Assay Detail
Binding
CHEMBL833529
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In vitro inhibitory concentration against human recombinant Poly (ADP-ribose) polymerase 1
33
Total Activities
33
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
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.33 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL185742 | — | — | 1 | 8.22 |
| CHEMBL365077 | — | — | 1 | 8.08 |
| CHEMBL251027 | — | — | 1 | 8.05 |
| CHEMBL188985 | — | — | 1 | 7.92 |
| CHEMBL364364 | — | — | 1 | 7.92 |
| CHEMBL186380 | — | — | 1 | 7.92 |
| CHEMBL251030 | — | — | 1 | 7.89 |
| CHEMBL189386 | — | — | 1 | 7.85 |
| CHEMBL365235 | — | — | 1 | 7.80 |
| CHEMBL399725 | — | — | 1 | 7.80 |
| CHEMBL187042 | — | — | 1 | 7.77 |
| CHEMBL184513 | — | — | 1 | 7.64 |
| CHEMBL251028 | — | — | 1 | 7.64 |
| CHEMBL359767 | — | — | 1 | 7.60 |
| CHEMBL251029 | — | — | 1 | 7.58 |
| CHEMBL359579 | — | — | 1 | 7.58 |
| CHEMBL186186 | — | — | 1 | 7.57 |
| CHEMBL362762 | — | — | 1 | 7.47 |
| CHEMBL184104 | — | — | 1 | 7.43 |
| CHEMBL186365 | — | — | 1 | 7.41 |
| CHEMBL249813 | — | — | 1 | 7.34 |
| CHEMBL361054 | — | — | 1 | 7.22 |
| CHEMBL186418 | — | — | 1 | 7.19 |
| CHEMBL187062 | — | — | 1 | 7.18 |
| CHEMBL189500 | — | — | 1 | 7.15 |
| CHEMBL364763 | — | — | 1 | 7.13 |
| CHEMBL187689 | — | — | 1 | 6.77 |
| CHEMBL186383 | — | — | 1 | 6.60 |
| CHEMBL186555 | — | — | 1 | 6.00 |
| CHEMBL188949 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL185742 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL365077 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL251027 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL188985 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL364364 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL186380 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL251030 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL189386 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL365235 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL399725 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL187042 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL184513 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL251028 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL359767 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL359579 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL251029 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL186186 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL362762 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL184104 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL186365 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL249813 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL361054 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL186418 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL187062 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL189500 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL364763 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL187689 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL186383 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL186555 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL188949 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL363307 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL81977 | 3-AMINOBENZAMIDE | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL189247 | — | IC50 | > | 1000.0 | nM | - |