Assay Detail
Binding
CHEMBL3769133
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Inhibition of human N-terminal truncated ChoKalpha1 (75 to 457 residues) using choline chloride as substrate measured over 10 to 30 mins by coupled ATP regeneration assay
20
Total Activities
20
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
Novel Small Molecule Inhibitors of Choline Kinase Identified by Fragment-Based Drug Discovery.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.00 | 7.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3763540 | — | — | 1 | 7.18 |
| CHEMBL3763931 | — | — | 1 | 7.07 |
| CHEMBL3763982 | — | — | 1 | 6.78 |
| CHEMBL3764278 | — | — | 1 | 6.63 |
| CHEMBL3765239 | — | — | 1 | 6.60 |
| CHEMBL3763453 | — | — | 1 | 6.59 |
| CHEMBL3763792 | — | — | 1 | 6.57 |
| CHEMBL3763801 | — | — | 1 | 6.34 |
| CHEMBL3764898 | — | — | 1 | 5.89 |
| CHEMBL3764767 | — | — | 1 | 5.84 |
| CHEMBL3763340 | — | — | 1 | 5.83 |
| CHEMBL3765567 | — | — | 1 | 5.58 |
| CHEMBL3765650 | — | — | 1 | 5.58 |
| CHEMBL3765077 | — | — | 1 | 5.41 |
| CHEMBL3764904 | — | — | 1 | 5.30 |
| CHEMBL3764395 | — | — | 1 | 4.76 |
| CHEMBL3763993 | — | — | 1 | 4.06 |
| CHEMBL3764475 | — | — | 1 | - |
| CHEMBL3763196 | — | — | 1 | - |
| CHEMBL3765610 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3763540 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3763931 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3763982 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3764278 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3765239 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL3763453 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL3763792 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL3763801 | — | IC50 | = | 457.0 | nM | 6.34 |
| CHEMBL3764898 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3764767 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL3763340 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL3765567 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3765650 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3765077 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3764904 | — | IC50 | = | 4950.0 | nM | 5.30 |
| CHEMBL3764395 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL3763993 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL3764475 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3763196 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL3765610 | — | IC50 | > | 2000000.0 | nM | - |