Assay Detail
Binding
CHEMBL3705507
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: The measurement of competition of compounds of Formula (I) with F-Bak for a Bcl-2 family protein (Bcl-xL) binding site using a Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) binding assay:Test compounds were serially diluted in DMSO starting at 50 .mu.M (2.times. starting concentration; 10% DMSO) and 10 .mu.L transferred into a 384-well plate. The samples are then mixed on a shaker for 1 minute then incubated for an additional 2 hours at room temperature. For each assay plate, a probe/antibody and protein/antibody/probe mixture were included as a negative and a positive control, respectively. Fluorescence was measured on the ENVISION plate reader (Perkin Elmer) using a 340/35 nm excitation filter and 520/525 (F-Bak) and 495/510 nm (Tb-labeled anti-his antibody) emission filters. Dissociation constants (K.sub.i) were determined using Wang's equation (Wang, Z. X.).
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.85 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3699077 | — | — | 1 | 10.40 |
| CHEMBL3699076 | — | — | 1 | 10.22 |
| CHEMBL3699066 | — | — | 1 | 10.00 |
| CHEMBL3699067 | — | — | 1 | 10.00 |
| CHEMBL3699075 | — | — | 1 | 9.85 |
| CHEMBL3699079 | — | — | 1 | 9.70 |
| CHEMBL3699078 | — | — | 1 | 9.10 |
| CHEMBL3699072 | — | — | 1 | 8.77 |
| CHEMBL3699080 | — | — | 1 | 8.30 |
| CHEMBL3699069 | — | — | 1 | 8.05 |
| CHEMBL3699073 | — | — | 1 | 7.96 |
| CHEMBL3699068 | — | — | 1 | 7.92 |
| CHEMBL3699071 | — | — | 1 | 7.77 |
| CHEMBL3699074 | — | — | 1 | 7.39 |
| CHEMBL3699070 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3699077 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3699076 | — | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL3699066 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3699067 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3699075 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL3699079 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3699078 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3699072 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3699080 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL3699069 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3699073 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3699068 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL3699071 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3699074 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL3699070 | — | Ki | = | 48.0 | nM | 7.32 |