Assay Detail
Binding
CHEMBL5332565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged BLM (unknown origin) expressed in Escherichia coli BL21 (DE3) using 5'-biotin-labeled duplex forked-DNA as substrate incubated for 10 mins followed by substrate addition measured after 30 mins in presence of ATP by electrophoretic mobility shift assay
26
Total Activities
26
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 N3-substituted quinazolinone derivatives as potential Bloom's Syndrome protein (BLM) helicase inhibitor for sensitization treatment of colorectal cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.33 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423610 | — | — | 1 | 6.10 |
| CHEMBL5440285 | — | — | 1 | 5.89 |
| CHEMBL5424781 | — | — | 1 | 5.64 |
| CHEMBL5433468 | — | — | 1 | 5.60 |
| CHEMBL5437731 | — | — | 1 | 5.54 |
| CHEMBL5433068 | — | — | 1 | 5.43 |
| CHEMBL5425282 | — | — | 1 | 5.40 |
| CHEMBL5405727 | — | — | 1 | 5.37 |
| CHEMBL5417970 | — | — | 1 | 5.32 |
| CHEMBL5411202 | — | — | 1 | 5.30 |
| CHEMBL4633662 | — | — | 1 | 5.29 |
| CHEMBL5436428 | — | — | 1 | 5.28 |
| CHEMBL5408314 | — | — | 1 | 5.28 |
| CHEMBL5408479 | — | — | 1 | 5.28 |
| CHEMBL5439207 | — | — | 1 | 5.24 |
| CHEMBL5394652 | — | — | 1 | 5.10 |
| CHEMBL5410036 | — | — | 1 | 5.08 |
| CHEMBL5439537 | — | — | 1 | 5.04 |
| CHEMBL5397042 | — | — | 1 | 5.01 |
| CHEMBL5430184 | — | — | 1 | 4.50 |
| CHEMBL5419427 | — | — | 1 | - |
| CHEMBL5408083 | — | — | 1 | - |
| CHEMBL5406659 | — | — | 1 | - |
| CHEMBL5409326 | — | — | 1 | - |
| CHEMBL5436259 | — | — | 1 | - |
| CHEMBL5398979 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423610 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5440285 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5424781 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5433468 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5437731 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5433068 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5425282 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5405727 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5417970 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5411202 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4633662 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5436428 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5408314 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL5408479 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL5439207 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL5394652 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5410036 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5439537 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL5397042 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL5430184 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL5419427 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL5408083 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL5406659 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL5409326 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL5436259 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL5398979 | — | IC50 | > | 32000.0 | nM | - |