Assay Detail
Binding
CHEMBL2319019
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Tdp1 (unknown origin) using 5'-[32P]-labeled single-stranded DNA oligonucleotide containing 3'-phosphotyrosine as substrate after 15 mins by PAGE analysis
50
Total Activities
50
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
Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 4.80 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL387152 | — | — | 1 | 6.00 |
| CHEMBL2312896 | — | — | 1 | 5.30 |
| CHEMBL2312906 | — | — | 1 | 5.28 |
| CHEMBL218884 | — | — | 1 | 5.24 |
| CHEMBL3217227 | — | — | 1 | 5.17 |
| CHEMBL2312893 | — | — | 1 | 4.96 |
| CHEMBL375623 | — | — | 1 | 4.96 |
| CHEMBL213072 | — | — | 1 | 4.92 |
| CHEMBL2312904 | — | — | 1 | 4.92 |
| CHEMBL2172212 | — | — | 1 | 4.92 |
| CHEMBL2312899 | — | — | 1 | 4.82 |
| CHEMBL2172214 | — | — | 1 | 4.75 |
| CHEMBL2312571 | — | — | 1 | 4.75 |
| CHEMBL2312882 | — | — | 1 | 4.43 |
| CHEMBL2172208 | — | — | 1 | 4.43 |
| CHEMBL2312886 | — | — | 1 | 4.43 |
| CHEMBL2312883 | — | — | 1 | 4.43 |
| CHEMBL2312884 | — | — | 1 | 4.43 |
| CHEMBL242413 | — | — | 1 | 4.43 |
| CHEMBL2312572 | — | — | 1 | 4.43 |
| CHEMBL2312570 | — | — | 1 | 4.35 |
| CHEMBL2312914 | — | — | 1 | 4.21 |
| CHEMBL2312890 | — | — | 1 | - |
| CHEMBL2312889 | — | — | 1 | - |
| CHEMBL2312888 | — | — | 1 | - |
| CHEMBL2312887 | — | — | 1 | - |
| CHEMBL2312885 | — | — | 1 | - |
| CHEMBL2312569 | — | — | 1 | - |
| CHEMBL2312917 | — | — | 1 | - |
| CHEMBL2312916 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL387152 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2312896 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2312906 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL218884 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3217227 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL2312893 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL375623 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2172212 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL213072 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2312904 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2312899 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2172214 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2312571 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2312886 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2172208 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2312883 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2312882 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2312884 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL242413 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2312572 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL2312570 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL2312914 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL2312891 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312892 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312894 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312895 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312897 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312898 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312901 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2172296 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2172218 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2172215 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2172300 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312902 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312903 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312905 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312909 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312910 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312911 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312912 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312913 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312915 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312916 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312917 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312569 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312885 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312887 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312888 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312889 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2312890 | — | IC50 | > | 111000.0 | nM | - |