Assay Detail
Binding
CHEMBL826331
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Inhibition of human Poly (ADP-ribose) polymerase 1 enzyme
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 7.27 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL361447 | — | — | 1 | 8.42 |
| CHEMBL131719 | — | — | 1 | 8.22 |
| CHEMBL363893 | — | — | 1 | 8.22 |
| CHEMBL361489 | — | — | 1 | 8.19 |
| CHEMBL188989 | — | — | 1 | 8.17 |
| CHEMBL362111 | — | — | 1 | 8.16 |
| CHEMBL186461 | — | — | 1 | 8.12 |
| CHEMBL426618 | — | — | 1 | 8.09 |
| CHEMBL362322 | — | — | 1 | 8.04 |
| CHEMBL188728 | — | — | 1 | 8.04 |
| CHEMBL189698 | — | — | 1 | 8.03 |
| CHEMBL361675 | — | — | 1 | 7.96 |
| CHEMBL365630 | — | — | 1 | 7.96 |
| CHEMBL426070 | — | — | 1 | 7.90 |
| CHEMBL189670 | — | — | 1 | 7.84 |
| CHEMBL187389 | — | — | 1 | 7.66 |
| CHEMBL185702 | — | — | 1 | 7.57 |
| CHEMBL188477 | — | — | 1 | 7.42 |
| CHEMBL189466 | — | — | 1 | 7.41 |
| CHEMBL188824 | — | — | 1 | 7.39 |
| CHEMBL188743 | — | — | 1 | 7.37 |
| CHEMBL123904 | — | — | 1 | 7.28 |
| CHEMBL189304 | — | — | 1 | 7.27 |
| CHEMBL361301 | — | — | 1 | 7.24 |
| CHEMBL424802 | — | — | 1 | 7.17 |
| CHEMBL125200 | — | — | 1 | 7.16 |
| CHEMBL187344 | — | — | 1 | 7.10 |
| CHEMBL188690 | — | — | 1 | 7.10 |
| CHEMBL186776 | — | — | 1 | 7.06 |
| CHEMBL366295 | — | — | 1 | 6.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL361447 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL131719 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL363893 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL361489 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL188989 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL362111 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL186461 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL426618 | — | Ki | = | 8.2 | nM | 8.09 |
| CHEMBL362322 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL188728 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL189698 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL361675 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL365630 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL426070 | — | Ki | = | 12.5 | nM | 7.90 |
| CHEMBL189670 | — | Ki | = | 14.3 | nM | 7.84 |
| CHEMBL187389 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL185702 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL188477 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL189466 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL188824 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL188743 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL123904 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL189304 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL361301 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL424802 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL125200 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL187344 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL188690 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL186776 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL366295 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL363978 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL188217 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL187720 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL187156 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL362301 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL360820 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL189173 | — | Ki | = | 304.0 | nM | 6.52 |
| CHEMBL362516 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL187566 | — | Ki | = | 337.0 | nM | 6.47 |
| CHEMBL188308 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL187667 | — | Ki | = | 606.0 | nM | 6.22 |
| CHEMBL362568 | — | Ki | = | 692.0 | nM | 6.16 |
| CHEMBL362875 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL189174 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL81977 | 3-AMINOBENZAMIDE | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL364362 | — | Ki | - | nM | - | |
| CHEMBL185634 | — | Ki | - | nM | - | |
| CHEMBL426977 | — | Ki | - | nM | - |