Assay Detail
Binding
CHEMBL4628249
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Displacement of tracer from PKN1 (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 | 4.53 | 5.96 |
| Ki | 15 | 4.75 | 6.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1990482 | — | — | 2 | 6.27 |
| CHEMBL4647033 | — | — | 2 | 5.66 |
| CHEMBL4635777 | — | — | 2 | 5.28 |
| CHEMBL4632420 | — | — | 2 | 4.72 |
| CHEMBL4634210 | — | — | 2 | 4.72 |
| CHEMBL379376 | — | — | 2 | 4.65 |
| CHEMBL4636367 | — | — | 2 | 4.59 |
| CHEMBL4649365 | — | — | 2 | 4.56 |
| CHEMBL4638916 | — | — | 2 | 4.55 |
| CHEMBL4646744 | — | — | 2 | 4.54 |
| CHEMBL4645636 | — | — | 2 | 4.52 |
| CHEMBL185288 | — | — | 2 | 4.49 |
| CHEMBL4637286 | — | — | 2 | 4.31 |
| CHEMBL160012 | — | — | 2 | 4.27 |
| CHEMBL4640475 | — | — | 2 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1990482 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL1990482 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4647033 | — | Ki | = | 2190.0 | nM | 5.66 |
| CHEMBL4647033 | — | IC50 | = | 4450.0 | nM | 5.35 |
| CHEMBL4635777 | — | Ki | = | 5200.0 | nM | 5.28 |
| CHEMBL4635777 | — | IC50 | = | 10590.0 | nM | 4.97 |
| CHEMBL4634210 | — | Ki | = | 18920.0 | nM | 4.72 |
| CHEMBL4632420 | — | Ki | = | 19050.0 | nM | 4.72 |
| CHEMBL379376 | — | Ki | = | 22360.0 | nM | 4.65 |
| CHEMBL4636367 | — | Ki | = | 25940.0 | nM | 4.59 |
| CHEMBL4649365 | — | Ki | = | 27810.0 | nM | 4.56 |
| CHEMBL4638916 | — | Ki | = | 27830.0 | nM | 4.55 |
| CHEMBL4646744 | — | Ki | = | 28930.0 | nM | 4.54 |
| CHEMBL4645636 | — | Ki | = | 30230.0 | nM | 4.52 |
| CHEMBL185288 | — | Ki | = | 32540.0 | nM | 4.49 |
| CHEMBL4632420 | — | IC50 | = | 38810.0 | nM | 4.41 |
| CHEMBL4634210 | — | IC50 | = | 38540.0 | nM | 4.41 |
| CHEMBL379376 | — | IC50 | = | 45540.0 | nM | 4.34 |
| CHEMBL4637286 | — | Ki | = | 48800.0 | nM | 4.31 |
| CHEMBL4636367 | — | IC50 | = | 52840.0 | nM | 4.28 |
| CHEMBL160012 | — | Ki | = | 53660.0 | nM | 4.27 |
| CHEMBL4638916 | — | IC50 | = | 56690.0 | nM | 4.25 |
| CHEMBL4649365 | — | IC50 | = | 56660.0 | nM | 4.25 |
| CHEMBL4646744 | — | IC50 | = | 58940.0 | nM | 4.23 |
| CHEMBL4645636 | — | IC50 | = | 61590.0 | nM | 4.21 |
| CHEMBL185288 | — | IC50 | = | 66290.0 | nM | 4.18 |
| CHEMBL4640475 | — | Ki | = | 67710.0 | nM | 4.17 |
| CHEMBL4637286 | — | IC50 | = | 99410.0 | nM | 4.00 |
| CHEMBL160012 | — | IC50 | = | 109300.0 | nM | - |
| CHEMBL4640475 | — | IC50 | = | 137920.0 | nM | - |