Assay Detail
Binding
CHEMBL5730005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time Resolved-Fluorescence Resonance Energy Transfer (TR-FRET) Assay: The inhibition constant (Ki) is the dissociation constant of an enzyme-inhibitor complex or a protein/small molecule complex, wherein the small molecule is inhibiting binding of one protein to another protein or peptide. Where the Ki for a compound is represented as > (greater than) a certain numerical value, it is intended to mean that the binding affinity value (e.g., for Bcl-XL) is greater than the limits of detection of the assay used. Where the binding selectivity ratio for a compound is represented as > (greater than) a certain numerical value, it is intended to mean that the selectivity of a particular compound for Bcl-2 over Bcl-XL is at least as great as the number indicated. Where the Ki for a compound is represented as < (less than) a certain numerical value, it is intended to mean that the binding affinity value (e.g., for Bcl-2) is lower than the limit of detection of the assay used. Inhibition constants were determined using Wang's equation (Wang Z-X).
39
Total Activities
13
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Bcl-2-selective apoptosis-inducing agents for the treatment of cancer and immune diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 10.18 | 10.85 |
| kon | 13 | - | - |
| k_off | 13 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4110818 | — | — | 3 | 10.85 |
| CHEMBL4111550 | — | — | 3 | 10.44 |
| CHEMBL3903167 | — | — | 3 | 10.44 |
| CHEMBL3137309 | VENETOCLAX | 4.0 | 3 | 10.44 |
| CHEMBL3961062 | — | — | 3 | 10.15 |
| CHEMBL3930583 | — | — | 3 | 8.78 |
| CHEMBL3986326 | — | — | 3 | - |
| CHEMBL3978114 | — | — | 3 | - |
| CHEMBL4114397 | — | — | 3 | - |
| CHEMBL4109545 | — | — | 3 | - |
| CHEMBL3915032 | — | — | 3 | - |
| CHEMBL3900610 | — | — | 3 | - |
| CHEMBL3925160 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4110818 | — | Ki | = | 0.014 | nM | 10.85 |
| CHEMBL3137309 | VENETOCLAX | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3903167 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL4111550 | — | Ki | = | 0.036 | nM | 10.44 |
| CHEMBL3961062 | — | Ki | = | 0.071 | nM | 10.15 |
| CHEMBL3930583 | — | Ki | = | 1.654 | nM | 8.78 |
| CHEMBL3986326 | — | k_off | = | - | s-1 | - |
| CHEMBL3986326 | — | Ki | < | 0.01 | nM | - |
| CHEMBL3961062 | — | kon | = | - | — | - |
| CHEMBL3961062 | — | k_off | = | - | s-1 | - |
| CHEMBL3978114 | — | Ki | < | 0.01 | nM | - |
| CHEMBL3978114 | — | kon | = | - | — | - |
| CHEMBL3978114 | — | k_off | = | - | s-1 | - |
| CHEMBL4110818 | — | kon | = | - | — | - |
| CHEMBL3915032 | — | k_off | = | - | s-1 | - |
| CHEMBL4114397 | — | Ki | < | 0.01 | nM | - |
| CHEMBL4114397 | — | kon | = | - | — | - |
| CHEMBL4114397 | — | k_off | = | - | s-1 | - |
| CHEMBL4109545 | — | Ki | < | 0.01 | nM | - |
| CHEMBL4109545 | — | kon | = | - | — | - |
| CHEMBL4109545 | — | k_off | = | - | s-1 | - |
| CHEMBL3915032 | — | Ki | < | 0.01 | nM | - |
| CHEMBL3925160 | — | Ki | < | 0.01 | nM | - |
| CHEMBL3925160 | — | kon | = | - | — | - |
| CHEMBL3900610 | — | Ki | < | 0.01 | nM | - |
| CHEMBL3900610 | — | kon | = | - | — | - |
| CHEMBL3900610 | — | k_off | = | - | s-1 | - |
| CHEMBL3930583 | — | kon | = | - | — | - |
| CHEMBL3930583 | — | k_off | = | - | s-1 | - |
| CHEMBL4111550 | — | kon | = | - | — | - |
| CHEMBL4111550 | — | k_off | = | - | s-1 | - |
| CHEMBL3986326 | — | kon | = | - | — | - |
| CHEMBL3915032 | — | kon | = | - | — | - |
| CHEMBL3925160 | — | k_off | = | - | s-1 | - |
| CHEMBL3903167 | — | kon | = | - | — | - |
| CHEMBL3903167 | — | k_off | = | - | s-1 | - |
| CHEMBL3137309 | VENETOCLAX | kon | = | - | — | - |
| CHEMBL3137309 | VENETOCLAX | k_off | = | - | s-1 | - |
| CHEMBL4110818 | — | k_off | = | - | s-1 | - |