Assay Detail
Binding
CHEMBL4386568
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Inhibition of humanized zebrafish TDP2 using 5'-(6-FAM-NHS) as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by fluorescence assay
34
Total Activities
34
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
Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.79 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441013 | — | — | 1 | 8.21 |
| CHEMBL4572376 | — | — | 1 | 8.19 |
| CHEMBL4436202 | — | — | 1 | 8.14 |
| CHEMBL4587441 | — | — | 1 | 7.85 |
| CHEMBL4520052 | — | — | 1 | 7.70 |
| CHEMBL4468174 | — | — | 1 | 7.48 |
| CHEMBL4560735 | — | — | 1 | 7.48 |
| CHEMBL4555612 | — | — | 1 | 7.46 |
| CHEMBL4521151 | — | — | 1 | 7.42 |
| CHEMBL2420480 | — | — | 1 | 7.39 |
| CHEMBL2420507 | — | — | 1 | 7.38 |
| CHEMBL4457155 | — | — | 1 | 7.19 |
| CHEMBL4546104 | — | — | 1 | 7.16 |
| CHEMBL4518508 | — | — | 1 | 6.89 |
| CHEMBL2420465 | — | — | 1 | 6.85 |
| CHEMBL4576353 | — | — | 1 | 6.82 |
| CHEMBL4557001 | — | — | 1 | 6.72 |
| CHEMBL4464179 | — | — | 1 | 6.70 |
| CHEMBL4471861 | — | — | 1 | 6.57 |
| CHEMBL4536546 | — | — | 1 | 6.52 |
| CHEMBL4444838 | — | — | 1 | 6.50 |
| CHEMBL4590491 | — | — | 1 | 6.42 |
| CHEMBL2420506 | — | — | 1 | 6.19 |
| CHEMBL4470162 | — | — | 1 | 6.06 |
| CHEMBL4585923 | — | — | 1 | 6.03 |
| CHEMBL4470609 | — | — | 1 | 6.02 |
| CHEMBL4473892 | — | — | 1 | 6.00 |
| CHEMBL4449643 | — | — | 1 | 6.00 |
| CHEMBL4585941 | — | — | 1 | 5.96 |
| CHEMBL4473717 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441013 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4572376 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4436202 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4587441 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4520052 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4468174 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4560735 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4555612 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4521151 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2420480 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2420507 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4457155 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4546104 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4518508 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2420465 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4576353 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4557001 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4464179 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4471861 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4536546 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4444838 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4590491 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2420506 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4470162 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4585923 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4470609 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4473892 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4449643 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4585941 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4473717 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4581905 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4525013 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4469686 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4434664 | — | IC50 | > | 10000.0 | nM | - |