Assay Detail
Binding
CHEMBL5732769
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ubiquitin Activating Enzyme (UAE) HTRF Assay: The UAE enzymatic reaction totals 50 μL and contains 50 mmol HEPES (pH 7.5), 0.05% BSA, 2.5 mM MgCl2, 0.1 uM ATP, 8 nM GST-Ubc-2, 35 nM flag-ubiquitin, 1 nM recombinant human UAE or mouse UAE. Compounds for this hUAE IC50 assay are tested at 10 point 3-fold dilution. The top concentration for this assay is 1 μM. Each compound is ordered in duplicate on the same plate. The enzymatic reaction mixture is incubated for 90 minutes at room temperature (24 degrees C.) in a 384 well plate prior to termination with a stop solution (0.1 M HEPES/0.05% Tween20, 20 mmol EDTA, 410 mM KF, 0.5 nM Eu Cryptate anti-FLAG M2-K antibody (Cis-bio International), 8 ug/mL Anti-GST XL-APC (Prozyme)). After incubation for 120 minutes, quantification of the FRET is performed on the Pherostar (BMG).
375
Total Activities
120
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
Ubiquitin-like modifier-activating enzyme 1 (CHEMBL5924) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 125 | 6.93 | 7.26 |
| kon | 125 | - | - |
| k_off | 125 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5864078 | — | — | 3 | 7.26 |
| CHEMBL6053122 | — | — | 3 | 7.26 |
| CHEMBL6065415 | — | — | 3 | 7.26 |
| CHEMBL5997651 | — | — | 3 | 7.26 |
| CHEMBL5828810 | — | — | 3 | 7.26 |
| CHEMBL5832385 | — | — | 3 | 7.26 |
| CHEMBL5971124 | — | — | 3 | 7.26 |
| CHEMBL5747752 | — | — | 3 | 7.26 |
| CHEMBL5940945 | — | — | 3 | 7.26 |
| CHEMBL5918592 | — | — | 3 | 7.26 |
| CHEMBL5954380 | — | — | 3 | 7.26 |
| CHEMBL5803994 | — | — | 3 | 7.26 |
| CHEMBL6003529 | — | — | 3 | 7.26 |
| CHEMBL5768102 | — | — | 3 | 7.26 |
| CHEMBL5887314 | — | — | 3 | 7.26 |
| CHEMBL5780833 | — | — | 3 | 7.26 |
| CHEMBL5759269 | — | — | 3 | 7.26 |
| CHEMBL5958476 | — | — | 3 | 7.26 |
| CHEMBL5743820 | — | — | 3 | 6.26 |
| CHEMBL5769060 | — | — | 3 | 6.26 |
| CHEMBL5960054 | — | — | 3 | 6.26 |
| CHEMBL5929395 | — | — | 3 | 6.26 |
| CHEMBL5762899 | — | — | 3 | 6.26 |
| CHEMBL6054356 | — | — | 3 | 6.26 |
| CHEMBL5799754 | — | — | 3 | 6.26 |
| CHEMBL5866556 | — | — | 3 | 6.26 |
| CHEMBL5793677 | — | — | 3 | 6.26 |
| CHEMBL6020119 | — | — | 6 | - |
| CHEMBL5917491 | — | — | 3 | - |
| CHEMBL6012674 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5887314 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6065415 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5997651 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5971124 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5780833 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5747752 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5864078 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6053122 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5803994 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5954380 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5768102 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5832385 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6003529 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5940945 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5828810 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5759269 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5958476 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5918592 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5762899 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5929395 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6054356 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5799754 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5743820 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5793677 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5960054 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5769060 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5866556 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5781268 | — | k_off | = | - | s-1 | - |
| CHEMBL5945158 | — | k_off | = | - | s-1 | - |
| CHEMBL5945158 | — | kon | = | - | — | - |
| CHEMBL5945158 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5983436 | — | k_off | = | - | s-1 | - |
| CHEMBL5983436 | — | kon | = | - | — | - |
| CHEMBL5781268 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5913390 | — | k_off | = | - | s-1 | - |
| CHEMBL5913390 | — | kon | = | - | — | - |
| CHEMBL5913390 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5870046 | — | k_off | = | - | s-1 | - |
| CHEMBL5870046 | — | kon | = | - | — | - |
| CHEMBL5870046 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5811200 | — | k_off | = | - | s-1 | - |
| CHEMBL5811200 | — | kon | = | - | — | - |
| CHEMBL5811200 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5873067 | — | k_off | = | - | s-1 | - |
| CHEMBL5873067 | — | kon | = | - | — | - |
| CHEMBL5873067 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL5924753 | — | k_off | = | - | s-1 | - |
| CHEMBL5924753 | — | kon | = | - | — | - |
| CHEMBL5835205 | — | kon | = | - | — | - |
| CHEMBL5924753 | — | IC50 | < | 10.0 | nM | - |