Assay Detail
Binding
CHEMBL4358945
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Inhibition of human N-terminal His6-tagged TEV protease site linked DHPS expressed in Escherichia coli BL21 (DE3) assessed as reduction in radiolabelled amino-butylidene incorporation in eIF5A using [3H]Spermidine trichloride as substrate after 90 to 120 mins in presence of eIF5A and 14 uM NAD+ by Topcount scintillation counting method
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 5.78 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4555677 | — | — | 1 | 7.21 |
| CHEMBL4543218 | — | — | 1 | 7.04 |
| CHEMBL4462702 | — | — | 1 | 6.92 |
| CHEMBL229457 | — | — | 1 | 6.85 |
| CHEMBL4442298 | — | — | 1 | 6.37 |
| CHEMBL4447948 | — | — | 1 | 6.08 |
| CHEMBL4470208 | — | — | 1 | 5.64 |
| CHEMBL4572958 | — | — | 1 | 5.27 |
| CHEMBL4439037 | — | — | 1 | 4.96 |
| CHEMBL4559429 | — | — | 1 | 4.66 |
| CHEMBL4572059 | — | — | 1 | 4.38 |
| CHEMBL4445752 | — | — | 1 | 4.00 |
| CHEMBL4437949 | — | — | 1 | - |
| CHEMBL4472269 | — | — | 1 | - |
| CHEMBL4520351 | — | — | 1 | - |
| CHEMBL4435260 | — | — | 1 | - |
| CHEMBL4517458 | — | — | 1 | - |
| CHEMBL4457831 | — | — | 1 | - |
| CHEMBL4456055 | — | — | 1 | - |
| CHEMBL4553169 | — | — | 1 | - |
| CHEMBL4437126 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4555677 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4543218 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4462702 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL229457 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4442298 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4447948 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4470208 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4572958 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4439037 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4559429 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4572059 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL4445752 | — | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL4437949 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4472269 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4520351 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4435260 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4517458 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4457831 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4456055 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4553169 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4437126 | — | IC50 | > | 100000.0 | nM | - |