Assay Detail
Binding
CHEMBL3705758
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogeneous Time-Resolve Fluorescence (HTRF) Assay: One potential limitation of the above FP assay is the risk of selection of compounds that may interfere with the FP assays and produce so called false-positives. Therefore, during development of embodiments of the present invention, a time-resolved fluorescence resonance energy transfer (TR-FRET) assay was utilized as a secondary, assay (e.g. for confirmation of results), commercialized by CIS-BIO as homogeneous time-resolve fluorescence (HTRF) assay. In some embodiments, the HTRF assay may be the primary assay and the FP assay is used as a secondary assay to confirm results. HTRF is based on the non-radiative energy transfer of the long-lived emission from the Europium cryptate (Eu3+-cryptate) donor to the allophycocyanin (XL665) acceptor, combined with time-resolved detection. When these two fluorophores are brought together by a biomolecular interaction, a portion of the energy captured by the Eu3+-cryptate during excitation at 337 nm is released through fluorescence emission.
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Compositions and methods for treatment of leukemia
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 4.77 | 5.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1401388 | — | — | 1 | 5.92 |
| CHEMBL3696195 | — | — | 1 | 5.16 |
| CHEMBL3696196 | — | — | 1 | 4.55 |
| CHEMBL3696206 | — | — | 1 | 4.48 |
| CHEMBL3696166 | — | — | 1 | 4.46 |
| CHEMBL3696165 | — | — | 1 | 4.07 |
| CHEMBL1703614 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1401388 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3696195 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL3696196 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL3696206 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL3696166 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL3696165 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL1703614 | — | IC50 | = | 200000.0 | nM | - |