Assay Detail
Binding
CHEMBL2174994
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant Tdp1 assessed as conversion of 14-mer 5'-32P-labeled 3'-phosphotyrosyl DNA substrate N14Y to 14-mer 5'-32P-labeled 3'-phosphate DNA product N14P after 15 mins by PAGE analysis
58
Total Activities
58
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
5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl-DNA phosphodiesterase I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 4.78 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170127 | — | — | 1 | 6.06 |
| CHEMBL2170149 | — | — | 1 | 5.66 |
| CHEMBL2170121 | — | — | 1 | 5.58 |
| CHEMBL2170125 | — | — | 1 | 5.39 |
| CHEMBL2170124 | — | — | 1 | 5.24 |
| CHEMBL2170137 | — | — | 1 | 5.17 |
| CHEMBL2170126 | — | — | 1 | 5.15 |
| CHEMBL2170135 | — | — | 1 | 5.11 |
| CHEMBL2170136 | — | — | 1 | 5.07 |
| CHEMBL2170131 | — | — | 1 | 4.96 |
| CHEMBL77030 | TYRPHOSTIN 47 | — | 1 | 4.92 |
| CHEMBL2170123 | — | — | 1 | 4.92 |
| CHEMBL2170154 | — | — | 1 | 4.92 |
| CHEMBL2170162 | — | — | 1 | 4.89 |
| CHEMBL2170133 | — | — | 1 | 4.82 |
| CHEMBL2170134 | — | — | 1 | 4.82 |
| CHEMBL2170122 | — | — | 1 | 4.80 |
| CHEMBL2170150 | — | — | 1 | 4.75 |
| CHEMBL2170139 | — | — | 1 | 4.72 |
| CHEMBL2170147 | — | — | 1 | 4.70 |
| CHEMBL2170129 | — | — | 1 | 4.58 |
| CHEMBL538427 | — | — | 1 | 4.57 |
| CHEMBL2170140 | — | — | 1 | 4.55 |
| CHEMBL2170148 | — | — | 1 | 4.54 |
| CHEMBL550345 | — | — | 1 | 4.52 |
| CHEMBL24057 | FURAMIDINE | -1.0 | 1 | 4.51 |
| CHEMBL2170145 | — | — | 1 | 4.50 |
| CHEMBL2170130 | — | — | 1 | 4.47 |
| CHEMBL2170144 | — | — | 1 | 4.47 |
| CHEMBL2170128 | — | — | 1 | 4.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170127 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL2170149 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2170121 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2170125 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2170124 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL2170137 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL2170126 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2170135 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL2170136 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL2170131 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL77030 | TYRPHOSTIN 47 | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2170123 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2170154 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2170162 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2170134 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2170133 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2170122 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2170150 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL2170139 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2170147 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2170129 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL538427 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2170140 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2170148 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL550345 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL24057 | FURAMIDINE | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL2170145 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL2170130 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2170144 | — | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2170128 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL1504370 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL2170141 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL2170143 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL2170132 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL2170138 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL2170158 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL2170142 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL2170156 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL2170155 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL2170165 | — | IC50 | = | 111000.0 | nM | - |
| CHEMBL2170153 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL2170152 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL2170151 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL2170120 | — | IC50 | > | 111000.0 | nM | - |
| CHEMBL2170146 | — | IC50 | = | 111000.0 | nM | - |
| CHEMBL310798 | TYRPHOSTIN 25 | IC50 | > | 333000.0 | nM | - |
| CHEMBL56543 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL296407 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL73820 | — | IC50 | > | 333000.0 | nM | - |
| CHEMBL496786 | — | IC50 | > | 333000.0 | nM | - |