Assay Detail
Binding
CHEMBL5318187
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Inhibition of N-terminal MBP tagged/C-terminal PARP2 (unknown origin) expressed in Escherichia coli in presence of NAD+
32
Total Activities
31
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
[1,2,4]Triazolo[3,4-<i>b</i>]benzothiazole Scaffold as Versatile Nicotinamide Mimic Allowing Nanomolar Inhibition of Different PARP Enzymes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 5.34 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5406267 | — | — | 2 | 7.44 |
| CHEMBL5421878 | — | — | 1 | 6.62 |
| CHEMBL5402584 | — | — | 1 | 5.89 |
| CHEMBL5398835 | — | — | 1 | 5.82 |
| CHEMBL5431108 | — | — | 1 | 5.80 |
| CHEMBL5433172 | — | — | 1 | 5.68 |
| CHEMBL5395721 | — | — | 1 | 5.62 |
| CHEMBL5412860 | — | — | 1 | 5.54 |
| CHEMBL5395131 | — | — | 1 | 5.41 |
| CHEMBL4296925 | — | — | 1 | 5.40 |
| CHEMBL5439304 | — | — | 1 | 5.35 |
| CHEMBL5402663 | — | — | 1 | 5.33 |
| CHEMBL5396332 | — | — | 1 | 5.28 |
| CHEMBL5409536 | — | — | 1 | 5.28 |
| CHEMBL5427721 | — | — | 1 | 5.16 |
| CHEMBL5427075 | — | — | 1 | 5.08 |
| CHEMBL5429120 | — | — | 1 | 5.08 |
| CHEMBL5398837 | — | — | 1 | 5.06 |
| CHEMBL5416085 | — | — | 1 | 5.04 |
| CHEMBL5404785 | — | — | 1 | 5.00 |
| CHEMBL2136900 | — | — | 1 | 4.92 |
| CHEMBL5394162 | — | — | 1 | 4.72 |
| CHEMBL5430541 | — | — | 1 | 4.70 |
| CHEMBL5400133 | — | — | 1 | 4.54 |
| CHEMBL5399492 | — | — | 1 | 4.36 |
| CHEMBL5412151 | — | — | 1 | 4.16 |
| CHEMBL5416726 | — | — | 1 | 4.01 |
| CHEMBL5394260 | — | — | 1 | - |
| CHEMBL5394776 | — | — | 1 | - |
| CHEMBL5403002 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5406267 | — | IC50 | = | 36.31 | nM | 7.44 |
| CHEMBL5406267 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5421878 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5402584 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5398835 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5431108 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5433172 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5395721 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5412860 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5395131 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4296925 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5439304 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL5402663 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5396332 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5409536 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL5427721 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL5427075 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL5429120 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL5398837 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL5416085 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5404785 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2136900 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5394162 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5430541 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5400133 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL5399492 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL5412151 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL5416726 | — | IC50 | = | 97000.0 | nM | 4.01 |
| CHEMBL5394776 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5434061 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5394260 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5403002 | — | IC50 | > | 100000.0 | nM | - |