Assay Detail
Binding
CHEMBL5734932
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorescence Resonance Energy Transfer (FRET) Assay: FRET assay can be used to effectively monitor the inhibition of CBF binding to the Runt domain of RUNX proteins (as well as for CBFβ-SMMHC binding to the Runt domain of RUNX proteins). For the assay, the green fluorescent protein derivative Cerulean is fused to the N-terminus of the Runt domain and the green fluorescent protein derivative Venus to the N-terminus of CBFβ.
48
Total Activities
15
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Runt-related transcription factor 1 (CHEMBL1615385) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cancer therapeutics
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.25 | 5.77 |
| kon | 16 | - | - |
| k_off | 16 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5817797 | — | — | 3 | 5.77 |
| CHEMBL5861850 | — | — | 3 | 5.76 |
| CHEMBL5767058 | — | — | 3 | 5.67 |
| CHEMBL5985101 | — | — | 3 | 5.58 |
| CHEMBL6030757 | — | — | 3 | 5.58 |
| CHEMBL5860717 | — | — | 3 | 5.53 |
| CHEMBL3675778 | — | — | 3 | 5.50 |
| CHEMBL5842188 | — | — | 3 | 5.32 |
| CHEMBL5878001 | — | — | 3 | 5.30 |
| CHEMBL5866082 | — | — | 3 | 5.05 |
| CHEMBL162609 | — | — | 6 | 4.46 |
| CHEMBL5850083 | — | — | 3 | 4.31 |
| CHEMBL3675771 | — | — | 3 | - |
| CHEMBL199982 | — | — | 3 | - |
| CHEMBL1335397 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5817797 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5861850 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL5767058 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL5985101 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL6030757 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL5860717 | — | IC50 | = | 2970.0 | nM | 5.53 |
| CHEMBL3675778 | — | IC50 | = | 3190.0 | nM | 5.50 |
| CHEMBL5842188 | — | IC50 | = | 4830.0 | nM | 5.32 |
| CHEMBL5878001 | — | IC50 | = | 4970.0 | nM | 5.30 |
| CHEMBL5866082 | — | IC50 | = | 8910.0 | nM | 5.05 |
| CHEMBL162609 | — | IC50 | = | 34300.0 | nM | 4.46 |
| CHEMBL162609 | — | IC50 | = | 34300.0 | nM | 4.46 |
| CHEMBL5850083 | — | IC50 | = | 48900.0 | nM | 4.31 |
| CHEMBL3675771 | — | kon | = | - | — | - |
| CHEMBL5842188 | — | kon | = | - | — | - |
| CHEMBL3675771 | — | k_off | = | - | s-1 | - |
| CHEMBL199982 | — | IC50 | > | 34300.0 | nM | - |
| CHEMBL199982 | — | kon | = | - | — | - |
| CHEMBL199982 | — | k_off | = | - | s-1 | - |
| CHEMBL1335397 | — | IC50 | > | 34300.0 | nM | - |
| CHEMBL1335397 | — | kon | = | - | — | - |
| CHEMBL5842188 | — | k_off | = | - | s-1 | - |
| CHEMBL162609 | — | kon | = | - | — | - |
| CHEMBL162609 | — | k_off | = | - | s-1 | - |
| CHEMBL3675778 | — | kon | = | - | — | - |
| CHEMBL3675778 | — | k_off | = | - | s-1 | - |
| CHEMBL5985101 | — | kon | = | - | — | - |
| CHEMBL5985101 | — | k_off | = | - | s-1 | - |
| CHEMBL5817797 | — | kon | = | - | — | - |
| CHEMBL5817797 | — | k_off | = | - | s-1 | - |
| CHEMBL5767058 | — | k_off | = | - | s-1 | - |
| CHEMBL5878001 | — | kon | = | - | — | - |
| CHEMBL5861850 | — | k_off | = | - | s-1 | - |
| CHEMBL5866082 | — | kon | = | - | — | - |
| CHEMBL5866082 | — | k_off | = | - | s-1 | - |
| CHEMBL5861850 | — | kon | = | - | — | - |
| CHEMBL5878001 | — | k_off | = | - | s-1 | - |
| CHEMBL5860717 | — | kon | = | - | — | - |
| CHEMBL5860717 | — | k_off | = | - | s-1 | - |
| CHEMBL3675771 | — | IC50 | > | 34300.0 | nM | - |
| CHEMBL5850083 | — | k_off | = | - | s-1 | - |
| CHEMBL6030757 | — | kon | = | - | — | - |
| CHEMBL5850083 | — | kon | = | - | — | - |
| CHEMBL6030757 | — | k_off | = | - | s-1 | - |
| CHEMBL5767058 | — | kon | = | - | — | - |
| CHEMBL1335397 | — | k_off | = | - | s-1 | - |
| CHEMBL162609 | — | kon | = | - | — | - |
| CHEMBL162609 | — | k_off | = | - | s-1 | - |