Assay Detail
Binding
CHEMBL5730205
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 μM (2× starting concentration; 10% DMSO) and 10 μL were transferred into a 384-well plate. Then 10 μL 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 probed antibody and protein/probe/antibody were included on each assay plate as negative and positive controls, respectively. Fluorescence was measured on the Envision (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.
1221
Total Activities
404
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 | 407 | 9.36 | 11.00 |
| kon | 407 | - | - |
| k_off | 407 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3653966 | — | — | 3 | 11.00 |
| CHEMBL3650632 | — | — | 3 | 10.92 |
| CHEMBL3654125 | — | — | 3 | 10.92 |
| CHEMBL3650520 | — | — | 3 | 10.89 |
| CHEMBL3654122 | — | — | 3 | 10.85 |
| CHEMBL3654127 | — | — | 3 | 10.85 |
| CHEMBL3654119 | — | — | 3 | 10.82 |
| CHEMBL3968773 | — | — | 3 | 10.80 |
| CHEMBL3654111 | — | — | 3 | 10.80 |
| CHEMBL3654038 | — | — | 3 | 10.77 |
| CHEMBL3654049 | — | — | 3 | 10.77 |
| CHEMBL3654099 | — | — | 3 | 10.77 |
| CHEMBL3654152 | — | — | 3 | 10.74 |
| CHEMBL3650649 | — | — | 3 | 10.72 |
| CHEMBL3654107 | — | — | 3 | 10.72 |
| CHEMBL3650522 | — | — | 3 | 10.72 |
| CHEMBL3650521 | — | — | 3 | 10.72 |
| CHEMBL3653975 | — | — | 3 | 10.70 |
| CHEMBL3654139 | — | — | 3 | 10.70 |
| CHEMBL3654146 | — | — | 3 | 10.70 |
| CHEMBL3650617 | — | — | 3 | 10.68 |
| CHEMBL3650517 | — | — | 3 | 10.66 |
| CHEMBL3650668 | — | — | 3 | 10.62 |
| CHEMBL3650523 | — | — | 3 | 10.57 |
| CHEMBL3653981 | — | — | 3 | 10.57 |
| CHEMBL3650624 | — | — | 3 | 10.55 |
| CHEMBL3650637 | — | — | 3 | 10.55 |
| CHEMBL3654078 | — | — | 3 | 10.55 |
| CHEMBL3654079 | — | — | 3 | 10.54 |
| CHEMBL3650524 | — | — | 3 | 10.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3653966 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL3650632 | — | Ki | = | 0.012 | nM | 10.92 |
| CHEMBL3654125 | — | Ki | = | 0.012 | nM | 10.92 |
| CHEMBL3650520 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL3654127 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3654122 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3654119 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL3968773 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3654111 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3654049 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL3654099 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL3654038 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL3654152 | — | Ki | = | 0.018 | nM | 10.74 |
| CHEMBL3650649 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3650522 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3650521 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3654107 | — | Ki | = | 0.019 | nM | 10.72 |
| CHEMBL3654139 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3654146 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3653975 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3650617 | — | Ki | = | 0.021 | nM | 10.68 |
| CHEMBL3650517 | — | Ki | = | 0.022 | nM | 10.66 |
| CHEMBL3650668 | — | Ki | = | 0.024 | nM | 10.62 |
| CHEMBL3653981 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3650523 | — | Ki | = | 0.027 | nM | 10.57 |
| CHEMBL3654078 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3650637 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3650624 | — | Ki | = | 0.028 | nM | 10.55 |
| CHEMBL3654079 | — | Ki | = | 0.029 | nM | 10.54 |
| CHEMBL3650524 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3650607 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3654170 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3653978 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL3650638 | — | Ki | = | 0.031 | nM | 10.51 |
| CHEMBL3650594 | — | Ki | = | 0.032 | nM | 10.49 |
| CHEMBL3654120 | — | Ki | = | 0.033 | nM | 10.48 |
| CHEMBL3650604 | — | Ki | = | 0.033 | nM | 10.48 |
| CHEMBL3654090 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL3650525 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL3650662 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL3650634 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL3654159 | — | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL3650664 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3650526 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3650655 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3650595 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3650645 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3653971 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL3654084 | — | Ki | = | 0.037 | nM | 10.43 |
| CHEMBL3653995 | — | Ki | = | 0.037 | nM | 10.43 |