Assay Detail
Binding
CHEMBL4329005
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Inhibition of recombinant human full-length N-terminal His-tagged Tdp1 expressed in Escherichia coli BL21 (DE3) using 5'-(5,6 FAM-aac gtc agg gtc ttc c-BHQ1)-3' as substrate measured every 1 min for 7 mins by fluorimetric method
19
Total Activities
19
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 tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.34 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438274 | — | — | 1 | 7.58 |
| CHEMBL4440514 | — | — | 1 | 7.46 |
| CHEMBL4440114 | — | — | 1 | 7.17 |
| CHEMBL4587610 | — | — | 1 | 7.07 |
| CHEMBL4475772 | — | — | 1 | 6.82 |
| CHEMBL4446104 | — | — | 1 | 6.80 |
| CHEMBL4551119 | — | — | 1 | 6.76 |
| CHEMBL4436400 | — | — | 1 | 6.72 |
| CHEMBL4533174 | — | — | 1 | 6.34 |
| CHEMBL4455616 | — | — | 1 | 6.21 |
| CHEMBL4452868 | — | — | 1 | 5.95 |
| CHEMBL4446028 | — | — | 1 | 5.92 |
| CHEMBL24057 | FURAMIDINE | -1.0 | 1 | 5.91 |
| CHEMBL4564100 | — | — | 1 | 5.90 |
| CHEMBL4451622 | — | — | 1 | 5.46 |
| CHEMBL4590510 | — | — | 1 | 5.42 |
| CHEMBL4566004 | — | — | 1 | 5.39 |
| CHEMBL4464001 | — | — | 1 | 5.23 |
| CHEMBL367881 | (+)-USNIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438274 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4440514 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4440114 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4587610 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4475772 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4446104 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL4551119 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4436400 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4533174 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL4455616 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4452868 | — | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL4446028 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL24057 | FURAMIDINE | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL4564100 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4451622 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4590510 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4566004 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4464001 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL367881 | (+)-USNIC ACID | IC50 | > | 50000.0 | nM | - |