Assay Detail
Binding
CHEMBL4628248
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Displacement of tracer from PKN2 (unknown origin) by TR-FRET assay
30
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.17 | 7.19 |
| Ki | 15 | 5.48 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1990482 | — | — | 2 | 7.52 |
| CHEMBL4647033 | — | — | 2 | 7.10 |
| CHEMBL4635777 | — | — | 2 | 5.97 |
| CHEMBL4646744 | — | — | 2 | 5.90 |
| CHEMBL4634210 | — | — | 2 | 5.60 |
| CHEMBL4636367 | — | — | 2 | 5.57 |
| CHEMBL379376 | — | — | 2 | 5.42 |
| CHEMBL4645636 | — | — | 2 | 5.16 |
| CHEMBL185288 | — | — | 2 | 5.09 |
| CHEMBL4637286 | — | — | 2 | 5.09 |
| CHEMBL160012 | — | — | 2 | 4.89 |
| CHEMBL4632420 | — | — | 2 | 4.81 |
| CHEMBL4649365 | — | — | 2 | 4.71 |
| CHEMBL4638916 | — | — | 2 | 4.68 |
| CHEMBL4640475 | — | — | 2 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1990482 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1990482 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4647033 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL4647033 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4635777 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL4646744 | — | Ki | = | 1250.0 | nM | 5.90 |
| CHEMBL4635777 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4634210 | — | Ki | = | 2510.0 | nM | 5.60 |
| CHEMBL4646744 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4636367 | — | Ki | = | 2690.0 | nM | 5.57 |
| CHEMBL379376 | — | Ki | = | 3850.0 | nM | 5.42 |
| CHEMBL4634210 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4636367 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4645636 | — | Ki | = | 6900.0 | nM | 5.16 |
| CHEMBL379376 | — | IC50 | = | 7710.0 | nM | 5.11 |
| CHEMBL185288 | — | Ki | = | 8190.0 | nM | 5.09 |
| CHEMBL4637286 | — | Ki | = | 8110.0 | nM | 5.09 |
| CHEMBL160012 | — | Ki | = | 12920.0 | nM | 4.89 |
| CHEMBL4645636 | — | IC50 | = | 13790.0 | nM | 4.86 |
| CHEMBL4632420 | — | Ki | = | 15640.0 | nM | 4.81 |
| CHEMBL185288 | — | IC50 | = | 16380.0 | nM | 4.79 |
| CHEMBL4637286 | — | IC50 | = | 16230.0 | nM | 4.79 |
| CHEMBL4649365 | — | Ki | = | 19420.0 | nM | 4.71 |
| CHEMBL4638916 | — | Ki | = | 21050.0 | nM | 4.68 |
| CHEMBL4640475 | — | Ki | = | 23830.0 | nM | 4.62 |
| CHEMBL160012 | — | IC50 | = | 25850.0 | nM | 4.59 |
| CHEMBL4632420 | — | IC50 | = | 31290.0 | nM | 4.50 |
| CHEMBL4649365 | — | IC50 | = | 38840.0 | nM | 4.41 |
| CHEMBL4638916 | — | IC50 | = | 42090.0 | nM | 4.38 |
| CHEMBL4640475 | — | IC50 | = | 47660.0 | nM | 4.32 |