 | nM | 6.47 |
| CHEMBL3936044 | — | Ki | = | 342.1 | nM | 6.47 |
| CHEMBL3904077 | — | Ki | = | 356.26 | nM | 6.45 |
| CHEMBL3956645 | — | Ki | = | 372.11 | nM | 6.43 |
| CHEMBL3910827 | — | Ki | = | 387.69 | nM | 6.41 |
| CHEMBL3942247 | — | Ki | = | 392.53 | nM | 6.41 |
| CHEMBL3982046 | — | Ki | = | 393.36 | nM | 6.41 |
| CHEMBL3947557 | — | Ki | = | 408.57 | nM | 6.39 |
| CHEMBL3903210 | — | Ki | = | 417.29 | nM | 6.38 |
| CHEMBL3974157 | — | Ki | = | 434.0 | nM | 6.36 |
| CHEMBL3926506 | — | Ki | = | 437.92 | nM | 6.36 |
| CHEMBL3957851 | — | Ki | = | 447.13 | nM | 6.35 |
| CHEMBL3939121 | — | Ki | = | 703.74 | nM | 6.15 |
| CHEMBL3933269 | — | Ki | = | 743.18 | nM | 6.13 |