Assay Detail
Binding
CHEMBL4625933
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Binding affinity to His-tagged BLM (642 to 1296 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells assessed as inhibition of protein interaction with 5'-biotin-labeled forked DNA measured after 1 hr by ELISA
4
Total Activities
4
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
Design, Synthesis, and Evaluation of New Quinazolinone Derivatives that Inhibit Bloom Syndrome Protein (BLM) Helicase, Trigger DNA Damage at the Telomere Region, and Synergize with PARP Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.06 | 5.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4633662 | — | — | 1 | 5.06 |
| CHEMBL4642601 | — | — | 1 | - |
| CHEMBL4632583 | — | — | 1 | - |
| CHEMBL4647503 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4633662 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4642601 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4632583 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4647503 | — | IC50 | > | 20000.0 | nM | - |